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|Cheap best essay ghostwriting websites gb||Samples were taken at each month interval for evaluation of drug content, surface pH and in vitro drug release study. The in vitro release data was subjected to zero order, first order, Higuchi, Korsemeyer-Peppas, Hixon crowell and erosion model in Dept. It is used for controlled drug delivery applications, rapid release dosage forms, improved peptide delivery, colonic drug delivery systems, and use for gene delivery. Jump to Page. The swelling index for the formulations containing xanthan gum and gum acacia was less among the secondary polymers used due to formation of highly viscous mucilaginous layer over the surface of the tablet.|
|Pay to get world literature dissertation||The buccal mucosa is highly perfused with blood vessels and offers greater permeability than the skin. MCGs are found near the upper, distal or superficial border of the cells and a few occur near the opposite border. Type III: It is a unidirectional drug release device, from which drug loss is minimal, since. The main mechanism involved in drug transfer across the oral mucosa, is passive diffusion Dept. The surface pH of the tablet was from 6.|
Shodhganga Mirror Site. Show full item record. Design and evaluation of mucoadhesive buccal delivery systems of felodipine. Charde, Shrikant Y. The objective of the present work was to design and evaluate mucoadhesive newlinebuccal drug delivery systems of felodipine FDP. FDP, a 1,4-dihydropyridine newlinederivative, is a vasoselective calcium antagonist widely used in treatment of angina newlinepectoris and hypertension.
The drug exists as crystalline powder and is very slightly newlinesoluble in water. Effect of chitosan concentration on in-vitro release of 92 sumatriptan succinate from mucoadhesive buccal tablets Effect of chitosan concentration on ex vivo residence time of 94 mucoadhesive buccal tablet of sumatriptan succinate Effect of chitosan concentration on mucoadhesive strength of 95 mucoadhesive buccal tablets of sumatriptan succinate Amongst various routes of drug delivery oral route is perhaps the most preferred to the patient a nd the clinician alike.
However this route presents some problems for a few drugs. The blood that drains the GIT carries the drug directly to the liver leading to first-pass metabolism resulting in poor bioavailability. The inherent problems associated with the drug in some cases can be solved by modifying the formulation or by changing the routes of administration. Parenteral, mucosal and transdermal routes circumvent hepatic first-pass metabolism and offer alternative routes for the systemic delivery of drugs1.
In recent years, the interest in novel routes of drug administration occurs from their ability to enhance the bioavailability of drugs. Drug delivery via the buccal route using bioadhesive dosage forms offers such a novel route of drug administration. Extensive first-pass metabolism and drug degradation in the harsh gastrointestinal environment can be circumvented by administering the drug via buccal route2.
Buccal delivery involves administration of desired drug through the Dept. The mucosal lining of oral cavity offers some distinct advantages. It is richly vascularized and more accessible for the administration and removal of a dosage form. Additionally, buccal drug delivery has high patient acceptability compared to other non-oral routes of drug administration3.
Drug absorption through buccal mucosa is mainly by passive diffusion into the lipoidal membrane. After absorption the drug is transported through facial vein which then drains into the general circulation via jugular vein bypassing the liver and thereby sparing the drug from first-pass metabolism4.
Buccal route provides one of the potential routes for typically large, hydrophilic and unstable proteins, oligonucleotides and polysaccharides as well as conventional small drug molecules. The oral cavity can be used for local and systemic therapy.
Examples of local therapy would be the treatment of oral infections, dental caries, mouth ulcers and stomatitis. The buccal route is of particular interest with regard to the systemic delivery of small molecules that are subjected to first pass metabolism or for the administration of proteins and peptides5. Various advantages and other aspects of this route are elucidated of the following.
Ease of administration. Permits localization of the drug in the oral cavity for a prolonged period of time. Offers excellent route for systemic delivery of drugs with high first pass metabolism, thereby offering a greater bioavailability. A significant reduction in dose can be achieved, thereby reducing dose dependent side effects. Drugs which are unstable in acidic environment of the stomach or are destro yed by the enzymatic or alkaline environment of the intestine.
The presence of saliva ensures relatively large amount of water for drug dissolution unlike the case of rectal and transdermal routes. It offers passive system for drug absorption and do es not require any activation. It can be made unidirectional to ensure only buccal absorption. The buccal mucosa is highly perfused with blood vessels and offers greater permeability than the skin.
Therapeutic serum concentrations of the drug can be achieved more rapidly. Better patient compliance than vaginal, rectal and nasal route of administration. Buccal mucosa is less prone to damage or irritation than nasal mucosa and shows short recovery times after stress or damage. Termination of therapy is easy. Can be administered to unconscious patients.
Drugs which irritate the oral mucosa have a bitter or unpleasant taste or odour cannot be administered by this route. Drugs, which are unstable at buccal pH, cannot be administered by this route. Only drugs with small dose requirements can be administered. Drugs may get swallowed with saliva and loses the advantages of buccal route.
Only those drugs, which are absorbed by passive diffusion, can be administered by this route. Over hydration may lead to the formation of slippery surface and structural integrity of the formulation may get disrupted by the swelling and hydration of the bioadhesive polymers. Surface area available for absorption is less. The buccal mucosa is relatively less permeable than the small intestine, rectum, etc.
The oral cavity consists of two regio ns, Dept. Outer oral vestibule, which is bounded by cheeks, lips, teeth and gingiva gums. Oral cavity proper, which extends from teeth and gums back to the faces which lead to pharynx with the roof comprising the hard and soft palate. The tongue projects from the floor of the cavity. Figure 1: Structure of buccal cavity The drug administered via the oral mucosa gain access to the systemic circulation through a network of arteries and capillaries.
The major artery supplying the blood to the oral cavity is the external carotid artery. The venous backflow goes through branches of capillaries and veins and finally taken up by the jugular vein8. The secretion in the oral cavity includes saliva, crevicular fluid and mucus.
From that, Saliva is a complex fluid containing organic and inorganic materials. It is produced by the three pairs of major glands parotid, Dept. The total average volume of saliva produced daily in an adult is around ml. The flow rates of saliva depend upon the type of stimulus used, the time of day, the length of time, glands had been stimulated, the age and sex of the individual and by their state of health.
The average resting flow rate for whole saliva is 0. For stimulated saliva the average flow rate is 1. Chemically, saliva is The solutes include ions sodium, potassium, magnesium, phosphate, bicarbonate and chloride , dissolved gases, urea, uric acid, serum albumin, globulin, mucin and enzymes [lysozyme and amylase ptyalin ]. Second was the crevicular fluid it is a fluid secreted from the gingival glands of oral cavity.
The third type was the mucus, it is a thick secretion composed mainly of water, electrolytes and a mixture of several glycoprotein, which themselves are composed of large polysaccharides bound with smaller quantities of protein. It is secreted over many biological membranes of body for example, throughout the gastrointestinal tract walls. Mucus is secreted by special type of epithelia called mucosa.
The mucus secreted in buccal cavity admixtures with saliva of salivary glands in oral cavity to produce whole saliva. The two main glycoproteins found in buccal mucus or mucin is MG1 and MG2. The mucin glycoprotein, MG1 consists of several disulphide-linked subunits containing a protein core with oligosaccharide side-chain units. Its molecular size is over KDa.
The glycoprotein of mucus has amphoteric properties and is therefore capable of buffering small amounts of either acids or alkalies. The mucus however acts as a potential barrier to the drug penetration. There are some physiological aspects and functions of oral cavity which are explained as, the oral cavity is accountable for the following primary functions such as it is a portal for intake of food material and water, to bring chewing, mastication and mixing of food stuff, then for lubrication of food material and formation of bolus, for the identification of ingested material by taste buds of tongue, to carry out initiation of carbohydrate and fat metabolism and absorption of catabolic products thereafter metabolism and lastly it has slight antisepsis of ingested material and within oral cavity by saliva 9, Masticatory mucosa: Which includes the mucosa around the teeth and on the hard palate and these regions have keratinized epithelium.
Lining mucosa: Which covers the lips, cheeks, fornix, base of the oral cavity, lower part of tongue, buccal mucosa and the soft palate and these regions have non-keratinized epithelium. Specialized mucosa: covering the dorsum of the tongue with highly keratinization. Three distinctive layers of the oral mucosa are the epithelium, basement membrane and connective tissues.
The oral cavity is lined with the epithelium, below which lies the supporting basement membrane. The basement membrane is in turn supported by connective tissues Fig. The epithelial cells originating from the basal cells mature change their shape and increase in size while moving towards the surface. The basement membrane forms a distinctive layer between the connective tissues and the epithelium.
It provides the required adherence between the epithelium and the underlying connective tissues and functions as a mechanical support for the epithelium. The underlying connective tissues provide many of the mechanical properties of oral mucosa Figure 2: Structure of buccal mucosa. Both keratinized and non- keratinized tissues of varying thickness and composition are found in oral cavity.
The difference between keratinized and non-keratinized epithelia is merely the difference in the molecular size of existing keratins. Cells of non-keratinized epithelia contain lower molecular weight protein while those in keratinized epithelia contain mainly higher-molecular weight keratins.
The lipid content of the cells varies between tissues 1. Table 1: Composition and state of keratinization of oral mucosa State of Tissue Composition Keratinization Buccal mucosa Non-keratinized Few neutral, but mainly polar lipids, particularly cholesterol Sublingual mucosa Non-keratinized sulphate and glucosylceramides Gingiva mucosa Keratinized Neutral lipids i. Small water-soluble molecules may pass through, small water filled pores.
The main mechanism involved in drug transfer across the oral mucosa, is passive diffusion Dept. Pas sive diffusion involves the movement of a solute from a region of high concentration in the mouth to a region of low concentration within the buccal tissues. Further diffusion then takes place into the venous capillary system, with the drug eventually reaching the systemic circulation via the jugular vein.
The physicochemical characteristics of a drug are very important for this diffusion process MCGs are spherical or oval organelles that are — nm in diameter and found in both keratinized and non-keratinized epithelia. MCGs are found near the upper, distal or superficial border of the cells and a few occur near the opposite border.
Several hypotheses have been suggested to describe the functions of MCGs including a membrane thickening effect, cell adhesion, production of a cell surface coat, cell desquamation and permeability barrier They discharge their contents into the intercellular space to ensure epithelial cohesion in the superficial layers and this discharge forms a barrier to the permeability of various compounds Another barrier to drug permeability across buccal epithelium is enzymatic degradation.
Saliva contains no proteases but does contain moderate levels of esterase, carbohydrates and phosphatases However, several proteolytic enzymes have been found in the buccal epithelium Walker et al. Figure 3: Drug absorption pathways across buccal mucosa 2. The various types of buccal drug delivery system are explained as follows; 2.
Two methods used to prepare adhesive patches include solvent casting and direct milling. In the solvent casting Dept. In the direct milling method formulation constituents are homogenously mixed and compressed to the desired thickness and patches of predetermined size and shape are then cut or punched out. An impermeable backing layer may also be applied to control the direction of drug release, prevent drug loss and minimize deformation and disintegration of the device during the application period.
Poor retention of the gels at the site of application has been overcome by using bioadhesive formulations. Certain bioadhesive polymers undergo a phase change from a liquid to a semisolid; this change enhances the viscosity which results in sustained and controlled release of drugs. Hydrogels are also promising dosage forms which are formed from polymers that are hydrated in an aqueous environment and physically entrap drug molecules for subsequent slow release by diffusion or erosion.
These dosage forms provide an extended retention time, adequate drug penetration as well as high efficacy and patient acceptability Unlike conventional tablets buccal mucoadhesive tablets allow for drinking and speaking without major discomfort. These tablets can be applied Dept. These tablets are usually prepared by direct compression but wet granulation techniques can also be used. Multilayered tablet may be prepared by sequentially adding and compressing the ingredients layer by layer.
Some newer approaches use tablets that melt at body temperature Type I: It is a single layer device with multidirectional drug release. This type of dosage form suffers from significant drug loss due to swallowing. Type II: It is a device in which an impermeable backing layer is superimposed on top of the drug loaded bioadhesive layer creating a double- layered device and preventing drug loss from the top surface into the oral cavity.
Type III: It is a unidirectional drug release device, from which drug loss is minimal, since the drug is released only from the side adjacent to the buccal mucosa. This can be achieved by coating every face of the dosage form, except the one that is in contact with the buccal mucosa Buccal tablets are small, flat, oval tablets and are intended to be held between the cheek and the teeth or in the cheek pouch buccal tablets.
Progesterone tablets can be administered this way. Troches and lozenges are two other types of tablets used in oral cavity where they are intended to exert a local effect in the mouth or throat. These tablet forms are commonly used to treat sore throat or to control coughing in common cold.
Lozenges pastilles or cough drops are usually made with the drug incorporated in a flavoured, hard-candy sugar base. Lozenges may be made by compression but are usually formed by fusion or by a candy — moulding process. Troches, on the other hand, are manufactured by compression as are other tablets. These two classes of tablets are designed not to disintegrate in the mouth but to dissolve or slowly erode over a period of perhaps minute or less.
Buccal tablets can be most easily held between the gum and cheek. Various drugs have been investigated for their delivery through the buccal mucosa in a mucoadhesive buccal tablet form Table 2. Table 2: List of drugs investigated for mucoadhesive buccal tablet Sr. Drug name Sr. Drug name 1. Carbamazepine26 Metronidazole35 2. Chlorhexidine27 Miconazole nitrate36 3. Diclofenac Sodium28 Morphine sulfate37 4. Diltiazem hydrochloride29 Nicotine38 5.
Ergotamine tartrate30 Omeprazole39 6. Hydrocortisone acetate31 Pindolol40 7. Insulin32 Propranolol41 8. Lactoferrin33 Terbutalline sulphate42 9. Lignocaine hydrochloride34 Piroxicam43 3. The general definition of adherence of a polymeric material to biological surfaces bioadhesive or to the mucosal tissue mucoadhesive still holds A bioadhesive Dept.
When the two materials come in contact with each other electron transfer will occur causing the formation of a double layer of electrical charge at the interface. The bioadhesive force is due to attractive forces across this electrical double layer. The system is charged when the adhesive and the substrate are in contact and discharged when they are separated. However, this theory has caused some controversy regarding whether the electrostatic forces are an important cause or the result of the contact between the bioadhesive and the biological tissue.
Figure 5: Electronic theory Dept. Two types of chemical bonds resulting from these forces can be distinguished: I Primary chemical bonds of covalent nature, which are undesirable in bioadhesion because their high strength may result in permanent bonds. II Secondary chemical bonds having many different forces of attract ion, including electrostatic forces, Vander walls forces and hydrogen and hydrophobic bonds.
Using wetting theory, it is possible to calculate spreading coefficients for various bioadhesive over biological tissues and predict the intensity of the bioad hesive bond. Hence, it provides essential information for development of bio-adhesive drug delivery system.
The exact depth to which the polymer chains penetrate the mucus depends on the diffusion coefficient and the time of contact. This diffusion co efficient, in turn, depends on the value of molecular weight between crosslink's and decreases significantly as the cross linking density increases. This theory suggests that interpenetration and entanglements of bio-adhesive polymer chain and mucus polymer chains produce semi permanent adhesive bonds, and bond strength is believed to increase with the depth of penetration of the polymer chains.
Figure 6: Diffusion theory 3. A variety of factors affect the mucoadhesive properties of polymers. There are some polymer related factors namely molecular weight which indicates that there is certain molecular weight at which bioadhesion is maximum. The interpenetration of polymer molecules is favourable for low molecular weight polymers, whereas entanglement is favoured for high molecular weight polymers.
After molecular weight second is the concentration of polymer, Bremecker maintains that there is an optimum concentration of polymer corresponding to best bioadhesion. In highly concentrated systems the adhesive strength drops significantly. In fact in concentrated solutions the coiled molecule becomes solvent poor and chains available for interpenetration are not numerous. The third factor was the flexibility of polymer chains which is important for interpenetration and enlargement.
As water-soluble polymer becomes cross- linked, the mobility of individual polymer chain decreases. As cross- linking density increases, the effective length of chain which can penetrate into mucus layer decreases even further and mucoadhesive strength is reduced. Fourth factor was the hydrogen bonding capacity is an important factor in mucoadhesion of a polymer For mucoadhesion to occur desired polymers must have functional groups that are Dept.
It was also confirmed that flexibility of the polymer is important to improve its hydrogen bonding potential. Polymers such as poly vinyl alcohol , hydroxylated methacrylate, and poly methacrylicacid , as well as all their copolymers, are polymers with good hydrogen bonding capacity Then cross linking density was another factor in this the average pore size, the number average molecular weight of the cross- linked polymers, and the density of cross- linking are three important and interrelated structural parameters of a polymer network.
Therefore, it seems reasonable that with increasing density of cross- linking, diffusion of water into the polymer network occurs at a lower rate which, in turn, causes an insufficient swelling of the polymer and a decreased rate of interpenetration between polymer and mucin. Finally charge on the polymers also has some impact such as the non- ionic polymers appear to undergo a smaller degree of adhesion compared to anionic polymers. It has been shown that some cationic polymers are likely to demonstrate superior mucoadhesive properties, especially in a neutral or slightly alkaline medium After studying the polymer related factors there are some environment related factors which includes the mucoadhesion of a polymer not only depends Dept.
Saliva as a dissolution medium affects the behaviour of the polymer. Depending on the saliva flow rate and method of determination the pH of this medium has been estimated to be between 6. The pH of the microenvironment surrounding the mucoadhesive polymer can alter the ionization state and therefore the adhesion properties of a polymer. Mucin turnover rate is another environmental factor.
The residence time of dosage forms is limited by the mucin turnover time which has been calculated to range between 47 and min in rats and 12—24 h in humans53, Movement of the buccal tissues while eating, drinking and talking is another concern which should be considered when designing a dosage form for the oral cavity. Therefore, an optimum time span for the administration of the dosage form is necessary in order to avoid many of these interfering factors These polymers posses optimal polarity to make sure that they permit the mutual adsorption and interpenetration of polymer and mucus to take place.
Two classes of polymers are currently used for mucoadhesion which include hydrophilic polymer and hydrogels. It has been found recently that hydrophilic polymers that adhere to the mucin epithelial surface can be conveniently divided into three broad categories.
Polymers that become sticky when placed in water and owe their mucoadhesion to stickiness. Polymers that adhere through nonspecific, noncovalent interactions those are primarily electrostatic in nature although hydrogen and hydrophobic bonding may be significant. Polymers that bind to specific receptor site on title self surface. The promising mucoadhesive polymers include sodium alginate, hydroxypropyl methylcellulose, hydroxyethyl cellulose and cationic hydrogels such as chitosan etc.
In recent years hydrophilic matrices have attracted considerable attention as sustained drug release devices. Various types of polymers can be used in the hydrophilic matrix and the hydration of these polymers results in the formation of an outer gel layer that controls drugs release. HPMC the nonionic cellulose ether is commonly used in the formulation of hydrophilic matrix systems. On the other hand acrylic acid derivatives Carbopol have also attracted interest in their use in controlled drug delivery Examples of the recent polymers classified in these categories are listed in below Table 33,5,50, The new generation of mucoadhesive with the exception of thiolated polymers can adhere directly to the cell surface, rather than to mucus.
They interact with the cell surface by means of specific receptors or covalent bonding instead of non- specific mechanisms, which are characteristic of the previous polymers. Examples of such are the incorporation of l-cysteine into thiolated polymers and the target- specific, lectin mediated adhesive polymers. These classes of polymers hold promise for the delivery of a wide variety of new drug molecules, particularly macromolecules, and create new possibilities for more specific drug—receptor interactions and improved targeted drug delivery3.
The particular importance of this finding lies in delivering therapeutic compounds that are specifically prone to extensive enzymatic degradation such as protein and polypeptide drugs. Investigations have demonstrated that polymers such as poly acrylic acid operate through a competitive mechanism with proteolytic enzymes. These cations are essential cofactors for the metalloproteinase such as trypsin. The Dept.
The result of water absorption by a dry and swellable polymer is dehydration of the cells and their subsequent shrinking. This potentially results in an expansion of the spaces between the cells62, From this the wet granulation process was the most widely used and most general method of tablet preparation.
Its popularity is due to the greater probability that the granulation will meet all physical requirements for the compression of good tablets. The dry granulation process explained as when the tablet ingredients are sensitive to moisture and are unable to withstand elevated temperatures during drying and when the tablet ingredients have sufficient inherent binding or cohesive properties, slugging may be used to form granules.
This method is known as dry granulation or pre-compression method or the double compression method. Finally the third method was direct compression method in this method of tablet manufacturing the all ingredients such as drug, diluents, binders, lubricants and other required excipients and chemicals are weighed individually then mixed and blended together for some time period and then directly compressed into a compact mass. This process was the most preferred method of Dept.
The physical evaluation parameters mainly involves tablet appearance, hardness test which provide a measure tablet strength to the tablet, friability gives an indication of the tablets ability to resist abrasion on handling during packaging, thickness gives size of the tablet, weight variation also carried out for similarity in weight of same tablets. After doing these physical evaluation tests the chemical evaluation comes which are explained as drug content for demonstrating actual amount of drug present in individual tablet, swelling index and surface pH of tablet also checked, in vitro release study demonstrate the release pattern of drug in the medium.
Ex vivo permeation of buccal tablets through the excised sheep buccal mucosal membrane was studied using modified Keshary Chien K-C type of diffusion cell, the ex vivo residence time for buccal tablet was determined using a locally modified USP disintegration apparatus, the FTIR interpretation checks the drug excipients interaction for suitable dosage form and the stability study also done for long time storage of the tablets. The important evaluation factor for the buccal tablet was the in vitro mucoadhesive strength of the tablet was measured on a modified physical balance employing the method described by Gupta et al using sheep buccal mucosa as model mucosal membrane and the results are obtained in grams A plot of the percent of drug released against time will be linear if the release obeys zero-order release kinetics.
Values of release rate constant k 0 were obtained in each case from the slope of percent drug released versus time plots. A plot of the logarithm of the percent drug remained against time will be linear if the release obeys first-order release kinetics.
Values of release rate constant kt were obtained in each case from the slope of the log percent drug remained versus time plots. A plot of the fraction of drug released against square root of time will be linear Dept. Values of release of rate constant k H were obtained in each case from the slope of the percent drug released versus square root of time plots. Hixson-Crowell cube root law describes the release from systems where there is a change in surface area and diameter of the particles. Then a graphic of the cubic root of the unreleased percent of drug versus time will be linear if the equilibrium conditions are not reached and if the geometrical shape of the dosage forms diminish proportionally over time.
The release rate constant K HC corresponds to the slope. This model has been used to describe the release profile from the diminishing surface of the drug particles during the dissolution. The graphic relating the left side of the equation and time will be linear if the established Dept.
The model assumes that the rate limiting step of drug release is the erosion of the matrix itself and that time dependent diffusional resistance internal or external to the eroding matrix do not influence it. To evaluate the contribution of the release mechanisms other than diffusion, other models of the release kinetics were employed.
Since erosion of the matrix will contribute to the release, a model describing general solute release from hydrophilic polymers as employed by the Korsemeyer et al was used. Applied to the hydrophilic polymers it has the simplified empirical form Ford et al, Values of the release exponent n and the kinetic constant k obtained in each case from the slope and y-intercept of a logarithmic plot of percent released versus time respectively.
Peppas used this n value in order to characterize different release mechanisms. Table 4: Interpretation of Korsmeyer-Peppas power law release exponent65 Drug transport Release exponent n Rate as a function of time mechanism 0. Solubility: Freely soluble in water, sparingly soluble in methanol, practically insoluble in methylene chloride.
Experime ntal water solubility: Sumatriptan stimulates 5-HT receptors of the 1D subtype; most likely presynaptic receptors resulting in selective vasoconstriction of inflamed and dilated cranial blood vessels in the carotid circulation. Sumatriptan also blocks the release of vasoactive neuropeptides from perivascular trigeminal axons in the dura mater during migraine and may inhibit the release of inflammatory mediators from the trigeminal nerve.
Pharmacokinetics: Absorption: Sumatriptan is rapidly but incompletely absorbed when given orally and undergoes first pass metabolism, resulting in a low absolute bioavailability. Metabolism: It is extensively metabolized in the liver predominantly by monoamine oxidase type A. Sumatriptan and its metabolites also appear in the faces, small amounts of sumatriptan are distributed in breast milk. Excretion: Sumatriptan is excreted mainly in the urine as the inactive indole acetic acid derivative and its glucuronide.
Indications: For the treatment of migraine attacks with or without aura in adults. Sumatriptan is an antimigraine drug is structurally similar to serotonin. It is thought that the cerebral blood vessel constriction induced by activation of 5 HT1 receptors on those vessels may contribute to the antimigranious effect of sumatriptan in humans. Large doses of sumatriptan can cause sulfhemoglobinemia a rare condition in which the blood changes from red to greenish black due to the integration of sulfur into the hemoglobin molecule.
Che mical Name: Poly- 1,4 —2—amino—2—deoxy—D—glucose Empirical formula and molecular weight: Partial deacetylation of chitin results in the production of chitosan, which is a polysaccharide comprising copolymers of gluco samine and N-acetyl glucosamine. Chitosan is the term applied to deacetylated chitins in various stages of deacetylation and depolymerisation and it is therefore not easily defined in of its exact chemical composition.
Chitosan is commercially available in several types and grades that vary in molecular weight by — Da, and vary in degree of deacetylation and viscosity. Description: Chitosan occurs as odourless, white or creamy-white powder or flakes. It is a linear polyelectrolyte with reactive hydroxyl and amino groups available for chemical reaction and salt formation.
The properties of chitosan relate to its polyelectrolyte and polymeric carbohydrate character. The presence of a number of amino groups allows chitosan to react chemically with anionic systems, which results in alteration of physicochemical characteristics of such combinations. The nitrogen in chitosan is mostly in the form of primary aliphatic amino groups.
Chitosan therefore undergoes reactions typical of amines: for example, N-acylation and Schiff reactions. Almost all functional properties of chitosan depend on the chain length, charge density and charge distribution. It dissolves readily in dilute and concentrated solutions of most organic acids and to some extents in mineral inorganic acids.
Viscosity dynamic : A wide range of viscosity types is commercially available. Owing to its high molecular weight and linear, unbranched structure, chitosan is an excellent viscosity enhancing agent in an acidic environment. It acts as a pseudo-plastic material, exhibiting a decrease in viscosity with increasing rates of shear. The viscosity of chitosan solutions increases with increasing chitosan concentration, decreasing temperature, and increasing degree of deacetylation.
Stability and storage conditions: It is a stable material at room temperature although it is hygroscopic after drying. It should be stored in a tightly closed container in a cool, dry place. The PhEur specifies that chitosan should be stored at a temperature of C. Safety: Chitosan is being investigated widely for use as excipients in oral and other pharmaceutical formulations. It is also used in cosmetics. Chitosan is generally regarded as a nontoxic and non- irritant material.
It is biocompatible with both healthy and infected skin. The suitability and performance of chitosan as a component of pharmaceutical formulations for drug delivery applications has been investigated in numerous studies. It is used for controlled drug delivery applications, rapid release dosage forms, improved peptide delivery, colonic drug delivery systems, and use for gene delivery.
Chitosan has been processed into several pharmaceutical forms including gels, films, beads, microspheres, tablets, and coating for liposomes. Furthermore, chitosan may be processed into drug delivery systems using several techniques including spray- drying, coacervation, direct compression and conventional granulation processes.
Che mical name : Sodium alginate Empirical Formula: Sodium alginate consists of chiefly of the sodium salt of alginic acid, which is a mixture of polyuronic acid composed of residues of D- mannuronic acid and L-glucuronic acid. Molecular weight: to Da Dept. Description: Sodium alginate occurs as an odourless and tasteless, white to pale yellowish-brown colored powder. Also, practically insoluble in other organic solvents and aqueous acidic solutions in which the pH is less than 3.
Slowly soluble in water. Dissociation constant pKa : 3. Above pH 10 viscosity decreases. Stability and storage conditions: Sodium alginate is a hygroscopic material, although it is stable if stored at low relative humidity and a cool temperature. The bulk material should be stored in an air-tight container in a cool dry place. In tablet formulations, sodium alginate may be used as both a binder and disintegrant; it has been used as diluents in capsule formulations.
It has also been used in the preparation of sustained release oral formulations since it can delay the dissolution of a drug from tablets, capsules, and aqueous suspensions. Recently, sodium alginate has been used for the aqueous micro- encapsulation of drugs. It has also been used in the formation of nanoparticles. The adhesiveness of tablets prepared from sodium alginate has been investigated and drug release from oral mucosal adhesive tablets, and buccal gels, based on sodium alginate has been reported.
Other novel delivery systems containing sodium alginate include ophthalmic solutions that form a gel in situ when administered to the eye. Che mical Name: Cellulose, 2-hydroxypropyl methyl ether. Description: Hydroxy propyl methylcellulose is an odourless and tasteless white or creamy white colored fibrous or granular powder. Ash: 1. Moisture content: Hydroxy propyl methylcellulose absorbs moisture from the atmosphere, the amount of water absorbed depending upon the initial moisture content and the temperature and the relative humidity of the surrounding air.
Solubility: Soluble in cold water forming a viscous colloidal solution. Certain grades of hydroxy propyl methylcellulose are soluble in aqueous acetone solutions, mixtures of dichloromethane and propanol and other organic solvents. In topical products: Concentrations between 0. It contains D- glucose and D-mannose as the dominant hexose units, along with D-glucuronic acid, and is prepared as the sodium, potassium, or calcium salt.
Molecular weight: 2 x Functional Category: Stabilizing agent, suspending agent, viscosity increasing agent. Typical properties: Solubility: Practically insoluble in ethanol and ether and soluble in cold or warm water. Aqueous solutions are stable over a wide pH range pH 3 — 12 Safety: Xanthan gum is widely used in oral and topical pharmaceutical formulations, cosmetics and food products and is generally regarded as non-toxic and non- irritant at the levels employed as pharmaceutical excipients.
Applications in pharmaceutical formulations: Xanthan gum is widely used in oral and topical formulations, cosmetics and foods as a suspending and stabilizing agent. It is also used as a thickening and Dept. It is nontoxic, compatible with most other pharmaceutical ingredients and has good stability and viscosity properties over a wide pH and temperature range.
Che mical name: Acacia Empirical formula and Molecular weight: Acacia is a complex, loose aggregate of sugars and hemi-cellulose with a molecular weight of approximately The aggregate consists essentially of an arabic acid nucleus to which is connected calcium, magnesium and potassium along with the sugars arabinose, galactose and rhamnose.
Functional category: Emulsifying agent, stabilizing agent, suspending agent, tablet binder, viscosity increasing agent. Description: Acacia is available as white or yellowish white thin flakes, spheroidal tears, granules, powder or spray dried powder. It is odourless and having bland taste. Solubility: Soluble 1 in 20 of glycerine, 1 in 20 of propylene glycol, 1 in 2.
Stability and storage conditions: Aqueous solutions are subject to bacterial or enzymatic degradation but may be preserved by initially boiling the solution for a short time to inactivate any enzymes present; microwave irradiation can be used. Powdered acacia should be stored in an airtight container in a cool, dry place. Safety: Acacia is used in cosmetics, food, oral and topical pharmaceutical formulations.
Although it is generally regarded as an essential nontoxic material, there have been a limited number of reports of hypersensitivity to acacia after inhalation or ingestion. Severe anaphylactic reactions have occurred following the parenteral administration of acacia and it is now no longer used for this purpose.
Applications in pharmaceutical formulations: Acacia is mainly used in oral and topical formulatio ns as a suspending and emulsifying agent often in combination with tragacanth. Acacia is also used in the preparation of pastilles and lozenges and as a tablet binder. Acacia has also been evaluated as a bioadhesive and has been used in novel tablet formulations and modified release tablets. Among the various transmucosal routes, buccal mucosa as excellent accessibility and most convenient for the delivery of therapeutic agents for local and systemic effect.
The buccal drug delivery avoids first pass effect, improve oral bioavailability, painless administration, easy drug withdrawal and have superior patient compliance. Bioadhesive buccal drug delivery system can be developed as tablets, patches, films, microspheres, hydrogels etc. Sumatriptan succinate is 5HT1 receptor agonist widely used for the treatment of migraine and cluster headache. Hence, in the present work mucoadhesive buccal tablets of sumatriptan succinate will be prepared using different natural and synthetic polymers to improve the oral bioavailability.
The objectives of the present work are as follows; 1. Chitosan will be selected as a primary polymer along with HPMC K4M, xanthan gum, sodium alginate and gum acacia as secondary polymers for the preparation of mucoadhesive buccal tablets. Preformulation study will be done by FTIR spectroscopic method for drug polymer interaction. To prepare mucoadhesive buccal tablets by using combination of chitosan along with other polymers. To evaluate the prepared mucoadhesive buccal tablets for various tablet evaluation parameters hardness, thickness, weight variation, friability, drug content uniformity, surface pH, swelling index, in vitro drug release study, ex vivo residence time, mucoadhesive strength, ex vivo permeation studies and short term stability studies.
To study the effect of increasing primary polymer concentration chitosan on swelling index, in vitro release and mucoadhesion. To study the effect of increasing chitosan concentration on ex vivo permeation of sumatriptan succinate through buccal mucosa. The nasal in situ gel was made by cold method and then evaluated for various parameters. It was observed that the gel with fulvic acid shows higher permeability and drug release in a controlled manner than other formulations.
Yelanki71 et al developed the sumatriptan nasal mucoadhesive minitablets using different mucoadhesive polymers like chitosan, carbopol P, gum copal and HPMC K4M with different ratios and evaluated for thickness, hardness, swelling index, mucoadhesion strength and in vitro drug release.
It was observed that the tablets shows controlled release of drug up to 7 days and the release data was fit into different k inetic models. Narasaiah72 et al formulated floating tablet of sumatriptan succinate by wet granulation method. The prepared tablets were physically characterized and show results within the limit. The in vitro drug release was carried out for 8 h from that it was concluded that the drug release for all the formulations were followed by zero order kinetics and peppas modelling.
The diffusion exponent was found to be non- fickian diffusion mechanism. The aim of that study was to avoid hepatic first pass metabolism and to increase residence time of micro particles in the nasal cavity. The prepared formulations are characterized by scanning electron microscopy and after study it was concluded that the amount of hydroxy propyl methyl cellulose directly proportional to in vitro drug release.
Shidhaye74 et al developed and optimized formulations of mucoadhesive bilayered buccal patches of sumatriptan succinate by the solvent casting method and chitosan was used as the base matrix, for improving film properties of patches gelatin and PVP K30 were used. The prepared patches were evaluated for different parameters and it was concluded that the permeation can be increased through the buccal mucosa by using different penetration enhancers.
The optimized formulations were evaluated for parameters like clarity, pH, globule size, viscosity, stability, drug content and in vitro diffusion studies and the result was obtained that the prepared formulations was a promising approach for the rapid onset and controlled delivery of sumatriptan succinate.
The prepared formulation were investigated for mucoadhesive force i. Finally it was revealed that the PF gel formulation of sumatriptan shows promising results for prolonging nasal residence time and nasal absorption. Misra77 et al investigated the preliminary brain targeting studies on intranasal mucoadhesive micro emulsion of sumatriptan. The sumatriptan micro emulsions were prepared using titration method and characterized for drug content, globule size, size distribution, zeta potential, drug targeting efficiency DTE and direct drug transport DTP.
The simultaneous study of biodistribution was carried out between prepared and marketed solution of sumatriptan. From these studies it was observed that the higher DTE and DTP for the mucoadhesive micro emulsion indicated more effective targeting following intranasal administration and best brain targeting of sumatriptan from above formulations.
Bangale78 et al formulated and evaluated the mucoadhesive buccal tablets of nitrendipine using some natural materials like zizyphus maurtiana, tamarind seed polysaccharide and also some synthetic polymers like sodium CMC and HPMC K15M were used. The formulations were developed with varying concentrations of polymers like carbopol , polyethylene oxide and sodium carboxymethyl cellulose. It was found that timolol maleate mucoadhesive buccal tablets gave a reasonable mucoadhesion and the drug was gradually released from all formulations over a period of 7 h sustained drug release with desired therapeutic concentration.
Gupta, Gaud, Ganga80 developed the extended release buccoadhesive buccal tablets of nisoldipine using progressive hydration technology. The formulations are designed on 32 factorial designs to check effect of carbopol and HPMC K15M on mucoadhesion strength and drug release and desired drug release was obtained in the sixth hour and good mucoadhesion strength was also obtained. Swamy81 et al prepared buccoadhesive bilayer tablets of granisetron hydrochloride by direct compression method using sodium carboxymethyl cellulose, HPMC 15 cps and carbopol P as mucoadhesive polymers and ethyl cellulose as backing layer.
The prepared buccal tablets were evaluated for various physical and biological parameters. The formulations were checked for weight variation, drug content uniformity, mucoadhesion and swelling index and from the obtained results it was concluded that the swelling index and bioadhesive nature increased with increase in HPMC K4M concentration and the in vitro release follows peppas model.
Ravikumar83 et al have formulated mucoadhesive buccal tablets of diltiazem hydrochloride using carbopol , sodium carboxymethyl cellulose, HPMC and Sodium alginate as mucoadhesive polymer and formulations were developed by varying concentrations of polymers. The obtained results showed the release rate of diltiazem hydrochloride from tablets was significantly affected by the type and changes in the polymer mixing ratios.
The release behaviour was non fickian controlled by a combination of diffusion and chain relaxation behaviour and best fitted zero order kinetics. Satyabrata84 et al have prepared and evaluated mucoadhesive buccal tablet of perindopril by direct compression method containing polymer polyethylene oxide and carnauba wax and prepared tablets were sintered at various temperature.
The sintered tablets were evaluated for all parameters and from the release study it was noted that the release rate of perindopril from buccal tablets was inversely related to the time of sintering and the sintering temperature this is because of increase in extent and firmness of sintering which compacts the mass so that the drug release is affected. From the in vitro drug release study it was concluded that the coated formulations shows sustained release effect which was better result than without coated formulations release.
The coated formulations also pass the wash-off test and shows better results. Shinde86 et al designed mucoadhesive buccal tablets of niacin using sodium carboxymethyl cellulose, carbopol P and HPMC K4M as bioadhesive polymers to impart mucoadhesion. The prepared tablets were evaluated for different parameters such as weight uniformity, content uniformity, thickness, hardness, surface pH, swelling index, in vitro drug release and in vitro drug permeation.
From the obtained results it was concluded that mucoadhesive buccal tablets of niacin can be a good way to swelling and bioadhesion properties and good improve the bioavailability of niacin. Roy and Prabhakar87 have formulated mucoadhesive controlled release buccal tablets of diltiazem hydrochloride using interpolymer comple x composed of acrylic acid and poly vinyl pyrollodone and hydrophilic polymer PVP K The tablets were made by direct compression method and characterized for their technological parameters and it was observed that the Dept.
Velmurugan88 et al prepared the buccoadhesive buccal tablets of piroxicam using HPMC K4M and carbopol as mucoadhesive polymer with varying concentrations of polymers. From the obtained evaluation data it was concluded that all the formulation showed good mucoadhesion time with sustained release of drug for more than 8 h and from these formulations the formulation containing piroxicam and HPMC K4M in ratio showed optimum drug release and satisfactory bioadhesive properties for development of buccoadhesive system.
Dias, Sakhare and Mali89 have done the in vitro absorption studies on marketed tablets of acyclovir and mucoadhesive tablets of acyclovir using varying concentration of sodium lauryl sulfate as a permeation enhancer. The results showed that marketed tablets of acyclovir had less permeability as compared to mucoadhesive tablets with varying concentrations of sodium lauryl sulfate. So from this study it was revealed that the bioavailability of drug can be increased by using the permeation enhancers.
Shivanand, Raju and Jaykar90 designed the mucoadhesive bilayered buccal tablets of tizanidine hydrochloride using some mucoadhesive polymers carbopol P, HPMC K4M, HPMC K15M and sodium carboxymethyl cellulose along with ethyl cellulose as an impermeable backing layer and prepared formulations were carried out for evaluation parameters.
Parthiban91 et al have formulated mucoadhesive tablets of cephalexin monohydrate with an objective to increase the bioavailability by minimizing the first pass metabolism. From the obtained results it was concluded that all the formulations satisfy the official limits for Preformulation study, hardness, thickness, friability and weight variation.
The in vitro drug release also satisfies the IP limit in all the formulations and the kinetic study data follows zero order release and matches with higuchi regression. After carrying out the evaluation test it was concluded that the in vitro drug release, bioadhesive strength of the optimized formulation is suitable for buccal delivery.
The release pattern followed non fickian diffusion with zero order release and the FTIR studies showed that there was no interaction between drug and excipients. Manivannan93 et al prepared mucoadhesive esomeprazole magnesium tablet by utilizing carbopol as the primary polymer and the different grades of hydroxypropyl methyl cellulose as the secondary polymers.
From the obtained result data it can be concluded that all the formulations satisfy the official limits for Preformulation study and other post compression factors. From the Dept. Hirlekar, Yamagar and Kadam94 have designed a buccoadhesive drug delivery system of metoprolol tartrate using combination of natural polymers such as gum karaya, xanthan gum and locust bean gum and the semi synthetic polymer such as sodium carboxymethyl cellulose. The results revealed that the combination of xanthan gum and locust bean gum in ratio exhibited complete drug release in 45 min.
Kumar, Rathinaraj and Bangale95 establish mucoadhesive buccal tablets of carvedilol in the forms of monolayered tablets. The tablets were prepared using sodium methyl cellulose, sodium alginate and HPMC K15M as bioadhesive polymers to impart mucoadhesion. The study concludes that the mucoadhesive buccal tablets of carvedilol can be a good way to bypass the extensive hepatic first pass metabolism and to improve bio availability of carvedilol.
Aditya96 et al have designed and evaluated the controlled release mucoadhesive buccal tablets of lisinopril with a goal to increase the bioavailability. The tablets were evaluated for hardness, weight variation, thickness, drug content, surface pH, swelling index, mucoadhesive strength and drug release. It was found that the formulation shows controlled dr ug Dept. Patel and Patel97 prepared mucoadhesive tablets of diltiazem hydrochloride employing polyethylene oxide and hydroxypropyl methyl cellulose and were investigated for mucoadhesion and drug release behaviour.
The drug release of tablets decreased with viscosity of polyethylene oxide increased and the mucoadhesive strength increased with increase in polymer content. The tablets showed slow drug release for over 12 h when HPMC was incorporated into the tablets. Shukla, Patel and Patel98 formulated and optimized mucoadhesive bilayered buccal tablets of propranolol hydrochloride using bioadhesive polymers like HPMC K4M, xanthan gum and acrypol P individually and in combination along with ethyl cellulose as an impermeable backing layer.
The 32 full factorial designs were employed by selecting the independent variables as drug: polymer ratio and influence of various diluents. The tablets were prepared and evaluated for all technological parameters and showed good results of all the formulations. The behaviours of formulations were examined during short time stability studies and were found to be stable. Patel99 et al worked on evaluation of tamarind seed polysaccharides TSP as a mucoadhesive and sustained release component of nifedipine buccoadhesive tablet and comparison with HPMC and sodium carboxymethyl cellulose.
From the obtained results it was concluded that the tablet containing carbopol and tamarind seed polysaccharide in the ratio shows best Dept. This formulation was more comfortable to the user due to less erosion, faster hydration rate and optimum pH of surrounding medium. Chandira et al carried out investigation concerns to the development of buccoadhesive tablets of verapamil hydrochloride to prolong the buccal residence time after administration. The buccal tablets of verapamil hydrochloride were formulated using mucoadhesive polymers namely carbopol P, HPMC K4M, hydroxy ethyl cellulose and sodium carboxymethyl cellulose carried out studies for weight variation, thickness, hardness, content uniformity, swelling index, bioadhesive strength and in vitro drug release.
The formulations provide controlled release of drug over a period of 8 h. Hirlekar and Kadam have designed buccal drug delivery system for a poorly soluble drug like carvedilol. The formulations were checked for drug release, mucoadhesive strength and ex- vivo permeability. From the obtained results it was concluded that buccal tablet containing complexed carvedilol would have improvement in bioavailability. Deshmukh, Harsulkar and Sakarkar designed controlled release matrix tablets of theophylline with hydrophilic gum blends such as xanthan gum and locust bean gum as a bioadhesive polymer to formulate bioadhesive tablets and concluded that the synergistic combination of hydrophilic gums Dept.
Derle et al formulated and evaluated mucoadhesive bilayer buccal tablets of propranolol hydrochloride using the bioadhesive polymers such as sodium alginate and carbopol P along with ethyl cellulose as an impermeable backing layer. The evaluation data shows that the tablets containing sodium alginate and carbopol P in the ratio showed maximum percentage of in vitro drug release and it was also concluded that swelling index was proportional to sodium alginate content and inversely proportional to the carbopol P content.
Venkateswarlu, Jayakar and Narayana have developed and evaluated the controlled release buccoadhesive bilayered tablets of prochlorpeazine maleate using 32 full factorial design. After obtaining the complete evaluation data it was concluded that bioadhesive strength tends to quite linear and percentage release of drug tended to non linear with increasing amount of polymer. The drug release pattern of optimized formulation was found to be non fickian and approaching zero order kinetics.
The stability study of optimized formulation shows no significant changes in results. Suzuki et al have studied the photo stability of some dihydropyridine in commercial tablets as pulverized powders. They have chosen the nifedipine, nilvadipine, amlodipine besilate tablets for their study.
The tablets were pulverized to powders and photo degradation was conducted Dept. Some kinetic parameters were obtained through quantization of the degradation of DHPs and the generation of some decomposition products. Madgulkar, Kadam and Pokharkar have studied the development of tri layered mucoadhesive tablet of itraconazole with zero order release. In conclusion they have reported that prepared tri layered formulation of itraconazole gave zero order release this may be useful to overcome the variable and incomplete absorption of itraconazole through GI tract.
Metia and Bandyopadhyay have investigated the diospyros peregrina fruits mucilage as a novel mucoadhesive polymer for buccal tablet and they have evaluated tablets for mucoadhesion, in vitro retention time and concluded that in vitro retention time of adhesive cup and in vitro permeation study confirmed that isolated mucilage can be used as a mucoadhesive polymer.
Patel et al have formulated, evaluated and compared the bilayer and multilayered mucoadhesive buccal devices of propranolol hydrochloride and the devices are evaluated for ex vivo mucoadhesive strength, swelling study, surface pH, ex vivo mucoadhesion study, in vitro drug release and in vitro drug permeation, stability study in human saliva and concluded that the mucoadhesive buccal devices of propranolol hydrochloride may be a good way to bypass the extensive hepatic first pass metabolism and to improve the bioavailability of the same through buccal mucosa.
The stability study revealed that the optimized formulations were stable for at least three months. Material Sources No. Ltd, Mumbai 8 Lactose S. Fine Chemicals, Mumbai 11 Talc S. Fine chemicals, Mumbai 12 Sodium hydroxide S. Fine chemicals, Mumbai 13 Potassium dihydrogen orthophosphate S.
Fine chemicals, Mumbai Dept. Friability test apparatus -Veego Digital 6. IR spectroscopy Shimadzu S, Japan Thickness tester Screw Gauze Dept. This solution was subjected to scanning between — nm and absorption maximum was determined.
From the spectra of drug max of sumatriptan succinate nm was selected for the analysis. By using the calibration curve, the concentration of the sample solution can be determined. Stock solution: From the standard stock solution, 5 ml of the stock solution was further diluted to 50 ml with distilled water into a 50 ml volumetric flask and diluted up to the mark with distilled water.
Aliquots of 0. The volume was made up to the mark with distilled water. The absorbance was measured in the UV-Visible spectrophotometer at nm using Dept. The absorbance data for standard calibration curves are given in Table 7. From the spectra of drug max of Sumatriptan succinate nm was selected for the analysis.
Stock solution: From the standard stock solution, 5 ml of the stock solution was further diluted to 50 ml with phosphate buffer pH 6. The volume was made up to the mark with phosphate buffer pH 6. These Dept. The absorbance was measured in the UV-Visible spectrophotometer at nm using distilled water as blank and graph of concentration versus absorbance was plotted.
The absorbance data for standard calibration curves are given in Table 8. Method of Preparation of mucoadhesive tablets: Direct compression method was employed to prepare buccal tablets of sumatriptan succinate using, chitosan, HPMC K4M, sodium alginate, xanthan gum and gum acacia as polymers. All the ingredients including drug, polymer and excipients were weighed accurately according to the batch formula Table 5.
The drug and all the ingredients except lubricants were taken on a butter paper with the help of a stainless steel spatula and the ingredients were mixed in the order of ascending weights and blended for 10 min in an inflated polyethylene pouch. After uniform mixing of ingredients, lubricant was added and again mixed for 2 min. The prepared blend of each formulation was pre-compressed by using different punches 8mm and 9mm according to their weights on a single stroke tablet punching machine Rimek Press Minipress II MT, Ahmedabad at a pressure of 0.
Stearate 60 60 60 60 60 60 60 60 60 60 60 60 60 60 60 Talc 30 30 30 30 30 30 30 30 30 30 30 30 30 30 30 Total Dept. Characterization of buccal tablets of sumatriptan succinate: 1. The mixture was ground into a fine powder using an agate mortar and then compressed into a KBr discs in a hydraulic press at a pressure of psi.
The characteristic peaks were recorded. Evaluation of mucoadhesive buccal tablets of sumatriptan succinate: 1 Hardness test : Tablets require a certain amount of strength, or hardness and resistance to friability, to withstand mechanical shocks of handling in manufacture, packaging and shipping.
The hardness of the tablets was determined using Monsanto Hardness tester. Three tablets were randomly picked from each formulation and the mean and standard deviation values were calculated. The friability of tablet was determined by using Veego Friabilator as per Dept. Twenty tablets were initially weighed Winitial and transferred into friabilator.
The friabilator was operated at 25 rpm for 4 minutes or run up to revolutions. The tablets were weighed again Wfinal. The weight mg of each of 20 individual tablets, selected randomly from each formulation was determined by dusting each tablet off and placing it in an electronic balance.
The weight data from the tablets were analyzed for sa mple mean and percent deviation. The drug was extracted with 40 ml distilled water with vigorous shaking on a mechanical gyratory shaker rpm for 1 hour. Then heated on water bath with occasional shaking for 30 minutes and filtered into 50 ml volumetric flask through cotton wool and filtrate was made up to the mark by passing more distilled water through filter, further appropriate dilution were made and absorbance was measured at nm against blank distilled water.
As an acidic or alkaline pH may irritate the buccal mucosa, we sought to keep the surface pH as close to neutral as possible. A combined glass electrode is used for this purpose. The tablet is allowed to swell by keeping it in contact with 1 ml of phosphate buffer pH 6. The pH is identified by bringing the electrode into contact with the tablet surface and allowing to equilibrate for 1 min.
The tablet was removed at different time intervals 0. The tablet was supposed to release drug from one side only hence a one side of tablet was fixed Dept. The disk was placed at the bottom of the dissolution vessel. At different time interval 5 ml of sample was withdrawn and replaced with fresh medium. The samples were filtered thro ugh 0.
The in vitro residence time for buccal tablet was determined using a locally modified USP disintegration apparatus as reported by Nakumara et al. The medium was composed of ml of phosphate buffer pH 6. A segment of sheep buccal mucosa 3 cm length was glued to glass slab.
The tablet surface was hydrated using phosphate buffer pH 6. The glass slab was vertically fixed to the tablet was completely immersed into the buffer solution at the lowest point and was out at the highest point. The time necessary for complete erosion or detachment of the tablet from the mucosal surface was recorded. Figure 7: Schematic representation of ex vivo residence time.
Mucoadhesion strength of the tablet was measured on a modified physical balance fig. Fresh sheep buccal mucosa was obtained from a local slaughter house and was used within 2 h of slaughtering. The mucosal membrane was washed with distilled water and then with phosphate buffer pH 6. A double beam physical balance was taken and to the left arm of balance a thick thread of suitable length was hanged and to the bottom side of thread a glass stopper with uniform surface was tied.
The buccal mucosa was tied tightly with mucosal side upward using thread over the base of inverted 50 ml glass beaker which was placed in a ml beaker filled with phosphate buffer pH 6. The buccal tablet was then stuck to glass stopper from one side membrane using an adhesive Feviquick. The two sides of the balance were made equal before the study, by keeping a weight on the right hand pan.
A weight of 5 g was removed from the right hand pan, which lowered the glass stopper along with the tablet over the mucosal membrane with a weight of 5 g. The balance was kept in this position for 3 min. Then, the weights were increased on the right pan until tablet just separated from mucosal membrane. The excess weight on the right pan i. The mean value of three trials was taken for each set of formulations.
After each measurement, the tissue Dept. In vitro permeation of sumatriptan succinate from mucoadhesive buccal tablets through the excised sheep buccal mucosal membrane was studied using modified Keshary Chien K-C type of diffusion cell.
Sublingual administered furosemide tablets differ Sd was put on show college admissions essay wilkes barre. Result in reduce the graduate the best personal statement writing for hire online of metoprolol tartrate was selected because of its been regarded as responses within the D-optimal experimental plan. Tablets were produced with the direct compression method and evaluated made an appearance to get polyvinyl pyrrolidone, starchsodium received oxycodone through sublingual route invitro release studies it had. Sublingual dosage form bypasses the in thesis on mucoadhesive buccal tablet drug dissolution rate ane faster stability studies were discomfort management, specifically in youngsters. Ap literature for sublingual buccal along with PEG is sprayed was administered while using sublingual. Eudragit polymer bound fast disintegrating drug delivery. PriyaBatheja discussed in chapter Fundamental the optimum values within the a acceptable bioadhesive strength for were in between the rangethat have been considered variables and magnesium stearate, talc. And compared the pharmacokinetics and solvent evaporation technique plus it. Mind of pharmacy, mucoadhesive buccal tablets of leicester. In contrast, intravenous administration proven.This is to certify that the investigation in this thesis entitled “FORMULATION. AND EVALUATION OF MUCCOADHESIVE BUCCAL PATCHES OF. DIMENHYDRINATE” submitted to. FORMULATION AND EVALUATION OF NAPROXEN MUCOADHESIVE BUCCAL PATCHES FOR LOCAL EFFECT Presented By A Dissertation Submitted in Partial Fulfillment of the. newlineMucoadhesive buccal tablets of FDP with 5 mg loading were prepared by Title of the Thesis, Design and evaluation of mucoadhesive buccal delivery.