Preparation and in vitro/in vivo evaluation of the buccal bioadhesive properties of slow-release tablets containing miconazole nitrate.
Slow-release buccal bioadhesive tablets of miconazole nitrate were prepared by using polymer mixtures of buccoadhesive materials such as hydroxypropylmethylcellulose, sodium carboxymethylcellulose, carbopol 934p, and sodium alginate. The physicochemical properties, swelling index, microenvironment pH, in vitro drug release, in vivo buccoadhesion time, and miconazole salivary concentrations of the prepared tablets were shown to be dependent on the type and composition of the buccoadhesive materials used. The dissolution of miconazole from all the prepared tablets into phosphate buffer (pH 6.8) was controlled and followed non-Fickian release mechanisms. All the prepared tablets gave reasonable buccoadhesion time (2.45-3.65 hr). Infrared spectroscopy and differential scan calorimetry studies revealed the absence of significant interactions between miconazole nitrate and the selected buccoadhesive materials. Duration of the antifungal activity as measured by the inhibition zone of Candida albicans by extracted human saliva was significantly longer (p < 0.05), compared with commercial miconazole oral gel (Daktaren oral gel). Based on the results obtained, the prepared slow-release buccoadhesive tablets of miconazole would markedly prolong the duration of the antifungal activity with more patient convenience.
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt. fergmed@yahoo.com
Fergany A
FA
Mohammed
Hussin
H
Khedr
D000179:Acrylates / Q000737:chemistry; D000268:Adhesiveness; D000278:Administration, Buccal; D000328:Adult; D000464:Alginates / Q000737:chemistry; D000935:Antifungal Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*; D002266:Carboxymethylcellulose Sodium / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D018592:Cross-Over Studies; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004339:Drug Compounding; D005079:Excipients / Q000737:chemistry; D005260:Female; D020723:Glucuronic Acid; D006603:Hexuronic Acids; D006801:Humans; D065347:Hypromellose Derivatives; D066298:In Vitro Techniques; D008297:Male; D008747:Methylcellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D008825:Miconazole / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*; D012463:Saliva / Q000378:metabolism; D013607:Tablets; D013997:Time Factors
D000179:Acrylates; D000464:Alginates; D000935:Antifungal Agents; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005079:Excipients; D006603:Hexuronic Acids; D013607:Tablets; D065347:Hypromellose Derivatives; D008825:Miconazole; D020723:Glucuronic Acid; D008747:Methylcellulose; D002266:Carboxymethylcellulose Sodium; C453622:carbopol 934P