AIMTo prepare buspirone hydrochloride buccal adhesive tablet and investigate factors that influence drug release behavior and the drug release mechanism.

METHODSBuspirone hydrochloride buccal adhesive tablet was prepared with double layers structure composed of drug core and adhesive layer. The materials of the drug core were carbopol 974 and lactose, the adhesive layers were carbopol 974 and HPMC K4M. The influence of drug release factors such as adhesive layer component, adhesive layer weight and adhesive tablet hardness was investigated. The relationship between adhesive layer weight and drug release mechanism in vitro was studied.

RESULTSThe results showed that the weight of the adhesive layer and the hardness of adhesive tablet showed significant effects on drug release, but the adhesive layer component showed no significant effect. The optimum prescription of buspirone hydrochloride buccal adhesive tablet was carbopol: HPMC = 1:1, adhesive layer weight = 50%, and adhesive tablet hardness = 4 kg. The study of drug release mechanism from adhesive tablet showed that it was double directions when adhesive layer weight was 20%, and single direction first then double directions when 33.33%, and single direction all along when 50%.

CONCLUSIONThe speed and direction of drug release from adhesive tablet can be controlled by regulating adhesive layer weight.

Acrylic Resins ; Adhesiveness ; Administration, Buccal ; Anti-Anxiety Agents ; administration & dosage ; Buspirone ; administration & dosage ; Delayed-Action Preparations ; Drug Carriers ; Hardness ; Lactose ; analogs & derivatives ; chemistry ; Methylcellulose ; analogs & derivatives ; chemistry ; Oxazines ; Polyvinyls ; chemistry ; Tablets ; Technology, Pharmaceutical

The aim of present study was to prepare buccal tablets of fluconazole for oral candidiasis. The dosage forms were designed to release the drug above the minimum inhibitory concentration for prolonged period of time so as to reduce the frequency of administration and to overcome the side effects of systemic treatment. The buccal tablets were prepared by using Carbopol 71G and Noveon AA-1 by direct compression method. Microcrystalline cellulose was used as the filler and its effect was also studied. The prepared dosage forms were evaluated for physicochemical properties, in vitro release studies and mucoadhesive properties using sheep buccal mucosa as a model tissue. Tablets containing 50% of polymers (Carbopol & Noveon) were found to be the best with moderate swelling along with favorable bioadhesion force, residence time and in vitro drug release. The in vitro drug release studies revealed that drug released for 8 h, which in turn may reduce dosing frequency and improved patient compliance in oral candidiasis patients.
Acrylates ; administration & dosage ; chemistry ; pharmacokinetics ; Acrylic Resins ; administration & dosage ; chemistry ; pharmacokinetics ; Adhesiveness ; Administration, Buccal ; Animals ; Candidiasis, Oral ; drug therapy ; Cellulose ; administration & dosage ; chemistry ; Delayed-Action Preparations ; Drug Combinations ; Drug Stability ; Excipients ; Fluconazole ; administration & dosage ; chemistry ; pharmacokinetics ; Mouth Mucosa ; metabolism ; Polymers ; administration & dosage ; Sheep ; Tablets