Abstract
Drug release kinetics from matrix dosage form is governed by polymer swelling and erosion, drug dissolution/diffusion and polymeric combination. For the preparation of controlled release dosage form, hydrophilic, swellable polymers in optimum combination are essential. The major objective of the current study is to prepare Amoxicillin trihydrate-loaded bucco-matrix tablets by direct compression technique and to study the effect of ratio of HPMCK100M and HPMCK15M used in the formulation on the basic properties and on drugrelease and permeation kinetics. The tablets offered satisfactory physicochemical results. The buccal strength, detachment force and bond strength of the tablets were good enough to hold the tablets in the buccal region. The drug release data generated during in vitro drug release study of bucco-matrix tablets in phosphate buffer pH 6.8 were evaluated by zero-order, first-order, Higuchi, Korsmeyer – Peppas, and Kopcha models. Release exponent (n) of Korsmeyer- Peppas equation of the formulations exhibited diffusion as the principal mechanism of drug release. It was further confirmed by Kopcha model. Evaluation of diffusion and erosion terms in the Kopcha model showed that diffusion dominated swelling or erosion process through out the study. The permeation kinetics of the drug showed linearity when studied across goat buccal mucosa. Permeation coefficient of drug decreased with increase in % swelling index of the formulations.
Highlights
Drug release kinetics from matrix dosage form is influenced by polymer swelling, polymer erosion, and drug dissolution/diffusion and polymer ratio
Drug release kinetics from matrix dosage form is governed by polymer swelling and erosion, drug dissolution/diffusion and polymeric combination
Though Carbopol 934p has been included as mucoadhesive agent at same quantity (30 mg/tablet) in all the batches, the change in buccal strength as well as detachment stress signifies that HPMCK100M and HPMCK15M have influence on buccoadhesion
Summary
Drug release kinetics from matrix dosage form is influenced by polymer swelling, polymer erosion, and drug dissolution/diffusion and polymer ratio. For the preparation of controlled release dosage form, hydrophilic, swellable polymers in optimum combination are essential. Successful buccal drug delivery using buccal adhesive systems should have good bioadhesion to hold the formulation in the buccal cavity and maximize the intimacy of contact with buccal membrane. This formulation needs a vehicle that is responsible for releasing the drug at an controlled rate in buccal environment. The use of biocompatible polymers has been the prime focus in the design of bucco-matrix tablets. Hyroxypropyl methylcellulose (HPMC) is a widely used polymer for oral controlled drug
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