Designing buccal mucoadhesive tablets of Doxofylline by using Ethocel, Carbopol 934P and Methocel K15M: A method to improve its bioavailability

Abstract

In order to avoid first pass metabolism and increase therapeutic effectiveness, the present studies were aimed to

develop a Doxofylline buccal mucoadhesive tablet using mucoadhesive polymers such as Methocel K15M,

Carbopol 934P and Ethocel. All the polymers were used alone or in combination as release retarding agent to

prolong the drug release as well as to increase mucoadhesive strength. The mucoadhesive buccal tablets were

prepared by direct compression method. The dry blend of drug and polymers were evaluated for precompression

parameters to ensure flow properties during tablet punching. The drug excipients compatibility was evaluated by

FTIR and DSC studies. The formulated mucoadhesive buccal tablets were evaluated for physicochemical parameters

such as hardness, thickness uniformity, weight variation, and moisture absorption studies. The prepared buccal

tablets were also evaluated for mucoadhesive strength, in vitro drug release and ex vivo drug permeation through

cellulose acetate membrane. FTIR and DSC results showed no evidence of interaction between the Doxofylline and

mucoadhesive polymers used for formulations. Ex vivo mucoadhesive strength, and in vitro release studies showed

that formulation DBMT15 containing 20% of Methocel K15M and 10% Ethocel of combination showed satisfactory

bioadhesive strength and exhibited optimum drug release (99.25% after 12h). The Stability of Doxofylline

mucoadhesive buccal tablets was determined in artificial human saliva and it was found that both Doxofylline and