Design and in vitro Evaluation of Mucoadhesive Buccal Tablets of Chelorpheniramine Maleate

Background:. The objective of study was to develop mucoadhesive buccal tablets of Chelorpheniramine maleate for extended period of time. The tablets were prepared using carbopol-934p as a primary polymer because of its excellent mucoadhesive property and secondary polymers like HPMCK4M, sodium alginate and guar-gum by direct compression method. Methods: Nine formulations were developed with varying concentrations of polymers. Buccal tablets were evaluated such as thickness, hardness, weight uniformity, content uniformity, swelling index, surface pH, ex vivo residence time, the tablets were evaluated for in vitro release in pH 6.8 phosphate buffer for 6 hr. Results: The ex vivo residence time for all formulations varied from 5.10 - 6.68 hr. The optimized formulation (F3) showed 6.68 hr, the surface pH was found to be 5.57 ± 0.30. This pH is near to the neutral therefore, it was inferred that neutral pH of the formulation does not cause any irritation on the mucosa. Tablets containing HPMCK4M (batch F1 to F3) as secondary polymers was found to exhibit least matrix erosion. Among the nine formulations of this group, F3 showed highest drug release (102.5 %), showed maximum swelling index of 123.2 %. The in vitro drug release profile of the optimized formulation (F3) was compared with marketed conventional tablet (chloral), the conventional tablet release only 64.44 % for 6 hrs where as the F3 formulation released up to 102.5 %. FTIR studies show no evidence on interaction between drug and polymers. Conclusion: Thus conclusion can be made that the stable mucoadhesive buccal tablets of chlorpheniramine maleate can be developed for the sustained release. Therefore, bioadhesive buccal delivery of chlorpheniramine maleate may be good way to by pass the first pass metabolism composed of (Drug: HPMCK4M) different ratios