FORMULATION, EVALUATION AND OPTIMISATION OF SUSTAINED RELEASE FLOATING BILAYER TABLETS OF ARTEMETHER

P. Dhaneshwar, P. Stephen and A. N. Rajalakshmi*

ABSTRACT

The present research work is aimed at formulation, evaluation and optimization of effervescent floating bilayer tablets containing Artemether as sustained release. Tablets were formulated using direct compression technology, composing of two layers, i.e. Floating layer containing effervescent components and a hydrocolloid forming polymer and SR layer containing drug and a rate controlling polymer, designed to increase the gastric residence time, thus prolong the drug release. Formulations were developed as per the standard experimental design protocol using Design Expert Software (Version7.1.6, Stat-Ease Inc, Minneapolis, MN), by varying concentrations of HPMC K100M and Carbopol 934P, a total number of thirteen formulations were prepared. Central composite design (2-factor, 3-level) was used for the optimization. Concentration of Carbopol and HPMC K100M were considered as independent variables. Total floating time and Time taken for 95% drug release were considered as dependent variables. All other formulative ingredients and processing variables were kept invariant throughout the study. The optimised formulation, suggested by Design Expert Software, F13 showed floating lag time of 45 sec, floating time of almost 12 hours and maximum drug release of 98.3 % at the end of 12 hours. It can be concluded from the study that the problem of short gastric residence time resulting in low bioavailability and poor efficacy encountered with an oral formulation of Artemether can be overcome with the sustained release bilayer floating tablets of Artemether for effective treatment of Malaria.

Keywords: Sustained release, Floating bilayer tablets, Artemether, HPMC, Carbopol 934.