Formulation and In –Vitro Evaluation of Bilayer Tablet of Atenolol for Biphasic Drug Release: Experimental Investigation
Challenges and Advances in Pharmaceutical Research Vol. 2,
21 April 2022
Objective: The goal of this study was to prepare a bilayer tablet of atenolol for biphasic drug release in order to improve its bioavailability and absorption in the lower gastrointestinal tract.
Methods: Croscarmellose sodium and sodium starch glycolate were used as super disintegrants in the formulation of immediate release crosspovidone, and it was directly compressed. Different grades of HPMC k4 M, HPMC K15 M, Gum Tragacanth, Gum Acacia, Guar gum, and Ethyl cellulose are used for the sustained release portion. Prior to compression, preformulation studies were carried out. Using a USP dissolution apparatus type 2(paddle), the compressed bilayer tablets were evaluated for weight variation, dimension, hardness, friability, drug content, disintegration time, and in-vitro drug release .
Results and Conclusion: The formulation IR3 showed regression coefficients value (r2) is 0.994. The data suggested that release kinetics follow first order drug release. IR3 formulation showed 95% drug release in 30 min and regression coefficients value (r2) value was found to be 0.994. It has 5%w/w crosspovidone used. The formulation F9 showed regression coefficients value (r2) is 0.992. The data suggested that release kinetics follow Zero order drug release. F9 formulation, using HPMC K15M and Gum acacia (1:1) showed 91.20% drug release at the end of 12 hrs. Formulation IR3F9 showed drug release for bilayer tablet faster release which containing 5%w/w crospovidone in immediate release layer and Sustained release which containing HPMC and guar gum (1:1). Formulation IR3F9 showed swelling index was found to be 206%, floating lag time was found to be 2 min. and total floating time up to 12 hrs. Dissolution profile for Bilayer tablet IR3F9 formulation a good relation between cumulative drug release and time. The release pattern showed 95.23% up to 12 hrs.
- Bilayer tablet
- biphasic drug release
- swelling index