Design and Evaluation of Gastroretentive Multiple Units of Atenolol – in- vitro and in-vivo Human Studies

Abstract

Objective: Atenolol is considered as a good candidate for incorporation into a gastroretentive dosage form due to its absorption window in the lower gastrointestinal tract. Hence this study was planned to formulate, characterize with in-vitro and in-vivo evaluation in human subjects.

Method: In this investigation multiple unit floating mini matrix tablets of Atenolol was formulated using HPMC (hydroxyl propyl methyl cellulose) polymers along with ethylcellulose by wet granulation method and prepared multiple units were again slightly compressed into single tablet within the hardness range of 3-4 Kg/cm2. The prepared tablets were subjected to physical evaluation, in-vitro drug release and in-vivo radiographic studies to determine residence time in human subjects.

Results: All the prepared batches showed in-vitro buoyancy. It was observed that the tablets remained buoyant for more than 12 h except F1 and F5 which remained buoyant upto 10 h. Formulation F3 was selected as the best formulation based on the in-vitro characteristics and used for in-vivo radiographic studies by replacing part of the drug by adding barium sulphate. These studies revealed that the tablets remained in the stomach for more than 6 hrs in human volunteers.

Conclusion: Based on in-vitro characteristics and in-vivo radiographic studies, it can be concluded that the best formulation is F3. By choosing multiple unit floating matrix tablets we can improve patient compliance and ensure better disease management due to increase in gastric retention.