Formulation and Optimization of Osmotically Controlled Release Tablets of Glipizide: Hot Melt Granulation

Abstract

Background: The use of water-soluble additives in osmotic release tablets often renders the wet granulation method unsuitable. Hence, it was proposed to investigate the feasibility of preparing granules comprising of osmogen (sodium chloride), alkalizer (sodium carbonate), polyvinyl pyrroidone (Kollidon^® K 30) and carboxymethyl cellulose sodium (Cekol^® 30000) by a hot melt technique for obtaining sustained release of glipizide from tablets. Materials and methods: Dry powder mixture wetted with Tween™ 80 was sequentially exposed to 45–110°C for obtaining granules. The effect of varying the quantities of osmogen, Cekol 30000 in granules and pore former in the film coating on in vitro release of glipizide was investigated. Results: Glipizide release increased with an increase in the amount of hydrophilic polymer, osmogen and alkalizer and decreased with increase in the thickness of the coating membrane. Zero-order release independent of stirring rate and media pH through 16 h was observed from tablets of the optimized formulation (glipizide osmotic tablet [GOT] 12). The f2 value of 70.2 indicated similarity in release profiles from this formulation and the marketed extended-release tablet. Accelerated tests (ICH guidelines) revealed stability of GOT 12 tablets.

Acknowledgements

The authors acknowledge Geena Malhotra, Head Pharma R&D, Cipla Limited, Mumbai, India for her technical help throughout the work.

Financial & competing interests disclosure

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties. No writing assistance was utilized in the production of this manuscript.