Application of melt granulation technology to enhance tabletting properties of poorly compactible high-dose drugs

✍ Scribed by Jay P. Lakshman; James Kowalski; Madhav Vasanthavada; Wei-Qin Tong; Yatindra M. Joshi; Abu T. M. Serajuddin

• Publisher: John Wiley and Sons
• Year: 2011
• Tongue: English
• Weight: 434 KB
• Volume: 100
• Category: Article
• ISSN: 0022-3549
• DOI: 10.1002/jps.22369

✦ Synopsis

Using metformin HCl as the model drug and hydroxypropylcellulose (HPC) as the polymeric excipient, a melt granulation (MG) process that employs a twin-screw extruder has been developed to enhance compactibility of poorly compactible high-dose drug substances. A high (90%) drug-load tablet formulation, containing 1025 mg of active pharmaceutical ingredients and 109 mg of excipients, was produced. Drug-polymer-powder mixtures were melt granulated at a temperature above glass transition of HPC (130°C) but below melting point of metformin HCl (224°C). MG was compared with modified wet granulation (WG) and solvent granulation (SG) processes. Under identical compression force, the hardness of tablets produced was MG>SG>WG and the friability was MG