It is Possible to Achieve Tablets With Good Tabletability From Solid Dispersions – The Case of the High Dose Drug Gemfibrozil

Author(s): Eduarda Rocha Bigogno, Luciano Soares, Matheus Henrique Ruela Mews, Melissa Zétola, Giovana Carolina Bazzo, Hellen Karine Stulzer, Bianca Ramos Pezzini*

Journal Name: Current Drug Delivery

Volume 18 , Issue 4 , 2021

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Background: Solid Dispersions (SDs) have been extensively used to increase the dissolution of poorly water-soluble drugs. However, there are few studies exploring SDs properties that must be considered during tablet development, like tabletability. Poorly water-soluble drugs with poor compression properties and high therapeutic doses, like gemfibrozil, are an additional challenge in the production of SDs-based tablets.

Objective: This study evaluates the applicability of SDs to improve both tabletability and dissolution rate of gemfibrozil. A SD-based tablet formulation was also proposed.

Methods: SDs were prepared by ball milling, using hydroxypropyl methylcellulose (HPMC) as a carrier, according to a 23 factorial design. The formulation variables were gemfibrozil:HPMC ratio, milling speed, and milling time. The response in the factorial analysis was the tensile strength of the compacted SDs. Dissolution rate and solid-state characterization of SDs were also performed.

Results: SDs showed simultaneous drug dissolution enhancement and improved tabletability when compared to corresponding physical mixtures and gemfibrozil. The main variable influencing drug dissolution and tabletability was the gemfibrozil:HPMC ratio. Tablets containing gemfibrozil- HPMC-SD (1:0.250 w/w) and croscarmellose sodium showed fast and complete drug release, while those containing the same SD and sodium starch glycolate exhibited poor drug release due to their prolonged disintegration time.

Conclusion: SDs proved to be effective for simultaneously improving tabletability and dissolution profile of gemfibrozil. Tablets containing gemfibrozil-HPMC-SD and croscarmellose sodium as disintegrating agent showed improved drug release and good mechanical strength, demonstrating the potential of HPMC-based SDs to simultaneously overcome the poor dissolution and tabletability properties of this drug.

Keywords: Gemfibrozil, solid dispersion, tabletability, tablet, drug dissolution, solubility.

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Article Details

Year: 2021
Page: [460 - 470]
Pages: 11
DOI: 10.2174/1567201817666201023121948
Price: $95

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PDF: 12