Development of nimesulide amorphous solid dispersions via supercritical anti-solvent process for dissolution enhancement.

Development of nimesulide amorphous solid dispersions via supercritical anti-solvent process for dissolution enhancement. Eur J Pharm Sci. 2020 Jul 06;:105457 Authors: Liu G, Gong L, Zhang J, Wu Z, Deng H, Deng S Abstract Formulating amorphous solid dispersions (ASDs) is one of the most promising strategies to overcome solubility limitations in drug development. In this work, development of nimesulide (NIM) ASDs via supercritical anti-solvent (SAS) process was proposed, where the mixtures of dichloromethane (DCM) and methanol (MeOH) were selected as the liquid solvent, and the mixtures of hydroxypropyl methylcellulose (HPMC) and polyvinylpyrrolidone (PVP) were the dispersing materials. The effects of NIM/HPMC/PVP (w/w/w) ratio and DCM/MeOH (v/v) ratio on particle solid-state properties were investigated to identify successful operating conditions. NIM-ASDs powders were formed by well separated spherical microparticles, where NIM crystals had transformed into amorphous state completely; the production yield was 93.6±1.14%; and the reproducibility was very high. For NIM-ASDs, intermolecular interactions between NIM and dispersing materials were formed; the residual solvent was far below the ICH limit; and the chemical structure of NIM did not be degraded or disrupted. Moreover, NIM-ASDs increased the NIM solubility in PBS (pH=6.8) more than 5-folds; the dissolution of NIM from NIM-ASDs granules was faster and more complete than that f...
Source: European Journal of Pharmaceutical Sciences - Category: Drugs & Pharmacology Authors: Tags: Eur J Pharm Sci Source Type: research