Physical properties of solid dispersion of a nonsteroidal anti-inflammatory drug (M-5011) with Eudragit E.

E Horisawa, K Danjo, M Haruna

Index: Drug Dev. Ind. Pharm. 26(12) , 1271-8, (2000)

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Abstract

Some acidic nonsteroidal anti-inflammatory drugs (NSAIDs) are poorly soluble in the stomach. In this study, M-5011, d-2-[4-(3-methyl-2-thienyl) phenyl] propionic acid, was used as a model substance. To increase the dissolution rate of M-5011, a solid dispersion of M-5011 was prepared by the powder mixing method using Eudragit E-100 (aminoacryl methacrylate copolymer) as a carrier. Evaluation by X-ray diffraction and differential scanning calorimetry (DSC) revealed that M-5011 easily formed a solid dispersion with E-100. The dissolution behavior of a physical mixture prepared immediately after mixing and the mixture stored for 14 days at 40 degrees C were examined. It was observed that the former, containing a great deal of E-100, showed a fairly good dissolution behavior, and the latter had a better dissolution rate. The mechanism of the interaction of M-5011 and E-100 was investigated by infrared (IR) spectroscopy and nuclear magnetic resonance (NMR). The interaction was simulated by NMR using a monomer of Eudragit E-100.