Physical properties of solid dispersion of a nonsteroidal anti-inflammatory drug (M-5011) with Eudragit E.
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.
Horisawa
E
E
Maruho R&D Laboratories, Pharmaceutical Research Section, 2763, Takamiya-cho, Hikone, Shiga 522-0201, Japan. horisawa_ahl@mii.maruho.co.jp
Danjo
K
K
Haruna
M
M
D000179:Acrylates / Q000008:administration & dosage; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000493:pharmacokinetics*; D004337:Drug Carriers; D005744:Gastric Acid; D006863:Hydrogen-Ion Concentration; D008768:Methylmethacrylates / Q000008:administration & dosage; D010666:Phenylpropionates / Q000493:pharmacokinetics*; D011208:Powders; D012995:Solubility; D013270:Stomach / Q000737:chemistry
D000179:Acrylates; D000894:Anti-Inflammatory Agents, Non-Steroidal; D004337:Drug Carriers; D008768:Methylmethacrylates; D010666:Phenylpropionates; D011208:Powders; C104139:2-(4-(3-methyl-2-thienyl)phenyl)propionic acid; C068685:Eudragit E 30D