title: Preparation and characterization of a powder containing an oily liquid drug with Eudragit EPO or L100 copolymer.
abstract: Oily liquid drugs are not convenient for oral administration. We developed a powder containing clofibrate (CF), a model of an oily drug, using aminoalkyl methacrylate copolymer (EPO) or methacrylic acid copolymer (L100). CF or a mixture of CF and soybean oil was emulsified with EPO or L100 aqueous solution. Using a high-pressure homogenizer, a stable emulsion was obtained, and a powder was then obtained by lyophilization of the emulsion. The content of CF in the powder depended on the formulation, with the highest contents being 24.6% and 27.1% for EPO and L100, respectively. The incorporation ratio of CF was higher for L100 than for EPO. The powder using EPO was sticky because of leaked CF and the low glass transition temperature of EPO. The powder using L100 was a typical powder obtained by lyophilization. The leakage of CF from the powder was <2%, lower than for EPO powder. The dissolution of CF from powder using EPO was fast, regardless of the pH of the medium, but the powder using L100 showed enteric-soluble characteristics, indicating that CF is well incorporated in L100.
authors.affiliation: a Department of Pharmaceutics and Biopharmaceutics , Showa Pharmaceutical University , Machida , Tokyo , Japan.
authors.forename: Makiko
authors.initials: M
authors.lastname: Fujii
authors.affiliation: a Department of Pharmaceutics and Biopharmaceutics , Showa Pharmaceutical University , Machida , Tokyo , Japan.
authors.forename: Ayari
authors.initials: A
authors.lastname: Kawakami
authors.affiliation: a Department of Pharmaceutics and Biopharmaceutics , Showa Pharmaceutical University , Machida , Tokyo , Japan.
authors.forename: Asumi
authors.initials: A
authors.lastname: Saito
authors.affiliation: a Department of Pharmaceutics and Biopharmaceutics , Showa Pharmaceutical University , Machida , Tokyo , Japan.
authors.forename: Haruna
authors.initials: H
authors.lastname: Tuchiya
authors.affiliation: a Department of Pharmaceutics and Biopharmaceutics , Showa Pharmaceutical University , Machida , Tokyo , Japan.
authors.forename: Naoya
authors.initials: N
authors.lastname: Koizumi
authors.affiliation: a Department of Pharmaceutics and Biopharmaceutics , Showa Pharmaceutical University , Machida , Tokyo , Japan.
authors.forename: Yoshiteru
authors.initials: Y
authors.lastname: Watanabe
mesh_terms: D000180:Acrylic Resins / Q000737:chemistry; D000284:Administration, Oral; D002626:Chemistry, Pharmaceutical / Q000379:methods; D002994:Clofibrate / Q000737:chemistry*; D004339:Drug Compounding / Q000379:methods; D016503:Drug Delivery Systems / Q000379:methods; D004655:Emulsions / Q000737:chemistry; D006863:Hydrogen-Ion Concentration; D011108:Polymers / Q000737:chemistry*; D011109:Polymethacrylic Acids / Q000737:chemistry*; D011208:Powders / Q000737:chemistry*; D012995:Solubility; D013024:Soybean Oil / Q000737:chemistry*; D044366:Transition Temperature
chemical_list: D000180:Acrylic Resins; D004655:Emulsions; D011108:Polymers; D011109:Polymethacrylic Acids; D011208:Powders; C038300:methylmethacrylate-methacrylic acid copolymer; D013024:Soybean Oil; C518398:Eudragit E PO; D002994:Clofibrate
keywords: Clofibrate; Eudragit EPO; Eudragit L100; emulsion; microfluidization; powderization