Preparation of Griseofulvin for Topical Application Using N-Methyl-2-pyrrolidone
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概要
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We attempted to prepare a new griseofulvin formulation for topical application using N-methyl-2-pyrrolidone (NMP). Griseofulvin dissolves poorly in both water and oil, but dissolves in NMP to a concentration of about 100 mg/ml. A soybean oil-water emulsion with soybean lecithin and NMP as emulsifier and co-solvent, respectively, was prepared using a Microfluidizer, a high-pressure homogenizer. The size of the droplets in emulsion was about 200 nm, and the emulsion was stable for over 3 months. The skin permeation of griseofulvin through Yucatan micropig skin was studied in vitro using vertical type cells under donor phase open conditions. The permeation of griseofulvin from the NMP-water mixture (0-40%) into the skin tended to increase with increasing NMP concentration, although this finding was not statistically significant. Permeation from emulsion (oil phase, 20%; NMP 10-40%) was significantly higher than that from the water-NMP mixture. Permeation from the oil-NMP mixture was highest among the formulations investigated, and permeation from emulsion under donor phase closed conditions was significantly lower than that under open conditions. We believe that the evaporation of water from the emulsion after application to the skin was an important factor in skin permeation enhancement. When the emulsion containing 3% l-menthol was applied, a sufficient skin concentration (47μg/cm^3 in dermis) was obtained.
- 公益社団法人日本薬学会の論文
- 2000-11-01
著者
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WATANABE Yoshiteru
Showa Pharmaceutical University
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FUJII Makiko
Showa Pharmaceutical University
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Matsumoto M
Osaka Medical Center For Cancer And Cardiovascular Diseases Osaka
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Matsumoto Misako
Department Of Immunology Osaka Medical Center For Cancer And Cardiovascular Diseases
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Fujii Makiko
Showa Pharmaceutical Univ.
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Fujii Makiko
Showa College Of Pharmaceutical Sciences
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Yoshida Minako
Showa Pharmaceutical University
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Fujii M
Department Of Pharmaceutics And Biopharmaceutics Showa Pharmaceutical University
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Matsumoto Mitsuharu
Takeda Chemical Industries Ltd. Pharmaceutical Research Division
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BOUNO Masayo
Showa Pharmaceutical University
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FUJITA Sachie
Showa Pharmaceutical University
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MATSUMOTO Mitsuo
Showa Pharmaceutical University
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Fukuoka Masamichi
Department Of Clinical Pharmacology And Toxicology Showa Pharmaceutical University
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Fukuoka Masamichi
Division Of Medical Chemistry National Institute Of Hygienic Sciences
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Watanabe Y
Showa Pharmaceutical Univ.
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Fujii M
Showa Univ. Tokyo Jpn
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Watanabe Yoshiteru
Showa Pharmaceutical Univ.
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Matsumoto Mitsuhiro
First Department Of Internal Medicine Kumamoto University School Of Medicine
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Matsumoto Mitsuo
Department Of Pharmaceutics And Biopharmaceutics Showa Pharmaceutical University
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Matsumoto Mitsuo
Showa College Of Pharmaceutical Sciences
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