Application of Tumbling Melt Granulation (TMG) Method for Controlled Enteric-Release Beads by Coating Mixture of Hydrogenated Castoer Oil and Higher Fatty Acid

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概要

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• Controlled-release beads which can release drugs faster in the higher pH regions (pH 5-7.5) than in the acidic region (pH 1-5) were prepared using the newly developed tumbling melt granulation (TMG) method, in which process a powdered meltable material was coated onto the core beads without use of any organic solvent. This function could be obtained by using a mixture of hydrogenated castor oil (HCO) and higher fatty acids as coating materials. Controlled-release beads containing various kinds of drugs were prepared. Use of stearic acid as a fatty acid resulted in excellent coating producibilities when the mixing ratio of stearic acid (X_<FA>) was less than 30%. The dissolution rates determined in purified water, 1st fluid, and 2nd fluid tended to increase with the increase of X_<FA>. This tendency was especially remarkable in the 2nd fluid. The effect of the carbon number (12-22) of the fatty acid was then determined. The permeability coefficient, P, calculated from the dissolution rate, decreased with the increase of carbon number. This seemed to be due to the difference of the release rate of fatty acid from the coating layer composed of HCO and fatty acid. Determination of the dependency of P value on the pH of the dissolution medium showed that the P values changed little in the acidic region (pH 1.2 to 5.0), but increased exponentially with an increase of pH over pH 5.5. Logarithm of relative P values (P_<pH>/P_w : P_w means the P values in purified water) plotted against pH were distributed on the same line irrespective of fatty acid. An empirical equation which predicts the dissolution rates in the enteric medium was proposed using this relationship.

• 公益社団法人日本薬学会の論文
• 1997-08-15

著者

• KOBAYASHI MASAO

  Pharmaceutics Division Department, Product & Technology Development Laboratory, Tanabe Seiyaku Co.,

• Kobayashi M

  Fujisawa Pharmaceutical Co. Ltd. :(peresent Address)fujisawa Research Insitute Of America Inc. North

• Osawa T

  Laboratory Of Food And Biodynamics Nagoya University Graduate School Of Bioagricultural Sciences

• Osawa T

  Pharmaceutical Research Laboratory Tanabe Seiyaku Co. Ltd.

• Osawa Takashi

  Pharmaceutics Research Laboratory Tanabe Seiyaku Co. Ltd.

• Kobayashi M

  Faculty Of Pharmaceutical Sciences Osaka University

• Kobayashi Masao

  Pharmaceutical Research Laboratory Tanabe Seiyaku Co. Ltd.

• MAEJIMA Toru

  Pharmaceutics Research Laboratory, Tanabe Seiyaku Co., Ltd.

• 小林 資正

  Graduate School Of Pharmaceutical Sciences Osaka University

• Maejima T

  Pharmaceutical Research Laboratory Tanabe Seiyaku Co. Ltd.

• Maejima Toru

  Pharmaceutics Research Laboratory Tanabe Seiyaku Co. Ltd.

• Osawa Takashi

  Pharmaceutics Department Cmc Research Laboratory Tanabe Seiyaku Co Ltd

• NAKAJIMA Kingo

  Pharmaceutics Research Laboratory, Tanabe Seiyaku Co., Ltd.,

• Nakajima K

  Sankyo Co. Ltd. Tokyo Jpn

• Nakajima Kingo

  Pharmaceutical Research Laboratory, Tanabe Seiyaku Co., Ltd.,

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