Application of Tumbling Melt Granulation (TMG) Method for Preparing Controlled Release Beads Coated with Hydrogenated Castor Oil

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概要

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• The tumbling melt granulation (TMG) method by a centrifugal fluidizing granulator (CF) without any use of organic solvents was applied as a coating technique for preparing controlled-release spherical beads. The core beads containing four kinds of drugs with different solubilities : nicotinamide (NA), isoniazid (ISA), theophiline (THEO) and salicylic acid (SA), were driven in the CF and were previously heated at 61-63℃ before feeding powdered hydrogenated castor oil (HCO) to the CF. HCO was gradually fed and adhered on the surface of the core beads. At the bed temperature of 61-63℃, about 20% of the HCO was presumed to have melted. After the adherence of HCO, the coated beads were cooled at room temperature and thus the controlled-release beads were obtained. The dissolution rates of these coated beads were determined by use of the JP paddle method. The rates seemed to increase with an increase in the solubility of the drug. To clarify the mechanism of drug transport through the coated layer of HCO, the superposition method was applied for the dissolution profile of the coated beads with various coating levels. Then, in each of ISA, THEO, and SA, the dissolution curves were superposed completely, irrespective of their coating level. Permeability coefficients, P values of each drug calculated for various pH media, were coincident, irrespective of pH. These facts indicated that the limiting factor of the dissolution of HCO coated beads was diffusion, and that the permeability of the coated layer was pH independent. The equilibrium P values decreased with the increase in solubility of the drug. The partition coefficient between the layer surface and inner core medium, activity coefficient, viscosity, diffusion through waxy phase and so on, might be attributed to these phenomena.

• 公益社団法人日本薬学会の論文
• 1997-05-15

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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