Physical and Chemical Changes of Medicinals in Mixtures with Adsorbents in the Solid State. II. : Application of Reduced Pressure Treatment for the Improvement of Dissolution of Flufenamic Acid

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概要

• 論文の詳細を見る

• Flufenamic acid (FFA) was mixed with magnesium aluminum silicate (MAS) and stored at 60℃ at a reduced pressure of about 2.5 mmHg. After storage, when its concentration was not more than 20%, FFA was observed by X-ray diffraction and polarizing microscopy to be amorphous. The dissolution of FFA was thus enhanced in comparison with that of a freshly prepared mixture. Furthermore, the dissolution curves showed a typical supersaturation pattern, and the supersaturation state continued longer, the higher the pH value of the dissolution medium. Flufenamic acid, in a mixture with MAS, became amorphous more rapidly at reduced pressure than at atmospheric pressure, and therefore the effect improved dissolution appeared earlier at reduced pressure. Infrared spectral studies suggested that FFA, after storage at a reduced pressure with MAS, was dispersed monomolecularly in an ionic form. The technique of treating crystalline medicinals, that have poor solubility in water, with adsorbent at reduced pressure may be useful for improving their dissolution characteristics.

• 社団法人日本薬学会の論文
• 1989-09-25

著者

• 今野 勉

  Developmental Research Laboratories Daiichi Pharmaceutical Co. Ltd.

• 今野 勉

  Exploratory Research Laboratories III, Research Institute, Daiichi Pharmaceutical Co., Ltd.,

• 絹野 浩二

  Pharmaceutical Formulation Research Center

• 絹野 浩二

  Pharmaceutical Formulation Research Center:research Institute Daiichi Seiyaku Co. Ltd.

• Konno T

  Drug Metabolism & Physicochemical Property Research Laboratory Daiichi Pharmaceutical Co. Ltd.

関連論文

• Effects of Grinding on the Physical and Chemical Properties of Crystalline Medicinals with Microcrystalline Cellulose V : Comparison with Tri-O-methyl-β-cyclodextrin Ground Mixtures
• Effects of Grinding on the Physical and Chemical Properties of Crystalline Medicinals with Microcrystalline Cellulose. IV. Comparison of the IR Spectra of Medicinals in the Solid State and in Solution
• Effects of Grinding on Physical and Chemical Properties of Crystalline Medicinals with Microcrystalline Cellulose. III. Infrared Spectra of Medicinals in Ground Mixtures
• Preliminary Preformulation Studies of a 2-(3,4-Dimethoxyphenyl)ethylamine Derivative for Oral Administration at an Exploratory Stage of New Drug Development
• Physical and Chemical Changes of Medicinals in Mixtures with Adsorbents in the Solid State. IV. : Study on Reduced-Pressure Mixing for Practical Use of Amorphous Mixtures of Flufenamic Acid
• Physical and Chemical Changes of Medicinals in Mixtures with Adsorbents in the Solid State. III. : Determination of Vapor Pressure of Solid Drugs by Steam Distillation
• Physical and Chemical Changes of Medicinals in Mixtures with Adsorbents in the Solid State. II. : Application of Reduced Pressure Treatment for the Improvement of Dissolution of Flufenamic Acid
• Physical and Chemical Changes of Medicinals in Mixtures with Adsorbents in the Solid State. I. : Effect of Vapor Pressure of the Medicinals on Changes in Crystalline Properties
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