Model Analyses of Interfacial Transfer and Absorption Behaviors of Drugs following Dissolution : Approach to Evaluation Procedure of Bioavailability

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  • 薬物の溶解を伴う界面移行および吸収挙動のモデル解析 : バイオアベイラビリティ評価手法へのアプローチ
  • ヤクブツ ノ ヨウカイ オ トモナウ カイメン イコウ オヨビ キュウシュウ

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Description

To examine interfacial transfer and absorption behaviors of drugs with the dissolution from compressed tablet, two reliable methods were preliminarily developed. One of the methods (S-Lw-Lo system) was constructed based upon an interfacial transfer of the drug from aqueous phase (Lw) to organic phase (Lo) with the dissolution in Lw. Another method (S-Lw-in situ system) was constructed based upon perfusing the drug solution in rat intestinal tract in situ with the dissolution of the drug in a reservior (Lw). The experiments were carried out by using benzoic acids and barbiturates as test compounds to survey the validity and reproducibility of the methods. The drug appearance in organic phase of S-Lw-Lo system (Co) was well correlated with the drug disappearance in the reservior of S-Lw-in situ system, following the first order kinetics. The Co value was found to be simply estimated from solubility and partition coefficient of drug. The results indicated that the methods developed here can afford a quantitative evaluation of drug absorption behavior with high precision and may extend to evaluation procedure of bioavailability.

Journal

  • YAKUGAKU ZASSHI

    YAKUGAKU ZASSHI 100 (11), 1087-1096, 1980

    The Pharmaceutical Society of Japan

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