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一种用于确定口服药物吸收不良原因的综合模型。

An integrated model for determining causes of poor oral drug absorption.

作者信息

Yu L X

机构信息

Glaxo Wellcome, Inc., Research Triangle Park, North Carolina 27709, USA.

出版信息

Pharm Res. 1999 Dec;16(12):1883-7. doi: 10.1023/a:1018911728161.

Abstract

PURPOSE

To develop an integrated absorption model for estimating the fraction of dose absorbed and determining the causes of poor oral drug absorption.

METHODS

Both analytical and numerical methods were used to estimate the fraction of dose absorbed.

RESULTS

An integrated absorption model was developed by considering transit flow, dissolution, and permeation processes, simultaneously. A framework was proposed to determine permeability-, dissolution-, and solubility-limited absorption. Digoxin, griseofulvin, and panadiplon were employed to illustrate the applications of the integrated model in identifying the causes of poor absorption and guiding formulation development.

CONCLUSIONS

The integrated absorption model was successfully applied to digoxin, griseofulvin, and panadiplon to estimate the fraction dose absorbed and to roughly determine the causes of poor oral drug absorption.

摘要

目的

开发一种综合吸收模型,用于估算吸收剂量分数并确定口服药物吸收不良的原因。

方法

采用分析方法和数值方法估算吸收剂量分数。

结果

通过同时考虑转运流、溶解和渗透过程,开发了一种综合吸收模型。提出了一个框架来确定通透性、溶解性和溶解度限制的吸收。使用地高辛、灰黄霉素和泛地昔布来说明综合模型在识别吸收不良原因和指导制剂开发方面的应用。

结论

综合吸收模型成功应用于地高辛、灰黄霉素和泛地昔布,以估算吸收剂量分数并大致确定口服药物吸收不良的原因。

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