首页|口服药物吸收分数的评价及影响因素综述

口服药物吸收分数的评价及影响因素综述

扫码查看
吸收分数(fraction absorbed,Fa)是一个描述口服药物吸收高低的重要参数,是制剂处方工艺开发和优化的重要依据,由于容易与绝对生物利用度概念混淆而未得到工业界的足够重视。影响Fa的因素非常多且复杂,直接影响Fa大小的是三个时间因素:制剂完全释放所需时间、药物完全吸收所需时间以及胃肠道停留时间,这三个时间因素的彼此关系决定了 Fa的大小。通常大家更关心的是影响Fa大小的表观因素,包括自变量和协变量。自变量因素如给药剂量、途径、剂型等,协变量又分成内因和外因,外因包括食物因素、药物相互作用等;内因包括年龄、性别、疾病等。本文分析并系统梳理了自变量和协变量如何通过影响机体生理和内环境,直接或间接地影响三个时间因素,进而改变Fa这样一个复杂过程。了解该理论框架可以更好地优化自变量,以减少协变量对Fa的影响。另外本文还介绍了预测和评估Fa的最新进展,包括复杂溶出装置进展和软件预测的现状。
Review of evaluation and influencing factors of oral drug absorption fraction
Fraction absorbed(Fa)is an important parameter to describe the absorption level of oral drugs,and an important basis for the development and optimization of the formulation process.Because it is easily confused with the concept of absolute bioavailability,it has not received enough attention from the industry.There are many complex factors affecting Fa.There are three time-related factors that directly affect the extent of Fa:the release time,the absorption time,and the residence time.The relationship between these three time-related factors determines the extent of Fa.Generally,we are more concerned about the apparent factors that affect the extent of Fa,including independent variables and covariates;The independent variables include administered dose,route,dosage form,etc.The covariates are divided into internal and external factors,and external factors include food factors,drug interactions,etc.Internal causes include age,sex,disease,etc.This paper analyzes and systematically combs how independent variables and covariates directly or indirectly affect the three time-related factors by affecting the body's physiology and internal environment,thus changing the complex process of Fa.Understanding this theoretical framework can better optimize the independent variables to reduce the impact of covariates on Fa.In addition,this paper also introduces the latest progress of prediction and evaluation of Fa,including the progress of complex dissolution device and the status of software prediction.

fraction absorbedtime-related factorapparent factor

张萍、毕福林、杨劲

展开 >

中国药科大学药学院药理系,江苏南京 210009

吸收分数 时间因素 表观因素

2024

药学学报
中国药学会 中国医学科学院药物研究所

药学学报

CSTPCD北大核心
影响因子:1.274
ISSN:0513-4870
年,卷(期):2024.59(1)
  • 94