Article ID Journal Published Year Pages File Type
5809827 European Journal of Pharmaceutical Sciences 2015 5 Pages PDF
Abstract

Propiverine is a widely used antimuscarinic drug with bioavailability that is limited by intestinal first-pass extraction. To study the apparent heterogeneity in intestinal first-pass extraction, we performed a population analysis of oral concentration-time data measured after administration of an extended-release formulation of propiverine in ten healthy subjects. Using an inverse Gaussian function as input model, the assumption that the systemically available fraction increases as a sigmoidal function of time considerably improved the fit. The step-like increase in this fraction at time t = 3.7 h predicted by the model suggests that propiverine is predominantly absorbed in colon. A nearly perfect correlation was found between the estimates of bioavailability and mean dissolution time.

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Related Topics
Health Sciences Pharmacology, Toxicology and Pharmaceutical Science Drug Discovery
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