The influence of dissolution conditions on the drug ADME phenomena

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• 作者：Sara Cascone ; Felice De Santis ; Gaetano Lamberti  ; ;   ; ^{glamberti@unisa.it} ; Giuseppe Titomanlio
• 关键词：Dissolution ; Pharmacokinetic modeling ; Enteric coated ; ADME
• 刊名：European Journal of Pharmaceutics and Biopharmaceutics
• 出版年：2011
• 出版时间：October 2011
• 年：2011
• 卷：79
• 期：2
• 页码：382-391
• 全文大小：461 K
• ISSN：S093964111100141X

文摘

In this work, a review of the apparatuses available to mimic what happens to a drug (or to foodstuffs) once ingested is presented. Similarly, a brief review of the models proposed to simulate the fate of a drug administered to a living body is reported. Then, the release kinetics of extended release of diclofenac from a commercial enteric-coated tablet was determined both in a conventional dissolution tester (USP Apparatus 2, Method A) as well as in an apparatus modified to reproduce a given pH evolution, closer to the real one than the one suggested by USP. The two experimental release profiles were reported and discussed; therefore, they were adopted as input functions for a previously proposed pharmacokinetic model. The obtained evolutions with time of plasma concentration were presented and used to assess the effectiveness of the commercial pharmaceutical products. The importance of a correct in vitro simulation for the design of pharmaceutical dosage systems was thus emphasized.