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Comparative Oral Drug Classification Systems: Acetazolamide, Azithromycin, Clopidogrel, and Efavirenz Case Studies
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2018-06-21 00:00:00 , DOI: 10.1021/acs.molpharmaceut.8b00274 Maria Julia Mora 1 , Renée Onnainty 1 , Gladys Ester Granero 1
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2018-06-21 00:00:00 , DOI: 10.1021/acs.molpharmaceut.8b00274 Maria Julia Mora 1 , Renée Onnainty 1 , Gladys Ester Granero 1
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Biopharmaceutics classification systems based on the properties of solubility and permeability or the extension of metabolism are very important tools in the early stages of the development and regulatory stages of new products. However, until now, there was no clear understanding between the interplay among these classification systems. Therefore, the main objective of this work was to make a comparison of concepts of BCS and BDDCS to understand what are the key factors that allow for the integration of these biopharmaceutics classification systems. Also, the suitability of an in situ single-pass intestinal perfusion assay in rats (SPIP) development was assessed by us to determine the limit between high and low permeability following what the FDA BCS guidance suggests. An excellent correlation was found between the values of permeability obtained by applying SPIP assays and the extensions of the metabolism of the set of compounds studied in this work, with the exception of three compounds that showed disparity between their permeability coefficients (Peff), obtained herein by SPIP, and their metabolism (acetazolamide, azithromycin, and efavirenz). Discrepancies allowed us to elucidate the interrelationship between BCS and BDDCS.
中文翻译：
比较口服药物分类系统：乙酰唑胺，阿奇霉素，氯吡格雷和依非韦伦案例研究
在新产品开发和监管阶段的早期，基于溶解度和渗透性或代谢扩展的生物制药分类系统是非常重要的工具。但是，到目前为止，在这些分类系统之间的相互作用之间还没有明确的了解。因此，这项工作的主要目的是对BCS和BDDCS的概念进行比较，以了解哪些因素可以整合这些生物制药分类系统。此外，我们根据FDA BCS指南的建议，评估了大鼠原位单次肠道灌注试验（SPIP）发育的适用性，以确定高通透性和低通透性之间的界限。P EFF），由本文SPIP获得的，并且它们的代谢（乙酰唑胺，阿奇霉素，和依法韦仑）。差异使我们能够阐明BCS和BDDCS之间的相互关系。
更新日期：2018-06-21
中文翻译：
比较口服药物分类系统：乙酰唑胺，阿奇霉素，氯吡格雷和依非韦伦案例研究
在新产品开发和监管阶段的早期，基于溶解度和渗透性或代谢扩展的生物制药分类系统是非常重要的工具。但是，到目前为止，在这些分类系统之间的相互作用之间还没有明确的了解。因此，这项工作的主要目的是对BCS和BDDCS的概念进行比较，以了解哪些因素可以整合这些生物制药分类系统。此外，我们根据FDA BCS指南的建议，评估了大鼠原位单次肠道灌注试验（SPIP）发育的适用性，以确定高通透性和低通透性之间的界限。P EFF），由本文SPIP获得的，并且它们的代谢（乙酰唑胺，阿奇霉素，和依法韦仑）。差异使我们能够阐明BCS和BDDCS之间的相互关系。
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