Characterising Drug Release from Immediate-Release Formulations of a Poorly Soluble Compound, Basmisanil, Through Absorption Modelling and Dissolution Testing
作者: Cordula StillhartNeil J. ParrottMarc LindenbergPascal ChalusDarren BentleyAnikó Szepes
作者单位: 1F. Hoffmann-La Roche Ltd.
刊名: The AAPS Journal, 2017, Vol.19 (3), pp.827-836
来源数据库: Springer Journal
DOI: 10.1208/s12248-017-0060-1
关键词: Absorption modellingGastroPlusImmediate-release formulationIn vitro - in vivo correlationPoorly water-soluble compound
英文摘要: The study aimed to characterise the mechanism of release and absorption of Basmisanil, a biopharmaceutics classification system (BCS) class 2 compound, from immediate-release formulations via mechanistic absorption modelling, dissolution testing, and Raman imaging. An oral absorption model was developed in GastroPlus® and verified with single-dose pharmacokinetic data in humans. The properties and drug release behaviour of different oral Basmisanil formulations were characterised via biorelevant dissolution and Raman imaging studies. Finally, an in vitro - in vivo correlation (IVIVC) model was developed using conventional and mechanistic deconvolution methods for comparison. The GastroPlus model accurately simulated oral Basmisanil exposure from tablets and granules formulations...
原始语种摘要: The study aimed to characterise the mechanism of release and absorption of Basmisanil, a biopharmaceutics classification system (BCS) class 2 compound, from immediate-release formulations via mechanistic absorption modelling, dissolution testing, and Raman imaging. An oral absorption model was developed in GastroPlus® and verified with single-dose pharmacokinetic data in humans. The properties and drug release behaviour of different oral Basmisanil formulations were characterised via biorelevant dissolution and Raman imaging studies. Finally, an in vitro - in vivo correlation (IVIVC) model was developed using conventional and mechanistic deconvolution methods for comparison. The GastroPlus model accurately simulated oral Basmisanil exposure from tablets and granules formulations...
全文获取路径: Springer  (合作)
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影响因子:4.386 (2012)

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关键词翻译
关键词翻译
  • model 模型
  • absorption 吸收
  • Release 免除释放机构
  • dissolution 溶解
  • different 不相同的
  • release 释放
  • formulation 配方
  • tablet 药片
  • properties 道具
  • Testing 检测