کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2504875 1557472 2009 17 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
An interesting relationship between drug absorption and melting point
موضوعات مرتبط
علوم پزشکی و سلامت داروسازی، سم شناسی و علوم دارویی علوم دارویی
پیش نمایش صفحه اول مقاله
An interesting relationship between drug absorption and melting point
چکیده انگلیسی

The ability to predict the extent of passive intestinal drug absorption is very important for efficient lead candidate selection and development. Physicochemical-based absorption predictive models previously developed use solubility, partition coefficient and pKa as drug input parameters for intestinal absorption. Alternatively, this study looks at the relationship between melting point and passive transport for poorly soluble drugs. It is based entirely on the expression derived from the General Solubility Equation (GSE) that relates melting point to the product of intrinsic solubility and partition coefficient. Given that the melting point of a compound is one of the first and more reliable physical properties measured, it can be advantageously used as a guide in early drug discovery and development.This paper elucidates the interesting relationship between the melting point and dose to the fraction absorbed of poorly soluble drugs, i.e., class II and IV compounds in the Biopharmaceutics Classification System. The newly defined melting point based absorption potential (MPbAP) parameter is successful at distinguishing 90% of the 91 drugs considered being well absorbed (FA > 0.5) or poorly absorbed. In general, lower melting compounds are more likely to be well absorbed than higher melting compounds for any given dose. The fraction absorbed for drugs with high melting temperatures is limited by the dose to a greater degree than it is for low melting compounds.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: International Journal of Pharmaceutics - Volume 373, Issues 1–2, 21 May 2009, Pages 24–40
نویسندگان
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