Drug intestinal permeability evaluation using parallel artificial membrane permeability assay (PAMPA): applications in biopharmaceutical classification

• Grant number: 09/05814-0
• Support Opportunities: Regular Research Grants
• Start date: August 01, 2009
• End date: March 31, 2012
• Field of knowledge: Health Sciences - Pharmacy - Pharmaceutical Technology
• Principal Investigator: Cristina Helena dos Reis Serra
• Grantee: Cristina Helena dos Reis Serra
• Host Institution: Faculdade de Ciências Farmacêuticas (FCF). Universidade de São Paulo (USP). São Paulo , SP, Brazil

Abstract

The Biopharmaceutical Classification, based on permeability and solubility properties of active ingredients has been proposed as a tool for developing new pharmaceutical formulations, with or without new drug molecules, with the objective of assisting in the prediction of its availability in vivo. Accessing permeability is a crucial step in determinig drug's site of administration. Therefore, there is a great need for the implementation of hightroughput and low cost models, which must have a good correlation with the characteristics of permeability and absorption in vivo. Several in vitro models have been described for the studies of permeability, but it lacks for standardization of protocols and many of the available literature on these important properties are not reliable or conclusive. The model of parallel artificial membrane (PAMPA) recently described is fast, simple and has shown excellent correlation with models using animal excised intestine or cell monolayers, besides being a method more economically feasible than the other. As the study of permeability is a crucial step in determining the route of administration of a drug and currently no studies using PAMPA has been published in Brazil, different variations of PAMPA will be experimentally evaluated in this study, using samples of anti - retroviral drugs, to thus develop a protocol for optimal prediction of permeability characteristics of these compounds. (AU)