Bioavailability evaluation of furosemide complexed with cyclodextrin tablets

• Grant number: 12/13775-8
• Support Opportunities: Scholarships in Brazil - Scientific Initiation
• Start date: September 01, 2012
• End date: January 31, 2014
• Field of knowledge: Health Sciences - Pharmacy - Pharmaceutical Technology
• Principal Investigator: Cristina Helena dos Reis Serra
• Grantee: Caio de Marchi Huerta
• Host Institution: Faculdade de Ciências Farmacêuticas (FCF). Universidade de São Paulo (USP). São Paulo , SP, Brazil

Abstract

The current project for bioavailability evaluation is integrated by project FAPESP (2010/03133-3) and by the PhD project from the student Marina de Freitas Silva (2009/14658-2), both entitled "Bioavailability of furosemide complexed with beta-cyclodextrin: in Vitro - in Vivo Correlation evaluation from Human Volunteers." The study has been approved by the Ethics Committee (CEP) from the Faculty of Pharmaceutical Sciences and University Hospital. The bioavailability studies evaluate the drug present in the body, from a pharmaceutical form administration, as a time function. The in vitro-in vivo correlation refers to the rational relation establishment between biological properties, or derived parameters, produced by a pharmaceutical form and its physicochemical properties or characteristics. The establishment of such data correlation may allow in vivo studies replacement demonstrating the need for bioequivalence studies in vitro, in case of changes in the manufacturing process post-registration. In addition, these studies are used in biowaiver applications, as waived from bioequivalence pharmaceuticals studies. To obtain an adequate in vitro-in vivo correlation, some factors must be considered. Initially, it's important that the limit stage from drug absorption be the dissolution process. In this way, it's possible to expect an in vitro-in vivo correlation for class II drugs from biopharmaceutical classification, and for controlled drug release systems, since, in both cases, the limit stage process from drug absorption is dissolution. (Amidon et al., 1995). Furosemide is a drug whose biopharmaceutical classification is not completely defined, the drug is classified as class II and IV, having problems mainly concerning the permeability parameters determination (WHO, 2006). Based on work from Spricigo and co-workers (2008) is intended to conduct a bioavailability study using matrix tablets containing furosemide and cyclodextrin complexed, as it results were significantly better with respect to physicochemical, solubility, and dissolution properties of furosemide when the drug is complexed with cyclodextrin.(AU)