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Complexation of rifaximin to cyclodextrin and thermal and spectroscopic study of formed complex

Grant number: 17/18907-3
Support type:Scholarships abroad - Research Internship - Post-doctor
Effective date (Start): March 01, 2018
Effective date (End): April 30, 2018
Field of knowledge:Health Sciences - Pharmacy - Medicines Analysis and Control
Principal Investigator:Hérida Regina Nunes Salgado
Grantee:Ana Carolina Kogawa
Supervisor abroad: Leena Peltonen
Home Institution: Faculdade de Ciências Farmacêuticas (FCFAR). Universidade Estadual Paulista (UNESP). Campus de Araraquara. Araraquara , SP, Brazil
Local de pesquisa : University of Helsinki, Finland  
Associated to the scholarship:14/22019-8 - Chemical-pharmaceutical analysis of rifaximin in raw material and tablets, short term stability, dissolution and polymorphism studies, BP.PD

Abstract

Rifaximin is an oral antimicrobial, intestine - selective, with low level selection for mutations of resistant bacteria and no systemic with adverse effects compared to placebo. It is used for the treatment of hepatic encephalopathy, travelers' diarrhea, syndrome of irritable bowel, Clostridium difficile, ulcerative colitis and acute diarrhea. Rifaximin has low solubility in water, therefore it requires administration at relatively high doses for the success of the therapeutic effect. The complexation of drugs using cyclodextrins is welcome in this aspect by improving solubility and, consequently, increasing the rate of dissolution of poorly soluble drugs. This fact justifies new research in this area. Thus, this project aims to (i) perform the complexation of rifaximin to different cyclodextrins; (ii) study the inclusion complex formed by thermal and spectroscopic techniques; (iii) evaluate the stability of the formed complex and also (iv) to test the increase of solubility of rifaximin via nanonization by wet milling or precipitation techniques or making amorphous material.