Pharmacokinetics evaluation of sufentanil-2-hydroxypropyl-beta-cyclodextrin inclusion complex

• Grant number: 09/17715-7
• Support Opportunities: Regular Research Grants
• Start date: August 01, 2010
• End date: January 31, 2013
• Field of knowledge: Biological Sciences - Pharmacology - Clinical Pharmacology
• Principal Investigator: Giovana Tofoli Moniz
• Grantee: Giovana Tofoli Moniz
• Host Institution: Universidade São Francisco (USF). Campus Bragança Paulista. Bragança Paulista , SP, Brazil

Abstract

The therapeutics benefits of some drugs can be limited by physical, chemical and toxic properties and even by the presence of physiologic barriers. In the last decades the development of drug-delivery systems made it possible to manipulate some biopharmaceutical and pharmacological properties of drugs, improving their therapeutic effects (long duration of action associated to low systemic toxicity). Opioids, such as sufentanil, are widely used in clinical medicine for sedation or analgesia. However, these drugs can induce typical opioid side-effects, such as, bradycardia, respiratory depression or excessive sedation, even with the use of small dosages applied by different routes of admistration. Thus, the complexation of sufentanil with 2-hydroxypropyl-beta-cyclodextrin, would be interesting due to its improved complexing ability, water solubility and less toxicity, changing the pharmacological properties of this opioid and being potentially advantageous for the pain relief. The aims of this study are to determine the plasmatic levels with mass espectrometry (LC-MS/MS) and to evaluate the pharmacokinetics induced by sufentanil:2-hydroxypropyl-beta-cyclodextrin inclusion complex in comparison with its aqueous formulation in rats and pigs, looking forward to its clinical use. (AU)