HOMEPRODUCTSCOMPANYCONTACTFAQResearchDictionaryPharmaSign Up FREE or Login

Implantable technology for long-term delivery of nalmefene for treatment of alcoholism.

Abstract
Pharmacotherapy treatment for alcoholism is limited by poor compliance, adverse effects, and fluctuating drug levels after bolus administration. A long-term delivery system would improve upon these limitations. The current study describes the characterization of a sustained release implant containing nalmefene, an opioid antagonist, for treatment of alcoholism. Nalmefene was blended with ethylene vinyl acetate (EVA), extruded into 2.8 mm x 27 mm rods, and coated with EVA to optimize release. In vitro release was determined by HPLC, and in vivo release characteristics after subcutaneous implantation into rats were determined by LC-MS/MS analyses. Extrusion produced rods containing 80.09 +/- 6.0 mg nalmefene. In vitro release was high from the uncoated rods, and they were depleted of drug fairly quickly; however EVA coatings maintained release over longer periods. The 25 wt.% coated rods provided in vitro release of 0.36 mg/day/rod, and in vivo release of 0.29 mg/day/rod over 6 months, and showed dose-dependent nalmefene plasma concentrations (one rod: 3.33 +/- 0.56 ng/ml, three rods: 10.19 +/- 2.31 ng/ml). After explantation, nalmefene plasma concentrations were undetectable by 6 h. A sustained release nalmefene rod provides 6 months of drug with no adverse effects.
AuthorsLauren C Costantini, Sofie R Kleppner, Joseph McDonough, Marc R Azar, Raj Patel
JournalInternational journal of pharmaceutics (Int J Pharm) Vol. 283 Issue 1-2 Pg. 35-44 (Sep 28 2004) ISSN: 0378-5173 [Print] Netherlands
PMID15363499 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Delayed-Action Preparations
  • Narcotic Antagonists
  • Naltrexone
  • nalmefene
Topics
  • Alcoholism (drug therapy)
  • Animals
  • Area Under Curve
  • Delayed-Action Preparations
  • Equipment Design
  • Humans
  • Infusion Pumps, Implantable
  • Male
  • Naltrexone (administration & dosage, analogs & derivatives, pharmacokinetics, therapeutic use)
  • Narcotic Antagonists (administration & dosage, pharmacokinetics, therapeutic use)
  • Rats
  • Rats, Wistar
  • Technology, Pharmaceutical

Join CureHunter, for free Research Interface BASIC access!

Take advantage of free CureHunter research engine access to explore the best drug and treatment options for any disease. Find out why thousands of doctors, pharma researchers and patient activists around the world use CureHunter every day.
Realize the full power of the drug-disease research graph!


Choose Username:
Email:
Password:
Verify Password:
Enter Code Shown: