In-vitro and in-vivo characterization of a buprenorphine delivery system

The Journal of Pharmacy and Pharmacology
Sofie R KleppnerLauren C Costantini

Abstract

Buprenorphine is a mu-opioid receptor partial agonist with enhanced safety and comparable efficacy to methadone for treatment of opioid dependence. The sublingual formulation of buprenorphine, approved for treatment of opioid dependence, produces variable buprenorphine blood levels and requires frequent dosing that limits patient compliance. To achieve stable buprenorphine levels that may improve patient outcome, an implantable sustained buprenorphine delivery system was developed. Each implant consists of ethylene vinyl acetate copolymer and 90 mg buprenorphine HCl, and measures 26 mm in length and 2.4 mm in diameter. Steady-state release in-vitro was 0.5 mg/implant/day. In-vivo pharmacokinetics and safety were examined for up to 52 weeks in beagle dogs receiving 8, 16 or 24 subcutaneous implants. Plasma buprenorphine concentrations correlated with the number of implants administered. Peak buprenorphine concentrations were generally reached within 24 h after implantation. Steady-state plasma levels were attained between 3 and 8 weeks, and were maintained for study duration, with a calculated mean release rate of 0.14+/-0.04 mg/implant/day. There were no test-article-related adverse effects. This delivery system can provide lon...Continue Reading

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Citations

Oct 20, 2010·International Journal of Molecular Sciences·Heidi M MansourPatrick P Deluca
Jan 25, 2014·Journal of Pharmacy & Bioallied Sciences·Michael GuarnieriBarry Kobrin
Jul 14, 2009·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Jhi-Joung WangJia-You Fang
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Feb 12, 2021·Journal of Biomaterials Science. Polymer Edition·Ziqiang ZhangWenbing Qi
Apr 26, 2021·Advanced Drug Delivery Reviews·Jiawei WangMohammed Maniruzzaman

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