Relative oral bioavailability of morphine and naltrexone derived from crushed morphine sulfate and naltrexone hydrochloride extended-release capsules versus intact product and versus naltrexone solution: a single-dose, randomized-sequence, open-label, three-way crossover trial in healthy volunteers

Clinical Therapeutics
Franklin K JohnsonJoe Stauffer

Abstract

Morphine sulfate/sequestered naltrexone hydrochloride (HCl) (MS-sNT) extended-release fixed-dose combination capsules, approved by the US Food and Drug Administration (FDA) in August 2009 for chronic moderate to severe pain, contain extended-release morphine pellets with a sequestered core of the opioid antagonist naltrexone. MS-sNT was designed so that if the product is tampered with by crushing, the naltrexone becomes bioavailable to mitigate morphine-induced subjective effects, rendering the product less attractive for tampering. The primary aim of this study was to compare the oral bioavailability of naltrexone and its metabolite 6-beta-naltrexol, derived from crushed pellets from MS-sNT capsules, to naltrexone solution. This study also assessed the relative bioavailability of morphine from crushed pellets from MS-sNT capsules and that from the whole, intact product. This single-dose, randomized-sequence, open-label, 3-period, 3-treatment crossover trial was conducted in healthy volunteers. Adults admitted to the study center underwent a 10-hour overnight fast before study drug administration. Each subject received all 3 of the following treatments, 1 per session, separated by a 14-day washout: tampered pellets (crushed for...Continue Reading

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Mar 25, 2014·Journal of Analytical Toxicology·Janet C LiuBrookie M Best
Oct 26, 2012·Postgraduate Medicine·Marco Pappagallo, Marta Sokolowska
May 10, 2012·Expert Opinion on Drug Metabolism & Toxicology·Yin Cheong WongZhong Zuo
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Jan 10, 2017·Expert Opinion on Pharmacotherapy·Kammy Ks Poon, Steven Hs Wong
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Oct 18, 2012·Journal of Medical Toxicology : Official Journal of the American College of Medical Toxicology·Tammi Schaeffer
Apr 27, 2016·Expert Opinion on Pharmacotherapy·Ann C Childress

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