DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO
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SUBOXONE (buprenorphine and naloxone) sublingual film is an orange film, imprinted with a logo identifying the product and strength in white ink. It contains buprenorphine HCl, a mu-opioid receptor partial agonist and a kappa-opioid receptor antagonist, and naloxone HCl dihydrate, an opioid receptor antagonist, at a ratio of 4:1 (ratio of free bases). It is intended for sublingual administration and is available in four dosage strengths, 2 mg buprenorphine with 0.5 mg naloxone, 4 mg buprenorphine with 1 mg naloxone, 8 mg buprenorphine with 2 mg naloxone, and 12 mg buprenorphine with 3 mg naloxone . Each sublingual film also contains polyethylene oxide, hydroxypropyl methylcellulose, maltitol, acesulfame potassium, lime flavor, citric acid, sodium citrate, FD&C yellow #6, and white ink.
Chemically, buprenorphine HCl is (2S)-2-[17-Cyclopropylmethyl-4,5α-epoxy-3-hydroxy-6-methoxy-6α,14-ethano14α-morphinan-7α-yl]-3,3-dimethylbutan-2-ol hydrochloride. It has the following chemical structure:
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Buprenorphine HCl has the molecular formula C29H41NO4 • HCl and the molecular weight is 504.10. It is a white or off-white crystalline powder, sparingly soluble in water, freely soluble in methanol, soluble in alcohol, and practically insoluble in cyclohexane.
Chemically, naloxone HCl dihydrate is 17-Allyl-4,5 α -epoxy-3, 14-dihydroxymorphinan-6-one hydrochloride dihydrate. It has the following chemical structure:
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Naloxone hydrochloride dihydrate has the molecular formula C19H21NO4 • HCl • 2H 20 and the molecular weight is 399.87. It is a white to slightly off-white powder and is freely soluble in water, soluble in alcohol, and practically insoluble in toluene and ether.
Feb. 25, 2013 — The United States Food and Drug Administration (FDA) has approved generic versions of Reckitt Benckiser Healthcare’s Suboxone sublingual tablets. Buprenorphine HCl and Naloxone HCl Dihydrate SL Tablets, 2 mg/0.5 mg and 8 mg/2 mg will be produced by two U.S. based generic manufacturers – Actavis, Inc. and Amneal Pharmaceuticals, LLC.
Suboxone is indicated for maintenance treatment of opioid dependence.
For the 12 months ending December 31, 2012, Suboxone® tablets had total U.S. sales of approximately $625 million, according to IMS Health data. The generic equivalents are expected to save millions in healthcare costs.
buprenorphine
Chemical Name: (2S)-2-[(-)-(5R,6R,7R,14S)-9α-cyclopropylmethyl-4,5-epoxy-6,14-ethano-3-hydroxy-6-methoxymorphinan-7-yl]-3,3-dimethylbutan-2-ol
Uses: Pain, Opiate/Opioid Abuse Treatment
Routes: Sublingual
Half-Life (H½): 37 Hours
Bioavailability: ~50-60% (Sublingual Tablet)
Protein Binding: 96%
Potency: 30-50x (Oral Morphine)
New Drug Approvals 