Pharmaceutical products are sometimes the subject of abuse. For example, a particular dose of opioid agonist may be more potent when administered parenterally as compared to the same dose administered orally. Some formulations can be tampered with to provide the opioid agonist contained therein available for illicit use. Controlled release opioid agonist formulation are sometimes crushed by drug abusers to provide the opioid contained therein available for immediate release upon oral or parenteral administration.
Opioid antagonists have been combined with certain opioid agonists to deter the parenteral abuse of the opioid agonists. In the prior art, the combination of immediate release pentazocine and naloxone has been utilized in tablets available in the United States, commercially available as Talwin®Nx from Sanofi-Winthrop. Talwin®Nx contains immediate release pentazocine hydrochloride equivalent to 50 mg base and naloxone hydrochloride equivalent to 0.5 mg base. A fixed combination therapy comprising tilidine (50 mg) and naloxone (4 mg) has been available in Germany for the management of pain since 1978 (Valoron®N, Goedecke). A fixed combination of buprenorphine and naloxone was introduced in 1991 in New Zealand (Temgesic®Nx, Reckitt & Colman) for the treatment of pain.
Purdue Pharma L.P. currently markets sustained-release oxycodone in dosage forms containing 10, 20, 40 and 80 mg oxycodone hydrochloride under the tradename OxyContin.
U.S. Pat. Nos. 5,266,331; 5,508,042; 5,549,912 and 5,656,295 disclose sustained release oxycodone formulations.
U.S. Pat. No. 5,472,943 to Crain, et al. describes methods of enhancing the analgesic potency of bimodally acting opioid agonists by administering the agonist with an opioid antagonist.
U.S. Pat. Nos. 6,277,384; 6,475,494; and 6,375,957 to Kaiko et al.; and U.S. Pat. No. 6,228,863 to Colucci et al. are directed to decreasing the abuse potential associated with opioid analgesic dosage forms.
PCT Publication No. WO 01/58451 entitled “Tamper Resistant Oral Opioid Agonist Formulations,” is directed to decreasing the abuse potential associated with opioid analgesic dosage forms by the inclusion of a sequestered opioid antagonist in an opioid agonist dosage form.
There continues to exist a need in the art for an oral dosage form comprising an opioid agonist which has decreased abuse potential.
All references cited herein, including the foregoing, are hereby incorporated by reference in their entireties.
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USPTO Backgrounds