Solid dispersions of opioid antagonists

Details Solid dispersions of opioid antagonists Solid dispersions of opioid antagonists

2011-03-29

2011-03-29

Foley, Shanon A (Department: 1619)

Drug, bio-affecting and body treating compositions

Solid synthetic organic polymer as designated organic active...

Aftertreated polymer

C424S423000, C525S438000

Reexamination Certificate

active

07914776

ABSTRACT:
Solid dispersions of stable, amorphous opioid antagonists, particularly [[2(S)-[[4(R)-(3-hydroxyphenyl)-3(R),4-dimethyl-piperidinyl]methyl]-1-oxo-3-phenylpropyl]amino]acetic acid, with improved water solubility and bioavailability are disclosed. Also disclosed are methods of preventing or treating a side effect associated with an opioid. In addition, methods of treating or preventing pain, ileus, and opioid bowel dysfunction are disclosed.

REFERENCES:
patent: 4115400 (1978-09-01), Zimmerman
patent: 4581456 (1986-04-01), Barnett
patent: 4891379 (1990-01-01), Zimmerman et al.
patent: 5136040 (1992-08-01), Werner
patent: 5159081 (1992-10-01), Cantrell et al.
patent: 5250542 (1993-10-01), Cantrell et al.
patent: 5270328 (1993-12-01), Cantrell et al.
patent: 5434171 (1995-07-01), Frank et al.
patent: 6451806 (2002-09-01), Farrar
patent: 6469030 (2002-10-01), Farrar et al.
patent: 7276252 (2007-10-01), Payumo et al.
patent: 2001/0036951 (2001-11-01), Farrar et al.
patent: 2001/0047005 (2001-11-01), Farrar
patent: 2004/0254208 (2004-12-01), Weber et al.
patent: 2005/0124657 (2005-06-01), Christ et al.
patent: 2006/0258696 (2006-11-01), Moss et al.
patent: 2008/0194611 (2008-08-01), Alverdy et al.
Leuner et al. Improving Drug Solubility for Oral Delivery Using Solid Dispersions. 1999. (submitted in IDS).
Leuner et al. “Improving Drug Solubility for Oral Delivery Using Solid Dispersions” European Journal of Phamaceutics and Biopharmaceutics 50 (2000) pp. 47-60.
Petit et al. “The Amorphous State” Polymorphism: in the Pharmaceutical Industry Edited by Rolf Hilfker Wiley-VCH Verlag GmbH & Co. KGaA (2006) pp. 259-285.
Foss et al. Alvimopan (ENTEREG) A Novel Opioid Antagonist, Achieves Active Systemic Concentrations, Am. Soc. For Clin. Pharma. And Therapeutics (2005) p. 74.
Bhargava, H.N., et al., “Effect of nitric oxide synthase inhibition on tolerance to the analgesic action of D-Pen2, D-Pen5enkephalin and morphine in the mouse,”Neuropeptides, 1996, 30(3), 219-223.
Bilsky, E.J., et al., “Effects of naloxone and D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH2and the protein kinase inhibitors H7 and H8 on acute morphine dependence and antinociceptive tolerance in mice,”J. Pharmacol.&Exp. Ther., 1996, 277(1), 484-490.
Dorland's Illustrated Medical Dictionary, 27thEd., W.B. Saunders Co., 1988, p. 816.
Dorland's Illustrated Medical Dictionary, 27thEd., W.B. Saunders Co., 1988, p. 375.
Dourish, C.T., et al., “Enhancement of morphine analgesia and prevention of morphine tolerance in the rat by the cholecystokinin antagonist L-364, 718,”Eur. J. Pharmacol., 1988, 147, 469-472.
Greene, T.W., et al.,Protective Groups in Organic Synthesis, 2d Ed., Wiley & Sons, 1991, Index, 3 pages.
Livingston, E.H., et al., “Postoperative Ileus,”Digestive Diseases and Sciences, 1990, 35(1), 121-132.
Mao, M.J., et al., “Oral administration of dextromethorphan prevents the development of morphine tolerance and dependence in rats,”Pain, 1996, 67, 361-368.
Nichols, M.L., et al., “Enhancement of the antiallodynic and antinociceptive efficancy of spinal morphine by antisera to dynorphin A (1-13) or MK-801 in a nerve-ligation model of peripheral neuropathy,”Pain, 1997, 69, 317-322.
Orchin, M., et al.,The Vocabulary of Organic Chemistry, John Wiley & Sons, pp. v, 126-127, 1980.
Physicians' Desk Reference, Section 3, Product Category Index, 1999, 16 pages.
Resnick, J., et al., “Delayed gastric emptying and postoperative Ileus after nongastric abdominal surgery: Part II,”Am. J. of Gastroenterology, 1997, 92(6), 934-940.
Resnick, J., et al., “Delayed gastric emptying and postoperative Ileus after nongastric abdominal surgery: Part I,”Am. J. of Gastroenterology, 1997, 751-762.
Werner. J.A., et al., “Synthesis oftrans-3,4-dimethyl-4-(3-hydroxypheny)piperidine opioid antagonists: application of theCis-thermal elimination of carbonates to alkaloid synthesis,”J. of Organic Chemistry, 1996, 61, 587-597.

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