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(12) United States Patent (10) Patent No.: US 8,124,126 B2 Bosse Et Al

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(12) United States Patent (10) Patent No.: US 8,124,126 B2 Bosse Et Al USOO81241.26B2 (12) United States Patent (10) Patent No.: US 8,124,126 B2 BOSse et al. (45) Date of Patent: Feb. 28, 2012 (54) PHARMACEUTICAL COMPOSITIONS (58) Field of Classification Search ........................ None See application file for complete search history. (75) Inventors: Paul Bosse, Charleston, SC (US); John Ameling, Cincinnati, OH (US); Bernard (56) References Cited Schachtel, Jupiter, FL (US); Ray Takigiku, Loveland, OH (US) U.S. PATENT DOCUMENTS 4,113,866 A 9, 1978 Lednicer et al. (73) Assignee: Charleston Laboratories, Inc., (Continued) Charleston, SC (US) FOREIGN PATENT DOCUMENTS (*) Notice: Subject to any disclaimer, the term of this CA 2665841 10/2007 patent is extended or adjusted under 35 U.S.C. 154(b) by 0 days. (Continued) (21) Appl. No.: 12/351,704 OTHER PUBLICATIONS Alexander, etal. Comparison ofondansetron and droperidol in reduc (22) Filed: Jan. 9, 2009 ing postoperative nausea and vomiting associated with patient-con trolled analgesia. Anaesthesia. Dec. 1995:50(12): 1086-8. (65) Prior Publication Data (Continued) US 2009/O175939 A1 Jul. 9, 2009 Primary Examiner — Susan Tran Related U.S. Application Data (74) Attorney, Agent, or Firm — Wilson Sonsini Goodrich & (60) Provisional application No. 61/020,139, filed on Jan. Rosati 9, 2008, provisional application No. 61/043,037, filed on Apr. 7, 2008, provisional application No. (57) ABSTRACT 61/060,758, filed on Jun. 11, 2008. Methods and compositions are provided which comprise effective amounts of analgesic to treat a subject, including (51) Int. Cl. reducing or eliminating an adverse effect associated with the A6 IK9/20 (2006.01) analgesic. A6 IK9/24 (2006.01) (52) U.S. Cl. ........................................ 424/472: 424/464 24 Claims, 5 Drawing Sheets US 8,124,126 B2 Page 2 U.S. PATENT DOCUMENTS Hardy, et al. A double-blind, randomised, parallel group, multina 5,055.461 A 10, 1991 Kelleher et al. tional, multicentre study comparing a single dose of ondansetron 24 5,266,331 A 11/1993 Oshlack et al. mg p.o. with placebo and metoclopramide 10 mg t.d.s. p.o. in the 5,445,829 A 8, 1995 Paradissis et al. treatment of opioid-induced nausea and emesis in cancer patients. 5,478,577 A 12/1995 Sackler et al. Support Care Cancer. Apr. 2002; 10(3):231-6. 5,508,042 A 4, 1996 OShlack et al. International search report dated May 22, 2009 for Application No. 5,549,912 A 8, 1996 OShlack et al. US2009,30662. 5,656.295 A 8, 1997 OShlack et al. 5,738,874 A 4, 1998 Conte et al. International search report dated Sep. 23, 2008 for Application No. 5,827,852 A 10, 1998 Russell et al. US2007/8O831. 5,840,731 A * 1 1/1998 Mayer et al. .................. 514,289 Kovac, A. Prophylaxis of postoperative nausea and vomiting: con 5,863,922 A 1/1999 Mayer et al. troversies in the use of serotonin 5-hydroxytryptamine Subtype 3 5,866,161 A 2f1999 Childers et al. receptor antagonists. J Clin Anesth. Jun. 2006:18(4):304-18. 5,968,551 A 10, 1999 Oshlack et al. Paoloni, et al. Low incidence of nausea and vomiting with intrave 6, 160,020 A 12/2000 Ohannesian et al. 6,287,600 B1 9, 2001 Ouali et al. nous opiate analgesia in the ED. Am J Emerg Med. Nov. 6,335,033 B2 1/2002 Oshlack et al. 2002:20(7):604-8. 6,491.945 B1 12/2002 Childers et al. Foster, et al. Complicated pain management in a CYP450 2D6 poor 6,572,885 B2 6, 2003 Oshlack et al. metabolizer. Pain Pract. Dec. 2007;7(4):352-6. 6,699,502 B1 3/2004 Fanara et al. Promethazine HCI and Hydrocodone Bitartrate Syrup. WraSer Phar 6,733,783 B2 5, 2004 OShlack et al. maceuticals, Madison, MS. Jan. 2007. 6,773,783 B2 8, 2004 Saito et al. Ragg, et al. Comparison of the efficacy of paracetamol versus 7,029,698 B2 4/2006 Waranis et al. RE39,221 E 8, 2006 Raffa et al. paracetamol, codeine and promethazine (Painstop) for premedica 7,214.385 B2 5, 2007 Gruber tion and analgesia for myringotomy in children. Anaesth Intensive 2004.?0047907 A1 3, 2004 OShlack et al. Care. Feb. 1997:25(1):29-32. 2004/0170680 A1 9, 2004 OShlack et al. Richmond, B. S. Pharmacy & Therapeutics Committees. Antiemetic 2004/O185096 A1 9, 2004 OShlack et al. Prophylaxis and Treatment of Postoperative and Opioid-Induced 2004/0266807 A1 12/2004 O'Shlack et al. Nausea and Vomiting. Jul. 2007. 2005/OO74493 A1 4/2005 Mehta et al. Vinson, D.R. Treatment patterns of isolated benign headache in US 2005/0106249 A1 5/2005 Hwang et al. 2005/O158382 A1* 7/2005 Cruz et al. .................... 424/468 emergency departments. Ann Emerg Med. Mar. 2002;39(3):215-22. 2005, 0163856 A1 7/2005 Maloney et al. (Abstract). 2005/0232986 A1 10, 2005 Brown et al. Bosse, P. U.S. Appl. No. 12/444,521, entitled “Pharmaceutical Com 2005/0232987 A1 10, 2005 Srinivasan et al. positions', filed Apr. 6, 2009. 2005/0232993 A1* 10, 2005 Brown et al. ................. 424/468 Charleston Laboratories' Investigational New Drug Application, pp. 2005/0266.032 A1 12/2005 Srinivasan et al. 2005/027281.0 A1 12, 2005 Davis et al. 93-94, filed with the U.S. Food and Drug Administration on Sep. 5, 2005/0281875 A1 12/2005 Srinivasan et al. 2008. Charleston Laboratories is the assignee of the present applica 2006, OO29664 A1 2, 2006 Srinivasan et al. tion. 2006, OO57205 A1 3/2006 Srinivasan et al. Mayo Clinic Website. Cough and Cold Combination (Oral Route). 2006/0134207 A1 6/2006 Srinivasan et al. Available at www.mayoclinic.com/health/drug-infomation? 2006/0204578 A1 9/2006 Vergez et al. DR602361. Accessed Oct. 2, 2007. 2007, OOO3622 A1 1/2007 Srinivasan et al. European search opinion dated Dec. 1, 2009 for Application No. 2007/0148097 A1* 6/2007 Finn et al. .................... 424,102 O7871139.7. 2008/0044482 A1 2/2008 Oshlack et al. 2008, OO74208 A1 3/2008 Lee U.S. Appl. No. 12/967,423, filed Dec. 14, 2010, Bosse et al. 2008.0075781 A1 3/2008 Oshlack et al. U.S. Appl. No. 60/948,375, filed Jul. 6, 2007, Bosse et al. 2008. O181941 A1 7/2008 Oshlack et al. U.S. Appl. No. 61/020,139, filed Jan. 9, 2008, Bosse et al. 2009 OO68269 A1 3/2009 OShlack et al. U.S. Appl. No. 61/043,037, filed Apr. 7, 2008, Bosse et al. 2010.0143469 A1* 6/2010 Bosse ........................... 424,472 U.S. Appl. No. 61/060,758, filed Jun. 11, 2008, Bosse et al. U.S. Appl. No. 61/223,999, filed Jul. 8, 2009, Bosse et al. FOREIGN PATENT DOCUMENTS U.S. Appl. No. 61/224,424, filed Jul. 9, 2009, Bosse et al. DE 102005O13726 A1 9, 2006 International preliminary report on patentability dated Jul. 22, 2010 HK 101.054519 10/2007 JP 2009-531645 10/2007 for PCT Application No. US09/30662. JP 2010-542386 1, 2009 International search report dated Sep. 1, 2010 for PCT Application WO WO 2006,103418 A1 10, 2006 No. US2010,41433. WO WO 2008/027350 A2 3, 2008 Davis. Hydrocodone. Opioids for cancer pain. Oxford UK: Oxford WO WO 2008/027350 A3 5, 2008 University Press. 2005. pp. 59-68. ISBN 0-19-852943-0. WO WO 2008/070268 A2 6, 2008 Strenkoski-Nix, et al. Pharmacokinetics of promethazine hydrochlo WO WO 2008/074419 A1 6, 2008 WO WO 2008/070268 A3 11/2008 ride after administration of rectal Suppositories and oral syrup to WO WO 2009/0894.94 A2 T 2009 healthy subjects. Am J Health Syst Pharm. Aug. 15, WO WO 2009/0894.94 A3 1, 2010 2000:57(16): 1499-505. WO WO 2011/006O12 A1 1, 2011 Wikipedia. Acetaminophen. en.wikipedia.org/wiki/Acetaminophen (last visited, Aug. 30, 2011). OTHER PUBLICATIONS Wikipedia. Hydrocodone. en.wikipedia.org/wiki/Hydrocodone (last visited, Aug. 30, 2011). European serach report dated Dec. 1, 2009 for Application No. O7871139.7. * cited by examiner U.S. Patent Feb. 28, 2012 Sheet 1 of 5 US 8,124,126 B2 OH eUZeuleUOJ si eleulue).9 euopooOupAH i s s O Lo CN O d CN O ueudoujueleoW O d O LO O s s WUU U.S. Patent Feb. 28, 2012 Sheet 2 of 5 US 8,124,126 B2 A. RO. 1150R2.92. t 0.3043 (7.73) 0.33988.63) —D RO,8134 (R20.66 0.67951726) y 0.00600.15 BLENED LAND y RO.1330R3.38 R0.6590 R16.74) 0.04101.04 CUP DEPTH 0.2867.26 APPROX. FIG. 2 U.S. Patent Feb. 28, 2012 Sheet 3 of 5 US 8,124,126 B2 Standard Blank O5O 100 150 2.00 250 3.00 3.50 4.OO 450 5.OO 5.5O 6.00 Minutes FIG. 3 U.S. Patent Feb. 28, 2012 Sheet 4 of 5 US 8,124,126 B2 Acetaminophen Promethazine Hydrocodone O5O 100 1.50 2.00 250 3.00 3.50 4.OO 450 5.OO 5.50 6.00 Minutes FIG. 4 U.S. Patent Feb. 28, 2012 Sheet 5 of 5 US 8,124,126 B2 8 g CD O - C a O Cs r 9, it as if 8 CD as cy N. O. O. E CD Y- as 5 O SE d. 9 U. 9 £5 9,O 9 H CC O S o 9 O O O O O O O O O. O. O. 3 o CO N.
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