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(12) Patent Application Publication (10) Pub. No.: US 2012/0201888 A1 Bosse Et Al

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(12) Patent Application Publication (10) Pub. No.: US 2012/0201888 A1 Bosse Et Al US 201202O1888A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2012/0201888 A1 BOSse et al. (43) Pub. Date: Aug. 9, 2012 (54) PHARMACEUTICAL COMPOSITIONS Publication Classification (51) Int. Cl. (75) Inventors: Paul Bosse, Charleston, SC (US); A6II 3/545 (2006.01) John Ameling, Cincinnati, OH A63L/454 (2006.01) (US); Bernard Schachtel, Jupiter, A63/495 (2006.01) FL (US); Ray Takigiku, Loveland, A6II 3/538 (2006.01) A 6LX 3/557 (2006.01) OH (US) A 6LX 3/553 (2006.01) A 6LX 3/573 (2006.01) (73) Assignee: CHARLESTON A6IR 9/24 (2006.01) LABORATORIES, INC., A6IP 25/04 (2006.01) Charleston, SC (US) A6IP 25/06 (2006.01) A6IP 7/02 (2006.01) (21) Appl. No.: 13/347,552 A6IP 25/08 (2006.01) A6IP 29/00 (2006.01) A6IP 9/00 (2006.01) (22) Filed: Jan. 10, 2012 A6IR 9/00 (2006.01) A 6LX 3/5.377 (2006.01) Related U.S. Application Data (52) U.S. Cl. ................... 424/472: 514/226.2: 514/230.8; (63) Continuation of application No. 12/351,704, filed on 514/323: 514/225.8: 514/255.04: 514/230.5; Jan. 9, 2009, now Pat. No. 8,124,126. 514/225.5; 514/220; 514/221; 514/171; 424/400 (57) ABSTRACT (60) Provisional application No. 61/020,139, filed on Jan. Methods and compositions are provided which comprise 9, 2008, provisional application No. 61/043,037, filed effective amounts of analgesic to treat a Subject, including on Apr. 7, 2008, provisional application No. 61/060, reducing or eliminating an adverse effect associated with the 758, filed on Jun. 11, 2008. analgesic. Patent Application Publication Aug. 9, 2012 Sheet 1 of 5 US 2012/02O1888A1 OH euZeuleUOJ si eleulue).9 euopooOupAH . s s s. s ueudoujueleoW- 1 s i s WUU Patent Application Publication Aug. 9, 2012 Sheet 2 of 5 US 2012/02O1888A1 A. RO.1150R2.92) 0.3043 (7.73) 0.33988.63 -> RO,8134 (R20.66) 0.679517.26 y 0.0060 (0.15 BLENED LAND y RO. 1330R3.38) RO,6590 R16.74) 0.04101.04) CUP DEPTH 0.2867.26 APPROX. FIG 2 Patent Application Publication Aug. 9, 2012 Sheet 3 of 5 US 2012/02O1888A1 Standard Blank 0.50 100 150 2.00 2.50 3.00 3.50 4.00 450 5.00 5.50 6.00 Minutes FIG. 3 Patent Application Publication Aug. 9, 2012 Sheet 4 of 5 US 2012/02O1888A1 Acetaminophen Promethazine Hydrocodone 0.50 100 1.50 2.00 2.50 3.00 3.50 4.00 450 5.00 5.50 6.00 Minutes FIG. 4 Patent Application Publication Aug. 9, 2012 Sheet 5 of 5 US 2012/02O1888A1 CD 9 2- 5 9, it era. ifgld itd cD 8S l) N O E CD Yale as as d SE a U. 9 Ss, 3 HE <C e 3 uOnOSSO 9% US 2012/020 1888 A1 Aug. 9, 2012 PHARMACEUTICAL COMPOSITIONS blocker, serotonin receptor agonist, vasoconstrictor, anti platelet agent, anti-convulsant, triptan, ergot, or calcitonin CROSS-REFERENCE gene-related peptide receptor antagonist; and (2) a pharma 0001. This application claims the benefit of U.S. Provi ceutically acceptable carrier or vehicle. sional Application Nos. 61/020,139, filed Jan. 9, 2008, 0013. In another embodiment this invention provides 61/043,037, filed Apr. 7, 2008, and 61/060,758, filed Jun. 11, compositions comprising (1) an effective amount of (a) an 2008, each of which is incorporated by reference herein in its opioid analgesic agent and (b) Sumatriptan or a pharmaceu entirety. tically acceptable salt thereof, and (2) a pharmaceutically acceptable carrier or vehicle. BACKGROUND OF THE INVENTION 0014. In another embodiment this invention provides compositions consisting of (1) an effective amount of (a) 0002 Available pain medications may have adverse Sumatriptan or a pharmaceutically acceptable salt thereof and effects, such as nausea, vomiting, and skin rashes and seda (b) promethazine or a pharmaceutically acceptable salt tion. As a result of Such adverse effects, many subjects are thereof, and (2) a pharmaceutically acceptable carrier or unable to tolerate recommended dosages needed for effective vehicle. pain relief because of adverse effects. Accordingly, there 0015. In another embodiment this invention provides remains a need for effective therapeutics with reduced compositions comprising (1) an effective amount of (a) an adverse effects. opioid analgesic agent, (b) a CoX-2 inhibitor agent, an anti depressant agent, an anti-convulsant agent, an anti-cholin BRIEF DESCRIPTION OF DRAWINGS ergic agent, an NMDA receptor antagonist agent, an anes 0003 FIG. 1 illustrates a chromatograph for example of a thetic agent or an O-adrenoreceptor agonist agent, (c) an standard solution. opioid antagonist agent, (d) an agent that reduces or elimi 0004 FIG. 2 illustrates one embodiment of a tablet of the nates an adverse effect of the opioid agent; and (2) a pharma invention. A. Illustrates a top view of the tablet (numerals in ceutically acceptable carrier or vehicle. square brackets refer to measurements in millimeters and 0016. In another embodiment this invention provides numerals not in square brackets are in inches); B. illustrates a compositions comprising (1) an effective amount of (a) an side view of the tablet (numerals in square brackets refer to opioid analgesic agent, (b) a non-opioid analgesic agent, (c) measurements in millimeters and numerals not in square cyclazacine or levallorphan; (d) an agent that reduces or brackets are in inches). eliminates an adverse effect of the opioid analgesic agent; and 0005 FIG.3 illustrates an example of chromatograph of a (2) a pharmaceutically acceptable carrier. diluent blank and standard solution. 0017. In another embodiment this invention provides a 0006 FIG. 4 illustrates an example of a dissolution chro composition comprising (1) an effective amount of (a) an matograph for a composition of the invention. opioid analgesic agent, (b) a non-opioid analgesic agent, (c) 0007 FIG. 5 illustrates an example of dissolution release an antiemetic; (d) an abuse deterrent agent; and (2) a phar profile for a composition of the invention. maceutically acceptable carrier. In one embodiment the abuse deterrentagent is niacin or a pharmaceutically acceptable salt SUMMARY OF THE INVENTION thereof; zinc sulfate; or sodium lauryl sulfate. 0008. In one embodiment this invention provides compo 0018. In another embodiment this invention provides sitions comprising (1) an effective amount of: (a) an opioid compositions comprising (1) an effective amount of (a) an analgesic; (b) a stimulant; (c) an antiemetic; and (2) a phar opioid analgesic agent, (b) a non-opioid analgesic agent, (c) maceutically acceptable carrier or vehicle. an opioid antagonist agent, (d) aprepitant, perphenazine, 0009. In another embodiment this invention provides acetylleucine monoethanolamine, aZasetron, benzquina compositions comprising (1) an effective amount (a) oxyc mide, bietanautine, bromopride, clebopride, diphenidol. odone or a pharmaceutically acceptable salt thereof, (b) methallatal, metopimazine, oxyperndyl, pipamazine, promethazine or a pharmaceutically acceptable salt thereof, Sulpiride, thiethylperazine, thioproperazine, or a pharmaceu (c) modafinil or a pharmaceutically acceptable salt thereof tically acceptable salt thereof, and (2) a pharmaceutically and (d) naltrexone or a pharmaceutically acceptable salt acceptable carrier or vehicle. thereof, and (2) a pharmaceutically acceptable carrier or 0019. In another embodiment this invention provides bi vehicle. layer tablets comprising: (1) a controlled-release layer com 0010. In another embodiment this invention provides prising from about 6.5 mg to about 8.5 mg of hydrocodone or compositions comprising (1) an effective amount of (a) mor a pharmaceutically acceptable salt thereof, and from about phine or a pharmaceutically acceptable salt thereof, (b) 290 to about 360 mg of acetaminophen or a pharmaceutically promethazine or a pharmaceutically acceptable salt thereof, salt; and (2) an immediate-release layer comprising from and (c) modafinil or a pharmaceutically acceptable salt about 11 mg to about 14 mg of promethazine or a pharma thereof, and (2) a pharmaceutically acceptable carrier or ceutically salt thereof. In another embodiment this invention vehicle. provides bilayer tablets comprising (1) an effective amount of 0011. In another embodiment this invention provides (a) an opioid analgesic or a pharmaceutically acceptable salt compositions comprising an effective amount ofbutalbital or thereof and (b) one or more antiemetic or a pharmaceutically a pharmaceutically acceptable salt thereof, acetaminophen acceptable salt thereof, and (2) a pharmaceutically acceptable and promethazine or a pharmaceutically acceptable salt carrier or vehicle. thereof, and a pharmaceutically acceptable carrier or vehicle. 0020. In another embodiment this invention provides 0012. In another embodiment this invention provides bilayer tablets comprising: (1) a controlled release layer com compositions comprising (1) an effective amount of (a) an prising (a) from about 6.5 mg to about 8.5 mg of hydrocodone opioid analgesic agent; (b) an anti-emetic agent and (c) a beta or a pharmaceutically acceptable salt thereof, (b) from about US 2012/020 1888 A1 Aug. 9, 2012 290 to about 360 mg of acetaminophen or a pharmaceutically of (a) an opioid analgesic agent; and (b) an antiemetic agent. acceptable salt thereof, (c) from about 135 mg to about 170 In one embodiment the photophobia is associated with mg of silicified microcrystalline cellulose, (d) from about 17 migraine headache. mg to about 23 mg of hydroxy methyl propyl cellulose, (e) 0029. In another embodiment this invention provides from about 1 mg to about 4 mg of magnesium Stearate, and (f) methods for treating or preventing headache comprising: from about 1 mg to about 4 mg of Stearic acid; and (2) an administering to a subject in need thereof (1) an effective immediate release layer comprising (a) from about 11 mg to amount of (a) triptan or a pharmaceutically acceptable salt about 14 mg of promethazine or a pharmaceutically accept thereof and (b) promethazine or a pharmaceutically accept able salt thereof, (b) from about 100 mg to about 140 mg of able salt thereof, and (2) a pharmaceutically acceptable car silicified microcrystalline cellulose, (c) from about 12 mg to rier or vehicle.
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