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Home , Aceprometazine, Alimemazine, Antazoline, Astemizole, Azatadine, Bamipine

US 20140094438A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2014/0094438 A1 Mitchell (43) Pub. Date: Apr. 3, 2014

(54) COMPOSITIONS AND METHODS FOR THE A63/37 (2006.01) TREATMENT OF PAN A63L/25 (2006.01) A613 L/4402 (2006.01) (71) Applicant: GM Pharmaceuticals, Inc., Arlington, A613 L/495 (2006.01) TX (US) A63L/09 (2006.01) A63L/045 (2006.01) (72) Inventor: Odes W. Mitchell, Arlington, TX (US) A613 L/60 (2006.01) A 6LX3 L/505 (2006.01) (73) Assignee: GM Pharmaceuticals, Inc., Arlington, TX (US (52) U.S. Cl. (US) CPC ...... A61 K3I/616 (2013.01); A61K3I/60 (2013.01); A61 K3I/522 (2013.01); A61 K (21) Appl. No.: 14/043,722 31/194 (2013.01); A61K 31/137 (2013.01); 1-1. A6 IK3I/505 (2013.01); A61 K3I/4402 (22)22) FileFiled: Oct.Cl. 1, 2013 (2013.01); A61 K3I/495 (2013.01);s A61 K Related U.S. Application Data 3 1/09 (2013.01); A61K3I/045 (2013.01); A6 IK31/125 (2013.01) (60) Provisional application No. 61/708,533, filed on Oct. USPC ...... 514/161; 562/471; 560/193: 514/263.31 1, 2012. (57) ABSTRACT Publication Classification The claimed invention relates to compositions that may be in (51) Int. Cl. a form of a liquid, Solid, gel, cream or gel capsule comprising A6 IK3I/66 (2006.01) an , and methods for administering these composi A6 IK3I/522 (2006.01) tions for treatment of patients suffering from various forms of A6 IK3I/94 (2006.01) pain. US 2014/0094438 A1 Apr. 3, 2014

COMPOSITIONS AND METHODS FOR THE 0009. In another embodiment of the present invention, the TREATMENT OF PAIN compositions may comprise an analgesic/antipyretic from one or more of the group consisting of acetaminophen, CROSS-REFERENCES TO RELATED , , , . APPLICATIONS , , diamorphine (), hydroc odone, , , , nalbu 0001. This Application claims the benefit under 35 U.S.C. phine, , , , , S119(e) of U.S. Provisional Patent Application No. 61/708, , , , , 533 filed Oct. 1, 2012, which is incorporated herein by refer , , , , tetrahydro ence in its entirety as if fully set forth herein. cannabinol, acetylsalicylic acid, salicylate, magne sium salicylate, sodium salicylate, , and FIELD OF THE INVENTION . 0002 The present invention relates to compositions com 0010. In another embodiment of the present invention, the prising an analgesic that may be in the form of a liquid, gel. compositions may comprise an analgesic adjunct from one or cream, or gel capsules, and methods for administering more of the group consisting of S (+)-, metoclopra these compositions for treatment of patients suffering from mide, ciramadol, sulfentanil, and . various forms of pain. (0011. The compositions of the present invention may be administered to the patient for oral use and may be in the form BACKGROUND OF THE INVENTION of an elixir, syrup and/or suspension according to an indi 0003 Pain is an unpleasant sensation with a wide range in vidual patient's preferences. In another embodiment of the severity that can be localized or prevalent throughout the present invention, the compositions may further comprise a body. Pain is affected by nerve stimulation that carries flavorant. impulses to the brain and is a symptom of an underlying 0012. In certain embodiments of the invention, the com disease, disorder, or physical injury. positions of the claimed invention may be administered to the 0004. It is estimated that 100 million Americans currently patient as a tablet, gel, cream or gel capsules. suffer with pain. Clinical complaints due to pain come in 0013. In another embodiment of the present invention, the many varieties. Such complaints may be due to such ailments compositions may be substantially free of other added active as arthritis, back pain, neuropathy, or a headache. ingredients. The other added active ingredient may comprise 0005. A headache, also known as cephalalgia, ranks an , such as one or more of the group consisting amongst the most common clinical pain complaints and can of , hydrochloride, bro be caused from a wide variety of physiological effects. Such mpheneramine, , chloropheniramine, pyril causes range from hormonal changes, muscle tension in the amine maleate, pyrilamine tannate, , back of the neck, or from dehydration. Because headaches , , alimemazine , amoxy come in many forms, they may be treated or prevented by dramine camsilate, chlorhydrate, antazoline mesi various methods. These methods may include maintaining a late, antazoline phosphate, , dimaleate, healthy lifestyle, reducing stress or making use of various hydrochloride, hydrochloride, benac . Such medications can be antianxiety , tyzine hydrochloride, tosilate, hydro or nonsteroidal anti-inflammatories chloride, maleate, dihydrochlo (NSAIDs). However, when these drugs are ineffective or not ride, bufexamac, maleate acid, cetiedil citrate, possible to use due to allergic reactions, other combina dihydrochloride, hydrochloride, tions may be prescribed. maleate, hydrochloride, hydrochloride, , SUMMARY OF THE INVENTION fumarate, hexachlorophenate, clemizole penicil line, clemizole undecylenate, dihydrochloride. 0006 An embodiment of the invention is directed to a , clofenetamine hydrochloride, hydro composition comprising an analgesic/antipyretic compound. chloride, maleate, di (acefylline) In certain embodiments of the invention, the composition diphenhydramine, difencloxazine, dimelazine hydrochlo further comprises an analgesic adjunct or an antihistamine. ride, , hydrochloride, cimeto Embodiments of the invention provide for the composition as tiazine mesilate, diphenhydramine hydrochloride, diphenhy a liquid, solid, gel/cream, tablet or gel capsule. dramine mesilate, hydrochloride, diprocqualone camsilate, , succinate, DETAILED DESCRIPTION OF EXEMPLARY eprozinol dihydrochloride, dimaleate, etyben EMBODIMENTS Zatropine bromhydrate, hydrochloride, 0007. The present invention provides compositions and hydrochloride, hydrochloride, methods of using the compositions for the therapeutic treat hydrochloride, , hydro ment of pain. Specifically, the present invention comprises a chloride, decanoate, flupentixol dihydrochloride, composition of an analgesic/antipyretic either with or without hydrochloride, hydroxyzine dihydrochloride, an analgesic adjunct and either with or without an antihista hydroxyzine embonate, indoramine hydrochloride, mine, where said composition is in the form of a liquid, Solid hydrochloride, ketotifene fumarate, levocabas or gel/cream. tine hydrochloride, , levomepromazine 0008. As used herein, the term “analgesic/antipyretic' hydrochloride, levomepromazine embonate, levomepro refers to a compound or compounds that are effective in mazine maleate, , hydrochloride, treating pain (analgesic) and are also effective at reducing maprotiline mesilate, maprotiline resinate, meclozine hydro fever (antipyretic). chloride, hydrochloride, fuma US 2014/0094438 A1 Apr. 3, 2014

rate, mefenidramium metilsulfate, maleate, those skilled in the art from this detailed description. The meduitazine, , hydrochloride, invention will be further illustrated by the following non hydrochloride, , hydrochlo limiting examples. ride, , hydrochloride, oxaflumazine disuccinate, , benzilate, oxolamine cit WORKING EXAMPLES rate, , oXomemazine hydrochloride, parathiaz ine teoclate, perimetazine, maleate, phenoxy 0022. The products listed below exemplify certain of the benzamine hydrochloride, , products in accordance with the claimed invention. In the phenyltoloxamine citrate, , , piprete products listed below, only the primary active ingredients, col dihydrochloride, pizotifene malate, prednazoline, profe i.e., analgesic/antipyretic, analgesic adjunct or antihistamine namine hydrochloride, , promethazine hydro is listed. It would be apparent to one of ordinary skill in the art chloride, promethazine embonate, promethazine that the listed product formulations could contain inertingre polyvinylbenzene-metacrylate, , , dients such as buffers, fillers and other inactive ingredients. tartrate, hydrochloride, thiazina mium metilsulfate, hydrochloride, tripelen Product 1 namine hydrochloride, hydrochloride, and tyma (0023 Choline Salicylate 870 mg Zoline hydrochloride, and combinations thereof. (0024 Caffeine 65 mg 0014. In another embodiment, the compositions of the present invention may comprise one or more of about 1 mg to Product 2 1500 mg of an analgesic/antipyretic, 1 mg to 200 mg of an analgesic adjunct and 1 mg to 200 mg of an antihistamine. In (0025 Choline Salicylate 870 mg certain embodiments of the invention, the compositions may 0026 Diphenhydramine Citrate 76 mg comprise from about 435 mg to 1.338 mg of an analgesic/ antipyretic. Product 3 0.015. In certain embodiments of the invention, the anal (0027 Choline Salicylate 870 mg gesic adjunct is caffeine. In certain embodiments of the inven tion, the antihistamine is diphenhydramine citrate. In other Product 4 embodiments of the invention, the antihistamine is either diphenhydramine hydrochloride or Pyrliamine Maleate. 0028 Acetylsalicylic acid 845 mg 0016. In another embodiment of the present invention, the (0029 Caffeine 65 mg compositions may be administered to a patient to treat and/or alleviate the occurrence or negative effects from one or more Product 5 of the group consisting of chronic pain and acute pain. 0030 Acetylsalicylic acid 1000 mg 0017. In certain embodiments of the invention, the com 0031 Caffeine 65 mg positions of the invention are dissolved in Solvents containing one or more buffering salts. Examples of these buffers Product 6 include, but are not limited to, calcium carbonate, magnesium oxide, magnesium carbonate, aluminum hydroxide and 0032. Choline Salicylate 1,338 mg sodium hydroxide. The use of one or more of these salts 0033 Caffeine 65 mg causes the analgesic/antipyretic, analgesic adjunct and anti compounds to stay in Solution. Product 7 0018. In other embodiments of the invention, the compo 0034 Choline Salicylate 870 mg sitions of the invention comprise simethicone. Simethicone is 0035 Diphenhydramine HCl 76 mg an orally administered anti-foaming agent used to reduce bloating, discomfort or pain caused by excessive gas. Product 8 0019. In certain embodiments of the invention, the com positions of the invention comprise a diuretic agent. In some 0036 Choline Salicylate 1,338 mg embodiments of the invention, the diuretic agent is pam 0037 Diphenhydramine HCl 50 mg abrom, which is a 1:1 mixture of 2-amino-2-methyl-1-pro panol and 8-bromotheophyllinate. Product 9 0020. In another embodiment of the present invention, the 0038 Choline Salicyate 1,338 mg compositions may be administered to a patient to treat and/or alleviate the occurrence or negative effects of headaches. 0039. Diphenhydramine Citrate 76 mg Compositions of the invention are formulated as a liquid in order to facilitate efficient absorption particularly by older Product 10 individuals. 0040 Choline Salicylate 1,338 mg 0021. Other objectives, features and advantages of the present invention will become apparent from the following Product 11 specific examples. The specific examples, while indicating specific embodiments of the invention, are provided by way 0041 Choline Salicylate 870 mg of illustration only. Accordingly, the present invention also 0042 Chlophedianol HCl 25 mg includes those various changes and modifications within the 0043. Thonzylamine HCl 100 mg/or Pyrilamine Maleate spirit and scope of the invention that may become apparent to 50 mg/or Chlorcyclizine HCl 18.75 mg US 2014/0094438 A1 Apr. 3, 2014

Product 12 Product 23 0044) Choline Salicylate 1,338 mg (0077 Choline Salicylate 435-1338 mg 0045 HC160 mg 0078 Acetaminophen 250 mg 0046 Pyrilamine Maleate 50 mg (0079 Caffeine 60 mg 0047 Chlophendianol 25 mg 0080 Pyrilamine Maleate 15 mg Product 13 Product 24 0048 Choline Salicylate 870 mg I0081. Choline Salicylate 435 mg to 1,338 mg 0049 HCl 10 mg I0082 Acetaminophen 1 mg to 1,000 mg 0050 400 mg I0083 Caffeine 65 mg Product 14 Product 25 (Cream/Rub) I0084 Choline Salicylate 435 mg to 1,338 mg 0051 Choline Salicylate 870 mg I0085 10% by weight 0052 Phenylephrine HCl 10 mg I0086 30% by weight 0053 Thonzylamine HCl 100 mg I0087 4% by weight Product 15 Product 26 (Liquid) 0054 Choline Salicylate 870 mg 0088 Acetaminophen 1 mg to 1000 mg 0055 Caffeine 65 mg 0089 Caffeine 32 mg to 200 mg 0056 Pyrilamine Maleate 15 mg Product 27 (Cream/Rub) Product 16 (0090 Choline Salicylate 435 mg to 1,338 mg (0091 Trolamine Salicylate 10% by weight 0057 Choline Salicylate 870 mg 0092. While specific embodiments of the present inven 0058 Pamabrom 25 mg tion have been described, other and further modifications and changes may be made without departing from the spirit of the Product 17 invention. All further and other modifications and changes are 0059 Choline Salicylate 870 mg included that come within the scope of the invention as set forth in the claims. The disclosures of all publications cited 0060 Pamabrom 25 mg above are expressly incorporated by reference in their entire 0061 Pyrilamine Maleate 15 mg ties to the same extent as if each were incorporated by refer Product 18 ence individually. What is claimed is: 0062. Choline Salicylate 870 mg 1. A composition comprising an analgesic/antipyretic 0063 250 mg compound. 0064 Pamabrom 25 mg 2. The composition of claim 1, wherein said analgesic/ antipyretic is selected from one or more of the group consist Product 19 ing of acetaminophen, buprenorphine, butorphanol, codeine, dextropropoxyphene, dihydrocodeine, fentanyl, diamor 0065 Choline Salicylate 870 mg phine, , hydromorphone, ketobemidone, mor 0066 Magnesium Salicylate 250 mg phine, , oxycodone, oxymorphone. pentazocine, 0067 Caffeine 65 mg pethidine, tramadol, acetylsalicylic acid, diflunisal ethenza mide, aminophenaZone, metamizole, phenaZone, phenacetin, Product 20 Ziconotide, , acetylsalicylic acid, cho line salicylate, magnesium salicylate, Sodium salicylate, ibu 0068 Choline Salicylate 435-1338 mg profen, naproxen and ketoprofen. 0069. Acetaminophen 250 mg 3. The composition of claim 1 further comprising an anal gesic adjunct. Product 21 4. The composition of claim 3, wherein said analgesic 0070 Choline Salicylate 435-1338 mg adjunct is selected from one or more of the group consisting 0071 Acetaminophen 250 mg of S (+)-ketamine, , ciramadol, , 0072 Diphenhydramine Citrate (76 mg) or Diphenhy caffeine and remifentanil. dramine hydrochloride (50 mg) 5. The composition of claim 1 further comprising an anti histamine. Product 22 6. The composition of claim 5, wherein said antihistamine is selected from the group consisting of diphenhydramine, 0073 Choline Salicylate 435-1338 mg cyproheptadine hydrochloride, brompheneramine, hydrox 0074 Acetaminophen 250 mg yZine, chloropheniramine, pyrilamine maleate, pyrilamine 0075 Pyrilamine Maleate 15 mg tannate, acepromazine, aceprometazine, alimemazine, alime 0076 Diphenhydramine Citrate (76 mg) or Diphenhy mazine tartrate, amoxydramine camsilate, antazoline chlo dramine hydrochloride (50 mg) rhydrate, antazoline mesilate, antazoline phosphate, astemi US 2014/0094438 A1 Apr. 3, 2014

Zole, azatadine dimaleate, azelastine hydrochloride, mepyramine maleate, meduitazine, methaqualone, methdila bamipine hydrochloride, hydrochloride, brety zine hydrochloride, metixene hydrochloride, mizolastine, lium tosilate, bromazine hydrochloride, brompheniramine moxisylyte hydrochloride, niaprazine, orphenadrine hydro maleate, buclizine dihydrochloride, bufexamac, carbinoxam chloride, oxaflumazine disuccinate, oxatomide, oxolamine ine maleate acid, cetiedil citrate, cetirizine dihydrochloride, benzilate, oxolamine citrate, oXomemazine, oXomemazine chlorcyclizine hydrochloride, chlorphenamine maleate, chlo hydrochloride, parathiazine teoclate, perimetazine, phe rphenoxamine hydrochloride, chlorprothixene hydrochlo niramine maleate, hydrochloride, phe ride, cinnarizine, clemastine fumarate, clemizole hexachlo nyltoloxamine, phenyltoloxamine citrate, pimethixene, pipo rophenate, clemizole penicilline, clemizole undecylenate, tiazine, pipretecol dihydrochloride, pizotifene malate, clocinizine dihydrochloride, clo?edanol, clofenetamine prednazoline, hydrochloride, promethazine, hydrochloride, cyclizine hydrochloride, dexchlorphe promethazine hydrochloride, promethazine embonate, niramine maleate, di (acefylline) diphenhydramine, difen promethazine polyvinylbenzene-metacrylate, propiomazine, cloxazine, dimelazine hydrochloride, dimenhydrinate, terfenadine, thenalidine tartrate, thenyldiamine hydrochlo dimethoxanate hydrochloride, cimetotiazine mesilate, ride, thiazinamium metilsulfate, thonzylamine hydrochlo diphenhydramine hydrochloride, diphenhydramine mesilate, ride, hydrochloride, triprolidine hydrochlo diphenylpyraline hydrochloride, diprocqualone camsilate, ride, and hydrochloride, and combinations dixyrazine, doxylamine Succinate, eproZinol dihydrochlo thereof. ride, etodroxizine dimaleate, etybenzatropine bromhydrate, 7. The composition of claim 1, wherein said composition etybenzatropine hydrochloride, etymemazine hydrochloride, comprises one or buffers selected from the group consisting fenethazine hydrochloride, fenoxazoline hydrochloride, fen of calcium carbonate, magnesium oxide and magnesium car pentadiol, flunarizine hydrochloride, flupentiXol decanoate, bonate. flupentixol dihydrochloride, histapyrrodine hydrochloride, 8. The composition of claim 1, wherein said composition is hydroxyzine dihydrochloride, hydroxyzine embonate, administrable to aid patient orally. indoramine hydrochloride, isothipendyl hydrochloride, keto tifene fumarate, hydrochloride, levomepro 9. The composition of claim 1, wherein said composition mazine, levomepromazine hydrochloride, levomepromazine comprises one or more of the group consisting of elixir, syrup embonate, levomepromazine maleate, loratadine, mapro and Suspension. tiline hydrochloride, maprotiline mesilate, maprotiline 10. The composition of claim 1, wherein said composition resinate, meclozine hydrochloride, mecysteine hydrochlo further comprises a flavorant. ride, medifoxamine fumarate, mefenidramium metilsulfate, k k k k k