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(12) United States Patent (10) Patent No.: US 7,700,128 B2 Doken Et Al

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(12) United States Patent (10) Patent No.: US 7,700,128 B2 Doken Et Al US007700128B2 (12) United States Patent (10) Patent No.: US 7,700,128 B2 Doken et al. (45) Date of Patent: Apr. 20, 2010 (54) SOLID PREPARATION COMPRISING AN 5,726,201 A * 3/1998 Fekete et al. ................ 514,471 INSULIN SENSITIZER, AN INSULIN 6,599,529 B1* 7/2003 Skinha et al. .... ... 424/458 SECRETAGOGUE ANDA 2003/0147952 A1* 8, 2003 Lim et al. ................... 424/468 POLYOXYETHYLENE SORBITAN EATTY 2003. O180352 A1 9, 2003 Patel et al. ACD ESTER 2004/O147564 A1 7/2004 Rao et al. 2004/0175421 A1* 9, 2004 Gidwani et al. ............. 424/465 (75) Inventors: Kazuhiro Doken, Osaka (JP); Tetsuya FOREIGN PATENT DOCUMENTS Kawano, Osaka (JP); Hiroyoshi EP O749751 A2 12/1996 Koyama, Osaka (JP): Naoru FR 2758461 7, 1998 Hamaguchi, Osaka (JP) GB 23990 15 9, 2004 JP 58065213 * 4f1983 (73) Assignee: Takeda Pharmaceutical Company WO WO95/12385 5, 1995 Limited, Osaka (JP) WO WO98, 11.884 3, 1998 WO WO 98,31360 7, 1998 (*) Notice: Subject to any disclaimer, the term of this WO WO 98/36755 8, 1998 patent is extended or adjusted under 35 WO WO98,57649 12/1998 U.S.C. 154(b) by 711 days. WO WO99.03476 1, 1999 WO WO99.03477 1, 1999 (21) Appl. No.: 10/544,581 WO WO99.03478 1, 1999 WO WOOO,274O1 5, 2000 WO WOOO.28989 5, 2000 (22) PCT Filed: Oct. 21, 2004 WO WOO1? 41737 A2 6, 2001 WO WOO1, 51463 T 2001 (86). PCT No.: PCT/UP2004/O15958 WO WOO2,04024 1, 2002 WO WO O2/O55009 T 2002 S371 (c)(1), WO WO 03/066028 A1 8, 2003 (2), (4) Date: Apr. 5, 2006 WO WO 2004/OO6921 1, 2004 WO WO 2004/030700 A1 4/2004 (87) PCT Pub. No.: WO2005/041962 WO WO 2004/067001 A1 8, 2004 PCT Pub. Date: May 12, 2005 OTHER PUBLICATIONS Database WPI, Section Ch, Week 199007, Derwent Publications (65) Prior Publication Data Ltd., London, GB; an 1990-048246. US 2006/022387OA1 Oct. 5, 2006 * cited by examiner (30) Foreign Application Priority Data Primary Examiner Robert A Wax Oct. 31, 2003 (JP) ............................. 2003-371 679 Assistant Examiner—Bethany Barham (74) Attorney, Agent, or Firm Foley & Lardner LLP (51) Int. Cl. A6 IK 9/20 (2006.01) (57) ABSTRACT (52) U.S. Cl. ...................................................... 424/465 A solid preparation useful as a diabetes-treating agent or the (58) Field of Classification Search ....................... None like and excellent in the dissolution properties of an insulin See application file for complete search history. sensitizer and an insulin secretagogue, which comprises an (56) References Cited insulin sensitizer, an insulin secretagogue and a polyoxyeth ylene sorbitan fatty acid ester is provided. U.S. PATENT DOCUMENTS 4,620,974 A * 1 1/1986 Hersh et al. ................. 424/453 5 Claims, No Drawings US 7,700,128 B2 1. 2 SOLID PREPARATION COMPRISING AN (5) the Solid preparation according to the above (1), INSULIN SENSITIZER, AN INSULIN wherein the polyoxyethylene sorbitan fatty acid ester is SECRETAGOGUE ANDA Polysorbate 80; POLYOXYETHYLENE SORBITAN EATTY (6) a solid preparation comprising pioglitaZone hydrochlo ACDESTER ride, glimepiride and Polysorbate 80; and the like. This application is the National Phase filing of Interna DETAILED EXPLANATION OF THE tional Patent Application No. PCT/JP2004/015958, filed Oct. INVENTION 21, 2004. 10 An insulin sensitizer used in the present invention means TECHNICAL FIELD any drug that restores the impaired function of an insulin receptor to the original state and thereby improves the insulin The present invention relates to a solid preparation com resistance. Specific examples of the insulin sensitizer include prising an insulin sensitizer, an insulin secretagogue and a pioglitazone, rosiglitazone, reglixane (JTT-501), GI-262570, polyoxyethylene Sorbitan fatty acid ester, useful as a diabetes 15 netoglitazone (MCC-555), balaglitazone (DRF-2593), treating agent. MB-13.1258, 5-(2,4-dioxothiazolidin-5-ylmethyl)-2-meth oxy-N-4-(trifluoromethyl)benzylbenzamide (KRP-297), BACKGROUND ART rivoglitazone (CS-011), FK-614, compounds described in W099/58510 (e.g. (E)-4-4-(5-methyl-2-phenyl-4-oxazolyl The following preparations containing an insulin sensitizer methoxy)benzyloxyimino-4-phenylbutyric acid), tesagli Such as thiazolidinediones and an insulin secretagogue were tazar (AZ-242), ragaglitazar (NN-622), Muraglitazar (BMS reported: 298.585), ONO-5816, LM-4156, MBX-102, LY-519818, 1) a pharmaceutical composition comprising an insulin MX-6054, LY-510929, T-131, THR-0921 and the like. sensitivity enhancer in combination with one or more antidia The insulin sensitizer may be in the form of a salt. Such a betics differing from the enhancer in the action mechanism 25 salt may be a pharmacologically acceptable salt, such as Salts (see EP 749751 A); with inorganic bases, salts with organic bases, salts with 2) a composition comprising synergistic effective amounts inorganic acids, salts with organic acids, and salts with basic ofa Sulfonylurea antidiabetic agent and glitaZone antidiabetic or acidic amino acids. agent (see WO 98/36755); Preferred examples of the salts with inorganic bases 3) a pharmaceutical composition containing an insulin sen 30 include salts with alkali metals such as Sodium and potas sitizer, an insulin secretagogue and a pharmaceutically sium; alkaline earth metals such as calcium and magnesium; acceptable carrier (see WO98757649); and aluminum, ammonium and the like. 4) a pharmaceutical composition containing an insulin sen Preferred examples of the salts with organic bases include sitizer, a Sub-maximal amount of an insulin secretagogue, and salts with trimethylamine, triethylamine, pyridine, picoline, a pharmaceutically acceptable carrier (see WO99/03476). 35 ethanolamine, diethanolamine, triethanolamine, dicyclo It is preferable that in a solid preparation comprising an hexylamine, N,N-dibenzylethylenediamine and the like. insulin sensitizer and an insulin secretagogue, the active Preferred examples of the salts with inorganic acids ingredients are biologically equivalent to those which are include salts with hydrochloric acid, hydrobromic acid, nitric contained in two separate Solid preparations as a single active acid, Sulfuric acid, phosphoric acid and the like. ingredient. 40 Preferred examples of the salts with organic acids include However, the present inventors found a problem in a solid salts with formic acid, acetic acid, trifluoroacetic acid, preparation comprising an insulin sensitizer and an insulin fumaric acid, oxalic acid, tartaric acid, maleic acid, citric secretagogue for the first time, that is, found that said Solid acid, Succinic acid, malic acid, methanesulfonic acid, benze preparation had the undesirable dissolution property of an nesulfonic acid, p-toluenesulfonic acid and the like. insulin secretagogue, that is, the dissolution rate of an insulin 45 Preferred examples of the salts with basic amino acids secretagogue from said solid preparation was slower as com include salts with arginine, lysine, ornithine and the like. pared with that from “a solid preparation containing an insu Preferred examples of the salts with acidic amino acids lin secretagogue as a single active ingredient'. include salts with aspartic acid, glutamic acid and the like. The insulin sensitizer may be anhydrous or hydrous. DISCLOSURE OF INVENTION 50 The insulin sensitizer is preferably pioglitaZone or a salt thereof (preferably, hydrochloride) or rosiglitazone or a salt The present inventors studied intensively in order to solve thereof (preferably, maleate) and more preferably pioglita the above problem. As a result, they found that the dissolution Zone hydrochloride. property of an insulin secretagogue could be improved by The insulin sensitizer used in the present invention may be incorporating a polyoxyethylene Sorbitan fatty acid ester in 55 a mixture of two or more insulin sensitizers at an appropriate the Solid preparation and accordingly completed the present proportion. invention. An insulin secretagogue used in the present invention That is, the present invention provides includes Sulfonylurea agents (e.g. tolbutamide, glibencla (1) a Solid preparation comprising an insulin sensitizer, an mide, gliclazide, chlorpropamide, tolaZamide, acetohexam insulin secretagogue and a polyoxyethylene Sorbitan fatty 60 ide, glyclopyramide, glimepiride, glipizide, glybuzole) and acid ester, non-Sulfonylurea insulin secretagogues (e.g. repaglinide, (2) the Solid preparation according to the above (1), nateglinide, mitiglinide or its calcium salt hydrate). wherein the insulin sensitizer is pioglitaZone hydrochloride; The insulin secretagogue may be in the salt form similar to (3) the Solid preparation according to the above (1), that of the above-mentioned insulin sensitizer and may be wherein the insulin secretagogue is a Sulfonylurea agent; 65 either anhydrous or hydrous. (4) the Solid preparation according to the above (3), The insulin secretagogue is preferably a Sulfonylurea wherein the Sulfonylurea agent is glimepiride; agent, more preferably glimepiride. US 7,700,128 B2 3 4 The insulin secretagogue used in the present invention may Corrigents include ascorbic acid, citric acid, tartaric acid, be a mixture of two or more insulin secretagogues at an malic acid and the like. appropriate proportion. Sweetenings include Aspartame, Acesulfame K, thauma A polyoxyethylene sorbitan fatty acid ester used in the tin, Saccharin Sodium, dipotassium glycyrrhizinate and the present invention includes Polysorbate 20, Polysorbate 40, like. Polysorbate 60, Polysorbate 65, Polysorbate 80 and the like. Flavors include menthol, peppermint oil, lemon oil, Vanil The polyoxyethylene
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