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(12) United States Patent (10) Patent No.: US 6,676,933 B2 Vergez Et Al

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(12) United States Patent (10) Patent No.: US 6,676,933 B2 Vergez Et Al USOO6676933B2 (12) United States Patent (10) Patent No.: US 6,676,933 B2 Vergez et al. (45) Date of Patent: Jan. 13, 2004 (54) PHARMACEUTICAL COMPOSITION Drug Launches: Product information, Nov. 1995, Pulsar CONTAINING MOSAPRIDE AND Enzimatico.* PANCREATIN Drug Launches: Product information, Jun. 1994, Sedolax (75) Inventors: Juan A. Vergez, Buenos Aires (AR); Enzematico.* Marcelo A. Ricci, Buenos Aires (AR); Marketletter: Highlights of Astra's Pipeline Presentation; Joaquina Faour, Buenos Aires (AR) Newsletter Jan. 1998. (73) Assignee: Osmotica Corp., Tortola (VG) Venturini, J., Ensayo Abierto con la ASOciacion Simeticona, Pancreatina, Acido Tioctico y Acidos Biliares, Prensa Med. (*) Notice: Subject to any disclaimer, the term of this Argent, 1996, 83 (5): 483-485. (and verified translation patent is extended or adjusted under 35 thereof). U.S.C. 154(b) by 66 days. MakSoud, F. et al., Simethicone Use in Antacid Medications, Manuf. Chem. Aerosol News, 1976, 47 (5): 35–36. (21) Appl. No.: 09/864,767 Auld, J. M., Use of Simethicone/Enzyme Agent in Relief of (22) Filed: May 23, 2001 Gastrointestinal Gas, Curr. Ther. Res., 1979, 26 (1): 55–61. (65) Prior Publication Data Suramo, I., et al., The Effect of Drugs, Position of the Patient and Filling of the Stomach on Pancreatic Sonography, Ann. US 2003/0007962 A1 Jan. 9, 2003 Clin. Res. Suppl., 1984, 16 (40): 62-64. (51) Int. Cl." ........................ A61K 31/74; A61K 38/54; A61K 38/43 * cited by examiner (52) U.S. Cl. ................................ 424/78.01; 424/94.21; 424/94.1 Primary Examiner-Christopher R. Tate (58) Field of Search ............................. 424/78.01, 94.1, ASSistant Examiner Patricia Patten 424/94.21; 514/2 (74) Attorney, Agent, or Firm-Rick Matos; Innovar, (56) References Cited L.L.C. FOREIGN PATENT DOCUMENTS (57) ABSTRACT WO WO95/O1803 1/1995 A pharmaceutical composition contains mosapride, pancre atin and optionally Simethicone and is used for treating, OTHER PUBLICATIONS preventing or alleviating the Symptoms of a gastrointestinal Drug Launches: Product information, Aug. 1999, Zypanar disorder. The pharmaceutical composition is provided in an Enzymatico.* oral dosage form for administration to a Subject. Drug Launches: Product information, Dec. 1996, Gasrimet Enzimat.* 8 Claims, No Drawings US 6,676,933 B2 1 2 PHARMACEUTICAL COMPOSITION desoxycholic acid, dehydrocholic acid and Simethicone, CONTAINING MOSAPRIDE AND among other things. The tablet was administered twice daily PANCREATIN to patients over a period of fourteen days. The tablet was reportedly effective at reducing the gastrointestinal discom fort associated with excessive gas. FIELD OF THE INVENTION Mosapride citrate (mosapride; (+/-)-4-amino-5-chloro-2- This invention concerns a pharmaceutical composition ethoxy-N-(4-(4-fluorobenzyl)-2-morpholinyl)methyl comprising moSapride and pancreatin for the treatment of benzamide citrate; AS-4370; CAS 112885-42-4) is a gastrointestinal discomfort. More particularly, the invention benzamide-type gastroprokinetic agent that enhances the pertains to an immediate release Solid oral dosage form gastro inte Stinal motility by Stimulating the comprising moSapride, pancreatin and optionally Simethi 5-hydroxytryptamine-4 (5-HT4) receptor. Mosapride citrate cone and to the use of this dosage form for the treatment or is clinically prescribed as a racemate and is metabolized to prevention of a gastrointestinal disorder or the Symptoms its des-4-fluorobenzyl structure (M1). The metabolites M1 asSociated therewith. and M2 of moSapride citrate are generally less efficacious BACKGROUND OF THE INVENTION 15 than moSapride. R. T. Sims et al (International Publication No. WO Simethicone is used for the relief of discomfort or painful 95/01803) disclose pharmaceutical compositions compris Symptoms caused by the presence of excessive gas in the ing an H2 antagonist, Such as famotidine, a gastrointestinal gastrointestinal tract. It is typically recommended for coad motility agent, Such as cisapride, and optionally Simethicone ministration with an antacid medication, where gas forma for the treatment, prevention, or treatment and relief of tion is a problem in effective therapy. Simethicone is avail various mild to moderate Symptoms associated with gas able in dosage forms including a capsule, Suspension, tablet trointestinal disorders including indigestion, Sour Stomach, or chewable tablet. Commercial products containing Sim overindulgence, heartburn, gastroesophageal reflux, ethicone include Phazyme TM, Extra Strength Maalox Anti constipation, dyspepsia, other gastrointestinal disorders and GasTM, FlatulexTM, Gas-XTM, Genasyme TM, Maximum 25 optionally flatulence. Strength Mylanta Gas ReliefTM, My Baby Gas Relief Thus, the prior art does not disclose a pharmaceutical DropsTM, MyliconTM Drops, OvolTM, and others. Phazyme TM composition comprising moSapride, pancreatin and option is a combination dosage form containing Simethicone and pancreatin. The dose of Simethicone required to provide a ally Simethicone for the treatment, prevention, or treatment relief from gastrointestinal pain will vary according to and relief of various mild to moderate Symptoms associated weight and age of a Subject receiving the medication. The with gastrointestinal disorders. conventional dose for adults and teenagers for the tablet or SUMMARY OF THE INVENTION capsule ranges from about 60 to 125 mg four times daily The present invention seeks to overcome at least Some of after meals and at bedtime. The conventional dose for adults the disadvantages present in the known compositions and to and teenagers for the chewable tablet ranges from about 40 35 provide a pharmaceutical composition for the treatment of, to 125 mg four times daily after meals and at bedtime or the prevention of, or treatment and relief of various mild to dose may be 150 mg three times daily after meals. Generally, moderate Symptoms associated with gastrointestinal disor the dose should not exceed 500 mg daily. A tablet containing ders including indigestion, Sour Stomach, overindulgence, Simethicone, pancreatin, pepsin and belladonna is known. heartburn, gastroesophageal reflux, constipation, dyspepsia, Pancreatin is an enzymatic preparation made from the other gastrointestinal disorders and optionally flatulence. pancreatic enzymes of animals. Pancreatin tablets are pre 40 The pharmaceutical composition comprises mosapride, pan Scribed for patients who are unable to digest food properly creatin and optionally Simethicone or dimethicone. The because of an insufficient amount of natural pancreatic pharmaceutical composition can be provided in an oral excretions. Commercially available products include Sol dosage form as disclosed herein. The dosage form can be an garTM pancreatin tablets, Twinlab'TM pancreatin tablets and 45 immediate release dosage form. The dosage form provides a others. These tablets generally contain other enzymes Such concurrent, Sequential, or combination thereof release of the as amylase, protease and lipase as well as a mixture of two and optionally three active agents. pharmaceutical excipients. The present invention provides a multi-action approach to S. A. Said et al. (Manuf. Chem. Aerosol News (1976), the treatment of gastrointestinal disorders in that a gas 47(5), 35-36) disclose an immediate release coated tablet 50 trointestinal motility agent Such as mosapride offers comprising a core containing Simethicone, pepsin, pancre enhanced motility while pancreatin promotes effective atin and belladonna and a coating Surrounding the core and digestion and Simethicone reduces gastrointestinal gas. The containing pepsin. This tablet is reportedly effective in combination simultaneously treats, relieves and/or prevents reducing gastrointestinal gas. Symptoms associated with excess of gastric acid Secretion in J. M. Auld (Curr. Ther. Res. (1979), 26(1), 55–61) dis 55 the esophagus. Prokinetic agents generally prevent the reflux closes an immediate release tablet comprising Simethicone of gastric acid from the Stomach to the esophagus. Condi and pancreatin. The tablet was administered four times daily tions or Symptoms relieved by the promotion of gastric to a group of patients over a 2-week period and was emptying include but are not limited to gastric Stasis, reportedly effective at reducing the discomfort and painful flatulence, dyspepsia, peptic ulcer and reflux esophagitis. Symptoms associated with excessive gastrointestinal gas. 60 The present invention therefore provides an effective I. Suramo et al. (Ann. Clin. Res., Suppl. (1984), 16(40), multi-component treatment of gastrointestinal disorders 62-64) disclose an immediate release tablet comprising using the combination of pancreatin with the gastrointestinal Simethicone and pancreatin. Two tablets were administered motility agent mosapride, and optionally with Simethicone four times daily to fifty patients. The tablet was reportedly or dimethicone. The claimed combination is particularly effective at reducing the amount of gastrointestinal gas. 65 useful for treating gastrointestinal distress. J. Venturini (Prensa Med. Argent. (1996),83(5), 483-485) One aspect of the invention provides a pharmaceutical discloses an immediate release tablet containing pancreatin, composition or dosage form consisting essentially of US 6,676,933 B2 3 4 moSapride, Simethicone and at least one pharmaceutical When employed, the amount of Simethicone per unit dose excipient. Another aspect of the invention provides a phar may vary depending upon the degree
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