Drug – bio-affecting and body treating compositions – Digestive system regulator containing solid synthetic...
Reexamination Certificate
2001-05-23
2004-01-13
Tate, Christopher R. (Department: 1654)
Drug, bio-affecting and body treating compositions
Digestive system regulator containing solid synthetic...
C424S094210, C424S094100
Reexamination Certificate
active
06676933
ABSTRACT:
FIELD OF THE INVENTION
This invention concerns a pharmaceutical composition comprising mosapride and pancreatin for the treatment of gastrointestinal discomfort. More particularly, the invention pertains to an immediate release solid oral dosage form comprising mosapride, pancreatin and optionally simethicone and to the use of this dosage form for the treatment or prevention of a gastrointestinal disorder or the symptoms associated therewith.
BACKGROUND OF THE INVENTION
Simethicone is used for the relief of discomfort or painful symptoms caused by the presence of excessive gas in the gastrointestinal tract. It is typically recommended for coadministration with an antacid medication, where gas formation is a problem in effective therapy. Simethicone is available in dosage forms including a capsule, suspension, tablet or chewable tablet. Commercial products containing simethicone include Phazyme™, Extra Strength Maalox Anti-Gas™, Flatulex™, Gas-X™, Genasyme™, Maximum Strength Mylanta Gas Relief™, My Baby Gas Relief Drops™, Mylicon™ Drops, Ovol™, and others. Phazyme™ is a combination dosage form containing simethicone and pancreatin. The dose of simethicone required to provide a relief from gastrointestinal pain will vary according to weight and age of a subject receiving the medication. The conventional dose for adults and teenagers for the tablet or capsule ranges from about 60 to 125 mg four times daily after meals and at bedtime. The conventional dose for adults and teenagers for the chewable tablet ranges from about 40 to 125 mg four times daily after meals and at bedtime or the dose may be 150 mg three times daily after meals. Generally, the dose should not exceed 500 mg daily. A tablet containing simethicone, pancreatin, pepsin and belladonna is known.
Pancreatin is an enzymatic preparation made from the pancreatic enzymes of animals. Pancreatin tablets are prescribed for patients who are unable to digest food properly because of an insufficient amount of natural pancreatic excretions. Commercially available products include Solgar™ pancreatin tablets, Twinlab™ pancreatin tablets and others. These tablets generally contain other enzymes such as amylase, protease and lipase as well as a mixture of pharmaceutical excipients.
S. A. Said et al. (
Manuf. Chem. Aerosol News
(1976), 47(5), 35-36) disclose an immediate release coated tablet comprising a core containing simethicone, pepsin, pancreatin and belladonna and a coating surrounding the core and containing pepsin. This tablet is reportedly effective in reducing gastrointestinal gas.
J. M. Auld (
Curr. Ther. Res.
(1979), 26(1), 55-61) discloses an immediate release tablet comprising simethicone and pancreatin. The tablet was administered four times daily to a group of patients over a 2-week period and was reportedly effective at reducing the discomfort and painful symptoms associated with excessive gastrointestinal gas.
I. Suramo et al. (
Ann. Clin. Res., Suppl
. (1984), 16(40), 62-64) disclose an immediate release tablet comprising simethicone and pancreatin. Two tablets were administered four times daily to fifty patients. The tablet was reportedly effective at reducing the amount of gastrointestinal gas.
J. Venturini (
Prensa Med. Argent.
(1996), 83(5), 483-485) discloses an immediate release tablet containing pancreatin, desoxycholic acid, dehydrocholic acid and simethicone, among other things. The tablet was administered twice daily to patients over a period of fourteen days. The tablet was reportedly effective at reducing the gastrointestinal discomfort associated with excessive gas.
Mosapride citrate (mosapride; (+/−)-4-amino-5-chloro-2-ethoxy-N-[[4-(4-fluorobenzyl)-2-morpholinyl]methyl]benzamide citrate; AS-4370; CAS 112885-42-4) is a benzamide-type gastroprokinetic agent that enhances the gastrointestinal motility by stimulating the 5-hydroxytryptamine-4 (5-HT4) receptor. Mosapride citrate is clinically prescribed as a racemate and is metabolized to its des-4-fluorobenzyl structure (M1). The metabolites M1 and M2 of mosapride citrate are generally less efficacious than mosapride.
R. T. Sims et al (International Publication No. WO 95/01803) disclose pharmaceutical compositions comprising an H2 antagonist, such as famotidine, a gastrointestinal motility agent, such as cisapride, and optionally simethicone for the treatment, prevention, or treatment and relief of various mild to moderate symptoms associated with gastrointestinal disorders including indigestion, sour stomach, overindulgence, heartburn, gastroesophageal reflux, constipation, dyspepsia, other gastrointestinal disorders and optionally flatulence.
Thus, the prior art does not disclose a pharmaceutical composition comprising mosapride, pancreatin and optionally simethicone for the treatment, prevention, or treatment and relief of various mild to moderate symptoms associated with gastrointestinal disorders.
SUMMARY OF THE INVENTION
The present invention seeks to overcome at least some of the disadvantages present in the known compositions and to provide a pharmaceutical composition for the treatment of, prevention of, or treatment and relief of various mild to moderate symptoms associated with gastrointestinal disorders including indigestion, sour stomach, overindulgence, heartburn, gastroesophageal reflux, constipation, dyspepsia, other gastrointestinal disorders and optionally flatulence. The pharmaceutical composition comprises mosapride, pancreatin and optionally simethicone or dimethicone. The pharmaceutical composition can be provided in an oral dosage form as disclosed herein. The dosage form can be an immediate release dosage form. The dosage form provides a concurrent, sequential, or combination thereof release of the two and optionally three active agents.
The present invention provides a multi-action approach to the treatment of gastrointestinal disorders in that a gastrointestinal motility agent such as mosapride offers enhanced motility while pancreatin promotes effective digestion and simethicone reduces gastrointestinal gas. The combination simultaneously treats, relieves and/or prevents symptoms associated with excess of gastric acid secretion in the esophagus. Prokinetic agents generally prevent the reflux of gastric acid from the stomach to the esophagus. Conditions or symptoms relieved by the promotion of gastric emptying include but are not limited to gastric stasis, flatulence, dyspepsia, peptic ulcer and reflux esophagitis.
The present invention therefore provides an effective multi-component treatment of gastrointestinal disorders using the combination of pancreatin with the gastrointestinal motility agent mosapride, and optionally with simethicone or dimethicone. The claimed combination is particularly useful for treating gastrointestinal distress.
One aspect of the invention provides a pharmaceutical composition or dosage form consisting essentially of mosapride, simethicone and at least one pharmaceutical excipient. Another aspect of the invention provides a pharmaceutical composition or dosage form consisting essentially of mosapride, simethicone, pancreatin and at least one pharmaceutical excipient. Still another aspect of the invention provides a pharmaceutical composition or dosage form comprising mosapride, simethicone, pancreatin and at least one pharmaceutical excipient.
Specific embodiments of the invention include those wherein: (a) at least one of the mosapride, pancreatin and simethicone or dimethicone is present in a sub-therapeutic amount; (b) wherein no less than 35% of the mosapride is released within 15 minutes and no less than 70% of mosapride is released within 30 minutes after exposure to an aqueous environment; (c) the mosapride, pancreatin and simethicone or dimethicone are released concurrently when the dosage form is placed in an aqueous environment of use; (d) the mosapride and simethicone or dimethicone are released concurrently and the pancreatin is released sequentially, with respect to the mosapride and simethicone or dimethicone, when the dosage form is placed in an aqu
Faour Joaquina
Ricci Marcelo A.
Vergez Juan A.
Innovar L.L.C.
Matos Rick
Osmotica Corp.
Patten Patricia
Tate Christopher R.
LandOfFree
Pharmaceutical composition containing mosapride and pancreatin does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Pharmaceutical composition containing mosapride and pancreatin, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Pharmaceutical composition containing mosapride and pancreatin will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-3229969