US2004048896A1PendingUtilityA1

Novel substituted benzimidazole dosage forms and method of using same

58
Priority: Jan 4, 1996Filed: Apr 18, 2003Published: Mar 11, 2004
Est. expiryJan 4, 2016(expired)· nominal 20-yr term from priority
Inventors:Jeffrey Phillips
A61K 9/2813A61K 36/42A61K 9/2086A61K 33/00A61K 9/0056A61K 9/209A61K 9/2009A61K 36/48A61K 31/4439A61K 47/02A61K 36/898A61K 9/2013A61P 1/04A61K 9/0095A61K 9/2081A61K 31/00A61K 9/0007A61K 9/2054A61K 45/06A61K 36/534A61K 36/742A61K 36/5777
58
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Claims

Abstract

Disclosed herein are compositions and methods for treating gastric acid disorders employing pharmaceutical compositions comprising a proton pump inhibitor (PPI) in a pharmaceutically acceptable carrier.

Claims

exact text as granted — not AI-modified
1 . A method for treating or preventing an acid-caused gastrointestinal disorder in a subject, comprising: 
 orally administering to the subject a solid pharmaceutical composition comprising: active ingredients consisting essentially of a proton pump inhibitor in an amount of about 2 mg to about 300 mg; and at least one primary essential buffer and at least one secondary essential buffer in a total amount of about 0.1 mEq to about 2.5 mEq per mg of proton pump inhibitor;    wherein upon administration to the subject the composition contacts stomach secretions; and the buffering agent is present in an amount that substantially prevents or inhibits acid degradation of the proton pump inhibitor in the stomach secretions.    
     
     
         2 . The method of  claim 1 , wherein the composition comprises an enteric coating.  
     
     
         3 . The method of  claim 1 , wherein the composition comprises a film coating.  
     
     
         4 . The method of  claim 1 , wherein the composition comprises a delayed-release coating.  
     
     
         5 . The method of  claim 1 , wherein the proton pump inhibitor is in a homogeneous mixture with the buffering agent.  
     
     
         6 . The method of  claim 1 , wherein the proton pump inhibitor is a substituted benzimidazole compound having H+, K+-ATPase inhibiting activity.  
     
     
         7 . The method of  claim 1 , wherein the proton pump inhibitor is selected from the group consisting of omeprazole, lansoprazole, rabeprazole, esomeprazole, pantoprazole, pariprazole, and leminoprazole, or an enantiomer, isomer, free base, salt, or mixture thereof.  
     
     
         8 . The method of  claim 1 , wherein the proton pump inhibitor is in an amount from about 2 mg to about 120 mg.  
     
     
         9 . The method of  claim 1 , wherein the proton pump inhibitor is in an amount of about 120 mg.  
     
     
         10 . The method of  claim 1 , wherein the proton pump inhibitor is in an amount of about 80 mg.  
     
     
         11 . The method of  claim 1 , wherein the proton pump inhibitor is in an amount from about 2 mg to about 60 mg.  
     
     
         12 . The method of  claim 1 , wherein the proton pump inhibitor is in an amount of about 2 mg, 10 mg, 20 mg, 30 mg, 40 mg, or 60 mg.  
     
     
         13 . The method of  claim 1 , wherein the proton pump inhibitor is in an amount from about 10 mg to about 20 mg.  
     
     
         14 . The method of  claim 1 , wherein the proton pump inhibitor is in an amount of about 15 mg.  
     
     
         15 . The method of  claim 1 , wherein the proton pump inhibitor is omeprazole.  
     
     
         16 . The method of  claim 1 , wherein the proton pump inhibitor is lansoprazole.  
     
     
         17 . The method of  claim 1 , wherein the proton pump inhibitor is rabeprazole.  
     
     
         18 . The method of  claim 1 , wherein the proton pump inhibitor is esomeprazole.  
     
     
         19 . The method of  claim 1 , wherein the proton pump inhibitor is pantoprazole.  
     
     
         20 . The method of  claim 1 , wherein the proton pump inhibitor is pariprazole.  
     
     
         21 . The method of  claim 1 , wherein the proton pump inhibitor is leminoprazole.  
     
     
         22 . The method of  claim 1 , wherein the composition further comprises a binder, a flavoring agent, a disintegrant, a flow aid, a lubricant, an adjuvant, a colorant, a diluent, a moistening agent, a preservative, an antifoaming agent, or a pharmaceutically compatible carrier, and mixtures thereof.  
     
     
         23 . The method of  claim 22 , wherein the binder comprises crospovidone, microcrystalline cellulose, or a sugar.  
     
     
         24 . The method of  claim 22 , wherein the flavoring agent comprises aspartame, dextrose, chocolate, vanilla, root beer, peppermint, spearmint, sucrose, cocoa, or watermelon.  
     
     
         25 . The method of  claim 22 , wherein the disintegrant comprises croscarmellose sodium, a calcium, and sodium alginate complex, or sodium starch glycolate.  
     
     
         26 . The method of  claim 22 , wherein the lubricant comprises magnesium stearate, calcium hydroxide, talc, or stearic acid.  
     
     
         27 . The method of  claim 22 , wherein the diluent comprises lactose, corn starch, potato starch, or mannitol.  
     
     
         28 . The method of  claim 22 , wherein the pharmaceutically compatible carrier comprises acacia, gelatin, colloidal silicon dioxide, calcium glycerophosphate, calcium lactate, maltodextrin, glycerine, magnesium silicate, sodium caseinate, soy lecithin, sodium chloride, tricalcium phosphate, dipotassium phosphate, sodium stearoyl lactylate, carrageenan, monoglyceride, diglyceride, or pregelatinized starch.  
     
     
         29 . The method of  claim 1 , wherein the primary essential buffer or the secondary essential buffer is selected from the group consisting of sodium bicarbonate, potassium bicarbonate, magnesium hydroxide, magnesium lactate, magnesium gluconate, magnesium oxide, magnesium carbonate, magnesium silicate, aluminum hydroxide, aluminum hydroxide/sodium bicarbonate coprecipitate, aluminum glycinate, sodium citrate, sodium tartarate, sodium acetate, sodium carbonate, sodium polyphosphate, potassium polyphosphate, sodium pyrophosphate, potassium pyrophosphate, disodium hydrogenphosphate, dipotassium hydrogenphosphate, trisodium phosphate, tripotassium phosphate, sodium acetate, potassium metaphosphate, magnesium oxide, magnesium hydroxide, magnesium carbonate, magnesium silicate, calcium acetate, calcium glycerophosphate, calcium chloride, calcium hydroxide, calcium lactate, calcium carbonate, and calcium gluconate, and mixtures thereof.  
     
     
         30 . The method of  claim 1 , wherein the amount of the primary essential buffer and the secondary essential buffer totals about 2 mEq to about 70 mEq.  
     
     
         31 . The method of  claim 1 , wherein the amount of the primary essential buffer and the secondary essential buffer totals about 10 mEq to about 50 mEq.  
     
     
         32 . The method of  claim 1 , wherein the amount of the primary essential buffer and the secondary essential buffer totals about 1 mEq to about 20 mEq.  
     
     
         33 . The method of  claim 1 , wherein the amount of the primary essential buffer and the secondary essential buffer totals about 12.5 mEq to about 30 mEq.  
     
     
         34 . The method of  claim 1 , wherein the amount of the primary essential buffer and the secondary essential buffer totals about 0.2 mEq, 1 mEq, 2 mEq, 3 mEq, 5 mEq, 10 mEq, 12.5 mEq, 15 mEq, 20 mEq, 25 mEq, 30 mEq, 50 mEq, 70 mEq, or 150 mEq.  
     
     
         35 . The method of  claim 29 , wherein the primary essential buffer or the secondary essential buffer is sodium bicarbonate.  
     
     
         36 . The method of  claim 29 , wherein the primary essential buffer or the secondary essential buffer is sodium carbonate.  
     
     
         37 . The method of  claim 29 , wherein the primary essential buffer or the secondary essential buffer is calcium carbonate.  
     
     
         38 . The method of  claim 29 , wherein the primary essential buffer or the secondary essential buffer is a mixture of sodium bicarbonate, and sodium carbonate.  
     
     
         39 . The method of  claim 29 , wherein the primary essential buffer or the secondary essential buffer is a mixture of sodium bicarbonate, and calcium carbonate.  
     
     
         40 . The method of  claim 1 , wherein the amount of the primary essential buffer or the secondary essential buffer is more than about 40 times the amount of the proton pump inhibitor on a weight to weight basis in the composition.  
     
     
         41 . The method of  claim 1 , wherein the proton pump inhibitor is micronized.  
     
     
         42 . The method of  claim 1 , wherein the primary essential buffer or the secondary essential buffer is micronized.  
     
     
         43 . The method of  claim 1 , wherein the solid pharmaceutical composition is in a form of a tablet, a capsule, a powder, a pellet, a granule, or a troche.  
     
     
         44 . The method of  claim 43 , wherein the tablet is a suspension tablet, a chewable tablet, or an effervescent tablet.  
     
     
         45 . The method of  claim 43 , wherein the powder is an effervescent powder.  
     
     
         46 . The method of  claim 43 , wherein the powder is a powder for suspension.  
     
     
         47 . The method of  claim 46 , wherein the powder is suspended in an aqueous medium before administration.  
     
     
         48 . The method of  claim 47 , wherein the aqueous medium is selected from the group consisting of water, and sodium bicarbonate solution.  
     
     
         49 . The method of  claim 1 , wherein the acid-caused gastrointestinal disorder comprises duodenal ulcer disease, gastric ulcer disease, gastroesophageal reflux disease, erosive esophagitis, poorly responsive symptomatic gastroesophageal reflux disease, pathological gastrointestinal hypersecretory disease, Zollinger Ellison Syndrome, or acid dyspepsia.  
     
     
         50 . The method of  claim 1 , wherein a therapeutically effective amount of the composition is administered to the subject.  
     
     
         51 . The method of  claim 1 , wherein the composition is administered to the subject once a day, or multiple times a day.

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