Claims for Patent: 5,460,812

Summary for Patent: 5,460,812

Title:	Compositions of digestive enzymes and salts of bile acids and process for preparation thereof
Abstract:	Disclosed are gastric acid-resistant polymer-coated buffered digestive enzymes/ursodeoxycholate compositions, process for their preparations and methods of treating digestive disorders, pancreatic enzyme insufficiency, impaired liver function, cystic fibrosis, for regulating the absorption of dietary iron and cholesterol, and for dissolving gallstones by administering the compositions to a mammal in need of such treatment.
Inventor(s):	Sipos; Tibor (Lebanon, NJ)
Assignee:	Digestive Care Inc. (Lebanon, NJ)
Application Number:	08/129,250
Patent Claims:	1. A buffered digestive enzyme/bile salt composition for the treatment of digestive enzyme/bile salt deficiency of mammals comprising, by weight per weight percentages based on the total weight of the composition: a) from about 10 to about 90.0% of a concentrate of an enzyme selected from the group consisting of pancreatin, pancreatic proteases, pancreatic lipases, pancreatic nucleases and pancreatic amylases; b) from about 0.3 to about 75% of a bile salt in powder form; c) from 7.3 of a buffering agent selected from the group consisting of anhydrous sodium carbonate, sodium bicarbonate, potassium carbonate, ammonium carbonate, tromethamine, di(tris(hydoxymethyl)aminomethane)carbonate, tris-glycine, di-arginine in the molecular weight range of 350 to 50,000 Daltons, tri-arginine in the molecular weight range of 350 to 50,000 Daltons, poly-arginine in the molecular weight range of 350 to 50,000 Daltons, di-lysine in the molecular weight range of 290 to 15,000 Daltons, tri-lysine in the molecular weight range of 290 to 15,000 Daltons, poly-lysine in the molecular weight range of 290 to 15,000 Daltons, diethylamine and triethanolamine; d) from about 0.9 to about 16% of a disintegrant selected from the group consisting of starch, modified starches, microcrystalline cellulose and propylene glycol alginate; e) from about 0.3 to about 15.0% of an adhesive polymer selected from the group consisting of hydroxypropyl cellulose, polyvinylpyrrolidone, cellulose acetate phthalate, methyl cellulose and propylene glycol alginate; and f) from about 7.0 to about 15% of an non-porous, gastric acid-resistant and pharmaceutically acceptable polymer-coating which contains from about 0.2 to about 2% talc and which is insoluble in the pH range of from about 1.5 to about 5 but is soluble in the pH range of from about 5.5 to about 9. 2. The composition of claim 1 wherein said concentrate of an enzyme is selected from the group consisting of pancreatin, pancrelipase, trypsin, chymotrypsin, chymotrypsin B, pancreatopeptidase. carboxypeptidase A, carboxypeptidase B, glycerol ester hydrolase, phospholipase A2, sterol ester hydrolase, ribonuclease, deoxyribonuclease, .alpha.-amylase, papain, chymopapain, bromelain, ficin, .beta.-amylase, cellulase, and .beta.-galactosidase. 3. The composition of claim 1 wherein the buffer component of said buffered digestive enzyme/bile salt is selected from the group consisting of anhydrous sodium carbonate, sodium bicarbonate, potassium carbonate, potassium bicarbonate, ammonium carbonate, tromethamine, tris-carbonate, tris-glycine, di-arginine, tri-arginine, poly-arginine, di-lysine, tri-lysine, poly-lysine, ethanolamine, diethanolamine and triethanolamine. 4. The composition of claim 1 wherein said bile salt is selected from the group consisting of sodium-ursodeoxycholate, sodium glycylursodeoxycholate, potassium-ursodeoxycholate, potassium glycylursodeoxycholate, ferrous-ursodeoxycholate, ferrous glycylursodeoxycholate, ammonium-ursodeoxycholate, ammonium glycylursodeoxycholate, sodium-tauroursodeoxycholate, sodium-N-methylglycylursodeoxycholate, potassium-tauroursodeoxycholate, potassium-N-methylglycylursodeoxycholate, ferrous-tauroursodeoxycholate, ferrous-N-methylglycylursodeoxycholate, ammonium-tauroursodeoxycholate, ammonium-N-methylglycylursodeoxycholate, sodium-N-methyltauroursodeoxycholate, potassium-N-methyltauroursodeoxycholate, ferrous-N-methyltauroursodeoxycholate, ammonium-N-methyltauroursodeoxycholate, sodium-cholate, sodium-deoxycholate, potassium-cholate, potassium-deoxycholate, ferrous-cholate, ferrous-deoxycholate, ammonium-cholate, ammonium-deoxycholate, sodium-chenodeoxycholate, sodium-glycylcholate, potassium-chenodeoxycholate, potassium-glycylcholate, ferrous-chenodeoxycholate, ferrous-glycylcholate, ammonium-chenodeoxycholate, ammonium-glycylcholate, sodium-taurocholate, sodium-N-methylglycylcholate, potassium-taurocholate, potassium-N-methylglycylcholate, ferrous-taurocholate, ferrous-N-methylglycylcholate, ammonium-taurocholate, ammonium-N-methylglycylcholate, sodium-N-methyltaurocholate, sodium-glycyldeoxycholate, potassium-N-methyltaurocholate, potassium-glycyldeoxycholate, ferrous-N-methyltaurocholate, ferrous-glycyldeoxycholate, ammonium-N-methyltaurocholate, ammonium-glycyldeoxycholate, sodium-taurodeoxycholate, sodium-N-methylglycyldeoxycholate, potassium-taurodeoxycholate, potassium-N-methylglycyldeoxycholate, ferrous-taurodeoxycholate, ferrous-N-methylglycyldeoxycholate, ammonium-taurodeoxycholate, ammonium-N-methylglycyldeoxycholate, sodium-N-methyltaurodeoxycholate, sodium-N-methylglycylchenodeoxycholate, potassium-N-methyltaurodeoxycholate, potassium-N-methylglycylchenodeoxycholate, ferrous-N-methyltaurodeoxycholate, ferrous-N-methylglycylchenodeoxycholate, ammonium-N-methyltaurodeoxycholat e, ammonium-N-methylglycylchenodeoxycholate, sodium-N-methyltaurochenodeoxycholate, potassium-N-methyltaurochenodeoxycholate, ferrous-N-methyltaurochenodeoxycholate; ammonium-N-methyltaurochenodeoxycholate, ethyl esters of ursodeoxycholate, propyl esters of ursodeoxycholate, sodium-glycylchenodeoxycholate, potassium-glycylchenodeoxycholate, ferrous-glycylchenodeoxycholate, ammonium-glycylchenodeoxycholate, sodium-taurochenodeoxycholate, potassium-taurochenodeoxycholate, ferrous-taurochenodeoxycholate, ammonium-taurochenodeoxycholate. 5. A method for treating digestive enzyme-bile salt deficiency in mammals comprising orally administering an effective amount, sufficient to effect a reduction in digestive enzyme/bile salt deficiency, of the composition of claim 1. 6. The method of claim 5 wherein said treatment is to effect a reduction in digestive enzyme/bile salt deficiency in pancreatic enzyme insufficiency, or impaired liver function, or insufficient absorption of dietary iron and cholesterol, or cystic fibrosis, or presence of gallstones. 7. The method of claim 5 wherein about 0.5 to 1.5 gms of the composition is administered to a digestive enzyme/bile salt deficient patient with each meal three times a day. 8. The method of claim 7 wherein said composition is administered in an acid soluble capsule containing from about 0.2 to about 0.5 grams of microspheres or microtablets. 9. The method of claim 7 wherein said composition is administered admixed with a liquid or a semi-solid food. 10. The method of claim 5 wherein said treatment is to effect a reduction in digestive enzyme/bile salt deficiency in digestive disorders.

Details for Patent 5,460,812

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Discure Medical, Llc	CHYMODIACTIN	chymopapain	For Injection	018663	November 10, 1982		2012-06-22
Discure Medical, Llc	CHYMODIACTIN	chymopapain	For Injection	018663	August 21, 1984		2012-06-22
Organon Usa Inc., A Subsidiary Of Merck & Co., Inc.	COTAZYM	pancrelipase	Capsule, Delayed Release	020580	December 09, 1996		2012-06-22

International Patent Family for US Patent 5,460,812

Country	Patent Number	Estimated Expiration
United States of America	5578304
United States of America	5324514
United States of America	5260074