Claims for Patent: 5,980,942

Summary for Patent: 5,980,942

Title:	Zero-order sustained release matrix tablet formulations of carbamazepine
Abstract:	A zero-order sustained-release delivery system for delivery of carbamazepine. A matrix tablet formulations of carbamazepine comprising hydrophilic polymer gel which inhibits transformation of carbamazepine into carbamazepine dihydrate by causing morphologic changes of carbamazepine crystals and results in amorphous form of carbamazepine present in the polymer matrix.
Inventor(s):	Katzhendler; Ifat (Jerusalem, IL), Friedman; Michael (Jerusalem, IL)
Assignee:	Yissum Research Development Company of the Hebrew University of Jerusalem (IL)
Application Number:	09/012,265
Patent Claims:	1. An erodible oral composition for sustained release delivery of a drug at a zero-order release rate comprising a pharmaceutical agent in combination with an erodible polymeric matrix formulated as a tablet, capsule or granule comprising at least one hydrophilic polymer or a mixture of two or more hydrophilic polymers, having viscosity between about 5 and about 100,000 mPa.multidot.s(cp) at concentration of 2% at 20.degree. C. and a molecular weight between 10,000 and 246,000, wherein said polymer matrix inhibits a crystallization of the pharmaceutical agent to the dihydrate form and wherein said composition erodes at a zero-order release rate, thereby releasing the pharmaceutical agent at a zero-order delivery rate. 2. An erodible oral composition for sustained release delivery of a drug at a zero-order release rate comprising carbamazepine as a first component and an erodible polymeric matrix formulated as a tablet, capsule or granule comprising at least one hydrophilic polymer or a mixture of two or more hydrophilic polymers having viscosity between about 5 and about 100,000 mPa.multidot.s(cp) at concentration of 2% at 20.degree. C. and a molecular weight between 10,000 and 246,000 as a second component, wherein said composition erodes at a rate producing a zero-order delivery rate of carbamazepine. 3. The composition according to claim 2 wherein said matrix is formulated as an erodible tablet and wherein said hydrophilic polymer is selected from the group consisting of methyl cellulose, hydroxypropyl methylcellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxyethyl methylcellulose, carboxymethylcellulose and sodium carboxymethylcellulose. 4. The composition according to claim 3 wherein said polymer is hydroxypropyl methylcellulose. 5. The composition according to claim 4 additionally containing a hydrophobic component. 6. The composition according to claim 5 wherein the hydrophobic component is selected from the group consisting of ethyl cellulose, glycerol palmitostearate, beeswax, glycowax, castrowax, carnaubawax, glycerol monostearate stearylalcohol, a hydrophobic polyacrylamide derivative and a hydrophobic methacrylic acid derivative. 7. The composition according to claim 6 wherein hydrophobic cellulose derivative is ethyl cellulose. 8. The composition according to claim 7 additionally containing pharmaceutically acceptable constituents and additives selected from the group consisting of proteins, arabinogalactans, chitosans, polysaccharides, hydrophilic polyacrylamide derivatives and hydrophilic methacrylic acid derivatives. 9. The composition according to claim 8 wherein the additive is a protein bovine albumin, human albumin, egg albumin, soy protein, gelatin or casein in the native or denatured state. 10. The composition according to claim 9 wherein the additive is a polysaccharide .beta.-cyclodextran or a starch derivative. 11. The composition according to claim 10 wherein said hydrophobic component is glycerol palmitostearate, beeswax, glycowax, castrowax, carnaubawax, glycerol monostearate or stearyl alcohol. 12. The composition according to claim 11 further comprising a pharmaceutically acceptable additive selected from the group consisting of salts, polyethylene glycol and surfactants. 13. A method for a sustained and controlled zero-order rate of drug delivery comprising: (a) preparation of erodible formulation in form of an erodible tablet, erodible capsule or erodible granules comprising a matrix consisting of a pharmaceutically active drug in admixture with a hydrophilic polymer having a viscosity between about 5 and about 100,000 mpa.multidot.s (cp) at a c ntration of 2% at 20.degree. C. temperature and a molecular weight between 10,000 and 246,000, or in admixture with a mixture of the hydrophilic and a hydrophobic polymer; and (b) administering said erodible formulation orally to a patient in need of such treatment wherein upon contact of the erodible formulation with aqueous condition of the digestive system, the formulation erodes at a zero-order rate and releases the pharmaceutical agent in the zero-order release rate; and wherein the erodible formulation prevents crystallization of the pharmaceutical agent into its dihydrate form.

Details for Patent 5,980,942

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Grifols Therapeutics Llc	ALBUKED, PLASBUMIN-20, PLASBUMIN-25, PLASBUMIN-5	albumin (human)	For Injection	101138	10/21/1942		2017-01-23
Baxalta Us Inc.	BUMINATE, FLEXBUMIN	albumin (human)	Injection	101452	03/03/1954		2017-01-23
Csl Behring Ag	ALBURX	albumin (human)	Injection	102366	07/23/1976		2017-01-23
Grifols Biologicals Llc	ALBUTEIN	albumin (human)	Injection	102478	08/15/1978		2017-01-23
Instituto Grifols, S.a.	HUMAN ALBUMIN GRIFOLS	albumin (human)	Injection	103352	02/17/1995		2017-01-23
Instituto Grifols, S.a.	HUMAN ALBUMIN GRIFOLS	albumin (human)	Injection	103352	06/11/2003		2017-01-23