Water insoluble polymer based sustained release formulation

• US 6,251,430 B1
• Filed: 02/04/1998
• Issued: 06/26/2001
• Est. Priority Date: 02/04/1998
• Status: Expired due to Fees

• Current Assignee: Guohua Zhang, Muhammad A. Ali, Prasad Pinnamaraju
• Original Assignee: Guohua Zhang, Muhammad A. Ali, Prasad Pinnamaraju
• Inventors: Zhang, Guohua, Pinnamaraju, Prasad, Ali, Muhammad A.
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): Seidleck, Brian K.
• Application Number:
  US09/018,522
• Time in Patent Office: 1,238 Days
• Field of Search: 424/464, 424/468, 424/474, 424/480, 424/482, 514/964
• US Class Current: 424/468
• CPC Class Codes: A61K 9/2027 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/205 Polysaccharides, e.g. alginate, gums; Cyclodextrin
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose

Abstract

Sustained release drug formulations contain the pharmaceutical itself and a three component release rate controlling matrix composition. The three components of the matrix composition are (1) water insoluble polymer, such as ethyl cellulose, (2) pH dependent gelling polymer, such as sodium alginate, and (3) a pH independent gelling polymer, such as hydroxypropyl methylcellulose. The drug release rate can be adjusted by changing the amount of one or more of these components of the composition.

Claims

1. A sustained release tablet comprising an effective amount of a drug to be released at a controlled rate and a homogenous mixture of three different types of polymers including a water insoluble polymer compound, a pH dependent gelling polymer, and a pH independent gelling polymer, wherein said water insoluble polymer comprises one or more of ethylcellulose and co-polymers of acrylic and methacrylic acid esters.

2. A sustained release tablet of claim 1 comprising effective amounts of said water insoluble polymer compound, pH independent gelling polymer, and pH dependent gelling polymer to control the release of said rate drug.

3. A tablet of claim 2 wherein said effective amount of pH dependent gelling polymer does not hydrate over the pH range in the stomach but hydrates over the pH range in the intestine controlling said release rate of said drug.

4. A tablet of claim 2 wherein said effective amount of pH independent gelling polymer hydrates in the stomach and intestine to control said release rate of said drug.

5. A tablet of claim 2, wherein said pH independent gelling polymer comprises one or more of hydroxypropyl methylcellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, hydroxypropyl ethylcellulose, methylcellulose, xanthum gum, polyethylene oxide and carboxypolymethylene.

6. A tablet of claim 2, wherein said pH dependent gelling polymer comprises one or more of sodium alginate and sodium carboxymethylcellulose.

7. A tablet of claim 5, wherein said pH independent gelling polymer has a viscosity within the range from about 50 to about 150,000 centipoises in a 2% by weight aqueous solution, measured using a Brookfield LV viscometer.

8. A tablet of claim 6 wherein said pH dependent gelling polymer has a viscosity within the range from about 50 to about 10,000 centipoises in a 2% by weight aqueous solution, measured using a Brookfield LV viscometer.

10. A tablet of claim 1, wherein said water insoluble polymer is from about 2% to about 30% of the tablet weight.

11. A tablet of claim 1, wherein said pH dependent gelling polymer is from about 2% to about 40 % of the tablet weight.

12. A tablet of claim 1, wherein said pH independent gelling polymer is from about 2% to about 30% of the tablet weight.

13. A tablet of claim 1, wherein said drug is etodolac.

14. A tablet of claim 1, wherein said drug is morphine sulfate.

15. A tablet of claim 1, wherein said drug is oxycodone hydrochloride.

16. A tablet of claim 1, wherein said drug is water soluble or water sparingly soluble, or water insoluble.

9. A method of forming a sustained release depot drug dosage form comprising introducing an effective amount of a drug in a tablet comprising and from about 6 to about 60 percent by weight of a homogenous mixture of three different types of polymers including water insoluble polymer compound, a pH independent gelling polymer, and a pH dependent gelling polymer, wherein said water insoluble polymer comprises one or more of ethylcellulose and co-polymers of acrylic and methacrylic acid esters.