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Claims for Patent: 8,475,841

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Claims for Patent: 8,475,841

Title:Controlled release metformin formulations
Abstract: Sustained release pharmaceutical formulations comprising an antihyperglycemic drug or a pharmaceutically acceptable salt thereof are disclosed. The formulations provide therapeutic plasma levels of the antihyperglycemic drug to a human patient over a 24 hour period after administration.
Inventor(s): Cheng; Xiu Xiu (Weston, FL), Jan; Steve (Coral Spings, FL), Chou; Joseph (Manasses, VA), Chen; Chih-Ming (Taipei, TW)
Assignee: Andrx Labs, LLC (Davie, FL)
Application Number:13/052,154
Patent Claims: 1. A method of treating a human diabetic patient with an oral solid sustained release tablet of metformin hydrochloride, comprising: administering the sustained release tablet to the human diabetic patient once a day with or after the patient's evening meal, wherein the sustained release tablet comprises (a) a homogeneous core; (b) optionally a seal coat surrounding the core and (c) a modified polymeric membrane surrounding the seal coat if present or the core if the seal coat is not present wherein: the core comprises: (a)(i) 75-95% metformin hydrochloride based upon the total weight of the core (a)(ii) 3-15% of a binder based upon the total weight of the core; and (a)(iii) a lubricant; and the modified polymeric membrane comprises: (c)(i) a polymer that controls or sustains the release of the metformin from the core; (c)(ii) a plasticizer selected from the group consisting of triacetin, acetylated monoglyceride, grape seed oil, olive oil, sesame oil, acetyltributylcitrate, acetyltriethylcitrate, glycerin sorbitol, diethyloxalate, diethylmalate, diethylfumarate, dibutylsuccinate, diethylmalonate, dioctylphthalate, dibutylsebacate, triethylcitrate, tributylcitrate, and glycerlotributyrate; (c)(iii) a water soluble or enteric flux enhancing agent selected from the group consisting of sodium chloride, potassium chloride, sucrose, sorbitol, mannitol, polyethylene glycol, propylene glycol, hydroxypropyl cellulose, hydroxypropyl methylcellulose, hydroxypropyl methylcellulose phthalate, cellulose acetate phthalate, polyvinyl alcohols, methacrylic acid copolymers and mixtures thereof; and the metformin is released from the core by a passageway and/or pores in the modified polymeric membrane so that the oral solid sustained release tablet exhibits the following in vitro dissolution profile when tested in a USP Type 2 apparatus at 75 rpms in 900 ml of a pH 7.5 phosphate buffer and 37.degree. C.: 0-25% of the metformin is released after 2 hours; 10-45% of the metformin is released after 4 hours; 30-90% of the metformin is released after 8 hours; not less than 50% of the metformin is released after 12 hours; not less than 60% of the metformin is released after 16 hours and not less than 70% of the metformin is released after 20 hours.

2. The method as defined in claim 1 wherein the oral solid sustained release tablet exhibits the following in vitro dissolution profile when tested in a USP Type 2 apparatus at 75 rpms in 900 ml of a pH 7.5 phosphate buffer and 37.degree. C.: 0-15% of the metformin is released after 2 hours; 20-40% of the metformin is released after 4 hours; 45-90% of the metformin is released after 8 hours; not less than 60% of the metformin is released after 12 hours; not less than 70% of the metformin is released after 16 hours and not less than 80% of the metformin is released after 20 hours.

3. The method of claim 1 wherein the polymer of the modified release polymeric membrane is cellulose acetate.

4. The method as defined in claim 1 wherein the modified polymeric membrane comprises about 3% of the total weight of the core and coatings.

5. The method as defined in claim 1 wherein the modified polymeric membrane comprises about 3% to about 5% of the total weight of the core and coatings.

6. A method of treating a human diabetic patient with an oral solid sustained release tablet of metformin hydrochloride, comprising: administering the sustained release tablet to the human diabetic patient once a day with or after the patient's evening meal, wherein the sustained release tablet comprises (a) a homogeneous core; (b) optionally a seal coat surrounding the core and (c) a modified polymeric membrane surrounding the seal coat if present or the core if the seal coat is not present wherein: the core comprises: (a)(i) 75-95% metformin hydrochloride based upon the total weight of the core (a)(ii) 3-15% of a binder based upon the total weight of the core; and (a)(iii) a lubricant; and the modified polymeric membrane comprises: (c)(i) cellulose acetate; (c)(ii) a plasticizer selected from the group consisting of triacetin, acetylated monoglyceride, grape seed oil, olive oil, sesame oil, acetyltributylcitrate, acetyltriethylcitrate, glycerin sorbitol, diethyloxalate, diethylmalate, diethylfumarate, dibutylsuccinate, diethylmalonate, dioctylphthalate, dibutylsebacate, triethylcitrate, tributylcitrate, and glycerlotributyrate; (c)(iii) a water soluble or enteric flux enhancing agent selected from the group consisting of sodium chloride, potassium chloride, sucrose, sorbitol, mannitol, polyethylene glycol, propylene glycol, hydroxypropyl cellulose, hydroxypropyl methylcellulose, hydroxypropyl methylcellulose phthalate, cellulose acetate phthalate, polyvinyl alcohols, methacrylic acid copolymers and mixtures thereof; and the metformin is released from the core by a passageway and/or pores in the modified polymeric membrane so that the oral solid sustained release tablet exhibits the following in vitro dissolution profile when tested in a USP Type 2 apparatus at 75 rpms in 900 ml of a pH 7.5 phosphate buffer and 37.degree. C.: 0-25% of the metformin is released after 2 hours; 10-45% of the metformin is released after 4 hours; 30-90% of the metformin is released after 8 hours; not less than 50% of the metformin is released after 12 hours; not less than 60% of the metformin is released after 16 hours and not less than 70% of the metformin is released after 20 hours.

7. The method as defined in claim 6 wherein the oral solid sustained release tablet exhibits the following in vitro dissolution profile when tested in a USP Type 2 apparatus at 75 rpms in 900 ml of a pH 7.5 phosphate buffer and 37.degree. C.: 0-15% of the metformin is released after 2 hours; 20-40% of the metformin is released after 4 hours; 45-90% of the metformin is released after 8 hours; not less than 60% of the metformin is released after 12 hours; not less than 70% of the metformin is released after 16 hours and not less than 80% of the metformin is released after 20 hours.

8. The method as defined in claim 6 wherein the modified polymeric membrane comprises about 3% of the total weight of the core and coatings.

9. The method as defined in claim 6 wherein the modified polymeric membrane comprises about 3% to about 5% of the total weight of the core and coatings.
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