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Claims for Patent: 9,060,941

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Claims for Patent: 9,060,941

Title:Pharmaceutical formulation containing a biguanide and a thiazolidinedione derivative
Abstract: A pharmaceutical dosage form comprising a controlled release component comprising an antihyperglycemic drug in combination with a second component comprising a thiazolidinedione derivative is herein disclosed and described.
Inventor(s): Lodin; Unchalee (North Miami Beach, FL), Cardinal; Jack (Tamarac, FL), Nangia; Avinash (Lincoln, RI), Okochi; Kazuhiro (Osaka, JP)
Assignee: ACTAVIS, INC. (Parsippany, NJ) TAKEDA PHARMACEUTICAL COMPANY LIMITED (Osaka, JP)
Application Number:11/093,742
Patent Claims: 1. A pharmaceutical tablet consisting of: (a) a controlled release core consisting of: (i) a compressed mixture consisting of: (A) 50-98% of metformin hydrochloride; (B) 0.1-40% of a binding agent; (C) 0-20% of an absorption enhancer; and (D) 0-5% of a lubricant; (ii) optionally a first seal coat surrounding the compressed mixture; and (iii) a sustained release membrane coating surrounding the compressed mixture or the optional first seal coat if present, comprising: (A) 50-99% of a polymer selected from the group consisting of cellulose acetate, cellulose diacetate, cellulose triacetate, cellulose acetate propionate, and cellulose acetate butyrate; (B) 0-40% of a flux enhancer; and (C) 0-25% of a plasticizer, said membrane having at least one passageway formed therein for release of the metformin hydrochloride, wherein the metformin hydrochloride is released from the pharmaceutical tablet so the peak plasma level of metformin is obtained about 6-12 hours after administration of the pharmaceutical tablet following a meal, and (b) a second seal coating surrounding the sustained release membrane of the controlled release core wherein the second seal coat does not contain an active pharmaceutical ingredient and dissolves or disperses in water; (c) an immediate release pioglitazone coating surrounding the second seal coating wherein the immediate release pioglitazone layer consists of: (i) pioglitazone hydrochloride; (ii) a low viscosity water soluble binder comprising hydroxypropyl cellulose, wherein the hydroxypropyl cellulose exhibits a viscosity between 2 and 6 mPaS when tested as a 2% aqueous solution at 20.degree. C.; (iii) lactose; (iv) a plasticizer selected from the group consisting of triacetin, polyethylene glycol, glycerin, triethyl citrate, and mixtures thereof; and (v) optionally dye or pigment; (d) optionally a color coating; and (e) optionally a polishing coating; wherein not less than 95% of the pioglitazone is released from the pharmaceutical tablet within 30 minutes when tested according to the United States Pharmacopeia 26, with Apparatus 1 at 100 rpm, 37.degree. C. and 900 ml of 0.3 M KCl-HCl Buffer, pH 2.0 and after storage at 40.degree. C. and 75% relative humidity for 3 months the pharmaceutical tablet has a total of not more than 0.5% of the following pioglitazone impurities: (+/-)-5-[p-[2-(5-ethyl-2-pyridyl)ethoxy]benzyl]-5-hydroxy-2,4-thiazolidin- edione; (z)-5-[p-[2-(5-ethyl-2-pyridyl)ethoxy]benzylidene]-2,4-thiazolidin- edione; (+/-)-5-[p-[2-(5-ethyl-2-pyridyl)ethoxy]benzyl]-3-[2-(5-ethyl-2-py- ridyl)ethyl]-2,4-thiazolidinedione; (+/-)-ethyl-2-carbamoyltio-3-[4-[2-(5-ethyl-2-pyridyl)ethoxy]phenyl]propi- onate; and ethyl-3-p-[2-(5-ethyl-2-pyridyl)ethoxy]phenyl-propionate as determined by high performance liquid chromatography and each of the pioglitazone impurities is present in an amount of not more than 0.20%.

2. The pharmaceutical tablet of claim 1 wherein each pioglitazone impurity in the pharmaceutical tablet is not more than 0.10%.

3. The pharmaceutical tablet of claim 1 wherein the polymer of the sustained release membrane coating surrounding the compressed mixture is cellulose acetate.

4. A pharmaceutical tablet consisting of: (a) a controlled release core consisting of: (i) a compressed mixture consisting of: (A) 50-98% of metformin hydrochloride; (B) 0.1-40% of a binding agent; (C) 0-20% of an absorption enhancer; and (D) 0-5% of a lubricant; (ii) optionally a first seal coat surrounding the compressed mixture; and (iii) a sustained release membrane coating surrounding the compressed mixture or the optional first seal coat if present, comprising: (A) 50-99% of cellulose acetate; (B) 0-40% of a flux enhancer; and (C) 0-25% of a plasticizer, said membrane having at least one passageway formed therein for release of the metformin hydrochloride, wherein the metformin hydrochloride is released from the pharmaceutical tablet so the peak plasma level of metformin is obtained about 6-12 hours after administration of the pharmaceutical tablet following a meal, and (b) a second seal coating surrounding the sustained release membrane of the controlled release core wherein the second seal coat does not contain an active pharmaceutical ingredient and dissolves or disperses in water; (c) an immediate release pioglitazone coating surrounding the second seal coating wherein the immediate release pioglitazone layer consists of: (i) pioglitazone hydrochloride; (ii) a low viscosity water soluble binder comprising hydroxypropyl cellulose, wherein the hydroxypropyl cellulose exhibits a viscosity between 2 and 6 mPaS when tested as a 2% aqueous solution at 20.degree. C.; (iii) lactose; (iv) polyethylene glycol; and (v) optionally dye or pigment; and (d) at least one aesthetic coating surrounding the immediate release pioglitazone coating wherein the aesthetic coating is selected from the group consisting of a color coating, a polishing coating and a combination thereof; wherein not less than 95% of the pioglitazone is released from the pharmaceutical tablet within 30 minutes when tested according to the United States Pharmacopeia 26, with Apparatus 1 at 100 rpm, 37.degree. C. and 900 ml of 0.3 M KCl-HCl Buffer, pH 2.0 and after storage at 40.degree. C. and 75% relative humidity for 3 months the pharmaceutical tablet has a total of not more than 0.5% of the following pioglitazone impurities: (+/-)-5-[p-[2-(5-ethly.about.-2-pyridyl)ethoxy]benzyl]-5-hydroxy-2,4-thia- zolidinedione; (z)-5-[p-[2-(5-ethyl-2-pyridyl)ethoxy]benzylidene]-2,4-thiazolidinedione; (+/-)-5-[p-[2-(5-ethyl-2-pyridyl)ethoxy]benzyl]-3-[2-(5-ethyl-2-pyridyl)e- thyl]-2,4-thiazolidinedione; (+/-)-ethyl-2-carbamoyltio-3-[4-[2-(5-ethyl-2-pyridyl)ethoxy]phenyl]propi- onate; and ethyl-3-p-[2-(5-ethyl-2-pyridyl)ethoxy]phenyl-propionate as determined by high performance liquid chromatography and each of the pioglitazone impurities is present in an amount of not more than 0.20%.
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