Pharmaceutical formulation containing a biguanide and a thiazolidinedione derivative
View Patent ↗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.
1. A method for preparing a sustained release oral tablet comprising:
a) forming a controlled release metformin hydrochloride tablet comprising 500 mg to 1000 mg of metformin;
b) preparing an immediate release coating solution comprising:
i) pioglitazone hydrochloride;
ii) water;
iii) an organic solvent selected from the group consisting of acetone, isopropyl alcohol, methanol or ethanol;
iv) a binder;
v) optionally a surfactant;
vi) optionally a pore forming agent
wherein the ratio of water to organic solvent is 50:50 to 2:98 and the ratio of binder to pioglitazone hydrochloride is 1:9 to 1:11;
c) applying the immediate release coating solution to the controlled release metformin hydrochloride tablet so that when tested in a United States Pharmacopeia (USP) Type 2 apparatus at 75 rpm in 900 ml of simulated intestinal fluid (pH 7.5 phosphate buffer) and at 37° C., not less than 75% of the pioglitazone hydrochloride is released from the sustained release tablet in 30 minutes.
2. The method of claim 1 wherein not less than 95% of the pioglitazone hydrochloride is released from the sustained release tablet in 30 minutes.
3. The method of claim 1 wherein the sustained release tablet is prepared without a gelling polymer.
4. The method of claim 1 wherein the controlled release metformin hydrochloride tablet is formed by:
A) mixing the metformin hydrochloride with at least one pharmaceutically acceptable excipient;
B) compressing the mixture of step (A) into a tablet; and
C) coating the tablet of step (B) with a membrane.
5. A tablet prepared by the method of claim 1 .
6. A method for preparing a sustained release oral tablet comprising:
i) forming a controlled release metformin hydrochloride tablet comprising 500 mg to 1000 mg of metformin and without a gelling polymer comprising the steps of:
a) mixing the metformin hydrochloride with at least one pharmaceutically acceptable excipient;
b) compressing the mixture of step (a) into a tablet; and
c) coating the tablet of step (b) with a membrane;
ii) preparing an immediate release coating solution comprising:
a) pioglitazone hydrochloride;
b) water;
c) an organic solvent selected from the group consisting of acetone, isopropyl alcohol, methanol or ethanol;
d) a binder;
e) optionally a surfactant;
f) optionally a pore forming agent
wherein the ratio of water to organic solvent is 50:50 to 2:98 and the ratio of binder to pioglitazone hydrochloride is 1:9 to 1:11;
iii) applying the immediate release coating solution to the membrane of the controlled release metformin hydrochloride tablet so that when tested in a United States Pharmacopeia (USP) Type 2 apparatus at 75 rpm in 900 ml of simulated intestinal fluid (pH 7.5 phosphate buffer) and at 37° C., not less than 95% of the pioglitazone hydrochloride is released from the sustained release tablet in 30 minutes.
7. A tablet prepared by the method of claim 6 .