Sustained Release Pharmaceutical Compositions for Highly Water Soluble Drugs
The present invention provides pharmaceutical compositions for controlled release of pharmaceutically active agents, especially those with a high water solubility, high dose, and/or short half-life. In addition, the present application provides methods for preparing and using such pharmaceutical compositions.
1 . A sustained release pharmaceutical tablet, said tablet comprising:
tramadol micronized at a dose selected from the group consisting of 90 mg, 180 mg, 300 mg and 600 mg;
a matrix comprising hydroxypropylmethyl cellulose (HMPC) and the micronized tramadol dispersed in the matrix;
microcrystalline cellulose; and
a tablet lubricant.
2 . The pharmaceutical tablet of claim 1 , wherein the pharmaceutically active agent contributes greater than 15% of the total weight of the pharmaceutical composition.
3 . The pharmaceutical tablet of claim 1 , wherein the pharmaceutically active agent contributes greater than 50% of the total weight of the pharmaceutical composition.
4 . The pharmaceutical tablet of claim 1 , wherein the pharmaceutically active agent is present in an amount of about 50% to about 80% by weight.
5 . The pharmaceutical tablet of claim 1 , wherein the hydrophilic polymer is present in an amount of about 15% to about 50% by weight.
6 . The pharmaceutical tablet of claim 1 , wherein the HPMC is a high molecular weight HPMC in an amount of about 20% to about 30% by weight of the tablet.
7 . The pharmaceutical tablet of claim 1 , wherein the tableting lubricant is present in an amount of about 1% to about 3% by weight of the tablet.
8 . The pharmaceutical tablet of claim 7 , wherein the tablet lubricant is magnesium stearate.
9 . The pharmaceutical tablet of claim 1 , further comprising a coating on the tablet.
10 . The pharmaceutical tablet of claim 9 , wherein said coating is a release-controlling layer.
11 . The pharmaceutical tablet of claim 9 , wherein said coating constitutes about 1% to about 5% by weight of the tablet.
12 . The pharmaceutical tablet of claim 9 , wherein said tablet is coated with a layer of film containing ethyl cellulose.
13 . The pharmaceutical tablet of claim 9 , wherein the tramadol dose is 90 mg.
14 . The pharmaceutical tablet of claim 9 , wherein the tramadol dose is 180 mg.
15 . The pharmaceutical tablet of claim 9 , wherein the tramadol dose is 300 mg.
16 . The pharmaceutical tablet of claim 9 , wherein the tramadol dose is 600 mg.
17 . A method for reducing pain in an animal, said method comprising:
administering a tramadol micronized tablet at a dose selected from the group consisting of 90 mg, 180 mg, 300 mg and 600 mg or a fragment thereof, said tablet comprising a matrix comprising hydroxypropylmethyl cellulose (HMPC) and the micronized tramadol dispersed in the matrix;
microcrystalline cellulose; and
a tablet lubricant, to reduce pain in the animal.
18 . The method of claim 17 , wherein the tramadol dose is 180 mg.
19 . The method of claim 17 , wherein the tramadol dose is 300 mg.
20 . The method of claim 17 , wherein the tramadol dose is 600 mg.