Pharmaceutical compositions comprising Brivaracetam
View Patent ↗The present invention relates to a pharmaceutical composition comprising brivaracetam as active ingredient, the invention relates specifically to a prolonged release formulation.
1. A sustained release pharmaceutical composition comprising a core and, optionally, a coating, wherein the core comprises Brivaracetam as active ingredient and, as an excipient, at least one hydrophobic matrix agent or inert matrix agent in an amount that is 5% to 90% by weight of the composition, the matrix agent being a polymer which is a polymethacrylic acid derivative, or a non-polymer material which is a C8-C30 alcohol or lipid, or a non-polymer material having a melting point greater than 40° C., and wherein the composition is in solid form, and wherein the amount of Brivaracetam released in an in vitro buffered aqueous media (USP <711>Apparatus 2) is no more than 40% after 1 hour, 35%-80% after 4 hours, and no less than 80% after 16 hours.
2. The pharmaceutical composition according to claim 1 , wherein the non-polymer material has a melting point from 43° C. to 80° C.
3. The pharmaceutical composition according to claim 1 or 2 , wherein the matrix agent is a fatty acid from or contained in an animal or vegetable fat or oil.
4. The pharmaceutical composition according to claim 3 , wherein the fatty acid is hydrogenated palm oil, hydrogenated castor oil, hydrogenated cottonseed oil, stearic acid, palmitic acid, or a mixture thereof.
5. The pharmaceutical composition according to claim 1 , wherein the matrix agent is a C8-C30 monohydric alcohol.
6. The pharmaceutical composition according to claim 1 wherein the matrix agent is a wax.
7. The pharmaceutical composition according to claim 6 , wherein the wax is hydrogenated castor oil, glyceryl behenate, hydrogenated soybean oil, lauroyl macrogolglycerides, stearyl macrogolglycerides, glyceryl palmitostearate, glycerol esters of fatty acids, cetyl alcohol, or a mixture thereof.