Pharmaceutical composition for treating parkinson's disease and preparation method thereof
AssigneeInnopharmax, Inc.
InventorsWeihua Hao, Jongjing Wang, Huiyun Chen
Life of this patent
Estimating the term…
Abstract
A pharmaceutical composition used to treat Parkinson's disease contains levodopa, carbidopa and entacapone or pharmaceutically acceptable salt thereof, and at least one kind of pharmaceutically acceptable excipients. Entacapone is not mixed with levodopa or carbidopa in the pharmaceutical composition. The preparation method of the pharmaceutical composition includes making the first particles with levodopa and carbidopa, making the second particles with entacapone, and then pressing the two kinds of particles into tablets.
Claims22
An oral solid pharmaceutical composition for treating Parkinson's disease, comprising first granules that comprise 25-300 milligrams of levodopa and 5-75 milligrams of carbidopa but that do not comprise entacapone, and
- second granules that comprise a binder that binds particles
- which comprise sodium dodecyl sulfate (SDS) and 25-300 milligrams of entacapone,
- which do not comprise levodopa or carbidopa, and
- which comprise entacapone particles having a diameter of at least about 150 micrometers,
- wherein
- the size of the particles,
- the identity of the binder, and
- the amounts of the binder, entacapone, and SDS in the second granules are selected such that when the composition is assessed using a modification of USP levodopa/carbidopa/entacapone dissolution method USP 32, NF27 (1791) in which the USP standard basket with a rotation speed of 125 rotations per minute and 900 milliliters of pH 5.5 phosphate buffer solution are used, the time required for 90% of the entacapone to dissolve in the buffer solution is greater than about 25 minutes, but not more than about 80 minutes.
A method for preparing an oral solid pharmaceutical composition for treating Parkinson's disease, the method comprising
- (a) mixing levodopa, carbidopa and a first excipient to obtain a first mixture;
- (b) granulating the first mixture to obtain first granules that do not contain entacapone;
- (c) mixing entacapone, a binder, and SDS to obtain a second mixture;
- (d) granulating the second mixture to obtain second granules in which the binder binds particles
- which comprise entacapone and SDS,
- which do not comprise levodopa or carbidopa, and
- which comprises entacapone particles having a diameter of at least about 150 micrometers;
- wherein
- the size of the particles,
- the identity of the binder, and
- the amounts of the binder, entacapone, and SDS in the second granules
- are selected such that when the composition is assessed using a modification of USP levodopa/carbidopa/entacapone dissolution method USP 32, NF27 (1791) in which the USP standard basket with a rotation speed of 125 rotations per minute and 900 milliliters of pH 5.5 phosphate buffer solution are used, the time required for 90% of the entacapone to dissolve in the buffer solution is greater than about 25 minutes, but not greater than about 80 minutes and
- (e) compressing first and second granules into a tablet.
Dependencies are inferred from the claim text.