| 摘要 |
#CMT# #/CMT# Solid pharmaceutical dosage form comprises a core comprising levetiracetam (I), a water-soluble polymer and a lubricant and a coating that is semipermeable to water. The dosage form contains 75-96 wt.% (I). #CMT# : #/CMT# An independent claim is also included for producing the dosage form by preparing a core comprising (I), a solution for wetting (I) and a lubricant, and coating the core. #CMT#ACTIVITY : #/CMT# Anticonvulsant. #CMT#MECHANISM OF ACTION : #/CMT# None given. #CMT#USE : #/CMT# The dosage form is useful for treating epilepsy (claimed). #CMT#ADVANTAGE : #/CMT# The dosage form provides sustained release of (I). #CMT#PHARMACEUTICALS : #/CMT# Preferred Dosage Form: (I) is present in an amount of 80-96% by weight of the dosage form and 90-98% by weight of the core. The polymer is polyvinylpyrrolidone or hydroxypropyl methylcellulose and is present in an amount of 1-10% by weight of the core. The lubricant is magnesium stearate or sodium stearyl fumarate and is present in an amount of 0.5-5% by weight of the core. The dosage form can also include a flow improver, e.g. colloidal silica, in an amount of 0.1-1% by weight of the core. The coating makes up 3-15% of the weight of the dosage form. Preferred Coating: This comprises 30-90 wt.% of a water-insoluble polymer (P1), especially ethyl cellulose, and 10-40 wt.% of a water-soluble polymer (P2), especially polyvinylpyrrolidone or hydroxypropyl methylcellulose. The P1:P2 ratio is 1-5:1. The coating can also include a plasticizer, especially polyethylene glycol or propylene glycol, in an amount of 5-25 wt.%. #CMT#EXAMPLE : #/CMT# Tablets with cores comprising levetiracetam (500 mg), polyvinylpyrrolidone (15 mg) and sodium stearyl fumarate (5 mg) and a coating comprising ethyl cellulose (25 mg), polyvinylpyrrolidone (6.5 mg) and polyethylene glycol 1500 (7 mg) had the following dissolution profile in 0.1 N hydrochloric acid: 8% after 2 hours, 27% after 4 hours, 67% after 8 hours, 79% after 10 hours, 97% after 16 hours, 100% after 20 hours. |
