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Combination of levodopa / carbidopa immediate release and controlled release dosage forms
专利权人:
INC.;IMPAX LABORATORIES
发明人:
HAN, Chien-Hsuan,HSU, Larry,HSU, Ann
申请号:
ES03756204
公开号:
ES2606463T3
申请日:
2003.05.23
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
Pharmaceutical dosage form having an immediate release component and a controlled release component, comprising: a) an immediate release component that includes a carbidopa: levodopa ratio of 1: 1 to 1: 5 and a disintegrant so that the In vitro dissolution rate of the immediate release component, according to measurements made using the 50 rpm USP paddle method in 900 ml of aqueous buffer at pH 4.37 ° C, is 10% to 99% of levodopa released after 15 minutes and 75% to 99% after 1 hour, the immediate release component comprising immediate release particles; and b) a controlled release component comprising controlled release particles with a diameter of 0.001 to 5.0 mm, including controlled release particles between 10 and 200 mg of carbidopa; between 25 and 600 mg of levodopa; the carbidopa: levodopa ratio being 1: 1 to 1: 5; and a retardant coating comprising a hydrophobic or hydrophilic material, such that the in vitro dissolution rate of the controlled release component, according to measurements made by the 50 rpm USP vane method in 900 ml of aqueous buffer at pH 4 , 37 ° C, is 10% to 60% of levodopa released after 1 hour; from 20% to 80% of levodopa released after 2 hours; and from 30% to 99% of levodopa released after 6 hours, the in vitro release rate being chosen such that the peak of initial levodopa plasma level obtained in vivo occurs between 0.1 and 2 hours after administration. of the dosage form to a patient and a controlled release profile over a period of 3, 4, 6, 8, 12 or 24 hours.Forma de dosificación farmacéutica que tiene un componente de liberación inmediata y un componente de liberación controlada, que comprende: a) un componente de liberación inmediata que incluye una relación carbidopa:levodopa de 1:1 a 1:5 y un disgregante de modo que la tasa de disolución in vitro del componente de liberación inmediata, de acuerdo con mediciones realizadas mediante el método de paleta USP de 50 rpm en 900 ml de tampón acuoso a pH 4, 37ºC, es del 10% al 99% de
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