公开(公告)号：US06419953B1

公开(公告)日：2002-07-16

申请号：US09216650

申请日：1998-12-18

申请人： Yihong Qiu ,  Paul Richard Poska ,  Howard S. Cheskin ,  J. Daniel Bollinger ,  Robert K. Engh

发明人： Yihong Qiu ,  Paul Richard Poska ,  Howard S. Cheskin ,  J. Daniel Bollinger ,  Robert K. Engh

IPC分类号： A61K920

CPC分类号： A61K9/2054 ,  A61K9/2009 ,  A61K9/2018 ,  A61K31/19

摘要： The present invention pertains to a hydrophilic matrix tablet suitable for the once-a-day administration of valproate compounds such as divalproex sodium. The tablet comprises from about 50 weight percent to about 55 weight percent of an active ingredient selected from the group consisting of valproic acid, a pharmaceutically acceptable salt or ester of valproic acid, divalproex sodium, and valpromide; from about 20 weight percent to about 40 weight percent hydroxypropyl methylcellulose; from about 5 weight percent to about 15 weight percent lactose, from about 4 weight percent to about 6 weight percent microcrystalline cellulose, and from about 1 weight percent to about 5 weight percent of silicon dioxide; all weight percentages based upon the total weight of the tablet dosage form. Other aspects of the invention relate to the use of this formulation in the treatment of epilepsy and to methods for manufacturing this dosage form.

摘要翻译： 本发明涉及一种适用于丙戊酸酯化合物例如双丙戊酸钠一天一次给药的亲水性基质片剂。 片剂包含约50重量％至约55重量％的选自丙戊酸，丙戊酸的药学上可接受的盐或酯，双丙戊酸钠和伏立康胺的活性成分; 约20重量％至约40重量％的羟丙基甲基纤维素; 约5重量％至约15重量％的乳糖，约4重量％至约6重量％的微晶纤维素和约1重量％至约5重量％的二氧化硅; 所有重量百分比均基于片剂剂型的总重量。 本发明的其它方面涉及该制剂在治疗癫痫中的用途以及制备该剂型的方法。

公开(公告)号：US06528091B1

公开(公告)日：2003-03-04

申请号：US10143559

申请日：2002-05-10

申请人： Yihong Qiu ,  Paul Richard Poska ,  Howard S. Cheskin ,  J. Daniel Bollinger ,  Robert K. Engh

发明人： Yihong Qiu ,  Paul Richard Poska ,  Howard S. Cheskin ,  J. Daniel Bollinger ,  Robert K. Engh

IPC分类号： A61K920

CPC分类号： A61K9/2054 ,  A61K9/2009 ,  A61K9/2018 ,  A61K31/19

摘要： A controlled release tablet formulation which permits once daily dosing in the treatment of epilepsy comprises from about 50 weight percent to about 55 weight percent of an active ingredient selected from the group consisting of valproic acid, a pharmaceutically acceptable salt or ester of valproic acid, divalproex sodium, and valpromide; from about 20 weight percent to about 40 weight percent hydroxypropyl methylcellulose; from about 5 weight percent to about 15 weight percent lactose, from about 4 weight percent to about 6 weight percent microcrystalline cellulose, and from about 1 weight percent to about 5 weight percent silicon dioxide having an average particle size ranging between about 1 micron and about 10 microns; all weight percentages based upon the total weight of the tablet dosage form. Also disclosed are pre-tableting granular formulations, methods of making the granular formulations and tablets, and a method of treating epilepsy employing the controlled release tablet formulations of the invention.

摘要翻译： 允许每日一次给药治疗癫痫的控释片剂制剂包含约50重量％至约55重量％的活性成分，选自丙戊酸，丙戊酸的药学上可接受的盐或酯，双丙戊酸 钠和valpromide; 约20重量％至约40重量％的羟丙基甲基纤维素; 约5重量％至约15重量％的乳糖，约4重量％至约6重量％的微晶纤维素和约1重量％至约5重量％的二氧化硅，平均粒度范围介于约1微米至约 10微米; 所有重量百分比均基于片剂剂型的总重量。 还公开了预压片颗粒制剂，制备颗粒制剂和片剂的方法，以及使用本发明的控释片剂制剂治疗癫痫的方法。