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the oral administration of extended release formulation of galeeniline molsidomiini

机译:口服加雷尼林莫西多米尼缓释制剂

摘要

The present invention relates to a novel sustained-release oral galenical form of molsidomine for the treatment of all forms of angina attack (angina of effort, spastic angina, mixed angina). According to the invention, this novel galenical form contains a therapeutically effective amount of molsidomine or one of its active metabolites and has an in vitro dissolution rate [measured spectrophotometrically at 286 or 311 nm by the method described in the European Pharmacopoeia, 3rd edition (or USP XXIV), at 50 rpm, in 500 ml of a 0.1 N HCl medium, at 37° C.] of: 15 to 25% of molsidomine released after 1 hour, 20 to 35% of molsidomine released after 2 hours, 50 to 65% of molsidomine released after 6 hours, 75 to 95% of molsidomine released after 12 hours, 85% of molsidomine released after 18 hours and 90% of molsidomine released after 24 hours, the plasma peak of molsidomine obtained in vivo occurring 2.5 to 5 hours, preferably 3 to 4 hours, following the administration of said form, and having a value of between 25 and 40 ng/ml of plasma. Application: therapeutics industry.
机译:本发明涉及用于治疗所有形式的心绞痛发作(努力型心绞痛,痉挛性心绞痛,混合型心绞痛)的新型莫斯多明缓释口服盖仑制剂。根据本发明,这种新颖的盖仑制剂形式包含治疗有效量的molsidomine或其活性代谢物之一,并具有体外溶解速率[通过欧洲药典第3版(或USP XXIV),在37摄氏度下于500毫升0.1 N HCl介质中以50 rpm的转速在37℃下冲洗:1小时后释放15至25%的莫西多明,2小时后释放20至35%的莫西多明, 6小时后释放出65%的莫斯多明,12小时后释放出75-95%的莫斯多明,18小时后释放出> 85%的莫斯多明和24小时后释放出> 90%的莫斯多明,在体内获得的莫斯多明的血浆峰发生在2.5在施用所述形式后的1至5小时,优选3至4小时,并且血浆值为25至40ng / ml。应用:治疗行业。

著录项

  • 公开/公告号EE200200472A

    专利类型

  • 公开/公告日2003-12-15

    原文格式PDF

  • 申请/专利权人 THERABEL PHARMACEUTICALS LIMITED;

    申请/专利号EEP200200472

  • 发明设计人 JOZSEF-MICHEL GECZY;

    申请日2001-02-22

  • 分类号A61K9/20;A61K31/535;

  • 国家 EE

  • 入库时间 2022-08-21 23:11:13

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