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1.发明授权Inclusion complex of nicardipine or its hydrochloride with beta-cyclodextrin, a process for preparing the same and a sustained release pharmaceutical preparation containing the same 失效的尼卡地平的相同包合物或它与β-环糊精，用于制备和含有药物制剂这个延迟作用的过程盐酸盐。
公开(公告)号：EP0324982B1
公开(公告)日：1995-08-30
申请号：EP88121797.0
申请日：1988-12-28
发明人： Husu, Breda , Milovac, Jenny , Kopitar, Zdravko, D.Sc. , Huc, Branko, M.Sc. , Zmitek, Janko, M.Sc. , Bukovec, Peter, Prof. D. Sc. , Zorz, Mirjan, M.Sc. , Rusjakovski, Boris , Cvelbar, Polona, M.Sc. , Jerala-Strukelj, Zdenka , Kofler, Bojan
IPC分类号： A61K31/715 , A61K31/44 , C07D211/90
CPC分类号： B82Y5/00 , A61K31/44 , A61K47/6951 , C08B37/0015 , Y10S514/929 , Y10S514/964
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2.发明公开Inclusion complex of nicardipine or its hydrochloride with beta-cyclodextrin, a process for preparing the same and a sustained release pharmaceutical preparation containing the same 失效的尼卡地平的相同包合物或它与β-环糊精，用于制备和含有药物制剂这个延迟作用的过程盐酸盐。
公开(公告)号：EP0324982A1
公开(公告)日：1989-07-26
申请号：EP88121797.0
申请日：1988-12-28
发明人： Husu, Breda , Milovac, Jenny , Kopitar, Zdravko, D.Sc. , Huc, Branko, M.Sc. , Zmitek, Janko, M.Sc. , Bukovec, Peter, Prof. D. Sc. , Zorz, Mirjan, M.Sc. , Rusjakovski, Boris , Cvelbar, Polona, M.Sc. , Jerala-Strukelj, Zdenka , Kofler, Bojan
IPC分类号： A61K31/715 , A61K31/44 , C07D211/90
CPC分类号： B82Y5/00 , A61K31/44 , A61K47/6951 , C08B37/0015 , Y10S514/929 , Y10S514/964
摘要： There is described a new inclusion complex of nicardipine or its hydrochloride with beta-cyclodextrin, which is prepared by admixing nicardipine or its hydrochloride with beta-cyclodextrin in a molar ratio of the compounds 1:0.9-1.1 under stirring at a temperature from about room temperature to the boiling temprature of the reaction mixture in an aqueous or ethanolic medium, cooling the reaction mixture to 0 ° to 5 °C and isolating the desired complex.
The inclusion complex of nicardipine or its hydrochloride possesses cerebrovascular-vasodilatory and coronary-vasodilatory properties, which are equally well expressed as those of nicardipine or its hydrochloride themselves, yet owing to the better solubility of the complex at a higher pH range, such as it exists e.g. in the intestinal tract, the manufacture of sustained release pharmaceutical forms is made possible, whereby a greater extent of dissolution of the active substance is provided also in the intestinal juice.摘要翻译： 中描述尼卡地平的新包合配合物或它与β-环糊精盐酸盐，所有这一切是通过在化合物1的摩尔比混合尼卡地平或其盐酸与β-环糊精制备：0.9-1.1在温度从约室温下搅拌 温度至反应混合物的在wässrige或乙醇介质沸腾温度图，该反应混合物至0℃冷却至5℃，分离所需配合物。 尼卡地平的包合配合物或其盐酸具有脑血管-血管舒张和冠状动脉血管舒张性质，这是同等充分表达的那些尼卡地平或其盐酸本身，但由于在较高的pH范围内的复合物的更好的溶解性，求，因为它 如存在 在肠道中，持续释放的药物剂型的用途成为可能，由此，活性物质的溶解在更大程度上在肠液被设置。
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