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1. 发明申请

WO0226263A3 STABLE SOLID DOSAGE FORMS OF AMINO ACIDS AND PROCESSES FOR PRODUCING SAME 审中-公开
标题翻译：氨基酸的稳定剂量形式及其生产方法
公开(公告)号：WO0226263A3
公开(公告)日：2003-01-03
申请号：PCT/US0130095
申请日：2001-09-26
申请人： SIGMAPHARM INC , SPIREAS SPIRIDON
发明人： SPIREAS SPIRIDON
IPC分类号： A61K9/16 , A61K31/195 , A61K9/20 , A61K47/00
CPC分类号： A61K9/1647 , A61K9/1694 , Y10S514/97
摘要： Pharmaceutical formulations, adn processes for making same, comprising an amino acid which is liable to formation of an undesirable lactam, and a stabilizer comprising a volatile alcohol; a non-volatile alcohol; a water immiscible liquid or solid; a liquid with a relatively low dielectric constant; a liquid surface active agent; a solid surface active agent; an antioxidant; a ketone, an aldehyde; a solid polyethylene glycol of high molecular weight; polyvinylpyrrolidone; a derived cellulose; silicon dioxide; or a combination thereof.
摘要翻译：药物制剂及其制备方法，其包含易于形成不合需要的内酰胺的氨基酸和包含挥发性醇的稳定剂; 不挥发性酒精; 与水不混溶的液体或固体; 具有较低介电常数的液体; 液体表面活性剂; 固体表面活性剂; 抗氧化剂酮，醛; 高分子量的固体聚乙二醇; 聚乙烯吡咯烷酮; 衍生的纤维素; 二氧化硅; 或其组合。

2. 发明申请

WO0228365A3 STABILIZATION OF SOLID DRUG FORMULATIONS 审中-公开
标题翻译：固体药物制剂的稳定化
公开(公告)号：WO0228365A3
公开(公告)日：2002-06-20
申请号：PCT/US0130093
申请日：2001-09-26
申请人： SIGMAPHARM INC , SPIREAS SPIRIDON
发明人： SPIREAS SPIRIDON
IPC分类号： A61K9/20 , A61K9/48
CPC分类号： A61K9/4858 , A61K9/2054 , A61K9/4816 , A61K9/485 , A61K9/4866
摘要： Pharmaceutical formulations and dosage forms are provided having improved stability to moisture-induced degradation when compared with conventional dosage forms, especially tablets. The invention features low compression forms of drugs known to be susceptible to moisture-induced degradation together with excipients, preferably in encapsulated forms. In other embodiments, relatively non-volatile oils can be admixed with the drug and/or the excipients to stabilize the formulation toward moisture-induced degradation. Hydrophobic powders are also optionally added to the formulations.
摘要翻译：提供了与常规剂型，尤其是片剂相比，具有改善的水分诱导降解稳定性的药物制剂和剂型。本发明的特征是低压缩形式的药物，其与赋形剂一起对水分引起的降解敏感，优选以包封形式存在。在其它实施方案中，可以将相对非挥发性的油与药物和/或赋形剂混合，以使制剂稳定于水分引起的降解。疏水粉末也可选地加入到配方中。

3. 发明申请

WO2004071526A1 STORAGE-STABLE AND BIO-STABLE FORMULATIONS OF ACE INHIBITORS, AND METHODS FOR PREPARATION THEREOF 审中-公开
标题翻译： ACE抑制剂的储存稳定和生物稳定配方及其制备方法
公开(公告)号：WO2004071526A1
公开(公告)日：2004-08-26
申请号：PCT/US2003/040132
申请日：2003-12-05
申请人： SIGMAPHARM, INC.
发明人： SPIREAS, Spiridon
IPC分类号： A61K38/55
CPC分类号： A61K9/1694 , A61K9/2054 , A61K9/2059 , A61K31/40 , A61K31/44 , A61K38/556
摘要： The present invention provides storage-stable and bio-stable formulations of ACE inhibitors, especially enalapril maleate and quinapril hydrochloride, that can be manufactured in a time efficient and cost effective manner. Such formulations can be prepared simply and on a large industrial scale using conventional methods and equipment. The present invention also provides methods for the preparation of highly manufacturable, storage-stable and bio-stable formulations of ACE inhibitors, especially enalapril maleate and quinapril hydrochloride. Methods for treatment of cardiovascular disorders using storage-stable and bio-stable formulations of ACE inhibitors, especially enalapril maleate and quinapril hydrochloride, are also provided.
摘要翻译：本发明提供ACE抑制剂的储存稳定和生物稳定的制剂，特别是马来酸依那普利和盐酸喹那普利，其可以以时间有效且具有成本效益的方式制造。可以使用常规方法和设备简单地并且在大型工业规模上制备这些制剂。本发明还提供了制备高度可制造，储存稳定和生物稳定的ACE抑制剂制剂，特别是马来酸依那普利和盐酸喹那普利的制剂的方法。还提供了使用ACE抑制剂的储存稳定和生物稳定制剂，特别是马来酸依那普利和盐酸喹那普利治疗心血管疾病的方法。

4. 发明申请

WO0228364A3 STABILIZATION OF SOLID THYROID DRUG FORMULATIONS 审中-公开
标题翻译：固体甲状腺药物制剂的稳定化
公开(公告)号：WO0228364A3
公开(公告)日：2002-06-06
申请号：PCT/US0129986
申请日：2001-09-26
申请人： SIGMAPHARM INC , SPIREAS SPIRIDON
发明人： SPIREAS SPIRIDON
IPC分类号： A61K9/20 , A61K9/48 , A61K31/198
CPC分类号： A61K9/485 , A61K9/2009 , A61K9/2054 , A61K9/4816 , A61K9/4858 , A61K9/4866 , A61K31/198
摘要： Pharmaceutical formulations and dosage forms are provided having improved stability to moisture-induced degradation when compared with conventional dosage forms, especially tablets. The invention features low compression forms of thyroid drugs together with excipients, preferably in encapsulated forms. In other embodiments, relatively non-volatile oils can be admixed with the drug and/or the excipients to stabilize the formulation toward moisture-induced degradation. Hydrophobic powders are also optionally added to the formulations.
摘要翻译：提供了与常规剂型，尤其是片剂相比，具有改善的水分诱导降解稳定性的药物制剂和剂型。本发明特征在于甲状腺药物与赋形剂一起的低压缩形式，优选以包封形式。在其它实施方案中，可以将相对非挥发性的油与药物和/或赋形剂混合，以使制剂稳定于水分引起的降解。疏水粉末也可选地加入到配方中。

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