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    • 3. 发明申请
    • METHOD FOR PRODUCING POWDERY PARTICLE-REDUCED FORMULATIONS WITH THE AID OF COMPRESSED GASES
    • 用于生产粉状颗粒减小的制剂使用压缩气体
    • WO0103671A3
    • 2001-05-10
    • PCT/EP0006709
    • 2000-07-13
    • SUEDDEUTSCHE KALKSTICKSTOFFHEIDLAS JUERGENOBER MARTINWIESMUELLER JOHANN
    • HEIDLAS JUERGENOBER MARTINWIESMUELLER JOHANN
    • A61K9/14A61K9/16B01J3/00
    • A61K9/14A61K9/1617Y10S514/959Y10S516/922Y10S516/928
    • The invention relates to the production of powdery particle-reduced formulations with the aid of compressed gases. The inventive method is characterized in that: the solid compound to be formulated, said compound consisting of a poorly soluble and mostly bioactive substance, is homogeneously comminuted together with 10-99 wt. % (with regard to the formulation) of a supporting material, which is essentially soluble in the compressed gas mixture, in an agitated autoclave provided with a mechanical comminution device in the presence of compressed gas or mixtures thereof, at method temperatures ranging from 10 to 200 DEG C, and under method pressures ranging from 5 to 500 bar, and, in a second method step; the compressed gas mixture, consisting mostly of dimethyl ether, pure propane and/or carbon dioxide, is expanded by lowering the pressure and is separated away from the homogenate that can also be provided in the form of a molten material. Finally, the powdery particle-reduced formulation is obtained from the resulting homogenate and exhibits significant improvements with regard to solubility properties and especially with regard to the biological availability of compounds which, initially, are poorly soluble or insoluble.
    • 对于具有压缩气体的辅助下粉状颗粒减小制剂的制备是要配制固体化合物,难溶的,并且通常的生物活性剂,连同10-99重量%(基于所述制剂)的载体材料的可溶于所述压缩气体混合物基本上, 在压缩气体,或它们的混合物与机械式粉碎机的搅拌高压釜中存在的情况下处理温度10至200℃,并在5和500之间的过程压力接地棒均匀,并且在第二处理阶段,压缩气体混合物,通常是二甲醚,纯丙烷和/或之间 二氧化碳,通过降低压力和匀浆其也可以作为熔体,分离放宽。 最后,从所得到的匀浆中回收,在粉粒降低制剂可以与释放性质的所指的改进,特别是重链和最初的非水溶性化合物的生物利用度来实现。
    • 6. 发明申请
    • METHOD FOR PRODUCING IMINODICARBOXYLIC ACIDS
    • 用于生产亚氨基二羧酸
    • WO0134560A3
    • 2001-12-13
    • PCT/EP0011092
    • 2000-11-09
    • SUEDDEUTSCHE KALKSTICKSTOFFGROEGER HARALDHAMMER BENEDIKT
    • GROEGER HARALDHAMMER BENEDIKT
    • C07C227/12C07C229/16
    • C07C227/12C07C229/16
    • The invention relates to a method for producing iminodicarboxylic acids by amidocarbonylating compounds of formula (I), wherein R = H, NH2, C1-28-alkyl, C6-12 aryl with carbon monoxide in the acidic medium and in the presence of a catalytic palladium complex and of an aldehyde as well as of the terminating hydrolytic cleavage of the N-acyl group. The inventive method is characterized in that the amidocarbonylation is carried out in a hydrous medium. Formamide, acetamide or urea are used as a particularly suitable starting material. Inorganic Pd(II) salts, such as palladium acetate or palladium chloride, or heterogeneous Pd catalysts are mainly used in mixtures containing a mineral acid and in quantities ranging from 0.01 to 0.25 mol %, whereby the catalytic system should contain, in particular, hydrobromic acid or hydrochloric acid. The invention also provides that the reaction is carried out in the presence of a maximum of 35 mol % of a halogenide salt.
    • 本发明是通过式(I),其中R = H,NH 2,C1-28烷基,C6-12芳基,与一氧化碳在在钯催化络合物的存在下,在酸性介质中,和化合物的酰胺基羰基的制备的亚氨基二羧酸的方法 醛和N-酰基基团,其特征在于,所述酰胺基羰基是在水性介质中进行的最终水解裂解。 一种特别合适的起始材料甲酰胺,可以使用乙酰胺或脲。 无机的Pd(II)盐,如乙酸或氯化钯,或钯多相催化剂主要用在用无机酸混合物,在0.01〜0.25摩尔%,其中所述催化体系的量,特别是溴 应包含或盐酸。 还提供的是在最大的存在下进行反应。 35摩尔%的卤化物盐。
    • 8. 发明申请
    • METHOD FOR PRODUCING OPTICALLY ACTIVE CYANHYDRINS
    • 生产光学活性氰氢的方法
    • WO0138554A3
    • 2001-12-27
    • PCT/EP0011743
    • 2000-11-24
    • SUEDDEUTSCHE KALKSTICKSTOFFGROEGER HARALDVORLOP KLAUS DIETERCAPAN EMINE
    • GROEGER HARALDVORLOP KLAUS-DIETERCAPAN EMINE
    • C12N11/08C12N11/10C12P13/00C12N9/88C12N11/00
    • C12P13/004C12N11/08C12N11/10C12Y401/0201
    • The invention relates to a method for producing optically active cyanhydrins by reacting oxo compounds, such as for example aldehyde and/or ketone with hydrogen cyanide and/or with a cyanide donor in the presence of an inclusion compound which contains an oxynitrilase with an increased molecular weight. According to said method, an oxynitrilase is used, whose molecular weight is first increased by cross-linkage and which is subsequently converted into a gel inclusion compound and/or a gel complex compound, said conversions occurring substantially in two independent steps. The method which is carried out in particular at temperatures of between - 10 and + 30 DEG C and at pH values of between 3.0 and 6.0, preferably in an aqueous or hydrous system, but also in organic solvents, uses a component which contains enzymes. In said component, the molecular-weight of the enzyme has been increased, in particular by co-cross-linkage or by flocculation and said enzyme is used either in a free form or is enclosed by natural or artificial cells. A deciding factor in this method is the fact that the enzyme is enclosed by or complexed in a gel, which results in negligibly small attrition and leaching losses at a practically constant high level of enzyme activity, rendering the method extremely effective and economic.
    • 公开了一种用于被氧化合物的反应的光学活性氰醇,如,醛和/或酮与氢氰化物和/或与一个包含molekuargewichtsvergrösserte氰醇,其中一个使用了氰醇的包合化合物的存在下,氰化物供体的制备方法, 其已经通过交联在两个独立步骤中基本上分子扩大,并随后转化为凝胶夹杂物和/或凝胶复合物化合物。 的方法,特别是,在之间的温度 - 10执行和+ 30℃,并以3.0至6.0的pH值,优选在含水或含水的系统中,而且在有机溶剂中,使用的酶 含有组分,其中所述酶本身是特别通过共交联或通过絮凝molekulargewichtsvergrössert并用于包括以游离形式或以天然或人工细胞。 关键在这个过程是酶被封装在凝胶或络合,使磨损小和浸出损失可以忽略不计在几乎不变的高酶活性,这使得该方法非常有效和经济的事实。
    • 9. 发明申请
    • FORMULATIONS FOR STATES OF DEHYDRATION
    • 配方脱水条件
    • WO0154676A2
    • 2001-08-02
    • PCT/EP0100863
    • 2001-01-26
    • SUEDDEUTSCHE KALKSTICKSTOFFGLOXHUBER CHRISTIANMERTSCHENK BERND
    • GLOXHUBER CHRISTIANMERTSCHENK BERND
    • A61K31/198A61P7/00A61K31/00
    • A61K31/198
    • Formulations for dehydration states are disclosed, which comprise creatine and/or creatine derivatives, such as creatine monohydrate, creatine ascorbate, and creatine pyruvate and/or mixtures thereof, in such quantities that the creatine components do not exceed a daily dose of 4g of creatine. Said formulations which are, most notably, available in the form of infusion solutions and drinks, but also as tablets, capsules and powders, are used, preferably in patients with dehydration states caused, in particular, by age and/or immobility and/or by a disturbed fluid uptake. Said formulations can also be applied in the framework of an adjutant therapy in dehydration states. Said formulations achieve not just a better and increased water uptake in the various body tissues, but also achieve a significantly longer storage of water in the tissue.
    • 描述的是用于脱水的条件制剂肌酸和/或肌酸衍生物如肌酸,肌酸抗坏血酸盐,肌酸丙酮酸和它们的任何混合物,其比例包含在特定使得肌酸组件不是肌酸4克的每日剂量 超过。 这些制剂,其主要存在于输注液和饮料的形式,也可作为片剂,胶囊和粉末在那些在特定年龄和/或immobilitätsbedingt和/或通过受损的液体摄入量导致患者脱水状态优选使用 ; 然而,所要求保护的制剂也可以作为在脱水条件下的辅助疗法的一部分。 用这些制剂,更好的和增强的水吸收到各种人体组织不仅实现新制剂的礼物也意味着组织水显著更长存储。