公开(公告)号：US5705192A

公开(公告)日：1998-01-06

申请号：US618790

申请日：1996-03-20

申请人： Horst Bethge ,  Kurt Klostermann ,  Roland Moller ,  Gerhard Sator

发明人： Horst Bethge ,  Kurt Klostermann ,  Roland Moller ,  Gerhard Sator

IPC分类号： C07D339/04 ,  A61K9/16 ,  A61K9/20 ,  A61K31/385 ,  A61K9/14

CPC分类号： A61K9/1688 ,  A61K31/385

摘要： 1. A method of producing flowable R,S-thioctic acid, R,S-thioctic acid and its use. 2.1. Known methods of preparing flowable thioctic acid which can be galenically further processed by pressing to highly-concentrated, solid presentations with active-substance contents of more than 200 mg pure substance require the mixing of the thioctic-acid forms of different origins and/or a spraying on of galenic adjuvants from aqueous solution and a subsequent grinding process in order to arrive at a pressable granulate. 2.2. As a result of the fact that thioctic acid of any origin is placed in the fluid bed of a device suited for producing a fluid bed and that a built-up granulate consisting of thioctic acid is obtained by spraying a solution of thioctic acid of any origin onto the matter placed in the fluid bed under simultaneous removal of the solvent, it is possible to make a thioctic-acid form available which does not adhere to the pressing tool or exhibit a tendency to form fissures on the tablet even when tablets with 600 mg or more active-substance content are prepared. The novel R,S-thioctic acid has a specific surface of >0.7 m.sup.2 /g and a number of mesopores with a diameter between 2 and 30 nm.

摘要翻译： 1.生产可流动的R，S-硫辛酸，R，S-硫辛酸及其用途的方法。 2.1。 制备可流动的硫辛酸的已知方法，其可以通过压制具有超过200mg纯物质的活性物质含量的高浓度固体表现物进一步加工而进一步加工，需要混合不同来源的硫辛酸形式和/或 从水溶液中喷洒盖仑佐剂并随后进行研磨处理以得到可挤压颗粒。 2.2。 由于任何来源的硫辛酸被放置在适于生产流化床的装置的流化床中，并且由硫辛酸组成的积层颗粒通过喷洒任何起源的硫辛酸溶液而获得 在同时除去溶剂的情况下放置在流化床中的物质上，可以制备硫辛酸形式，其不粘附到压制工具上，或者表现出在片剂上形成裂缝的趋势，即使具有600mg 或更多的活性物质含量。 新型R，S-硫辛酸具有> 0.7m 2 / g的比表面积和直径在2和30nm之间的多个中孔。

公开(公告)号：US4827029A

公开(公告)日：1989-05-02

申请号：US146637

申请日：1988-01-21

申请人： Axel Kleemann ,  Kurt Klostermann ,  Wolfgang Leuchtenberger ,  Rudi E. Moerck ,  Michael Karrenbauer

发明人： Axel Kleemann ,  Kurt Klostermann ,  Wolfgang Leuchtenberger ,  Rudi E. Moerck ,  Michael Karrenbauer

IPC分类号： B01J39/26 ,  C07C227/34 ,  C07C227/40 ,  C07C229/02 ,  C07C319/28 ,  C07C323/58 ,  C12P13/04 ,  C07C99/12

CPC分类号： C12P13/04

摘要： L-amino acids present in cleavage solutions obtained in the acylase-catalyzed cleavage of N-acetyl-D,L-amino acids are isolated by use of a strongly acidic ion exchanger in H+ form. First, the mother liquor from a previous treatment cycle is fed to the ion exchanger, and then the cleavage solution and finally the wash water and the discharge from the ion exchanger which is pH-controlled is analyzed into an "effluent water fraction", an "N-acetyl-D-amino acid fraction" and an "L-amino acid fraction". The last fraction is adjusted by addition of fresh cleavage solution to a pH of between 4.0 and 6.0, and from the mixture which is thus obtained the L-amino acid is isolated by crystallization. The mother liquor which is obtained is recycled back into a subsequent treatment cycle.

摘要翻译： 通过使用H +形式的强酸性离子交换剂分离存在于酰基转移酶催化的N-乙酰基-D，L-氨基酸切割中获得的切割溶液中的L-氨基酸。 首先，将来自先前处理循环的母液进料到离子交换器中，然后将分离溶液，最后洗涤水和从pH离子交换器排出的pH值控制分析为“流出水分数”， “N-乙酰基-D-氨基酸级分”和“L-氨基酸级分”。 通过将新鲜裂解溶液加入至4.0至6.0的pH来调节最后的级分，并且由此得到的混合物通过结晶分离L-氨基酸。 将获得的母液循环回到随后的处理循环中。