公开(公告)号：US5453280A

公开(公告)日：1995-09-26

申请号：US117285

申请日：1993-09-07

申请人： Thomas Moest ,  Uwe Loeffler ,  Hans Waiblinger

发明人： Thomas Moest ,  Uwe Loeffler ,  Hans Waiblinger

IPC分类号： A61K9/16 ,  A61K31/135 ,  A61K31/137 ,  A61K9/54 ,  B29B9/08 ,  B29B9/16

CPC分类号： A61K31/135 ,  A61K9/1688

摘要： A process for producing pellets which are markedly spherical and have a particle size in the range from 0.1 to 4 mm and an apparent density above 0.5 g/cm.sup.3, and which are composed of 90-100% by weight of an ephedrine derivative and 0-10% by weight of a pharmaceutical aid, entails suspending ephedrine derivative powder with an average particle size of from 0.5 to 50 .mu.m at 0.degree.-90.degree. C. with stirring in a water-immiscible non solvent with a boiling point in the range from 60.degree. to 160.degree. C., adding 5-60% by weight, based on the ephedrine derivative, of an agglomerating liquid while continuing stirring, and, if there has been previous heating, cooling to from -5 to 25.degree. C. at 5-40K per hour, with the stirring speed being adjusted after the agglomeration of the powder particles to a value which is necessary for the required average particle size, and removing and drying the resulting pellets. A drug which contains the active ingredient in the form of such pellets, with or without slowing of release, is also described.

摘要翻译： 一种制备显影球形，粒径为0.1〜4mm，表观密度为0.5g / cm 3以上的颗粒的方法，由90-100重量％的麻黄碱衍生物和0〜 10重量％的药物助剂，需要在0〜90℃下搅拌平均粒度为0.5〜50μm的麻黄碱衍生物粉末，在沸点范围内的不溶于水的非溶剂中搅拌 从60℃升至160℃，在连续搅拌的同时加入约5-60重量％的基于麻黄碱衍生物的附聚液，如果先前加热，冷却至-5〜25℃ 以每小时5-40K的速度调整粉末颗粒附聚后的搅拌速度至所需的平均颗粒尺寸所需的值，并除去和干燥所得的颗粒。 还描述了含有这种丸剂形式的活性成分的药物，其具有或没有减缓释放。

公开(公告)号：US5847216A

公开(公告)日：1998-12-08

申请号：US793458

申请日：1997-02-27

申请人： Silvia Ott-Dembrowski ,  Richard Cyrus ,  Jorg Schmidt ,  Hans Waiblinger

发明人： Silvia Ott-Dembrowski ,  Richard Cyrus ,  Jorg Schmidt ,  Hans Waiblinger

IPC分类号： C07C209/08 ,  C07C209/60 ,  C07C211/27 ,  C07C211/00

CPC分类号： C07C209/60

摘要： A process for preparing selegiline hydrochloride by reaction of R-(-)-N,.alpha.-dimethylphenylethylamine with 3-bromo-1-propyne is described, which consists in reacting the substances in a molar ratio of approximately 2:1 at 30.degree.-50.degree. C. in a solvent mixture of an aromatic hydrocarbon and water and isolating the selegiline from the organic phase and converting it into the hydrochloride.

摘要翻译： PCT No.PCT / EP95 / 03460 Sec。 371日期1997年2月27日 102（e）日期1997年2月27日PCT提交1995年9月2日PCT公布。 公开号WO96 / 08461 日期：1996年3月21日描述了通过R - （ - ） - N，α-二甲基苯乙胺与3-溴-1-丙炔反应来制备司来吉兰盐酸盐的方法，其中所述物质的摩尔比约为2： 1在30℃-50℃下在芳族烃和水的溶剂混合物中分离，并将其从有机相中分离并转化成盐酸盐。