摘要 |
The invention relates to a pharmaceutical preparation of a non-glycosylized t-PA derivative, K2P pro, with an enzymatic activity of at least 1.4 MU/ml and a pH of 4.5 to 6.5, containing citrate and at least one compound from the following group: a) ascorbic acid, b) EDTA, c) amino compounds of formula R<1>R<2>N - R - X, where X = SO3H, CH(NH2)-CO2H, CO2H, H, NH2 or OH, R = C1-C9 alkylene, preferably C4-C7 alkylene, C3-C6 cycloalkylene or benzylidene and R<1> and R<2>, independently of each other, are H or C1-C3 alkyl, d) guianidine analogs of formula (II), where Y = H2N+ or 0, Z = H or (CH2)m V, (CH2)mCH(NH2)-CO2H, CH(CO2H)-(CH2)mCO2H, V = NH2 or CO2H and m = 1 to 4, e) carboxylic acids substituted with one or more hydroxyl, keto and/or further carboxyl groups, f) dimethylbiguanide, g) pyrimidine nucleosides and pyrimidine nucleotides, h) trehalose, glucosamine. The invention also relates to a drug based on the t-PA derivative K2P pro as the active ingredient and a process for producing it.
|
申请人 |
BOEHRINGER MANNHEIM GMBH, 6800 MANNHEIM, DE |
发明人 |
KOHNERT, ULRICH, DIPL.-CHEM. DR.RER.NAT., 8121 HABACH, DE;RUDOLPH, RAINER, DIPL.-CHEM. DR.RER.NAT., 8120 WEILHEIM, DE |