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1. (WO1991008766) STABILIZATION OF t-PA pro
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1991/008766 International Application No.: PCT/EP1990/002251
Publication Date: 27.06.1991 International Filing Date: 19.12.1990
IPC:
A61K 38/49 (2006.01) ,A61K 47/12 (2006.01) ,A61K 47/18 (2006.01) ,A61K 47/22 (2006.01) ,A61K 47/26 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38
Medicinal preparations containing peptides
16
Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
43
Enzymes; Proenzymes; Derivatives thereof
46
Hydrolases (3)
48
acting on peptide bonds (3.4)
49
Urokinase; Tissue plasminogen activator
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
06
Organic compounds
08
containing oxygen
12
Carboxylic acids; Salts or anhydrides thereof
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
06
Organic compounds
16
containing nitrogen
18
Amines; Quaternary ammonium compounds
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
06
Organic compounds
22
Heterocyclic compounds
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
06
Organic compounds
26
Carbohydrates
Applicants:
BOEHRINGER MANNHEIM GMBH [DE/DE]; Sandhofer Straße 112-132 D-6800 Mannheim-Waldhof, DE (AllExceptUS)
KOHNERT, Ulrich [DE/DE]; DE (UsOnly)
RUDOLPH, Rainer [DE/DE]; DE (UsOnly)
Inventors:
KOHNERT, Ulrich; DE
RUDOLPH, Rainer; DE
Agent:
WEICKMANN, H. ; Möhlstraße 22 D-8000 München 80, DE
Priority Data:
P 39 42 143.020.12.1989DE
Title (DE) t-PA pro STABILISIERUNG
(EN) STABILIZATION OF t-PA pro
(FR) STABILISATION DE t-PA pro
Abstract:
(DE) Pharmazeutisches Präparat eines nicht glykosylierten t-PA mit einer enzymatischen Akivität von mindestens 0,1 MU/ml und einem pH-Wert von 4,5 bis 6, das Citrat und mindestens eine Verbindung aus der aus: a) Ascorbinsäure; b) EDTA; c) Aminoverbindungen der Formel: R1R2N - R - X, wobei X = SO3H, CH(NH2)-CO2H, CO2H, H, NH2 oder OH ist, R = C1-C9-Alkylen, C3-C6-Cycloalkylen oder Benzyliden ist und R1 und R2 voneinander unabhängig H oder C1-C3-Alkyl sind; d) Guanidinobuttersäure; e) Dimethylbiguanid; f) Arginin; g) glucosamin, Fructose; h) Pyrimidinnukleosiden und Pyrimidinnukleotiden; i) mit einer oder mehreren Hydroxy-, Keto- oder/und weiteren Carboxygruppen substituierte Carbonsauren bestehenden Gruppe enthält, sowie ein Arzneimittel auf Basis eines nicht glykosylierten t-PA als Wirkstoff und Verfahren zu seiner Herstellung.
(EN) The invention relates to a pharmaceutical preparation of a non-glycosylized t-PA with an enzymatic activity of at least 0.1 MU/ml and a pH of 4.5 to 6, containing citrate and at least one compound from the following group: a) ascorbic acid; b) EDTA; c) amino compounds of formula: R1R2N - R - X, where X = SO3H, CH(NH2)-CO2H, CO2H, H, NH2 or OH, R = C1-C9 alkylene, C3-C6 cycloalkylene or benzylidene and R1 and R2, independently of each other, are H or C1-C3 alkyl; d) guanidinobutyric acid; e) dimethylbiguanide; f) arginine; g) glucosamine, fructose; h) pyrimidine nucleosides and pyrimidine nucleotides; i) carboxylic acids substituted with one or more hydroxyl, keto and/or further carboxyl groups. The invention also relates to a drug based on a non-glycosylized t-PA as the active ingredient and a process for producing it.
(FR) Une composition pharmaceutique d'un t-PA non glycosylé, ayant une activité enzymatique d'au moins 0,1 MU/ml et une valeur de pH comprise entre 4,5 et 6, contient du citrate et au moins un composé du groupe formé par: a) l'acide ascorbique; b) l'EDTA; c) des composés amine ayant la formule: R1R2N - R - X, dans laquelle X = SO3H, CH(NH2)-CO2H, CO2H, H, NH2 ou OH, R = C1-C9-alkylène, C3-C6-cycloalkylène ou benzylidène et R1 et R2 représentent indépendamment l'un de l'autre H ou C1-C3-alkyle; d) l'acide guanidinobutyrique; e) la diméthylbiguanide; f) l'arginine; g) la glucosamine, le fructose; h) des nucléosides et des nucléotides de pyrimidine; i) des acides carboxyliques substitués par un ou plusieurs groupes hydroxyles, cétoniques et/ou des groupes carboxyles additionnels. L'invention concerne également un médicament à base d'un t-PA non glycosylé comme principe actif et son procédé de production.
Designated States: AU, CA, FI, HU, JP, KR, NO, SU, US
European Patent Office (AT, BE, CH, DE, DK, ES, FR, GB, GR, IT, LU, NL, SE)
Publication Language: German (DE)
Filing Language: German (DE)
Also published as:
FI913909NO19913118EP0458939US5352453JPH03505465CA2046929
KR1019920700684AU1991070375