초록

The invention relates to new formulations for improving the local tolerance of intravenously administered 4-(4-(2-pyrrolylcarbonyl)-1-piperazinyl)-3-trifluoromethyl-benzoylguanidine or one of the pharmacologically acceptable acid addition salts thereof.

대표청구항 ▼

We claim: 1. A pharmaceutical composition comprising a mixture or a complex, or both, of 4-(4-(2-pyrrolylcarbonyl)-1-piperazinyl)-3-trifluoromethyl-beazoylguanidine, or one of the pharmacologically acceptable acid addition salts thereof, and a pharmacologically acceptable cyclodextrin. 2. A pharm

We claim: 1. A pharmaceutical composition comprising a mixture or a complex, or both, of 4-(4-(2-pyrrolylcarbonyl)-1-piperazinyl)-3-trifluoromethyl-beazoylguanidine, or one of the pharmacologically acceptable acid addition salts thereof, and a pharmacologically acceptable cyclodextrin. 2. A pharmaceutical composition according to claim 1, wherein the pharmacologically acceptable cyclodextrin is HPβCD. 3. A pharmaceutical composition according to claim 1, wherein the cyclodextrin improves the local tolerance of 4-(4-(2-pyrrolylcarbonyl)-1-piperazinyl)-3-trifluoromethyl-benzoylguanidine or one of the pharmacologically acceptable acid addition salts thereof. 4. A pharmaceutical composition according to claim 1, in a form suitable for intravenous administration. 5. A pharmaceutical composition according to claim 4, wherein the 4-(4-(2-pyrrolylcarbonyl)-1-piperazinyl)-3-trifluoromethyl-benzoylguanidine, or one of the pharmacologically acceptable acid addition salts thereof, is present in a concentration of between 0.6 mg/ml and 40 mg/ml. 6. A method for treating acute myocardial infarction in a patient, comprising administering to said patient a therapeutically effective amount of a pharmaceutical composition according to claim 1. 7. A method for treating of perioperative myocardial necrosis in a patient undergoing a coronary artery bypass operation, comprising administering to said patient a pharmaceutical composition according to claim 1. 8. A pharmaceutical composition comprising a mixture or a complex, or both, of 4-(4-(2-pyrrolylcarbonyl)-1-piperazinyl)-3-trifluoromethyl-beuzoylguanidine, or one of the pharmacologically acceptable acid addition salts thereof, a pharmacologically acceptable cyclodextrin and a hydroxy acid. 9. A pharmaceutical composition according to claim 8, wherein the pharmacologically acceptable cyclodextrin is HPβCD. 10. A pharmaceutical composition according to claim 9, wherein the hydroxy acid is malic acid, acetic acid, lactic acid, tartaric acid or citric acid. 11. A pharmaceutical composition according to claim 10, where the hydroxy acid is citric acid. 12. A pharmaceutical composition according to claim 8, wherein the cyclodextrin and hydroxy acid improve the local tolerance of 4-(4-(2-pyrrolylcarbonyl)-1-piperazinyl)-3-trifluoromethyl-benzoylguanidine or one of thepharmacologically acceptable acid addition salts thereof. 13. A pharmaceutical composition according to claim 8, in a form suitable for intravenous administration. 14. A pharmaceutical composition according to claim 13, wherein the 4-(4-(2-pyrrolylcarbonyl)-1-piperazinyl)-3-trifluoromethyl-benzoylguanidine, or one of the pharmacologically acceptable acid addition salts thereof, is present in a concentration of between 0.6 mg/ml and 40 mg/ml. 15. A method for treating acute myocardial infarction in a patient, comprising administering to said patient a therapically effective amount of a pharmaceutical composition according to claim 8. 16. A method for treating of perioperative myocardial necrosis in a patient undergoing a coronary artery bypass operation, comprising administering to said patient a pharmaceutical composition according to claim 8.