Pharmaceutical Composition for the Parenteral Administration of Ultrashort-Effective Beta-Adrenoreceptor Antagonists

Abstract

The present invention relates to a pharmaceutical composition in the form of a storage-stable solution for the parenteral administration of ultrashort-effective β-adrenoreceptor antagonists, comprising a) an ultrashort-effective β-adrenoreceptor antagonist and/or a pharmaceutically acceptable salt thereof, b) water, and c) a cyclodextrin and/or a functional cyclodextrin derivative. The composition according to the invention has high stability, even without the presence of additional adjuvants.

What is claimed: 
     
         1 . A pharmaceutical composition comprising:
 a) landiolol or a pharmaceutically acceptable salt thereof;   b) water; and   c) β-cyclodextrin or a functional cyclodextrin derivative.   
     
     
         2 . The pharmaceutical composition of  claim 1 , wherein the pH value of the composition is 3 to 7.5. 
     
     
         3 . The pharmaceutical composition of  claim 2 , wherein the pH value of the composition is 5 to 7. 
     
     
         4 . The pharmaceutical composition of  claim 1 , wherein the concentration of the β-cyclodextrin or the functional cyclodextrin derivative is 0.1% to 20% (w/v). 
     
     
         5 . The pharmaceutical composition of  claim 1 , wherein the concentration of the β-cyclodextrin or the functional cyclodextrin derivative is 0.4 to 5% (w/v). 
     
     
         6 . The pharmaceutical composition of  claim 1 , wherein the functional cyclodextrin derivative is (2-hydroxypropyl)-β-cyclodextrin. 
     
     
         7 . The pharmaceutical composition of  claim 1 , wherein the concentration of landiolol or the pharmaceutically acceptable salt thereof is 0.1% to 30%. 
     
     
         8 . The pharmaceutical composition of  claim 1 , wherein the concentration of landiolol or the pharmaceutically acceptable salt thereof is 0.25%. 
     
     
         9 . The pharmaceutical composition of  claim 1 , wherein the composition has an osmolarity of 270 mosmol/l to 310 mosmol/l. 
     
     
         10 . The pharmaceutical composition of  claim 9 , wherein the composition has an osmolarity of 280 mosmol/l to 300 mosmol/l. 
     
     
         11 . The pharmaceutical composition of  claim 1 , wherein the composition is present in the form of a sales unit selected from the group consisting of: a 1 ml solution containing 5-20 mg landiolol or a pharmaceutically acceptable salt thereof, a 2 ml solution containing 5-100 mg landiolol or a pharmaceutically acceptable salt thereof, a 5 ml solution containing 10-500 mg landiolol or a pharmaceutically acceptable salt thereof, a 10 ml solution containing 10-5000 mg landiolol or a pharmaceutically acceptable salt thereof, a 25 ml solution containing 25-2500 mg landiolol or a pharmaceutically acceptable salt thereof, a 50 ml solution containing 50-5000 mg landiolol or a pharmaceutically acceptable salt thereof, a 100 ml solution containing 50-5000 mg landiolol or a pharmaceutically acceptable salt thereof, and a 250 ml solution containing 50-5000 mg landiolol or a pharmaceutically acceptable salt thereof. 
     
     
         12 . A method of reducing heart beat frequency in a patient comprising administering a composition of  claim 1  to a patient, whereby the heart beat frequency in the patient is reduced. 
     
     
         13 . The method of  claim 12 , wherein the patient has atrial fibrillation, atrial flutter, sinus tachycardia, atrioventricular tachycardia, AV node tachycardia, supraventricular tachycardia, ventricular arrhythmias, perioperative ischaemia, unstable angina pectoris, or acute myocardial infarction.