Parenteral solutions containing metolazone

Abstract

Disclosed herein are parenteral solutions containing 7-halo-1,2,3,4-tetrahydro-3-aryl-6-quinazoline sulfonamide in N,N-dimethylactamide, polyethylene glycol and D 5 W useful in the treatment of hypertension, heart failure and renal disease leading to edematous states. Also disclosed are methods for preparing such solutions.

1 . A quinazoline solution suitable for parenteral administration comprising an anti-hypertensive/diuretic compound of the formula 
       
         
           
           
               
               
           
         
         Where the X is halogen: 
         R 1 , R 2 , R 3  and R 4  are independently selected from hydrogen and alkyl having from 1 to 6 carbon atoms and R 5  is hydrogen or alkyl group having 1 to 6 carbon atoms, dissolved in 1% DMAC having a pH of from about 6.8 to 8. 
       
     
     
         2 . A solution suitable for parenteral administration according to  claim 1  wherein the quinazoline sulfonamide is metolazone dissolved in mixtures containing N,N-dimethylacetamide, PEG 300, 400, 600, polypropylene glycol, D 5 W and other suitable glycols at pH ranging from 6.8 to 8 with a concentration of metolazone ranging from 1 to 15 mg/ml. 
     
     
         3 . A solution of metolazone for the treatment of a patient suffering from hypertension, congestive heart failure or other edematous states which comprises the intravenous administration of an effective amount of a solution according to  claims 1  and  2 . 
     
     
         4 . Solution of metolazone for treating edematous states due to cardiac, renal or hepatic dysfunction. 
     
     
         5 . A solution of metolazone for the treatment of edematous states not responsive to loop diuretics such as furosemide, alone wherein the combination of a loop diuretic in conjunction with metolazone causes an increase diuresis more than with either drug given alone.