Unit dosage of apadenoson

Abstract

The present invention provides a unit dosage of Apadenoson, a pharmacological stress agent, and use of the same as a pharmacologic agent for myocardial perfusion imaging.

1 . A unit dose of Apadenoson, comprising: (a) Apadenoson and (b) a pharmaceutically acceptable carrier, wherein the unit dose is suitable for parenteral administration. 
   
   
       2 . The unit dose of  claim 1 , wherein the amount of Apadenoson present is selected from 76-175 μg. 
   
   
       3 . The unit dose of  claim 2 , wherein the amount of Apadenoson present is selected from 100-150 μg. 
   
   
       4 . The unit dose of  claim 3 , wherein the amount of Apadenoson present is 100 μg. 
   
   
       5 . The unit dose of  claim 3 , wherein the amount of Apadenoson present is 150 μg. 
   
   
       6 . The unit dose of  claim 1 , wherein the pharmaceutical carrier, comprises: a cyclodextrin (CD). 
   
   
       7 . The unit dose of  claim 6 , wherein the cyclodextrin is β-hydroxypropyl-CD. 
   
   
       8 . The unit dose of  claim 6 , wherein the concentration of CD is selected from 0.1-10% w/v of the final formulation. 
   
   
       9 . The unit dose of  claim 8 , wherein the concentration of CD is 1% w/v. 
   
   
       10 . The unit dose of  claim 8 , wherein the concentration of CD is 2% w/v. 
   
   
       11 . The unit does of  claim 1 , wherein the pharmaceutical carrier, comprises: buffered saline. 
   
   
       12 . The unit dose of  claim 11 , wherein the pharmaceutical carrier, comprises: buffered saline, comprising: saline and sodium citrate. 
   
   
       13 . The unit dose of  claim 1 , wherein the pH of the unit dose is selected from 4.6-5.0. 
   
   
       14 . The unit dose of  claim 13 , wherein the pH is 4.8. 
   
   
       15 . The unit dose of  claim 1 , wherein the volume of the unit dose is selected from 1-5 mL. 
   
   
       16 . The unit dose of  claim 1 , comprising:
 (a) 100 μg Apadenoson;   (b) a pharmaceutically acceptable carrier, comprising:
 (b i ) 2% w/v HP-β-CD; 
 (b ii ) sodium citrate buffer in an amount to buffer the unit dose to pH 4.8; and, 
 (b iii ) saline in an amount to form a 1-5 mL unit dose. 
   
   
   
       17 . The unit dose of  claim 1 , comprising:
 (a) 100 μg Apadenoson;   (b) a pharmaceutically acceptable carrier, comprising:
 (b i ) 1% w/v HP-β-CD; 
 (b ii ) sodium citrate buffer in an amount to buffer the unit dose to pH 4.8; and, 
 (b iii ) saline in an amount to form a 1-5 mL unit dose. 
   
   
   
       18 . The unit dose of  claim 1 , comprising:
 (a) 150 μg Apadenoson;   (b) a pharmaceutically acceptable carrier, comprising:
 (b i ) 2% w/v HP-β-CD; 
 (b ii ) sodium citrate buffer in an amount to buffer the unit dose to pH 4.8; and, 
 (b iii ) saline in an amount to form a 1-5 mL unit dose. 
   
   
   
       19 . The unit dose of  claim 1 , comprising:
 (a) 150 μg Apadenoson;   (b) a pharmaceutically acceptable carrier, comprising:
 (b i ) 2% w/v HP-β-CD; 
 (b ii ) sodium citrate buffer in an amount to buffer the unit dose to pH 4.8; and, 
 (b iii ) saline in an amount to form a 1-5 mL unit dose. 
   
   
   
       20 . A method of diagnosing myocardial perfusion abnormalities in a mammal, comprising:
 (a) parenterally administering to the mammal a unit dose of Apadenoson; and   (b) performing a technique on the mammal to detect the presence of coronary artery stenoses, assess the severity of coronary artery stenoses, or a combination thereof.   
   
   
       21 . The method of  claim 20 , wherein the patient weighs at least 40 kg.