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 μs. 
     
     
         3 . The unit dose of  claim 2 , wherein the amount of Apadenoson present is 100 μg. 
     
     
         4 . The unit dose of  claim 2 , wherein the amount of Apadenoson present is 150 μg. 
     
     
         5 . The unit dose of  claim 1 , wherein the pharmaceutical carrier includes β-hydroxypropyl-cyclodextrin (CD). 
     
     
         6 . The unit dose of  claim 1 , wherein the pH of the unit dose is selected from 4.6-5.0. 
     
     
         7 . The unit dose of  claim 6 , wherein the pH is 4.8. 
     
     
         8 . The unit dose of  claim 1 , wherein the volume of the unit dose is selected from 1-5 mL. 
     
     
         9 . The unit dose of  claim 1 , wherein the Apadenoson is 100 μg of Apadenoson and wherein the pharmaceutically acceptable carrier includes (i) 2% w/v HP-β-CD; (ii) sodium citrate buffer in an amount to buffer the unit dose to pH 4.8; and (iii) saline in an amount to form a 1-5 mL unit dose. 
     
     
         10 . The unit dose of  claim 1 , wherein the Apadenoson is 150 μg of Apadenoson and wherein the pharmaceutically acceptable carrier includes (i) 2% w/v HP-β-CD; (ii) sodium citrate buffer in an amount to buffer the unit dose to pH 4.8; and (iii) saline in an amount to form a 1-5 mL unit dose. 
     
     
         11 . A method comprising:
 (a) parenterally administering to a mammal a unit dose of Apadenoson; and   (b) performing a technique to detect the presence of coronary artery stenoses in the mammal, to assess the severity of coronary artery stenoses in the mammal, or a combination thereof.   
     
     
         12 . The method of  claim 11 , wherein the patient weighs at least 40 kg. 
     
     
         13 . The method of  claim 12 , wherein the unit dose of Apadenoson is 100 μg. 
     
     
         14 . The method of  claim 12 , wherein the unit dose of Apadenoson is 150 μg. 
     
     
         15 . The method of  claim 12 , wherein the administering step is performed using a prefilled syringe that is prefilled with the unit dose of Apadenoson. 
     
     
         16 . The method of  claim 11 , wherein the coronary artery stenoses are coronary artery restenoses. 
     
     
         17 . A prefilled syringe configured for parenteral administration comprising:
 a syringe;   a unit dose of Apadenoson; and   a pharmaceutically acceptable carrier;   wherein the unit dose is suitable for parenteral administration.   
     
     
         18 . The prefilled syringe of  claim 17  wherein the unit dose of Apadenoson is 100 μg. 
     
     
         19 . The prefilled syringe of  claim 17 , wherein the unit dose of Apadenoson is 150 μg. 
     
     
         20 . A method of preparing a unit dose, comprising:
 filling a syringe with a unit dose of Apadenoson at a first location; and   administering the prefilled syringe of Apadenoson to a mammal at a second location.   
     
     
         21 . The method of  claim 20 , wherein the filling step further comprises sealing the prefilled syringe in a sterile package.