UNIT DOSAGE OF APADENOSON

• US 20100003193A1
• Filed: 07/02/2009
• Published: 01/07/2010
• Est. Priority Date: 07/03/2008
• Status: Abandoned Application

• Current Assignee: University of Virginia
• Original Assignee: University of Virginia Patent Foundation (University of Virginia)
• Inventors: Stilley, William B., Hendel, Robert, Williams, Shannon P.
• Application Number:
  US12/496,949
• Publication Number:
  US 20100003193A1
• Time in Patent Office: Days
• US Class Current: 424/9.1
• CPC Class Codes: A61K 31/519 ortho- or peri-condensed with heterocyclic rings
• CPC Class Codes: A61K 31/7076 containing purines, e.g. adenosine, adenylic acid
• CPC Class Codes: A61K 47/02 Inorganic compounds
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: A61K 47/40 Cyclodextrins; Derivatives thereof
• CPC Class Codes: A61K 49/0004 Screening or testing of compounds for diagnosis of disorders, assessment of conditions, e.g. renal clearance, gastric emptying, testing for diabetes, allergy, rheuma, pancreas functions
• CPC Class Codes: A61K 9/0019 Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner non-active ingredients are additionally classified in A61K47/00
• CPC Class Codes: A61P 9/10 for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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.

Claims

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 μ

g.

3. The unit dose of claim 2, wherein the amount of Apadenoson present is selected from 100-150 μ

g.

4. The unit dose of claim 3, wherein the amount of Apadenoson present is 100 μ

g.

5. The unit dose of claim 3, wherein the amount of Apadenoson present is 150 μ

g.

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 μ

g 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 μ

g 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 μ

g 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 μ

g 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.