Parenteral formulation of clopidogrel
View Patent ↗Described herein are ways to solubilize clopidogrel for parenteral administration containing clopidogrel and a diluent NNDMA (N,N-dimethylacetamide); useful in the prevention of platelet aggregation in acute coronary syndrome, acute myocardial infarction or to prevent platelet facilitated thrombosis following coronary angioplasty and/or coronary stenting.
1. A parenteral formulation, comprising;
a) clopidogrel;
b) 1-50% by volume NNDMA (N,N-dimethylacetamide);
c) 18-61% by volume propylene glycol; and,
d) 38-81% by volume PEG-300.
2. The parenteral formulation of claim 1 , wherein 1.0 mg/mL to 150 mg/mL of clopidogrel is present in the formulation.
3. The parenteral formulation of claim 1 , wherein 7.5 mg/mL of clopidogrel is present in the formulation.
4. The parenteral formulation of claim 1 , wherein 15 mg/mL of clopidogrel is present in the formulation.
5. The parenteral formulation of claim 1 , wherein 60% by volume propylene glycol and 38% by volume PEG-300 is present in the formulation.
6. The parenteral formulation of claim 1 , wherein 50% by volume propylene glycol and 48% by volume PEG-300 is present in the formulation.
7. The parenteral formulation of claim 1 , wherein 33% by volume propylene glycol and 65% by volume PEG-300 is present in the formulation.
8. The parenteral formulation of claim 1 , wherein 18% by volume propylene glycol and 80% by volume PEG-300 is present in the formulation.
9. The parenteral formulation of claim 1 , wherein 20% by volume propylene glycol and 60% by volume PEG-300 is present in the formulation.
10. The parenteral formulation of claim 1 , wherein 1-5% by volume NNDMA is present in the formulation.
11. The parenteral formulation of claim 1 , wherein 1.5-2.5% by volume NNDMA is present in the formulation.
12. The parenteral formulation of claim 1 , wherein 2% by volume NNDMA is present in the formulation.
13. The parenteral formulation of claim 1 , wherein the pH of the formulation is from 4.5 to 6.5.
14. The parenteral formulation of claim 1 , wherein the pH of the formulation is 5.0.
15. The parenteral formulation of claim 1 , wherein the pH of the formulation is 5.5.
16. The parenteral formulation of claim 1 , wherein the pH of the formulation is 6.0.
17. The parenteral formulation of claim 1 , comprising:
a) 7.5 to 15 mg/mL clopidogrel;
b) 1.5-2.5% by volume NNDMA (N,N-dimethylacetamide);
c) 18-61% by volume propylene glycol; and,
d) 38-81% by volume PEG-300.
18. The parenteral formulation of claim 17 , comprising:
a) 7.5 mg/mL clopidogrel; and,
b) 2% by volume NNDMA (N,N-dimethylacetamide).
19. The parenteral formulation of claim 17 , comprising:
a) 15 mg/mL clopidogrel; and,
b) 2% by volume NNDMA (N,N-dimethylacetamide).
20. The parenteral formulation of claim 17 , wherein the formulation has a pH of from 4.5-6.5.
21. The parenteral formulation of claim 17 , comprising:
a) 7.5 mg/mL clopidogrel; and,
b) 2% by volume NNDMA (N,N-dimethylacetamide);
wherein the formulation has a pH of from 4.5-6.5.
22. The parenteral formulation of claim 17 , comprising:
a) 15 mg/mL clopidogrel; and,
B) 2% by volume NNDMA (N,N-dimethylacetamide);
wherein the formulation has a pH of from 4.5-6.5.