Injectable pharmaceutical composition of tecovirimat and preparation method thereof

11369,587

16/318044

July 04, 2017

The present invention relates to a pharmaceutical composition of Tecovirimat for injection, comprising Tecovirimat as an active ingredient, cyclodextrin and an additive. The present invention also relates to a method for preparing the pharmaceutical composition. The composition improves the solubility of Tecovirimat in water by using cyclodextrin and meglumine in combination, as compared with the solubility of Tecovirimat in water by using cyclodextrin or meglumine alone.

Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China (Beijing, CN)

Institute of Pharmacology and Toxicology Academy of Military Medical Sciences PLA China (Beijing, CN)

1. A pharmaceutical composition of Tecovirimat for injection, comprising Tecovirimat as an active ingredient, a cyclodextrin and an additive, wherein said additive is meglumine.

2. The pharmaceutical composition according to claim 1 , wherein said cyclodextrin is selected from the group consisting of α-cyclodextrin, β-cyclodextrin, γ-cyclodextrin, a hydroxypropyl-β-cyclodextrin, dimethyl-β-cyclodextrin, 2-hydroxyethyl-β-cyclodextrin, and trimethyl-β-cyclodextrin.

3. The pharmaceutical composition according to claim 1 , wherein said cyclodextrin and Tecovirimat have a weight ratio of 4-10:1.

4. The pharmaceutical composition according to claim 1 , wherein said additive and Tecovirimat have a weight ratio of 0.5-5:1.

5. The pharmaceutical composition according to claim 1 , wherein said additive and cyclodextrin have a weight ratio of 1:1-5.

6. The pharmaceutical composition according to claim 1 , wherein said pharmaceutical composition further comprises one or more components selected from the group consisting of water, glucose, and physiological saline.

7. The pharmaceutical composition according to claim 1 , wherein said pharmaceutical composition is a liquid.

8. The pharmaceutical composition according to claim 2 , wherein said cyclodextrin is the hydroxypropyl-β-cyclodextrin, and wherein an amount of said hydroxypropyl-β-cyclodextrin is 10% (w/v)-40% (w/v).

9. The pharmaceutical composition according to claim 2 , wherein said cyclodextrin is selected from the group consisting of dimethyl-β-cyclodextrin, 2-hydroxyethyl-β-cyclodextrin, 2-hydroxypropyl-β-cyclodextrin, 3-hydroxypropyl-β-cyclodextrin, and trimethyl-β-cyclodextrin.

10. The pharmaceutical composition according to claim 2 , wherein said cyclodextrin is selected from the group consisting of β-cyclodextrin, dimethyl-β-cyclodextrin, 2-hydroxyethyl-β-cyclodextrin, 2-hydroxypropyl-β-cyclodextrin, 3-hydroxypropyl-β-cyclodextrin, and trimethyl-β-cyclodextrin.

11. The pharmaceutical composition according to claim 2 , wherein said cyclodextrin is the hydroxypropyl-β-cyclodextrin, wherein the hydroxypropyl-β-cyclodextrin is selected from the group consisting of 2-hydroxypropyl-β-cyclodextrin and 3-hydroxypropyl-β-cyclodextrin.

12. The pharmaceutical composition according to claim 11 , wherein said cyclodextrin is 2-hydroxypropyl-β-cyclodextrin.

13. The pharmaceutical composition according to claim 3 , wherein said cyclodextrin and Tecovirimat have a weight ratio of 5-8:1.

14. The pharmaceutical composition according to claim 4 , wherein said additive and Tecovirimat have a weight ratio of 1-4:1.

15. The pharmaceutical composition according to claim 5 , wherein said additive and cyclodextrin have a weight ratio of 1:2-4.

16. The pharmaceutical composition according to claim 7 , wherein Tecovirimat has a concentration of 15-80 mg/ml.

17. A method for preparing the pharmaceutical composition according to claim 1 , comprising the following steps: a) dissolving an additive and cyclodextrin in a desired volume of water, and mixing well, wherein the additive is meglumine; b) adding Tecovirimat, and stirring well; and c) carrying out sterilization.

18. The method for preparing the pharmaceutical composition according to claim 17 , wherein said drying is freeze-drying.

19. A method for treating smallpox, comprising administering to a subject in need thereof a therapeutically and/or prophylactically effective amount of the pharmaceutical composition according to claim 1 .

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