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Last Updated: October 18, 2019

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Claims for Patent: 9,974,742

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Summary for Patent: 9,974,742
Title:Emulsion formulations of an NK-1 receptor antagonist and uses thereof
Abstract: Disclosed herein are novel pharmaceutical formulations of a neurokinin-1 (NK-1) receptor antagonist suitable for parenteral administration including intravenous administration. Also included are formulations including both the NK-1 receptor antagonist and dexamethasone sodium phosphate. The pharmaceutical formulations are stable oil-in-water emulsions for non-oral treatment of emesis and are particularly useful for treatment of subjects undergoing highly emetogenic cancer chemotherapy.
Inventor(s): Ottoboni; Thomas B. (Belmont, CA), Han; Han (Mountain View, CA)
Assignee: Heron Therapeutics, Inc. (San Diego, CA)
Application Number:15/012,532
Patent Claims: 1. An injectable pharmaceutical emulsion comprising: a neurokinase-1 (NK-1) receptor antagonist; 11 wt/wt % to 15 wt/wt % of an emulsifier; an oil; a co-surfactant which comprises an alcohol; a tonicity agent; a pH modifier; and water; wherein the pH of the emulsion ranges from about 7.5 to 9.0, and the ratio of the emulsifier to the NK-1 receptor antagonist ranges from about 18:1 to 22:1 (wt/wt %).

2. The emulsion according to claim 1, wherein the ratio of the oil to the NK-1 receptor antagonist ranges from about 5:1 to 15:1 (wt/wt %).

3. The emulsion according to claim 1, wherein the ratio of the oil to the NK-1 receptor antagonist ranges from about 10:1 to 15:1 (wt/wt %).

4. The emulsion according to claim 1, wherein the ratio of emulsifier to oil ranges from about 1:1 to 3:1 (wt/wt %).

5. The emulsion according to claim 1, wherein the emulsifier is a phospholipid.

6. The emulsion according to claim 1, wherein the emulsifier is an egg lecithin.

7. The emulsion according to claim 1, further comprising dexamethasone sodium phosphate, wherein the dexamethasone sodium phosphate is present in the aqueous phase.

8. The emulsion according to claim 1, wherein the NK-1 receptor antagonist is selected from the group consisting of rolapitant, netupitant, ezlopitant, vestipitant, serlopitant, maropitant, casopitant, befetupitant, and orvepitant.

9. The emulsion according to claim 1, wherein the pH modifier is oleic acid or a salt thereof.

10. The emulsion according to claim 1, wherein the pH modifier is a buffer.

11. The emulsion according to claim 10, wherein the buffer is Tris buffer.

12. The emulsion according to claim 1, wherein the oil is soybean oil.

13. The emulsion according to claim 1, wherein the alcohol is ethanol.

14. The emulsion according to claim 13, wherein the ethanol is present in the emulsion at less than 10 wt/wt %.

15. The emulsion according to claim 1, wherein the NK-1 receptor antagonist is not aprepitant.

16. A method for preparing an injectable pharmaceutical emulsion comprising: (a) combining a NK-1 receptor antagonist, an emulsifier, and an alcohol with an oil to generate an oil phase; (b) combining water, a tonicity agent, a pH modifier, and optionally a buffer to generate an aqueous phase; (c) homogenizing the oil phase with the aqueous phase to generate the pharmaceutical emulsion; and (d) sterilizing the pharmaceutical emulsion.

17. The method according to claim 16, wherein step (c) comprises homogenizing the oil phase with the aqueous phase to generate a crude emulsion, and step (c) further comprises homogenizing the crude emulsion to generate a fine emulsion wherein the fine emulsion is the pharmaceutical emulsion.

18. The method according to claim 17, wherein homogenizing the crude emulsion comprises using a microfluidizer at a pressure between 10,000 to 30,000 psi.

19. The method according to claim 18, wherein homogenizing the crude emulsion comprises 4 to 15 passes through the microfluidizer.

20. The method according to claim 16, wherein the sterilizing comprising passing the pharmaceutical emulsion through a filter having a pore size of about 0.2 microns.

21. The method according to claim 16, further comprising adding a solution of dexamethasone sodium phosphate to the pharmaceutical emulsion prior to sterile filtration.

22. The method according to claim 16, wherein the receptor antagonist is selected from the group consisting of rolapitant, netupitant, ezlopitant, casopitant, befetupitant, vestipitant, serlopitant, maropitant, and orvepitant.

23. The method according to claim 16, wherein the NK-1 receptor antagonist is not aprepitant.

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