Claims for Patent: 11,865,112

Summary for Patent: 11,865,112

Title:	Compositions and methods for opioid antagonist delivery
Abstract:	Disclosed in certain embodiments is a pharmaceutical formulation (e.g., parenteral formulation) comprising a therapeutically effective amount of nalmefene or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable adjuvant (e.g., parenterally acceptable adjuvant) that promotes the rate at which the nalmefene or salt thereof is more rapidly absorbed into the systemic circulation of a subject identified as in need thereof.
Inventor(s):	Haiyong Hugh Huang, Manjunath S. Shet
Assignee:	Purdue Pharma LP
Application Number:	US16/674,755
Patent Claims:	1. A parenteral formulation comprising a therapeutically effective amount of nalmefene or a pharmaceutically acceptable salt thereof and a parenterally acceptable adjuvant comprising magnesium chloride at a concentration ranging from about 0.5% (w/v) to about 1% (w/v), wherein the formulation provides a time to onset of opioid antagonistic action of less than 5 minutes post administration via an intramuscular or subcutaneous injection to a subject experiencing an opioid agonist overdose. 2. The parenteral formulation of claim 1, wherein the formulation provides a mean time to maximum plasma concentration of nalmefene of about 2.0 hours or less post an intramuscular administration to a population of healthy subjects. 3. The parenteral formulation of claim 2, wherein the formulation provides a mean time to maximum plasma concentration of nalmefene of about 1.0 hour or less post an intramuscular administration to a population of healthy subjects. 4. The parenteral formulation of claim 1, wherein the formulation provides a time to clinically manifested onset of opioid antagonistic action of about 4 minutes or less post intramuscular or subcutaneous injection to a subject experiencing an opioid agonist overdose. 5. The parenteral formulation of claim 2, wherein the formulation provides a mean time to maximum plasma concentration of nalmefene of about 1.5 hours or less post intramuscular injection to a population of healthy subjects. 6. The parenteral formulation of claim 3, wherein the formulation provides a mean time to maximum plasma concentration of nalmefene of about 0.5 hour or less post an intramuscular administration to a population of healthy subjects. 7. The parenteral formulation of claim 1, wherein the formulation provides a time to clinically manifested onset of opioid antagonistic action of less than 5 minutes post intramuscular injection to a subject experiencing an opioid agonist overdose. 8. The parenteral formulation of claim 1, wherein the formulation provides a time to clinically manifested onset of opioid antagonistic action of less than 5 minutes post subcutaneous injection to a subject experiencing an opioid agonist overdose. 9. The parenteral formulation of claim 2, wherein the adjuvant promotes the systemic absorption rate and/or the total amount absorbed of the nalmefene or pharmaceutically acceptable salt thereof post injection as compared to the same formulation but without the adjuvant. 10. The parenteral formulation of claim 2, comprising nalmefene hydrochloride. 11. A method of providing opioid overdose rescue to a subject comprising intramuscularly or subcutaneously administering to a subject in need thereof a parenteral formulation comprising a therapeutically effective amount of nalmefene or a pharmaceutically acceptable salt thereof and magnesium chloride at a concentration ranging from about 0.5% (w/v) to about 1% (w/v), wherein the formulation provides a time to onset of opioid antagonistic action of less than 5 minutes post administration via an intramuscular or subcutaneous injection to a subject experiencing an opioid agonist overdose. 12. A method of preparing a subject prior to entering a locale having a potentially toxic level of an opioid such that the subject is protected from experiencing an opioid overdose as a result of entering the locale, said preparation comprising administering to the subject prior to the subject entering the locale a parenteral formulation comprising a therapeutically effective amount of nalmefene or a pharmaceutically acceptable salt thereof and magnesium chloride at a concentration ranging from about 0.5% (w/v) to about 1% (w/v), wherein the formulation provides a mean time to maximum plasma concentration of nalmefene of about 2.0 hours or less post an intramuscular administration to a population of healthy subjects. 13. A drug delivery system comprising an injection device containing a parenteral formulation of claim 2. 14. The drug delivery system of claim 13, wherein the parenteral formulation is disposed within a pre-filled syringe, a vial, an injection pen, or an auto-injector. 15. The parenteral formulation of claim 1, wherein the magnesium chloride is at a concentration of about 0.9%. 16. The method of claim 11, wherein the magnesium chloride is at a concentration of about 0.9%. 17. The method of claim 12, wherein the magnesium chloride is at a concentration of about 0.9%.