4-methylpyrazole formulations
View Patent ↗Provided herein are 4-methylpyrazole (4-MP) formulations, stable under storage conditions of up to about 55° C.
1. A solid formulation comprising:
(a) 4-methylpyrazole, or a physiologically acceptable salt form thereof; and
(b) an excipient, wherein the excipient is a polyethylene glycol having a total weight average molecular weight of from 5000 to 10,000 Da;
wherein the formulation is in a solid form at temperatures of from at least 25° C. to up to about 40° C.
2. The formulation of claim 1 wherein the formulation is in a solid form at temperatures of up to about 35° C.
3. The formulation of claim 1 wherein the formulation is in a solid form at temperatures of up to about 30° C.
4. The formulation of claim 1 wherein the excipient is PEG 8000.
5. The formulation of claim 1 wherein the formulation further comprises one or more additional excipients.
6. The formulation of claim 5 wherein the additional excipient is a surfactant.
7. The formulation of claim 5 wherein the additional excipient is selected from the group consisting of propylene glycol monocaprylate and diethylene glycol monoethyl ether.
8. The formulation of claim 1 wherein the formulation is provided as a unit dosage.
9. The formulation of claim 8 wherein the unit dosage is in the form of a tablet or capsule.
10. The formulation of claim 8 wherein the unit dosage is in the form of a capsule.
11. The formulation of claim 10 wherein the capsule comprises hard gelatin.
12. The formulation of claim 8 wherein the unit dosage comprises about 10 mg of 4-methylpyrazole.
13. The formulation of claim 8 wherein the unit dosage comprises about 100 mg of 4-methylpyrazole.
14. The formulation of claim 9 wherein the formulation is physically stable for 8 months or more at room temperature and at relative humidities of up to about 60%±5%.
15. The formulation of claim 9 wherein the formulation is chemically stable for 8 months or more at room temperature and at relative humidities of up to about 60%±5%.
16. A hard gelatin capsule encapsulating:
(a) 4-methylpyrazole, or a physiologically acceptable salt form thereof; and
(b) an excipient, wherein the excipient is a polyethylene glycol having a total weight average molecular weight of from 5000 to 10,000 Da;
wherein the capsule retains physical integrity when stored for 8 months or more at room temperature and at relative humidities of up to about 60%±5%.
17. The hard gelatin capsule of claim 16 wherein the excipient is PEG 8000.
18. The hard gelatin capsule of claim 16 wherein the contents of the capsule are in a solid form.
19. The formulation of claim 1 wherein the formulation is suitable for oral administration in a human.
20. A method for treating or ameliorating a symptom of ethanol intolerance in a subject comprising the step of administering to the subject a formulation of claim 1 .