4-Methylpyrazole Formulations
Provided herein are 4-methylpyrazole (4-MP) formulations, stable under storage conditions of up to about 55° C.
1 . A formulation comprising:
(a) 4-methylpyrazole, or a physiologically acceptable salt form thereof; and
(b) an excipient, wherein the excipient is polyethylene glycol;
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 . (canceled)
5 . The formulation of claim 1 wherein the polyethylene glycol has a total weight average molecular weight of from about 5000 to about 10,000.
6 . The formulation of claim 5 wherein the excipient is PEG 8000.
7 . The formulation of claim 1 wherein the formulation further comprises one or more additional excipients.
8 . The formulation of claim 7 wherein the additional excipients is a surfactant.
9 . The formulation of claim 7 wherein the additional excipient is selected from the group consisting of propylene glycol monocaprylate and diethylene glycol monoethyl ether.
10 . The formulation of claim 1 wherein the formulation is provided as a unit dosage.
11 . The formulation of claim 10 wherein the unit dosage is in the form of a tablet or capsule.
12 . The formulation of claim 10 wherein the unit dosage is in the form of a capsule.
13 . The formulation of claim 12 wherein the capsule comprises hard gelatin.
14 . The formulation of claim 10 wherein the unit dosage comprises about 10 mg of 4-methylpyrazole.
15 . The formulation of claim 10 wherein the unit dosage comprises about 100 mg of 4-methylpyrazole.
16 . The formulation of claim 11 wherein the formulation is physically stable for 8 months or more at room temperature and at relative humidities of up to about 60%±5%.
17 . The formulation of claim 11 wherein the formulation is chemically stable for 8 months or more at room temperature and at relative humidities of up to about 60%±5%.
18 . A hard gelatin capsule encapsulating:
(a) 4-methylpyrazole, or a physiologically acceptable salt form thereof; and
(b) an excipient, wherein the excipient is polyethylene glycol;
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%.
19 . The hard gelatin capsule of claim 18 wherein the excipient is PEG 8000.
20 . The hard gelatin capsule of claim 18 wherein the contents of the capsule are in a solid form.
21 . The formulation of claim 1 wherein the formulation is suitable for oral administration in a human.
22 . 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 .
23 . (canceled)
24 . The formulation of claim 1 comprising approximately 2% to 60% wt/wt % 4-MP or a physiologically acceptable salt form thereof.
25 . The hard gelatin capsule of claim 18 wherein the capsule retains at least 90% of the 4-MP when stored up to 8 months at room temperature.