4-Methylpyrazole Formulations

Abstract

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.