Antispasmodic 1,2-diols and 1,2,3-triols

Abstract

The present invention is directed to pharmaceutical compositions comprising antispasmodic C 4 -C 8 aliphatic-1,2-diols and C 4 -C 8 aliphatic-1,2,3-triols and their use to relieve the spasms associated with pain. These agents may be administered topically or orally and may be combined with anti-inflammatory agents such as a non-steroidal anti-inflammatory drug or a corticosteroid. Administration of the C 4 -C 8 aliphatic-1,2-diols and C 4 -C 8 aliphatic-1,2,3-triols with vitamin D 3 is indicated for conditions such as bone loss, weight gain and autoimmune diseases such as lupus and rheumatoid arthritis.

1 - 15 . (canceled) 
     
     
         16 . A pharmaceutical composition comprising about 0.5% to about 20% (w/w) of a C 4 -C 8 aliphatic-1,2,3-triol together with an optional C 4 -C 8 aliphatic-1,2-diol; and a pharmaceutically acceptable carrier. 
     
     
         17 . The pharmaceutical composition of  claim 16  wherein the C 4 -C 8 aliphatic-1,2,3-triol is a C 4 -C 8 alkane-1,2,3-triol, and the optional C 4 -C 8 aliphatic-1,2-diol is a C 4 -C 8 alkane-1,2-diol, the composition further comprising about 0.5% to about 20% of a non-steroidal anti-inflammatory drug or a steroidal anti-inflammatory drug, or pharmaceutically acceptable salts thereof. 
     
     
         18 . The pharmaceutical composition of  claim 17  wherein the C 4 -C 8 alkane-1,2,3-triol is 1,2,3-hexanetriol. 
     
     
         19 . (canceled) 
     
     
         20 . A method of treating bone loss, weight gain, arthritis, or autoimmune disease comprising administration to a patient in need thereof a pharmaceutical composition comprising about 0.5% to about 20% (w/w) of one or more agents independently selected from the group consisting of a C 4 -C 8 aliphatic-1,2-diol and a C 4 -C 8 aliphatic-1,2,3-triol; and a therapeutically effective amount of vitamin D 3 . 
     
     
         21 . The method of  claim 20 , wherein the patient suffers from muscle spasms, the method comprising administering about 0.5% to about 20% (w/w) of one or more agents independently selected from the group consisting of a C 4 -C 8 aliphatic-1,2-diol and a C 4 -C 8 aliphatic-1,2,3-triol; a therapeutically effective amount of vitamin D 3 ; and optionally a therapeutically effective amount of an anti-inflammatory agent. 
     
     
         22 . A topical pharmaceutical composition comprising a pharmaceutically acceptable carrier, about 0.5% to about 20% (w/w) 1,2-hexanediol, and a therapeutically effective amount of diclofenac, or a pharmaceutically acceptable salt thereof. 
     
     
         23 . The topical pharmaceutical composition of  claim 22  comprising about 1% diclofenac, or a pharmaceutically acceptable salt thereof. 
     
     
         24 . The topical pharmaceutical composition of  claim 22  comprising about 5% (w/w) 1,2-hexanediol. 
     
     
         25 . The topical pharmaceutical composition of  claim 23  comprising about 5% (w/w) 1,2-hexanediol. 
     
     
         26 . A method of treating muscle spasms comprising administering topically to a patient in need thereof the composition of  claim 22 .