Dialkylated glycol compositions and medicament preparations containing same

Abstract

A pharmaceutical preparation having a minor amount of a medicament, a major amount of a dialkylated mono- or poly-alkylene glycol vehicle therefor, and a minor amount of one or more antioxidants for the dialkylated glycol vehicle.

What is claimed is: 
     
       1. A composition .Iadd.containing a minimum amount of water, up to 5%, and .Iaddend.comprising a major amount of dialkylated glycol represented by the formula: ##EQU2## where R and R 1  are independently lower alkyl having 1 to 6 carbon atoms, R 2  is hydrogen or a lower alkyl having 1 to 6 carbon atoms m is integer from 1 to 6, and n is an integer from 1 to a very large number such that the molecular weight of said dialkylated glycol is up to about 20,000, and a minor amount of at least one antioxidant for said dialkylated glycol material, said composition being substantially devoid of peroxides and other oxidation products in quantities which interfere with the carrier or stabilizing properties of said composition .Iadd., said composition being suitable for use as a vehicle for medicament preparations.Iaddend.. 
     
     
       2. The composition of claim 1 wherein said dialkylated glycol is a dimethyl ether of a polyethylene glycol. 
     
     
       3. The composition of claim 2 wherein said dialkylated glycol has a molecular weight from about 350 to about 750. 
     
     
       4. The composition of claim 1 wherein said dialkylated glycol is 1,2-dimethoxyethane. 
     
     
       5. The composition of claim 1 wherein said dialkylated glycol is a dimethyl ether of triethylene glycol. 
     
     
       6. The composition of claim 1 wherein R and R 1  are methyl. 
     
     
       7. The composition of claim 1 wherein R and R 1  are methyl, and R 2  is hydrogen. 
     
     
       8. The composition of claim 1 wherein said antioxidant is selected from the group consisting of propyl gallate, vitamin E, butylated hydroxyanisole, butylated hydroxytoluene, and mixtures thereof. 
     
     
       9. The composition of claim 1 wherein said composition includes about 0.01% to about 1.0% of said antioxidant. 
     
     
       10. The composition of claim 1 wherein said composition includes about 0.025% butylated hydroxy anisole and about 0.025% butylated hydroxytoluene. 
     
     
       11. The composition of claim 1 further including a therapeutically effective amount of active medicament material, or a pharmaceutically acceptable salt thereof. .[.12. The composition of claim 1 wherein said composition contains less than 5% water..]. .[.13. The composition of 
     
     
        claim 11 wherein said composition contains less than 5% water..]. 14. The 
     
     
        composition of claim 11 wherein said medicament is an antibiotic. 15. The composition of claim 11 wherein said medicament is relatively chemically unstable and the chemical activity of said medicament in said composition is stabilized by said dialkylated glycol over an extended period of time. 
     
     
         6. The composition of claim 11 wherein said medicament is an 
     
     
        anti-inflammatory steroid. 17. The composition of claim 11 wherein said medicament is 6α,9α-difluoro-11β-hydroxy-16α,17α-isopropyli 
     
     
       denedioxypregna-1,4-diene-3,20-dione. 18. The composition of claim 11 wherein said medicament is 9α,11β,21-trichloro-6α-fluoro-16α,17α-isoprop 
     
     
       ylidenedioxypregna-1,4-diene-3,20-dione. 19. The composition of claim 11 wherein said medicament is a naturally occurring or synthetic 
     
     
        prostaglandin. 20. The composition of claim 11 whererin .[.said composition contains less than 5% water, and.]. said medicament is PGE 2 , said dialkylated glycol serving to stabilize the chemical activity of said PGE 2  in said composition over extended periods of 
     
     
        time. 21. The composition of claim 11 wherein .[.said composition contains less than 5% water, and.]. said medicament is acetyl salicylic acid, said dialkylated glycol serving to stabilize the chemical activity of said acetyl salicylic acid in said composition over extended periods of time. 
     
     
          . The composition of claim 11 wherein .[.said composition contains less than 5% water, and.]. said medicament is N,N-bis(2-hydroxyethyl)-oleamide, said dialkylated glycol serving to stabilize the chemical activity of said N,N-bis-(2-hydroxyethyl)-oleamide in said composition over extended 
     
     
        periods of time. 23. A composition .Iadd.containing a minimum amount of water, up to about 5%, and .Iaddend.comprising a major amount of a dialkylated glycol represented by the formula: ##EQU3## where R and R 1  are independently lower alkyl having 1 to 6 carbon atoms, R 2  is hydrogen or a lower alkyl having 1 to 6 carbon atoms, m is an integer from 1 to 6, and n is an integer from 1 to a very large number such that the molecular weight of said dialkylated glycol is up to about 20,000, and a therapeutically effective amount of an active medicament or a pharmaceutically acceptable salt thereof, said composition being substantially devoid of peroxides and other oxidation products in quantities which interfere with the carrier or stabilizing properties of 
     
     
        said composition. 24. The composition of claim 23 wherein said dialkylated glycol is selected from the group consisting of the dimethyl ether of polyethylene glycol, the dimethyl ether of triethylene glycol, glyme, 
     
     
        diglyme, triglyme, and tetraglyme. 25. The composition of claim 23 wherein 
     
     
        said medicament is an anti-inflammatory steroid. 26. The composition of claim 23 wherein said medicament is a naturally occurring or synthetic 
     
     
        prostaglandin. 27. The composition of claim 23 wherein .[.said composition contains less than 5% water, and.]. said medicament is selected from the group consisting of acetyl salicylic acid, PGE 2 , and N,N-bis(2-hydroxyethyl)-oleamide, said dialkylated glycol serving to stabilize the chemical activity of said medicament in said composition over extended periods of time. .[.28. The composition of claim 23 wherein 
     
     
        said composition contains less than 5% water..]. 29. The composition of 
     
     
        claim 23 wherein said medicament is an antibiotic. 30. The composition of claim 23 wherein said medicament is relatively chemically unstable and the chemical activity of said medicament in said composition is stabilized by said dialkylated glycol over an extended period of time.