Transdermal compositions
The present invention is directed to transdermal compositions and the uses thereof. These compositions include at least one of the following components: a C 1 -C 6 dialkyl, C 12 -C 30 dialkyl quaternary ammonium salt, a C 12 -C 30 fatty acid, a nitrogenous organic base, C 12 -C 30 fatty alcohol, monoglyceride or the reaction products thereof.
1. A composition comprising an antimicrobial effective amount of povidone iodine and tertiary amide of the formula:
or pharmaceutically acceptable salts thereof wherein R 4 is a fatty group of 11-29 carbon atoms;
R 5 and R 6 are independently lower alkyl, aryl, aryl lower alkyl, or fatty group containing 11-29 carbon atoms or R 7 ;
R 7 is
R 1 —Ar—O—R 2 —O—R 3 —;
R 2 and R 3 are independently lower alkylene groups containing 1-6 carbon atoms,
R 1 is a lower alkyl, and
Ar is aryl.
2. The composition of claim 1 wherein R 4 is a fatty group containing 15-21 carbon atoms.
3. The composition of claim 1 wherein R 5 is aryl or aryl lower alkyl; and R 6 is
R 1 —Ar—O—R 2 —O—R 3 —;
R 2 and R 3 are independently alkylene containing 1-3 carbon atoms; and
Ar is aryl.
4. The composition according to claim 3 wherein Ar is phenyl.
5. The composition according to claim 4 wherein R 5 is aryl lower alkyl.
6. The composition according to claim 5 wherein R 5 is benzyl.
7. The composition according to claim 5 wherein R 4 is saturated,
8. The composition according to claim 5 wherein R 4 is unsaturated.
9. The composition according to claim 8 wherein R 4 contains 1-8 carbon-carbon double bonds.
10. The composition according to claim 1 wherein the tertiary amide is distearyl stearamide, distearyl linoleamide, benzethonium linoleamide or benzethonium stearamide.
11. The composition according to claim 1 wherein the povidone iodine is present in an amount ranging from about 3% to about 15% by weight of the composition.
12. The composition according to claim 11 wherein the povidone-iodine is present in an amount ranging from about 5% to about 10% by weight of the composition.
13. The composition according to claim 12 wherein the povidone iodine is present in an amount ranging from about 6% to about 8% by weight of the composition.
14. The composition according to claim 1 in the form of a cream.
15. A composition comprising an anti-microbial effective amount of povidone-iodine and a tertiary amide of the formula:
or pharmaceutically acceptable salts thereof wherein
R 4 is a fatty group of 11-29 carbon atoms;
R 5 and R 6 are independently aryl, aryl lower alkyl, or fatty group containing 11-29 carbon atoms containing one to eight carbon-carbon double bonds or R 7 ;
R 7 is
R 1 —Ar—O—R 2 —O—R 3 —;
R 2 and R 3 are independently lower alkyl alkylene groups containing 1-6 carbon atoms;
R 1 is an alkyl group containing 1-15 carbon atoms; and
Ar is aryl.
16. The composition according to claim 15 when R 4 is a fatty group containing 15-21 carbon atoms.
17. The composition according to claim 15 in the form of a cream.
18. A composition comprising an anti-microbial effective amount of povidone-iodine and a tertiary amide hydrate formed from the process comprising heating a mixture of water, a quaternary surfactant, a fatty acid and an alkanolamine at a temperature greater than the melting point of said acid and less than 100° C. for sufficient time and under conditions effective to form a tertiary amide, cooling said tertiary amide to ambient temperature for sufficient time and under effective conditions for the pH of the water to stabilize and for said tertiary amide hydrate to form.
19. The composition according to claim 18 wherein the tertiary amide hydrate wherein the alkanolamine is triethanolamine, trimethanolamine, tris (hydroxyethyl) aminomethane, or tris (hydroxyethyl methyl) aminoethane.
20. A composition comprising an anti-microbial effective amount of povidine-iodine and a therapeutically effective amount of an amide hydrate of a tertiary amide, where the tertiary amide has the formula:
or pharmaceutically acceptable salts thereof wherein
R 4 is a fatty group of 11-29 carbon atoms;
R 5 and R 6 are independently lower alkyl, aryl, aryl lower alkyl, or fatty group containing 11-29 carbon atoms or R 7 ;
R 7 is
R 1 —Ar—O—R 2 —O—R 3 —;
R 2 and R 3 are independently alkylene groups containing 1-6 carbon atoms;
R 1 is an alkyl group containing 1-15 carbon atoms; and
Ar is aryl.
21. The composition according to claim 20 wherein R 4 is a fatty group containing 15-21 carbon atoms.
22. The composition according to claim 20 wherein R 5 is aryl or aryl lower alkyl; and
R 6 is
R 1 —Ar—O—R 2 —O—R 3 —
R 2 and R 3 are independently alkylene containing 1-3 carbon atoms; and
Ar is aryl.
23. The composition according to claim 22 wherein Ar is phenyl.
24. The composition according to claim 23 wherein R 5 is lower aryl lower alkyl.
25. The composition according to claim 24 wherein R 5 is benzyl.
26. The composition according to claim 25 wherein R 4 is saturated.
27. The composition according to claim 25 wherein R 4 is unsaturated.
28. The composition according to claim 27 wherein R 4 contains 1-8 carbon-carbon double bonds.
29. The composition according to claim 20 wherein the amide hydrate is the amide hydrate of a tertiary amide selected from the group consisting of distearyl stearamide, distearyl linoleamide, benzethonium linoleamide and benzethonium stearamide.
30. The composition according to claim 15 or 20 wherein the povidone iodine is present in an amount ranging from about 3% to about 15% by weight of the composition.
31. The composition according to claim 30 wherein the povidone-iodine is present in an amount ranging from about 5% to about 10% by weight of the composition.
32. The composition according to claim 31 wherein the povidone iodine is present in an amount ranging from about 6% to about 8% by weight of the composition.
33. The composition according to claim 20 in the form of a cream.