Stabilized steroid composition and method for its preparation
View Patent ↗Stabilized, 17-substituted hydrocortisone containing compositions and methods of manufacture are disclosed. Isomerization of the hydrocortisone component of topical steroid compositions is markedly reduced by including an omega-6 acid component in the form of a free acid or as a compound such as an ester. Specifically disclosed are methods for preventing the isomerization of hydrocortisone 17-butyrate into hydrocortisone 21-butyrate through the use of safflower oil.
1. A composition of matter comprising:
(a) About 0.1% (w/w) hydrocortisone 17-butyrate;
(b) About 60% to about 80% (w/w) of a lipid system,
(i) Said lipid system comprising at least one omega-6 fatty acid or omega-6 acid ester;
(ii) Said lipid system comprising up to about 24% (w/w) of a fatty alcohol (and/or ester formable by condensing said fatty alcohol with a fatty acid);
(c) Quantum sufficit of water;
(d) Surfactant having a hydrophilic:lipophilic balance of less than about 12;
(i) said surfactant present in an amount sufficient to emulsify said lipid system and said water to form an emulsion suitable for topical application;
(ii) said emulsion having a pH of less than about 5;
(iii) said omega-6 acid or omega-6 acid ester present in an amount whereby said composition of matter contains not more than about 0.05% (w/w) of hydrocortisone 21-butyrate.
2. The composition of claim 1 , wherein said lipid system comprises not more than about 5% of the fatty alcohol and/or ester formable by condensing the fatty alcohol with a fatty acid.
3. The composition of claim 1 , wherein said lipid system comprises at least about 10% of the fatty alcohol and/or ester formable by condensing the fatty alcohol with a fatty acid.
4. The composition of claim 1 , said emulsion selected from the group consisting of: an oil-in-water emulsion; a water-in-oil emulsion; and a complex emulsion.
5. The composition of claim 4 , wherein said emulsion comprises an oil-in-water emulsion.
6. The composition of claim 4 , wherein said emulsion comprises a complex emulsion.
7. The composition of claim 1 , wherein said surfactant comprises a surfactant system comprised of at least two surfactants, wherein said surfactant system has a hydrophilic:lipophilic balance of less than about 14.
8. The composition of claim 1 , wherein said Omega-6 acid or omega-6 acid ester comprises safflower oil.
9. The composition of claim 1 , wherein said composition contains not more than about 0.02% (w/w) of hydrocortisone 21-butyrate.
10. A composition of matter comprising:
(a) Hydrocortisone 17-butyrate in an amount sufficient to treat the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses;
(b) About 60% to about 80% (w/w) of a lipid system,
(i) Said lipid system comprising at least one omega-6 fatty acid or omega-6 acid ester;
(ii) Said lipid system comprising up to about 24% (w/w) of a fatty alcohol (and/or ester formable by condensing said fatty alcohol with a fatty acid);
(c) Quantum sufficit of water;
(d) Surfactant having a hydrophilic:lipophilic balance of less than about 12;
(i) said surfactant present in an amount sufficient to emulsify said lipid system and said water to form an emulsion suitable for topical application;
(ii) said emulsion having a pH of less than about 5;
(iii) said omega-6 acid or omega-6 acid ester thereof present in an amount whereby said composition of matter contains not more than about 0.05% (w/w) of hydrocortisone 21-butyrate.
11. The composition of claim 10 , wherein said lipid system comprises not more than about 5% of the fatty alcohol and/or ester formable by condensing the fatty alcohol with a fatty acid.
12. The composition of claim 10 , wherein said lipid system comprises at least about 10% of the fatty alcohol and/or ester formable by condensing the fatty alcohol with a fatty acid.
13. The composition of claim 10 , said emulsion selected from the group consisting of: an oil-in-water emulsion; a water-in-oil emulsion; and a complex emulsion.
14. The composition of claim 13 , wherein said emulsion comprises an oil-in-water emulsion.
15. The composition of claim 13 , wherein said emulsion comprises a complex emulsion.
16. The composition of claim 10 , wherein said surfactant comprises a surfactant system comprised of at least two surfactants, wherein said surfactant system has a hydrophilic:lipophilic balance of less than about 14.
17. The composition of claim 10 , wherein said Omega-6 acid or omega-6 acid ester comprises safflower oil.
18. The composition of claim 10 , wherein said composition contains not more than about 0.02% (w/w) of hydrocortisone 21-butyrate.
19. A composition of matter comprising:
(a) About 0.1% (w/w) hydrocortisone 17-butyrate;
(b) About 60% to about 80% (w/w) of a lipid system,
(i) Said lipid system comprising at least one omega-6 fatty acid or omega-6 acid ester;
(c) Quantum sufficit of water;
(d) At least one surfactant;
(i) said surfactant present in an amount sufficient to emulsify said lipid system and said water to form an emulsion suitable for topical application;
(ii) said emulsion having a pH of less than about 5;
(iii) said omega-6 acid or omega-6 acid ester present in an amount whereby said composition of matter contains not more than about 0.05% (w/w) of hydrocortisone 21-butyrate.