Claims for Patent: 6,352,998

Summary for Patent: 6,352,998

Title:	Pharmaceutical compositions
Abstract:	This invention provides a topical composition, in the form of an emulsion, that comprises a compound of the FK506 class; a physiologically acceptable alkanediol, ether diol or diether alcohol containing up to 8 carbon atoms as solvent for the compound of the FK506 class; an unsaturated fatty alcohol and water. In another aspect, this invention provides a topical pharmaceutical composition that comprises a macrolide in suspension. In a further aspect, this invention provides the use of an unsaturated fatty alcohol to stabilize a macrolide in a pharmaceutical composition.
Inventor(s):	Jackman; Martin (Allschwil, CH), Popp; Xue-Ping (Basel, CH), Richter; Friedrich (Grenzach-Wyhlen, DE), Schmook; Fritz (Vienna, AT)
Assignee:	Novartis AG (Basel, CH)
Application Number:	09/767,656
Patent Claims:	1. A topical composition, in the form of an emulsion, consisting essentially of an immunosupressant effective amount of 33-epi-chloro-33-desoxyascomycin, an alkanediol, ether diol, or diether alcohol containing up to 8 carbon atoms as solvent for the 33-epi-chloro-33-desoxyascomycin, a C.sub.8 -C.sub.22 unsaturated fatty alcohol, water, a liquid oil, a thickening agent, an emulsifier and a preservative. 2. A topical composition according to claim 1 in which the solvent is hexylene glycol or propylene glycol. 3. A topical composition according to claim 1 wherein the unsaturated fatty alcohol is oleyl alcohol or elaidic alcohol. 4. A topical composition according to claim 1 wherein the unsaturated fatty alcohol contains one, two or three double bonds. 5. A topical composition according to claim 1 wherein the unsaturated fatty alcohol contains one double bond. 6. A topical composition according to claim 1 wherein the double bond has a cis configuration. 7. A topical composition, in the form of an emulsion, consisting essentially of 33-epi-chloro-33-desoxyascomycin; an alkanediol, ether diol, or diether alcohol containing up to 8 carbon atoms as solvent for the 33-epi-chloro-33-desoxyascomycin; a C.sub.8 -C.sub.22 unsaturated fatty alcohol; water; a liquid oil; a thickening agent; an emulsifier; and a preservative, wherein the 33-epi-chloro-33-desoxyascomycin is present in the emulsion in an amount of about 0.01 to about 10% w/w. 8. A topical composition according to claim 7 wherein the 33-epi-chloro-33-desoxyascomycin is present in the emulsion in an amount of about 0.1 to about 1% w/w. 9. A topical composition according to claim 1 wherein the alkanediol solvent is selected from propylene glycol, butylene glycol, 2-ethyl-1,3-hexanediol and 2-methyl-2,4-pentanediol. 10. A topical composition according to claim 1 wherein the ether diol is selected from dipropylene glycol and diethylene glycol. 11. A topical composition according to claim 1 wherein the diether alcohol is diethylene glycol monoethyl ether. 12. A topical composition according to claim 1 wherein the unsaturated fatty alcohol is a lanolin alcohol or a C.sub.16 -C.sub.18 fatty alcohol. 13. A topical composition according to claim 1 wherein the unsaturated fatty alcohol is oleyl alcohol.