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Generated: May 27, 2018

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Claims for Patent: 6,787,529

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Summary for Patent: 6,787,529
Title: Topical composition
Abstract:The present invention relates to a pharmaceutical gel composition for application on skin, said composition comprising at least one vitamin D or vitamin D analogue and at least one corticosteroid as well as a viscosity-increasing excipient.
Inventor(s): H.o slashed.y; Gert (Jyllinge, DK), Didriksen; Erik Johannes (Ballerup, DK)
Assignee: Leo Pharmaceutical Products Ltd. A/S (Ballerup, DK)
Application Number:09/984,072
Patent Claims: 1. A substantially non-aqueous pharmaceutical gel composition for application on skin, said composition comprising at least one vitamin D analogue selected from the group consisting of seocalcitol; calcipotriol; hydrate of calcipotriol; calcitriol; tacalcitol, maxacalcitol; paricalcitol; falecalcitriol; 1.alpha., 24S-dihydroxy-vitamin D2; and 1(S),3(R)-dihydroxy-20(R)-[((3-(2-hydroxy-2-propyl)-phenyl)-methoxy)-methy l]-9,10-secopregna-5(Z),7(E),10(19)-triene and mixtures thereof, at least one corticosteroid, a viscosity-increasing excipient in an amount resulting in a viscosity in the range of from about 5 mPa.s to about 500 mPa.s, and at least one solvent selected from the group consisting of: (i) compounds of the general formula R.sup.3 (OCH.sub.2 C(R.sup.1)H).sub.x OR.sup.2 (I) wherein x is in the range of 2-60, R.sup.1 in each of the x units independently is H or CH.sub.3, R.sup.2 is straight chain or branched C.sub.1-20 alkyl or benzoyl, and R.sup.3 is H or phenylcarbonyloxy; (ii) di-(straight or branched)-C.sub.4-10 alkyl esters of C.sub.4-C.sub.8 dicarboxylic acids; (iii) straight or branched C.sub.12-18 -alkyl benzoates; (iv) straight or branched C.sub.2-4 -alkyl esters of straight or branched C.sub.10-18 -alkanoic or -alkenoic acids; (v) propylenglycol diesters with C.sub.8-14 -alkanoic acids; and (vi) branched primary C.sub.18-24 alkanols, said composition being stable when stored at 40.degree. C. for 3 months.

2. The composition according to claim 1, which has a viscosity in the range of from about 10 mPa.s to about 250 mPa.s.

3. The composition according to claim 1, wherein the viscosity-increasing excipient is a thixotropic gelling agent.

4. The composition according to claim 3, wherein the thixotropic gelling agent is hydrogenated castor oil.

5. The composition according to claim 1, wherein said composition comprises a viscosity-increasing excipient which is a wax, polyethylene or a microcrystalline wax.

6. The composition according to claim 1, wherein said solvent is selected from compounds of the general formula H(OCH.sub.2 C(R.sup.1)H).sub.x OR.sup.2 (I) wherein R.sup.1, x, and R.sup.2 are as defined in claim 1 and mixtures thereof.

7. The composition according to claim 1, wherein R.sup.1 is CH.sub.3.

8. The composition according to claim 6, wherein said solvent is polyoxypropylene-15-stearyl ether.

9. The composition according to claim 1, wherein said vitamin D analogue is selected from the group consisting of calcipotriol; calcitriol; tacalcitol, maxacalcitol; 1(S),3(R)-dihydroxy-20(R)-[((3-(2-hydroxy-2-propyl)-phenyl)-methoxy)-methy l]-9,10-seco-pregna-5(Z),7(E),10(19)-triene, as well as mixtures thereof,

10. The composition according to claim 1, wherein the vitamin D analogue is effective against psoriasis and sebo-psoriasis of the scalp in humans.

11. The composition according to claim 1, wherein said vitamin D analogue is calcipotriol or its hydrate.

12. The composition according to claim 1, wherein said corticosteroid is selected from the group consisting of Betamethasone, Clobetasol, Clobetasone, Desoximethasone, Diflucortolon, Diflorasone, Fluocinonid, Flumethasone, Fluocinolon, Fluticasone, Fluprednidene, Halcinonide, Hydrocortisone, Momethasone, Triamcinolon, Pharmaceutically acceptable esters thereof, acetonides thereof and mixtures thereof.

13. The composition according to claim 12, wherein said esters or acetonides are selected from the group consisting of 17-valerate, 17-propionate, 17,21-dipropionate acetonide, acetonide-21N-benzoyl-2-methyl-.beta.-alaninate, acetonide-21-(3,3-dimethylbutyrate) and 17-butyrate.

14. The composition according to claim 1, wherein said composition contains 0.001-0.25 mg/g or ml of said vitamin D analogue and 0.05-2 mg/g or ml of said corticosteroid.

15. The composition according to claim 1, wherein said composition comprises the following ingredients (per g of the composition): betamethasone (as dipropionate: 0.643 mg) 0.5 mg calcipotriol (as hydrate: 52.2 .mu.g) 50 .mu.g polyoxypropylene-15-stearyl ether 170 mg hydrogenated castor oil 30 mg heptamethylnonane to make 1 g.

16. The composition according to claim 1, which further comprises an antifungal agent.

17. The composition according to claim 1 for application on the scalp.

18. The composition according to claim 17, additionally comprising a surfactant.

19. The composition according to claim 18, wherein the surfactant is selected from the group consisting of octoxynol-n of formula C.sub.8 H.sub.17 C.sub.6 H.sub.4 (OCH.sub.2 CH.sub.2).sub.n OH, wherein n is an integer of from 1 to 70, nonoxynol-n of formula C.sub.9 H.sub.19 C.sub.6 H.sub.4 (OCH.sub.2 CH.sub.2).sub.p OH, wherein p is an integer of from 4 to 40, and a polyoxyethylene C.sub.12-22 alkyl ether.

20. A method of treating psoriasis or sebo-psoriasis of the scalp, the method comprising administering to an affected skin area of a patient in need thereof an effective amount of the composition according to claim 1.

21. The method of claim 20, wherein said composition is administered once or twice a day.

22. The method of claim 20, wherein said composition is administered to the scalp.

23. The method of claim 20, wherein said composition is administered once a day.

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Serving hundreds of leading biopharmaceutical companies globally:

Farmers Insurance
Cerilliant
McKinsey
Chinese Patent Office
Express Scripts
Baxter
Johnson and Johnson
Daiichi Sankyo
Fish and Richardson

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