|Abstract:||A pharmaceutical composition comprising: (A) an androgen; (B) a cyclic enhancer of the type used in the compositions and methods claimed by U.S. Pat. No. 5,023,252 to Hsieh; and (C) a thickening agent; including, for example, a composition in which the cyclic enhancer is a macrocyclic ester or a macrocyclic ketone; the use of the composition to treat a condition, for example, male hypogonadism, in a patient by applying the composition to the membrane of the patient; and a method for making the composition.|
|Inventor(s):||Gyurik; Robert J. (Exeter, NH)|
|Assignee:||FCB I LLC (Wilmington, DE)|
1. A method for maintaining a therapeutically effective concentration of testosterone in the blood serum of a male for treating hypogonadism which comprises
transdermally delivering to the male by applying to the skin a composition which is in the form of a topical gel, which has a viscosity of about 500 to about 20,000 cps and a pH of about 3 to about 9, and comprises: (A) about 0.1 to about 5 wt. % of
testosterone; (B) about 0.5 to about 25 wt. % of a Hsieh enhancer; (C) about 0.1 to about 10 wt. % of a thickening agent; and (D) a mixture of solvents which include about 40 to about 80 wt. % of lower alkanol; wherein the Hsieh enhancer is selected
from the group consisting of 3-methylcyclopentadecanone, 9-cycloheptadecen-1-one, cyclohexadecanone, cyclopentadecanone and oxacyclohexadecan-2-one.
2. The method according to claim 1 in which testosterone is delivered transdermally to the blood of a male patient by use of the composition in the form of a unit dose such that, following a single application of the unit dose to the patient, the amount of circulating testosterone (AUC.sub.0-24) in the blood serum of the patient achieved in the 24-hour period following the application is about 100 to about 35,000 ngh/dL greater than the amount of circulating testosterone (AUC.sub.0-24) in the blood serum of the patient that would have been achieved in the same 24-hour period had the dose not been administered.
3. The method of claim 1, wherein the composition further comprises a crystallization inhibitor.
4. The method of claim 3, wherein the crystallization inhibitor is polyethylene glycol.
5. The method of claim 4, wherein the polyethylene glycol is present in an amount ranging from about 0.001 to about 5 wt. %.
6. The method of claim 1, wherein the composition has a viscosity ranging from about 1,000 to about 9,000 cps.
7. The method of claim 1, wherein the composition has a pH ranging from about 4 to about 8.
8. The method of claim 1, wherein the mixture of solvents comprises a co-solvent selected from the group consisting of glycerin, propylene glycol, polyethylene, polypropylene, silicone and mixtures thereof.
9. The method of claim 8, wherein the co-solvent comprises glycerin.
10. The method of claim 8, wherein the co-solvent comprises propylene glycol.