| 摘要 |
The invention provides novel curcuminoid formulations which have improved aqueous solubility and bioavailability when compared to known curcuminoid dosage forms. Formulations of the invention exhibit an enhanced intestinal absorption of curcuminoids, a slower curcuminoid metabolism and a reduced rate of systemic curcuminoid elimination. Additionally, upon administration in vivo, the formulations described and claimed herein produce a high, sustained level of the curcuminoid metabolite tetrahydrocurcumin. For example, at about eight to about ten hours after oral administration to a human, tetrahydrocurcumin plasma levels of between about 50 ng/mL to about 175 ng/mL are detectable, even when that metabolite is absent from the administered formulation. Novel processes for making curcuminoid formulations which have improved aqueous solubility and oral bioavailability, and methods of treating a wide variety of inflammatory, immune and neurogenerative disorders and cancers, are also provided. |
| 主权项 |
1. A pharmaceutical composition comprising:
(a) a therapeutically effective amount of one or more curcuminoids, curcuminoid analogs and/or curcuminoid metabolites; (b) an absorption enhancer; and, optionally, (c) a water-in-oil emulsifier and/or essential oil of Curcuma longa L. (turmeric oil); and (d) optionally, one or more additional, pharmaceutically-acceptable excipients; wherein the weight percentage ratio of the one or more curcuminoids, curcuminoid analogs and/or curcuminoid metabolites to the absorption enhancer is between about 20:1 to about 1:60, or between about 15:1 to about 1:45, or between about 10:1 to about 1:40, or between about 9:1, 8:1, 7:1, 6:1, 5:1, 4:1, 3:1, 2:1 or 1:1 to about 1:2, 1:3, 1:4, 1:5, 1:6, 1:7, 1:8, 1:9, 1:10, 1:15, 1:20, 1:25, 1:30, or 1:35, and preferably is about 20:1, 19:1, 18:1, 17:1, 16:1, 15:1, 14:1, 13:1, 12:1, 11:1, 10:1, 9:1, 8:1, 7:1, 6:1 or 5:1. |
