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A Highly Oral Bioavailable Formulation of Curcumin (Ora-Curcumin)

详细技术说明

The present invention is based on the preparation of a novel formulation that potentially enhances the oral bioavailability (% of administered dose reaching blood circulation) of curcumin by increasing its aqueous solubility and also by preventing its metabolic breakdown. This invention will have a great commercial potential as this formulation could be used as a neutraceutical based supplement to prevent or treat several chronic diseases. The recent interest in curcumin formulation by several pharmaceutical/biotech companies further endorses its commercial potential.

*Abstract

Curcumin is herbal neutral-ceutical that has great potential to prevent and treat a wide spectrum of diseases such as cancer, Alzheimer's disease, inflammatory bowel syndrome, arthritis, etc. It is safe to take even at high doses (12 g/day). A regular intake of curcumin as a supplement may delay or prevent these diseases. Despite its high potential in treating various chronic diseases, it is not clinically available for regular use because of its poor oral bioavailability. It is suggested that a person is required to consume large doses (about 12-20 g/day) of curcumin in order to achieve detectable serum concentrations. The peak serum concentration achieved in humans after taking 12 g of curcumin was 50 ng/ml. This means that a person has to take 24 – 40 curcumin capsules of 500 mg each to produce a therapeutic plasma concentration of curcumin. These doses are considered too high, and therefore, not feasible to incorporate in the treatment regimen or use as a meaningful supplement. For any substance, to achieve high oral bioavailability, first it has to dissolve in gastric fluid, permeate through intestinal membrane and should not be metabolized rapidly before, during or immediately after absorption. The lowbioavailability of curcumin is attributed to its extremely low aqueous solubility (-1 g/mL) and high rate of metabolism. Once soluble, curcumin will absorb very well through intestinal membranes. To address the issue of low aqueous solubility of curcumin, several approaches have been explored so far including the use of polymer nanoparticles, liposomes, cyclodextrin inclusion complexes, poIy--caprolactone, solid lipid nanoparticles and biodegradable polymeric micelles, etc. However, the majority of these approaches are not suitable for commercial use of curcumin as a regular oral supplement because the cost of these polymers (liposomes, PLGA, etc.) is very high. On the other hand, use of adjuvants such as piperine, quercetin, green tea and soybean extracts has been widely explored to inhibit the metabolism of curcumin. Among these, piperine is the most promising adjuvant due to its ability to inhibit both hepatic as well as intestinal metabolism (glucoronidation) of curcumin. Preventing the metabolism alone without enhancing the solubility of curcumin was not successful in clinical trials.

国家/地区

美国