Diterpene glycosides as natural solubilizers

A - Human Necessities – 61 – K

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A61K 9/08 (2006.01) A61K 31/122 (2006.01) A61K 31/165 (2006.01) A61K 31/337 (2006.01) A61K 31/7048 (2006.01) A61K 38/13 (2006.01) A61K 47/26 (2006.01) A61P 43/00 (2006.01)

Patent

CA 2758122

Several diterpene glycosides (e.g., rubusoside, rebaudioside, steviol monoside and stevioside) were discovered to enhance the solubility of a number of pharmaceutically and medicinally important compounds, including but not limited to, paclitaxel, camptothecin, curcumin, tanshinone HA, capsaicin, cyclosporine, erythromycin, nystatin, itraconazole, and celecoxib. The use of the diterpene glycoside rubusoside increased solubility in all tested compounds. The diterpene glycosides are a naturally occurring class of water solubility- enhancing compounds that are non-toxic and that will be useful as new complexing agents or excipients in the pharmaceutical, agricultural (e.g., solubilizing pesticides), cosmetic and food industries. Aqueous solutions by using rubusoside to increase the solubility of otherwise insoluble drugs will have several new routes of administration. In addition, aqueous solutions of therapeutic compounds with rubusoside were shown to retain the known pharmacological activity of the compounds.

On a découvert que plusieurs glycosides de diterpène (par exemple, rubusoside, rébaudioside, monoside de stéviol et stévioside) amplifient la solubilité dun certain nombre de composés importants aux plans pharmaceutique et médicinal, y compris, sans s'y limiter, le paclitaxel, la camptothécine, la curcumine, la tanshinone IIA, la capsaïcine, la cyclosporine, lérythromycine, la nystatine, litraconazole, et le célécoxib. Lutilisation du glycoside de diterpène rubusoside augmente la solubilité de tous les composés testés. Les glycosides de diterpène appartiennent à une classe naturelle de composés augmentant la solubilité dans leau, qui sont non toxiques et qui seront utiles comme nouveaux agents complexants ou excipients dans les industries pharmaceutique, agricole (par exemple, solubilisation de pesticides), cosmétique et alimentaire. Les solutions aqueuses utilisant le rubusoside pour augmenter la solubilité de médicaments sinon insolubles pourront être administrées par plusieurs nouvelles voies dadministration. En outre, linvention montre que des solutions aqueuses de composés thérapeutiques avec le rubusoside conservent lactivité pharmacologique connue des composés.

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