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专利名称：Method of preparation of a soluble
formulation of water-insoluble pentacyclicand tetracyclic terpenoids, a solubleformulation of a pentacyclic or tetracyclicterpenoid and a pharmaceutical compositioncontaining this soluble formulation
发明人：Jan Sarek,Marian Hajduch,Michal
Svoboda,Katerina Novakova,Pavla
Spacilova,Tomas Kubelka,David Biedermann
申请号：US12443304申请日：20070925公开号：US08653056B2公开日：20140218
摘要：The invention relates to a method of preparation of a soluble formulation ofwater-insoluble pentacyclic and tetracyclic terpenoids, wherein the water-insolubleterpenoid having a free carboxylic, hydroxy or amino functional group is derivatized onthis functional group with a substituent selected from the group comprising substituentsof general formula Xa bound to the hydroxy group of the terpenoid, wherein Xa is —OC—R—COOH, substituents of general formula Xa bound to the amino group of theterpenoid, wherein Xa is —OC—R—COOH, quarternary ammonium substituents ofgeneral formula Xb bound to the carboxy group of the terpenoid, wherein Xb is —(CH2)nN+R3Y—, quarternary ammonium substituents of general formula Xc bound to thecarboxy group of the terpenoid, wherein Xc je —(CH2)nR+Y—, substituents of general
formula Xd bound to the carboxy group of the terpenoid, wherein Xd represents —R—COOH, glycosylic substituents Xe bound by alpha or beta glycosidic bond to the hydroxygroup or to the carboxy group of the terpenoid, wherein Xe is selected from the groupcomprising glucosyl, galactosyl, arabinosyl, rhamnosyl, lactosyl, cellobiosyl, maltosyl andthe 2-deoxyanalogues thereof, and subsequently, the prepared derivative is dissolved inthe solution containing water, a cyclodextrin and optionally pharmaceutically acceptableauxiliary substances, forming an inclusion derivative with the cyclodextrin. Object of theinvention is further a soluble formulation of a pentacyclic or tetracyclic triterpenoid,containing an inclusion complex of the derivatized pentacyclic or tetracyclic terpenoidwith a cyclodextrin, and optionally water and pharmaceutically acceptable auxiliarysubstances and further a pharmaceutical composition containing the soluble formulation.
申请人：Jan Sarek,Marian Hajduch,Michal Svoboda,Katerina Novakova,PavlaSpacilova,Tomas Kubelka,David Biedermann
地址：Horni Mecholupy CZ,Moravsky Beroun CZ,Praha CZ,Kladno CZ,Ostrava CZ,PrahaCZ,Praha CZ
国籍：CZ,CZ,CZ,CZ,CZ,CZ,CZ
代理机构：Notaro, Michalos & Zaccaria P.C.
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