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专利名称：METHOD OF PREPARATION OF A SOLUBLE
FORMULATION OF WATER-INSOLUBLEPENTACYCLIC AND TETRACYCLIC
TERPENOIDS, A SOLUBLE FORMULATION OFA PENTACYCLIC OR TETRACYCLICTERPENOID AND A PHARMACEUTICALCOMPOSITION CONTAINING THIS SOLUBLEFORMULATION
发明人：SAREK, Jan,HAJDUCH, Marian,SVOBODA,
Michal,NOVAKOVA, Katerina,SPACILOVA,Pavla,KUBELKA, Tomas,BIEDERMANN, David
申请号：EP07801129.3申请日：20070925公开号：EP2068882A2公开日：20090617
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 the terpenoid,wherein Xa is -OC-R-COOH, quarternary ammonium substituents of general formula Xbbound to the carboxy group of the terpenoid, wherein Xb is -(CH2)nN+R3Y-, quarternary
ammonium substituents of general formula Xc bound to the carboxy group of theterpenoid, wherein Xc je -(CH2)nR+Y-, substituents of general formula Xd bound to thecarboxy group of the terpenoid, wherein Xd represents -R-COOH, glycosylic substituentsXe bound by alpha or beta glycosidic bond to the hydroxy group or to the carboxy groupof the terpenoid, wherein Xe is selected from the group comprising glucosyl, galactosyl,arabinosyl, rhamnosyl, lactosyl, cellobiosyl, maltosyl and the 2-deoxyanalogues thereof,and subsequently, the prepared derivative is dissolved in the solution containing water, acyclodextrin and optionally pharmaceutically acceptable auxiliary substances, forming aninclusion derivative with the cyclodextrin. Object of the invention is further a solubleformulation of a pentacyclic or tetracyclic triterpenoid, containing an inclusion complex ofthe derivatized pentacyclic or tetracyclic terpenoid with a cyclodextrin, and optionallywater and pharmaceutically acceptable auxiliary substances and further a pharmaceuticalcomposition containing the soluble formulation.
申请人：Univerzita Karlova V Praze, Prírodovedecká Fakulta,Univerzita palackeho VOlomouci,I.Q.A., A.S.
地址：Albertov 6 128 43 Praha 2 CZ,Krizkovskeho 8 77147 Olomouc CZ,JindrichaPlachty 16 150 00 Praha 5 CZ
国籍：CZ,CZ,CZ
代理机构：Gabrielova, Marta
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