LADIKA, Mladen,ZHAO, Jin,TULCHINSKY, Michael L.,KALANTAR, Thomas H.,HARRIS, J. Keith
申请号：
USUS2014/011284
公开号：
WO2014/149160A1
申请日:
2014.01.13
申请国别(地区):
WO
年份:
2014
代理人:
摘要：
The present invention relates to the use of polyalkoxylated alcohols of the formula R-O-(AO)-H, wherein R is a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, aralkyl or heterocyclic group having 7 to 25 carbon atoms, (AO) is a polyoxyalkylene moiety of the composition (BO)m(EO)n(DO)r with random or blockwise arrangement of the constituting oxyalkylene units, wherein m, n and r represent the average number of oxybutylene (BO) units, oxyethylene (EO) units and oxyalkylene units derived from at least one epoxide selected from styrene oxide and alkylene oxides having from 5 to 10 carbon atoms (DO) per molecule of the polyalkoxylated alcohol, respectively, m being a number greater than or equal to 1, n being a number greater than or equal to 1 and r being a number in the range from 0 to 50 under the proviso that (m+n+r) is less than or equal to 200 and the ratio n/(m+r) is in the range of 1 to 20, as excipients in pharmaceutical compositions. Said polyalkoxylated alcohols enable very effective solubilisation of poorly soluble active pharmaceutical ingredients in aqueous media. Solid or semi-solid pharmaceutical compositions comprising one or more such polyalkoxylated alcohol combined with at least one active pharmaceutical ingredient are further long term stable under typical storage conditions and can be readily provided in various dosage forms such as tablets and filled capsules.La présente invention concerne lutilisation dalcools polyalcoxylés de la formule R-O-(AO)-H, dans laquelle R représente un groupe alkyle, alcényle, alcynyle, aryle, aralkyle ou hétérocyclique substitué ou non substitué ayant 7 à 25 atomes de carbone, (AO) représente une fraction polyoxyalkylène de la composition (BO)m(EO)n(DO)r avec une disposition aléatoire ou par bloc des unités oxyalkylène de constitution, où m, n et r représentent le nombre moyen dunités oxybutylène (BO), dunités oxyéthylène (EO) et dunités oxyalkylène issues dau moins un époxyde choisi parmi loxyde de styrène
