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POLYALKOXYLATED ALCOHOLS AS EXCIPIENTS FOR PHARMACEUTICAL COMPOSITIONS
专利权人:
发明人:
LADIKA MLADEN,ZHAO JIN,TULCHINSKY MICHAEL L,KALANTAR THOMAS H,HARRIS J KEITH
申请号:
IN9091/DELNP/2015
公开号:
IN2015DN09091A
申请日:
2015.10.01
申请国别(地区):
IN
年份:
2016
代理人:
摘要:
The present invention relates to the use of polyalkoxylated alcohols of the formula R-0 -(AO)-H, wherein R is a sub-stituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, aralkyl or heterocyclic group having 7 to 25 carbon atoms, (AO) is a polyoxyal kylene 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.
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