HISTAMINE-RELEASE IN DOGS BY CREMOPHOR-EL AND ITS DERIVATIVES - OXETHYLATED OLEIC-ACID IS MOST EFFECTIVE CONSTITUENT

HISTAMINE-RELEASE IN DOGS BY CREMOPHOR-EL AND ITS DERIVATIVES - OXETHYLATED OLEIC-ACID IS MOST EFFECTIVE CONSTITUENT
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DOI:
10.1007/bf01964882
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发表时间:
1977-01-01
期刊:
AGENTS AND ACTIONS
影响因子:
--
通讯作者:
DOENICKE, A
DOENICKE, A
中科院分区:
其他
文献类型:
--
作者:
LORENZ, W;REIMANN, HJ;DOENICKE, A

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在狗中测试Cremophor El®的几种制剂、几种其他非离子洗涤剂和Cremophor El的几种组分的组胺释放能力。Lutensol AP 10和1,2-丙二醇的衍生物是无效的,但作为洗涤剂显示出优异的性能。因此,组胺释放能力不一定与表面活性剂的表面活性剂作用相结合,吐温80和Cremophor El中的油酸似乎是最有效的成分,但醇似乎对组胺释放能力也很重要。开发一种亲脂性药物的无毒增溶剂似乎具有相当大的临床意义。
Several preparations of Cremophor El®, several of other non-ionic detergents and several components of Cremophor El were tested for their histamine-releasing capacity in dogs. Lutensol AP 10 and a derivative of 1,2-propylenglycol were ineffective, but showed excellent properties as detergents. Thus the histamine-releasing capacity was not necessarily combined with the tenside effect of the surfactants.Oleic acid found in Tween 80 as well as in Cremophor El seems to be the most effective constituent, but the alcohol seems also to be important for the histamine-releasing capacity. The development of a non-toxic solubilizer for lipophilic drugs seems of considerable clinical interest.