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[粒径和乳化剂对胃肠外给予脂肪乳剂药代动力学值的影响]

[Effect of particle size and emulsifier on pharmacokinetic values of a parenterally administered fat emulsion].

作者信息

Weidler B, Peil J, von Bormann B, Lohmann E, Elmadfa I, Sommermeyer K, Schwanen N

出版信息

Infusionsther Klin Ernahr. 1987 Apr;14(2):78-88.

PMID:3610312
Abstract

To evaluate pharmacokinetic data during parenteral application of a fat emulsion a controlled study in healthy volunteers was performed. Another aim of the study was to investigate whether these kinetics could be changed by modification of the emulsion. For this purpose, 10 male medical students--free of any metabolic disorders--received modified batches of one fat emulsion (Lipovenös), differing with respect to particle size or emulsifier. The emulsions were applied using a pump-controlled continuous infusion technique. The dosage was calculated according to body weight: 0.1 g/kg B.W./h. There was a 7-10 day interval between one application and the following study period, again using the same volunteers. Thus every volunteer served as his own control. Routine laboratory parameters as well as parameters relating to fat metabolism were measured. While routine laboratory parameters were not statistically different between the groups, pharmacokinetic data showed differences according to the batches used. Highest triglyceride and free fatty acid levels i.s. were present after application of the emulsion with low medium particle size, while lowest levels were found after increasing the particle size to 380 nm. In addition, it could be documented that an increase in medium particle size resulted in higher elimination rate, transfer and pool size. The modified emulsifier led to an additional increase of these effects, thus inducing beneficial metabolic profiles. The results of the present investigation might perhaps enable us to adjust the profile of future fat emulsions, with the aim of optimizing or restoring metabolic hemostasis.

摘要

为了评估脂肪乳剂肠胃外应用期间的药代动力学数据,在健康志愿者中进行了一项对照研究。该研究的另一个目的是调查这些动力学是否会因乳剂的改变而发生变化。为此,10名无任何代谢紊乱的男性医学生接受了一批经过改良的脂肪乳剂(Lipovenös),这些乳剂在粒径或乳化剂方面存在差异。采用泵控连续输注技术应用这些乳剂。剂量根据体重计算:0.1 g/kg体重/小时。一次应用与下一个研究阶段之间间隔7至10天,再次使用相同的志愿者。因此,每个志愿者都作为自己的对照。测量了常规实验室参数以及与脂肪代谢相关的参数。虽然各组之间的常规实验室参数没有统计学差异,但药代动力学数据根据所用批次显示出差异。中等粒径较低的乳剂应用后,甘油三酯和游离脂肪酸水平最高,而粒径增加到380 nm后,水平最低。此外,可以证明中等粒径的增加会导致更高的消除率、转运和池大小。改良的乳化剂导致这些作用进一步增加,从而产生有益的代谢特征。本研究结果或许能使我们调整未来脂肪乳剂的特性,以优化或恢复代谢稳态。

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