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阿苯达唑亚砜的脂质基质:它是全身感染的一种替代选择吗?

Lipidic matrix of albendazole sulphoxide: is it an alternative for systemic infections?

作者信息

Domínguez L, Savio E, Saldaña J, Malanga A, Quevedo D, Camarote C, Ochoa A, Fagiolino P

机构信息

Laboratory of Pharmacology and Biopharmaceutics, Faculty of Chemistry, Montevideo, Uruguay.

出版信息

Boll Chim Farm. 1998 Nov;137(10):383-6.

PMID:9880943
Abstract

As albendazole sulphoxide (ABZS) shows better dissolution properties than albendazole (ABZ), a lipidic matrix with this drug was formulated in order to evaluate if its absorption and so systemic infection chemotherapy could be improved. A cross-over, randomised study in 8 healthy volunteers was carried out, after single administration of 1 g of albendazole or albendazole sulphoxide in lipidic matrix of Gelucire 44/14 (ABZLM and ABZSLM). Absorption was followed performing albendazole sulphoxide dosage in urine samples by high pressure liquid chromatography analysis, during 48 hours. Significant differences were found (p = 0.02) between the urinary recoveries (% E48), being 1.74% and 0.19% the percentage of dose recovered when ABZSLM or of ABZLM were respectively administered. In a previous study of our group similar values were obtained of urinary recovery percentages after albendazole sulphoxide powder administered to another group of healthy volunteers. Lipidic matrix does not improve the physicochemical properties of albendazole sulphoxide powder.

摘要

由于阿苯达唑亚砜(ABZS)的溶解特性优于阿苯达唑(ABZ),因此配制了含有该药物的脂质基质,以评估其吸收情况以及全身感染化疗效果是否能够得到改善。在8名健康志愿者中开展了一项交叉随机研究,单次服用1克阿苯达唑或阿苯达唑亚砜的Gelucire 44/14脂质基质(ABZLM和ABZSLM)后,通过高压液相色谱分析对尿液样本中的阿苯达唑亚砜进行定量,在48小时内跟踪吸收情况。尿液回收率(% E48)之间存在显著差异(p = 0.02),分别服用ABZSLM或ABZLM时,剂量回收百分比分别为1.74%和0.19%。在本研究小组之前的一项研究中,向另一组健康志愿者服用阿苯达唑亚砜粉末后,获得了相似的尿液回收率百分比。脂质基质并未改善阿苯达唑亚砜粉末的物理化学性质。

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