Bassissi Firas, Lespine Anne, Alvinerie Michel
INRA-Toulouse, Laboratoire de Pharmacologie-Toxicologie, Toulouse, France.
Parasitol Res. 2006 Feb;98(3):244-9. doi: 10.1007/s00436-005-0073-z. Epub 2005 Dec 10.
Ivermectin is a member of the macrocyclic lactone family widely used in livestock, pets, and humans as a potent parasiticide. Slight differences in formulation may change the plasma kinetics and efficacy of these compounds. The aim of the study is to evaluate the ability of a liposomal formulation of ivermectin to generate an efficient exposure of the animal to the drug. Ten rabbits were subcutaneously administered with 0.3 mg kg(-1) of ivermectin using Ivomec (n=5) or a liposomal formulation (n=5). The areas under serum concentration-time curve were similar after both treatments, indicating the same bioavailability for the two formulations. However, the liposomal formulation gave a higher C(max) value (33.33 ng ml(-1)) compared with Ivomec (20.82 ng ml(-1)) and a significantly faster absorption as indicated by the T(max) of 0.23 days compared with 1.13 days for the Ivomec formulation. The use of liposomal formulation shows promise as this system improves the efficacy of ivermectin and related drugs.
伊维菌素是大环内酯类药物家族的一员，作为一种强效驱虫剂，广泛应用于家畜、宠物和人类。制剂上的细微差异可能会改变这些化合物的血浆动力学和疗效。本研究的目的是评估伊维菌素脂质体制剂使动物有效接触该药物的能力。十只兔子皮下注射0.3 mg kg(-1)的伊维菌素，其中五只使用伊沃梅克（Ivomec），另外五只使用脂质体制剂。两种治疗后血清浓度-时间曲线下面积相似，表明两种制剂的生物利用度相同。然而，脂质体制剂的C(max)值更高（33.33 ng ml(-1)），相比伊沃梅克（20.82 ng ml(-1)），并且吸收明显更快，脂质体制剂的T(max)为0.23天，而伊沃梅克制剂为1.13天。脂质体制剂的应用显示出前景，因为该系统提高了伊维菌素及相关药物的疗效。
