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首页> 外文期刊>Life sciences >A novel emulsifier, labrasol, enhances gastrointestinal absorption of gentamicin.
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A novel emulsifier, labrasol, enhances gastrointestinal absorption of gentamicin.

机译：新型乳化剂拉布拉索可增强庆大霉素在胃肠道的吸收。

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Gentamicin (GM) is an important aminoglycoside antibiotic for the treatment of infections caused by a wide spectrum of aerobic gram-negative bacilli and gram-positive cocci. As a class, the aminoglycosides are poorly absorbed from the gastrointestinal (GI) tract and are commonly used as injectable and topical preparations. This study was aimed at finding the effect of a novel emulsifier, Labrasol, on the absorption of GM from the GI tract of rats. GM formulations were prepared, either as saline solution or as Labrasol microemulsions, and were administrated to rat small intestine and colon. Plasma GM levels following intestinal application were compared to those obtained with intravenous (i.v.) administration. A 5 mg/kg dose of GM preparation containing Labrasol, 1 ml/kg, administrated into colon resulted in the mean AUC of 21.179+/-1.374 microg x h/ml, compared to 7.813+/-0.105 microg x h /ml obtained with i.v. administration of GM, 1 mg/kg. The absolute bioavailability (BA) of the Labrasol preparation was 54.2%. Labrasol facilitates the transmucosal delivery of GM from rat colon by forming microemulsions, and the BA obtained with Labrasol microemulsion was higher than with other surfactants (8.4% for Tween 80 and 3.4% for Transcutol P). Additionally, in vitro permeation studies demonstrated that Labrasol also inhibited the intestinal secretory transport. The effect of Labrasol is ascribed to both (1) enhanced GM absorption from the GI lumen into the systemic circulation and (2) inhibition of efflux of GM from the enterocytes to the GI lumen.
机译：庆大霉素（GM）是一种重要的氨基糖苷类抗生素，用于治疗由多种需氧革兰氏阴性杆菌和革兰氏阳性球菌引起的感染。作为一类，氨基糖苷类药物很难从胃肠道吸收，通常用作注射剂和局部用制剂。这项研究旨在发现新型乳化剂拉布拉索对大鼠胃肠道中GM吸收的影响。 GM制剂可以盐溶液或Labrasol微乳形式制备，并用于大鼠小肠和结肠。将肠内施用后的血浆GM水平与静脉内（i.v.）施用获得的血浆GM水平进行比较。施用给结肠的5mg / kg剂量的包含Labrasol的1ml / kg的GM制剂导致21.179 +/-1.374μg×h / ml的平均AUC，而通过静脉注射获得的7.813 +/-0.105μg×h / ml。 GM，1 mg / kg。 Labrasol制剂的绝对生物利用度（BA）为54.2％。 Labrasol通过形成微乳状液，促进了GM从大鼠结肠的透粘膜递送，并且用Labrasol微乳状液获得的BA高于使用其他表面活性剂（Tween 80为8.4％，Transcutol P为3.4％）。另外，体外渗透研究证明拉布拉索尔还抑制肠的分泌转运。 Labrasol的作用归因于（1）从GI腔进入全身循环的GM吸收增强，以及（2）GM从肠细胞到GI腔的外排抑制。

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