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通过肠内途径评估油酸水包油包水型多重乳液作为潜在药物载体的性能。

Evaluation of an oleic acid water-in-oil-in-water-type multiple emulsion as potential drug carrier via the enteral route.

作者信息

Oba N, Sugimura H, Umehara Y, Yoshida M, Kimura T, Yamaguchi T

机构信息

First Department of Surgery, Hamamatsu University School of Medicine, Japan.

出版信息

Lipids. 1992 Sep;27(9):701-5. doi: 10.1007/BF02536028.

Abstract

A water-in-oil-in-water (W/O/W) emulsion composed of oleic acid was used as a carrier of carboxyfluorescein (CF) via the enteral route, as a model for future drug transport. The absorption of CF in the small intestine of rats given the emulsion (W/O/W group) was compared with the absorption in a group administered CF alone (CF group), and a group administered a mixed micelle of oleic acid and a surface-active agent in CF solution (MM group). Higher amounts of CF were absorbed in the W/O/W and MM groups than in the CF group. At 120 min, the amount of CF remaining in the intestinal tract was smaller in the MM group than in the W/O/W group. In the early period, CF excretion into bile was higher in the MM group than in the W/O/W group, but from 120 to 360 min, CF excretion in the W/O/W group was higher than in the MM group (non-specific). The blood CF level was significantly higher at 240 and 360 min in the W/O/W group than in the other two groups. The highest concentration in lymph was found in the W/O/W group. The W/O/W emulsion was considered superior to the micelles because it maintained a higher blood level of CF over long periods and transferred it to the lymph. This suggests that the W/O/W emulsion is applicable as a drug carrier via the enteral route.

摘要

一种由油酸组成的水包油包水(W/O/W)乳液通过肠内途径用作羧基荧光素(CF)的载体,作为未来药物运输的模型。将给予该乳液的大鼠(W/O/W组)小肠中CF的吸收与单独给予CF的组(CF组)以及在CF溶液中给予油酸和表面活性剂混合胶束的组(MM组)的吸收进行比较。W/O/W组和MM组中吸收的CF量高于CF组。在120分钟时,MM组肠道中剩余的CF量低于W/O/W组。在早期,MM组胆汁中CF的排泄高于W/O/W组,但在120至360分钟期间,W/O/W组中CF的排泄高于MM组(非特异性)。在240和360分钟时,W/O/W组的血液CF水平显著高于其他两组。在W/O/W组中发现淋巴中的浓度最高。W/O/W乳液被认为优于胶束,因为它能长时间维持较高的CF血液水平并将其转移至淋巴。这表明W/O/W乳液可作为肠内途径的药物载体。

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