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不同制剂中红霉素的局部给药:一项无毛小鼠体内研究。

Topical delivery of erythromycin from various formulations: an in vivo hairless mouse study.

作者信息

Jayaraman S C, Ramachandran C, Weiner N

机构信息

College of Pharmacy, University of Michigan, Ann Arbor 48109-1065, USA.

出版信息

J Pharm Sci. 1996 Oct;85(10):1082-4. doi: 10.1021/js960040u.

Abstract

Topical products containing erythromycin, a macrolide antibiotic with poor aqueous solubility, are usually formulated as high alcohol content solutions or gels. In this study, we evaluated the deposition of erythromycin base into various strata of hairless mouse skin following topical in vivo application from various low- and nonalcoholic formulations. The formulations tested included nonionic liposomal formulation composed of glyceryl dilaurate, cholesterol, and polyoxyethylene-10-stearyl either at a weight ratio of 57:15:28, two nonionic oil-in-water (o/w) liposomal emulsions containing isopropyl myristate or light mineral oil as the oil phase, a conventional o/w emulsion, a 40% hydroalcoholic solution, and two commercially available topical products. Eight hours after topical administration of these formulations, the efficiency of uptake of erythromycin into the living skin strata was in the order: liposomal isopropyl myristate emulsion > > liposomal mineral oil emulsion > > nonionic liposomes approximately Emgel approximately Theramycin-Z > > conventional emulsion > > hydroalcoholic solution. Alcohol-free liposomal systems are shown to be as efficient as high alcohol content products in facilitating permeation of erythromycin through the stratum corneum into living skin tissue.

摘要

含有红霉素(一种水溶性差的大环内酯类抗生素)的局部用产品通常被配制成高酒精含量的溶液或凝胶。在本研究中,我们评估了在体内从各种低酒精和无酒精制剂局部应用后,红霉素碱在无毛小鼠皮肤各层中的沉积情况。所测试的制剂包括由二月桂酸甘油酯、胆固醇和聚氧乙烯-10-硬脂酸酯按重量比57:15:28组成的非离子脂质体制剂、两种以肉豆蔻酸异丙酯或轻质矿物油为油相的非离子水包油(o/w)脂质体乳液、一种传统的o/w乳液、一种40%的水醇溶液以及两种市售局部用产品。在局部应用这些制剂8小时后,红霉素进入活皮肤层的摄取效率顺序为:脂质体肉豆蔻酸异丙酯乳液>>脂质体矿物油乳液>>非离子脂质体≈Emgel≈Theramycin-Z>>传统乳液>>水醇溶液。无酒精脂质体系统在促进红霉素透过角质层进入活皮肤组织方面显示出与高酒精含量产品一样有效。

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