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N-乙酰-D-葡萄糖胺的透皮渗透性。

Transdermal permeability of N-acetyl-D-glucosamine.

作者信息

Garner Solomon T, Israel Bridgétte J, Achmed Hishamaldin, Capomacchia Anthony C, Abney Trina, Azadi Parastoo

机构信息

Department of Pharmaceutical and Biomedical Sciences, The University of Georgia, Atlanta, GA 30602, USA.

出版信息

Pharm Dev Technol. 2007;12(2):169-74. doi: 10.1080/10837450701212560.

DOI:10.1080/10837450701212560
PMID:17510888
Abstract

Transdermal permeation of N-acetyl-D-glucosamine (NAG), a metabolite of glucosamine was examined. Glucosamine salts are nutraceuticals used in the oral treatment of osteoarthritis. Sparse information is available regarding glucosamine and NAG transdermal or percutaneous transport and absorption. Permeability of NAG in various enhancer suspensions was evaluated by using shed snakeskin as a model membrane via Franz-type cell diffusion studies. Negligible permeability was observed for NAG in neat solutions of known membrane permeation enhancers ethanol, oleic acid, isopropyl myristate, and isopropyl palmitate, as well as from saturated solutions of NAG in water or phosphate buffer. Permeability measurements obtained from saturated solutions of NAG in DMSO and phosphate buffer solutions containing ethanol at 2%, 5%, 10%, 25%, and 50% demonstrated excellent permeation. Permeability coefficients of the phosphate buffer/ethanol solutions at 5%, 10%, and 25% were about threefold larger in value as those for saturated DMSO solution, whereas the 2% and 50% solution values were lower.

摘要

对氨基葡萄糖的代谢产物N-乙酰-D-氨基葡萄糖(NAG)的透皮渗透进行了研究。氨基葡萄糖盐是用于口服治疗骨关节炎的营养保健品。关于氨基葡萄糖和NAG的透皮或经皮转运及吸收的信息稀少。通过使用脱落的蛇皮作为模型膜,采用Franz型细胞扩散研究评估了NAG在各种增强剂悬浮液中的渗透性。在已知的膜渗透增强剂乙醇、油酸、肉豆蔻酸异丙酯和棕榈酸异丙酯的纯溶液中,以及在NAG的水或磷酸盐缓冲液饱和溶液中,观察到NAG的渗透性可忽略不计。从NAG在二甲基亚砜(DMSO)中的饱和溶液以及含有2%、5%、10%、25%和50%乙醇的磷酸盐缓冲溶液中获得的渗透性测量结果显示出良好的渗透性。5%、10%和25%的磷酸盐缓冲液/乙醇溶液的渗透系数值约为饱和DMSO溶液的三倍,而2%和50%溶液的值较低。

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