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冰片修饰的秋水仙碱醇质体的制备及体外扩散性评价

张楠 宋辉 汪志强 张宇佳 郑稳生

中国药房2018,Vol.29Issue(7):902-906,5.
中国药房2018,Vol.29Issue(7):902-906,5.DOI:10.6039/j.issn.1001-0408.2018.07.09

冰片修饰的秋水仙碱醇质体的制备及体外扩散性评价

Preparation and in vitro Transdermal Permeation Evaluation of Borneol-modified Colchicine Ethosome

张楠 1宋辉 1汪志强 1张宇佳 1郑稳生1

作者信息

  • 1. 北京协和医学院/中国医学科学院药物研究所/药物传输技术及新型制剂北京市重点实验室,北京100050
  • 折叠

摘要

Abstract

OBJECTIVE:To prepare borneol-modified colchicine ethosome,and to evaluate its in vitro transdermal permeation. METHODS:Borneol-modified colchicine ethosome was prepared with ultrasonic injection-probe ultrasonic method,and its ethosome was characterized. The content and moditication rate of borneol in borneol-modified colchicine ethosome was determined by GC;content and encapsulation rate of colchicine was determined by HPLC.Accumulative permeability and permeation rate were investigated for colchicine ethanol solution,colchicine-borneol-ethanol solution,colchicine ethosome without borneol-modification, borneol- modified colchicine ethosome after diffused for 1,3,6,8,12,16,24,48 h. RESULTS:The average particle size of borneol- medified colchicine ethosome was about(110.4 ± 5.1)nm,polydispersity index was 0.110 ± 0.030,Zeta potential was (2.33±0.20)mV,prepared ethosome is approximately spherical in shape and multilaminar vesicles in structure. Encapsulation rate of colchicine was 56.12%,and modification rate was 9.85%. The in vitro diffusion tests showed that after diffused for 48 h, accumulative permeability per unit area of borneol-modified colchicine ethosome was 103.52 μ g/cm2;permeation rate was 1.26 times as colchicine ethosome without borneol-modification,1.77 times as colchicine-borneol-ethanol solution and 5.14 times as colchicine ethanol solution. CONCLUSIONS:Prepared borneol-modified colchicine ethosome has small particle size,narrow particle size distribution,high modification rate and good transdermal permeation.

关键词

秋水仙碱/冰片修饰/醇质体/制备/修饰率/体外扩散/包封率/累积渗透量

Key words

Colchicine/Borneol-modified/Ethosome/Preparation/Modification rate/in vitro diffusion/Encapsulation rate/Accumulative permeability

分类

医药卫生

引用本文复制引用

张楠,宋辉,汪志强,张宇佳,郑稳生..冰片修饰的秋水仙碱醇质体的制备及体外扩散性评价[J].中国药房,2018,29(7):902-906,5.

基金项目

国家科技重大专项子课题(No.2014ZX09507006) (No.2014ZX09507006)

中国医学科学院医学与健康科技创新工程(No.2017-I2M-1-011) (No.2017-I2M-1-011)

中国药房

OA北大核心CSTPCD

1001-0408

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