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川芎嗪体外透皮的特性

Study on Transdermal Permeability of Tetramethylpyrazine

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【作者】 翁伟宇; 徐惠南;

【Author】 Weng Weiyu,Xu Huinan (Department of Pharmaceutics,School of Pharmacy,Shanghai Medical University,Shanghai 200032)

【机构】 上海医科大学药学院药剂学教研室!上海200032;

【摘要】 目的 研究川芎嗪的基本透皮特性。方法 采用VC水平扩散池,以渗透系数为指标研究川芎嗪在完整小鼠、大鼠、裸鼠皮肤、人皮和去角质层大鼠皮肤中的透过性。考察常用促透剂乙醇、丙二醇、月桂氮卓艹酮(Azone)和一些挥发油对川芎嗪透皮特性的影响。结果 川芎嗪能较好透过皮肤,其渗透系数受药物浓度、解离度和介质pH值等因素的影响。在所用各类透皮促进剂中,2%桉油的促透效果最好,优于同浓度的Azone。结论 本研究的结果为川芎嗪透皮制剂的研制奠定了理论基础

【Abstract】 To investigate the transdermal permeability of tetramethylpyrazine (TMP). Methods HPLC was need to determine the concertration of TMP in skin extraction. Results It was found that the rat skin was a suitable model of human skin and the stratum corneum was the main barrier to the permeation of TMP.The fluxs of TMP were affected by drug concentration,ionization degree and pH value of solvent. Permeation experiments revealed that the penetration enhancers varied in their abilities to enhance the fluxs of TMP.1%-3% Azone greatly increased the fluxs and the permeability coefficient of TMP in 2% Azone was 8 times greater than that of the controlled group.EtOH and PG were less effective enhancers and both of them showed negative influence in high concentration.The volatile oils used in the present work all had enhancing ability among which the potency of Eucalyptus oil was greater than that of Azone.The mixture of EtOH,PG and Azone did not reveal any cooperative effect. Results It was found that the rat skin was a suitable model of human skin and the stratum corneum was the main barrier to the permeation of TMP.The fluxs of TMP were affected by drug concentration,ionization degree and pH value of solvent. Permeation experiments revealed that the penetration enhancers varied in their abilities to enhance the fluxs of TMP.1%-3% Azone greatly increased the fluxs and the permeability coefficient of TMP in 2% Azone was 8 times greater than that of the controlled group.EtOH and PG were less effective enhancers and both of them showed negative influence in high concentration.The volatile oils used in the present work all had enhancing ability among which the potency of Eucalyptus oil was greater than that of Azone.The mixture of EtOH,PG and Azone did not reveal any cooperative effect. Conclusions TMP is a suitable drug for transdermal delivery system and deserved for further studies.

  • 【文献出处】 上海医科大学学报 , 编辑部邮箱 ,1999年05期
  • 【分类号】R944.9
  • 【被引频次】29
  • 【下载频次】225
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