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4种促渗剂对痛宁凝胶中 延胡索乙素离体鼠皮透过的研究
尹忠鹏1,2, 庞晓晨1,2, 刘志东1,2, 张倩1,2, 萧伟3,4
1.天津市现代中药重点实验室-省部共建国家重点实验室培育基地, 天津 300193;2.现代中药发现与制剂技术教育部工程研究中心, 天津 300193;3.江苏康缘药业股份有限公司, 连云港 222001;4.中药制药过程新技术国家重点实验室, 连云港 222001
摘要:
[目的] 研究新型促渗剂氮酮(Azone)、Transcutol P(Trans P)、Labrasol(Lab)以及传统促渗剂丙二醇(PG)对痛宁凝胶中延胡索乙素透皮行为的影响。[方法] 采用改良Franz 扩散池, 考察Trans P、Lab、Azone和PG 在不同浓度下, 对痛宁凝胶中延胡索乙素离体大鼠皮透过行为的影响。[结果] 与空白对照组相比, 0.5%Lab、0.5%PG、0.5%Azone、3%Azone与7%Trans P的表观渗透系数分别提高了1.50、1.52、1.42、1.46和1.66倍, 差异有统计学意义(P<0.01).几种促渗剂对延胡索乙素透过的促渗作用依次为7% Trans P>0.5%PG>0.5%Lab>3%Azone>0.5%Azone.[结论] 0.5%Lab、0.5%PG、0.5%Azone、3%Azone和7%Trans P促渗效果比较明显, 可进一步应用于痛宁凝胶制剂中。
关键词:  促渗剂  痛宁凝胶  延胡索乙素  经皮吸收
DOI:10.11656/j.issn.1672-1519.2013.03.18
分类号:
基金项目:国家重点实验室开放基金项目(SKL2010M0301).
Effects of four kinds of penetration enhancers on percutaneous absorption of Tetrahydropulmatine in Tongning gel in vitro
YIN Zhong-peng1,2, PANG Xiao-chen1,2, LIU Zhi-dong1,2, ZHANG Qian1,2, XIAO Wei3,4
1.Tianjin Modern Chinese Medicine Key Laboratory-Province and Ministry Co-established State Key Laboratory Cultivation Base, Tianjin University of TCM, Tianjin 300193, China;2.Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry f Education, Tianjin University of TCM Tianjin 300193, China;3.Jiangsu Kanion Pharmaceut Co. Ltd., Lianyungang 222001, China;4.State Key Laboratory of New-tech for ChineseMedicine Pharmaceutical Process, Lianyungang 222001, China
Abstract:
[Objective] To study the effects of Azone, Trans P, Lab and PG on percutaneous absorption of Tetrahydropulmatine across the skin of rats. [Methods] The Franzdiffusion chamber was applied for evaluating the effect of each penetration enhancer(PE) with different concentrations on the percutaneous absorption of tetrahydropulmatine in vitro. [Results] Compared with the control group, 0.5%Lab, 0.5%PG, 0.5%Azone, 3%Azone and 7% Trans P showed the permeability coefficient as much as 1.50, 1.52, 1.42, 1.46 and 1.66 folds respectively (P<0.01). Their penetration-increasing rates were 7% Trans P﹥0.5% PG﹥0.5%Lab﹥3%Aone﹥0.5%Azone in turn. [Conclusion] The enhancing effect of 0.5%Lab, 0.5%PG, 0.5%Azone, 3%Azone and 7%Trans P is significant and can be further used in the preparation of Tongning gel.
Key words:  penetration enhancer  Tongning gel  Tetrahydropulmatine  percutaneous absorption
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