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促渗剂对痛宁凝胶在体经皮渗透性的影响
刘志东1,2, 尹忠鹏1,2, 庞晓晨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, 天津中医药大学, 天津 300193;2.现代中药发现与制剂技术教育部工程研究中心, 天津中医药大学, 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] 研究痛宁凝胶的经皮渗透性,并考察7%Transcutol P和0.5%Labrosal对痛宁凝胶在大鼠体内经皮渗透性的影响.[方法] 应用经皮微渗析在体取样技术,以SD大鼠为模型进行实验.在体回收率采用反向渗析法测定.[结果] 反向渗析法测定的在体回收率对照组为(57.8±5.09)%,7%Transcutol P组为(53.02±1.25)%,0.5%Labrosal组为(46.57±0.49)%,渗析液中的药物的稳态流量(Js)分别为1.06、11.38、2.28ng/h,滞后时间(Tlag)分别为-0.32、0.75、0.25h.[结论] 7%Transcutol P能极大提高药物在渗析液及皮肤中的浓度,适合经皮给药,可进一步应用于痛宁凝胶制剂中.
关键词:  微渗析  痛宁凝胶  促渗剂  经皮吸收  延胡索乙素
DOI:10.11656/j.issn.1672-1519.2013.10.14
分类号:
基金项目:国家重点实验室开放基金项目(SKL2010M0301)
Influence of penetration enhancer on transdermal permeation of Tongning gel in vivo
LIU Zhi-dong1,2, YIN Zhong-peng1,2, PANG Xiao-chen1,2, 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 of 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 Chinese Medicine Pharmaceutical Process, Lianyungang 222001, China
Abstract:
[Objective] To study the transdermal absorption of Tongning gel in rats with or without the widely used enhancer 7% Transcutol P and 0.5% Labrosal. [Methods] Using in vivo transcutaneous sampling technique with micro-dialysis and taking SD rats as the model the experiment was performed. The recovery rate in vivo was assessed with retrograde microdialysis probe.[Results] The in vivo recovery of the control, the 7%Transcutol P and the 0.5% Labrosal was 57.8%±5.09%, 53.02%±1.25% and 46.57%±0.49% respectively. The steady state flux of Tetrahydropalmatine in dialysate(Js) was 1.06, 11.38 and 2.28 ng/h respectively. The lag time was-0.32, 0.75 and 0.25 h. [Conclusion] The concentrations of tetrahydropalmatine in the dialysate and the dermis are increased greatly by 7% Transcutol P. So this preparation is suitable for transdermal drug delivery, and is likely to apply in the preparation of the Tongning gel.
Key words:  microdialysis  Tongning gel  penetration enhancer  transdermal delivery  tetrahydropalmatine
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