Pharmacokinetics study on matrine gels based on micro dialysis
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摘要: 目的 建立同步测定经皮给药制剂在皮肤、血液中药动学的方法,研究苦参碱凝胶在体内的药动学行为。 方法 应用经体外和体内回收率校正建立的基于微透析探针的皮肤血液双位点同步微透析系统,通过在皮肤和颈静脉植入探针,在大鼠腹部脱毛部位给予苦参碱凝胶,连续收集探针中12 h的透析液,并采用LC-MS微量检测技术测定探针透析液中的药物浓度。 结果 本研究成功构建了双位点同步微透析药动学评价系统,大鼠皮肤给予苦参碱凝胶后,皮肤中的药物浓度、AUC值、半衰期均显著高于血液中药物浓度。 结论 本研究建立的微透析结合LC-MS的取样及检测技术为经皮给药制剂的药动学研究提供了新的技术平台。Abstract: Objective To establish a pharmacokinetic method for simultaneous determination the drug concentration in the skin and blood for transdermal formulations,and to study the absorption and metabolism of matrine gel in vivo. Methods A micro dialysis probe-based skin-blood synchronous micro dialysis system was established.After the probe was implanted into the skin and jugular vein,the matrine gel was administered.The dialysate in the probe was continuously collected for 12 h.The concentration of the drug in the probe dialysate was determined by LC-MS. Results In this study,a two-site synchronous micro dialysis pharmacokinetic evaluation system was successfully established.After given matrine gel,the concentration,AUC and half-life of the drug in skin were significantly higher than that in blood. Conclusion The established micro dialysis system combined with LC-MS could provide a new technology platform for the pharmacokinetic study on transdermal formulations.
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Key words:
- matrine /
- micro dialysis /
- transdermal delivery systems /
- pharmacokinetics
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[1] 张明发,沈雅琴.苦参碱抗炎和免疫抑制药理作用的研究进展[J].抗感染药学,2018,15(5):737-743. [2] 张明发,沈雅琴.苦参碱类生物碱抗病毒的临床药理作用研究进展[J].抗感染药学,2018,15(2):185-191. [3] 周峰,蔡鑫君,倪坚军,等.苦参碱类药物新型给药系统研究进展[J].浙江中西医结合杂志,2015,25(7):710-713. [4] 刘梅,刘雪英,程建峰.苦参碱的药理研究进展[J].中国中药杂志,2003,28(9):801-804. [5] ZHANG Y T,ZHANG K,GUO T,et al.Transdermal baicalin delivery using diethylene glycol monoethyl ether-mediated cubic phase gel[J].Int J Pharm,2015,479(1):219-226. [6] 王华富,许守涛,储卫华,等.微透析技术在药学研究中的应用[J].海峡药学,2018,30(10):30-33. [7] 杨盟,杨帝顺,顾永卫,等.基于皮肤、血液双位点同步微透析技术的雷公藤甲素纳米乳体内药动学研究[J].中国药学杂志,2018,53(11):894-899. [8] GU Y W,TANG X M,YANG M,et al.Transdermal drug delivery of triptolide-loaded nanostructured lipid carriers:Preparation,pharmacokinetic,and evaluation for rheumatoid arthritis[J].Int J Pharm,2019,554:235-244. [9] 刘继勇,韩盈,胡晋红,等.基于微乳凝胶新载体的丹皮酚经皮给药系统的构建及药代动力学研究[J].药学学报,2012,47(2):244-249. [10] YANG M,GU Y W,YANG D S,et al.Development of triptolide-nanoemulsion gels for percutaneous administration:physicochemical,transport,pharmacokinetic and pharmacodynamic characteristics[J].J Nanobiotechnology,2017,15(1):88. [11] 蒋阿梅,李娟,韩鑫玥,等.微透析技术研究蒙脱石镶嵌盐酸倍他洛尔微球混悬液在兔眼房水的药动学特征[J].广东药科大学学报,2019,35(3):327-332.
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