消肿止痛贴体外透皮吸收性能考察及其抗炎活性研究  

In vitro Transdermal Absorption Performance and Anti-inflammatory Activity of Detumescence and Analgesic Plaster

作　　者：李春霞 李玮婕 翟保嵘 王博 毛鹏 宋丽娟 LI Chunxia;LI Weijie;ZHAI Baorong;WANG Bo;MAO Peng;SONG Lijuan(State Key Laboratory for Quality Ensurance and Sustainable Use of Dao-di Herbs,Institute of Chinese Materia Medica,China Academy of Chinese Medical Sciences,Beijing 100700,China;Key Laboratory for Research and Evaluation of Traditional Chinese Medicine,National Medical Products Administration,Beijing 100700,China;Tianjin University of Traditional Chinese Medicine,Tianjin 301617,China;Shaanxi Momentum Qixuehe Pharmaceutical Co.,Ltd.,Shaanxi 712000,China)

机构地区：[1]中国中医科学院中药研究所,道地药材品质保障与资源持续利用全国重点实验室,北京100700 [2]国家药品监督管理局中医药研究与评价重点实验室,北京100700 [3]天津中医药大学,天津301617 [4]陕西摩美得气血和制药有限公司,咸阳712000

出　　处：《世界中医药》2024年第24期3785-3790,3801,共7页World Chinese Medicine

基　　金：国家重点研发计划项目(2023YFC2308200);中国中医科学院基本科研业务费优秀青年科技人才培养专项(ZZ16-YQ-026);中央级公益性科研院所基本科研业务费专项(ZXKT22056)。

摘　　要：目的:考察消肿止痛贴所含成分体外透皮渗透特性,并对其抗炎作用进行初探。方法:首先采用改良的Franz扩散池法,以离体小鼠皮肤为渗透屏障,通过体外透皮吸收实验,并进行方法学考察,计算体外透皮吸收动力学参数及其建立透皮曲线。取昆明小鼠36只,随机分为对照组(涂抹溶剂组)、模型组、消肿止痛贴低剂量0.085 mg/g、中剂量组0.171 mg/g和高剂量组0.342 mg/g,阳性组(复方醋酸地塞米松乳膏组0.1 mg/g),每组6只,进行二甲苯致小鼠耳肿胀实验,考察消肿止痛贴抗炎作用。结果:绿原酸、咖啡酸和1,5二咖啡酰奎宁酸可透过离体皮肤,24 h累计透过量分别为49.871、5.713、45.524μg/cm^(2),而滞留量较少分别为2.953、0.213和5.333μg/cm 2,表明这3个透皮成分较易到达病灶发挥药效。3个透皮成分的累积透过量-时间曲线符合一级动力学模型,表明消肿止痛贴具有缓释效果。耳肿胀实验显示消肿止痛贴低中高剂量的抑制率分别为45.78%,42.16%和39.76%,具有较好的抗炎活性。结论:消肿止痛贴体外透皮吸收良好并具有缓释功效,且有良好的抗炎活性,为消肿止痛贴的开发研究和临床推广提供参考。Objective:To investigate in vitro transdermal permeability characteristics of the components contained in Detumescence and Analgesic Plaster(DAP)and its anti-inflammatory effects.Methods:Firstly,in vitro transdermal absorption experiments were conducted by using the modified Franz diffusion cell method,with sampled mouse skin as the permeation barrier,and methodological studies were conducted to calculate the transdermal absorption kinetic parameters and establish a transdermal curve.A total of 36 Kunming mice were randomly divided into a control group(solvent application group),model group,low-dose DAP group(0.085 mg/g)medium-dose DAP group(0.171 mg/g),high-dose DAP group(0.342 mg/g),and positive group(compound dexamethasone acetate cream group of 0.1 mg/g),with six mice in each group.The experiment on ear swelling induced by xylene was carried out to investigate the anti-inflammatory effect of DAP.Results:Chlorogenic acid,caffeic acid,and 1,5-dicaffeoylquinic acid could penetrate through the skin in vitro,with a cumulative transmittance of 49.871,5.713,and 45.524μg/cm 2 after 24 hours,respectively,while the retention amount was relatively low(2.953,0.213,and 5.333μg/cm^(2)),indicating that these three transdermal components were more likely to reach the lesion and exerted the pharmacological effects.The cumulative transmittance-time curve of the three transdermal components accorded to a first-order kinetic model,indicating that DAP had a sustained-release effect.The ear swelling experiment showed that the inhibition rates of low-,medium-,and high-dose DAP were 45.78%,42.16%,and 39.76%,respectively,showing good anti-inflammatory activity.Conclusion:DAP has excellent in vitro transdermal absorption,exhibiting sustained-release effects and good anti-inflammatory activity,which may provide a reference for the development,research,and clinical promotion of DAP.

关 键 词：消肿止痛贴 Franz扩散池法 体外透皮吸收 沙蒿子 绿原酸 咖啡酸 1 5二咖啡酰奎宁酸 抗炎 

分 类 号：R284.2[医药卫生—中药学] R285.5[医药卫生—中医学]