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不同促透剂对Ex-RAD凝胶体外透皮吸收的影响党学良;赵军;李晰;苏静妹;王庆伟【摘要】目的研究不同透皮吸收促透剂对Ex-RAD凝胶透皮作用的影响.方法采用改良的Franz扩散装置,以体外大鼠腹部皮肤为透皮屏障,0.9％氯化钠溶液为透皮体系接收液,采用反相高效液相色谱(RP-HPLC)法对Ex-RAD进行测定,考察不同透皮促进剂(薄荷醇、氮酮、冰片、麝香酮)对Ex-RAD凝胶的促渗效果,并优选出最佳促渗剂.结果氮酮对Ex-RAD具有较好透皮促进作用,在实验浓度范围内,随氮酮浓度增大,促透效应越强;麝香酮对Ex-RAD的促透作用较弱,随浓度的增加,促透作用基本无变化;薄荷醇在浓度为1％和3％时显示促透作用,但浓度增加到5％时,反而抑制Ex-RAD的皮肤渗透;1％冰片对Ex-RAD有一定的促透作用,随浓度增大,也表现出抑制渗透作用.结论 4种促透剂中,对于药物Ex-RAD凝胶增渗效果最好的促透剂是氮酮,而且5％氮酮效果最佳.【期刊名称】《医药导报》【年(卷),期】2016(035)010【总页数】5页(P1050-1054)【关键词】Ex-RAD凝胶;辐射保护剂;氮酮;薄荷醇;冰片;麝香酮;促透剂【作者】党学良;赵军;李晰;苏静妹;王庆伟【作者单位】第四军医大学唐都医院药剂科,西安710032;第四军医大学唐都医院药剂科,西安710032;第四军医大学唐都医院药剂科,西安710032;商洛学院生物制药工程系,商洛726000;第四军医大学唐都医院药剂科,西安710032【正文语种】中文【中图分类】R979.6;R969.1放射性皮肤损伤是临床放射治疗(放疗)过程中最常见的不良反应。
临床主要表现为：皮肤滤泡样黯色红斑，触痛性或鲜色红斑，片状湿性脱皮，皮肤皱褶以外部位的融合的湿性脱皮，凹陷性水肿，甚至发生溃疡，出血坏死[1-2]。
这不仅会影响放疗计划的顺利实施，还严重降低患者的生活质量，给患者带来极大痛苦。
透皮吸收促进剂对大黄中蒽醌类有效成分透皮吸收的影响【摘要】目的探讨不同浓度的氮酮、丙三醇、油酸对大黄中蒽醌类有效成分透皮吸收的影响。
方法以离体小鼠皮为透皮屏障，采用改良franz扩散池装置，采用高效液相色谱法同时测定接收池中蒽醌类物质大黄素，大黄酚，大黄素甲醚，大黄酸的含量，计算累积透过量。
结果氮酮、丙三醇和油酸对大黄中蒽醌类物质均有促透作用，其促透作用强弱顺序为：2%氮酮>1%氮酮>4%氮酮>6%氮酮；6%丙三醇>4%丙三醇>2%丙三醇>1%丙三醇；2%油酸>4%油酸>6%油酸>1%油酸。
结论氮酮、丙三醇和油酸对大黄中蒽醌类物质大黄素、大黄酚、大黄甲醚、大黄酸的促透作用具有一定的量效关系。
【关键词】透皮吸收；促进剂；大黄；蒽醌类；有效成分abstract：objectiveto evaluate the effect of azone, propanetriol and oleic acid under different concentrations on transdermal absorption of effective components in anthraquinones from rhubard. methodsa piece of excised abdominal hairless mouse skin was set in a franz-type diffusion cell.penetrations of emodin, rhein, physcion and chrysophanol were detected by hplc and cumulative permeation(q) calculated.resultslaurocapram, propanetriol and oleic acid were found permeation enhancing effect to anthraquinones (emodin, rhein, physcion and chrysophanol) in rhubard. the permeation enhancing effect was 2% oleic acid >4% oleic acid >6%oleic acid >1% oleic acid; 2%laurocapram >1% laurocapram >4% laurocapram >6% laurocapram; 6% propanetriol >4% propanetriol >2% propanetriol >1% propanetriol. conclusionlaurocapram, propanetriol and oleic acid have permeation enhancing effect to anthraquinones (emodin, rhein, physcion and chrysophanol) in rhubard with dose-effect relationship.key words：transdermal absorption;potentiation;rhubard;anthraquinones;effective components大黄具有较强的抗炎、收敛止血等成效，被广泛用于治疗皮肤病、湿疹、丹毒等疾病以及化装品中；临床上多用大黄粉或与其它药物配伍，以醋、植物油等调敷外用。
几种促透剂联合使用对双氯芬酸钠体外经裸小鼠皮肤吸收的影响作者：沈非沉王晖郭源源陈丽张瑞涛【摘要】目的：研究几种促透剂联合使用对药物体外经皮渗透的影响。
方法：在离体透皮吸收装置上，采用正交试验的设计方法研究不同浓度的氮酮、薄荷醇、冰片联用对双氯芬酸钠在离体裸小鼠背部皮肤上的透皮行为，以累积透过量、渗透速率和滞后时间为药效指标，运用Topsis法评价促透效果。
结果：对双氯芬钠的促透作用，氮酮2%、薄荷醇2%、冰片1%联用促透效果最好，其中以氮酮的促透作用最为明显。
结论：三种促透剂的联合使用能有效促进双氯芬酸钠的透皮吸收，Topsis法可客观、公正地评价促透剂的促透效果并选出最优方案。
【关键词】氮酮薄荷醇冰片双氯芬酸钠透皮吸收Topsis法Effect of Using Several Transdermal Enhancers Together on Absorption of Diclofenac Sodium through Skin on Nude Mice in VitroAbstract Objective: To study the effect of using sevearal transdermal enhancers together on absorption of drugs through skin in vitro. Method:We set up an orthogonal experiment, use diclofenac sodium as drug model, detect the pemeate velocity(P), lag time(Tlag), and transit dose accumulated in 24 hours(Q24) as index of drug action of azone, menthol and camphol using together on skin of back of unde rat on the equipment of percutaneous absorption in vitro, evaluate the contribution of transdermal enhancers by Topsis. Result:Together use of azone 2%,menthol 2% and camphol 1% has the best transdermal enhance effect of the absorption of diclofenac sodium, of which azone has the strongest effect on percutaneous absorption of diclofenac sodium. Conclusion:Using three transdermal enhancers together promotes the percutaneous absorption of diclofenac sodium in vitro effectively. Topsis can evaluate the effect of transdermal enhancers and find the best match objectively.Key words azone; menthol; camphol; diclofenac sodium; percutaneous absorption; Topsis氮酮是目前应用最广泛的透皮吸收促进剂之一，薄荷醇和冰片是近年研究较多的萜类透皮吸收促进剂的代表［1］，薄荷醇和氯酮对双氯芬酸钠的促透作用已有研究［2，3］，但三者联用的促透效果未见文献具体报道。
促渗剂对青蒿琥酯贴剂体外经皮吸收的影响作者：邱琳,王乃婕,杜丰,梁秉文,叶祖光【摘要】目的考察几种促渗剂对青蒿琥酯体外经皮吸收的影响,为青蒿琥酯贴剂的开发提供参考。
方法采用TK-6A型透皮扩散仪,以SD大鼠腹部皮肤为透皮屏障,测定含有不同浓度促渗剂的青蒿琥酯贴剂的累计透过量和经皮渗透速率。
结果各促渗剂对青蒿琥酯促渗作用大小依次为：油酸(OA)＞N-甲基吡咯烷酮(NMP)＞丙二醇(PG)＞氮酮(Azone)＞己二酸二异丙酯(IPA)。
NMP和OA的促渗作用呈浓度依赖性,IPA和PG的促渗效果不随浓度的升高而增强,处方中高浓度的IPA 和PG反而会抑制青蒿琥酯的透皮吸收。
结论 10%OA对青蒿琥酯的促渗作用最显著。
【关键词】青蒿琥酯；贴剂；经皮吸收；促渗剂；大鼠Abstract：Objective To investigate the effect of penetration enhancers on the percutaneous absorption of artesunate, and provide a reference for the development of artesunate transdermal delivery systems. Methods Penetration enhancers (in different concentrations) were incorporated into a 25% w/w artesunate matrix patch formulation. Modified Franz diffusion chambers and SD rat abdominal skin were used for invitro skin permeation studies, the transdermal flux and permeation rate of artesunate in vitro were determined by HPLC. Result The enhancing effectiveness of the enhancers decreased in the order：OA＞NMP＞PG＞Azone＞IPA. Skin permeation was significantly enhanced by increasing the loading concentration of OA or NMP, larger IPA amount (8%) or PG amount (20%) could inhibit the permeation of artesunate. Conclusion Oleic acid was found to be the most efficient enhancer for artesunate, 10% is the most effective concentration.Key words：artesunate；transdermal delivery system；percutaneous absorption；penetration enhancers；rat青蒿琥酯(Artesunate)为常用的抗疟药,在临床上对抢救和治疗脑型疟和恶性疟等疗效显著,目前研究还发现其具有平喘、治疗弓形虫病、抗肿瘤、免疫调节等作用。
