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1.
经皮给药制剂(Transdermal Drug Delivery Systems,TDDS),是指经皮肤给药而发挥全身治疗作用的控释制剂。作为第三代药物制剂研究的新型给药系统,其优点有:可以绕过肝脏的首过效应及胃肠道的破坏,提供可预定的和较长的作用时间,维持稳定持久的血药浓度,降低药物毒性和副作用,提  相似文献   

2.
目的 比较穴位与非穴位皮肤的电阻、角质层厚度、生物化学组成,并研究白芥子涂方经穴位和非穴位给药芥子碱的渗透特性,探讨皮肤生物物理学性质对芥子碱经皮给药的影响,为白芥子涂方临床穴位贴敷预防和治疗哮喘提供实验支持.方法 以自制装置测定穴位与非穴位皮肤电阻;皮肤组织切片经HE染色后,在光学显微镜下测量皮肤和角质层厚度;以激光显微拉曼光谱法比较皮肤的生物化学组成;以芥子碱为评价指标,采用HPLC法定量,用Franz扩散池法研究白芥子涂方离体经穴位和非穴位皮肤的渗透特性;在体渗透实验采用胶带粘贴法剥离角质层,比较穴位与非穴位皮肤各层中药物的分布.结果 穴位皮肤电阻在给药前后各时间点均显著低于非穴位皮肤(P<0.05);穴位皮肤角质层厚度显著低于非穴位(P<0.05);激光显微拉曼光谱显示穴位与非穴位皮肤的生物化学组成基本一致.给药24 h后,离体实验中芥子碱经穴位皮肤的单位面积累积透过量是经非穴位皮肤的6.8倍(P<0.05);穴位皮肤稳态透皮速率是非穴位的6.1倍;离体透皮实验和在体渗透实验中,24 h皮肤中药物滞留量均为穴位>非穴位(P<0.05),各时间点角质层中药物滞留量均为穴位>非穴位(P<0.05).结论 芥子碱经穴位皮肤的透过量和皮肤滞留量均显著高于经非穴位皮肤.穴位皮肤的低电阻、角质层薄有利于药物的经皮吸收和贮存,验证了涂方临床使用以穴位经皮给药的科学性.  相似文献   

3.
徐月红  叶卉  官素桃  郭秀彩  刘霞  吴传斌 《中成药》2011,33(12):2068-2072
目的研究白芥子涂方(白芥子、延胡索、甘遂、细辛等)凝胶膏剂的体外释放和透皮特性,为开发白芥子涂方贴敷预防和治疗哮喘的药物新型给药系统提供实验支持。方法分别以透析膜和大鼠皮肤为屏障,以扩散池法进行体外释放和透皮实验,以方中君药白芥子的有效成分芥子碱硫氰酸盐为指标,利用反相高效液相色谱分析,测定白芥子涂方凝胶膏剂释放介质和透皮接收液中的药物浓度,分别以累积释放量和透皮量对时间做图,计算释放和透皮速率。结果芥子碱硫氰酸盐自凝胶膏剂中体外释放的方程为QR=45.65t+3.193,r2=0.994 6,释放速率为45.65μg/(cm2.h);其透皮特性方程为QT=0.502 1t+0.178 0,r2=0.997 1;透皮速率0.502 1μg/(cm2.h)。结论芥子碱硫氰酸盐的释放速率远大于透皮速率,释放速率可保证其稳定透皮的动力,其透皮过程不受其释放的限制,限速步骤主要是由于皮肤的屏障作用导致,寻找合适的透皮促进剂对白芥子涂方凝胶膏剂发挥疗效具有重要意义。  相似文献   

4.
微透析联用反相高效液相色谱研究白芥子涂方皮肤药动学   总被引:4,自引:4,他引:4  
目的研究白芥子涂方皮肤给药后皮肤局部药动学特征,为白芥子涂方贴敷预防和治疗哮喘的药物作用机制研究提供参考。方法大鼠在体贴敷白芥子涂方后,以方中君药白芥子的有效成分芥子碱硫氰酸盐为指标,利用微透析采样技术,结合反相高效液相色谱分析,测定白芥子涂方贴敷给药后透析液的药物质量浓度,通过相对损失率的校正,计算皮肤药物质量浓度,并利用Kinetica 4.4软件对皮肤药物质量浓度和时间进行非房室模型拟合,计算相关统计矩参数。以相对累积吸收量对时间做图,计算稳态的吸收速率。结果白芥子涂方贴敷给药后芥子碱硫氰酸盐达峰时间为1.5 h,平均滞留时间(MRT)约为22 h,半衰期(t1/2)约15 h,稳态吸收速率为13.65μg/h。结论微透析取样技术结合反相高效液相色谱分析可研究白芥子涂方给药后的皮肤药动学,给药后的皮肤药动学行为与其临床作用特点相一致,可为阐明白芥子涂方贴敷预防和治疗哮喘的药物作用机制提供研究手段。  相似文献   

5.
目的:建立复方白芥子巴布剂的质量标准。方法:采用薄层色谱法鉴别处方中的芥子、甘遂;采用高效液相色谱法测定延胡索乙素的含量。结果:在选定的薄层色谱条件下,可检出芥子、甘遂的特征斑点;延胡索乙素在16.59~165.9μg/mL的浓度范围内与峰面积呈良好线性关系(r=0.9999),平均回收率为98.08%,RSD为2.2%(n=6)。结论:所建立的方法可用于控制该制剂的质量。  相似文献   

6.
目的:观察穴位贴药治疗哮喘发作状态及远期疗效.方法:用纯中药白芥子散配六神丸和生姜汁贴敷于定喘穴(双)、肺俞穴(双)、膏肓穴(双)、膻中穴,在每年三伏天和三九天外贴.结果:临床50例哮喘患者治疗1个疗程,治愈率达98.90%,较纯西药治疗效果明显提高.结论:说明该药具有明显的止咳平喘、固本益气功效,达到了冬病夏治的目的.  相似文献   

7.
目的:探讨“冬病夏治”全方配伍和无白芥子配伍延胡索乙素在模型家兔“肺俞”穴皮下药代动力学特征及药代动力学-药效动力学(PK-PD)模型的相关性。方法:支气管哮喘模型家兔随机分成延胡索单方组、缺白芥子组、全方组,微透析技术收集14 h穴位皮下透析液,液相色谱-质谱法(Liquid Chromatography Mass Spectrometry, LCMS)法检测方中君药延胡索主要成分延胡索乙素浓度,获得药代动力学参数;酶联免疫吸附试验(ELISA)法检测对应时间点模型动物血清中IgE水平,获得药效学参数;对药动学、药效学参数进行PK-PD模型拟合。结果:白芥子配伍后的药峰浓度(Cmax)、药时曲线下面积(AUC0-t)、平均滞留时间(MRT0-t)均显著增加(P<0.01,P<0.01,P<0.05),达峰时间(Tmax)提前(P<0.01);“浓度-时间-效应”三维曲线表明,方中有白芥子配伍时,药效出现更快、消退更慢,起效时间晚于峰浓度,具有一定滞后性。结论:动力学参数、P...  相似文献   

8.
目的:考察氮酮、丙二醇及二者混合物对白芥子散贴剂中延胡索乙素透过量的影响,为该复方的凝胶膏剂研制提供参考。方法:采用改良Franz扩散池,以离体雄性大白兔皮肤为模型,通过HPLC测定延胡索乙素含量,流动相甲醇-0.1%磷酸溶液(三乙胺调p H 6.0)(60∶40),检测波长280 nm,拟合延胡索乙素透皮吸收的累积透过量,考察不同促渗剂对白芥子散贴剂体外透皮效果的影响。结果:以2%氮酮制备的白芥子散贴剂累积透过量最高;促渗剂合用时以2%氮酮+5%丙二醇促渗作用较好,但其合用效果弱于2%氮酮单用的效果。结论:氮酮能显著提高白芥子散贴剂的透皮吸收效果。  相似文献   

9.
支气管哮喘是一种常见的慢性呼吸道疾病,往往反复发作,缠绵难愈,给患者、家庭和社会带来沉重的负担。自清代张璐·《张氏医通》创制白芥子涂法治疗哮病以来,穴位贴敷治疗哮喘沿用至今。其方由白芥子、延胡索、甘遂、细辛、生姜汁、麝香组成,《本草经疏》:"白芥子味极辛,气温能搜剔内外痰结及胸膈寒痰,令涎壅塞者殊效。"穴位贴敷药物多选择辛香走窜、药性威猛的药物,关鹏等通过查阅文献,分析中药穴位贴敷治疗哮喘的临床文献101篇,统计涉及中药65味,其中白芥子使用频次为100次,使用率最高。近现代医家多在张氏白芥子涂法基础上对穴位贴敷的药物、剂型、方法等加以改进,并取得了确切疗效。现将白芥子穴位贴敷治疗哮喘的研究概况综述如下。  相似文献   

10.
目的:比较“冬病夏治”方中有、无白芥子配伍以及经穴、非经穴给药,对延胡索乙素皮肤渗透性的影响。方法:弗氏完全佐剂法制备类风湿性关节炎家兔模型,随机将48只模型家兔分为空白组(不加白芥子)、非经穴白芥子低剂量组、非经穴白芥子中剂量组、非经穴白芥子高剂量组、非经穴组(处方量)、“足三里”白芥子低剂量组、“足三里”白芥子中剂量组和“足三里”白芥子高剂量组,每组6只,取模型家兔“足三里”穴位处皮肤,非穴位处皮肤,Franz扩散法进行体外释放实验,UPLC法测定延胡索乙素的含量,计算累积透过量,绘制12 h内释放曲线图,比较累积渗透率。结果:空白组的累积透过量、稳态渗透速率和累积渗透率显著低于白芥子配伍的高、中、低剂量组(P <0.01)。在白芥子促进下,经穴给药的累积透过量、稳态渗透速率和累积渗透率均显著高于非经穴给药(P <0.01),白芥子高剂量组促渗效果倍数高于中、低剂量组。结论:白芥子在“冬病夏治”方中起到“药物-透皮促进剂”的“双重”作用。透皮促进体现在两个方面,一是穴位用药优于非穴位用药;二是随白芥子用量增加而增强。因此,该方更优的透皮给药方案应当是方中重用白芥子,于穴...  相似文献   

11.
目的:探讨藏药螃蟹甲中环烯醚萜类成分糙苏素(phlomiol)的抗肿瘤作用.方法:采用MTT法检测糙苏素对体外培养的2种人肿瘤细胞增殖的抑制作用;体内试验采用小鼠实体瘤S180、肝癌H22细胞株接种小鼠,连续给药14 d,计算抑瘤率.采用MTT比色法检测糙苏素对S180荷瘤小鼠NK细胞杀伤活性的影响和对S180荷瘤小鼠T淋巴细胞增殖反应的影响.结果:糙苏素在50~150 mg·L-1对2种肿瘤细胞增殖均有抑制作用,且呈剂量依赖关系(r=0.989,P<0.05);体内试验结果显示小鼠分别灌胃给予2.5,5,10 mg·kg-13个剂量的糙苏素,对接种的实体瘤S180、肝癌H22细胞株的抑瘤率分别为28.5%~65.0%.35.0%~74.5%.同时,糙苏素可显著提高S180荷瘤小鼠淋巴细胞增殖活性(P<0.05),显著增加S180荷瘤小鼠NK细胞的杀伤能力(P<0.05).结论:糙苏素对体外培养的人肿瘤细胞和接种的小鼠肿瘤具有明显抑制作用,能够增强淋巴细胞增殖功能和NK细胞的杀伤能力,具有抗肿瘤和免疫调节功能.  相似文献   

12.
目的:研究柳氮磺胺吡啶栓剂体内外释药规律。方法:于不同时间点采样,测定柳氮磺胺吡啶栓剂溶出度,分析累积释药量;新西兰兔直肠给柳氮磺胺吡啶栓,测定不同时间点血浆中柳氮磺吡啶(SASP)的浓度,应用3P97软件进行药动学分析。结果:SASP栓剂体外释放率较低,家兔体内吸收入血较快,Tpeak0.606 272 h,Cmax2.404 431 mg.L-1。结论:柳氮磺胺吡啶栓剂体内外释药具有较好的相关性。  相似文献   

13.
射干提取物体内体外抑菌作用的研究   总被引:2,自引:6,他引:2  
目的:研究射干提取物的体内外抑菌作用。方法:通过测定抑菌圈直径考察射干提取物对不同菌株的敏感性;采用2倍稀释法检测射干提取物的最小抑菌浓度(MIC);通过ip金黄色葡萄球菌观察射干提取物低、中、高(0.46,0.92.1.84g.kg-1)3个剂量ig给药7 d对小鼠的致死保护率。结果:肺炎链球菌、铜绿假单胞菌对射干提取物有较强的敏感性,金黄色葡萄球菌、大肠埃希菌、无乳链球菌、化脓链球菌、痢疾志贺菌对射干提取物中度敏感;射干提取物对金黄色葡萄球菌、肺炎链球菌、大肠埃希菌、铜绿假单胞菌、无乳链球菌、化脓链球菌、痢疾志贺菌的最小抑菌浓度(MIC/g.mL-1)分别为0.062 5,0.015 6,0.250 0,0.031 2,0.015 6,0.015 6,0.062 5;射干提取物低、中、高3个剂量组均显著降低金黄色葡萄球菌酵母悬液引起的小鼠死亡率,死亡率分别为45%,35%,30%,与模型对照组死亡率100%比较差异有统计学意义(P<0.05或P<0.01)。结论:射干提取物体内体外对所试菌株均有抑菌作用。  相似文献   

14.
采用改良Franz扩散池法进行实验,以延胡索乙素为指标,HPLC测定样品的含量,考察止痛凝胶膏剂的体外释放和经皮渗透行为。经统计分析,24 h内延胡索乙素累积释药率和释药速率为81.9%,2.26 μg·cm-2·h-1;24 h累积经皮渗透率和速率分别为12.53%,0.27 μg·cm-2·h-1,48 h内累积经皮渗透率和速率为20.31%,0.22 μg·cm-2·h-1,表明止痛凝胶膏剂具有较好的释放和透皮性能,透皮行为符合零级动力学过程。  相似文献   

15.

Aims of study

The purpose of this study was to investigate the protective effects of KIOM-79, a combination of four plant extracts, on retinal pericytes loss, which is one of the histopathological hallmarks of early diabetic retinopathy.

Materials and methods

To investigate the protective effect of KIOM-79 on pericyte apoptosis, we have used methylglyoxal (MGO)-treated primary rat retinal pericytes and retinal vessels from intravitreally MGO-injected eyes. Primary rat retinal pericytes were exposed to 400 μM MGO for 6 h with or without KIOM-79. 400 μM final intravitreal concentration of MGO with or without KIOM-79 (10 μg/ml final intravitreal concentration) were intravitreally injected into the right eyes of rats for 2 days. The left eyes were received 3 μl of saline only. Retinal vessels were then isolated. We examined apoptosis, ROS productions, 8-OHdG in cultured rat retinal pericytes and retinal vessels.

Results

In CCK-8 assay and TUNEL staining, MGO-induced apoptosis of rat retinal pericytes was markedly inhibited by KIOM-79. KIOM-79 significantly reduced intracellular ROS productions and oxidative damage induced by MGO. In addition, the intravitreal injection of KIOM-79 prevented apoptosis of retinal microvascular cells, MGO accumulation and oxidative DNA damage in intravitreally MGO-injected eye.

Conclusion

These observations suggest that KIOM-79 acts through an antioxidant mechanism to protect against oxidative stress-induced apoptosis in retinal pericytes.  相似文献   

16.

Ethnopharmacological relevance

Swertia punicea Hemsl. (Gentianaceae) is more commonly known as “Ganyan-cao” and used mainly as a traditional Chinese folk medicine for the treatment of acute bilious hepatitis, cholecystitis, fever, intoxification and jaundice.

Materials and methods

The active hepatoprotective constituents of Swertia punicea were purified using various column chromatography techniques. The structures of two isolated compounds were determined on the basis of spectroscopic data interpretation such as NMR analysis. The hepatoprotective activities of isolated compounds were evaluated by using hepatotoxicity in vitro and dimethylnitrosamine-induced rat hepatic fibrosis in vivo, respectively.

Results

Two xanthones, 1, 7-dihydroxy-3, 4, 8-trimethoxyxanthone (1) and bellidifolin (2) were isolated from the stems of Swertia punicea. The compounds 1 and 2 exhibited notable hepatoprotective activities against carbon tetrachloride (CCl4) -induced HepG2 cell damage, and effectively alleviated the levels of aspartate transaminase (AST), lactate dehydrogenase (LDH), superoxide dismutase (SOD) and malonic dialdehyde (MDA) induced by CCl4 in a concentration-dependent manner. Co-treatment with compound 2 significantly increased the cell viability compared with N-acetyl-p-aminophenol (APAP) treatment. Compound 2 also alleviated APAP-induced hepatotoxicity by increasing glutathione (GSH) content and decreasing hydroxyl free radical (·OH) levels and reactive oxygen specises (ROS) production. In addition, the protective effect of compound 1 significantly alleviated DMN-induced liver inflammation and fibrosis. Oral administration of compound 1 recovered the reduction of albumin (ALB) and reversed the elevation of serum alanine transaminase (ALT), AST and total bilirubin (TBIL) in dimethylnitrosamine (DMN)-induced fibrotic rats. Severe oxidative stress induced in fibrotic rats was evidenced by a 1.5-fold elevation in MDA and a fall in the SOD activity, and treatment with compound 1 protected against these adverse effects. Recovery of rat liver tissue against DMN-induced hepatocellular necrosis, inflammatory changes and hepatic fibrosis by compound 1 is also confirmed by H&E and Masson stained histopathological evaluation of liver tissue.

Conclusion

Two xanthones from Swertia punicea exhibited hepatoprotective activities in vitro (compounds 1 and 2) and in vivo (compound 1), respectively.  相似文献   

17.
冬虫夏草提取物调血脂与抗氧化活性   总被引:6,自引:5,他引:1  
目的:研究冬虫夏草提取物(YCC)在调血脂与抗氧化方面的活性。方法:建立高脂饮食诱导的高脂血症金黄地鼠模型,连续ig给予200 mg·kg-1的YCC 4周后,比色法测定动物血清中总胆固醇(TC)、甘油三酯(TG)、低密度脂蛋白胆固醇(LDL-c)与高密度脂蛋白胆固醇(HDL-c)的含量,观察YCC调节脂质代谢的活性;基于体外分子水平反应体系,运用比色、荧光、化学发光的方法评价不同浓度YCC对DPPH、超氧阴离子、羟自由基、脂质过氧自由基、过氧化氢及过氧亚硝基的清除活性;建立铜离子诱导人低密度脂蛋白(LDL)氧化修饰模型,并观察YCC对LDL氧化过程的影响。结果:与模型组比较,YCC在200 mg·kg-1剂量下明显降低了高脂饮食饲养的地鼠血清中TC,TG,LDL-c含量,同时升高HDL-c/LDL-c(P<0.05);YCC对1,1-二苯基-2-苦肼基自由基(DPPH)和过氧化氢的半数抑制浓度(IC50)分别为(125.6±3.4)mg·L-1,(758.9±11.2)mg·L-1;YCC对脂质过氧自由基、过氧亚硝基、羟自由基的最大清除率分别为(86.5±14.5)%,(64.4±3.3)%,(44.1±6.0)%;YCC在50,100 mg·L-1浓度下可明显延长铜离子诱导LDL氧化过程的滞留时相。结论:YCC在体内显示出调血脂、体外显示出抗氧化活性。  相似文献   

18.
雄黄致体内外染色体畸变   总被引:2,自引:1,他引:2  
目的:用仓鼠体内染色体畸变试验和中国仓鼠肺细胞CHL细胞染色体畸变试验评价雄黄的遗传毒性.方法:体内染色体畸变试验用毛足属仓鼠连续ig5 d给予33.25,66.5,133 mg·kg-1剂量雄黄悬浊液,处死前2 h ip秋水仙素.处死后取骨髓细胞制备染色体.油镜下观察每只动物骨髓细胞的有丝分裂指数和100个中期分裂相细胞的畸变类型.CHL细胞染色体畸变试验用雄黄浸出液终质量浓度为0.15,0.3,0.6g.L-1作用于CHL细胞,培养24 h或48 h,终止培养前4h加入秋水仙素.收获细胞,制备染色体,油镜下观察CHL细胞有丝分裂指数和200个中期分裂相细胞的畸变类型.结果:①雄黄265.0 mg· kg -1组和雄黄530.0 mg·kg-1组ig给药和雄黄浸出液(1.2,2.4g·L-1)作用于CHL细胞显示有明显的抑制有丝分裂作用.②与阴性对照组比较,雄黄ig给药仓鼠体内染色体畸变率和雄黄体外给药CHL细胞染色体畸变率均显著升高,差异有极显著意义,且有明显的量效关系.但体内试验的畸变率低于体外试验.③雄黄给药后CHL细胞染色体畸变试验中可见较多的染色体断片,而仓鼠体内染色体畸变试验中未发现,这可能与体内外药物作用的方式不同.结论:①雄黄能致体内外细胞染色体畸变,具有遗传毒性.②仓鼠体内染色体畸变试验可作为中药新药遗传毒性评价试验组合的方法之一.  相似文献   

19.

Ethnopharmacological relevance

Achyrocline alata is a locally marketed (Mato Grosso do Sul/ Brazil) herb used in folk medicine as an anti-inflammatory and a sedative. Evaluate the anti-inflammatory properties of Achyrocline alata in both in vivo and in vitro models.

Materials and methods

A hydroethanolic extract from inflorescences of Achyrocline alata (HEAa) was characterized by HPLC-DAD and compared to standards (chlorogenic acid; isoquercetrin; quercetin; 4,2?,4?-trihydroxy-6?-methoxychalcone; gnaphalin; 3-O-methyl-quercetin; 3,5-dicaffeoyl-quinic acid and 4,5-dicaffeoyl-quinic acid). The in vivo anti-inflammatory properties of the HEAa (4, 20 and 100 mg/kg, per os) were evaluated using the following animal models: carrageenan-induced paw edema in rats, carrageenan-induced vascular permeability and peritonitis in mice and an acetic acid-induced writhing model to test antihyperalgesic activity in mice. In vitro assays were performed to study the effects of the HEAa (0.16, 0.8 and 4 mg/ml) on the cell viability, cell spreading and production of NO and H2O2 in stimulated macrophages.

Results

The A. alata extract inhibited the development of edema and vascular permeability, reduced polymorphonuclear cell recruitment in the acute peritonitis assay and decreased the amount of writhing induced by acetic acid. The HEAa did not increase NO/H2O2 production, while it did inhibit production when the macrophages were stimulated by LPS or PMA at all tested concentrations. In the presence of HEAa, macrophage spreading did not increase even after stimulation with LPS. Additionally, the HEAa was nontoxic to macrophages at all tested concentrations.

Conclusions

The HEAa displayed anti-inflammatory and antihyperalgesic effects, which supports the use of this plant in folk medicine. These effects might be due to the flavonoids and phenylpropanoids derivatives present in the HEAa.  相似文献   

20.

Ethnopharmacological relevance

Acer tegmentosum, which contains salidroside and tyrosol, has been used for the treatment of hepatic disorders in eastern Asia. However, little is known about its safety.

Aim of the study

To determine the safety of Acer tegmentosum, we evaluated its acute oral toxicity and genotoxicity profiles.

Materials and methods

Salidroside and tyrosol present in Acer tegmentosum were quantified using high-performance liquid chromatography. Acute oral toxicity testing of Acer tegmentosum was performed in rats. Genotoxicity of Acer tegmentosum was assessed by bacterial reverse mutation, chromosomal aberration, and bone marrow micronucleus tests. All the tests were conducted in accordance with the good laboratory practices.

Results

The amounts of salidroside and tyrosol in Acer tegmentosum were found to be 85.01±1.21 mg/g and 3.12±0.04 mg/g, respectively. In the bacterial reverse mutation test, Acer tegmentosum increased the number of revertant Salmonella typhimurium TA98 colonies, regardless of metabolic activation by S9 mixture. In contrast, Acer tegmentosum application did not significantly increase the number of chromosomal aberrations in Chinese hamster ovary (CHO)-K1 cells and micronucleated polychromatic erythrocytes in mice. In the acute oral toxicity test, the median lethal dose (LD50) of Acer tegmentosum was found to be >2000 mg/kg in rats.

Conclusion

Take together, Acer tegmentosum exhibits mutagenicity, which was evident from the bacterial reverse mutation test. Further studies are needed to identify the components responsible for such an effect and the underlying mechanisms.  相似文献   

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