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不锈钢微针经皮给药的研究 总被引:2,自引:0,他引:2
目的:将不锈钢微针阵列应用于经皮给药。考察离体大鼠皮肤经不同针形微针预处理相同时间、相同针形微针预处理不同时间后,模型药物鬼臼毒素经大鼠皮肤的透皮能力。方法:微针预处理大鼠皮肤后,用改进的Franz扩散池研究鬼臼毒素对皮肤的透皮速率。高效液相色谱法测定鬼臼毒素的含量。结果:皮肤经微针预处理后进行鬼臼毒素透皮,其透皮速率比未经微针处理时有明显提高。三角形微针、梯形微针、矛形微针对鬼臼毒素的促渗能力依次增强;三者所引起的鬼臼毒素在皮肤中的滞留量有显著差异。同种针形微针预处理皮肤时间越长,鬼臼毒素的透皮速率越大;但微针预处理时间对皮肤中的药物滞留量无显著影响。结论:微针用于药物经皮给药时,微针针形、微针的预处理时间对药物的经皮渗透具有重要影响。 相似文献
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对促进中药经皮吸收的药剂学方法,即促进剂促渗和剂型因素对中药经皮给药促渗作用的研究概况进行综述。初步分析与探讨中药经皮给药研究中存在的问题与发展方向,为深入研究中药经皮给药制剂提供参考依据。 相似文献
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目的:考察5种促渗剂在不同浓度下对苯妥英钠体外经皮渗透的影响。方法:用改良的Franz卧式扩散池,在离体透皮试验装置上,以0·9%的生理盐水作为接收液,用高效液相色谱法测定接收液中苯妥英钠的含量并计算经皮累积透过量和稳态渗透速率,观察苯妥英钠经不同促渗剂(3%、5%、10%油醇,3%、5%、8%薄荷醇,0·5%、1%、3%桉油,1%、3%、5%氮酮,3%、5%、8%N-甲基吡咯烷酮)处理过的小鼠腹部皮肤的渗透性。结果:5种促渗剂对苯妥英钠经皮吸收均有促渗作用,并且具有浓度依赖性。不同透皮促渗剂在最佳浓度时促渗作用的大小顺序为:5%N-甲基吡咯烷酮<5%油醇<5%薄荷醇<1%桉油<3%氮酮。结论:1%桉油和3%氮酮对苯妥英钠的促渗作用相似,但是氮酮使苯妥英钠的滞后时间延长,并且用量较大,因此桉油对苯妥英钠的促渗效果最好。 相似文献
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不同密度滚轮微针对曲安奈德的透皮促渗作用 总被引:1,自引:1,他引:0
目的探讨不同密度滚轮微针对曲安奈德经皮渗透的影响。方法采用改良Franz扩散池法考察体外经皮渗透特性,以离体裸鼠皮肤为屏障,对照组、192针、540针滚轮微针处理组分别于2、4、6、8、10、12h取接收液0.2ml,用HPLC法测定曲安奈德含量,计算累积渗透量,并测定皮肤内曲安奈德滞留量。采用测定血药浓度法考察在体吸收特性,在体给药2h后HPLC法测定各组皮肤及血浆中曲安奈德的含量。结果两种密度滚轮微针对曲安奈德均有不同程度的促透作用。离体透皮实验结果显示,192针微针处理组和540针微针处理组的累积渗透量Q分别是对照组的1.3倍和2.2倍,相应的皮肤内滞留量也分别是对照组的1.9倍和2.8倍。在体实验结果显示,192针微针和540针微针组的皮肤滞留量是对照组的2.1和2.3倍,同时也将血药浓度提高了1.3倍和1.4倍。结论结论两种不同密度滚轮微针均能有效提高曲安奈德的经皮渗透量,提高皮肤内药物含量,同时也导致血药浓度的增加,且不同密度微针的促透作用有所不同。 相似文献
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无痛微针透皮贴片对局部应用利多卡因的促渗作用 总被引:1,自引:0,他引:1
目的评价NS-TP-5B型无痛微针透皮贴片对局部应用利多卡因的透皮促渗效果及安全性.方法入选30名健康志愿者,采用随机、双盲、自身对照试验设计.每名志愿者左右臂随机分为试验组和对照组,分别采用无痛微针透皮贴片和模拟贴片处理,测定局部应用2%利多卡因注射液前后的疼痛评分.结果试验组20
min测定的疼痛评分与基线相比下降,且具有统计学意义(4.7±1.5 vs 6.1±1.5,P<0.001).对照组20
min结果与基线相比无显著差异.结论无痛微针透皮贴片对局部应用利多卡因具有一定的透皮促渗作用. 相似文献
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自溶性微针的制备及其对盐酸青藤碱凝胶透皮性能的影响 总被引:1,自引:0,他引:1
目的:优选出自溶性微针的处方工艺,并考察所制备的微针对盐酸青藤碱凝胶透皮性能的影响。方法采用浇注法制备自溶性微针,穿刺试验考察其机械性能,并采用改良Franz扩散池考察自溶性微针预处理皮肤,对盐酸青藤碱凝胶透皮性能的影响。结果采用浇注法制备自溶性微针,其最佳处方为:基质材料硫酸软骨素和聚乙烯吡咯烷酮(PVP)按照1∶1的比例混合,加入重量比60%的水;所制得的微针针形完整、机械强度良好,能够很好的穿刺铝箔和大鼠皮肤;体外透皮实验显示,自溶性微针使得盐酸青藤碱凝胶的累积渗透量增加了3.62倍。结论优选的自溶性微针的处方与制备工艺简单、可行,可显著提高盐酸青藤碱凝胶的透皮性能,为载药微针的进一步研究提供参考依据。 相似文献
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渗透促进剂对莫达芬尼透皮作用的影响 总被引:3,自引:0,他引:3
目的:研究10种渗透促进剂对莫达芬尼透皮吸收的影响。方法:采用改良的Franz扩散池,以40%PEG-400生理盐水溶液为接受介质,以大鼠离体腹部皮肤为透皮屏障,计算不同单元渗透促进剂作用下莫达芬尼累积渗透量Q、稳态流量Js及相关参数。结果:不同促渗剂对莫达芬尼有不同程度的促渗作用,氮酮、丁香油、月桂酸、薄荷醇对莫达芬尼促透作用比较显著,其增渗倍数分别是空白对照组的17.3850,16.3303,9.3297,8.7037倍。结论:此研究为莫达芬尼透皮吸收制剂处方的设计提供依据。 相似文献
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目的:阐述微针在经皮给药领域的研究。方法:简述并分析微针的特点、研究应用、存在的问题以及今后研究的重点。结果:作为一种新型的经皮给药技术,微针可能成为一种较为理想的经皮给药载体。结论:随着研究成果逐渐走入市场,微针将会带来良好的社会效益和经济效益。 相似文献
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Vaccination is undoubtedly the most effective health intervention for disease prevention and eradication. Nevertheless, currently there is still a need for improving immunization coverage worldwide. A promising strategy to achieve this goal nowadays relies on the use of delivery carriers capable of inducing an effective immune response and providing improved stability, safety and cost effectiveness. This article focuses on analyzing the critical aspects in the design of these carriers, and reviewing the state of the art of currently marketed formulations and those in advanced clinical development. These vaccine delivery carriers include emulsions, liposomes and polymeric particulate carriers. Finally, particular attention is given to the evolution in the design of polymeric nanocarriers, which have been receiving increasing attention and hold promise to generate novel platforms for needle-free administration and single-dose vaccination. 相似文献
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《European journal of pharmaceutics and biopharmaceutics》2014,86(2):284-291
The aim of this project was to study the effect of stainless steel solid microneedles and microneedle rollers on percutaneous penetration of verapamil hydrochloride and amlodipine besylate.Verapamil, 2-(3,4-dimethooxyphenyl)-5-[2-(3,4 dimethoxyphenyl)ethyl-methyl-amino]-2-propan-2-yl-pentanenitrile is a calcium channel blocker agent that regulates high blood pressure by decreasing myocardial contractilty, heart rate and impulse conduction. Amlodipine, (R, S)-2-[(2-aminoethoxy) methyl]-4-(2-chlorophenyl)-3-ethoxycarbonyl-5-methoxycarbonyl-6-methyl-1, 4-dihydropyridine, is a calcium channel blocker that is used for the management of hypertension and ischemic heart disease. Passive penetration of verapamil and amlodipine across the skin is low. In vitro studies were performed with microneedle-treated porcine ear skin using vertical static Franz diffusion cells (PermeGear, Hellertown, PA, USA). The receiver chamber contained 5 ml of PBS (pH7.4) and was constantly maintained at 37 °C temperature with a water circulation jacket. The diffusion area of the skin was 1.77 cm2. The donor compartment was loaded with 1 ml of the solution containing 2.5 mg/ml of amlodipine besylate. The donor chamber was covered with parafilm to avoid evaporation. Passive diffusion across untreated porcine skin served as control. Aliquots were taken every 2 h for 12 h and analyzed by liquid chromatography–mass spectrometry. Transcutaneous flux of verapamil increased significantly from 8.75 μg/cm2/h to 49.96 μg/cm2/h across microneedle-roller treated porcine skin. Percutaneous flux of amlodipine besylate following the use of stainless steel microneedles was 22.39 μg/cm2/h. Passive flux for the drug was 1.57 μg/cm2/h. This enhancement of amlodipine flux was statistically significant. Transdermal flux of amlodipine with microneedle roller was 1.05 μg/cm2/h in comparison with passive diffusion flux of 0.19 μg/cm2/h. The difference in flux values was also statistically significant. Stainless steel solid microneedles and microneedle rollers increased percutaneous penetration of verapamil hydrochloride and amlodipine besylate. It may be feasible to develop transdermal microneedle patches for these drugs. 相似文献
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C57B1/6 mice aged 2–3 and 13–14 months were treated i.p. with 3-methylcholanthrene. A single dose of 25 mg/kg reduced primary antibody production to the T-dependent antigen sheep red blood cells by 20% in mice aged 2–3 months and by 90% in 13–14-month-old animals. The same treatment did not reduce antibody production to the T-independent antigen pneumococcal polysaccharide type IlI in young mice, but reduced this response by 50% in 13–14-month-old animals. Blastogenesis to concanavalin A, phytohemagglutinin and alloantigens, that is mediated by T lymphocytes, was consistently reduced in young animals but only marginally affected, when at all, in 13–14-month-old mice. Blastogenesis to lipolpolysaccharide, mediated by B lymphocytes, was reduced in mice of both ages, though in older mice it was affected later than in younger animals. Addition of 3-methylcholanthrene in vitro increased T lymphocyte responses equally in mice of both ages and did not modify B lymphocyte proliferation. Results presented here show that older mice are not necessarily more susceptible to all types of immunosuppression induced by a xenobiotic like 3-methylcholanthrene and that the sensitivity of the different facets of the immune response can change with aging. 相似文献
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Hyoung-Chun Kim Wang-Kee Jhoo Myung-Sang Kwan Jau-Shyong Hong 《Archives of pharmacal research》1995,18(4):267-270
We examined the chronic effect of dextromethorphan (DM) on the cellular immune responses in mice. T cell stimulator, phytohemagglutinin
did not show significant effect on lymphocyte proliferation. Costimulator of T and B cell, pokeweed mitogen, and B cell stimulator,
lipopolysaccharide exhibited DM-induced decreased lymphocyte proliferation. Significantly suppressed natural killer (NK) cell
cytotoxicity was evidenced following 6 months DM exposure. These results suggest that chronic DM administration perturb B
cell functioning and NK cell cytotoxicity. In addition, prenatal DM exposure did not potentiate the immunomodulation in postnatal
effect induced by chronic DM. 相似文献
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Transdermal delivery of levosimendan 总被引:2,自引:0,他引:2
Riitta Valjakka-Koskela Jouni Hirvonen Jukka Mnkknen Juha Kiesvaara Saila Antila Lasse Lehtonen Arto Urtti 《European journal of pharmaceutical sciences》2000,11(4):14787-350
The aim of this study was to determine if transdermal penetration of levosimendan, a novel positive inotropic drug, could be enhanced and controlled by formulation modifications. Penetration of levosimendan across human epidermis in vitro was determined using abdominal excised skin and diffusion cells. Predicted steady-state plasma concentrations of levosimendan were estimated using permeabilities and pharmacokinetic parameters of levosimendan. For penetration enhancement we used different pH values, co-solvents, cyclodextrins, surfactants, penetration enhancers, liposomes, and iontophoresis. Sodium lauryl sulfate, ethanol, oleic acid, and soya phosphatidylcholine or their combinations clearly increased levosimendan permeation across the skin in vitro. Iontophoresis was also an efficient method to increase transdermal permeation of levosimendan. A hydrophilic co-solvent/penetration enhancer is needed to achieve better permeability of levosimendan across the skin. In conclusion, transdermal delivery of levosimendan can be significantly increased by formulation modification. Based on kinetic calculations, therapeutic plasma concentrations may be achievable transdermally. 相似文献