共查询到18条相似文献,搜索用时 62 毫秒
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透皮促进剂在透皮吸收制剂中的应用 总被引:4,自引:0,他引:4
透皮给药是一个新兴的领域 ,具有许多优点而受到药学工作者的重视。其理论基础为给药后药物能迅速穿透皮肤 ,被吸收进入血液循环而产生疗效。因此 ,研究经皮给药制剂首先必须解决药物对皮肤的穿透性和透皮速率。安全、有效、作用强的透皮促进剂的开发应用 ,已成为药学工作者的研究重点。1 新型促渗剂①目前使用最多的是氮酮 (Azone) ,对亲水性或疏水性药物都能显著增强透皮速率。Michniak等[1] 合成了 2 吡咯烷酮 1 醋酸及其各种酯类、N 环庚基酰胺类同系物和Azone的 11个同系物 ,以考察其对氢化可的松的促渗作用。结… 相似文献
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促进剂对酮洛芬巴布剂体外透皮性的影响探讨 总被引:2,自引:0,他引:2
目的:通过几种常用促进剂对酮洛芬巴布剂体外促渗作用研究,筛选出适合用于酮洛芬巴布剂的透皮促进剂。方法:分别制备单独含2%或4%的桉叶油、油酸、薄荷脑、聚乙二醇400、月桂氮芯卓酮、聚山梨醇酯-80的酮洛芬巴布剂贴片,以及4%的桉叶油分别与2%的油酸、薄荷脑、聚乙二醇400合用的酮洛芬巴布剂贴片,采用改良Franz透皮扩散池,以离体小鼠背部皮肤为透皮屏障,贴敷12h,以渗透速率及12h累积渗透量为指标,探讨促进剂对酮洛芬体外透皮性的影响。结果:与空白组对照,2%聚山梨醇酯-80、2%月桂氮卓芯酮单独使用不能明显提高酮洛芬的渗透速率(P>0.05),4%聚山梨醇酯-80、4%月桂氮卓芯酮和其他的促进剂都能明显的提高酮洛芬的经皮渗透(P<0.01),对酮洛芬透皮速率提高大小顺序为油酸≥桉叶油>薄荷脑>聚乙二醇400>月桂氮卓芯酮>聚山梨醇酯-80。结论:油酸、桉叶油、薄荷脑、聚乙二醇400均可作为酮洛芬巴布剂透皮促进剂。 相似文献
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本文介绍了透皮释放给药系统的特点,阐明了透皮促进剂的作用及其机理;介绍了国内外常用的透皮促进剂,综述其在透皮释放给药系统中合理知科学的应用。同时展示了透皮促进剂的新发展和药物增加透皮吸收的新研究。 相似文献
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透皮促进剂在经皮给药系统中的应用近况 总被引:3,自引:0,他引:3
透皮促进剂是指所有能够增加药物透皮速度而对皮肤不造成严重刺激和损害的物质。近年来 ,经皮给药系统的基础实验取得了可喜进展 ,透皮制剂的组方及用现代方法对药物在体内或体外透皮吸收进行较系统的研究成绩显著。经皮给药的理论基础为给药后 ,药物能迅速穿透皮肤 ,被吸收进入血液循环而产生疗效。因此 ,研究经皮给药制剂时首先必须解决药物对皮肤的穿透性和透皮速率。目前的技术多采用添加月桂氮酮(Azone)、亚油酸、丙二醇 (PG)等透皮促进剂来增加药物的穿透性和提高药物的透皮速率。在应用这些促进剂时 ,研究者又发现按一定比… 相似文献
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目的:考察不同促透剂对马钱子巴布剂中马钱子碱、士的宁的体外透皮吸收的影响,筛选合适的促透剂。方法:采用改良Franz扩散池对离体大鼠皮肤进行体外透皮实验,RP-HPLC法测定含不同促透剂的马钱子巴布剂中活性成分的累积渗透量(Q_n)和透过率(T)。结果:马钱子巴布剂体外透皮吸收符合零级动力学方程,不同的促透剂对透皮吸收影响的顺序为:DMF>月桂氮芯卓酮(氮酮)>丙二醇>薄荷醇。在给定的范围内(≤5%),氮酮和薄荷醇的促透性能均是随着浓度增大而先升后降,二甲基甲酰胺和丙二醇的促透效果都是随着浓度增大而增强。结论:不同浓度的促透剂均能一定程度促进马钱子巴布剂活性成分的透皮吸收,其中以5%DMF的促渗效果最好。 相似文献
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利用改良的Franz扩散池和离体小鼠皮肤,以增渗倍数和迟滞时间为考察指标,考察不同浓度的促渗剂(月桂氮革酮、油酸、冰片、薄荷醇和吐温-80)对巴布剂中双氯芬酸钠体外透皮的影响.结果表明,与不加促渗剂的空白对照组相比,加入1%月桂氮革酮、3%油酸、1%冰片、3%薄荷醇和1%吐温-80的巴布剂中双氯芬酸钠的增渗倍数分别为1.26、2.99、3.10、3.31和0.94,迟滞时间分别为3.30、0.33、0.15、0.04和1.25 h.可见,1%吐温-80无明显促渗作用,油酸、冰片和薄荷醇的促渗效果比月桂氮革酮更显著,且迟滞时间明显缩短. 相似文献
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Bupranolol (BPL) is a suitable drug candidate for transdermal drug delivery system development based on its favorable physicochemical and pharmacokinetic properties. The effect of different penetration enhancers on the permeation of BPL across rat skin was studied using side-by-side diffusion cells. 2-pyrrolidone (PY), 1-methyl-2-pyrrolidone (MPY), and propylene glycol (PG) at various concentrations were used as penetration enhancers along with 0.4% w/v aqueous suspension of BPL. Menthol at different concentrations in isopropanol-water (6:4) mixture also was used as an enhancer wherein BPL at 0.4% w/v was completely solubilized. Skin pretreatment studies were carried out with all the above enhancers to understand their role in the penetration enhancement effect. PY and MPY at 5% w/v concentrations increased the permeation of BPL by 3.8- and 2.4-fold, respectively, versus control (p < .01). PG at 10% and 30 w/v concentrations increased the flux of BPL by 2.5- and 5.0-fold, respectively, versus control (p < .001). Menthol at 2% w/v concentration increased the flux of BPL by 3.8-fold (p < .01) and further increase in menthol concentration significantly decreased the flux of BPL. Overall, pyrrolidones and menthol at low concentrations (5% w/v or less) and PG at 30% w/v concentration were effective as penetration enhancers for BPL. 相似文献
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考察了凝胶基质种类及浓度和促渗剂对姜黄素脂质体凝胶经小鼠离体皮肤的累积渗透量及皮肤滞留量的影响.所得优化处方为:以1%卡波姆为凝胶基质,加入2%月桂氮草酮和2%薄荷醇为复合促渗剂.所得制品的24h累积渗透量、稳态渗透速率及皮肤滞留量均显著高于姜黄素脂质体. 相似文献
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Structure/Effect Studies of Fatty Acid Isomers as Skin Penetration Enhancers and Skin Irritants 总被引:1,自引:0,他引:1
Comparisons were made of branched vs unbranched saturated fatty acids and cis vs trans unsaturated fatty acids as skin penetration enhancers and primary skin irritants. Skin penetration studies used naloxone base as the diffusant, propylene glycol as the vehicle, and human skin. Maximum naloxone flux was with C9–12-branched and unbranched fatty acids. For C5–14 fatty acids, branched and unbranched isomers had similar effects. One branched C18 fatty acid isomer (C16-branched isostearic acid) was more effective in enhancing skin penetration than a differently branched (C2-branched isostearic acid) or unbranched C18 isomer (stearic acid). There was no significant difference between cis and trans unsaturated C16–18 fatty acid isomers in their effects on naloxone flux, and all unsaturated fatty acids were more effective enhancers than the corresponding saturated isomers. Several of these fatty acid/propylene glycol vehicles were evaluated in a rabbit primary skin irritation test. Irritation indices were poorly correlated with the effectiveness of the vehicles in enhancing naloxone flux. It was possible to enhance naloxone skin penetration greatly with a vehicle with only minimal skin irritation potential. 相似文献
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Rachakonda VK Yerramsetty KM Madihally SV Robinson RL Gasem KA 《Pharmaceutical research》2008,25(11):2697-2704
Purpose A novel technique is presented for identifying potential chemical penetration enhancers (CPEs) based on changes in the electrical
resistance of skin.
Methods Specifically, a multi-well resistance chamber was designed and constructed to facilitate more rapid determination of the effect
of CPEs on skin resistance. The experimental setup was validated using nicotine and decanol on porcine skin in vitro. The multi-well resistance chambers were capable of operating at 37°C in order to simulate the physiological temperature
of the human body. Further, the utility of the multi-well resistance chamber technique was validated using standard Franz
diffusion cells. Electrical resistance measurements were used to evaluate the potency of seven new potential CPEs, identified
using virtual screening algorithms. From the resistance measurements, the chemicals 1-dodecyl-2-pyrrolidinone (P), menthone
(M) and R(+)-3-amino-1-hydroxy-2-pyrrolidinone (C) were identified as the better penetration enhancers among the seven tested.
Further, traditional permeation experiments were performed in Franz diffusion cells to confirm our findings.
Results The permeation test results indicated that, of the three CPEs deemed potentially viable using the newly-developed resistance
screening technique, both P and M increased the permeation of the test drug (melatonin) through skin in 48 h.
Conclusion In summary, this resistance technique can be used to effectively pre-evaluate potential CPEs, thereby reducing the time required
to conduct the permeability studies. 相似文献
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