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鼻腔与脑在解剖生理上的独特联系使得鼻腔给药作为脑内递药途径成为可能.鼻腔给药作为脑靶向的途径之一,可有效地使通过其他给药途径不易透过血脑屏障的药物绕过血脑屏障到达脑部,为中枢神经系统疾病的治疗提供了一种极有发展前景的脑内递药途径.就鼻腔给药脑靶向的依据、影响因素、评价方法、剂型等方面对经鼻脑靶向递药系统的研究现状进行总结. 相似文献
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脑内靶向给药研究进展 总被引:3,自引:0,他引:3
血脑屏障 (bloodbrainbarrier,BBB)是药物进入脑部肿瘤组织和其他中枢神经系统 (centralnervesystem ,CNS)疾病病灶的最主要屏障。目前 ,虽然对于脑部疾病的研究取得了许多进展 ,但是如何将药物传递入脑仍是一个难题。BBB是由一层极化的血管内皮细胞紧密连接而成 ,其腔面侧 (luminal)的细胞膜与血液相接触 ,基膜侧 (abluminal)的细胞膜与脑细胞外液相接触。BBB是一选择性屏障 ,能够起到脑与血液循环相隔离的作用 ,又能够转运营养物质入脑 ,此外还能够清除脑内有毒物质。但… 相似文献
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《药学学报》2009,44(5):515-518
本文比较了灯盏花素鼻腔给药、口服给药与静脉给药在大鼠脑内的药物分布。采用SD大鼠尾静脉注 射、经鼻给药和灌胃0.4 mg·kg-1灯盏花素后, 于一定时间点用小脑延髓池穿刺术采集大鼠脑脊液, 125I标记法测定其在大鼠脑脊液,以及大脑、小脑、延脑、嗅区和嗅球等脑组织及血浆中药物含量, 梯形法分别计算其AUC。结果显示鼻腔给药组大鼠脑脊液、大脑、小脑、延脑、嗅区、嗅球及血浆中AUC0-240 min (μg·min·g-1) 分别为11.686 ± 1.919, 5.676 ± 1.025, 7.989 ± 0.925, 7.956 ± 1.159, 17.465 ± 2.136, 24.2 ± 2.906和78.51 ± 12.05; 静脉给药组AUC0-240 min分别为6.79 ± 0.661, 6.251 ± 0.40, 10.805 ± 1.161, 9.146 ± 1.04, 9.892 ± 1.532, 7.871 ± 0.842和173.91 ± 10.02; 口服给药组AUC0-240 min分别为0.868 ± 0.167, 1.708 ± 0.266, 2.867 ± 0.725, 2.067 ± 0.313, 1.361 ± 0.308, 1.206 ± 0.255和 45.2 ± 7.52。口服、静脉注射、鼻腔给药后脑组织的AUC0-240 min分别为血浆AUC0-240 min的22.29%, 29.18%, 95.49%, 说明鼻腔给药的吸收率高于口服给药和静脉给药, 并且鼻腔给药后药物在脑组织中分布较高, 其与药效的关系值得进一步探讨。
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目的:了解牙周递药系统的研究进展。方法:根据文献,对牙周炎疾病的治疗药物的载药方式进行综述。结果与结论:牙周递药系统的载药方式包括脂质体、纤维剂、棒剂、膜剂、微球、缓释凝胶、黏固剂。牙周递药系统已由传统给药方式逐渐转为以高分子材料为载体的缓释制剂,具有局部给药剂量小、可持续稳定释放药物、使药物浓集于牙周袋内、提高药物疗效等特点,是很有发展潜力的药物传递系统。 相似文献
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以牛血清白蛋白为载体,采用高压均质法制备替莫唑胺白蛋白纳米粒,并运用脑微透析技术,考察该纳米粒经大鼠尾静脉注射给药后的脑内递药特性.结果表明,白蛋白纳米粒形态圆整,平均粒径为(117.60±3.40) nm,ξ电位为(14.70±3.51)mV,包封率与载药量分别为(52.16±2.23)%和(5.33±0.10)%.替莫唑胺白蛋白纳米粒组的tmax和AUC0→1比其溶液剂组显著提高,但Cmax无显著差异.结果提示本品可延长药物在脑内的持续时间,促进药物的脑内吸收,有望成为替莫唑胺脑部递药的有效载体. 相似文献
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脂质体透皮给药研究进展 总被引:2,自引:0,他引:2
对脂质体与表皮角质层的作用作了综述。脂质体能增加角质层的含水量及水合作用,并与角质细胞间的脂质结合,可以削弱表皮角质层的屏障功能,促进透皮吸收。 相似文献
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紫杉醇靶向制剂的研究进展 总被引:9,自引:0,他引:9
目的:介绍紫杉醇靶向制剂的研究进展。方法:综述近年来有关的国内外文献,介绍和评价紫杉醇靶向制剂的制备、性质和药效等。结果:紫杉醇靶向制剂可以大大提高药物疗效,降低毒副作用。结论:紫杉醇靶向制剂为癌症化疗开辟了新的途径,可望在不久的将来,应用于临床。 相似文献
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透皮给药新进展 总被引:7,自引:0,他引:7
经皮治疗系统 (transdermaltherapeuticsystem ,TTS)或称经皮给药系统 (transdermaldrugdeliverysystem ,TDDS) ,是药物通过皮肤吸收的一种方法 ,它可避免肝脏首过效应 ,较长时间维持恒定速率给药及有效血药浓度。药物透皮吸收的主要屏障是角质层 (由约 4 0 %的蛋白质、4 0 %的水、15 %~ 2 0 %的类脂组成 ) ,其中类脂与蛋白质水凝胶组成网状结构。药物的透皮吸收过程就是药物在类脂相与水相间的分配、扩散、吸附和解吸附过程[1] 。但很多药物透皮吸收很难达到临床治疗所… 相似文献
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David C. Dorman Karrie A. Brenneman Anna M. McElveen Sean E. Lynch Kay C. Roberts Brian A. Wong 《Journal of toxicology and environmental health. Part A》2013,76(20):1493-1511
Experiments examining the dosimetry of inhaled manganese generally focus on pulmonary deposition and subsequent delivery of manganese in arterial blood to the brain. Growing evidence suggests that nasal deposition and transport along olfactory neurons represents another route by which inhaled manganese is delivered to certain regions of the rat brain. The purpose of this study was to evaluate the olfactory uptake and direct brain delivery of inhaled manganese phosphate ( 54 MnHPO 4 ). Male, 8-wk-old, CD rats with either both nostrils patent or the right nostril occluded underwent a single, 90-min, nose-only exposure to a 54 MnHPO 4 aerosol (0.39 mg 54 Mn/m 3 ; MMAD 1.68 w m, σ g 1.42). The left and right sides of the nose, olfactory pathway, striatum, cerebellum, and rest of the brain were evaluated immediately after the end of the 54 MnHPO 4 exposure and at 1, 2, 4, 8, and 21 d postexposure with gamma spectrometry and autoradiography. Rats with two patent nostrils had equivalent 54 Mn concentrations on both sides of the nose, olfactory bulb, and striatum, while asymmetrical 54 Mn delivery occurred in rats with one occluded nostril. High levels of 54 Mn activity were observed in the olfactory bulb and tubercle on the same side (i.e., ipsilateral) to the open nostril within 1-2 d following 54 MnHPO 4 exposure, while brain and nose samples on the side ipsilateral to the nostril occlusion had negligible levels of 54 Mn activity. Our results demonstrate that the olfactory route contributes to 54 Mn delivery to the rat olfactory bulb and tubercle. However, this pathway does not significantly contribute to striatal 54 Mn concentrations following a single, short-term inhalation exposure to 54 MnHPO 4 . 相似文献
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膜活性肽在胞内靶向给药系统中的应用 总被引:4,自引:0,他引:4
药物的靶向给药从到达的部位讲可以分为 3级 ,第 1级指到达特定的器官或组织 ;第 2级指到达器官或组织内的特定的细胞 (如肿瘤细胞而不是正常细胞 ,肝细胞而不是Kupffer细胞 ) ,第 3级指到达靶细胞内的特定的细胞器 (例如溶酶体 ,线粒体 ) [1] 。至今 ,前两级的靶向给药系统研究已经取得了长足的进步。如 80年代发展的微粒类被动靶向给药系统已经在制备方法、质量标准、体内分布、药效、毒性等方面有了许多研究报道。又如很多学者致力于将药物与配体通过共价的或物理的方式相连 ,配体与细胞表面的特异性受体接合 ,而到达器官或组织内… 相似文献
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MS Roberts 《Clinical and experimental pharmacology & physiology》1997,24(11):874-879
1. Drug delivery through the skin has been used to target the epidermis, dermis and deeper tissues and for systemic delivery. The major barrier for the transport of drugs through the skin is the stratum corneum, with most transport occurring through the intercellular region. The polarity of the intercellular region appears to be similar to butanol, with the diffusion of solutes being hindered by saturable hydrogen bonding to the polar head groups of the ceramides, fatty acids and other intercellular lipids. Accordingly, the permeability of the more lipophilic solutes is greatest from aqueous solutions, whereas polar solute permeability is favoured by hydrocarbon-based vehicles. 2. The skin is capable of metabolizing many substances and, through its microvasculature, limits the transport of most substances into regions below th. dermis. 3. Although the flux of solutes through the skin should be identical for different vehicles when the solute exists as a saturated solution, the fluxes vary in accordance with the skin penetration enhancement properties of the vehicle. It is therefore desirable that the regulatory standards required for the bio-equivalence of topical products include skin studies. 4. Deep tissue penetration can be related to solute protein binding, solute molecular size and dermal bloo. flow. 5. Iontophoresis is a promising area of skin drug delivery, especially for ionized solutes and when a rapid effect i. required. 6. In general, psoriasis and other skin diseases facilitate drug delivery through th. skin. 7. It is concluded that the variability in skin permeability remains an obstacle in optimizing drug delivery by thi. route. 相似文献
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睾酮经皮吸收膜剂选用硅橡胶为骨架材料,由铝塑背衬层、含药模层、压敏胶层、剥离纸组成。并用HPLC方法检测睾酮体外释药及经皮渗透速率,结果表明其离体渗透符合零级动力学过程。 相似文献