用于全身治疗的鼻腔给药系统

从药剂学角度对鼻的解剖生理及给药特点、影响药物在鼻腔中吸收的因素，特别就吸收促进剂和剂型因素与多肽和蛋白质类药物鼻腔给药的关系进行了综述。     

中药鼻腔给药系统研究现状

依据近年来国内外相关文献资料,对有关鼻腔给药系统自身及其在中医药中的应用发展进行了综述,介绍了鼻腔给药系统的特点及其在中医药中的传统应用与最新进展.通过文献研究发现鼻腔给药在中医药中的应用有悠久的历史,而中药现代鼻腔给药系统的研究值得关注.     

鼻腔给药的研究进展

鼻腔给药是一种极具潜力的药物转运系统。本文对影响鼻腔给药药物吸收的因素进行了介绍,并对鼻腔药物转运系统中所使用的药物吸收促进剂、生物粘附材料、研究方法等进行了综述。     

鼻腔给药系统的鼻粘膜毒性及解决途径

就鼻腔给药系统可能导致的鼻粘膜毒性的评价方法、易产生毒性的制剂组分及解决毒性的方法进行简要的综述。     

鼻腔给药的研究进展

鼻腔给药具有生物利用度高、起效快、无损伤性、使用方便等特点，成为制剂领域的研究热点；鼻腔与脑部的生理联系，使鼻腔给药成为有效治疗脑部疾病的一种新途径。鼻腔给药存在的最大问题是大分子药物的促吸收和鼻粘膜纤毛毒性问题。本文结合鼻腔的生理特点，综述了近年来鼻腔给药的研究进展。     

鼻腔给药系统的研究新进展

近年来药物的鼻腔给药系统受到了越来越多的关注.全球众多制药行业都在致力于基因和多肽类药物新型鼻腔给药系统的研发.现阐述了鼻腔生理特点和药物鼻黏膜转运机制及其影响因素,并对近年来鼻腔给药系统的促吸收途径和发展动向作一概述.     

鼻腔局部给药治疗全身疾病的研究进展

目的:对鼻腔局部给药治疗全身疾病的研究进展进行综述.方法:检索国内外近5年的文献,对其分析综述.结果:鼻腔给药具有生物利用度高、吸收迅速、起效快、损伤小、使用方便等特点,鼻腔局部用药已经成为治疗全身疾病的有效途径.结论:鼻腔局部给药可治疗全身疾病,值得临床推广和深入研究.     

用于全身治疗的鼻腔给药系统研究概况

目的介绍用于全身治疗的鼻腔给药系统研究概况。方法综述了鼻腔给药的特点、手段、制剂方法、要求、影响因素及研究状况。结果与讨论鼻腔给药可以产生全身作用,可以代替静脉给药,有广泛的应用前景。     

用于全身治疗的鼻腔给药系统研究概况

目的介绍用于全身治疗的鼻腔给药系统研究概况。方法综述了鼻腔给药的特点、手段、制剂方法、要求、影响因素及研究状况。结果与讨论鼻腔给药可以产生全身作用,可以代替静脉给药,有广泛的应用前景。     

鼻腔给药系统研究进展

从鼻粘膜的生理特性、药物动力学、剂型、影响药物吸收及生物利用度的因素、对鼻粘膜的毒性、动物模型等方面综述鼻腔给药系统的研究进展情况.     

胰岛素鼻腔给药制剂的试验研究

目的:将胰岛素制成一个较稳定的鼻腔给药制剂,为临床提供一个初步可行的用药依据。方法:采用LGY(国外药物透皮扩散室)扩散小室法,用人的胎盘膜模拟鼻黏膜先在体外做累积溶出度试验,再用大白兔做效用试验,验证制剂的可行性及试用性,并采用不同pH值、不同温度控制制剂的稳定性,观察其最稳定的保存时间及温度。结果:本课题采用了氮酮、油酸、丙二醇为联合促透剂,聚乙二醇为基质及稳定剂,以丙三醇为保湿剂,形成一个较稳定的新制剂;本制剂的平均回收率为63.53%,体外累积溶出度6 h,达高峰为42.31%,其制剂在pH 4.0时较稳定,保存温度为2℃,放置1个月后其含量为66.59%;在动物药效试验中,皮下注射组血糖值在给药后1 h降至最低,8 h基本恢复正常;而试验组给药后2 h降至最低,维持较低血糖值的时间比皮下注射组相对较长。结论:体外试验及动物试验表明,胰岛素在促透剂的作用下可以透过鼻黏膜,但所需的剂量较大,经济上损耗大,有待于今后进一步研究。     

Effect of route of administration on drug disposition

While the first-pass effect is a fairly generally understood phenomenon in the gross sense, it is not commonly appreciated that the rate at which the drug is delivered to the liver can influence the fraction of the administered dose which reaches the fluids of distribution. The drug molecules being absorbed via the hepatic portal vein intermix with previously absorbed drug recycling in the hepatic artery. The concentration of the drug returning via the hepatic artery is affected by the volume of distribution of the drug into body tissues (and the relative partition of the drug between the blood and the tissues). If one presumes that liver uptake is controlled by a Michaelis-Menten process of metabolism, it can be readily shown that the extent of extraction of the drug by the liver is controlled not only by the Michaelis-Menten constants, but also by the concentration of the drug transitting the liver per unit time. The effects of dose, rate of absorption, partitioning, and tissue distribution characteristics are systematically discussed and referred to in relation to selected examples of drugs in common use.The work reported here was supported in part by grant NIGMS16496-05.Presented by S. Reigelman at the Conference on Pharmacology and Pharmacokinetics: Problems and Perspectives, October 30–November 1, 1972, at the Fogarty International Center, National Institutes of Health, Bethesda, Maryland. This paper, in a slightly different format, will be published in the Proceedings of the Conference by Plenum Press, New York.     

Evaluation of effect of ephedrine on the transport of drugs from the nasal cavity to the systemic circulation and the central nervous system

It has been shown that vasoconstrictive drugs such as ephedrine derivatives are able to decrease systemic absorption of drugs administered by mucosal surfaces. The present paper set out to evaluate in the rat model the effect of co-administered nasal ephedrine on the absorption of GR138950 in a simple and in a pectin self-gelling formulation. It was hypothetised that a decrease in nasal systemic absorption would lead to an increase in direct nose-to-brain transport as demonstrated by the drug concentration in the olfactory lobes of the brain. It was found that ephedrine administered nasally with the drug in a simple aqueous solution resulted in a significant increase in nasal systemic absorption and also an increase in brain delivery; however, this trend was not observed with the pectin formulations. The pectin formulation with ephedrine resulted in lower systemic absorption of GR138950 and lower brain uptake compared to the simple solution formulation containing ephedrine.     

薄荷醇预处理对胰岛素鼻腔给药药理生物利用度的影响

目的　探讨薄荷醇预处理对胰岛素 (Insulin ,Ins)鼻腔给药药理生物利用度的影响。方法　建立糖尿病大鼠模型 ,用薄荷醇预处理鼻腔 ,2h后滴入胰岛素 ,不同时间取血测血糖浓度 ,计算曲线上面积和药理生物利用度。结果　用不同浓度薄荷醇预处理鼻腔后 ,在 2 0～ 3 0h时薄荷醇对Ins的鼻腔吸收具有显著的促进作用 ,Ins鼻腔吸收的药理生物利用度比空白对照组分别增加 5 77、7 0 0和 3 12倍。结论　薄荷醇可促进胰岛素的鼻腔吸收。     

药物鼻黏膜递送的影响因素

鼻腔给药以其吸收快、使用方便、可避免药物胃肠道降解和肝脏首过效应、生物利用度高、实现脑靶向等特点，日益受到人们的重视，成为制剂学领域的研究热点之一。现综述影响药物在鼻腔内吸收的各种因素，包括生理因素、药物的理化性质、剂型和辅料的性质，以及给药装置的影响，为鼻腔给药系统的研究提供参考。     

中药白芷乳剂大鼠鼻腔给药的体内研究

目的：探讨白芷乳剂量腔给药的可行性。方法：以白芷主要有效成分欧前胡素和异欧前胡素为检测指标,探讨白芷乳剂大鼠鼻腔给药的药物动力学参数及脑组织中的含量。结果：欧前胡素和异欧前胡素鼻腔给药的tmax均为0．500h,Cmax分别为3．161,2．916μg/ml,AUC0p→∞分别为为20．205,28．117μg.h/ml,T1/2分别为4．779,6．301h,给药15min,即可透过血脑屏障,进入脑组织,4h时脑组织中含量分别为40．368,22．849μg/100mg。结论。白芷乳剂鼻腔给药具有一定的可行性。     

鼻用原位凝胶给药系统中药物吸收的影响因素与改进措施

药物的吸收主要是由药物的理化性质、剂型以及给药途径所决定的。原位凝胶是指在生理条件刺激下能发生分散状态或构象的可逆变化、完成溶液与凝胶间相互转变的新剂型。原位凝胶经鼻腔给药,既避免了药物的胃肠首过效应,又因其能延长药物在给药部位滞留时间,从而避免药物被鼻纤毛快速清除。本文通过系统查阅近年国内外鼻用原位凝胶给药系统的相关文献,就鼻腔的生理特点、药物理化性质与原位凝胶的制剂处方等影响其药物吸收的主要因素及改进措施,进行分析、整理和归纳,旨在为鼻用原位凝胶给药系统的设计与质量控制提供参考。     

吸收促进剂的作用机制及其在鼻腔给药中的研究进展

随着新的蛋白质及肽类治疗药物的开发,非侵入性给药途径-鼻腔给药日益受到关注。与口服给药和注射给药相比,鼻腔给药既可避免注射给药带来的生理和心理创伤,也可消除口服给药过程中肝脏的首过效应;且鼻腔黏膜下血管丰富,有助于药物的吸收,也更加便于患者的抢救和自救。然而,由于鼻黏膜屏障的存在,药物很难达到理想的治疗效果,因此需要加入鼻黏膜吸收促进剂来增强药物的吸收。该文主要探讨鼻黏膜吸收促进剂的作用机制及分类,并对FDA已上市鼻腔制剂中的吸收促进剂进行汇总,同时对新型黏膜吸收促进剂在鼻腔给药制剂中的应用进行阐述,以期为鼻腔给药制剂的开发提供依据。     

各种吸收促进剂对黄芩苷鼻腔吸收的影响

目的研究黄芩提取物中黄芩苷的鼻腔吸收规律和9种吸收促进剂对黄芩苷鼻腔吸收的促进作用,寻找有效的鼻腔吸收促进剂。方法采用大鼠在体鼻腔循环法考察黄芩苷鼻腔吸收,以鼻腔吸收的一级动力学常数来衡量各种吸收促进剂促吸收作用的强弱。结果黄芩苷鼻腔吸收需加入吸收促进剂,各种不同质量分数吸收促进剂的促进作用为:1%去氧胆酸钠0.5%壳聚糖≈0.5%冰片≈5%甲基化-β-环糊精>5%HP-β-CD>5%β-CD>1%Tween-80≈0.1%EDTA-Na2≈1%磷脂,其中加入最后三者的促吸收效果与不加吸收促进剂时无显著性差异。结论质量分数为1%去氧胆酸钠促吸收效果最好,但鼻黏膜毒性较大,0.5%壳聚糖、0.5%冰片、5%甲基化-β-环糊精和5%HP-β-CD可安全有效地促进黄芩苷的鼻腔吸收。     

Thermally reversible xyloglucan gels as vehicles for nasal drug delivery

The aim of this study was to investigate the potential application of thermosensitive gels formed by a xyloglucan polysaccharide derived from tamarind seed for nasal drug delivery. Xyloglucan that had been partially degraded by β-galactosidase to eliminate 45% of galactose residues formed gels at concentrations of 2.5% w/w at gelation temperatures decreasing over the range 27–28°C. The in vitro release of ondansetron hydrochloride from the enzyme-degraded xyloglucan gels followed higuchi kinetics over a period of 5?h at 34°C by anomalous transport mechanism. The ex vivo permeation of ondansetron hydrochloride from the gels was sustained. Histological examination of nasal mucosa following a single administration of the gels showed no evidence of mucosal damage. Finally, the bioavailability study in rabbits revealed that the absolute bioavailability of ondansetron hydrochloride was significantly increased from 28.64% in the case of the oral drug solution to 52.79% in the case of the nasal in situ gel. The results of this study suggest the potential of the enzyme-degraded xyloglucan gels as vehicles for nasal delivery of drugs.