Department of Clinical Pharmacology, Maastricht University Medical Centre, Maastricht, the Netherlands.
Clin Ther. 2009 Dec;31(12):2954-87. doi: 10.1016/j.clinthera.2009.12.015.
Interest in the development of drug-delivery devices that might improve treatment compliance is growing. A dosage formulation that is easy to use, such as intranasal application with transmucosal absorption, may offer advantages compared with other routes of drug delivery. The literature concerning intranasal application is diffuse, with a large number of published studies on this topic. Some cerebroactive pharmaceuticals delivered intranasally might follow the pathway from the nose to the systemic circulation to the brain. To determine the suitability of these drugs for intranasal drug delivery, a systematic review was performed.
The aim of this review was to compare the pharmacokinetic properties of intranasal, intravenous, and oral formulations in 3 classes of cerebroactive drugs that might be suitable for intranasal delivery-opioids, benzodiazepines, and antimigraine agents.
A search of MEDLINE, PubMed, Cumulative Index of Nursing and Allied Health Literature, EMBASE, and Cochrane Database of Systematic Reviews (dates: 1964-April 2009) was conducted for pharmacokinetic studies of drugs that might be suitable for intranasal delivery. A comparison of pharmacokinetic data was made between these 3 routes of administration.
A total of 45 studies were included in this review. Most of the opioids formulated as an intranasal spray reached a T(max) within 25 minutes. The bioavailability of intranasal opioids was high; in general, >50% compared with opioids administered intravenously. Intranasal benzodiazepines had an overall T(max) that varied from 10 to 25 minutes, and bioavailability was between 38% and 98%. T(max) for most intranasal antimigraine drugs varied from 25 to 90 minutes. Intranasal bioavailability varied from 5% to 40%.
This review found that intranasal administration of all 3 classes of drugs was suitable for indications of rapid delivery, and that the pharmacokinetic properties differed between the intranasal, oral, and intravenous formulations (intravenous > intranasal > oral).
人们对于能够提高治疗顺应性的药物输送装置的开发越来越感兴趣。与其他药物输送途径相比，易于使用的剂型，如经鼻腔应用和黏膜吸收，可能具有优势。关于经鼻腔应用的文献很多，有大量关于这个主题的已发表研究。一些经鼻腔给予的脑活性药物可能会沿着从鼻子到全身循环再到大脑的途径。为了确定这些药物经鼻腔给药的适用性，进行了系统评价。
本综述的目的是比较 3 类可能适合经鼻腔给药的脑活性药物（阿片类药物、苯二氮䓬类药物和抗偏头痛药物）的经鼻腔、静脉内和口服制剂的药代动力学特性。
对 MEDLINE、PubMed、Cumulative Index of Nursing and Allied Health Literature、EMBASE 和 Cochrane Database of Systematic Reviews（日期：1964 年-2009 年 4 月）进行了检索，以获取可能适合经鼻腔给药的药物的药代动力学研究。对这 3 种给药途径的药代动力学数据进行了比较。
本综述共纳入 45 项研究。大多数制成鼻腔喷雾剂的阿片类药物达到 T(max)的时间在 25 分钟内。鼻腔给予阿片类药物的生物利用度较高；通常与静脉内给予的阿片类药物相比，大于 50%。鼻腔给予的苯二氮䓬类药物的总体 T(max)为 10-25 分钟，生物利用度为 38%-98%。大多数经鼻腔给予的抗偏头痛药物的 T(max)为 25-90 分钟。经鼻腔的生物利用度为 5%-40%。
本综述发现，这 3 类药物的经鼻腔给药均适用于快速递送的适应证，并且药物动力学特性在经鼻腔、口服和静脉内制剂之间存在差异（静脉内>经鼻腔>口服）。
