Aoki F Y, Crowley J C
Br J Clin Pharmacol. 1976 Oct;3(5):869-78. doi: 10.1111/j.1365-2125.1976.tb00640.x.
The efficacy of antiviral drugs and vaccines administered intranasally may depend upon the technique of application. The distribution and time-course of removal of human serum albumin-technetium 99m (HSA-Tc 99m)-instilled intranasally were studied in eleven healthy volunteers using a gamma camera and an anterior sodium iodide scintillation detector. In 100 randomized studies material was delivered as drops in the supine position or as a spray to seated subjects. A significantly higher proportion of 'good' distributions (62 in 73 tests) was obtained with drops compared with spray (1 in 27). The volume administered was varied between 0.10 ml and 0.75 ml and the concentration of HSA was changed from 3 to 30% with no significant effect upon the distribution of time-course of removal; pertechnetate in isotonic saline was distributed and removed in a manner comparable to HSA-Tc 99m. Activity recorded by the detector showed an initial rapid fall associated with removal of most of the material from the nasal cavity, followed by a slower decline associated with the removal of material mainly from the anterior region of the nose. A multidose study confirmed that frequent administration by drops is required to maintain a high level of activity in the nasal cavity. Using this technique it should be possible to correlate measurements of antiviral efficacy and vaccines take-rates with certain characteristics of intranasal applicators; such studies may lead to the design of better devices.
经鼻给药的抗病毒药物和疫苗的疗效可能取决于给药技术。使用γ相机和前部碘化钠闪烁探测器,在11名健康志愿者中研究了经鼻滴注人血清白蛋白-锝99m(HSA-Tc 99m)的分布及清除时间过程。在100项随机研究中,将材料以滴剂形式给仰卧位受试者或喷雾形式给坐位受试者。与喷雾给药(27次中有1次)相比,滴剂给药获得“良好”分布的比例显著更高(73次测试中有62次)。给药体积在0.10 ml至0.75 ml之间变化,HSA浓度从3%变为30%,对清除时间过程的分布无显著影响;高锝酸盐在等渗盐水中的分布和清除方式与HSA-Tc 99m相当。探测器记录的活性显示,最初快速下降与鼻腔内大部分物质的清除有关,随后下降较慢,与主要从鼻前部区域清除物质有关。一项多剂量研究证实,需要频繁滴注才能在鼻腔内维持高水平的活性。使用该技术应该能够将抗病毒疗效和疫苗接种率的测量结果与鼻内给药器的某些特性相关联;此类研究可能会促成更好装置的设计。