Newman S P, Steed K P, Hooper G, Brickwell J
Pharmaceutical Profiles Ltd, Highfields Science Park, Nottingham, UK.
J Pharm Pharmacol. 1995 Oct;47(10):818-21. doi: 10.1111/j.2042-7158.1995.tb05747.x.
The distributions of fusafungine (Locabiotal, Servier) radiolabelled with 99mTc, and delivered either orally or intranasally, have been assessed in healthy volunteers from a pressurized metered-dose aerosol inhaler (125 micrograms per dose) and from a novel mechanical pump spray device (500 micrograms per dose). More than 90% of the dose was initially deposited in the oropharynx for oral dosing (n = 8), and more than 90% in the nose for nasal dosing (n = 9), with no significant penetration of aerosol into the lungs. Although not statistically significant, the mean area of deposition, measured in terms of gamma camera picture elements (pixels), was greater with the pump spray for both oral and nasal dosing. The area of deposition with the nasal pump spray extended into the turbinates in six of nine subjects, compared with only three of nine subjects for the pressurized aerosol. The data suggest that the distribution patterns of pump sprays and pressurized aerosols of fusafungine in the oropharynx and in the nasal passages are similar, and that the former can be substituted for the latter with little change in drug delivery.
已对健康志愿者使用99mTc标记的夫沙芬净（Locabiotal，施维雅公司）通过定量压力气雾剂吸入器（每剂125微克）和新型机械泵喷雾装置（每剂500微克）经口服或鼻内给药后的分布情况进行了评估。口服给药（n = 8）时，超过90%的剂量最初沉积在口咽部，鼻内给药（n = 9）时，超过90%的剂量沉积在鼻腔，气雾剂无明显进入肺部的情况。尽管无统计学意义，但就γ相机图像元素（像素）而言，口服和鼻内给药时泵喷雾的平均沉积面积均大于定量气雾剂。鼻用泵喷雾的沉积面积在9名受试者中有6名延伸至鼻甲，而定量气雾剂在9名受试者中只有3名如此。数据表明，夫沙芬净的泵喷雾和定量气雾剂在口咽部和鼻腔的分布模式相似，且前者可替代后者，药物递送变化不大。
