Newman S P
Pharmaceutical Profiles Ltd., Nottingham, U.K.
Crit Rev Ther Drug Carrier Syst. 1993;10(1):65-109.
Drugs are delivered to the upper or lower respiratory tract as aerosols via a range of inhalation devices in order to achieve either topical or systemic effects. It is important to be aware of the deposition pattern within the target organ inasmuch as treatment or prophylaxis will be effective only if sufficient drug is delivered directly to the required site. Drugs delivered to the nasal passages must be retained in the nose sufficiently long enough to exert a local effect or to be absorbed before they are removed by mucociliary clearance. Gamma-scintigraphy is a noninvasive technique capable of giving information about total and regional deposition in the lungs, or deposition in and subsequent clearance from the nasal passages, thus providing data that are difficult or impossible to obtain by other means. Radiolabeling strategies for scintigraphic studies of the respiratory tract usually involve the radionuclide 99mTc, which is added to the formulation in order to trace the location of the drug substance in the body. It is difficult to find suitable gamma ray-emitting radionuclides for direct chemical labeling of drug molecules. Pharmacoscintigraphic studies, combining scintigraphy and conventional pharmacokinetics, are able to give valuable insights into the in vivo behavior of compounds delivered to the systemic circulation via the respiratory tract.
药物通过一系列吸入装置以气雾剂形式输送至上呼吸道或下呼吸道,以实现局部或全身效应。了解药物在靶器官内的沉积模式很重要,因为只有当足够的药物直接输送到所需部位时,治疗或预防才会有效。输送到鼻腔的药物必须在鼻腔内保留足够长的时间,以发挥局部作用或被吸收,然后才被黏液纤毛清除。γ闪烁扫描是一种非侵入性技术,能够提供有关肺部总沉积和区域沉积的信息,或鼻腔内沉积及随后从鼻腔清除的信息,从而提供其他方法难以或无法获得的数据。用于呼吸道闪烁扫描研究的放射性标记策略通常涉及放射性核素99mTc,它被添加到制剂中以追踪药物在体内的位置。很难找到适合药物分子直接化学标记的γ射线发射放射性核素。药物闪烁扫描研究结合了闪烁扫描和传统药代动力学,能够深入了解通过呼吸道输送到体循环的化合物的体内行为。