Merkus F W, Schüsler-van Hees M T
Center for Biopharmaceutical Sciences, Leiden University, The Netherlands.
Allergy. 1992 Jun;47(3):230-3. doi: 10.1111/j.1398-9995.1992.tb00655.x.
The effects of levocabastine, a new fast-acting, highly potent H1-antagonist, on nasal ciliary epithelial function were investigated in an in vitro and in vivo study. In the in vitro study, a suspension of levocabastine in Locke-Ringer solution was applied to 10 bioptic specimens of ciliated human adenoid tissue. Each specimen was exposed to the test solution for 60 min. Ciliary beat frequency (CBF) was recorded with a photoelectric recording device at 10-min intervals. There were small, insignificant decreases in CBF, which were minimal compared to that observed with ciliotoxic agents. In the in vivo study, 8 healthy volunteers were given, intranasally, one droplet of the levocabastine suspension. Mucociliary transit time (MTT) was measured by placing a saccharin particle drenched in indigo carmine in the nose just below the top of the concha and measuring the time until appearance of the dye in the pharyngeal cavity. No statistically significant differences were found in the MTT before and after application of the levocabastine suspension. The studies thus indicate that nasally administered levocabastine does not interfere with ciliary beat frequency and mucociliary function.
在一项体外和体内研究中,对新型速效、高效H1拮抗剂左卡巴斯汀对鼻纤毛上皮功能的影响进行了研究。在体外研究中,将左卡巴斯汀在洛克林格溶液中的悬浮液应用于10个有纤毛的人腺样体组织活检标本。每个标本暴露于测试溶液60分钟。用光电记录装置每隔10分钟记录一次纤毛摆动频率(CBF)。CBF有微小的、不显著的下降,与用纤毛毒性剂观察到的情况相比,这种下降是最小的。在体内研究中,8名健康志愿者经鼻给予一滴左卡巴斯汀悬浮液。通过将浸有靛胭脂的糖精颗粒置于鼻甲顶部下方的鼻腔中,并测量染料在咽腔中出现之前的时间来测量黏液纤毛传输时间(MTT)。应用左卡巴斯汀悬浮液前后的MTT未发现统计学上的显著差异。因此,这些研究表明经鼻给药的左卡巴斯汀不会干扰纤毛摆动频率和黏液纤毛功能。