Wang Chengshuo, Deng Qiu, Han Demin, Zhang Luo
Department of Otolaryngology, Head and Neck Surgery, Beijing TongRen Hospital, Capital Medical University, Beijing, China.
ORL J Otorhinolaryngol Relat Spec. 2012;74(3):149-53. doi: 10.1159/000337830. Epub 2012 Apr 13.
Preservatives are indispensable components of aqueous multidose topical formulations. The purpose of our study was to investigate the effects of two representative preservatives, benzalkonium chloride (BKC) and potassium sorbate (PS), on rabbit tracheal ciliary beat frequency (CBF).
Rabbit tracheal ciliated cell culture was established and CBF was determined using high-speed digital imaging methods. The effects of preservatives at different concentrations on CBF were observed over a 10-min exposure period.
BKC induced inhibition of CBF in a concentration-dependent manner. Ciliary beating was stopped by 0.01% BKC after 5 min of exposure. A low concentration of PS (0.12%) only resulted in a mild decrease in CBF during a 10-min exposure. The CBF decreased by 13.0% from baseline after 10 min. However, there was no statistically significant difference compared with the corresponding control condition. Application of 0.24, 0.48 and 0.96% of PS to rabbit tracheal cells resulted in an increase in CBF, with an increase of 105 ± 9.8, 107.6 ± 4.0, and 117.1 ± 9.5% relative to baseline CBF after 10 min of exposure, respectively.
PS could be considered as a safer and more promising preservative than BKC for use in topical formulations.
防腐剂是水性多剂量局部用制剂中不可或缺的成分。我们研究的目的是调查两种代表性防腐剂苯扎氯铵(BKC)和山梨酸钾(PS)对兔气管纤毛摆动频率(CBF)的影响。
建立兔气管纤毛细胞培养体系,采用高速数字成像方法测定CBF。在10分钟的暴露期内观察不同浓度防腐剂对CBF的影响。
BKC以浓度依赖性方式诱导CBF抑制。暴露5分钟后,0.01%BKC可使纤毛摆动停止。低浓度的PS(0.12%)在10分钟暴露期间仅导致CBF轻度下降。10分钟后,CBF较基线下降了13.0%。然而,与相应的对照条件相比,没有统计学上的显著差异。将0.24%、0.48%和0.96%的PS应用于兔气管细胞导致CBF增加,暴露10分钟后,相对于基线CBF分别增加了105±9.8%、107.6±4.0%和117.1±9.5%。
对于局部用制剂,PS可被认为是比BKC更安全、更有前景的防腐剂。