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各种局部酒石酸溴莫尼定滴眼剂的趋化性质。

The chemotactic properties of various topical brimonidine tartrate ophthalmic preparations.

机构信息

Department of Ophthalmology, Fluminense Federal University, Niteroi, Rio de Janeiro, Brazil.

The Henry C. Witelson Ocular Pathology Laboratory, McGill University, Montreal, Canada.

出版信息

BMC Pharmacol Toxicol. 2020 Mar 23;21(1):24. doi: 10.1186/s40360-020-0401-z.

Abstract

BACKGROUND

The study aimed to evaluate and compare the leukocyte chemotactic activities of various brimonidine tartrate (BT) eye drop formulations.

METHODS

A 96-well dot-blot platet using a Boyden-style well was used to study the chemotactic effects of BT ophthalmic preparations. A modification was made to create blind wells where the tested agents were placed. Leukocytes were isolated from the peripheral blood of healthy volunteers. As positive controls, we used diluted drugs, benzalkonium chloride solution (BAK), zymosan-activated serum, and formyl-methionine-leucine-phenylalanine peptides. The negative control in our study was a phosphate-buffered saline solution. For each experimental condition, we measured leukocyte migration through a Millipore membrane. The differences in the mean migration distance between groups were compared using the analysis of variance (ANOVA).

RESULTS

The measured migration distances (in μm ± SD) were 62.14 ± 3.71 for BT 0.2% with BAK (Alcon Laboratories Inc.); 63.61 ± 3.81 for BT 0.2% with BAK (Allergan Inc); 40.36 ± 3.17 for BT 0.15% without BAK; and 41.02 ± 2.17 for BAK alone. The negative controls showed no chemotactic activity, while the positive controls showed the highest neutrophil migration of all experimental conditions. The differences between BT 0.15% without BAK and the other commercial formulations were statistically significant.

CONCLUSION

Commercial ophthalmic preparations of BT 0.2% with BAK 0.005% had higher chemotactic properties than the alternative of a lower concentration of BT and without the preservative BAK. Therefore, the latter should be considered for patients with glaucoma or ocular hypertension in order to minimize iatrogenic ocular inflammation.

摘要

背景

本研究旨在评估和比较各种酒石酸溴莫尼定(BT)滴眼液制剂的白细胞趋化活性。

方法

使用 Boyden 式孔的 96 孔点印迹平板研究 BT 眼用制剂的趋化作用。通过创建盲孔来进行改良,将测试药物放置在盲孔中。白细胞从健康志愿者的外周血中分离出来。作为阳性对照,我们使用了稀释药物、苯扎氯铵溶液(BAK)、酵母聚糖激活的血清和甲硫氨酸-亮氨酸-苯丙氨酸肽。我们研究中的阴性对照是磷酸盐缓冲盐水溶液。对于每个实验条件,我们通过 Millipore 膜测量白细胞迁移。使用方差分析(ANOVA)比较组间平均迁移距离的差异。

结果

测量的迁移距离(μm±SD)分别为:含 BAK(Alcon Laboratories Inc.)的 0.2% BT 为 62.14±3.71;含 BAK(Allergan Inc.)的 0.2% BT 为 63.61±3.81;不含 BAK 的 0.15% BT 为 40.36±3.17;单独 BAK 为 41.02±2.17。阴性对照没有趋化活性,而阳性对照显示所有实验条件下的中性粒细胞迁移最高。不含 BAK 的 0.15% BT 与其他商业制剂之间的差异具有统计学意义。

结论

含 BAK 0.005%的商业 BT 0.2%滴眼剂制剂具有比替代的低浓度 BT 和不含防腐剂 BAK 更高的趋化活性。因此,对于青光眼或高眼压患者,应考虑使用后者,以最大程度地减少医源性眼部炎症。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b093/7092528/f486e6acfc15/40360_2020_401_Fig1_HTML.jpg

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