依巴斯汀抗组胺活性的随机、双盲、安慰剂对照研究

目的:研究单次口服依巴斯汀10mg的药效动力学特点。方法:60名健康受试者随机、双盲口服依巴斯汀10mg或安慰剂1片,于服药前和服药后2、4、24h,对全部受试者行组胺皮肤点刺滴定试验。在揭盲后,对依巴斯汀组的受试者于服药后48h再做一次组胺皮肤点刺滴定试验。以剂量-反应曲线下面积(AUDRC)和痒觉积分为参数,评价依巴斯汀的抗组胺活性。结果:服药前两组数据无统计学差异。依巴斯汀组的风团和红晕AUDRC于服药后2h即明显低于安慰剂组,而痒觉积分于服药后4h才明显低于安慰剂组(P<0.01)。服用依巴斯汀后24h,AUDRC和痒觉积分均降至最低;48h上述两者均有所升高,但仍明显低于服药前(P<0.01)。结论:依巴斯汀的抗组胺作用起效较慢,作用较强,持续时间较长。

A randomized, double-blind, placebo controlled study of the antihistamine activity of ebastine

Objective: To evaluate the pharmacodynamic characteristics of single dose of ebastine 10 mg. Methods: Ebastine 10 mg or 1 tablet of placebo was given to 60 healthy volunteers in randomized, double-blind manner. Histamine titration tests were performed for each volunteer before dosing and 2, 4, and 24 hours after dosing. Then opened the blind, the titration tests were performed for ebastine group 48 hours after dosing. The antihistamine activity of ebastine was evaluated by the area under dose-response curve (AUDRC) and itch score. Results: The data of two groups was comparable before dosing. The significant differences of AUDRC between ebastine and placebo group were observed 2, 4 and 24 hours after dosing, but the differences of itch score were observed 4 and 24 hours after dosing (P < 0.01). The AUDRC and itch score reached the lowest level 24 hours after dosing ebastine. At 48 hours, both of them were increased, but were still significantly different with those before dosing (P < 0.01). Conclusion: The present results show that ebastine has a slow onset of therapeutic effect, but potent and long-acting.