Vogelson Cullen T, Abelson Mark B, Pasquine Terri, Stephens Donna M, Gamache Daniel A, Gross Robert D, Robertson Stella M, Yanni John M
Alcon Research, Ltd., 6201 South Freeway, Fort Worth, TX 76134, USA.
Allergy Asthma Proc. 2004 Jan-Feb;25(1):69-75.
Pharmacologic studies examined the potential of a solution containing olopatadine to maintain and extend antiallergic efficacy after single topical ocular drop administration over 24 hours. Results of these preclinical experiments conducted in guinea pigs indicated that olopatadine 0.2% (wt/vol) solution was significantly effective 24 hours after dosing. This concentration of olopatadine provided significantly more efficacy than Patanol (olopatadine 0.1%) 24 hours after administration while being as effective as Patanol (olopatadine 0.1%) 5 minutes after administration. Results from a human conjunctival allergen challenge trial in sensitive subjects confirmed clinical efficacy of olopatadine 0.2% solution over 24 hours. When individuals were challenged with antigen at onset, 16 and 24 hours after drug administration onto the eye, significant reductions were observed in the scores for active drug as compared with placebo for pruritus (77, 77, and 61%), conjunctival redness (35, 28, and 20%), and chemosis (53, 41, and 31%), respectively. These data suggest that topically applied olopatadine 0.2% solution will be an effective once-a-day therapy for allergic conjunctivitis.
药理学研究考察了含奥洛他定的溶液在单次局部滴眼给药后24小时内维持和延长抗过敏疗效的潜力。在豚鼠身上进行的这些临床前实验结果表明，0.2%（重量/体积）的奥洛他定溶液在给药24小时后具有显著疗效。该浓度的奥洛他定在给药24小时后的疗效显著高于帕坦洛（0.1%奥洛他定），而在给药5分钟后的疗效与帕坦洛（0.1%奥洛他定）相当。在敏感受试者中进行的一项人类结膜过敏原激发试验结果证实了0.2%奥洛他定溶液在24小时内的临床疗效。当个体在给药于眼部后即刻、16小时和24小时接受抗原激发时，与安慰剂相比，活性药物在瘙痒（分别为77%、77%和61%）、结膜充血（分别为35%、28%和20%）和球结膜水肿（分别为53%、41%和31%）方面的评分显著降低。这些数据表明，局部应用0.2%奥洛他定溶液将是过敏性结膜炎一种有效的每日一次治疗方法。
