哌仑西平眼部离子导入治疗近视的药效学研究

目的观察哌仑西平眼部离子导入治疗近视的药效，为哌仑西平的临床使用提供实验依据。方法出生3周的花色豚鼠81只,随机分为9组，其中7组以单眼眼睑缝合法建立形觉剥夺性近视模型。在进行近视诱导的同时,9个组别分别接受如下处理：3组进行形觉剥夺眼的哌仑西平电场促透（离子导入），其中包括高、中、低三种不同的电流强度（PIRx-MD）；1组为形觉剥夺眼的空白对照组高电流强度离子导入（Vehicle0．3-MD）；1组为无电场促透的哌仑西平局部滴眼（PIR-MD）；1组为无电场促透的阿托品局部滴眼（At-ropine-MD）；1组为单纯形觉剥夺对照组（Normal-MD）；其余2组未建立形觉剥夺，作为对照。处理时间30d。检验指标包括屈光度、眼球前后径、眼球重量和组织病理学。结果Normal-MD和Vehicle 0．3-MD组实验眼诱导出-4．64D和-4．33D的近视,哌仑西平离子导入的3组分别诱导出-2．15D、-0．17D、-1．30D的近视；Normal-MD组实验眼的眼球前后径在实验结束时较对照眼增加0．3mm。哌仑西平离子导入的3组分别增加-0.1mm、0mm、-0．1mm：Normal-MD组眼球重量较对照眼增加0．02g,哌仑西平离子导入的3组分别增加0g、0g、-0．02g。两者之间差异均有统计学意义。所有实验眼光镜病理检查未发现异常改变。结论哌仑西平眼部离子导入抑制实验性近视效果明显优于局部滴眼,和阿托品作用类似；同时不引起眼组织的病理改变。

Study of the pharmacodynamics of pirenzepine iontophoresis for experimental myopia

Objective The purpose of the investigation was to examine the effect of pirenzepine iontophoresis on controlling experimental myopia and the possibility of injury to ocular tissues. Methods Three-week-old guinea pigs were monocularly deprived （MD） by lid-suture for a period of 30 days. During the 30 days, three of the MD groups received daily iontophoresis of pirenzepine （variable current intensity） （PIRx-MD）; one group received daily iontophoresis of vehicle （Vehicle 0.3-MD）. Control groups （PIR-MD, Atropine-MD, Normal-MD） were used to assess the effects of MD, the iontophoresis regimen, and drug effects. Retinoscopy, anterior/ posterior dimensions, and eye weight were measured and a histological examination was performed. Results In Normal-MD and Vehicle 0.3-MD guinea pigs, 30 days of MD produced -4.64 D and -4.33 D of axial myopia, respectively. In pirenzepine ion- tophoresis MD guinea pigs, 30 days of MD induced an axial myopia of only -2.15 D, -0.17 D and -1.30 D, respectively, The increments in anterior/posterior dimensions were -0.1 mm, 0 mm and -0.1 mm, respectively, in the three PIRx-MD groups, and 0.3 mm in the Normal-MD group. The increments in eye weight were 0 g, 0g and -0.02 g in the three PIRx-MD groups and 0.02 g in the Normal-MD group. Histological examination revealed no evidence of gross toxic effects. Conclusion Iontophoresis can enhance the corneal penetration of pirenzepine. Chronic administration of pirenzepine by iontophoresis can safely prevent experimentally induced myopia more effectively than topical instillation.