Oláh Z, Veselovský J, Gressnerová S, Veselá A
Klinika oftalmológie LF UK, Bratislava.
Cesk Slov Oftalmol. 2005 Jan;61(1):3-12.
The article documents results of experiments focused to influence the physiological IOP values after application of the COSOPT eye drops (double combination of bbb-blocker and carbonic anhydrase inhibitor), aminoacid 10% L-arginin.HCl and their mixture in rabbits.
COSOPT followed by 10% L-arginin.HCl and mixture of 10% L-arginin.HCl with COSOPT was instilled weekly into the left conjunctival sac of 5 adult rabbits (females of the New Zealand White species). The IOP and pupilar diameter were measured in 5, 15, 30, 60, 120, 180, 240 min. and 24 hours after instillation. The right eye was used as control.
The antiglaucomatic COSOPT no significantly decreased the rabbit IOP during 24 hours (mean value 1.85 %) in vivo. The aminoacid 10% L-arginin.HCl achieved significant decrease of the IOP: the mean value was 16.03% reaching maximum in 60th and 180th min. After instillation of the 10% L-arginin.HCl and COSOPT mixture in the IOP showed significant decrease with mean value of 9,64% (except values in 5th min. and 24th hour). Compared with control eye, the major decrease of the IOP was measured in 240th min. (mean value 17.98%). However even in 24 hours after instillation the IOP was not reaching the values of the control eye, shoving also the IOP decrease.
We assume that in a double combination of antiglaucomatics in COSOPT a new substance was created. This substance interacted in vitro with the aminoacid 10% L-arginin.HCl resulting in a new "bio-antiglaucomatis" better penetrating into the target area. This new substance was responsible for more significant decrease after the mixture application compared with COSOPT alone. The presence of aminoacid can slow down the undesirable effect of the antiglaucomatics together with the possible neuroprotection.
本文记录了在兔体内应用COSOPT眼药水（β受体阻滞剂和碳酸酐酶抑制剂的复方制剂）、10% L-精氨酸盐酸盐及其混合物后，旨在影响生理性眼压值的实验结果。
每周将COSOPT、随后的10% L-精氨酸盐酸盐以及10% L-精氨酸盐酸盐与COSOPT的混合物滴入5只成年兔（新西兰白兔雌性）的左眼结膜囊。在滴入后5、15、30、60、120、180、240分钟及24小时测量眼压和瞳孔直径。右眼作为对照。
抗青光眼药物COSOPT在体内24小时内未显著降低兔眼压（平均值1.85%）。10% L-精氨酸盐酸盐使眼压显著降低：平均值为16.03%，在第60和180分钟达到最大值。滴入10% L-精氨酸盐酸盐与COSOPT的混合物后，眼压显著降低，平均值为9.64%（第5分钟和第24小时的值除外）。与对照眼相比，在第240分钟眼压下降幅度最大（平均值17.98%）。然而，即使在滴入后24小时，眼压也未达到对照眼的值，也显示出眼压下降。
我们推测在COSOPT这种抗青光眼药物复方制剂中形成了一种新物质。该物质在体外与10% L-精氨酸盐酸盐相互作用，产生了一种新的“生物抗青光眼药物”，能更好地渗透到靶区域。与单独使用COSOPT相比，这种新物质在应用混合物后导致眼压更显著下降。氨基酸的存在可减缓抗青光眼药物的不良作用并可能具有神经保护作用。
