A benzamidine derivative from diminazene was tested for a novel activity: treatment of primary open‐angle glaucoma. This drug was incorporated into mucoadhesive polymeric inserts prepared using chitosan (Chs) and chondroitin sulfate (CS). Of current interest is the mucoadhesion, which increases the contact time with the ocular surface, resulting in improved bioavailability; also, the inserts are made to act as a prolonged release system. In the present work the inserts were prepared by the solvent casting method using different polymeric proportions (30:70, 50:50, 75:25% w/w Chs:CS and 100% Chs). Thermal analysis and infrared spectroscopy both demonstrated physical dispersion of the active drug. The most promising was the 50:50% Chs:CS which demonstrated that it was not fragile and has an in vitro release profile of up to 180 minutes. In addition, it presented greater adhesion strength in relation to the other formulations. These physicochemical results corroborate the in vivo tests performed. In this sense, we also demonstrated that the treatment with the 50:50% insert can control the intraocular pressure (IOP) for at least 3 weeks and prevents damage to the retinal ganglion cells (RGCs) compared to the placebo insert. Thus, this indicates thus that the new drug is quite viable and promising in glaucoma treatment.

中文翻译：

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用于治疗开角型青光眼的新型抗青光眼剂：用于药物释放和体外和体内研究的聚合物插入物。

测试了来自 diminazene 的苯甲脒衍生物的新活性：治疗原发性开角型青光眼。该药物被掺入使用壳聚糖 (Chs) 和硫酸软骨素 (CS) 制备的粘膜粘附聚合物插入物中。目前感兴趣的是粘膜粘附，它增加了与眼表的接触时间，从而提高了生物利用度；此外，插入物可用作延长释放系统。在目前的工作中，使用不同的聚合物比例（30:70、50:50、75:25% w/w Chs:CS 和 100% Chs）通过溶剂浇铸方法制备嵌件。热分析和红外光谱都证明了活性药物的物理分散。最有希望的是 50:50% Chs:CS，它证明了它并不脆弱，并且具有长达 180 分钟的体外释放曲线。此外，与其他配方相比，它具有更高的粘合强度。这些物理化学结果证实了进行的体内试验。在这个意义上，我们还证明，与安慰剂插入物相比，使用 50:50% 插入物的治疗可以控制眼内压 (IOP) 至少 3 周，并防止对视网膜神经节细胞 (RGC) 的损伤。因此，这表明该新药在青光眼治疗中是非常可行和有前景的。