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用于治疗细菌性结膜炎的新型缓释基质中的磺胺哒嗪钠

[Sodium sulfapyridazine in new delayed-action bases for the treatment of bacterial conjunctivitis].

作者信息

Maĭchuk Iu F, Pozdniakov V I, Kur'iazov I K, Moldaver B L, Rusak A V

出版信息

Antibiot Khimioter. 1991 Apr;36(4):26-8.

PMID:1892429
Abstract

Possible preparation of 10 per cent sodium sulfapyridazine ophthalmic drops containing aubazidan, a microbial polysaccharide, providing prolongation of the drops action and stability on the storage was studied. The pharmacokinetic studies showed that aubazidan which is a natural polymer provided high prolongation of the sulfapyridazine effect in the tissues of the anterior part of the eye in rabbits. The prolonged effect was similar to the previously observed effect of the solutions containing synthetic polymers such as 1 per cent polyacrylamide and polyvinyl . Satisfactory tolerance by the rabbit eye tissues of 6-fold daily instillations of the 10 per cent sodium sulfapyridazine solution with aubazidan for the observation period of 1 month was stated. When stored in vials the 10 per cent sodium sulfapyridazine ophthalmic drops with 0.5 per cent of aubazidan preserved the stability for 24 months with respect to the colour, transparency, viscosity, pH and drug content. It was demonstrated with using the agar diffusion method and Staphylococcus aureus, Proteus vulgaris, Escherichia coli and Pseudomonas aeruginosa as the test cultures that sodium sulfapyridazine completely preserved its antimicrobial activity in the presence of aubazidan. The data suggested that clinical trials of the 10 per cent sodium sulfapyridazine solution with 0.2-0.5 per cent of aubazidan were promising in prevention and therapy of bacterial conjunctivitis.

摘要

研究了含微生物多糖奥巴齐丹的10%磺胺吡啶嗪眼药水的可能制剂,该制剂可延长眼药水的作用时间并在储存时保持稳定性。药代动力学研究表明,作为天然聚合物的奥巴齐丹可使磺胺吡啶嗪在兔眼前部组织中的作用显著延长。这种延长的作用类似于先前观察到的含有合成聚合物(如1%聚丙烯酰胺和聚乙烯)的溶液的作用。在为期1个月的观察期内,兔眼组织对含奥巴齐丹的10%磺胺吡啶嗪溶液每日6次滴注具有良好的耐受性。当储存在小瓶中时,含0.5%奥巴齐丹的10%磺胺吡啶嗪眼药水在颜色、透明度、粘度、pH值和药物含量方面保持24个月的稳定性。使用琼脂扩散法以及以金黄色葡萄球菌、普通变形杆菌、大肠杆菌和铜绿假单胞菌作为测试培养物表明,在奥巴齐丹存在的情况下,磺胺吡啶嗪完全保留了其抗菌活性。数据表明,含0.2 - 0.5%奥巴齐丹的10%磺胺吡啶嗪溶液在预防和治疗细菌性结膜炎方面的临床试验前景良好。

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