Lee V H, Swarbrick J, Stratford R E, Morimoto K W
J Pharm Pharmacol. 1983 Jul;35(7):445-50. doi: 10.1111/j.2042-7158.1983.tb04319.x.
The influence of pH, tonicity, preservatives, polymers and instilled drop size on the disposition of sodium cromoglycate, an agent used in the prophylaxis of vernal keratoconjunctivitis, in the tear chamber of the albino rabbit eye has been examined. Radiotracer techniques were used throughout. The initial decline in concentration in the tear chamber was found to be unaffected by the presence of preservatives, pH, and tonicity over the ranges studied. However, significant increases in the residence time of sodium cromoglycate in the precorneal area were noted when a smaller instilled drop size was used and when 5% polyvinyl alcohol (PVA) was added to the aqueous vehicle. Tissue uptake was found to be greatest in the conjunctiva, followed by the cornea, the iris-ciliary body and the aqueous humor. In both the conjunctiva and the cornea, the addition of 5% PVA produced an elevation in the peak concentration of sodium cromoglycate and an increase in the time at which the peak concentration was achieved, indicating improved drug delivery to these sites.
已研究了pH值、张力、防腐剂、聚合物和滴入液滴大小对白化兔眼泪腔中用于预防春季角结膜炎的色甘酸钠分布的影响。整个过程采用放射性示踪技术。在所研究的范围内，发现泪腔中浓度的初始下降不受防腐剂、pH值和张力的影响。然而，当使用较小的滴入液滴大小以及向水性载体中添加5%聚乙烯醇（PVA）时，色甘酸钠在前角膜区域的停留时间显著增加。发现组织摄取在结膜中最大，其次是角膜、虹膜睫状体和房水。在结膜和角膜中，添加5% PVA均使色甘酸钠的峰值浓度升高，并使达到峰值浓度的时间增加，表明药物向这些部位的递送得到改善。
