Liu S X, Chiou G C
Department of Medical Pharmacology and Toxicology, Texas A&M University, College of Medicine, College Station.
J Ocul Pharmacol. 1994 Fall;10(3):587-90. doi: 10.1089/jop.1994.10.587.
To determine the minimum effective concentration of insulin eyedrops for human use, insulin eyedrops at 0.01%, 0.05%, and 0.25% plus 0.5% Brij-78 were instilled into rabbit eyes. Brij-78 (0.5%) eyedrops were instilled as control. It was found that very low concentrations of insulin such as 0.05% plus 0.5% Brij-78 can reduce the blood glucose effectively in rabbits. The 0.05% insulin with 0.5% Brij-78 seems to be the best choice. Assuming the human body weight is approximately 25 times that of the rabbit, the concentration of insulin to be used for human patients would be 1.25% insulin (0.05% x 25), which is equivalent to 1.25 mg insulin/75 kg body weight. Because the absorption rate of insulin eyedrops plus Brij-78 is approximately 60-70%, 1.25% insulin plus Brij-78 would easily reach the therapeutic dose of insulin by injection (0.4-0.5 mg/75 kg). These results indicate that it is feasible to use insulin eyedrops to lower the blood glucose in humans. There was no statistical difference in blood glucose levels between animals instilled with 0.5% Brij-78 alone as control and those instilled with 0.01% insulin plus 0.5% Brij-78.
为确定人用胰岛素滴眼液的最低有效浓度，将含0.01%、0.05%和0.25%胰岛素加0.5%月桂醇聚醚-78的胰岛素滴眼液滴入兔眼。滴入含0.5%月桂醇聚醚-78的滴眼液作为对照。结果发现，极低浓度的胰岛素如0.05%加0.5%月桂醇聚醚-78可有效降低兔的血糖。含0.5%月桂醇聚醚-78的0.05%胰岛素似乎是最佳选择。假设人体重约为兔体重的25倍，用于人类患者的胰岛素浓度应为1.25%胰岛素（0.05%×25），相当于1.25毫克胰岛素/75千克体重。由于加了月桂醇聚醚-78的胰岛素滴眼液的吸收率约为60 - 70%，1.25%胰岛素加月桂醇聚醚-78很容易达到注射用胰岛素的治疗剂量（0.4 - 0.5毫克/75千克）。这些结果表明，使用胰岛素滴眼液降低人体血糖是可行的。单独滴入0.5%月桂醇聚醚-78作为对照的动物与滴入0.01%胰岛素加0.5%月桂醇聚醚-78的动物之间血糖水平无统计学差异。
