Penetration of topical cyclosporine into the rabbit cornea, aqueous humor, and serum.
Penetration of topical cyclosporine into the rabbit cornea, aqueous humor, and serum.
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DOI：
10.1001/archopht.1985.01050010107030
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发表时间：
1985
影响因子：
--
通讯作者：
M. Mosteller;B. Gebhardt;A. Hamilton;H. Kaufman
中科院分区：
文献类型：
--
作者：
M. Mosteller;B. Gebhardt;A. Hamilton;H. Kaufman
用放射免疫法测定了10%环孢素软膏在兔角膜、眼房水和血清中的全身和眼部吸收。角膜中的药物浓度在施用后3小时达到900 ng/mL的峰值。在24小时时仍存在大量水平。在房水和血清中测量到相对较低的浓度，表明这种疏水性环肽在角膜基质中聚集。局部眼部应用环孢霉素可以减少或消除药物的全身毒性作用，同时保持局部免疫抑制活性的治疗水平。
Systemic and ocular absorption of topically applied 10% cyclosporine ointment was determined in rabbit cornea, aqueous humor, and serum by radioimmunoassay. The concentration of the drug in the cornea reached a peak of 900 ng/mL three hours after application. Substantial levels were still present at 24 hours. Relatively low concentrations were measured in the aqueous humor and serum, suggesting corneal stromal pooling of this hydrophobic cyclic peptide. Topical ocular application of cyclosporine may reduce or eliminate the drug's systemic toxic effects while maintaining a therapeutic level of local immunosuppressive activity.