三七总皂苷眼用凝胶在兔眼部的组织分布研究

Study on the tissue distribution of Panax notoginseng saponins ophthalmic gel in rabbit eyes

关键词:  三七皂苷R1  人参皂苷Rg1  眼用凝胶  组织分布

Key words:  Notoginsenoside R1  Ninsenoside Rg1  ophthalmic gel  tissue distribution

摘要:

[目的] 研究三七总皂苷眼用凝胶在兔眼组织的药物分布。[方法] 选取12只新西兰大白兔，随机分为4组，每组3只兔子。每只兔眼分别给予凝胶41.67 μL/kg（即三七皂苷R1 0.132 mg/kg，人参皂苷Rg1 0.452 mg/kg）。给药后于0.5、1、1.5、2 h空气栓塞各处死1组兔子。取眼球，分离各眼组织。采用UPLC-MS检测不同时间点各眼组织的药物含量。[结果] 兔眼给予三七总皂苷眼用凝胶后，三七皂苷R1在兔角膜、晶状体、房水、玻璃体中的最大含量分别为13.16、1.16、0.86、0.10 μg/g，人参皂苷Rg1在角膜、晶状体、房水、玻璃体中的最大含量分别为38.49、4.50、3.38、0.28 μg/g。[结论] 三七总皂苷眼用凝胶滴到兔眼后，三七皂苷R1和人参皂苷Rg1可透过角膜分散到各眼组织。在0~2 h内，各眼组织中的药物含量由高到低依次为角膜、晶状体、房水、玻璃体，表明三七皂苷R1和人参皂苷Rg1可透过角膜，到达眼后部组织，在2 h时各眼部组织的药物含量依然较高，在眼组织的保留时间长。

Abstract:

[Objective] Study on the tissue distribution of Panax notoginseng saponins ophthalmic gel in rabbit eyes.[Method] Twelve New Zealand white rabbits were randomly selected and divided into 4 groups, 3 rabbits in each group. Each rabbit eye was given the gel 41.67 μL/kg (Notoginsenoside R1 0.132 mg/kg, Ginsenoside Rg1 0.452 mg/kg) respectively. One group of rabbits were sacrificed by air embolism at 0.5, 1, 1.5, and 2 h after administration. Their eyeballs were removed, and the tissues of each eye were separated. UPLC-MS was used to detect the drug content of each eye tissue at different time.[Results] The maximum drug content of Notoginsenoside R1 in the cornea, lens, aqueous humor and vitreous of rabbits are 13.16, 1.16, 0.86, 0.10 μg/g, and the maximum drug content of Ginsenoside Rg1 in cornea, lens, aqueous humor and vitreous body are 38.49, 4.50, 3.38, 0.28 μg/g after the rabbit eyes were given Panax notoginsenoside ophthalmic gel, respectively.[Conclusion] Notoginsenoside R1 and Ginsenoside Rg1 and could disperse into various eye tissues through the cornea after the ophthalmic gel of Panax notoginseng saponins are dropped into the eyes of rabbits. Within 0~2 h, the drug content in each eye tissue from high to low is cornea, lens, aqueous humor, vitreous, indicating that Notoginsenoside R1 and Ginsenoside Rg1 and can penetrate the cornea and reach the posterior tissue of the eye. The drug content in each eye tissue was still high at 2 h, and the retention time in the eye tissue is long.