冰片和熊去氧胆酸对黄芩苷角膜透过性的影响

目的 研究冰片、熊去氧胆酸对黄芩苷离体角膜透过率的影响,探讨其在眼用制剂中的应用.方法 采用离体角膜渗透技术考察不同质量浓度的冰片、熊去氧胆酸对黄芩苷角膜透过率的影响.结果 0.2 mg/mL的冰片使黄芩苷表观渗透系数(Papp)增加了1.36倍,与对照组相比具有显著性差异(P＜0.05);0.3、0.4、0.5、0.7 mg/mL的冰片使黄芩苷Papp分别增加了1.35、1.43、1.51、3.47倍,0.2、0.3、0.4、0.5、0.7 mg/mL的熊去氧胆酸使黄芩苷Papp分别增加了1.19、2.25、1.24、0.35、0.68倍,与对照组相比均具有非常显著性差异(P＜0.01).结论 0.2、0.3、0.4、0.5、0.7 mg/mL的冰片、熊去氧胆酸能够显著增大黄芩苷的Papp,且对角膜无刺激性.

Effects of borneol and ursodesoxycholic acid on corneal permeability of baicalin

Abstract: Objective To investigate the effects of borneol and ursodesoxycholic acid on the corneal permeability of baicalin in vitro, and to discuss their application in ocular preparation. Methods The effects of borneol and ursodesoxycholic acid with different concentration on the corneal permeability of baicalin were investigated in vitro using the isolated corneal penetration technology. Results Borneol (0.2 mg/mL) could significantly increase the apparent permeability (P_app) of baicalin in 1.36-fold compared with the control group (P < 0.05). Borneol (0.3, 0.4, 0.5, and 0.7 mg/mL) could increase the P_app of baicalin in 1.35-, 1.43-, 1.51-, and 3.47-folds, respectively, and ursodesoxycholic acid (0.2, 0.3, 0.4, 0.5, and 0.7 mg/mL) could significantly increase the P_app of baicalin in 1.19-, 2.25-, 1.24-, 0.35-, and 0.68-folds, respectively compared with the control group (P < 0.01). Conclusion Borneol and ursodesoxycholic acid (0.2, 0.3, 0.4, 0.5, and 0.7 mg/mL) could significantly increase the P_app of baicalin without stimulation on rabbit cornea.