目的 研究冰片、熊去氧膽酸對(duì)黃芩苷離體角膜透過(guò)率的影響，探討其在眼用制劑中的應(yīng)用。方法 采用離體角膜滲透技術(shù)考察不同質(zhì)量濃度的冰片、熊去氧膽酸對(duì)黃芩苷角膜透過(guò)率的影響。結(jié)果 0.2 mg/mL的冰片使黃芩苷表觀滲透系數(shù)（P_app）增加了1.36倍，與對(duì)照組相比具有顯著性差異（P＜0.05）；0.3、0.4、0.5、0.7 mg/mL的冰片使黃芩苷P_app分別增加了1.35、1.43、1.51、3.47倍，0.2、0.3、0.4、0.5、0.7 mg/mL的熊去氧膽酸使黃芩苷P_app分別增加了1.19、2.25、1.24、0.35、0.68倍，與對(duì)照組相比均具有非常顯著性差異（P＜0.01）。結(jié)論 0.2、0.3、0.4、0.5、0.7 mg/mL的冰片、熊去氧膽酸能夠顯著增大黃芩苷的P_app，且對(duì)角膜無(wú)刺激性。

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.

國(guó)家自然科學(xué)基金資助項(xiàng)目（81001645）；中國(guó)博士后科學(xué)基金（20090460701）；天津市自然科學(xué)基金項(xiàng)目（12JCYBJC18700）