合成冰片对地塞米松角膜渗透性的影响

Effect of synthetic borneol on transcorneal permeability of dexamethasone

目的:研究合成冰片对地塞米松的角膜通透作用的影响,并评估其眼部刺激性。方法:采用完整及去上皮离体角膜进行兔体外扩散实验,供给池中分别加入不含冰片和含合成冰片的地塞米松滴眼液,用高效液相色谱仪测定接受池中不同时间点样品中地塞米松的含量,计算表观渗透系数。测定完整角膜的角膜水化值。观察合成冰片点眼对角膜的刺激性。结果:与对照组相比,合成冰片使地塞米松在完整角膜的表观渗透系数增加2.40倍,差异有统计学意义(P<0.05),合成冰片不能显著增加地塞米松在去上皮角膜的表观渗透系数,差异无统计学意义(P>0.05)。角膜水化值及刺激性试验表明,合成冰片不会明显增加角膜水化值及白兔眨眼次数,差异无统计学意义(P>0.05)。结论:合成冰片能够提高脂溶性药物地塞米松的角膜通透性,无明显角膜刺激性。

·AIM： To study the effect of synthetic borneol on transcorneal permeability of dexamethasone. The ocular irritation was also evaluated. ·METHODS：The freshly excised corneas,whole corneas or de-epithelialized corneas, were immediately mounted in perfusion cells. Dexamethasone containing free -borneol or borneol was added into the deliver chamber respectively in each group. At different time point after addition of solution, 50μL of the receptor solution was removed. The concentration of dexamethasone was determined and the apparent＆amp;nbsp;permeability coefficient （ Papp ） was calculated. Hydration level of cornea was measured and irritation test was observed. ·RESULTS： The Papp for dexamethasone in whole cornea increased by 2. 40 fold in borneol group （ P〈0. 05）. The Papp for dexamethasone in de-epithelialized cornea did not increased apparently （P〉0. 05）. Synthetic borneol did not increase hydration level and irritation of cornea（P〉0. 05）. ·CONCLUSION： Synthetic borneol can improve the corneal permeation of lipophilic drug dexamethasone and do not damage corneal tissue.