Wu Chun-jie, Huang Qin-wan, Qi Hong-yi, Guo Ping, Hou Shi-xiang
West China School of Pharmacy, Sichuan University, Chengdu, PR China.
Pharmazie. 2006 Sep;61(9):783-8.
Studies on the influence of borneol on the penetration of puerarin eye drops and timolol maleate eye drops through the cornea, and evaluation of the ocular irritability were conducted to provide a theoretical basis for the application of borneol in enhancing corneal permeability. The cornea penetrative experiment in vitro was conducted to observe the quantitative change of puerarin and timolol maleate penetrated through the cornea after administering different dosages of borneol. The corneal hydration level and blinking frequency were recorded as irritability indexes in vitro and in vivo. The steady-flow J of high, middle and low dosage groups of puerarin eye drops with borneol were increased by 49%, 32%, 5% respectively, and permeability parameter Kp increased by 49%, 32%, 5% respectively, as compared to that of the control group. The steady-flow J of high dosage group of timolol maleate eye drops with borneol was increased by 5%; middle and low dosage groups with borneol were decreased by 6%, 3% respectively. The permeability parameter Kp of high dosage group increased by 5%, while middle and low dosage groups with borneol were decreased by 6%, 3% respectively, as compared to that of the control group. Evaluation showed no ocular irritability caused by borneol. The results of this study suggest that the promoting effect of borneol on the permeability of drugs through the cornea in vitro is selective, which indicates that borneol has the potential to be used as an ophthalmic penetration enhancer.
研究冰片对葛根素滴眼液和马来酸噻吗洛尔滴眼液角膜透过性的影响,并评价其眼刺激性,为冰片在增强角膜通透性方面的应用提供理论依据。进行体外角膜透过实验,观察给予不同剂量冰片后葛根素和马来酸噻吗洛尔透过角膜的量的变化。记录角膜水化水平和眨眼频率作为体外和体内的刺激性指标。与对照组相比,含冰片的葛根素滴眼液高、中、低剂量组的稳态流量J分别增加了49%、32%、5%,渗透系数Kp分别增加了49%、32%、5%。含冰片的马来酸噻吗洛尔滴眼液高剂量组的稳态流量J增加了5%;含冰片的中、低剂量组分别降低了6%、3%。与对照组相比,含冰片的高剂量组渗透系数Kp增加了5%,而中、低剂量组分别降低了6%、3%。评价显示冰片未引起眼刺激性。本研究结果表明,冰片在体外对药物角膜通透性的促进作用具有选择性,这表明冰片有潜力用作眼部渗透促进剂。