Mohanty Biswaranjan, Mishra Sagar Kumar, Majumdar Dipak K
Department of Pharmaceutics, Seemanta Institute of Pharmaceutical Sciences, Jharpokharia, Mayurbhanj, Orissa, India.
Department of Pharmaceutical Sciences, Utkal University, Bhubaneswar, Orissa, India.
J Adv Pharm Technol Res. 2013 Oct;4(4):210-6. doi: 10.4103/2231-4040.121416.
The purpose of this research was to evaluate the effect the formulation factors on in vitro permeation of voriconazole through freshly isolated goat and sheep corneas. An increase in the pH of the drops from 4.0 to 8.0 resulted in significant (P < 0.05) increase drug permeation. Raising concentration of the drops from 0.05% to 0.2% (w/v) significantly, (P < 0.05) increased drug permeation, but decreased the percent permeation. Corneal transport of voriconazole is both pH and concentration dependent. Eye drops containing disodium edetate (ethylenediaminetetraacetic acid) alone or combination with benzalkonium chloride showed significantly (P < 0.05) higher permeation as compared with control formulation. Addition of beta-cyclodextrin to the formulation enhanced corneal permeation of voriconazole. Compared with control formulation, voriconazole 0.2% (w/v) drop containing viscosity modifier produced significant (P < 0.05) decrease in permeation. Most of the formulations showed higher zone of inhibition against Candida albicans.
本研究的目的是评估制剂因素对伏立康唑通过新鲜分离的山羊和绵羊角膜的体外渗透作用的影响。滴眼液的pH值从4.0增加到8.0会导致药物渗透显著增加（P<0.05）。将滴眼液的浓度从0.05%提高到0.2%（w/v）可显著增加（P<0.05）药物渗透，但渗透百分比会降低。伏立康唑的角膜转运既依赖于pH值也依赖于浓度。与对照制剂相比，单独含有依地酸二钠（乙二胺四乙酸）或与苯扎氯铵联合使用的滴眼液显示出显著更高（P<0.05）的渗透率。向制剂中添加β-环糊精可增强伏立康唑的角膜渗透。与对照制剂相比，含有粘度调节剂的0.2%（w/v）伏立康唑滴眼液的渗透率显著降低（P<0.05）。大多数制剂对白色念珠菌显示出更高的抑菌圈。
