司帕沙星眼用pH敏感原位凝胶的制备及体外角膜透过性考察

摘要目的制备司帕沙星眼用pH敏感原位凝胶（SF ISG），并考察其体外角膜透过性。方法以0.3%卡波姆与14%泊洛沙姆为基质，制备SF ISG；测定其黏度；以同浓度司帕沙星滴眼液为对照，进行家兔眼滞留性研究，并利用Franz扩散池对其体外角膜透过性进行考察。结果SF ISG具有假塑性流体特性，黏度随着pH的增加而迅速增大；与SF滴眼液相比，可显著延长兔眼滞留性，并显著提高对体外角膜的透过量（P＜0.05）。结论SF ISG具有明显的pH敏感性、眼部滞留性及促进角膜透过性，值得进一步研究。

Preparation of Sparfloxacin pH-Sensitive in-situ Ophthalmic Gel and Its Corneal Penetration in Vitro

Objective To prepare sparfloxacin(SF) pH-sensitive in-situ ophthalmic gel(ISG) and study the corneal penetration in vitro.Methods 0.3% carbopol and 14% poloxamer was applied as gel base to prepare the SF-ISG.The viscosity of the gel was determined.SF eye-drops at the same concentration served as control.Retention capability and corneal penetration of SF-ISG were studied in vitro.Results The SF-ISG had the property of pseudoplastic fluid and the viscosity increased significantly with the increase of pH value.Compared with the SF eye-drops,the gel could significantly enhance the retention capability and corneal penetration in vitro(P<0.05).Conclusion The SF-ISG with promising pH-sensitivity,retention capability and corneal penetration in vitro is valuable to be studied further.