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目的制备苄达赖氨酸离子敏感型眼用原位凝胶(BDZL-ISG),对其流变学特征、体外释放性和离体角膜渗透性等进行评价,并研究药物在兔眼房水初步的药动学特征。方法利用黏度和胶凝能力对处方进行单因素考察,筛选出最优处方;以市售滴眼液或溶液剂为对照,采用透析膜法考察该处方的体外释放性;采用Franz扩散池对该处方进行离体角膜渗透研究。并采用微透析取样技术初步研究了药物在兔眼房水中的药动学特征。结果该处方具有剪切稀释特性,相比于对照组缓释效果明显;离体角膜渗透研究结果表明,该处方角膜累积渗透率与市售处方无显著性差异。房水药动学结果表明,苄达赖氨酸离子敏感型眼用原位凝胶组给药后ρ_(max)(13.25μg·L~(-1))为市售组的2.38倍,AUC0-t为市售组的2.2倍,眼部生物利用度显著提高。结论苄达赖氨酸离子敏感型眼用原位凝胶缓释效果明显,能有效提高药物的眼部生物利用度,有望成为治疗白内障的新剂型。
OBJECTIVE To prepare bendenyl lysine ion sensitive in situ gels (BDZL-ISG) for evaluation of rheological characteristics, in vitro release and in vitro corneal permeability, Preliminary pharmacokinetic characteristics. Methods The prescriptions were investigated by single factor method with viscosity and gelling ability, and the optimal prescriptions were screened out. The eyedrops solution or solution was used as a control, and the release of the prescription was investigated by dialysis membrane method. Prescription for corneal in vitro studies. The microdialysis sampling technique was used to study the pharmacokinetics of the drug in rabbit aqueous humor. Results The prescription has the characteristics of shear dilution, compared with the control group slow release effect obvious; ex vivo corneal penetration study results show that the prescription corneal cumulative permeability and commercial prescription no significant difference. Aqueous humor pharmacokinetics results showed that the ρ max (13.25 μg · L -1) of bendarysine ion sensitive ophthalmic otic gels group was 2.38 times that of the commercially available group, AUC0 -t 2.2 times that of the commercial group, significantly improving the bioavailability of the eye. CONCLUSION: The sustained-release effect of bendarysine ion sensitive in situ ophthalmic gel is obvious, which can effectively improve the ocular bioavailability of the drug and is expected to be a new dosage form for the treatment of cataract.