摘要
目的:比较N-三甲基壳聚糖(TMC60)包衣的维生素A棕榈酸酯(VAP)阳离子脂质体-原位凝胶(TMC60-VAPL-ISG组)与市售VAP凝胶(诺沛组)在兔眼房水的药物动力学。方法:采用自身对照,两种制剂滴用后,用HPLC法测定不同时间点的兔眼房水中的VAP浓度,用3P97软件拟合求得药动学参数。结果:用药0.25 h后,TMC60-VAPL-ISG组各时间点房水内药物浓度均明显高于诺沛组,房水药物浓度-时间曲线下面积(AUC0-24)也明显高于诺沛组(P<0.05)。结论:TMC60-VAPL-ISG可明显延长药物在眼部的滞留时间,增加房水中药物浓度,显著提高VAP的眼部生物利用度。
Objective ： To compare rabbit aqueous humor phannacokinetics of vitamin A palmitate （VAP） cationic liposomal in-situ gels coated by N-trimethyl chitosan （TMC60-VAPL-ISG） with that of the commercially available ophthalmic gels Nuopei. Method： Self-control study was applied. After administration of the two preparations, the rabbit aqueous humor concentrations of vitamin A pal- mitate at different time points were analyzed by HPLC, and the pharmacokinetic parameters were calculated by 3P97 program. Result： After 0.25 h of the administration, the aqueous drug concentrations at all time points in TMC60-VAPL-ISG group were significantly higher than those of the Nuopei group. The area under the curve（AUC0_24 ）was also significantly higher than that of the Nuopei group （P 〈 0.05 ）. Conclusion： TMC60-VAPL-ISG can significantly increase the drug penetration into rabbit aqueous humor, prolong the residence time and enhance the ocular bioavailability of VAP in the eyes.
出处
《中国药师》
CAS
2012年第6期767-770,共4页
China Pharmacist
