论文部分内容阅读
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 vitamin A palmitate (VAP) cationic liposome-in situ gels (TMC60-VAPL-ISG group) coated with N-trimethylchitosan (TMC60) with commercial VAP gels Pei group) in rabbits aqueous humor pharmacokinetics. Methods: By using self-control, the VAP concentration in aqueous humor of rabbits at different time points was determined by HPLC after dripping with two kinds of preparations. The pharmacokinetic parameters were obtained by fitting with 3P97 software. Results: The drug concentration in aqueous humor in TMC60-VAPL-ISG group at each time point was significantly higher than that in Nano-Pei group after 0.25 h administration, and the area under the aqueous humor concentration-time curve (AUC0-24) (P <0.05). Conclusion: TMC60-VAPL-ISG can significantly prolong drug retention in the eye, increase the concentration of drug in aqueous humor and significantly improve the ocular bioavailability of VAP.