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目的:研究环孢素A-Eudragit S100纳米粒冻干粉制剂(freeze-dried cyclosporine A-Eudragit S100 nanoparticles,CyA-S100-NP)在家犬体内药动学及相对生物利用度。方法:以双周期交叉随机试验设计法,高效液相色谱法测定6只家犬口服给予环孢素A-Eudragit S100纳米粒冻干粉硬胶囊和新山地明微乳软胶囊(Neoral)后环孢素A的血药浓度,采用3P97软件计算药动学参数。结果:经3P97软件拟合,环孢素A的药动学过程符合二室模型。与Neoral相比,CyA-S100-NP的AUC显著增大(P<0.05),CL显著降低(P<0.05),相对生物利用度为135.9%。结论:CyA-S100-NP可促进药物口服吸收,显著提高环孢素A的生物利用度,有望开发成为一种新型口服环孢素A纳米粒固体制剂。
Objective: To study the pharmacokinetics and relative bioavailability of Cyclosporine A-Eudragit S100 nanoparticles (CyA-S100-NP) in dogs. METHODS: Six dogs were orally administered cyclosporine A-Eudragit S100 freeze-dried powder capsules and Neo-Sham-Ming soft capsule (Neoral) posterior ring by double-cycle randomized trial design and HPLC. Sporin A blood concentration, using 3P97 software to calculate pharmacokinetic parameters. Results: The 3P97 software fitting, cyclosporin A pharmacokinetic process in line with two-compartment model. Compared with Neoral, AUC of CyA-S100-NP was significantly increased (P <0.05), CL was significantly decreased (P <0.05), and relative bioavailability was 135.9%. Conclusion: CyA-S100-NP can promote oral absorption of drugs, significantly improve the bioavailability of cyclosporin A, is expected to develop into a new oral cyclosporin A nanoparticles solid preparation.