溴吡斯的明纳米乳的体外释放及体内动力学研究

Preliminary research on drug release in vitro and pharmacokinetics in vivo of pyridostigmine bromide nanoemulsion

目的:对溴吡斯的明纳米乳(pyridostigmine bromide nanoemulsion,PBNE)在体外的释放行为和体内的药动学行为进行初步研究。方法:建立高效液相色谱法考察体外释放行为和体内药动学行为。结果:PNBE与溴吡斯的明(pyridostigmine bromide,PB)在4种释放介质(pH1.2的盐酸溶液,pH6.8、pH7.4、pH7.8的磷酸缓冲溶液)中的体外释放行为相似,PBNE的MRT(0-24 h)值较PB增加0.98 h,PBNE的Cmax值是PB的1.55倍,PBNE的口服生物利用度是PB的1.82倍。结论:PBNE在不同介质中的体外释药行为相似,PBNE可改变体内的药动学行为,其口服生物利用度比PB好,PBNE具有一定的缓释作用。

Objective ：To explore the drug release behaviors in vitro and pharmacokinetics in vivo of pyridostigmine bromide na- noemulsion（PBNE）. Methods：The high performance liquid chromatography was established to investigate the release behaviors in vitro and pharmacokinetic behaivors in vivo. Results：The release behaviors of PBNE in 4 media（pH1.2 HCl,pH6.8 PBS, pH7.4 PBS, pH7.8 PBS） was similar to those of pyridostigmine bromide（PB）. The MRT（0-24h）〉 of PBNE increased by 0.98 h than PB;the Cmax of PBNE was 1.55 times that of PB ; the oral bioavailability of PBNE was 1.82 times that of PB. Conclusion ： The release behaviors of PBNE in different release medium are similar in vitro. PBNE can change the pharmacokinetic behaviors in vivo;the oral bioavailability of PBNE is higher than PB and PBNE has a sustained-release effect in vivo.