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

摘要:

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 bro－mide，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。

Abstract:

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（0-24 h） 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 bioavailabil－ity of PBNE is higher than PB and PBNE has a sustained-release effect in vivo.