论文部分内容阅读
目的通过超声波技术制备多奈哌齐缓释微球。方法应用超声波装置制备多奈哌齐缓释微球,进行载药量、粒径、体外释放实验等体外评价,并用LC-MS/MS研究多奈哌齐微球家兔体内的药动学。结果应用超声波装置制备多奈哌齐缓释微球,载药量为12.1%,粒径分布在40~130μm,体外可累计释药一个月,经家兔皮下单剂量30.0 mg·kg-1注射给药,主要药动学参数为:ρmax=40.63μg·L-1,t max=2.47 d,MRT=14.81 d,AUC0→∞=646.96μg·d·L-1。结论应用超声波技术成功制备具有明显缓释特性的多奈哌齐微球。
Objective To prepare donepezil sustained-release microspheres by ultrasonic technique. Methods Donepezil sustained-release microspheres were prepared by ultrasonic device. The drug loading, particle size and release in vitro were evaluated in vitro. The pharmacokinetics of donepezil microspheres was studied by LC-MS / MS. Results Donepezil sustained-release microspheres were prepared by using ultrasonic device with a drug loading of 12.1% and a particle size distribution of 40 ~ 130μm. The drug release was cumulatively released in vitro for one month. After a single subcutaneous dose of 30.0 mg · kg-1, The main pharmacokinetic parameters were ρmax = 40.63μg · L-1, tmax = 2.47d, MRT = 14.81d, AUC0 → ∞ = 646.96μg · d · L-1. Conclusions Donepezil microspheres with obvious sustained-release properties were prepared successfully by using ultrasonic technique.