阿立哌唑长效注射混悬剂的制备及药动学

Preparation and pharmacokinetics of aripiprazole long-acting injectable suspension

制备阿立哌唑长效注射制剂,并对其在家兔体内的药动学进行研究.用高压匀质法制得混悬剂,冷冻干燥后得成品;家兔大腿内侧肌注给药,高效液相法测定血药浓度.制得的长效注射混悬制剂粒径均匀稳定,对动物组织没有明显刺激性.体内药动学结果表明:阿立哌唑长效注射制剂在体内缓释效果良好,可持续释放15d.阿立哌唑长效注射制剂质量可控,可相对持续平稳地释放,有望为精神分裂病人提供一种方便、安全、有效的给药新剂型.

To prepare aripiprazole long-acting injectable suspension and study its pharmacokinetics in rabbits.Suspension was prepared by high-pressure homogenization and the product was obtained after freeze-drying;The concentration of drug in plasma was determined by high performance liquid chromatography.The long-acting injectable suspension formulation obtained was uniform and stable in particle size and had no significant irritation to animal tissues.The in vivo pharmacokinetics results showed that the long-acting injection has a good sustained-release effect in vivo and can be sustainedly released for 15 days.Aripiprazole long-acting injectable suspension have controllable quality and can be released continuously and steadily,which is expected to provide a convenient,safe and effective new dosage form for schizophrenic patients.