阿立哌唑长效注射混悬剂的制备及药动学

doi:10.3969/j.issn.1000-1565.2018.06.009

河北大学学报(自然科学版) ›› 2018, Vol. 38 ›› Issue (6): 610-616.DOI: 10.3969/j.issn.1000-1565.2018.06.009

阿立哌唑长效注射混悬剂的制备及药动学

李心,刘浩帆,杨晗,赵娜,张东浩,胡连栋

收稿日期:2018-02-25 出版日期:2018-11-25 发布日期:2018-11-25
通讯作者: 胡连栋(1978—),男,河北石家庄人,河北大学教授,博士,主要从事药物新制剂研究.E-mail:hbupharm@126.com
作者简介:李心(1994—),男,河北保定人,河北大学在读硕士研究生. E-mail: 2450372784@qq.com
基金资助:
国家自然科学基金资助项目(21878065);河北省青年拔尖人才项目;河北省高等学校科学研究项目(ZD2016136)

Preparation and pharmacokinetics of aripiprazole long-acting injectable suspension

LI Xin,LIU Haofan,YANG Han,ZHAO Na,ZHANG Donghao,HU Liandong

Key Laboratory of Pharmaceutical Quality Control of Hebei Province, College of Pharmacy, Hebei University, Baoding 071002, China

Received:2018-02-25 Online:2018-11-25 Published:2018-11-25

摘要/Abstract

摘要： 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15 d. 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.

关键词: 精神分裂, 阿立哌唑, 长效混悬剂, 肌注, 药动学

Abstract: 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.

Key words: schizophrenia, aripiprazole, long-acting suspension, intramuscular injection, pharmacokinetics

中图分类号:

O643

李心,刘浩帆,杨晗,赵娜,张东浩,胡连栋. 阿立哌唑长效注射混悬剂的制备及药动学[J]. 河北大学学报(自然科学版), 2018, 38(6): 610-616.

LI Xin,LIU Haofan,YANG Han,ZHAO Na,ZHANG Donghao,HU Liandong. Preparation and pharmacokinetics of aripiprazole long-acting injectable suspension[J]. Journal of Hebei University (Natural Science Edition), 2018, 38(6): 610-616.

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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

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