桂利嗪
药代动力学
药理学
乳状液
分布(数学)
化学
体内
组织分布
分配量
药品
色谱法
麻醉
医学
生物化学
内科学
数学分析
数学
生物技术
生物
作者
Shuai Shi,Hao Chen,Lin Xia,Xing Tang
标识
DOI:10.1016/j.ijpharm.2009.09.025
摘要
The aim of this study was to assess the potential of cinnarizine loaded in lipid emulsion to modify the pharmacokinetics, tissue distribution and safety of cinnarizine. The cinnarizine-loaded emulsion (CLE) which can remain stable over 18-month storage at 4 ± 2 °C was prepared by high-pressure homogenization. Nicomp™ 380 particle sizing system and HPLC were used to evaluate CLE in vitro, while UPLC/MS/MS for pharmacokinetic and tissue distribution study. The pharmacokinetics and tissue distributions of CLE were assessed by comparing with the solution form after intravenous administration to rats at a dose of 2 mg/kg. The CLE showed significant higher AUC and lower clearance and distribution volume than those of solution form. This helped cinnarizine to reach higher level in vessel, and circulate in the blood stream for a longer time resulting in better therapeutic effect. The tissue distribution exhibited significant lower uptake of CLE emulsion in lung and brain, indicating the advantage of CLE over the solution form in reducing drug precipitation in vivo and toxicity in CNS. Drug safety assessment studies including hemolysis test, intravenous stimulation and injection anaphylaxis revealed that the CLE was safe for intravenous injection.
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