Comparative Pharmacokinetic Analysis of а Novel Prolonged Release Dosage Form of Lithium Citrate in Mice

A. Kotlyarova, A. Letyagin, T. Tolstikova, L. N. Rachkovskaya, T. Popova
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Abstract

This study assessed the comparative pharmacokinetics of a novel prolonged release dosage form of lithium citrate in white outbred mature mice – males after single intragastrically administration. In the experiment mice were divided into two groups (8-10 animals each group) which were received lithium citrate (LC) (75 mg/kg) or complex based on lithium citrate, aluminum oxide and organosilicone polymer (LCAS) (1120 mg/kg) once intragastrically. These doses were calculated based on lithium containing at the ratio 5,6 mg/kg. Pharmacokinetic parameters and relative bioavailability were calculated based on lithium ions concentration in serum and brain, which was measured by inductively-coupled plasma atomic emission spectrometry (ICP-AES). According to received pharmacological data of LCAS the Cmax of lithium ions in serum is lower by 4,3 times, than if administration of LC, relative bioavailability of LCAS is 44.41% of standard LC. Performed research has proven that combining aluminium oxide and organosilicone polymer as supportive components with lithium citrate helps to maintaining a stable lithium ions concentration in blood and brain which is important for achieving positive lithium therapy effect.
柠檬酸锂新型缓释剂型在小鼠体内的比较药动学分析
本研究评估了一种新型延长释放剂量的枸橼酸锂单次灌胃给药给药后在纯种成熟雄性小鼠体内的比较药代动力学。实验小鼠分为两组(每组8 ~ 10只),分别灌胃枸橼酸锂(LC) (75 mg/kg)或枸橼酸锂-氧化铝-有机硅聚合物复合物(LCAS) (1120 mg/kg) 1次。这些剂量是根据含锂比例5,6 mg/kg计算的。采用电感耦合等离子体原子发射光谱法(ICP-AES)测定血清和脑内锂离子浓度,计算药代动力学参数和相对生物利用度。根据收到的药理学资料,LCAS的血清中锂离子的Cmax比给药时降低了4,3倍,相对生物利用度为标准LC的44.41%。已有研究证明,将氧化铝和有机硅聚合物作为支持成分与柠檬酸锂结合,有助于维持血液和大脑中稳定的锂离子浓度,这对实现积极的锂治疗效果很重要。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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