hplc法测定人唾液中卡马西平浓度及其药代动力学
HPLC法测定人唾液中卡马西平浓度及其药代动力学
HPLC法测定人唾液中卡马西平浓度及其药代动力学
作者:唐哲,文爱东,吴寅,赵磊,李宏力,石茹【关键词】 卡马
西平 Determination of carbamazepine concentration in human saliva by HPLC and its pharmacokinetic study 【Abstract】
AIM: To determine carbamazepine(CBZ) concentration in human saliva by HPLC and study its pharmacokinetics. METHODS: Shimpack CLCODS C18 (150 mm×6 mm, 5 μm) spectrum analytical
column was used and methanolwater(53?47)was adopted as the mobile phase. Flow rate was 1.0 mLțmin-1, detection wavelength was 2 nm, column temperature was 23? and the dosage of CBZ was 50 μL. The pharmacokinetic parameters of CBZ tablets taken by 6 healthy volunteers at a single oral dose of 200 mg were calculated according to CBZ concentration in saliva. RESULTS: The standard curve was linear (r=0.999) within the range of 0.40~4.32 mgțL-1 for CBZ. The limit of detection in saliva was 30 μgțL-1 (S/N?3). The average recovery
was 99.17%-104.80%;the interday RSD and intraday RSD was
2.6%-4.9% and 3.0%-8.6% respectively.The results showed that the pharmacokinetics of CBZ was in accordance with the onecompartment open model. Tmax, Cmax, ke, T1/2 and AUC(0~inf) was (4.50?3.15) h, (1.52?0.22) mgțL-1, (0.0090?0.0006)
h-1, (77.16?5.26) h and (132.18?8.82) mg țhțL-1
respectively. After single dosing, the concentrationtime curve of CBZ in saliva presented multiple peaks. CONCLUSION: This method is simple, quick and specific, and can be used to determine CBZ concentration in human saliva and to study its pharmacokinetics. 【Keywords】 chromatography, high
pressure liquid; carbamazepine; saliva; pharmacokinetics 【摘要】 目的: 利用HPLC法测定人唾液中卡马西平浓度,并观察
其药代动力学特征. 方法: 采用Shimpack CLCODS C18色谱分析柱
(150 mm×6 mm, 5 μm),以甲醇水(53?47)为流动相,流速为1.0 mLțmin-1,检测波长为2 nm,柱温为室温,进样量50 μL. 根据唾液药物浓度求算6名健康受试者单剂量口服卡马西平片剂的药代动力学参数. 结果: 本测定方法线形范围为0.40~4.32 mgțL-1,相关系数r=0.999,最低检出浓度为30 μgțL-1 (按S/N?3计),方法平均回收率为99.17%-104.80%;日内RSD、日间RSD分别在2.6%-4.9%和3.0%-8.6%. 药动学参数表明,卡马西平人体内过程符合单室开放模型,Tmax, Cmax, ke, T1/2, AUC(0~inf)
分别为(4.50?3.15)h, (1.52?0.22) mgțL-1, (0.0090?0.0006) h-1, (77.16?5.26) h, (132.18?8.82)
mgțhțL-1. 单次给药后,CBZ唾液浓度时间曲线出现多峰现象. 结论: 该法简便、快速、专一性强,适用于卡马西平唾液药物浓度测定及药代动力学研究之用. 【关键词】 色谱法,高压液相;卡马西平;唾液;药代动力学 0引言 卡马西平
(carbamazepine, CBZ)是临床上常用的抗癫痫药. 由于此药的药代动力学个体差异大,吸收不
,血药浓度治疗窗窄(4~ mgțL-1),容易引起毒副反应. 我们采用蛋白沉淀法,较萃取法回收率高,操作简便快速、价廉,而且避免了有机试剂挥发给操作者带来的健康损害. 本实验建