| HPLC法测定人唾液中卡马西平浓度及其药代动力学
| | 免费小论文 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 mL・min-1, detection wavelength was 212 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 mg・L-1 for CBZ. The limit of detection in saliva was 30 μg・L-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) mg・L-1, (0.0090±0.0006) h-1, (77.16±5.26) h and (132.18±8.82) mg ・h・L-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】 目的免费小论文： 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 mL・min-1,检测波长为212 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免费小论文药代动力学参数. 结果： 本测定方法线形范围为0.40~4.32 mg・L-1，相关系数r=0.999，最低检出浓度为30 μg・L-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) mg・L-1, (0.0090±0.0006) h-1, (77.16±5.26) h, (132.18±8.82) mg・h・L-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，吸收不规则，血药浓度治疗窗窄（4~12 mg・L-1）,容易引起毒副反应［1］. 为保证药品质量及临床疗效，把好临床合理用药关［2-4］，有必要对其进行血药浓度监测和个体化用药. 但血样采集常增加患者痛苦，且操作较繁琐［5］，尤其对于婴幼儿更为不便. 而唾液取样具有无创伤、经济简便、易于接受等优点. 为探讨用无创伤性生物制品取代血样的新途径，通过监测唾液中药物浓度,实现个体化用药,并在社区、家庭推广，取代传统的患者到医院门诊抽取血样的不方便模式，我们利用HPLC法测定卡马西平唾液浓度，并通过药代动力学研究，考察其适用性［6］.
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