目的 研究沙格列汀片在精神分裂症合并2型糖尿病患者中多次给药后的药动药效学。方法 10例精神分裂症合并2型糖尿病男性住院患者口服沙格列汀片5 mq qd 7 d,在第7天采集12 h内动态血标本,采用HPLC-MS/MS测定血浆中沙格列汀的浓度,同时测定全血样本中血糖水平,并用DAS3.2.4软件对试验数据进行处理,计算药动学参数。结果 多次口服沙格列汀片5 mg qd的主要药动学参数ρmax为(16.27±9.28)μg·L-1,tmax为(1.70±0.48) h,t1/2为(3.33±0.59) h,AUC0-12为(45.19±18.67) μg·h·L-1,AUC0-∞为(49.15±19.71) μg·h·L-1。沙格列汀的血药浓度与血糖水平无特异相关性。结论 沙格列汀应用于精神分裂症合并2型糖尿病患者药动学特征在正常范围内,安全性较好,对于部分血糖波动较大的患者控制血糖能力一般。
Abstract
OBJECTIVE To investigate the pharmacokinetics and pharmacodynamics of saxagliptin tablets in Chinese schizophrenia patients complicated with T2DM. METHODS Ten male schizophrenia patients complicated with T2DM were enrolled. The protocol was to afford multi-dose of 5 mg qd for 7 d. The blood samples were collected up to 12 h after the oral administration. The plasma concentrations of saxagliptin were determined by a validated HPLC-MS/MS method. The levels of blood glucose were also measured. The pharmacokinetic parameters were calculated by DAS 3.2.4 software.RESULTS The main pharmacokinetic parameters of saxagliptin after multi-dose of 5 mg qd were as follows: ρmax was (16.27±9.28) μg·L-1, tmax was (1.70±0.48) h, t1/2 was (3.33±0.59) h, AUC0-12 was (45.19±18.67) μg·h·L-1, AUC0-∞ was (49.15±19.71) μg·h·L-1, respectively. No significant correlation of plasma concentration and blood glucose was observed. CONCLUSION The main pharmacokinetic parameters of saxagliptin are in the normal range among Chinese schizophrenia patients complicated with T2DM. The clinical use of the drug is generally safe, while the control of blood glucose was not effective enough for patients with great fluctuation.
关键词
沙格列汀 /
精神分裂症 /
2型糖尿病 /
药动学 /
血糖
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Key words
saxagliptin /
schizophrenia /
T2DM /
pharmacokinetics /
blood glucose
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中图分类号:
R969.1
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参考文献
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脚注
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基金
广东省药学会医院药学研究基金(2012C01);广州市医药卫生科技项目(20141A010037)
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