布南色林片在中国健康志愿者体内的药代动力学

倪晓佳; 胡海棠; 张明; 胡晋卿; 尚德为; 温预关

doi:10.11665/j.issn.1000-5048.20130610

布南色林片在中国健康志愿者体内的药代动力学

1.
广州市脑科医院国家药物临床试验机构
2.
丽珠医药集团股份有限公司

基金项目: 国家临床重点专科资助项目(No.201201007)和广东省重大科技专项资助项目(No.2011A080300003,No.2012A080204017)

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- 刊出日期: 2013-12-24

Pharmacokinetics of blonanserin tablets in Chinese healthy volunteers

摘要

摘要: 为了研究布南色林片单次给药后的中国健康志愿者体内的药代动力学，30例健康志愿者单次口服4 mg、8 mg和12 mg布南色林片后，采集60 h内动态血标本，采用LC-MS/MS测定血浆中布南色林的浓度，并用DAS 3.2.4软件对试验数据进行处理，计算药代动力学参数。单次口服4 mg、8 mg和12 mg布南色林片的主要药代动力学参数c_max分别为(539.61±388.74)、(1 190.39±736.51)和(1 637.34±481.45)ng/L，t_max分别为(1.00±0.47)、(1.38±0.79)和(1.43±0.94)h，t_1/2分别为(12.05±3.49)、(14.76±3.78)和(13.68±3.92)h，AUC_{0-60 h}分别为(4 692.21±3 041.75)、(7 964.42±3 988.07)和(9 648.22±2 565.07)ng·h/L，AUC_0-∞分别为(5 060.91±3 146.10)、(8 547.61±4 209.87)和(9 986.15±2 659.51)ng·h/L。可见，在4~12 mg给药剂量范围内，布南色林片的主要药代动力学参数的c_max、AUC_{0-60 h}、AUC_0-∞与剂量呈正相关。
- 布南色林 /
- 片剂 /
- LC-MS/MS /
- 药代动力学
Abstract: To study the pharmacokinetics of blonanserin tablets in thirty Chinese healthy volunteers grouped into three single-dose levels of 4, 8 and 12 mg. The blood samples were collected up to 60 h after oral administration. The plasma concentration of blonanserin was determined by a validated LC-MS/MS method. The pharmacokinetic parameters were calculated by DAS 3. 2. 4 software. The main pharmacokinetic parameters of blonanserin after the single dose of 4, 8 and 12 mg were as follows: c_max were(539. 61±388. 74), (1 190. 39±736. 51)and(1 637. 34±481. 45)ng/L; t_max were(1. 00±0. 47), (1. 38 ±0. 79)and(1. 43±0. 94)h; t_1/2 were(12. 05±3. 49), (14. 76±3. 78)and(13. 68±3. 92)h; AUC_{0-60 h} were(4 692. 21±3 041. 75), (7 964. 42±3 988. 07)and(9 648. 22±2 565. 07)ng ·h/L; AUC_0-∞ were(5 060. 91±3 146. 10), (8 547. 61±4 209. 87)and(9 986. 15±2 659. 51)ng ·h/L, respectively. The main pharmacokinetic parameters of blonanserin positively correlated with the dose over the range of 4-12 mg.
- blonanserin /
- tablet /
- LC-MS/MS /
- pharmacokinetics

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参考文献(4)

[1]	Chang MH,Li YH.A new antipsychotic agent:blonanserin[J].Chin J New Drugs Clin Rem(中国新药与临床杂志),2010(29):571-575.
[2]	Wen YG,Ni XJ,Zhang M,et al.Simultaneous determination of blonanserin and its metabolite in human plasma and urine by liquid chromatography-tandem mass spectrometry:application to a pharmacokinetic study[J].J Chromatogr B Analyt Technol Biomed Life Sci,2012,903(15):46-52.
[3]	Suzuki H,Gen K.The relationship between the plasma concentration of blonanserin,and its plasma anti-serotonin 5-HT(2A)activity/anti-dopamine D₂ activity ratio and drug-induced extrapyramidal symptoms[J].Psychiatry Clin Neurosci,2012,66(2):146-152.
[4]	Saruwatari J,Yasui-Furukori N,Inoue Y,et al.Effect of dose timing in relation to food intake on systemic exposure to blonanserin[J].Eur J Clin Pharmacol,2010,66(9):899-902.

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布南色林片在中国健康志愿者体内的药代动力学

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Pharmacokinetics of blonanserin tablets in Chinese healthy volunteers

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