国产氯沙坦钾片在中国健康志愿者的药动学及生物等效性研究

方翼 关鑫 顾景凯 陈欣 王茜 李玉珍 管华诗

中国药学杂志 ›› 2010, Vol. 45 ›› Issue (20) : 1572-1576.

PDF(1113 KB)
PDF(1113 KB)
中国药学杂志 ›› 2010, Vol. 45 ›› Issue (20) : 1572-1576.
论 著

国产氯沙坦钾片在中国健康志愿者的药动学及生物等效性研究

  • 方翼1,2,关鑫3,顾景凯3,陈欣2,王茜2,李玉珍2 , 管华诗1*
作者信息 +

Pharmacokinetic and Relative Bioavailability of Losartan Potassium Tablet in Chinese Healthy Volunteers

  • FANG Yi1,2, GUAN Xin3, GU Jing-kai3, CHEN Xin2, WANG Qian2, LI Yu-zhen2, GUAN Hua-shi1
Author information +
文章历史 +

摘要

目的 评价国产氯沙坦钾片在健康人体的生物等效性。方法 纳入20例中国健康成年男性志愿者,随机分为两组,按自身前后对比双周期交叉给药,晨起空腹口服试验制剂或参比制剂50 mg。使用HPLC-MS/MS法检测单次空腹口服试验制剂与参比制剂后血浆中氯沙坦及其活性代谢产物E-3174的浓度。药代参数的计算与处理及生物等效性评价使用DAS 2.1.1统计分析软件。结果 试验制剂与参比制剂中,原型药物的ρmax分别为(207.50±68.14),(187.23±89.92)μg·L-1; tmax分别为(1.69±1.70 ),(1.53±0.76)h; AUC0-12 h分别为(457.79±126.46),(442.08±137.48) μg·h·L-1;t1/2分别为(2.09±0.59),(2.01±0.33) h。代谢产物E-3174的ρmax分别为(642.05±280.08),(659.91±295.72) μg·L-1 ;tmax分别为(4.10±1.86),(4.23±1.69) h;AUC0-12 h分别为(4 702.39±1 803.18),(4 703.28±1 959.33)μg·h·L-1;t1/2为(4.82±0.84),(5.13±1.94) h。结论 试验制剂和参比制剂中相应的原型药物和E-3174的主要药代参数差异无统计学意义,试验制剂与参比制剂生物等效。

Abstract

OBJECTIVE To evaluate the bioequivalence of test and reference losartan potassium tablets in healthy volunteers. METHODS A single oral dose of 50 mg test or reference preparation was administrated to 20 healthy volunteers in a randomized cross-over study. The concentration of losartan and E-3174 in human plasma were determined by HPLC-MS/MS. The pharmacokinetic parameters were calculated by DAS 2.1.1 analysis software. RESULTS For losartan test and reference formulations, the unchanged losartan ρmax were (207.50±68.14), (187.23±89.92) μg·L-1, tmax were (1.69±1.70), (1.53±0.76) h, AUC0-12 h were (457.79±126.46), (442.08±137.48) μg·h·L-1, t1/2 were (2.09±0.59), (2.01±0.33) h, respectively. ρmax of E-3174 were (642.05±280.08), (659.91±295.72)μg·L-1, tmax were (4.10±1.86), (4.23±1.69) h, AUC0-36 h were (4 702.39±1 803.18), (4 703.28±1 959.33)μg·h·L-1, t1/2 were (4.82±0.84), (5.13±1.94) h, respectively. CONCLUSION The analysis of variance showed no significant difference on the pharmacokinetic parameters. The test formulation was considered bioequivalent to the reference formulations.

关键词

氯沙坦 / E-3174 / 生物等效性 / 高效液相质谱联用法

Key words

losartan / E-3174 / bioequivalent / HPLC-MS/MS

引用本文

导出引用
方翼 关鑫 顾景凯 陈欣 王茜 李玉珍 管华诗. 国产氯沙坦钾片在中国健康志愿者的药动学及生物等效性研究[J]. 中国药学杂志, 2010, 45(20): 1572-1576
FNG Yi;GUN Xin;GU Jing-ki;CHEN Xin;WNG Qin;LI Yu-zhen;GUN Hu-shi. Pharmacokinetic and Relative Bioavailability of Losartan Potassium Tablet in Chinese Healthy Volunteers[J]. Chinese Pharmaceutical Journal, 2010, 45(20): 1572-1576

参考文献


[1] CHEN X Q, JIN Y Y, TANG G. New Edit Pharmacology (新编药物学)[M]. Vol 16. Beijing:People′s Medical Publishing House,2007: 53.
[2] KOYTCHEV R,OZALP Y,ERENMEMISOGLU A, et al. Combination of losartan and hydrochlorothiazide: In vivo bioequivalence[J]. Drug Res,2004, 54: 611-617.
[3] WEI Y, HUANG H F, SHAO Q X, et al. Relative bioavailability of losartan tablet in healty volunteers[J]. Chin J Clin Pharmacol (中国临床药理学杂志),2000,16(2):106-110.
[4] YUAN Y, LIU X L, GUO X, et al. Bioequivalence of losartan capsule in human volunteers [J]. Central South Pharmacy (中南药学),2007,5(5):467-470.
[5] MAN-WAI L, MICHEAL R G, JACQUELINE B M, et al. Pharmacokinetics of losartan, an angitensin II receptor antagonist, and its active metabolite EXP3174 in human [J]. Clin Pharmacol Ther, 1995, 58:641-649.
[6] YANG P, WANG Y J, LI L, et al. Bioequivalence of losartan capsule and tablet in healthy volunteers[J]. Chin J Clin Pharmacol (中国临床药理学杂志),2006,22(6):436-439.
PDF(1113 KB)

Accesses

Citation

Detail

段落导航
相关文章

/