摘要
目的 评价国产西尼地平胶囊与国产上市西尼地平片剂在中国健康人体内的生物等效性。 方法 入选20名男性健康志愿者，随机交叉单剂量口服西尼地平胶囊或西尼地平片剂10 mg，液质联用测定血浆中西尼地平浓度。结果 西尼地平胶囊及片剂的药动学参数分别如下：ρmax分别为（11.08±4.42）和（2.94±3.44）μg·L-1；tmax分别为（1.30±0.56）和（2.21±1.25）h；t1/2 分别为（3.99±1.90）和（4.55±1.75）h，AUC0-t分别为（35.28±14.63）和（13.22±12.44）μg·h·L-1，AUC0-∞分别为（38.05±16.49）和（15.43±13.59）μg·h·L-1。2种制剂的ρmax、tmax、AUC0-t、AUC0-∞均存在显著差异（P＜0.01）。结论 国产西尼地平胶囊与国产上市西尼地平片剂生物不等效。
Abstract
OBJECTIVE To evaluate the bioequivalence of domestic cilnidipine capsules and commercially available cilnidipine tablets in healthy Chinese volunteers. METHODS Twenty healthy male Chinese volunteers were enrolled and orally administrated 10 mg cilnidipine capsules or tablets randomly and the concentrations of cilnidipine in plasma were determined by HPLC-MS/MS. RESULTS The pharmacokinetic parameters of two cilnidipine productions were as following： ρmax（11.08±4.42）and（2.94±3.44）μg·L-1， tmax（1.30±0.56）and（2.21±1.25）h， t1/2 (3.99±1.90) and (4.55±1.75) h，AUC0-16 h (35.28±14.63) and (13.22±12.44) μg·h·L-1，AUC0-∞(38.05±16.49) and (15.43±13.59) μg·h·L-1，respectively. There were significant differences in ρmax, tmax, AUC0-t and AUC0-∞ between the two formulations. CONCLUSION The domestic cilnidipine capsules were not bioequivalent to the marketed cilnidipine tablets in China.
关键词
西尼地平 /
药动学 /
生物等效性
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Key words
cilnidipine /
pharmacokinetics /
bioequivalence
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李晓光 赵荣生 张现化 佘飞 翟所迪 陈凤荣 李海燕.
两种西尼地平制剂在中国健康志愿者体内的生物等效性[J]. 中国药学杂志, 2010, 45(5): 381-384
Bioequivalence of Two Cilnidipine Formulations in Healthy Chinese Volunteers[J]. Chinese Pharmaceutical Journal, 2010, 45(5): 381-384
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参考文献
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