摘要
目的评价2种氨氯地平片剂在中国健康志愿者体内的生物等效性。方法24名健康男性受试者,随机分为2组,分别单剂量口服氨氯地平受试制剂或参比制剂10mg。14d清洗期后再交叉给药。于服药前(0h)和服药后2、4、6、8、10、14、24、36、48、72、96、120h抽取静脉血,采用LC-MS/MS法测定血浆中氨氯地平的浓度。利用DAS2.1.1软件计算主要药动学参数,并对2种制剂进行生物等效性评价。结果受试制剂和参比制剂的tmax分别为(6.7±s2.1)h和(6.8±1.8)h,ρmax分别为(7.0±1.3)μg·L-1和(7.3±1.8)μg·L-1,AUC0～120分别为(329±73)μg·h·L-1和(325±83)μg·h·L-1,AUC0～∞分别为(383±96)μg·h·L-1和(369±97)μg·h·L-1。受试制剂的相对生物利用度为(105±24)%。结论2种氨氯地平片剂在中国健康志愿者体内具有生物等效性。
AIM To evaluate the bioequivalence of two kinds of amlodipine tablets in Chinese healthy volunteers. METHODS The study was performed in 24 healthy male volunteers according to a randomized 2-way crossover design. The blood samples were collected at 0 h, and 2, 4, 6, 8, 10, 14, 24, 36, 48, 72, 96, 120 h after taking 10 mg of two kinds of amlodipine tablets （test and reference）, and with repeated sampling of the crossover drug administration 14 d after clearence. The concentration of amlodipine in plasma was determined by LC-MS/MS. Pharmacokinetic parameters were calculated and compared statistically to evaluate the bioequivalence between the two kinds tablets by DAS 2.1.1. RESULTS The major pharmacokinetic parameters of the test and reference tablets of amlodipine were as follows： （6.7 ± s 2.1） h and （6.8 ± 1.8） h for tmax, （7.0 ＋ 1.3） μg·L^-1 and （7.3 ± 1.8） μg·L^-1 for ρmax, （329 ± 73） μg·h·L^-1 and （325 ± 83）μg·h·L^-1 for AUC0-120, （383 ± 96）μg·h·L^-1 and （369 ± 97）μg·L^-1 for AUC0-∞, respectively. The relative bioavailability of test tablets was （ 105 ± 24）%. CONCLUSION Statistical analysis showed the two kinds of amlodipine tablets were bioequivalent in Chinese healthy volunteers.
出处
《中国新药与临床杂志》
CAS
CSCD
北大核心
2009年第8期599-603,共5页
Chinese Journal of New Drugs and Clinical Remedies
关键词
氨氯地平
色谱法
高压液相
光谱法
质量
电喷雾电离
药动学
生物等效性
amlodipine
chromatography, high pressure liquid
spectrometry, mass, electrospray ionization
pharmacokinetics
bioequivalence
