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托伐普坦片在健康人体的生物等效性 被引量:7

Bioequivalence of tolvaptan tablets in healthy volunteers
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摘要 目的研究托伐普坦片的生物利用度,评价其生物等效性。方法用三周期自身交叉试验设计,36名健康男性受试者分别单剂量口服受试药物1,受试药物2或参比药物30 mg,用高效液相色谱-质谱法测定血浆中托伐普坦的浓度,用Phoenix WinNonlin 6.1计算药代动力学参数,并进行生物等效性评价。结果受试药物1,受试药物2和参比药物中托伐普坦的c max分别为(244.76±123.46),(241.30±90.36)和(244.92±108.52)μg·L-1,t max分别为(2.10±1.14),(2.15±1.26)和(1.96±0.87)h,t1/2分别为(8.52±3.77),(8.87±4.71)和(7.44±3.11)h;AUC0-tn分别为(1978.59±873.20),(1958.74±903.51)和(1835.98±643.02)μg·L-1·h。受试药物1的相对生物利用度F0-tn、F0-∞分别为(114.68±52.66)%和(114.65±52.43)%,受试药物2的相对生物利用度F0-tn、F0-∞分别为(112.22±53.35)%和(112.77±53.07)%。结论 2种受试药物和参比药物均具有生物等效性。 Objective To evaluate the bioequivalence of tolvaptan in healthy volunteers. Methods The blood concentrations of tolvaptan in 36 healthy male volunteers were determined by HPLCMS / MS after a single oral dose with a randomized crossover method. Results The main pharmaeokinetie parameters of the tolvaptan in the test 1,test 2 and reference preparation were as follows: c max were( 244. 76 ± 123. 46),( 241. 30 ±90. 36) and( 244. 92 ±108. 52) μg·L1; t max were( 2. 10 ± 1. 14),( 2. 15 ± 1. 26) and( 1. 96 ± 0. 87) h; t 1 /2 were( 8. 52 ± 3. 77),( 8. 87 ± 4. 71) and( 7. 44 ± 3. 11) h; AUC 0tn were( 1978. 59 ± 873. 20),( 1958. 74 ± 903. 51) and( 1835. 98 ± 643. 02) μg·L1·h; F 0tn,F 0∞ of test 1 preparation were( 114. 68 ± 52. 66) % and( 114. 65 ±52. 43) %,of test 2 preparation were( 112. 22 ± 53. 35) % and( 112. 77 ± 53. 07) %. Conclusion The test preparations were bioequivalent to the reference preparation.
出处 《中国临床药理学杂志》 CAS CSCD 北大核心 2013年第12期931-933,共3页 The Chinese Journal of Clinical Pharmacology
关键词 托伐普坦 高效液相色谱-质谱 生物等效性 tolvaptan HPLC-MS /MS biovequivalence
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