论文部分内容阅读
目的研究2种复方氯唑沙宗片在健康志愿者体内的生物等效性。方法 20例男性健康志愿者随机交叉口服2种复方氯唑沙宗(氯唑沙宗250 mg,对乙酰氨基酚300 mg)片,间隔为1 wk。以格列吡嗪和非那西丁为内标,用高效液相色谱质谱联用法测定氯唑沙宗和对乙酰氨基酚的血药浓度。结果 20名健康志愿者口服复方氯唑沙宗受试片和参比片后,其对乙酰氨基酚p~(max)分别为(5.1±1.5)和(5.2±1.7)mg·L~(-1);t~(max)分别为(0.6±0.4)和(0.6±0.4)h;t_(1/2)分别为(3.0±0.4)和(3.0±0.5)h;AUC_(0-12)分别为(16.4±4.7)和(17.0±5.5)mg·h·L~(-1);AUC0_(0-∞)分别为(17.6±5.1)和(18.2±6.0)mg·h·L~(-1)。氯唑沙宗p~(max)分别为(7.0±1.3)和(7.0±1.3)mg·L~(-1);t~(max)分别为(0.9±0.6)和(1.0±0.5)h;t1/2分别为(0.9±0.1)和(0.9±0.1)h;AUC_(0-10)分别为(16.6±3.5)和(17.0±4.1)mg·h·L~(-1);AUC_(0-∞)分别为(16.7±3.5)和(17.0±4.1)mg·h·L~(-1),2种片剂的药动学参数均无显著差异(P>0.05)。对乙酰氨基酚和氯唑沙宗2种成分的相对生物利用度分别为(99.3±14.3)%和(99.5±14.8)%。结论复方氯唑沙宗受试片与参比片在健康人体内具有生物等效性。
Objective To study the bioequivalence of two kinds of compound chlorzoxazone tablets in healthy volunteers. Methods Twenty healthy male volunteers were randomized to receive 2 doses of chlorzoxazone (250 mg of chlorzoxazone and 300 mg of paracetamol) at intervals of 1 wk. Glipizide and phenacetin as internal standard, high performance liquid chromatography-mass spectrometry determination of chlorzoxazone and acetaminophen blood concentration. Results 20 healthy volunteers received oral chlorzoxazone test and reference tablets with pmax of (5.1 ± 1.5) and (5.2 ± 1.7) mg · L -1 1; t max was 0.6 ± 0.4 and 0.6 ± 0.4 h, t 1/2 was 3.0 ± 0.4 and 3.0 ± 0.5 h, AUC 0-12, (16.4 ± 4.7) and (17.0 ± 5.5) mg · h · L -1, respectively. The AUC0_ (0-∞) were 17.6 ± 5.1 and 18.2 ± 6.0 mg · h · L ~ -1). The pmax of the zazofloxacin were (7.0 ± 1.3) and (7.0 ± 1.3) mg · L -1, respectively, and the t max were (0.9 ± 0.6) and (1.0 ± 0.5) h ; t1 / 2 were (0.9 ± 0.1) and (0.9 ± 0.1) h respectively; AUC 0-10 were (16.6 ± 3.5) and (17.0 ± 4.1) mg · h · L -1; (0-∞) were (16.7 ± 3.5) and (17.0 ± 4.1) mg · h · L -1, respectively. There was no significant difference in pharmacokinetic parameters between the two tablets (P> 0.05). The relative bioavailability of acetaminophen and chlorzoxazone were (99.3 ± 14.3)% and (99.5 ± 14.8)%, respectively. Conclusion The compound chlorzoxazone test and reference tablets are bioequivalent in healthy volunteers.