摘要
目的研究美索巴莫胶囊(肌松药)在健康人体的药代动力学及其生物等效性。方法按两制剂双周期自身对照交叉试验设计,18名男性健康志愿者分别单剂量口服2种国产美索巴莫胶囊(参比制剂)和(受试制剂),用RP-HPLC法测定血药浓度,计算药代动力学参数,并评价2制剂的生物等效性。结果口服美索巴莫胶囊参比制剂和受试制剂750mg后的主要药代动力学参数:Cmax分别为(13.87±2.44)和(14.34±2.99)μg.mL-1;tmax分别为(0.82±0.21)和(0.80±0.23)h;AUC0-12分别为(32.79±10.03)和(33.90±8.40)μg.h.mL-1;AUC0-∞分别为(33.91±9.89)和(35.00±8.79)μg.mL-1;t1/2Ke分别为(1.91±0.58)和(1.79±0.59)h;美索巴莫的相对生物利用度F0-12平均为(105.0±11.2)%,F0-∞平均为(104.3±10.2)%。结论2种美索巴莫胶囊制剂生物等效。
Objective To study the pharmacokinetics and bioequivalence of methocarbamol capsule in healthy volunteers. Methods A single dose 750 mg of reference and test methocarbamol capsules was given to 18 healthy volunteers in randomized 2 - way cross - over study. The pharmacokinetics as well as relative bioavailability was measured by RP -HPLC. Results The main pharmacokinetic paranceters of the reference and test capsules were as follow ： Cmax were （ 13.87 ± 2.44 ） and （14.34±2.99）μg ·mL^-1;tmax were （0.82 ±0.21） and （0.80± 0.23） h;AUC（0-12） were （32.79 ± 10.03） and （-33.90 ± 8.40） μg·h ·mL^-1;AUC（0-∞） were（33.91 ± 9. 89 ） and （ 35. 00 ±8.79） μg ·h· mL^-1;t（1/2Ke）were （1.91 ±0.58） and （1.79 ±0.59） h. The relative bioavailability of AUC（0-12） was （ 105.0 ± 11.2 ）% and AUC（0-∞） was （ 104.3 ± 10.2 ） %, respectively. Conclusion The reference and test methocarbamol capsules were bioequivalence.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
2007年第5期365-368,共4页
The Chinese Journal of Clinical Pharmacology
