摘要
目的通过18名健康志愿者，研究利巴韦林分散片的药动学和生物等效性。方法HPLC（C18,150mm×4．6mm，5μm，紫外检测器，波长215nm）测定血浆中提取的药物，流动相为0．01mol·L^-1磷酸二氢铵和磷酸，流速1．5mL·min^-1。18名健康志愿者单次口服利巴韦林分散片或利巴韦林普通片600mg，采用随机自身交叉试验方法，测定药动学参数和相对生物利用度。结果标准曲线线性范围0．05—1．60mg·L^-1，最低检测限0．05mg·L^-1。利巴韦林质量浓度为0．1、0．4、1．6mg·L^-1时平均回收率分别为102．5％、101．7％和101．9％，日内RSD、日间RSD分别为（3．9±1．4）％和（3．1±2．4）％，药-时曲线显示两制剂符合二室模型。利巴韦林分散片和普通片的主要药动学参数如下：t1／2β（28．36±3．12）和（28．71±2．95）h，tmax（1．24±0．33）和（1．28±0．31）h，ρmax（0．651±0．127）和（0．654±0．081）mg·L^-1，AUC0→72h（13．22±2．28）和（13．23±2．09）mg·h·L^-1，两剂型主要药动学参数差异无显著性意义（P〉0．05）；利巴韦林分散片相对生物利用度为（100．65±13．85）％。结论利巴韦林分散片与普通片生物等效。
AIM To study the bioequivalence and pharmacokinetics of ribavirin dispersible tablet in 18 healthy vol- unteers. METHODS The drug was extracted from plasma,and then analyzed by HPLC with a C18 column（150 mm×4.6 mm,5 μm）and UV detector set at 215 nm.Monoammonium phosphate and phosphoric acid were used as the mobile phase. The flow rate was 1.5 mL· min^-1.600 mg single oral dose of dispersible tablet and conventional tablet were given to 18 healthy volunteers in an open randomized crossover study, The pharmacokinetic parameters as well as relative bioavailability were measured. RESULTS The calibration curve was linear within the range of 0,05 - 1.60 mg· L^-1 and the measurable lowest limit was 0.05 mg· L^-1. The average recovery of ribavirin at the concentrations of 0.1,0.4,1,6 mg· L^-1 were 102,5% ,101.7%and 101.9% ,respectively.The average RSD of within-day and between-day were（3.9 ± 1.4） % and （3.1 ± 2.4） %, respectively. The results showed that the concentration-time curves of the two preparations were fitted to a two-compartment model. The major pharmacokinetic parameters of dispersible tablet and conventional tablet were as follows： t1/2β was（28.36 ± 3.12）h and（28.71 ± 2.95）h; tmax Was（ 1.24 ± 0.33）h and（ 1.28 ± 0.31）h; ρmax Was（0,651 ± 0. 127） mg· L^-1 and （0.654 ± 0.081） mg· L^-1, AUC0→72 h were（ 13.22 ± 2.28）mg·h·L^-1 and（ 13.23 ± 2.09） mg·h·L^-1.There were no significant differences between the main pharmacokinetic parmeters of the two preparations （ P 〉 0.05）. The relative bioavailability of dispersible tablet was（ 100.65 ± 13.85） %. CONCLUSION The result of the statistical analysis shows that the two preparations are bioequivalent.
出处
《中国临床药学杂志》
CAS
2006年第1期14-17,共4页
Chinese Journal of Clinical Pharmacy
关键词
利巴韦林
分散片
药动学
生物等效性
ribavirin
dispersible tablets
bioequivalence
pharmacokinetics
