摘要
目的:建立人血清中苯酰甲硝唑体内代谢产物--甲硝唑的反相高效液相色谱分析方法,比较苯酰甲硝唑分散片和苯酰甲硝唑胶囊生物等效性。方法:采用Eurosphex-100 C18柱,以乙腈-KH2PO4(0.01 mol·L-1)(22:78,v/v)为流动相,替硝唑作内标,紫外检测波长为318 nm,测定血清中甲硝唑的血药浓度。结果:血清中甲硝唑的浓度在0.1-20.0μg·ml-1范围内线性关系良好,r=0.999 9(n=8)。受试制剂及参比制剂的Cmax分别为(10.475±2.135)和(10.118±2.116),Tmax分别为(4.000±1.414)和(4.667±1.138)h,t1/2分别为(11.247±2.264)和(10.800±2.000)h,根据AUC0→t计算受试制剂的相对生物利用度为(100.9±20.2)%。结论:本方法操作简便、灵敏度高、重现性好,可用于血清中甲硝唑浓度的测定。苯酰甲硝唑分散片和苯酰甲硝唑胶囊具有生物等效性。
Objective: To develop a RP-HPLC method for the blood concentration of metrortidazole which was the metabolite of benzometronidazole and compare the bioequivalence between dispersible tablets and capsules of benzoylmetronidazole. Method: Euros- phex-100 Cl8 column was used,the mobile phase was constituted by acetonitrile -0.01 mol·L^-1 potassium dihydrogen phosphate buffer (22:78 ,v/v). The detection wavelength was 318 nm. Result: The standard curve was linear within a concentration range of 0. 1 - 20.0 μg·L^-1 with r= 0. 999 9 ( n = 8 ). The main pharmaeokinetic parameters Cmax,Tmax, t1/2 were ( 10. 475 ± 2. 135 ) μg· ml^-1, (4. 000 ± 1. 414) h and ( 11. 247 ± 2. 264 ) h for the reference tablets, also ( 10.118 ± 2.116 ) μg· ml^-1, ( 4.667 ± 1. 138 ) h and ( 10.800 ± 2. 000) h for the test tablets respectively, the relative bioavalability of the test tablets was ( 100.9 ± 20.2) %. Conclusion: This method is simple, sensitive, accurate and fine reproducible for determination of serum concentration in metronidazole. The results of statistical analysis demonstrated that the two preparations of benzoylmetronidazole are bioequivalent.
出处
《中国药师》
CAS
2006年第4期307-310,共4页
China Pharmacist