奥美拉唑肠溶胶囊人体相对生物利用度  

Determination of relative bioavailability of omeprazole enteric-coated capsules in healthy volunteers

作　　者：王平全[1] 安富荣[1] 刘振[2] 左明[2] 秦绮[2] 

机构地区：[1]上海第二医科大学仁济医院临床药理药学研究室,上海200001 [2]复旦大学医学院药物分析教研室,上海200032

出　　处：《中国医院药学杂志》2002年第8期453-456,共4页Chinese Journal of Hospital Pharmacy

摘　　要：目的 :建立测定奥美拉唑血药浓度的反相高效液相色谱法 ,并测定奥美拉唑肠溶胶囊的人体相对生物利用度。方法 :色谱柱 :DikmaDiamonsilC18(15 0mm× 4 .6mm ,5 μm) ;流动相 :醋酸铵缓冲液 (0 .1mol·L-1,pH 7.0 ) 乙腈 甲醇 (6 0∶35∶5 ,v/v) ;流速 :1.2ml·min-1;检测波长 :UV 30 2nm。以内标法定量 ,内标物为对羟基苯甲酸乙酯。进行人体随机交叉自身对照试验 ,血样以二氯甲烷一次提取 ,测定奥美拉唑肠溶胶囊的相对生物利用度。结果 :血药浓度测定的线性范围为 0 .0 0 4～ 5 .0μg·ml-1,回归方程为Y =3.0 2 18C - 0 .0 0 79(r =0 .9998,n =7) ,最低检测浓度为 2 .5ng·ml-1(S/N =3)。平均方法回收率为 10 2 .6 0 % ,日内、日间精密度均小于 5 %。结论 :方法简便 ,准确 ,灵敏 ,可用于奥美拉唑血药浓度的测定。两种制剂具有生物等效性 ,试验胶囊的相对生物利用度为 (10 0 .4± 13.8) %。OBJECTIVE A resersed phase high performance liquid chromatography (RP HPLC) was established to determine the concentration of omeprazole in human plasma in order to determination the relative bioavailability of omeprazole enteric coated capsules in healthy volunteers. METHODS Agilant 1100 instrument was used with the column of Dikma Diamonsil C 18 ( 150 mm × 4.6 mm , 5 μm ). The mobile phase was composed of NH 4Ac buffer ( 0.1 mol·L -1 , pH 7.0 ) acetonitrile methanol (60:35:5, v/v). Flow rate was 1.2 ml·min -1 . Detection wavelength was 302 nm. The plasma samples were extracted singly with 4.0 ml dichloromethane and ethyl P hydroxybenzoate was chosen as the internal standard. Select 28 healthy volunteers and sift out acceptance volunteers by determining their concentrations of omeprazole in plasma after they took orally omeprazole capsules 5 hours later, and select 20 volunteers to conduct the experiment of relative bioabailability. RESULTS The standard curve equation was Y = 3.0218 C - 0.0079 ( r = 0.9998 , n =7). The linear range was 0.004 ～ 5.0 μg·ml -1 . The minimum detection limit was 2.5 ng·ml -1 (S/N=3). The average recoveries rate were 102.60% . The intra day and inter day precisions were less than 5%. CONCLUSIONS The RP HPLC method is simple, rapid and sensitive. It is applicable to determine the concentrations of omeprazole in human plasma. The two formulations were of bioequivalence. The relative bioavailability of the test capsule was ( 100.37 ± 13.82 )%.

关 键 词：奥美拉唑肠溶胶囊 反相高效液相色谱法 血药浓度 生物利用度 药物代谢动力学 

分 类 号：R969.1[医药卫生—药理学] R927.1[医药卫生—药学]