苦参素片健康人体药动学及生物等效性研究

目的:研究苦参素片在健康人体内的药动学及生物等效性。方法:22名健康男性志愿者随机交叉单剂量口服苦参素片或胶囊0·3g,血样加入内标(西咪替丁)经预处理后采用高效液相色谱-质谱法测定药物浓度,检测离子为m/z265(苦参素)、m/z253(内标)。结果:苦参素片与胶囊的t1/2分别为(2·30±1·09)、(1·90±0·58)h;tmax分别为(1·86±0·74)、(1·68±0·55)h;Cmax分别为(525·09±208·94)、(530·32±202·04)ng/ml;AUC0~11分别为(2048·5±749·4)、(2042·0±743·0)(ng·h)/ml;AUC0~∞分别为(2163·2±783·1)、(2136·4±792·1)(ng·h)/ml;苦参素片的相对生物利用度为(101·06±9·41)%。结论:苦参素片与胶囊具有生物等效性。

Study on Pharmacokinetics and Bioequiavailability of Kushenin Tablets in Healthy Volunteers

OBJECTIVE: To study the endosomatic pharmacokinetics and bioequiavailability of kushenin tablets in health adults. METHODS: The blood concentrations of the blood samples taken from 22 healthy volunteers were determined by HPLC-MS after a single oral 0.3g kushenin (either tablet or capsule) dose and pretreatment with the internal standard (cimetidine) with m/z 265 (kushenin) taken as the detection ions and m/z 253 as the internal standard. RESULTS: The main pharmacokinetic parameters of the tablet and capsule of kushenin were as follows: t1/2 stood at (2.30±1.09)h and (1.90±0.58) h, respectively; tmax stood at (1.86±0.74)h and (1.68±0.55) h, respectively; Cmax stood at (525.09±208.94)ng/ml and (530.32±202.04) ng/ml, respectively; AUC0～11 stood at(2 048.5±749.4)(ng·h)/ml and (2 042.0±743.0)(ng·h)/ml, respectively;AUC0～∞ stood at(2 163.2±783.1)(ng·h)/ml and (2 136.4±792.1)(ng·h)/ml, respectively. The relative bioavailability of the kushenin tablet stood at (101.06±9.41) %. CONCLUSION:The tablet and capsule of kushenin were bioequiva_lent.