西北药学杂志
西北藥學雜誌
서북약학잡지
Northwest Pharmaceutical Journal
2015年
5期
605-609
,共5页
郭倩倩%张雅%赵航%王四旺
郭倩倩%張雅%趙航%王四旺
곽천천%장아%조항%왕사왕
苦龙胆酯苷%高效液相色谱法%药代动力学
苦龍膽酯苷%高效液相色譜法%藥代動力學
고룡담지감%고효액상색보법%약대동역학
amarogentin%HPLC%pharmacokinetics
目的：建立测定大鼠血浆中苦龙胆酯苷质量浓度的 HPLC 方法，研究苦龙胆酯苷在大鼠体内的药代动力学过程。方法雄性SD大鼠，尾静脉注射苦龙胆酯苷6．25，12．5和25 mg · kg －1，于不同时间采集血液。色谱柱为Woburn Stamsil C18，流动相为甲醇‐水（40∶60），流速为1．0 mL · min－1，柱温为30℃，内标为胡黄连苷Ⅰ，检测波长为260 nm ，应用药代动力学软件DAS 2．0拟合房室模型，并进行药代动力学参数的计算和数据分析。结果在选定的条件下，苦龙胆酯苷和胡黄连苷Ⅰ峰形良好，二者峰面积比值与苦龙胆酯苷血药质量浓度在一定范围内线性关系良好（ r＝0．9994），线性范围在0．114～114μg · m L－1，日内和日间精密度RSD均小于10％，提取回收率为101．1％～106．2％，稳定性的RSD均小于3％。大鼠尾静脉给药后，体内药代动力学过程符合二室模型，在6．25～25 mg · kg －1范围内，药物的最大血药质量浓度（Cmax ）或进入体循环的药量（用AUC表示）的变化与给药剂量的改变不成正比。结论所建立的HPLC法简便、快捷、灵敏、准确，适用于苦龙胆酯苷的药代动力学研究。
目的：建立測定大鼠血漿中苦龍膽酯苷質量濃度的 HPLC 方法，研究苦龍膽酯苷在大鼠體內的藥代動力學過程。方法雄性SD大鼠，尾靜脈註射苦龍膽酯苷6．25，12．5和25 mg · kg －1，于不同時間採集血液。色譜柱為Woburn Stamsil C18，流動相為甲醇‐水（40∶60），流速為1．0 mL · min－1，柱溫為30℃，內標為鬍黃連苷Ⅰ，檢測波長為260 nm ，應用藥代動力學軟件DAS 2．0擬閤房室模型，併進行藥代動力學參數的計算和數據分析。結果在選定的條件下，苦龍膽酯苷和鬍黃連苷Ⅰ峰形良好，二者峰麵積比值與苦龍膽酯苷血藥質量濃度在一定範圍內線性關繫良好（ r＝0．9994），線性範圍在0．114～114μg · m L－1，日內和日間精密度RSD均小于10％，提取迴收率為101．1％～106．2％，穩定性的RSD均小于3％。大鼠尾靜脈給藥後，體內藥代動力學過程符閤二室模型，在6．25～25 mg · kg －1範圍內，藥物的最大血藥質量濃度（Cmax ）或進入體循環的藥量（用AUC錶示）的變化與給藥劑量的改變不成正比。結論所建立的HPLC法簡便、快捷、靈敏、準確，適用于苦龍膽酯苷的藥代動力學研究。
목적：건립측정대서혈장중고룡담지감질량농도적 HPLC 방법，연구고룡담지감재대서체내적약대동역학과정。방법웅성SD대서，미정맥주사고룡담지감6．25，12．5화25 mg · kg －1，우불동시간채집혈액。색보주위Woburn Stamsil C18，류동상위갑순‐수（40∶60），류속위1．0 mL · min－1，주온위30℃，내표위호황련감Ⅰ，검측파장위260 nm ，응용약대동역학연건DAS 2．0의합방실모형，병진행약대동역학삼수적계산화수거분석。결과재선정적조건하，고룡담지감화호황련감Ⅰ봉형량호，이자봉면적비치여고룡담지감혈약질량농도재일정범위내선성관계량호（ r＝0．9994），선성범위재0．114～114μg · m L－1，일내화일간정밀도RSD균소우10％，제취회수솔위101．1％～106．2％，은정성적RSD균소우3％。대서미정맥급약후，체내약대동역학과정부합이실모형，재6．25～25 mg · kg －1범위내，약물적최대혈약질량농도（Cmax ）혹진입체순배적약량（용AUC표시）적변화여급약제량적개변불성정비。결론소건립적HPLC법간편、쾌첩、령민、준학，괄용우고룡담지감적약대동역학연구。
Objective To establish a method for the determination of amarogentin in rat plasma ,and to study the pharmacokinetics of amarogentin in rats .Methods Male SD rats were injected amarogentin in three doses of 6 .25 ,12 .5 and 25 mg · kg -1 through cauda vein ,followed by collecting blood samples at different time .The separation was performed on the column of Woburn Stam‐sil C18 using methanol‐water (40∶60) as the mobile phase at a flow of 1 .0 mL · min-1 .The column temperature and ultraviolet detection were set at 30 ℃ and 260 nm ,respectively .Picroside Ⅰ was chosen as an internal standard .The data were calculated by DAS2 .0 software .Results The determination method of amarogentin was established by HPLC .A good linear relationship was obtained between the peak‐area ratios of amarogentin and picroside Ⅰ and amarogentin′s concentration in plasma samples over the range of 0 .114‐114 μg · mL -1 (r=0 .999 4) .The RSD of inter‐day and intra‐day were both within 10% and the extraction re‐covery was between 101 .1% and 106 .2% .The RSDs of stability for plasma amarogentin were within 3% .The concentration‐time curve of amarogentin in rats plasma after iv administration fitted with the two‐compartment model .Within the range of 6 .25‐25 mg · kg -1 ,the Cmax and AUC did not show direct proportion with the dosage .Conclusion The method of detecting plasma am‐arogentin is simple ,rapid ,sensitive and accurate which is suitable for the pharmacokinetic study of plasma amarogentin in rats .
