海南医学
海南醫學
해남의학
Hainan Medical Journal
2015年
19期
2931-2934
,共4页
甘草酸苷%生物等效性%液-质联用
甘草痠苷%生物等效性%液-質聯用
감초산감%생물등효성%액-질련용
Glycyrrhetic acid%Bioequivalence%High performance liquid chromatography-mass spectrometry (HPLC-MS)
目的 研究复方甘草酸苷胶囊在健康男性体内的药代动力学和生物等效性.方法 用自身前后对照方法,24例健康男性受试者按随机号分为受试组和参比组,交替服用75 mg复方甘草酸苷胶囊和复方甘草酸苷片两种制剂,72 h内间断采血;采用液-质联用法测定甘草酸苷代谢物甘草次酸的血药浓度,计算药代动力学参数,判定两制剂是否人体生物等效.结果 复方甘草酸苷胶囊和片剂在人体内药时曲线符合二室模型,主要药代动力学参数AUC0~t分别为(4 284±1 149) ng·h/ml和(4 513±1 639) ng·h/ml,AUC0~∞分别为(4 369±1 179) ng·h/ml和(4 691±1 839) ng·h/ml,Cmax分别为(290.0±69.6) ng/ml和(293.4±80.9) ng/ml,Tmax分别为(12.08±1.38) h和(11.92±2.32) h;两种制剂的主要药代动力学参数Cmax,AUC0~t经对数转换后进行方差分析及双单侧t检验,并计算90%置信区间,表明两种制剂人体生物等效,受试制剂复方甘草酸苷胶囊的人体相对生物利用度为(112.7±51.6)%.结论 两制剂具有生物等效.
目的 研究複方甘草痠苷膠囊在健康男性體內的藥代動力學和生物等效性.方法 用自身前後對照方法,24例健康男性受試者按隨機號分為受試組和參比組,交替服用75 mg複方甘草痠苷膠囊和複方甘草痠苷片兩種製劑,72 h內間斷採血;採用液-質聯用法測定甘草痠苷代謝物甘草次痠的血藥濃度,計算藥代動力學參數,判定兩製劑是否人體生物等效.結果 複方甘草痠苷膠囊和片劑在人體內藥時麯線符閤二室模型,主要藥代動力學參數AUC0~t分彆為(4 284±1 149) ng·h/ml和(4 513±1 639) ng·h/ml,AUC0~∞分彆為(4 369±1 179) ng·h/ml和(4 691±1 839) ng·h/ml,Cmax分彆為(290.0±69.6) ng/ml和(293.4±80.9) ng/ml,Tmax分彆為(12.08±1.38) h和(11.92±2.32) h;兩種製劑的主要藥代動力學參數Cmax,AUC0~t經對數轉換後進行方差分析及雙單側t檢驗,併計算90%置信區間,錶明兩種製劑人體生物等效,受試製劑複方甘草痠苷膠囊的人體相對生物利用度為(112.7±51.6)%.結論 兩製劑具有生物等效.
목적 연구복방감초산감효낭재건강남성체내적약대동역학화생물등효성.방법 용자신전후대조방법,24례건강남성수시자안수궤호분위수시조화삼비조,교체복용75 mg복방감초산감효낭화복방감초산감편량충제제,72 h내간단채혈;채용액-질련용법측정감초산감대사물감초차산적혈약농도,계산약대동역학삼수,판정량제제시부인체생물등효.결과 복방감초산감효낭화편제재인체내약시곡선부합이실모형,주요약대동역학삼수AUC0~t분별위(4 284±1 149) ng·h/ml화(4 513±1 639) ng·h/ml,AUC0~∞분별위(4 369±1 179) ng·h/ml화(4 691±1 839) ng·h/ml,Cmax분별위(290.0±69.6) ng/ml화(293.4±80.9) ng/ml,Tmax분별위(12.08±1.38) h화(11.92±2.32) h;량충제제적주요약대동역학삼수Cmax,AUC0~t경대수전환후진행방차분석급쌍단측t검험,병계산90%치신구간,표명량충제제인체생물등효,수시제제복방감초산감효낭적인체상대생물이용도위(112.7±51.6)%.결론 량제제구유생물등효.
Objective To study the bioequivalence and pharmacokinetics of compound glycyrrhizin capsules in human plasma. Methods 75 mg compound glycyrrhizin preparations were given to 24 healthy male volunteers in randomized two-way crossover design for the pharmacokinetic and relative bioavailability study. The volunteers were equally and randomly divided into test preparation group and reference preparation group, which were given com-pound glycyrrhizin capsules followed by compound glycyrrhizin tablets, compound glycyrrhizin tablets followed by compound glycyrrhizin capsules, respectively, with an interval of 14 d. The blood samples were collected within 72 h after taking medicine. Plasma concentration of glycyrrhetic acid were determined by high performance liquid chroma-tography-mass spectrometry (HPLC-MS). Results The concentration-time curves of compound glycyrrhizin cap-sules and compound glycyrrhizin tablets in vivo were in accordance with two compartment model. The main pharmaco-kinetic parameters of the two preparations were: AUC0~t (4 284±1 149) ng·h/ml and (4 513±1 639) ng·h/ml, AUC0~∞(4 369±1 179) ng·h/ml and (4 691±1 839) ng·h/ml, respectively, Cmax (290.0±69.6) ng/ml and (293.4±80.9) ng/ml, Tmax (12.08 ± 1.38) h and (11.92 ± 2.32) h. The mean relative bioavailability of test preparation to reference preparation were (112.7±51.6)%. Conclusion The reference preparation and the test preparation are bioequivalent.
