[摘要] 目的:利用反相高效液相色譜法,分別比較復(fù)方與單味藥材提取物中淫羊藿苷在大鼠體內(nèi)的藥代動(dòng)力學(xué)(藥動(dòng)學(xué))參數(shù)差別,探討配伍對(duì)藥效成分體內(nèi)過程的影響。方法:實(shí)驗(yàn)大鼠分別灌胃復(fù)方及單味藥材提取物后,測(cè)定不同時(shí)間點(diǎn)血漿中淫羊藿苷的濃度,采用藥動(dòng)學(xué)程序3P97對(duì)數(shù)據(jù)進(jìn)行統(tǒng)計(jì)學(xué)處理,進(jìn)行藥動(dòng)學(xué)模型擬合并計(jì)算相關(guān)藥代動(dòng)力學(xué)參數(shù)。結(jié)果:復(fù)方及單味藥材中淫羊藿苷在大鼠體內(nèi)分別呈二室和一室模型,主要藥代動(dòng)力學(xué)參數(shù)為:復(fù)方組Cmax=(3.133±0.290) μg/ml,t1/2(Ka)=(0.753±0.809) h,Tmax=(2.089±0.144) h,AUC0-24=(30.839±3.680) μg·h/ml。單味藥材組Cmax=(2.318±0.218) μg/ml,Tmax=(1.497±0.521) h,AUC0-24=(19.947±2.555) μg·h/ml。結(jié)論:與單味藥材相比,復(fù)方中淫羊藿苷在大鼠體內(nèi)吸收增加、消除及達(dá)峰時(shí)間延長、血漿清除率減少,因此復(fù)方配伍對(duì)淫羊藿苷體內(nèi)過程有顯著影響。
　　[關(guān)鍵詞] 藥代動(dòng)力學(xué);淫羊藿;淫羊藿苷;HPLC
　　[中圖分類號(hào)]R965 [文獻(xiàn)標(biāo)識(shí)碼] A[文章編號(hào)] 1673-7210(2009)07(a)-081-04
　　
　　Pharmacokinetics analysis of icariin in rats coming from Chinese medicine compound recipe and single medicinal materials
　　DUAN Xuguang, ZHOU Chongwen, CHEN Ke, ZENG Lei
　　(Hunan Environment and Biologic Polytechnic, Hengyang 421005, China)
　　[Abstract] Objective: To compare the difference of kinetic parameter of medication-metabolism in rats of the icarrin, which come from compound recipe and single medicinal materials using RP-HPLC, and disscuss the influence of compatibility of medicines to body. Methods: The rats were intragastric administered with compound recipe and extractive of Longspur Epimedium respectively. The blood concentration of different time points were tested by proposed established RP-HPLC. Data were dealed with pharmacokinetic programme, and fitted to kinetic parameter. It showed that icarrin in the compound recipe was in two-chamber in mouse, and single medicinal materials in one-chamber. Results: Main kinetic parameters were that compound group was Cmax=(3.133±0.290) μg/ml, t1/2(Ka)=(0.753±0.809) h, Tmax=(2.089±0.144) h, AUC0-24=(30.839±3.680) μg·h/ml. Single medicinal materials group was Cmax=(2.318±0.218) μg/ml, Tmax=(1.497±0.521) h, AUC0-24=(19.947±2.555) μg·h/ml. Conclusion: The results show that there are some significance differences of icariin between the compound recipe and single herber. The elimination, absorption, peak time of icariin in the compound recipe are higer than in Longspur Epimedium.
　　[Key words] Pharmacokinetics; Longspur Epimedium; Icariin; HPLC
　　
　　復(fù)方肝康顆粒(以下簡稱為“復(fù)方”)是在“乙肝湯劑”的基礎(chǔ)上,經(jīng)過拆方解方和劑型研究改進(jìn)而來,長期臨床療效表明,該復(fù)方能明顯改善慢性乙肝患者的癥狀和體征,具有護(hù)肝和抗病毒的作用[1]。淫羊藿苷是淫羊藿的主要有效成分,是一種分子式為C33H40O16的異戊烯基黃酮醇苷類化合物。近年來的研究表明,淫羊藿苷具有多方面藥理作用,主要包括:心血管方面,在降低心肌耗氧量的同時(shí)降低外周阻力,減輕心臟后負(fù)荷,對(duì)心肌缺血和心律失常等心血管疾病有改善作用[2],擴(kuò)張血管平滑肌,改善微循環(huán),對(duì)腦部缺血、低氧有保護(hù)作用;內(nèi)分泌方面表現(xiàn)為性激素樣作用,具有補(bǔ)腎壯陽作用;促進(jìn)體外培養(yǎng)成骨細(xì)胞增殖和分化;能增強(qiáng)免疫功能,起到免疫調(diào)節(jié)作用,抑制腫瘤細(xì)胞增殖,促進(jìn)凋亡[3],還具有延緩衰老、抗疲勞和耐低氧作用,促進(jìn)蛋白質(zhì)合成與核酸代謝,對(duì)肝細(xì)胞具有保護(hù)作用[4-5]。
　　1 試驗(yàn)材料
　　1.1 儀器
　　北京西東電子高效液相色譜儀LC5500(SPD-10A VP 紫外檢測(cè)器,LC-10AT VP 泵,CBM-102 Communication Bus Module 工作站,HT-230A柱溫箱);WH-2 微型漩渦混合儀(上海滬西分析儀器廠有限公司);TGL16M 高速冷凍離心機(jī)(長沙英泰儀器有限公司);AFX2-1001-P 艾科浦超純水系統(tǒng)(重慶頤洋企業(yè)發(fā)展有限公司);HZ-9811K 雙層雙速振蕩器(上海康華生化儀器制造廠);CH1050超級(jí)恒溫槽(上海恒平科學(xué)儀器有限公司);SKG-02400 電熱恒溫干燥箱(黃石市恒豐醫(yī)療器械有限公司);XS105 DualRange 萬分之一電子天平(METTLER TOLEDO,瑞士);BCD-179K Haier冰箱。
　　1.2 試藥
　　復(fù)方肝康顆粒(批號(hào)為060305),復(fù)方所用藥材及淫羊藿(均購自邵陽藥材公司,淫羊藿批號(hào)為070208),淫羊藿藥材提取物(自制);淫羊藿苷對(duì)照品(中國藥品生物制品檢定所,批號(hào)為110737-200312);苯甲酸對(duì)照品(中國藥品生物制品檢定所,批號(hào)為100419-200301);肝素鈉(南京新百藥業(yè)有限公司);乙腈(美國TEDIA公司,色譜純);冰醋酸(天津化學(xué)試劑有限公司,分析純);乙酸乙酯(天津化學(xué)試劑有限公司,分析純);甲醇(天津化學(xué)試劑有限公司,分析純);重蒸水(自制)。

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