ObjectiveTo study the bioequivalence of memantine hydrochloride sustained-release capsules produced by two differen manufacturers on fasting and fed state in Chinese healthy subjects.Methods In this study,a single-center,randomized,open,doublecycle,double-crossover,single-dose trial design was adopted.Twenty-eight healthy subjects were enrolled in fasting group and fed group respectively,and 28 mg of memantine hydrochloride sustained-release capsule test or reference preparation was taken orally once per cycle.The plasma concentration of memantine hydrochloride was determined by LC-MS/MS method,and the pharmacokinetic parameters were calculated,and the two memantine hydrochloride sustained-release was carried out.Results The t 1/2 of test preparation and reference preparation in fasting group were（66.99±13.32） and （66.79±10.43） h,respectively;the median of t max were 28.00 （14,40） h and 30.00 （14,40） h,and the C max were （31.42±4.47） and （30.69±4.26） ng·m L -1 ,respectively;AUC 0-t were（3 592.17±578.74） and （3 533.52±516.64） h·ng·m L -1 ,and AUC 0-∞ were （3 776.91±674.44） and（3 712.86±575.83） h·ng·m L -1 ,respectively.The statistical results of 90%confidence intervals of geometric mean ratio （test preparation/reference preparation） of main pharmacokinetic parameters C max ,AUC 0-t and AUC 0-∞ of the subjects included in the bioequivalence set （BES） are within the acceptable equivalence range,which are 99.58%-106.67%and 96.82%-105.54%,respectively.In the fed group,the t 1/2 of the test preparation and the reference preparation were （71.21±18.14） and （70.99±16.52） h,respectively;the median of t max were 14.00 （10,30） h and 14.00 （6,34） h,and the C max were （37.95±6.37） and （36.99±6.58） ng·m L -1 respectively;AUC 0-t were（4 063.27±615.23） and （4 002.03±693.03） h·ng·m L -1 ;AUC 0-∞ were （4 303.71±741.49） and（4 242.14±814.13） h·ng·m L -1 ,respectively.The statistical of 90%confidence intervals of geometric mean ratio（test preparation/reference preparation） of C max ;AUC 0-t and AUC 0-∞ were 98.86%-105.19%,97.67%-105.95%and 97.27%-106.28%respectively.Conclusion Memantine hydrochloride sustained-release capsule test preparation and reference preparation were bioequivalent in fasting and fed state.

目的 对五味子研究现状和热点趋势进行分析,为五味子今后的研究方向提供参考.方法 在中国知网和Web of science核心合集数据库中检索五味子研究相关的中、英文文献,采用CiteSpace 5.8.R1软件分别对作者、机构和关键词等类型的节点进行可视化处理,并结合可视化图谱对五味子研究现状和热点趋势进行分析.结果 筛选后共纳入2459篇中文文献和1053篇英文文献;作者合作分析结果显示中文文献发文量最多的是陈建光、王春梅团队,英文文献发文量最多的是Handong Sun,Weilie Xiao团队;机构合作分析结果显示北华大学药学院和中国科学院分别为中、英文文献发文量最多的研究机构;关键词分析结果表明中文文献侧重于中医传承和用药规律研究,而英文文献更侧重于药理作用研究.结论 五味子研究仍受到国内外学者重视,我国在该领域的贡献较大;研究主要集中在成分研究、中医传承、临床应用及药理作用;体内作用机制、用药规律等方向可能成为五味子今后的研究热点和前沿.

目的 研究2种盐酸特比萘芬片在中国健康受试者体内的生物等效性.方法 空腹试验和餐后试验各入组40例健康受试者,随机、开放、双周期、双交叉单剂量口服盐酸特比萘芬片受试制剂和参比制剂125 mg,用液相色谱串联质谱(LC-MS/MS)法测定给药后不同时间点特比萘芬的血药浓度.用Phoenix WinNonlin?8.1软件计算药代动力学参数,考察两制剂生物等效性.结果 空腹试验中受试制剂和参比制剂特比萘芬的药代动力学参数Cmax分别为(644.17±274.24)和(663.98±274.76)ng·mL-1,AUC0-t分别为(2440.59±1034.53)和(2521.69±1056.85)ng·mL-1·h,AUC0-∞分别为(2668.83±1153.59)和(2797.24±1234.36)ng·mL-1·h.餐后试验中受试制剂和参比制剂特比萘芬的药代动力学参数Cmax分别为(735.70±266.51)和(705.16±236.93)ng·mL-1,AUC0-t分别为(3762.86±1203.85)和(3718.49±1262.15)ng·mL-1·h,AUC0-∞分别为(4159.11±1400.04)和(4174.91±1690.98)ng·mL-1·h.受试制剂与参比制剂Cmax、AUC0-t和AUC0-∞几何均数比值的90％置信区间均在85.12％～111.81％内,表明盐酸特比萘芬片受试制剂和参比制剂在空腹状态和餐后给药时均具有生物等效性.结论 2种盐酸特比萘芬片在中国健康受试者体内具有生物等效性.

目的 评价单次和多次口服非布司他片在中国健康受试者中的药代动力学特征以及安全性.方法 本研究共纳入24例健康受试者,单次给药试验12例,多次给药试验12例.单次给药试验采用随机、自身对照、三剂量水平三周期交叉设计,分为3组,每组4例,依据周期先后分别服用非布司他片20,40,80 mg,每1周期用药1次.另入选12例受试者进行40 mg剂量的多次给药试验.试验第1天口服40 mg,第3天继续服用40 mg,每日1次,并连续给药6次至第8天.单次给药和多次给药试验均按计划的采血时间点采集静脉血,通过高效液相串联质谱法检测受试者血浆样本中非布司他的浓度.绘制药时曲线,用WinNonlin8.0软件进行药代动力学参数计算和分析.结果 单次给药试验3个组的AUC0-t分别为(2.52±1.09)×103、(5.82±1.83)×103和(13.61±5.02)×103 ng·h·mL-1;Cmax分别为(1.10±0.48)×103、(2.34±0.62)×103和(4.31±1.54)×103 ng·mL-1.多次口服非布司他片试验第1天非布司他的药代动力学参数,AUC0-24h为(6.49±2.04)×103 ng·h·mL-1,Cmax为(2.31±0.78)×103ng·mL-1.多次口服非布司他片后,试验第8天非布司他的药代动力学参数,AUC0-∞为(6.65±2.21)×103 ng·h·mL-1,AUC0-24h为(6.28±2.11)×103 ng·h·mL-1,Css_max为(1.89±0.82)×103ng·h·mL-1.结论 单、多次口服给药后,非布司他20～80 mg在人体内的药代动力学过程基本符合线性特征,建议非布司他片在Ⅱ、Ⅲ期临床试验等的单次口服给药剂量范围20～80 mg,多次口服给药剂量为40 mg,给药间隔为24 h.

目的 以健康受试者为对象进行单次及多次口服奥美拉唑干混悬剂(Ⅱ)的药代动力学试验,明确单次和多次给药后的药代动力学特征,并以市售奥美拉唑镁肠溶片为参比制剂,进行药代动力学比较研究.方法 用单中心、随机、两周期、两交叉、自身对照试验设计,空腹条件下入组28例受试者,随机分为2组,每周期连续用药7天,每天口服奥美拉唑干混悬剂40 mg/1680 mg或奥美拉唑镁肠溶片40 mg,在第1天及第7天服药前后和第5～6天服药前分别按方案进行药代动力学血样采集,用LC-MS/MS技术测定血浆中奥美拉唑浓度,采用Win-Nonlin 7.0计算药代动力学参数,并进行两种制剂的生物等效性评价.结果 受试者单次服用奥美拉唑受试制剂和参比制剂的Cmax分别为(2256.30±793.61),(1415.11±764.68)ng·mL-1;AUC0-24分别为(3812.88±3328.65),(3766.63±3272.82)ng·h·mL-1;AUC0-∞分别为(3832.50±3347.36),(3788.94±3290.35)ng·h·mL-1;Cmax、AUC0-24、AUC0-∞的90％CI分别为152.25％～194.41％,96.83％～117.39％和96.72％～117.13％.受试者连续给药奥美拉唑受试制剂和参比制剂后Cssmax和AUCss显著增大,Cssmax较单次给药分别增大了51.4％和71.5％,AUCss较单次给药AUC0-24分别增大了91.3％和95.6％.结论 奥美拉唑不同剂型口服给药后,AUC均生物等效,单次给药的Cmax生物不等效,多次给药后稳态平均血药浓度生物不等效,受试制剂比参比制剂起效快.

目的 以健康受试者为对象进行单次及多次口服奥美拉唑干混悬剂(20 mg,Ⅰ)的药代动力学试验,明确单次和多次给药后的药代动力学特征,并以市售奥美拉唑镁肠溶片为参比制剂,进行药代动力学比较研究.方法 用单中心、随机、两周期、两交叉、自身对照试验设计,空腹条件下入组28例受试者,随机分为2组,每周期连续用药7天,每天口服奥美拉唑干混悬剂20 mg或奥美拉唑镁肠溶片20 mg,在第1天及第7天服药前后和第5～6天服药前分别按方案进行药代动力学血样采集,采用LC-MS/MS技术测定血浆中奥美拉唑浓度,采用WinNonlin 7.0计算药代动力学参数,并进行两种制剂单多次给药后的药代动力学比较评价.结果 受试者单次服用奥美拉唑受试制剂和参比制剂后血浆中的Cmax分别为(914.00±420.65),(668.61±435.34)ng·mL-1,AUC0-24分别为(1408.87±1599.59),(1417.82±1806.58)ng·h·mL-1,AUC0-∞分别为(1416.42±1607.95),(1427.42±1824.80)ng·h·mL-1,Cmax、AUC0-24、AUC0-∞的90％CI分别为125.66％ ～176.95％,95.89％ ～113.21％ 和95.95％～113.26％.多次给药后奥美拉唑(20 mg)受试制剂和参比制剂后AUCss的90％CI为91.14％～107.21％.结论 奥美拉唑受试制剂和参比制剂(20 mg)口服给药后,AUC均生物等效,单次给药的Cmax生物不等效,多次给药后稳态平均血药浓度生物不等效,受试制剂比参比制剂起效快,受试制剂的Tm a x小于参比制剂.

目的 研究健康受试者空腹单次口服胶体果胶铋胶囊(受试制剂T1)、胶体果胶铋颗粒(受试制剂T2)和枸橼酸铋钾片(参比制剂R1)、枸橼酸铋钾颗粒(参比制剂R2)的药代动力学特征及评价其安全性.方法 本研究采用随机、开放、四制剂组、平行设计,入选48例受试者,随机分为A、B、C、D组,每组12人,男女各半,A、B、C、D组受试者分别单次空腹服用枸橼酸铋钾片240 mg(以Bi2 O3计)、枸橼酸铋钾颗粒2.0 g(含铋220 mg)、胶体果胶铋颗粒2包[每包含胶体果胶铋(以铋计)0.15 g]和胶体果胶铋胶囊6粒[每粒含胶体果胶铋(以铋计)50 mg].用电感耦合等离子体质谱(ICP-MS)法对健康人血浆中铋元素浓度进行检测,计算药代动力学参数,评价受试制剂胶体果胶铋颗粒、胶体果胶铋胶囊分别与参比制剂枸橼酸铋钾片、枸橼酸铋钾颗粒的AUC0-t,AUC0-∞和Cmax差异,并评价其安全性.结果 单剂量空腹给药后铋制剂的主要药代动力学参数如下:C、D、A、B组的Cmax分别(1.79±0.98),(0.96±0.38),(111.54±98.78),(6.40±2.50)ng·mL-1,AUC0-t分别为(15.46±9.92),(12.02±7.60),(240.70±191.08),(28.62±10.41)ng·h·mL-1,AUC0-∞分别为(19.27±11.55),(41.10±66.72),(253.39±199.52),(45.11±31.30)ng·h·mL-1.受试制剂的AUC0-t、AUC0-∞和Cmax不高于参比制剂.结论 健康受试者单次口服胶体果胶铋颗粒、胶体果胶铋胶囊的人体铋吸收低于枸橼酸铋钾片和枸橼酸铋钾颗粒,具有良好的安全性.

目的 评价盐酸克林霉素胶囊在中国健康受试者中的药代动力学特征,并评价两种制剂的生物等效性.方法 空腹、餐后各入组24例健康受试者,采用随机、开放、两序列、两周期双交叉给药的试验设计,受试者单次口服盐酸克林霉素胶囊受试药物和参比药物150 mg,采用液相色谱-串联质谱法(LC-MS/MS)检测人血浆中克林霉素的浓度,使用WinNonlin7.0软件计算药代动力学参数,评价两种制剂的生物等效性.结果 单剂量空腹给药受试药物和参比药物克林霉素的主要药代动力学参数如下:Cmax分别为(2.91±0.86),(2.83±0.83)μg·mL-1,AUC0-t分别为(7.86±3.06),(7.39±2.39)μg·h·mL-1,AUC0-∞分别为(8.06±3.23),(7.59±2.50)μg·h·mL-1.单剂量餐后给药受试药物和参比药物克林霉素后的主要药代动力学参数如下:受试制剂和参比制剂的Cmax分别为(1.98±0.52),(2.05±0.41)μg·mL-1,AUC0-t分别为(9.68±3.35),(9.16±2.66)μg·h·mL-1,AUC0-∞分别为(9.53±2.98),(9.60±3.24)μg·h·mL-1.两药物的主要药代动力学参数Cmax、AUC0-t、AUC0-∞经对数转换后进行方差分析,其90％置信区间空腹状态下分别为94.75％～111.37％,198.81％～111.74％,98.34％～111.66％;餐后状态下分别为84.81％ ～104.19％、94.33％ ～112.92％,93.99％ ～113.64％.结论 空腹和餐后状态下,两种盐酸克林霉素胶囊的主要药代动力学参数相近,具有生物等效性.

目的 评价2种布洛芬片在中国健康受试者中的生物等效性,为一致性评价和临床使用提供依据.方法 采用单次给药、随机、开放、两周期、双交叉设计,空腹、餐后各42例健康受试者,分别随机分为2组,单次口服布洛芬片受试制剂和参比制剂各0.2 g,用液相色谱-串联质谱法(LC-MS/MS)检测人血浆中布洛芬的浓度,用Phoenix WinNonlin软件(8.0版本),以非房室模型计算药代动力学参数,并评价两种制剂的生物等效性;在试验期间对受试者进行相关的安全性评价.结果 单剂量空腹给药后布洛芬主要药代动力学参数如下.受试制剂和参比制剂的Cmax分别为(1.76×104±3218.46)和(1.94×104±4513.33)ng·mL-1,AUC0-t分别为(6.69×104±1.17×104)和(6.45×104±1.34×104)h·ng·mL-1,AUC0-∞分别为(6.88×104±1.23×104)和(6.69×104±1.33×104)h·ng·mL-1.受试制剂和参比制剂的Cmax、AUC0-t和AUC0-∞的几何均值比的90％ 置信区间分别为85.13％ ～100.62％,100.11％ ～109.88％ 和99.64％ ～107.56％.单剂量餐后给药后布洛芬主要药代动力学参数如下.受试制剂和参比制剂的Cmax分别为(1.61×104±4083.11)和(1.62×104±4688.51)ng·mL-1,AUC0-t分别为(5.97×104±1.09×104)和(6.02×104±1.29×104)h·ng·mL-1,AUC0-∞分别为(6.26×104±1.33×104)和(6.32×104±1.48×104)h·ng·mL-1.受试制剂和参比制剂的Cmax、AUC0-t和AUC0-∞的几何均值比的90％ 置信区间分别为93.08％ ～109.35％,97.16％ ～102.40％ 和96.78％ ～102.22％,均在80％ ～125％,判断两种制剂具有生物等效性.此外,在试验期间所有受试者所发生的不良事件均为轻度呈一过性,未发生严重不良事件.结论 布洛芬片受试制剂和参比制剂具有生物等效性,安全性良好.

目的 研究洛伐他汀对七叶皂苷在大鼠体内药代动力学的影响.方法 将SD大鼠随机分为2组:实验组和对照组,每组6只.实验组灌胃洛伐他汀20 mg·kg-1,对照组灌胃等量溶媒后,2组均尾静脉注射注射用精氨酸七叶皂苷钠1.67 mg·kg-1(分别相当于0.5 mg·kg-1七叶皂苷A、0.3 mg·kg-1七叶皂苷B、0.5 mg·kg-1七叶皂苷C和0.3 mg·kg-1七叶皂苷D),并于注射前和注射后0.083,0.25,0.5,1,1.5,2,3,4,6,8,12,24,36和48 h经大鼠眼眶静脉采血,用液相色谱-质谱联用(LC-MS/MS)法测定七叶皂苷A、B、C、D的血药浓度.流动相为0.05％甲酸10 mmol·L-1醋酸铵和甲醇:乙腈=1:1(v/v),梯度洗脱;内标为罗红霉素.用Topfit 2.0软件计算药代动力学参数.结果 实验组和对照组主要药代动力学参数如下:实验组七叶皂苷A、B、C、D的平均AUC0-t分别为(11.89±2.81),(3.83±0.71),(28.33±8.00),(6.45±3.42)μg·h·mL-1,对照组分别为(8.73±2.54),(2.46±0.78),(22.54±18.55),(6.08±2.16)μg·h·mL-1;实验组 平 均AUC0-∞ 分 别 为(12.02±2.86),(3.86±0.78),(29.69±9.12),(6.50±3.63)μg·h·mL-1,对照组分别为(8.93±2.70),(2.51±0.81),(23.95±20.50),(6.21±2.24)μg·h·mL-1;实验 组 平 均CL分 别 为(3.05±1.36),(1.79±0.41),(0.32±0.14),(1.58±0.67)mL·min-1,对 照 组 分 别 为(2.29±3.10),(2.92±1.59),(0.61±0.43),(0.93±0.21)mL·min-1;实验组平均t1/2分别为(8.76±0.15),(4.86±1.91),(8.23±2.43),(4.21±2.46)h,对照组分别为(8.53±2.78),(3.21±2.47),(8.19±4.92),(6.09±2.21)h.实验组与对照组比较,七叶皂苷B的AUC0-t和AUC0-∞ 均 增 加,差 异 均 有 统 计 学 意 义(均P<0.05).结论 洛伐他汀可影响七叶皂苷的大鼠体内药代动力学行为,增加其体内暴露水平.

目的:研究空腹及餐后状态下口服两种不同厂家生产的瑞舒伐他汀钙片在中国健康受试者体内的生物等效性.方法:本研究采用单中心、随机、均衡、开放、两序列、两周期、双交叉、单次给药的试验设计,空腹组和餐后组各入组52名健康受试者,每周期单次空腹/餐后口服瑞舒伐他汀钙片受试制剂或参比制剂10 mg,采用经过验证的LC-MS/MS法测定血浆中瑞舒伐他汀钙片的药物浓度,计算药动学参数,进行两种瑞舒伐他汀钙片的人体生物等效性及安全性评价.结果:空腹组受试制剂和参比制剂的t1/2分别为(10.1±3.9)h和(11.4±7.6)h,tmax分别为(3.9±1.1)h和(3.9±1.1)h,Cmax分别为(8.4±3.8)ng/mL和(8.3±4.2)ng/mL,AUC0-72分别为(75.8±34.7)ng·mL-1·h和(73.2±33.2)ng·mL-1·h,AUC0-∞分别为(77.4±34.9)ng·mL-1·h和(75.2±33.2)ng·mL-1·h.纳入生物等效性集(BES)的51例受试者的主要药动学参数Cmax、AUC0-72、AUC0-∞的几何均数比值(受试制剂/参比制剂)的90％置信区间统计结果均在可接受的等效范围内,分别为95.47％ ～109.71％、98.68％～110.57％、98.31％～109.50％.餐后给药组受试制剂和参比制剂的t1/2分别为(16.7 ±12.8)h和(14.5±5.5)h,tmax分别为(3.8±1.5)h和(3.7±1.4)h,Cmax分别为(5.9±2.9)ng/mL和(5.6±2.7)ng/mL,AUC0-72分别为(64.0±33.4)ng·mL-1·h和(62.2±32.0)ng·mL-1·h,AUC0-∞分别为(67.9±33.5)ng·mL-1·h和(65.5±31.9)ng·mL-1·h;Cmax、AUC0-72、AUC0-∞的几何均数比值(受试制剂/参比制剂)的90％ 置信区间统计结果分别为98.91％～110.68％、99.70％～108.03％、99.83％～108.32％.结论:瑞舒伐他汀钙片受试制剂和参比制剂在空腹和餐后状态下生物等效.服用高脂餐对瑞舒伐他汀钙片的药动学特征并无影响,瑞舒伐他汀钙片与食物或不与食物同服均可.

目的 评价2种匹伐他汀钙片在中国健康受试者中的生物等效性和安全性.方法 采用单次给药、随机、开放、两周期、双交叉设计,空腹入组36例健康受试者,餐后入组48例健康受试者,随机交叉单次口服匹伐他汀钙受试制剂和参比制剂各2 mg,采用液相色谱-串联质谱法(LC-MS/MS)检测人血浆中匹伐他汀的浓度,用Phoenix WinNonlin8.1软件计算药代动力学参数,并进行两种制剂的生物等效性评价.结果 受试者服用受试制剂和参比制剂后,空腹血浆中匹伐他汀主要药代动力学参数如下:Cmax分别为(41.90±16.53),(41.75±21.05)ng·mL-1,AUC0-t分别为(119.62±39.52),(115.29±44.80)ng·h·mL-1,AUC0-∞ 分别为(127.78±43.46),(122.95±48.59)ng·h·mL-1.餐后组血浆中匹伐他汀主要药代动力学参数如下:受试制剂和参比制剂的Cmax分别为(35.75±16.63),(39.78±23.93)ng·mL-1,AUC0-t分别为(120.16±46.74),(121.80±51.16)ng·h·mL-1,AUC0-∞ 分别为(126.24±49.91),(127.99±54.65)ng·h·mL-1.2种制剂的Cmax、AUC0-t和AUC0-∞经对数转换后90％置信区间分别为空腹状态下96.95％ ～109.37％,101.70％～109.43％,101.79％ ～109.64％;餐后状态下83.06％ ～101.84％,94.59％～103.45％和94.59％～103.58％.结论 2种匹伐他汀钙片在中国健康受试者中具有生物等效性,安全性良好.

目的 在高脂血症大鼠模型中研究七叶皂苷对洛伐他汀药代动力学的影响.方法 采用高脂饲料喂饲大鼠,构建高脂血症大鼠模型,通过血清生化分析确定造模成功.选择12只造模成功的大鼠,随机分成2组,即单独给药组和联合给药组,每组6只大鼠.单独给药组和联合给药组大鼠分别经尾静脉注射给予0.9％生理盐水和注射用七叶皂苷钠(0.5 mg/kg,qd),连续14 d.第14天,给药后,两组大鼠灌胃给予洛伐他汀(20 mg/kg,0.5％CMC-Na溶液),并于洛伐他汀给药前和给药后不同时间点采集血样,采用HPLC-MS/MS方法测定洛伐他汀及其活性代谢物洛伐他汀酸的血药浓度,计算药动学参数.结果 长期给予七叶皂苷钠导致洛伐他汀酸的血浆暴露水平显著升高,Cmax、AUC0-t、AUC0-∞分别是单独给药组的2.43 (90％CI:1.55,3.31)、2.66(90％CI:1.67,3.66)和2.99倍(90％CI:1.44,4.55),两组比较差异有统计学意义(P＜0.05).与单独给药组相比,联合给药组洛伐他汀的血浆暴露也略有增加,但两组Cmax和AUC比较差异无统计学意义(P＞0.05).结论 七叶皂苷可抑制高脂血症模型大鼠的洛伐他汀代谢,增加其体内暴露水平.

Objective To investigate the drug -metabolizing enzyme gene cytochrome P450 2C9 ( CYP2C9 ) distribution in Chinese Korean healthy population .Methods Two hundred healthy volunteers from Chi-nese Korean were recruited .A polymerase chain reaction -restriction fragment length polymorphism ( PCR-RFLP) method was developed to detect CYP2 C9*2 and *13 allele frequencies and compare genetic po-lymorphism differences with other ethnic groups from literatures .Results Six cases of CYP2C9 *1/*2 mutation individuals , 1 case of CYP2C9*2/*2 mutation individual and 1 case of CYP2C9*1/*13 mutated individuals in Korean health subjects were found in this study . The allele frequencies of CYP2C9*2 and *13 gene were 2.98% and 0.37%respectively.The results showed that there were similar ethnic in the distribution of CYP2C9 in Chinese Korean and Mongolian. Conclusion The results showed that Chinese Korean existed CYP 2C9 gene polymorphism distribution , and the distribution was similar to the Mongolian in Chifeng region .

目的 研究大鼠多剂量sc丹红注射液后丹酚酸B的药动学.方法 将Wistar大鼠分为3组,分别于尾sc低、中、高剂量(1.25、2.5、5.0 mL·kg-1)丹红注射液,用LC-MS/MS法测定给药后不同时间点丹酚酸B的血药浓度,并采用DAS 2.0软件以非房室模型计算药动学参数.结果 注射低、中、高剂量后,大鼠体内丹酚酸B的Cmax分别为1.8071、3.6004、7.3480 μg·mL-1,AUC0-t分别为0.4927、0.9926、1.9145 μg·mL-1·h,t1/2分别为1.34、1.64、1.42 h;Cmax、AUC0-t与剂量呈线性关系,t1/2与剂量无明显相关性.结论 静脉注射丹红注射液后,丹酚酸B在大鼠体内的药动学行为与剂量呈线性.

Objective To study the effect of diammonium glycyrrhizinate on the pharmacokinetic of simvastain in rats.Methods A parallel de-sign was applied in this study.12 male Wistar rats were randomly divided into 2 groups:control group and treatment group ( n=6).Rats in control group were given simvastain alone 40 mg? kg-1 , while those in the treat-ment group were given diammonium glycyrrhizinate 40 mg? kg -1 followed by intragastric administration of simvastain 40 mg? kg -1 .The plasma concentration of simvastain was determined by LC -MS/MS method. Pharmacokinetic parameters were compared between the two groups. Results The pharmacokinetic parameters of simvastain in control group and treatment group were as follow:Cmax were(148.7 ±37.6) and (221.8 ±61.8) ng?mL-1;AUC0-t were (916.9 ±177.8) and (1573.2 ±676.6) ng?mL-1?h;and CLz were (10.4 ±1.7) and (7.1 ±2.7) L? kg-1? h-1 , respectively. Compared with control group, Cmax and AUC0-t in treatment group increased by about 48% and 72%, respectively, while the CLz decreased by about 32%.There was a significant difference between the two groups ( P<0.05) . Conclusion Diammonium glycyrrhizinate affected the pharmacokinetics of simvastain in rats.

Escin is a mixture of triterpenic saponins which has been used in the treatment of chronic venous insufficiency , haemorrhoids , post-operative edema and trauma.This article reviewed the progress on pharmacokinetic study of escin and aimed to provide reference for clinical rational use of escin.

Objective To study the effect of Aescine on the content of livermicrosome protein , cytochrome P450 ( CYP450 ) and the activity of CYP1A2, CYP2D6, CYP3A4 and CYP2C19 in cytomicrosome of rat liver.Methods Rats were given Aescine by oral administration ( 4.0 mg· kg-1 · d-1 ) for 7 days to detect the content of livermicrosome pro-tein and CYP450 and the activity of CYP1A2, CYP2D6, CYP3A4 and CYP2C19 in cytomicrosome taking 0.9%NaCl, ethanol-5%glucose so-lution and phenobarbital as blank , solvent and positive control group , re-spectively.Results Compared to solvent control group , Aescine in-creased the content of livermicrosome protein , however , it had no statisti-cal significance.Aescine had no effect on the content of CYP 450 , and the activity of CYP1A2, CYP2D6, CYP3A4 and CYP2C19 in solvent control group and Aescine group was comparable.Conclusions Aescine showed no effect on CYP 450 in rats.

Nanomedicine is a kind of pharmaceutical preparation which having the characteristic similar to phospholipid bilayer structure.Compared with traditional forms of drug absorbed in free state,nanomedicine is absorbed most in nano-aggregation state while small in free state,which resulted in different processes in vivoand generated special biological activity.This paper reviews the pharmacokinetics study of nanomedicine base on the recent papers.

Objective To study the serum pharmacochemistry and pharmacokinetics of Naoxuening Injection(NXI).Methods Based on the established HPLC fingerprint of NXI,analysis and comparison were carried out among the HPLC profiles of NXI,blank plasma and human serum samples obtained after intravenous administration of NXI.and the main compounds were identified and then the pharmacokinetics of the main compounds were studied.Results Three compounds were i- dentified from the serum after intravenous administration of NXI.Two were the compounds containing in NXI,which were named after geniposide and paeonol,respectively.The other one was identified as metabolic product.The concentration- time curve of geniposide in blood accorded with one-compartment model of pharmacokinetics,and 70 % of geniposie was cleared from the kidney.The concentration-time curve of paenol in blood accorded with two - compartment model of pharmacoki- netics,and 0.04 % of geniposie was cleared from the kidney.Conclusion The compounds contained in the blood and their metabolites are the effective constituents,and the further serum pharmacochemical research will be beneficial to the pharmacol- ogy and the therapeutic mechanism of of NXI.