HPLC法同时测定蒲公英中单咖啡酰酒石酸、绿原酸、咖啡酸、菊苣酸的含量

摘 要 目的：建立HPLC法同时测定蒲公英中4种有机酸类成分含量。方法: 采用Thermo C18柱（250 mm×4.6 mm,5 μm）,流动相为甲醇 0.2%磷酸溶液,梯度洗脱,检测波长为328 nm,流速为1.0 ml·min-1,柱温为35℃。结果: 单咖啡酰酒石酸、绿原酸、咖啡酸、菊苣酸分别在11.59~115.90(r=0.999 9),2.50~24.96(r=0.999 8),2.27~22.70(r=0.999 5),12.44~124.4(r=0.999 8) μg·mL^-1范围内线性关系良好,平均回收率分别为102.50%,99.29%,96.71%,95.36%,RSD分别为2.30%,0.43%,0.78%,1.30%。结论: 该法简单方便、重复性好、准确可靠,可用于蒲公英的质量控制。     

HPLC波长切换法同时测定参茸固本片中7个成分的含量

摘 要 目的：建立HPLC波长切换法同时测定参茸固本片中7个成分含量的方法。 方法: 采用Waters Sunfire C18（250 mm×4.6 mm,5 μm）色谱柱,柱温30 ℃,以乙腈 0.1%磷酸溶液为流动相,梯度洗脱,流速为0.9 ml·min-1, 检测波长分别为330 nm（毛蕊花糖苷、马替诺皂苷）、230 nm（芍药内酯苷、芍药苷）和203 nm（人参皂苷Rg1、人参皂苷Re、人参皂苷Rb1）。 结果:毛蕊花糖苷、马替诺皂苷、芍药内酯苷、芍药苷、人参皂苷Rg1、人参皂苷Re和人参皂苷Rb1 质量浓度分别在6.38～159.50 μg·ml-1（r=0.999 3）、3.19～79.75 μg·ml-1（r=0.999 9）、4.37～109.25 μg·ml-1（r=0.999 5）、14.26～356.50 μg·ml-1（r=0.999 4）、1.95～48.75 μg·ml-1（r=0.999 8）、2.21～55.25 μg·ml-1（r=0.999 7）、2.09～52.25 μg·ml-1（r=0.999 1）范围内与峰面积线性关系良好;平均加样回收率（RSD）分别为98.24%（1.11%）、97.64%（1.43%）、99.23%（0.80%）、100.13%（0.65%）、96.99%（1.56%）、98.10%（1.24%）和97.75%（1.37%）。结论:本文所建立的方法实现了同时测定参茸固本片中毛蕊花糖苷、马替诺皂苷、芍药内酯苷、芍药苷、人参皂苷Rg1、人参皂苷Re和人参皂苷Rb1的含量,可用于参茸固本片的质量控制。     

基于HPLC波长切换法对舒肝益脾液中7种成分的质量控制研究

摘 要 目的：建立HPLC波长切换法同时测定舒肝益脾液中7个成分。 方法: 色谱柱：Luna C18柱（250 mm×4.6 mm,5 μm）;流动相：乙腈 0.05％磷酸溶液,梯度洗脱;流速：0.9 ml·min-1;检测波长：345 nm（滨蒿内酯）、254 nm（毛蕊异黄酮苷、芒柄花苷、毛蕊异黄酮和芒柄花素）和210 nm（去氢茯苓酸和茯苓酸）;柱温：30 ℃,进样量：10 μl。结果: 滨蒿内酯、毛蕊异黄酮苷、芒柄花苷、毛蕊异黄酮、芒柄花素、去氢茯苓酸、茯苓酸7个成分的线性范围分别为6.09～152.25 μg·ml-1(r=0.999 9)、2.42～60.50 μg·ml-1(r=0.999 8)、1.61～40.25 μg·ml-1(r=0.999 6)、2.95～73.75 μg·ml-1(r=0.999 4)、6.88～172.00 μg·ml-1(r=0.999 9)、2.55～63.75 μg·ml-1(r=0.999 5)、2.09～52.25 μg·ml-1(r=0.999 9);平均加样回收率分别为98.96%（RSD=1.18%）,97.89%（RSD=1.41%）,97.18%（RSD=0.88%）,96.87%（RSD=0.97%）,99.32%（RSD=1.25%）,96.77%（RSD=0.86%）和98.55%（RSD=1.03%）（n=9）。结论: 本文建立的HPLC波长切换法同时测定舒肝益脾液中的7个成分,方法简便,可作为舒肝益脾液全面可靠的质量控制方法。     

蝙蝠葛苏林碱对HEK293细胞中L-型钙通道CaV1.2的作用

摘 要 目的：探讨蝙蝠葛苏林碱（DS）对人胚肾细胞（HEK293）上表达的L 型钙通道Cav1.2的作用。方法: 采用脂质体转染法,将L 型钙通道Cav1.2蛋白基因转染到HEK293细胞上,全细胞膜片钳技术记录L 型钙电流ICav1.2,观察DS对L 型钙通道电生理特性的影响。结果:DS在1, 3, 10 μmol·L-1浓度范围内呈浓度依赖性抑制ICav1.2 电流,其抑制率分别为（14.68±4.02）%、（32.37±6.63）% 和（59.63±5.23）%;3 μmol·L-1 的DS对ICav1.2的抑制率与相同浓度的伊拉地平比较,其抑制强度约为伊拉地平的40%。结论:DS可浓度依赖性抑制HEK293细胞上表达的Cav1.2,其作用强度比特异性L 型钙通道阻断药伊拉地平要弱。     

HPLC-ELSD法测定托盘根药材中蔷薇酸的含量

摘 要 目的：建立托盘根药材中蔷薇酸的高效液相色谱-蒸发光散射检测（HPLC ELSD）测定方法。方法: 采用高效液相色谱法,蒸发光散射检测器。色谱柱：Vision HT C18 HL柱（250 mm×4.6 mm,5 μm）;柱温：35℃;流动相：甲醇 0.1%三氟乙酸（66〖KG*9〗∶〖KG-*2〗34）,流速：0.8 ml·min-1;ELSD条件：漂移管温度：90℃,载气流速：2.3 L·min-1。结果: 蔷薇酸进样量在0.155～4.346 μg范围内呈良好线性关系（r=0.999 9）,平均加样回收率为100.4%,RSD=1.88%（n=6）。结论: 该方法简便,结果准确,重复性好,可用于托盘根药材中蔷薇酸的含量测定。     

HPLC法同时测定鼻炎愈合剂中阿魏酸、绿原酸和蒙花苷含量

摘 要 目的：建立HPLC法测定鼻炎愈合剂中阿魏酸、绿原酸和蒙花苷含量。方法: 以Agilent ZORBAX SB C18柱（250 mm×4.6 mm,5 μm）为色谱柱,流动相为乙腈 0.1%磷酸溶液,梯度洗脱,流速为1.0 ml·min-1,柱温30℃,检测波长326 nm。结果: 绿原酸、阿魏酸、蒙花苷分别在3.039 7~30.396 8 μg·ml-1 (r=0.999 7),3.999 9~39.999 4 μg·ml-1 (r=0.999 9),5.820 7~58.207 2 μg·ml-1(r=0.999 9)范围内与峰面积呈良好线性关系,其平均加样回收率分别为98.92%,100.81%,99.89%,RSD分别为1.00%,1.02%,0.99%（n=6）。结论: 该方法操作简便、准确、重现性好,可用于鼻炎愈合剂的质量控制。     

HPLC法测定人血清中百草枯含量

摘 要 目的：建立HPLC法测定人血清中百草枯含量。方法: 色谱柱：Kromasil C18柱（200 mm×4.6 mm,5 μm）,流动相：乙腈 水（含0.03 mol·L-1庚烷磺酸钠,0.24 mol·L-1磷酸）=3〖KG*9〗∶〖KG-*2〗97（用三乙胺调pH至2.0）;检测波长258 nm;柱温25℃;进样体积20 μl;流速0.8 ml·min-1。结果: 百草枯在0.106~10.6 mg·L-1浓度范围内线性关系良好( r=0.999 3),最低检出浓度为0.065 mg·L-1。高、中、低3种浓度样品绝对回收率＞89.4%,方法回收率＞94.4%,日内精密度RSD在0.12%～1.74%之间,日间精密度RSD在0.44%～2.89%之间。结论: 该方法操作简便易行、灵敏度高、专属性强,适用于百草枯的人体血清浓度测定。     

HPLC法同时测定神农茶颗粒中的夏佛塔苷、异夏佛塔苷、去氧地胆草内酯和4,5-二咖啡酰奎宁酸

摘 要 目的： 建立同时测定神农茶颗粒中夏佛塔苷、异夏佛塔苷、去氧地胆草内酯、4,5-二咖啡酰奎宁酸4个成分的高效液相色谱测定方法。 方法: 采用Hypersil C₁₈色谱柱（200 mm×4.6 mm,5 μm）;以乙腈 0.025 mol·L^-1磷酸溶液为流动相进行梯度洗脱,体积流量：1.3 ml·min^-1,检测波长：270 nm（夏佛塔苷和异夏佛塔苷）、208 nm（去氧地胆草内酯）、327 nm（4,5-二咖啡酰奎宁酸）,柱温为室温。结果:夏佛塔苷、异夏佛塔苷、去氧地胆草内酯和4,5-二咖啡酰奎宁酸分别在5.850～117.000,4.650～93.000,4.160～83.200,5.470～109.400 μg·ml^-1范围内线性良好,r值均大于0.999,平均加样回收率分别为97.70％、96.87％、97.53％、99.29％,RSD分别为1.40％、1.13%、1.69%、1.01％(n=6)。 结论: 该方法简便,结果准确,可用于神农茶颗粒的含量测定。     

HPLC法测定复方枸橼酸喷托维林颗粒中枸橼酸喷托维林和盐酸麻黄碱的含量

摘 要 目的：建立HPLC法测定复方枸橼酸喷托维林颗粒中枸橼酸喷托维林和盐酸麻黄碱含量的方法。方法: 采用Kromasil C18（150 mm×4.6 mm,5 μm）色谱柱,流动相为1%三乙胺溶液（磷酸调节pH至3.0） ∶〖KG-*4〗甲醇,梯度洗脱,流速1.0 ml·min-1,检测波长210 nm,柱温35 ℃。结果: 枸橼酸喷托维林在0.08～1.99 g·L-1（r=1.000 0）质量浓度范围内线性关系良好,平均加样回收率为99.1%, RSD为0.7%。盐酸麻黄碱在0.05～1.27 g·L-1（r=0.999 9）质量浓度范围内线性关系良好,平均加样回收率为98.6%,RSD为0.6%。结论: 本方法简便、准确,可用于复方枸橼酸喷托维林颗粒的质量控制。     

HPLC法测定八角茴香中莽草酸和反式茴香脑含量

摘 要 目的：建立同时测定八角茴香中莽草酸和反式茴香脑的方法。方法: 采用HPLC法,以Waters Sunfire C18柱（250 mm×4.6 mm,5 μm）为色谱柱,以乙腈 0.05%磷酸为流动相,梯度洗脱,流速为1.0 ml·min-1,检测波长为210 nm,柱温为30℃。结果: 莽草酸在进样量为0.078～1.558 μg范围内线性关系良好(r=0.999 9),平均回收率为101.38%,RSD=1.67%(n=6);反式茴香脑在进样量为0.093～1.868μg范围内线性关系良好(r=0.999 7),平均回收率为99.02%,RSD=1.47%(n=6)。结论: 该方法简便、准确、重复性好,可以用于八角茴香中莽草酸和反式茴香脑的含量测定。     

Interindividual variability in metabolic activation in humans in vivo

In assessing interindividual variability in metabolic activation, the toxic metabolite is often too unstable for conventional analysis. Possible alternatives include a stable product of the reactive metabolite e.g. cysteinyl derivatives of N-acetyl-4-benzoquinoneimine, the toxic metabolite of paracetamol, adducts with DNA or protein, and indirect measurement of the activity of the enzyme(s) producing the active metabolite. An example of the last approach is the use of furafylline, a highly specific inhibitor of human CYP1A2, to determine the extent of the metabolic activation of the cooked food mutagens PhIP and MeIQx. The extent of inhibition, determined from levels of unchanged amine in urine, is an indirect measure of the activity of the activation pathway. Further refinement of this approach, allied to improved measures of the biological process of interest should prove of value in evaluating interindividual variability and its role in the risk assessment process.     

Quantitative in vivo and in vitro sex differences in artemisinin metabolism in rat

1. The pharmacokinetics of the antimalarial compound artemisinin were compared in the male and female Sprague-Dawley rat after single dose i.v. (20 mg.kg) or i.p. (50 mg.kg) administration of an emulsion formulation. 2. Plasma clearance of artemisinin was 12.0 (95% confidence interval: 10.4, 13.0) l.h. kg in the male rat and 10.6 (95% CI: 7.5, 15.0) l.h. kg in the female rat suggesting high hepatic extraction in combination with erythrocyte uptake or clearance. Artemisinin half-life was 0.5 h after both routes of administration in both sexes. Values for plasma clearance and half-lives did not statistically differ between the sexes. 3. After i.p. administration artemisinin AUCs were 2-fold higher in the female compared with male rat (p 0.001). Artemisinin disappearance was 3.9-fold greater in microsomes from male compared with female livers and it was inhibited in male microsomes by goat or rabbit serum containing antibodies against CYP2C11 and CYP3A2 but not CYP2B1 or CYP2E1. 4. The unbound fraction of artemisinin in plasma was lower (p 0.001) in plasma obtained from the male (8.8 2.0%) compared with the female rat (11.7 2.2%). 5. The possibility of a marked sex difference, dependent on the route of administration, has to be taken into account in the design and interpretation of toxicological studies of artemisinin in this species.     

Theophylline kinetics in peripheral tissues in vivo in humans

Several biochemical and cellular effects have been described for methylxanthines under in vitro conditions. However, it is unknown, whether threshold concentrations required to exert these effects are attained in target tissues in vivo. We therefore employed the microdialysis technique for measuring theophylline concentrations in peripheral tissues under in vivo conditions.Following in vitro and in vivo calibration, microdialysis probes were inserted into the medial vastus muscle and into the periumbilical subcutaneous adipose layer of healthy volunteers. Following single oral dose administration of 300 mg or i.v. infusion of 240 mg theophylline, in vivo time courses of theophylline concentrations were monitored in tissues and plasma. Major pharmacokinetic parameters (c_max, t_max, AUC) were calculated for plasma and tissue time courses. The mean AUC_tissue /AUC_plasma-ratio was 0.56 (p.o.) and 0.55 (i.v.) for muscle and 0.55 (p.o.) and 0.72 (i.v.) for subcutaneous adipose tissue.We conclude that microdialysis provides important information on the distribution and the tissue pharmacokinetics of theophylline.Abbreviations FPIA Fluorescence polarisation immuno assay - AUC Area under the curve - t_max Time to peak concentration - c_max Peak concentration     

休克时血中氧自由基的变化

本实验测定10名休克患者血浆和红细胞的丙二醛(MDA)、血浆总抗的氧化活性(AOA)的含量。结果表明:休克病人红细胞膜和血浆 MDA 含量(4.298±0.722;5.348±0.834)与对照组(3.235±0.682;4.356±1.081)比较明显增高(P<0.05);血浆 AOA(39.65±7.858)与对照组(48.21±10.81)比较明显降低(P<0.01)。提示:休克时,患者机体内自由基反应增强是引起组织细胞损伤的原因之一。     

Polymorphisms in genes involved in neurotransmission in relation to smoking

Smoking behavior is influenced by both genetic and environmental factors. The genetic contribution to smoking behavior is at least as great as its contribution to alcoholism. Much progress has been achieved in genomic research related to cigarette-smoking within recent years. Linkage studies indicate that there are several loci linked to smoking, and candidate genes that are related to neurotransmission have been examined. Possible associated genes include cytochrome P450 subfamily polypeptide 6 (CYP2A6), dopamine D₁, D₂, and D₄ receptors, dopamine transporter, and serotonin transporter genes. There are other important candidate genes but studies evaluating the link with smoking have not been reported. These include genes encoding the dopamine D₃ and D₅ receptors, serotonin receptors, tyrosine hydroxylase, trytophan 2,3-dioxygenase, opioid receptors, and cannabinoid receptors. Since smoking-related factors are extremely complex, studies of diverse populations and of many aspects of smoking behavior including initiation, maintenance, cessation, relapse, and influence of environmental factors are needed to identify smoking-associated genes. We now review genetic polymorphisms reported to be involved in neurotransmission in relation to smoking.     

Tramadol concentrations in blood and in cerebrospinal fluid in a neonate

Based on blood and cerebrospinal fluid samples collected in a full-term neonate, the penetration of tramadol in the central nervous system is described. Following intravenous administration of tramadol, a lag time of about 4 h was observed until full blood–brain equilibration was achieved. This pharmacokinetic observation is in line with a recent pharmacodynamic evaluation of the central opioid effects of tramadol in adults.     

Disease control in asthmatic children seen in private practice in Switzerland

ABSTRACT

Background: Asthma is the most common chronic childhood disease in Switzerland with a prevalence of 10%. Asthma has a high economic burden accounting for high medical costs. Assessment of disease control is likely to be of help in the implementation of strategies to improve asthma. Therefore, we aimed to evaluate asthma control and therapy regimens among children in private practice.

Methods: We assessed asthma control as well as therapy regimens in 575 asthmatic children in an experience programme in Switzerland by using an abbreviated questionnaire based on the asthma control questionnaire and the child health questionnaire on Visit 1 and Visit 2.

Results: Good asthma control at Visit 1 was only present in 25.7% of asthmatic children. Occasional asthma symptoms, limitation of physical activity, nocturnal awakening and anxiety of the parent was present in 80.5%, 41.2%, 46.8% and 57% of the children, respectively. After adjustment of therapy regimens at Visit 1, mainly by adding a leukotriene receptor antagonist, asthma control was reported to be much better in 53.4% of the children at Visit 2.

Conclusions: As asthma control is inadequately achieved within a major portion of asthmatic children, it is imperative to find measures to improve asthma control and hence, to reduce the burden of disease.