贵州不同产地坚龙胆药材及饮片中龙胆苦苷含量测定

目的测定贵州产坚龙胆中龙胆苦苷的含量,并评价不同产地坚龙胆药材及饮片的质量。方法利用正交试验研究了龙胆苦苷的最佳提取方法。结果测定了贵州不同产地坚龙胆药材及饮片中龙胆苦苷的含量。结论贵州不同地区间龙胆药材及饮片质量均符合《中国药典》2005年版要求,各地区之间无明显差异。     

不同产地新疆赤芍中芍药苷的含量测定

目的 测定10个不同产地新疆赤芍药材中芍药苷含量. 方法 采用Agilent TC-C18色谱柱（4.6 mm×150 mm,5 μm）;流动相为甲醇-0.05 mol•L^-1磷酸二氢钾溶液（34.8：65.2）;检测波长：230 nm;流速1 mL•min^-1;进样量10 μL. 结果 芍药苷线性范围为0.100 2～1.002 0 mg,r＝0.999 9（n＝6）;平均加样回收率为98.8%～101.5%,RSD为0.355%～1.770%（n＝9）. 结论 该实验准确测定10个不同产地新疆赤芍中芍药苷的含量,10批药材中芍药苷的含量均符合《中华人民共和国药典》标准.     

反相高效液相色谱法测定 胆芩注射液中3种成分含量

［摘要］目的同时测定胆芩注射液中黄芩苷、靛玉红、绿原酸的含量。方法采用反相高效液相色谱法 ,色谱柱为Kromasil C18（150 mm×4.6 mm ,5 μm）,流动为甲醇 乙腈 0.4%磷酸（ 40：13：47）,流速为 1.0 mL•min 1 ,检测波长为 277 nm,柱温20 ℃。结果黄芩苷、靛玉红、绿原酸分别在 2.10～21.00 μg•mL 1 （r＝0.999 9）; ０.４５～4.50 μg•mL 1（r＝0.999 9） 和0.25～1.85 μg•mL 1（r＝0.999 9）范围内呈线性关系,加样回收率分别为 100.2% （RSD＝0.34%）,99.3%（ RSD＝0.68%） 和 99.9%（ RSD＝0.26%）。结论该方法简便 、快速、准确、灵敏、可靠、重复性好,一次测定多组分,可作为胆芩注射液质量控制方法。     

高效液相色谱法测定硫辛酸注射液含量

目的建立测定硫辛酸注射液含量的高效液相色谱（HPLC）法。方法色谱柱：Acclaim C18 柱（250 mm×4.6 mm,5 μm）,流动相1：0.005 mol•L－1 磷酸二氢钾溶液（磷酸调节pH＝3.0） 乙腈（50：50）,流动相2：0.005 mol•L－1 磷酸二氢钾溶液（磷酸调节pH＝3.0） 甲醇 乙腈（50：48：2）;流速：1.0 mL•min－1;柱温：30 ℃;检测波长：212 nm;进样量：5 μL。结果硫辛酸在 0.3～1.6 mg•min－1 内,两种色谱条件均呈良好线性关系（R12＝0.999 8,R22＝0.999 4）;平均回收率分别为99.90%（RSD＝0.196%）,100.52%（RSD＝0.464%）。结论所建立的两种方法简便、准确,均可用于硫辛酸注射液的含量测定。     

高效液相色谱-蒸发光散射法测定扶正强筋片中黄芪甲苷含量

目的建立扶正强筋片中黄芪甲苷的含量测定方法。方法采用高效液相色谱 蒸发光散射法测定扶正强筋片中黄芪甲苷的含量,色谱条件：Licrosorb C18色谱柱（4.6 mm×150 mm,5 μm）,流动相为乙腈 水（34：66）,流速为0.8 mL•min－1,蒸发光散射检测气载气流速1.6 L•min－1,检测器漂移管温度为49 ℃,增益为4。结果黄芪甲苷在0.052～1.034 mg• mL－1范围内线性关系良好,加样回收率分别为102.2%（RSD＝1.00%,n＝3）,99.1%（RSD＝1.36%,n＝3）,102.4%（RSD＝1.49%,n＝3）。结论该方法准确、重复性好,可用于测定扶正强筋片中黄芪甲苷的含量。     

重感片质量标准研究

［摘要］目的提高重感片的质量标准。方法采用薄层色谱法对重感片中的马兜铃酸A进行薄层色谱鉴别;采用高效液相色谱法测定主药龙胆和秦艽中龙胆苦苷的含量,色谱柱为依利特Hyperisil ODS2色谱柱（4.6 mm×250 mm,5 μm）;流动相：甲醇 水 冰醋酸（25：74：1）;流速1.0 mL•min-1;检测波长为270 nm;柱温常温。结果薄层色谱法可鉴别阳性样品中所含的马兜铃酸A,该制剂中未检出马兜铃酸A。龙胆苦苷进样量在0.23～5. 97 μg范围内有良好的线性关系,r=0.999 8,平均回收率为99. 3%,RSD为0.99%（n=5）。结论该方法简单、准确、灵敏、重复性好,能有效控制重感片的质量。     

不同产地龙胆中龙胆苦苷的含量测定

目的建立龙胆中龙胆苦苷的RP HPLC定量分析方法 ,并对 3 8批不同产地的龙胆进行含量测定。方法采用DiamonsilC18色谱柱 ( 5 μm,2 0 0mm× 4 6mmi d ) ,以乙腈 水 醋酸 (V∶V∶V =1 0∶80∶1 )为流动相 ,流速为 1 0mL·min-1,紫外检测波长为 2 70nm ,柱温为室温 ,内标物为对羟基苯甲酸 ( 1 0 0mg·L-1)。结果龙胆苦苷在 1 2 8～ 1 5 3 6mg·L-1质量浓度内线性关系良好(r=0 9999) ,方法回收率为 99 1 % ,RSD为 0 4% (n =9)。 3 8批龙胆中龙胆苦苷的含量差异较大。结论该方法可用于质量控制 ,并为不同产地龙胆中龙胆苦苷的含量比较提供了依据。     

高效液相梯度洗脱法同时测定复方诺氟沙星滴耳液中3组分的含量

（1. ［摘要］目的建立高效液相色谱（HPLC）法同时测定复方诺氟沙星滴耳液中诺氟沙星、甲硝唑和丙酸倍氯米松的含量。方法Kromasil C18 柱（4.6 mm×250 mm, 5 μm）,流动相为甲醇 乙腈 0.025 mol•L 1磷酸溶液（用三乙胺调至pH至3.0） 注射用水,梯度洗脱。结果诺氟沙星、甲硝唑和丙酸倍氯米松的线性范围分别为15.0～150.0 μg•mL 1（r＝0.999 4）, 15.1～151.0 μg•mL 1（r＝0.999 3）和2.6～ 26.0 μg•mL 1（r＝0.999 4）;平均回收率分别为99.5%, 99.7%和99.5%;RSD分别为0.80%,0.78%和0.92%（n＝9）。结论该方法操作简便,快速,准确度较高,适合复方诺氟沙星滴耳液含量测定。     

吡罗昔康肠溶片含量及其均匀度测定

目的建立测定吡罗昔康肠溶片含量及含量均匀度的高效液相色谱法。方法色谱柱：Diamonsil C18（2）柱 （250 mm×4.6 mm,5 μm）,流动相：乙腈 0.05 moL•L－1磷酸二氢钾溶液（磷酸调pH 至3.0 ）（40：60）,检测波长：243 nm,流速：1.0 mL• min－1,柱温：30 ℃,进样量：20 μL。结果吡罗昔康在20～200 μg• mL－1范围内线性关系良好（r ＝ 0.999 9）,平均回收率99.59%,RSD为1.24%（n ＝ 9）。结论该方法专属性强,重复性好,结果准确可靠,可用于吡罗昔康肠溶片含量及含量均匀度测定。     

高效液相色谱法测定甲磺酸沙喹那韦胶囊主药及有关物质含量

目的建立测定甲磺酸沙喹那韦胶囊含量及有关物质的高效液相色谱法。方法色谱柱为C8柱（250 mm×4.6 mm,5 μm）;流动相为0.02 mol•L 1磷酸盐缓冲液（pH值＝6.7） 乙腈（40：60）,流速：1.0 mL•min 1,检测波长：240 nm 。结果甲磺酸沙喹那韦在16.44～61.64 μg•mL 1的范围内,峰面积与浓度呈线性关系,r＝1.000 0,平均回收率99.98%,RSD＝0.76%（n＝9）。结论高效液相色谱法测定甲磺酸沙喹那韦胶囊含量及有关物质方法简便,结果准确。     

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.     

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 x kg(-1)) or i.p. (50 mg x kg(-1)) administration of an emulsion formulation. 2. Plasma clearance of artemisinin was 12.0 (95% confidence interval: 10.4, 13.0) 1 x h(-1) x kg(-1) in the male rat and 10.6 (95% CI: 7.5, 15.0) 1 x h(-1) x kg(-1) in the female rat suggesting high hepatic extraction in combination with erythrocyte uptake or clearance. Artemisinin half-life was approximately 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.     

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.     

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。     

Changes in angiopoietin expression in glomeruli involved in glomerulosclerosis in rats with daunorubicin-induced nephrosis

AIM: To study the potential pathological role of endogenous angiopoietins in daunorubicin-induced progressive glomerulosclerosis in rats. METHODS: Seventy male Wistar rats were allocated randomly into a daunorubicin group (DRB; n=40) or a control group (n=30). The rats in the DRB group were injected with DRB (15 mg/kg), in their tails. Subsequently, at intervals of 1, 2, 4, 6, 8, and 12 weeks, 5 male Wistar rats in each group were chosen randomly for 24 h urinary protein quantitative measurements (24 h UPQM), and determination of plasma tumor necrosis factor alpha (TNF-alpha), angiopoietin-1 (Ang1), and angiopoietin-2 (Ang2) levels. Kidney sections were examined by electron microscopy, Periodic Acid Schiff (PAS) staining, immunohistochemical staining and in situ hybridization histochemistry. RESULTS: As glomerulosclerosis progressed in the DRB group, expression of Ang1 mRNA and protein in glomeruli decreased and expression of TNF-alpha protein, Ang2 mRNA and protein in glomeruli increased. Expression of Ang1 mRNA and protein in glomeruli were negatively correlated with 24 h UPQM, Fn protein expression, and mean area of extracellular matrix (MAECM). In comparison, expression of Ang2 mRNA and protein in glomeruli were positively correlated with 24 h UPQM, Fn protein expression and MAECM; furthermore, there was a positive correlation between plasma Ang2 and 24 h UPQM. Plasma TNF-alpha and expression of TNF-alpha in glomeruli were positively correlated with expression of Ang2 mRNA and protein in glomeruli. There was a negative correlation between Ang1 protein expression and Ang2 protein expression in glomeruli. CONCLUSION: During DRB-induced glomerulosclerosis, podocyte injury led to a shift in the balance of Ang1 and Ang2 in glomeruli. Increased TNF-alpha in plasma and glomeruli may upregulate Ang2 expression in glomeruli. Elevated Ang2 in both plasma and glomeruli may mediate protein permeability through the glomerular filtration barrier. Moreover, local expression of Ang2 may facilitate the progress of glomerulosclerosis by upregulating a component expression of extracellular matrix.     

Trichinellosis in immigrants in Switzerland

We describe a case of trichinellosis diagnosed at the Division of Infectious Diseases, Hospital of Lugano, in January 2009. This case was associated with a cluster of cases and was traced to the consumption of contaminated meat after a wild boar hunt in Bosnia.