HPLC测定复方胆通胶囊中大黄素和大黄酚的含量

目的:建立以高效液相色谱法测定复方胆通胶囊中大黄素和大黄酚含量的方法。方法:色谱柱为C18柱(250 mm×4．6 mm,5μm),流动相为乙腈-水(85:15);检测波长254 nm;流速为0．8 mL·min-1。结果:大黄素和大黄酚在0．01～0．06 mg和0．02～0．12 mg范围内呈良好的线性关系;相关系敬分别0．999 0和0．999 2;大黄素和大黄酚的平均加样回收率专99．12％(RSD=1．2％)和99．52％(RSD=0．6％)。结论:该方法灵敏、简便,结果准确,适用于复方胆通胶囊中大黄素、大黄酚含量测定。     

HPLC测定骨折挫伤胶囊中大黄素和大黄酚的含量

目的：建立骨折挫伤胶囊中大黄素和大黄酚的含量测定方法;方法：高效液相色谱法,采用C18柱,以甲醇-0．1％磷酸溶液(85：15)为流动相,流速1．0ml／min,检测渡长254nm。结果：大黄素在0．004μg～0．08μg,大黄酚在0．008μg～0．16μg,范围内呈良好线性关系,(r=0．9994,r=0．9993),大黄素、大黄酚在骨折挫伤胶囊中的回收率分别为96．56％、97．35％,RSD分别为1．45％和1．46。结论：本法简便,快速、准确,可用于骨折挫伤胶囊的质量评价和生产工艺的监控。     

消炎散质量标准研究

目的 :建立消炎散的质量标准。方法 :采用薄层色谱法对方中大黄、金银花、栀子进行定性鉴别 ;采用高效液相色谱法测定大黄素、大黄酚的含量。结果 :大黄素的线性范围为21 12～105 6ng/ml(r=0.9998 ,n=5) ,平均回收率为98.78 % ;大黄酚的线性范围为29 28～146 4ng/ml(r=0 9998 ,n=5) ,平均回收率为99.45 %。结论 :本方法操作简便、可靠 ,重现性好 ,专属性强 ,可作为消炎散的内在质量控制方法     

反相高效液相色谱法同时测定熊胆丸中大黄素和大黄酚含量

目的建立高效液相色谱（RP-HPLC）法测定熊胆丸中大黄素和大黄酚的含量。方法色谱柱为Hypersil C18柱（200mm×4．6mm,5μm）,以甲醇-0．1％醋酸（75：25）为流动相,流速为1．0mL／min,检测波长225nm。结果大黄素和大黄酚质量浓度线性范围分别为0．605—6．050μg／mL和2．04～20．40μg／mL,r=0．9999（n=5）,平均加样回收率分别为99．40％和100％,RSD分别为1．83％和0．91％。结论该方法准确、简便、专属性强,可用于控制熊胆丸的质量。     

高效液相色谱法测定痔疮片中大黄素和大黄酚的含量

目的：建立痔疮片中大黄素和大黄酚的含量测定方法。方法：高效液相色谱法。Kromarsil C18柱，甲醇-0.1％磷酸液(90：10)为流动相，流速为1mL／min，检测波长254nm。结果：痔疮片中大黄素和大黄酚能有效分离，且无杂质干扰。大黄素进样量在0．046～O．230μg，大黄酚进样量在0．100～0．500μg，均呈良好线性关系，r=0．9998。大黄素和大黄酚平均回收率分别为99．7％和96．1％(n=5，RSD分别为1.1％和1.9％)。结论：本法准确、可靠。可作为痔疮片的质量控制方法。     

高效液相色谱法测定痔疮胶囊中大黄素和大黄酚的含量

目的：建立高效液相色谱法测定痔疮胶囊中大黄素和大黄酚含量的方法。方法：采用C18柱（250mm×4．6mm,5μm）,以甲醇-0．1％磷酸液（75：25）为流动相,流速为1．0ml·min^-1,检测波长为254nm。结果：痔疮胶囊中大黄素和大黄酚能有效分离,且无杂质干扰。大黄素在0．0261—0．1480μg（r=0．9999）、大黄酚在0．0509—0．2886μg（r=0．9998）均呈良好线性关系。大黄素和大黄酚平均回收率分别为99．0％和98．8％,（n=9,RSD均为1．3％）。结论：本法简便、快速、准确、可靠。     

牛黄净脑片质量标准研究

目的 建立牛黄净脑片的质量控制方法.方法:对冰片、大黄、黄连、连翘、金银花、葛根、栀子进行了薄层色谱鉴别;采用高效液相色谱法测定大黄素、大黄酚的含量.色谱柱为CAPCELL PAK C18,甲醇-乙腈-0.1％磷酸溶液(25∶ 40∶ 35)为流动相;检测波长为254nm.结果 测得线性范围为大黄素0.00526～0.526μg(r=0.9999),大黄酚0.0103～1.03μg (r=0.9999).平均回收率为大黄素98.9％,RSD为1.4％(n=9);大黄酚99.9％,RSD为0.6％(n=9).结论 本法简便、准确、重复性好.     

高效液相色谱法测定热毒平胶囊中大黄素及大黄酚的含量

用高效液相色谱法测定热毒平胶囊中大黄素和大黄酚含量结果线性范围分别为大黄素0.075～1.50μg(r=0.9999,n=7)、大黄酚0.106～1.06μg(r=0.9999,n=5),平均回收率分别为大黄素(98.3±1.5)%、大黄酚(101.9±1.2)%.     

HPLC法测定舒痔丸中大黄素与大黄酚的含量

目的：建立舒痔丸中大黄素与大黄酚的含量测定方法。方法：采用高效液相色谱法,色谱柱为Phenomenex C18（250mm×4．6mm,5μm）,以甲醇-0．1％磷酸（85：15）为流动相,流速为1．0ml·min^-1,柱温30℃,检测波长为254nm。结果：大黄素和大黄酚线性范围分别在2．46～14．78μg·ml^-1（r=0．9999）和5．33～31．97μg·ml^-1（r=0．9999）;浓度范围内呈良好的线性关系。平均回收率分别为99．13％（RSD=0．99％）和99．64％（RSD=0．27％）（n=6）。结论：本方法简便准确,重复性好,可用于舒痔丸质量控制。     

反相高效液相色谱法同时测定芩黄喉症胶囊3组分的含量

目的建立同时测定芩黄喉症胶囊中黄芩苷、大黄素及大黄酚含量的反相高效液相色谱法。方法色谱柱为Agilent C18柱，流动相为甲醇-0．4％磷酸水溶液，梯度洗脱，流速为1．0mL／min，检测波长为254nm，柱温为室温。结果黄芩苷、大黄素及大黄酚的质量浓度分别在8．8～1389mg／L（r=0．9999），0．52～86、54mg／L（r=0．9996），0．42～62．42mg／L（r=0．9998）范围内与峰面积呈良好线性关系。平均回收率分别为99．8％，100．4％，99．8％；方法精密度及重现性良好，RSD均不大于1、3％。结论反相高效液相色谱法简便准确且效率高，可作为芩黄喉症胶囊中黄芩苷、大黄素及大黄酚含量的测定方法。     

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     

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.     

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.     

Genotoxic effects of chlorophenoxy herbicide diclofop-methyl in mice in vivo and in human lymphocytes in vitro

Diclofop-methyl (DM) is a chlorophenoxy derivative used in large quantities for the control of annual grasses in grain and vegetable crops. In this study, the genotoxic effects of DM were investigated by measuring chromosomal aberrations (CAs) in mouse bone-marrow cells and CA and the comet assay in human peripheral lymphocytes. Mice were treated with 15.63, 31.25, 62.5, and 125?mg/kg body weight of DM intraperitoneally for 24 hours, and 15.63-, 31.25-, 62.5-, 125-, and 250-µg/mL concentrations were applied to human lymphocytes for both 24 and 48 hours. In in vivo treatments, DM significantly, but not dose dependently, increased the total chromosome aberrations, compared to both negative and solvent controls. Cell proliferation was significantly, but not dose dependently, affected by all doses. In in vitro treatments, DM (except 15.63 µg/mL) significantly and dose dependently increased the frequency of chromosome aberrations. Also, 250 µg/mL of 48-hour treatment was found to be toxic. Cell proliferation was significantly and dose dependently affected by DM applications, when compared to negative control. In in vitro treatments, DM significantly decreased the mitotic index only at the highest concentration for 24 hours, and 62.5- and 125-µg/mL concentrations for 48 hours. In the comet assay, a significant and dose-dependent increase in comet-tail intensity was observed at 62.5-, 125-, and 250-µg/mL concentrations. The mean comet-tail length was significantly increased in all concentrations. Our results demonstrate that DM is genotoxic in mammalian cells in vivo and in vitro.     

2010调脂治疗领域进展

2010年在调脂治疗领域针对他汀治疗心血管病的防治又进行了许多探索。本文通过综述他汀类药物的国际大规模临床试验结果,重新评价了他汀类药物在冠心病一级预防和冠心病二级预防中的地位,阐明了强化他汀治疗的意义;对他汀的心肾保护作用和安全性新证据进行了说明。     

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.