十二种国产麻黄的品质评价

本文应用高效液相色谱法对我国24个产地所产的12种麻黄生药进行了六种生物碱的定量分析,这六种生物碱是:麻黄碱(ephedrine),伪麻黄碱(pseudoephedrine),去甲基麻黄碱(norephedrine),去甲基伪麻黄碱(norpseudoephedrine),甲基麻黄碱(methylephedrine)和甲基伪麻黄碱(methylpseudoephedrine)。根据分析结果,对这些麻黄生药的品质作出了评价。     

去甲伪麻黄碱的提取与转化

麻黄中含有十几种生物碱,其中有六种结构相似的生物碱:麻黄碱(一)Ephedrine、伪麻黄碱(+)Pseudo-ephedrine、甲基麻黄碱(-)N-Methylephedrine、甲基伪麻黄碱(+)N-Methylpseudo-ephedrine、去甲麻黄碱(-)Nor-ephedrine、去甲伪麻黄碱(+)Nor-pseudo-ephedrine为人们所熟知。目前国内麻黄碱、伪麻黄碱、甲基麻黄碱已由麻     

不同地区市售麻黄药材中盐酸麻黄碱、盐酸伪麻黄碱和总生物碱的含量测定

目的:对全国不同地区市售麻黄药材中盐酸麻黄碱、盐酸伪麻黄碱和总生物碱的含量进行测定,从化学成分的角度对其质量进行评估。方法:收集了28个批次来源于全国7个不同产地、21个不同地区的麻黄药材,按照2010版《中国药典》的方法测定其中盐酸麻黄碱、盐酸伪麻黄碱的含量;建立酸性染料比色法测定药材中的总生物碱。结果:有10个批次的麻黄药材(占全部批次的35.7%)达不到2010版《中国药典》的要求(盐酸麻黄碱和盐酸伪麻黄碱的总质量分数不得少于0.80%),且28个批次的样品中两种生物碱的总质量分数最高与最低相差45倍,总生物碱的质量分数最高与最低相差33倍。结论:所建立的酸性染料比色法测定麻黄总生物碱的含量方法简便、重复性好。市售麻黄药材以草麻黄为主,有效成分生物碱的含量差异较大,劣质情况较为严重。有必要加强麻黄药材的市场监管,保证其临床应用的安全、有效。     

麻黄中麻黄生物碱的气相色谱测定法

本文应用毛细管气相色谱法,配备氮磷检测器对麻黄中六种生物碱:麻黄碱、伪麻黄碱、去甲麻黄碱、去甲伪麻黄碱、甲基麻黄碱和甲基伪麻黄碱进行分离、测定。对生药样品预处理方法作了较大改进,采用直接碱化醚提法。简化操作步骤。用内标法,线性方程定最测定了国产十二种麻黄,结果与高效液相色谱法基本一致。     

麻黄-桂枝配伍对麻黄类生物碱、桂皮酸及桂皮醇在大鼠体内药动学的影响

目的建立UPLC-MS/MS法,对麻黄-桂枝药对提取物、单味麻黄提取物和单味桂枝提取物中麻黄类生物碱、桂皮醇及桂皮酸的血浆药动学进行比较研究,探讨中药复方配伍对药效成分体内过程的影响。方法实验大鼠分别灌胃麻黄、桂枝及麻黄-桂枝提取物,测定不同时间点大鼠血浆中麻黄类生物碱、桂皮醇和桂皮酸的浓度,采用DAS3.0软件计算药动学参数,SPSS13.0对两组的药动学参数进行统计分析。结果麻黄-桂枝组中去甲基麻黄碱、去甲基伪麻黄碱、麻黄碱、伪麻黄碱和甲基麻黄碱的达峰浓度(C_(max))均明显大于麻黄组(P<0.05);麻黄-桂枝组中去甲基伪麻黄碱的药时曲线下面积(AUC_(0-t))明显大于麻黄组(P<0.05);麻黄-桂枝组中去甲基麻黄碱、麻黄碱、伪麻黄碱和甲基麻黄碱的平均驻留时间(MRT_(0-t))均明显小于麻黄组(P<0.05);麻黄-桂枝组中去甲基麻黄碱、麻黄碱和甲基麻黄碱的半衰期(T_(1/2z))明显小于麻黄组(P<0.05)。麻黄-桂枝组中桂皮醇、桂皮酸的AUC_(0-t)和MRT_(0-t)均明显大于桂枝组(P<0.05)。结论麻黄与桂枝配伍后,增加了5种麻黄生物碱在体内的吸收浓度,延缓了去甲麻黄碱、麻黄碱、伪麻黄碱和甲基麻黄碱在体内的消除,提高了桂皮醇和桂皮酸的生物利用度。     

HPLC-UV法同时测定麻黄中5种麻黄生物碱的含量

目的建立同时分离检测麻黄中麻黄碱(Ephedrine)、伪麻黄碱(Pseudoephedrine)、去甲麻黄碱(Norephedrine)、去甲伪麻黄碱(Norpseudoephedrine)和甲基麻黄碱(Methylephedrine)的含量测定方法。方法采用HPLC-UV法,色谱柱:苯基柱(Alltima Phenyl,250mm×4.6 mm,5μm);流动相:0.02 mol/L磷酸二氢钾溶液-乙腈(96∶4);流速:0.6 ml/min;检测波长:210 nm;柱温:25℃。结果 5种生物碱在13.5 min内即可达到完全分离,E在2.000 8～40.016 0μg/ml线性关系良好;PE在1.003 6～20.072 0μg/ml线性关系良好;NME在0.199 2～3.984 0μg/ml线性关系良好;NMP在0.200 0～4.00 0μg/ml线性关系良好;ME在0.200 4～4.008 0μg/ml线性关系良好。各生物碱的平均回收率均在92%～104%(RSD≤5.76%)。结论本方法可操作性强,简便快速,分离效果好,重现性好,可为麻黄及含麻黄的中西药制剂提供有效的检测手段。     

内蒙西部草麻黄中生物碱的动态研究

本文应用高效液相色谱法研究了内蒙西部草麻黄主产区麻黄生物碱的动态变化。样品均采自该区两个固定观测区(5M~2以内),数量多,目前已成为定期供应工厂提取地区。在一般年份,生长期间麻黄碱与伪麻黄碱之比几乎平行,其总生物碱的含量在7月和10月初达高蜂,较之其它地区高(约2.5％)。     

麻黄、含麻黄中成药及生物体液中麻黄碱的定量分析方法

麻黄是一种常用中药 ,为麻黄科多年生草本状小灌木草麻黄 (ＥｐｈｅｄｒａｓｉｎｉｃａＳｔａｐｆ.)或木贼麻黄(Ｅ .ｅｑｕｉｓｅｔｉｎａＢｕｎｇｅ .)和中麻黄 (Ｅ .ｉｎｔｅｒｍｅｄｉａＳｃｈｒｅｎｋｅｔＭｅｙ .)的草质茎 ,是提取麻黄碱和制成多种制剂的原料。麻黄含生物碱 10种以上 ,主要是 3对立体异构的生物碱 ,即 :左旋麻黄碱 (ｌ -ｅｐｈｅｄｒｉｎｅ) ,右旋伪麻黄碱 (ｄ -ｐｓｅｕｄｏｅｐｈｅｄｒｉｎｅ) ;左旋去甲基麻黄碱 (ｌ-ｎｏｒｅｐｈｅｄｒｉｎｅ) ,右旋去甲基伪麻黄碱 (ｄ -ｎｏｒｐｓｅｕｄｏｅｐｈｅｄｒｉｎｅ) ;…     

利用高效液相色谱法测定麻黄浸膏中几种麻黄碱的含量

目的:本文采用高效液相色谱法分离测定麻黄浸膏粉中去甲基麻黄碱,去甲基伪麻黄碱,麻黄碱,伪麻黄碱和甲基麻黄碱的含量.方法:最佳流动相组成磷酸二氢钠0.02mol/l(用盐酸和三乙胺调PH至3.2)-甲醇(99.8:0.2).检测波长210nm.流速1.5ml/min.柱温为室温.色谱柱为HIQSIL C18柱.结果:此法重现性较好,各组分均能达到基线分离,工作曲线线性良好.     

配伍对麻黄甘草药对中麻黄类生物碱在大鼠体内组织分布的影响

目的：研究麻黄与甘草配伍前后麻黄类生物碱在 SD 大鼠组织分布特点,从药物相互作用角度揭示甘草对麻黄类生物碱组织分布的影响。方法采用超高效液相色谱-串联质谱（ UPLC - MS/ MS）法在多反应监测（MRM）模式下测定麻黄与甘草配伍前后不同时间点大鼠各组织液中麻黄类生物碱的浓度,比较麻黄与甘草配伍前后麻黄类生物碱组织分布的差异。结果与麻黄组相比,麻黄与甘草配伍后,促进了去甲基麻黄碱、麻黄碱和伪麻黄碱在研究组织中的吸收和分布;加快了去甲基麻黄碱、麻黄碱、伪麻黄碱和甲基麻黄碱从脑组织中消除;抑制了去甲基伪麻黄碱在心和脑组织中的吸收和分布,并加快了其从心和脑组织中的消除;不同程度地加快了去甲基麻黄碱从心、肺、肾的消除,加快了麻黄碱从心组织中消除,加快了甲基麻黄碱从肺和肾中的消除。结论麻黄与甘草配伍对麻黄类生物碱在大鼠组织中的分布具有显著的影响。     

吲哚美辛缓释栓剂在家兔体内的生物药剂学评价

家兔应用吲哚美辛通栓剂、微囊栓剂及两种复３合微囊栓剂（即缓释栓剂）等四种栓剂后血药浓度的测定，表明缓释栓剂在家兔体内释药性能明显优于普通栓剂和微囊栓剂。     

ROLE OF UTERINE FACTORS IN THE DEVELOPMENT OF HYPERTENSION IN SHR

1. To examine whether the uterine environment plays a role in the development of hypertension in the spontaneously hypertensive rats (SHR), we have compared fetal weight, placental weight, and amniotic fluid composition of SHR and Wistar-Kyoto (WKY) rats after 20 days of gestation. 2. Pregnant SHR and WKY were anaesthetized at 20 days of gestation and the uterus and embryonic sacs removed. Fetal and placental weights were recorded and amniotic fluid collected for measurement of volume, osmolality and electrolyte composition. 3. No significant difference was found in litter size and placental weight between SHR and WKY. Total embryonic sac weight and fetal weight of SHR were significantly lower than WKY. Amniotic fluid volume, sodium concentration and osmolality of SHR were significantly higher than WKY, while amniotic fluid potassium concentration of SHR was significantly lower than WKY. 4. Thus, the SHR foetus was significantly underweight compared to the WKY and was bathed in amniotic fluid with a significantly higher osmolality and sodium concentration. As the mature foetus is known to drink amniotic fluid, it is hypothesized that the elevated Na/K ratio in SHR amniotic fluid may instigate or accelerate the hypertensive process.     

ROLE OF NITRIC OXIDE IN THE DEVELOPMENT OF CORTICOTROPIN-INDUCED HYPERTENSION IN SHEEP

1. The possibility that altered synthesis of vascular nitric oxide (NO) plays a role in the development of corticotropin-induced hypertension in sheep was examined by determining the effect of concomitant infusion of L-arginine, a precursor of NO, on the development of the hypertension. 2. Corticotropin (5 μg/kg per h) infused over 2 days increased mean arterial pressure (MAP) from 83 ± 4 to 99 ± 4 mmHg in five conscious sheep. Concomitant infusion of L-arginine (60 mg/kg per h) did not alter this response; infusion of L-arginine alone had no effect on blood pressure. 3. The dose of L-arginine (60 mg/kg per h) used blocked the rise in MAP (+16 mmHg) in response to a 5 h infusion of N-nitro-L-arginine (1 mg/kg per h). 4. These findings suggest that disruption of NO synthesis does not play a role in the development of corticotropin hypertension in sheep.     

HPLC测定川产六种鹿蹄草中高熊果苷的含量

目的　对川产 6种鹿蹄草中的高熊果苷进行含量测定。方法　用HPLC ,色谱柱SynchromSi(5 μm ,15 0mm× 4 .6mm) ,流动相为正己烷 -醋酸乙酯 -甲醇 (30∶10∶9) ,检测波长 2 80nm。结果和结论　线性范围为 0 .5 2 4～2 .6 4 μg(r=0 .9997) ,平均回收率 96 .6 8% ,RSD =3.72 %。该方法可行     

新达罗治疗泌尿生殖系统感染52例

目的：验证了国产头孢克罗（新达罗）的临床疗效。方法：５２例泌尿生殖系统感染患者应用新达罗治疗,并与头孢拉定治疗４６例进行对照。结果：治疗组与对照组临床总有效率分别为９２．３％和８７％,其中单纯性泌尿系统感染有效率分别为１００．０％和９４．１％,复杂性尿路感染分别为９０．５％和８４．２％,前列腺炎分别为８３．３％和８０．０％,两组疗效间差异无显著性（Ｐ〉０．０５）,治疗组和对照组细菌清除率分别为８８     

β肾上腺素受体拮抗剂对点燃的调控机理

目的　研究中枢β肾上腺素受体(β-AR)及其亚型在大鼠点燃模型的调控机理。方法　建立大鼠杏仁核电刺激点燃和戊四唑化学性点燃模型,观察β-AR亚型激动剂和拮抗剂对点燃和小鼠最大电休克的影响。结果　β-AR拮抗剂普萘洛尔明显延缓杏仁核点燃进程;普萘洛尔和β₁-AR拮抗剂美托洛尔均能显著抑制杏仁核点燃和化学性点燃;β₁-AR激动剂多巴酚丁胺完全逆转普萘洛尔对点燃的抑制作用,β₂-AR激动剂特布他林对普萘洛尔抑制作用无明显影响。结论　中枢β₁-AR参与杏仁核电刺激点燃和戊四唑化学性点燃的抑制作用。     

盐藻β-胡萝卜素预防实验性动脉粥样硬化形成的形态学观察

以鹌鹑动脉粥样硬化(AS)为模型,对从盐泽杜氏藻中提取的以顺式结构为主的β-胡萝卜素(β-C)预防实验性AS进行病理形态学观察,发现Ⅱ组(高饲对照组)动脉病变重,泡沫细胞约10～20层,平滑肌细胞增生,斑块发生率为91.67％。β-C组动脉病变轻,泡沫细胞仅约2～4层,斑块发生率明显少于Ⅱ组(P<0.05),且存在剂量依赖关系。结果表明,β-C能有效地抑制AS斑块的形成和发展。     

INVOLVEMENT OF OXIDATIVE AND L-ARGININE-NO PATHWAYS IN THE NEUROTOXICITY OF DRUGS OF ABUSE IN VITRO

1. Inhibitors of nitric oxide (NO) formation or ADP-ribosylation attenuate methamphetamine (METH)- and methyl-enedioxymetamphetamine (MDMA)-induced neurotoxicity on dopaminergic and serotonergic cells in primary cultures. 2. They also prevent METH-induced reactive gliosis in dopaminergic cultures. 3. Overexpression of superoxide dismutase (SOD) in cells obtained from SOD-transgenic mice also attenuates drug-induced toxicity. 4. These data indicate a role for oxygen-based and NO free radicals in the mechanisms of cell death associated with drugs of abuse in vitro.     

PARTICIPATION OF PROSTANOIDS IN CHEMICAL ACTIVATION OF THE PERICARDIAL PRESSOR REFLEX IN DOGS

1. Experiments were performed on anaesthetized, open-chest dogs to determine the reflex effects on systemic blood pressure and heart rate produced by stimulation of the parietal pericardium with bradykinin, prostacyclin, prostaglandin E₂ (PGE₂), prostaglandin D₂ (PGD₂) and arachidonic acid. 2. Pericardial application of bradykinin (1 μg) consistently elicited reflex increases in blood pressure and heart rate, whereas application of prostanoids or arachidonic acid in doses up to 10 μg failed to produce any cardiovascular responses. 3. Indomethacin, applied either directly to the parietal pericardium (1 μg/ml) or given intravenously (5 mg/kg) caused a long lasting reduction of the reflex responses to bradykinin. The reflex effects of bradykinin could be temporarily restored by treatment of the pericardium with either prostacyclin (0.1 μg/min) or PGE₂ (0.1 μg/min). PGD₂ (0.1-1 μg/min) did not influence the bradykinin induced pericardial reflex. 4. Superfusion of arachidonic acid (3 μg/min) over the pericardium amplified the reflex effects of bradykinin when given before, but not when given after indomethacin treatment. 5. The results indicate that locally formed prostanoids, specifically prostacyclin and PGE₂, can facilitate activation of the pericardial pressor reflex by bradykinin. The findings may be relevant to the changes in cardiovascular activity occurring during pericardial inflammation.