一测多评法测定肉苁蓉中2种有效成分的含量

摘 要 目的： 建立同时测定肉苁蓉中松果菊苷、毛蕊花糖苷的高效液相色谱一测多评法。方法: 以松果菊苷和毛蕊花糖苷为考察指标, 建立两者间的相对校正因子,并用校正因子计算另一个成分的含量,将一测多评法的计算值与外标法实测值进行比较。结果: 建立的相对校正因子重现性良好,采用校正因子计算的含量值和外标法实测值之间没有显著性差异。结论: 同时测定肉苁蓉中2 种成分的一测多评法方法可靠,结果准确,可用于控制肉苁蓉药材及其饮片的质量。     

壮药毛冬青配方颗粒一测多评的定量研究

目的 建立一测多评法同时测定毛冬青配方颗粒中6种酚酸类成分的含量。方法 以绿原酸为内参物,分别建立其与隐绿原酸、咖啡酸、异绿原酸B、异绿原酸A、异绿原酸C的相对校正因子,并利用该相对校正因子计算含量;同时利用外标法测定该6种酚酸的含量,比较2种测定方法的差异,验证一测多评法的准确性和可行性。结果 相对校正因子的重现性良好,8批毛冬青配方颗粒的计算值与实测值无显著性差异。结论 该方法可用于毛冬青配方颗粒中多指标成分质量评价。     

一测多评法测定弯管列当中4种苯乙醇苷类成分

目的 建立弯管列当中4个苯乙醇苷类成分毛蕊花糖苷、crenatoside、2’-乙酰毛蕊花糖苷、isocrenatoside的一测多评法,验证该方法在弯管列当含量测定中应用的可行性及技术适应性。方法 以毛蕊花糖苷为内标,建立crenatoside、2’-乙酰毛蕊花糖苷、isocrenatoside的相对校正因子,利用相对校正因子计算3个成分的含量,实现一测多评;同时采用外标法测定这4个成分的含量,将2种方法进行分析比较。结果 24批弯管列当药材中4个苯乙醇苷成分按一测多评方法进行测定,其计算值与外标法实测值间无明显差异。结论 以毛蕊花糖苷为内参物同时测定crenatoside、2’-乙酰毛蕊花糖苷、isocrenatoside的一测多评法用于弯管列当的定量分析是可行的、准确的。     

一测多评法测定金鸡胶囊中巴马汀、小檗碱和药根碱的含量

摘 要 目的： 建立金鸡胶囊中3个主要生物碱的一测多评含量测定方法。方法: 以巴马汀为内参物,建立巴马汀与药根碱、小檗碱的相对校正因子,计算药根碱和小檗碱的含量,实现一测多评。采用外标法测定金鸡制剂中巴马汀、药根碱和小檗碱含量,Pearson相关系数法比较计算值和测定值的差异。结果:一测多评法的计算值和外标法测定值间无显著差异,试验所得的校正因子可信。结论: 以外标法测定巴马汀,利用相对校正因子实现对药根碱和小檗碱成分含量测定可行。     

一测多评法测定华佗豆4种生物碱

目的 建立一测多评法检测华佗豆药材中4种生物碱的量。方法 以华佗豆碱乙为内标,建立华佗豆碱甲、碱丙、碱丁的相对校正因子,在考察相对校正因子的重现性后,进一步采用外标法与一测多评法所计算出的成分含量进行比较。结果 6批华佗豆药材中,各成分采用相对因子计算的量与采用外标法计算的结果无显著差异。结论 一测多评法操作简单、结果准确、可靠,可用于华佗豆4种生物碱的测定。     

一测多评法测定毛郁金中5种成分

目的 建立毛郁金药材中不同成分同时测定的一测多评法。方法 以毛郁金中莪术二酮为指标,建立莪术二醇、ocathydro-1,4-dihydroxy-1,4-dimethyl-7-（propan-2-ylidene）azulen-5（1H）-one、原莪术醇和姜黄素的相对校正因子,在考察相对校正因子的重现性后,进一步采用外标法对一测多评法所计算出的成分含量进行验证。结果 10批毛郁金药材中,各成分采用相对因子计算的含量与采用外标法计算的结果无显著差异。结论 以莪术二酮为参照物,采用一测多评测定和计算其他4种成分含量的方法是可行的,结果较为准确。     

一测多评法同时测定小儿麻甘颗粒中5种成分含量

摘 要 目的：建立小儿麻甘颗粒中盐酸麻黄碱、苦杏仁苷、甘草苷、黄芩苷、甘草酸铵5种成分的含量一测多评法。方法: 以苦杏仁苷为内参照物,建立盐酸麻黄碱、甘草苷、黄芩苷、甘草酸铵与苦杏仁苷的相对校正因子,分别采用一测多评法与外标法测定5种成分的含量,比较两种方法测得结果的差异,验证一测多评法的可行性。结果:苦杏仁苷与盐酸麻黄碱、甘草苷、黄芩苷、甘草酸铵的相对校正因子分别为1.237,1.318,1.327,0.884,一测多评法与外标法测得结果无显著差异,相对误差小于0.3%。结论:一测多评法运用于小儿麻甘颗粒的含量测定准确可行。     

一测多评法测定防风中4种色原酮类成分

摘 要 目的：建立测定防风中4种色原酮类成分的一测多评法。方法: 以升麻素苷为内标,分别建立升麻素、5-O-甲基维斯阿米醇苷、亥茅酚苷的相对校正因子,计算防风中升麻素、5-O-甲基维斯阿米醇苷、亥茅酚苷的量,实现一测多评。同时采用外标法测定防风中4种色原酮类成分的量,并比较计算值和实测值的差异,以验证一测多评法在测定中的科学性及可行性。结果:各相对校正因子重现性良好,各成分利用相对校正因子计算的量值与外标法测定值之间无显著差异。结论:该方法准确可靠,简便可行,且节约对照品及检测成本,该方法可作为防风药材多指标成分测定质量控制方法。     

一测多评法测定左归丸中3种环烯醚萜苷类成分的含量

目的：建立以马钱苷为内参物,同时测定左归丸中莫诺苷、马钱苷和山茱萸新苷含量的一测多评法（QAMS）。方法：采用高效液相色谱法,Phenomenex C18（250 mm×4.6 mm,5 μm）硅胶色谱柱;流动相：乙腈（A）-0.3%磷酸水溶液（B）梯度洗脱;柱温35℃;检测波长（0~65 min,240 nm,检测莫诺苷和马钱苷;66~80 min,218 nm,检测山茱萸新苷）。以马钱苷为内参物,建立其与莫诺苷、山茱萸新苷的相对校正因子（RCFS）,并进行含量计算,实现一测多评;同时采用外标法（ESM）测定左归丸中3种有效成分的含量,比较一测多评法计算值与外标法实测值的差异。结果：在一定线性范围内,马钱苷与莫诺苷、山茱萸新苷的相对校正因子分别为1.048、1.390。建立的相对校正因子重现性良好,7批左归丸中3种成分的计算值与实测值间无显著差异。结论：采用本研究建立的“一测多评”法控制左归丸的质量是可行的。     

一测多评法测定茵栀黄颗粒中4个环烯醚萜苷类成分

目的 建立同时测定茵栀黄颗粒中栀子苷、山栀苷、去乙酰车叶草苷酸甲酯和京尼平-1-β-D-龙胆二糖苷的一测多评法,验证该方法在茵栀黄颗粒质量控制应用中的科学性和可行性。方法 采用高效液相色谱法,以栀子苷为内参物,建立该成分与山栀苷、去乙酰车叶草苷酸甲酯和京尼平-1-β-D-龙胆二糖苷的相对校正因子,利用相对校正因子来计算各成分的质量分数,同时用外标法测定茵栀黄颗粒中栀子苷等4个成分的质量分数,对一测多评的计算值和外标法实测值进行比较,验证一测多评法在茵栀黄颗粒中应用的科学性和准确性。结果 各相对校正因子重复性良好,一测多评法测定结果与外标法测定结果无显著差异。结论 在缺少对照品的情况下,以栀子苷为内标同时测定栀子苷、山栀苷、去乙酰车叶草苷酸甲酯和京尼平-1-β-D-龙胆二糖苷的一测多评法可用于茵栀黄颗粒的定量分析。     

Deamination of beta-phenylethylamine by monoamine oxidase--inhibition by imipramine

The oxidative deamination of tyramine (Tyr), 5-hydroxytryptamine (5-HT), and β-phenylethylamine (PEA) by mitochondrial preparations of rabbit lung and brain was inhibited by imipramine. This tricyclic iminodibenzyl antidepressant drug was most effective in decreasing the deamination of PEA: at 1 × 10^?4M imipramine, deamination of PEA, Tyr and 5-HT was inhibited by approximately 70, 45 and 45 per cent, respectively, when either lung or brain mitochondrial monoamine oxidase (MAO) preparations were used. Imipramine-induced inhibition of MAO was shown to be of a mixed type based on Lineweaver-Burk plots, but was found to be completely reversible. The desmcthyl and didesmethyl derivatives of imipramine were equally as effective as the parent drug in inhibiting the deamination of PEA, whereas the N-oxide analog of imipramine was less effective as an inhibitor of this reaction. These results support the premise that the action of imipramine as a clinically effective antidepressive agent may be related to its inhibitory effect on the specific form of MAO which deaminates PEA.     

Augmentation by serrapeptase of tissue permeation by cefotiam

Cefotiam (CTM) is a new cephalosporin with a broad spectrum of activity against both Gram-positive and Gram-negative microorganisms. Cephalosporins are widely used for prophylaxis of infections in patients undergoing thoracotomy. Augmentation by serrapeptase on tissue permeation of CTM was examined in 35 thoracotomy patients with lung cancer. The subjects were divided into two groups according to the method of the administration of CTM. Group I consisted of 17 subjects, each of whom received a single dose of 2 g of CTM alone by an instillation for 30 minutes. Group II consisted of 18 subjects, each of whom received a combination of CTM and serrapeptase; serrapeptase was given 2 tablets (10 mg) each time for three times/day until the day before surgery, and then CTM was administered by the same procedure. The following results were obtained: Individual difference was observed for the permeation of CTM into tissues. Pathologic differences also affected the permeation. Nevertheless, the CTM levels in pulmonary tissues reached about a half of those in the blood in both the single dose group and the combination group, hence sufficient concentrations exceeding MIC80 for main microorganisms that caused infections in the lung were obtained. The concentrations of CTM in inflammatory tissues have showed lower levels than those of normal tissues in both CTM single dose and the combination groups. Decrease of blood flow volume may have contributed to the reduction in levels of CTM in the inflammatory tissues. The ratio of the concentration of the drug in pulmonary tissues to that in the blood was 29.1 +/- 2.5% in the single dose group, and 44.2 +/- 6.0% in the combination group, the latter showing quite a significant increase (P less than 0.05). Combined administrations of CTM and serrapeptase deserves more trials in the case when surgical treatments of the lung are performed. An antiinflammatory effect of serrapeptase in the respiratory system is expected, and in addition, the combined use of CTM and serrapeptase should stimulate permeation of the antibiotic into tissues.     

Antagonism of morphine by beta-melanocyte-stimulating hormone and by tetracosactin

Using the decerebrate—spinal Lloyd preparation morphine depressed evoked mono- and polysynaptic reflex activity, β-melanocyte-stimulating hormone enhanced monosynaptic reflex activity, and tetracosactin had no effect. When morphine injection was preceded either by β-melanocyte-stimulating hormone or by tetracosactin a statistically significant depression was not observed. The stimulant actions of β-melanocyte-stimulating hormone did not appear to account for its capacity to antagonize morphine. The fall of blood pressure which follows the administration of morphine in this preparation was not antagonized by the prior administration of either polypeptide.     

Analgesia induced by brief footshock is inhibited by 5-hydroxytryptamine but unaffected by antagonists of 5-hydroxytryptamine or by naloxone

Exposure to footshock (1 mA) for 30 sec induced a marked analgesia that was enhanced by pretreatment with the 5HT synthesis inhibitor, p-chlorophenylalanine, and attenuated by the 5HT releasing drugs p-chloroamphetamine and fenfluramine, by the 5HT re-uptake inhibitor, fluoxetine and by the 5HT agonists, 5-methoxy-N,N-dimethyltryptamine and MK212. However, agonists, quipazine and trifluoromethylphenylpiperazine, with greated reported affinities for 5HT binding sites on rat brain membranes than MK212 were without effect as were the antagonists metergoline, methysergide, cyproheptadine, mianserine and methiothepin. The specific opioid antagonist naloxone was also without effect. The results in general indicate that analgesia induced by brief footshock (1 mA, 30 sec) is inversely related to 5HT availability but thereis little evidence of involvement of known 5HT receptors.     

Synergism by caffeine and by cocaine of the motor control deficit produced by midazolam

To evaluate the effects of caffeine and cocaine on the impairment of discriminative motor control produced by midazolam, rats were trained to hold a force transducer operated with a paw so that it remained between upper and lower limits of a force band for a continuous 1.5-s period to deliver each food pellet. Acute doses of 3 mg/kg midazolam SC impaired motor performance. Except for one animal, caffeine (10-40 mg/kg IP) had little or no effect on performance, while cocaine (3.75-22.5 mg/kg IP) produced dose-related impairment. When each dose of caffeine was combined with 3 mg/kg midazolam, a marked synergism in motor performance impairment occurred. Cocaine plus midazolam produced mainly an additive synergism. The conspicuous synergistic action of caffeine on the motor control deficit produced by midazolam contrasts with the typical antagonism found between the benzodiazepines and methylxanthines when performance is evaluated by psychomotor tests not requiring fine motor control.     

The inhibition of cyclo-oxygenase of rabbit platelets by aspirin is prevented by salicylic acid and by phenanthrolines.

Salicylic acid, 1,10- and 1,7-phenanthroline prevented inhibition by aspirin of platelet aggregation and of generation of thromboxane A2 due to arachidonic acid, to the ionophore A21387, to thrombin and to collagen. Dithiothreitol, another drug which prevents aggregation and formation of thromboxane A2, but only reversibly, failed to interfere with the inhibition by aspirin. Irreversible inhibition by indomethacin and by the substrate analogue 5,8,11,14-tetraynoic acid was also unaffected by salicylic acid or by 1,10-phenanthroline, which thus probably exert a specific interaction with the aspirin-binding site. Inactivation of platelet cyclo-oxygenase with arachidonic acid led to inhibition of the formation of thromboxane A2 and of aggregation due to arachidonic acid itself and to collagen, but barely affected aggregation by thrombin, even though generation of thromboxane A2 was blocked. Use of salicylic acid and of reversible inhibitors of cyclo-oxygenase may help to unravel the mechanism of inhibition due to other agents.     

冠舒注射液的薄层色谱鉴别及含量测定

报道了冠舒注射液中葛根和元胡的薄层色谱鉴别结果，方法简便。并用分光光度法对其总黄酮的含量进行了测定，以便控制产品质量，结果可靠、重现性好．三批样品含量分别为８．７８３、７．９０６和８．１３４ｍｇ／ｍｌ。     

Dose-dependent reductions by naloxone of analgesia induced by cold-water stress

Animals exposed to cold-water swims, rotation, or inescapable shocks, display analgesia comparable to that of 10 mg/kg of morphine. The present study investigated whether a narcotic antagonist would eliminate analgesia induced by cold-water swims. In one group of 12 rats, naloxone at 0, 1, 5, 10 and 20 mg/kg was administered at weekly intervals immediately preceding forced cold-water swims (2°C for 3.5 min) and alterations in flinch-jump thresholds were determined 30 min thereafter. In a second group of six rats, the effects of the same dose range of naloxone were determined upon normal flinch-jump thresholds. Naloxone dose-dependently attenuated the cold-water swim-induced analgesia up to a maximal reduction of 50% at 20 mg/kg. In contrast, all doses of naloxone had no effects upon normal flinch-jump thresholds. Since low doses of naloxone completely abolish morphine-induced analgesia, the present data suggest that the analgesia induced by stress is not identical to that of opiates.