清热止咳糖浆质量标准

目的：建立清热止咳糖浆的质量标准。方法：采用薄层色谱法对其中的麻黄,甘草,桔梗进行定性鉴别,以高效液相色谱法对其主要药材麻黄中的麻黄碱进行含量测定。结果：麻黄、甘草、桔梗的供试品薄层色谱中,在与对照品相同位置上显相同颜色的斑点;盐酸麻黄碱在1．71—54．65μg·ml^-1浓度范围内线性关系良好（r=1．0000）。结论：本方法简便、准确、灵敏、重复性好,可用于本品的质量控制。     

咳嗽枇杷糖浆质量标准研究

目的制定咳嗽枇杷糖浆质量标准。方法采用薄层色谱法对处方中的枇杷叶、麻黄、甘草、百部、薄荷脑进行鉴别;采用高效液相色谱法对盐酸麻黄碱进行含量测定。结果采用薄层色谱法能够检出枇杷叶、麻黄、甘草、百部、薄荷脑;含量测定盐酸麻黄碱的线性范围为0.18~0.9μg,r=0.9997,平均回收率为98.6%;RSD=0.85(n=5)。结论该方法简单、快速、准确,可作为咳嗽枇杷糖浆的质量控制方法。     

桉叶止咳糖浆的质量标准研究

目的：对桉叶止咳糖浆的质量标准进行研究，提高质量标准控制水平。方法：采用薄层色谱法对桔梗、枇杷叶进行鉴别，用高效液相色谱测定盐酸麻黄碱的含量。结果：桔梗、枇杷叶的薄层色谱斑点清晰，分离度好，专属件强。阴性无干扰。盐酸麻黄碱测定方法经方法学验证，结果线性、精密度、重复性、溶液稳定性较好，方法可行。结论：提高后的质量标准方法町行，能够对桉叶止咳糖浆的质量进行控制。     

甘草麻黄碱片的质量控制方法研究

目的:建立甘草麻黄碱片的质量控制方法。方法:采用薄层色谱法对甘草麻黄碱片中甘草进行定性鉴别;采用高效液相色谱法测定甘草麻黄碱片中盐酸麻黄碱含量。结果:在薄层色谱中能检测出甘草;盐酸麻黄碱检测浓度在0.502～7.530μg/ml范围内呈良好的线性关系(r=0.9998),平均加样回收率为98.80%(RSD=0.42%)。结论:本方法可用于甘草麻黄碱片的质量控制。     

HPLC测定麻杏止咳糖浆中盐酸麻黄碱的含量

目的建立用高效液相色谱法测定麻杏止咳糖浆中盐酸麻黄碱含量的方法.方法采用十八烷基础烷键合硅胶为填充剂,0.01 mol/L磷酸二氢钾-甲醇(94:6)为流动相,检测波长为210 mm.结果盐酸麻黄碱进样量在0.3145～3.1450 μg范围内呈现良好的线性关系,平均回收率为99.38%,RSD为0.59%(n=5).结论本方法结果准确,重现性好,可用于麻杏止咳糖浆中盐酸麻黄碱的含量测定.     

4个厂家83批复方桔梗麻黄碱糖浆(Ⅱ)的质量分析

目的:通过对4个厂家83批复方桔梗麻黄碱糖浆(Ⅱ)的国家评价性抽验结果进行分析,评价其质量。方法:采用法定检验方法和探索性研究进行样品检测,统计分析并评价。探索性研究内容包括采用高效液相色谱法测定防腐剂苯甲酸等的含量和盐酸麻黄碱的含量,处方抑菌效力检查研究,溶液pH值测定;采用旋光光度法测定蔗糖的含量,氯化铵含量与微生物污染之间联系的研究,采用顶空气相色谱法同时测定薄荷脑和乙醇的含量,采用薄层色谱法对桔梗流浸膏进行鉴别研究。结果:法定检验结果显示,在83批样品中,80批合格,3批不合格,合格率为96.4%。不合格项目分别为装量、微生物限度及氯化铵含量、氯化铵含量。法定检验联合探索性研究结果表明,本品存在处方抑菌效力不符合规定、部分原辅料未按处方量投料、产品质量不均等情况。建议修订本品质量标准:增加桔梗薄层色谱鉴别、p H值测定、防腐剂含量测定、薄荷脑含量测定;将盐酸麻黄碱含量测定方法修订为高效液相色谱法等。结论:复方桔梗麻黄碱糖浆(Ⅱ)样品总体质量较差,部分厂家的生产工艺及质量控制存在较大缺陷,质量标准有待提高。     

杏苏止咳糖浆的质量控制研究

目的建立杏苏止咳糖浆的质量标准。方法采用薄层色谱法对杏苏止咳糖浆中的麻黄、黄芩、浙贝母、桔梗、紫苏叶进行定性鉴别;采用高效液相色谱法测定苦杏仁苷的含量。结果薄层鉴别重现性好,苦杏苷在16.15～80.75μg范围内呈良好的线性关系,r=0.999,平均回收率为101.71%,精密度RSD为2.88%,重现性RSD为4.22%。结论该方法简便、可靠、准确,可用于该制剂的质量控制。     

HPLC测定麻杏止咳糖浆中盐酸麻黄碱的含量

目的建立用高效液相色谱法测定麻杏止咳糖浆中盐酸麻黄碱含量的方法。方法采用十八烷基硅烷键合硅胶为填充剂,0.01mol·L-1磷酸二氢钾-甲醇(94∶6)为流动相,检测波长为210nm。结果盐酸麻黄碱进样量在0.3145～3.1450μg范围内呈现良好的线性关系,平均回收率为99.38%,RSD为0.59%(n=5)。结论本方法结果准确,重现性好,可用于麻杏止咳糖浆中盐酸麻黄碱的含量测定。     

复方桔梗麻黄碱糖浆(Ⅱ)的质量标准研究

目的建立复方桔梗麻黄碱糖浆(Ⅱ)的质量标准。方法采用薄层色谱法进行定性鉴别,以反相高效液相色谱法测定盐酸麻黄碱的含量。采用C18柱,流动相为乙腈-0.1%磷酸溶液(含0.1%三乙胺)(5∶95),检测波长为210nm。结果薄层色谱分离度较好,盐酸麻黄碱的线性范围为40.94～1 637.6 ng(r=0.999 9,n=5),平均回收率为100.8%(RSD=1.1%,n=9)。结论该法简便、准确、专属性强,可有效地控制复方桔梗麻黄碱糖浆(Ⅱ)的质量。     

金麻杏止咳片快速薄层色谱鉴别与3成分同时定量测定研究

目的 建立简便、快捷的金麻杏止咳片质量控制方法.方法 在5块薄层板上鉴别前胡、黄芩、麻黄、枇杷叶、金银花、苦杏仁和桔梗.采用高效液相色谱法,以乙腈-甲醇-0.1%磷酸(4.5:9:86.5)为流动相,测定样品中盐酸麻黄碱、盐酸伪麻黄碱与苦杏仁苷的含量.结果 通过方法学考察,盐酸麻黄碱进样量在0.0505～0.505 μg(r=0.999997),苦杏仁苷进样量在0.1488～1.488μg(r=0.99996)范围内分别与峰面积呈良好的线性关系.盐酸麻黄碱回收率为100.14%,RSD为1.98%(n=9);苦杏仁苷回收率为97.88%,RSD为1.64%(n=9).结论 所用方法简便、快捷、实用,可用于金麻杏止咳片的质量控制.     

EFFECT OF POLICOSANOL SUCCESSIVE DOSE INCREASES ON PLATELET AGGREGATION IN HEALTHY VOLUNTEERS

Policosanol is a cholesterol-lowering drug with hypocholesterolemic effects demonstrated in experimental models, healthy volunteers and type II hypercholesterolemic patients. In addition, antiplatelet effects of policosanol have been shown in experimental models and healthy volunteers. The effect of successively increasing doses of policosanol on platelet aggregation was investigated in a randomized, placebo-controlled, double-blind study conducted in 37 healthy volunteers. The volunteers were on a placebo-baseline period (two tablets per day) for 7 days and thereafter they received randomly, under double-blind conditions, placebo or policosanol (10mgday⁻¹) for 7 days. After this period dosage was doubled to 20mgday⁻¹for the next 7 days and then again doubled to 40mgday⁻¹, while the control group received placebo tablets all the time. Platelet aggregation as well as coagulation time was measured at baseline and after each dosing step. Results showed that antiplatelet effects of policosanol were successfully enhanced throughout the study, thus suggesting a dose-dependent relationship. No significant effect was reached during the first dosing period, but significant reductions of epinephrine and ADP-induced platelet aggregation were observed after the second one. Finally, a significant inhibition of platelet aggregation induced by all the agonists was observed at the last dosing step. Coagulation time remained unchanged during the trial.     

NEURAMIDE STIMULATES ADRENOCORTICOTROPIN BUT NOT PROLACTIN RELEASE FROM RAT PITUITARY

Neuramide (NMD), a substance found in crude preparations of porcine stomach extract, is a viral inhibitor that also has putative immunostimulatory effects. The effects of NMD on stress-hormone (ACTH and prolactin—PRL) release were assessed inin vivoandin vitrostudies. In the former, blood levels of corticosterone and PRL were measured in NMD-treated male rats.In vitroexperiments were performed to evaluate the effects of NMD and three of its fractions (obtained with high performance liquid chromatography) on ACTH and PRL release from perfused rat pituitary slices. NMD increased plasma corticosterone levelsin vivoand produced dose-dependent increases inin vitropituitary release of ACTH. No effects on PRL secretion were observedin vivoorin vitro. The stimulatory effects on ACTH release were caused by the NMD fraction with a molecular weight of >5000<10000Da.     

Synthesis and evaluation of 2,6-piperidinedione derivatives as potentially novel compounds with analgesic and other CNS activities

New 2,6-piperidinediones 2_a–g and 4_a–d were prepared by initial condensation of aromatic aldehydes or cycloalkanones with cyanoacetamide to give α-cyanocinnamides l_a–g or cycloalkylidenes 3_a,b which underwent Michae1 addition with ethyl cyanoacetate or diethylmalonate. Compounds 4_a–d were alkylated by various alkyl halides to produce the N-alkylated 2,6-piperidinedione derivatives 5_a–m. Some new selected compounds 2_a–c,f, 4_a–d & 5_e,h,j were pharmacologically evaluated for potential anticonvulsant, sedative and analgesic activities. These compounds exhibited significant anticonvulsant and analgesic effects after a single I.P. administration 100 mg/kg b.wt. . On the other hand all the investigated compounds induced hypnotic activity and prolonged the phenobarbital sodium- induced sleep as compared with the control group and the most potent compound was found to be 2_f.     

INDIRECT PARASYMPATHOMIMETIC ACTIVITY OF THE CLASS III ANTIARRHYTHMIC SUBSTANCE / -SOTALOLIN VITRO: REVERSIBLE INHIBITION OF CHOLINESTERASE ISOENZYMES FROM BLOOD AND THE HUMAN CENTRAL NERVOUS SYSTEM

Inhibitory effects of the class III antiarrhythmic compound / -sotalol on acetylcholinesterase (AChE; EC 3.1.1.7) isoenzymes of both erythrocytes and the human caudate nucleus and on serum cholinesterase (ChE; EC 3.1.1.8) were studiedin vitrousing a spectrophotometric kinetic assay with acetylthiocholine (ASCh) as substrate. Sotalol concentrations in the assays varied from 0.32 to 3.2m . All isoenzymes studied were inhibited by / -sotalol in a reversible and concentration-dependent manner. Double reciprocal plots of the reaction velocity against varying ASCh concentrations revealed that / -sotalol reduced substrate affinity (apparent Michaelis constant, KM, increased) of serum ChE, but did not change the enzyme's maximal rate of ASCh hydrolysis (V_max). Thus, / -sotalol inhibition of serum ChE was of the competitive type (rate constant for reversible competitive inhibition: K_i=0.51m ). In contrast, / sotalol reduced the maximal reaction velocity of the AChE isoenzyme from the central nervous system (caudate nucleus), but had no influence on substrate affinity of the enzyme (K_Mwith ASCh unchanged) indicating purely non-competitive inhibition kinetics (rate constant of reversible non-competitive inhibition: K_i′=0.44m ). / -sotalol inhibition of erythrocyte AChE was of mixed competitive/non-competitive type (K_i=0.31m , K_i′=0.49m ). Non-competitive / -sotalol inhibition of caudate nucleus AChE and the non-competitive component of erythrocyte AChE inhibition cannot be overcome by increased concentrations of the cholinergic transmitter acetylcholine (ACh). Peak / -sotalol plasma levels as described in the literature for both humans (15μ ) and experimental animals (dogs: 18μ ; rats: 260μ ) as well as maximal myocardial concentrations of the substance (dogs: 46μ ; rats: 478μ ) are in the range of about 2% to 100% of the sotalol inhibition rate constants determined in the present paper for cholinesterase isoenzymesin vitro. Thus, / -sotalol inhibition of ACh hydrolysisin vivomay contribute to both the well known antiarrhythmic potential and proarrhythmic side effects of the compound.     

EFFECTS OF 2-GUANIDINE-4-METHYLQUINAZOLINE ON GASTRIC ACID SECRETION IN RATS

In this study 2-guanidine-4-methylquinazoline (2-GMQ) appeared to decrease basal and stimulated gastric acid secretion, while structurally related compounds as dimethyl- biguanide, cyanoguanidine and 2-cyanoamino-4-methylpyrymidine did not. Thus, there is an antisecretory effect when the biguanide group is associated with a lipophilic structure. The antisecretive effects exerted by 2-GMQ are associated with anti H₂-histamine activity.The anti H₂-histamine nature of the effects of 2-GMQ was confirmed by the capacity of this compound of depressing the chronotropic activity of the isolated guinea pig auricle increased by histamine, as well as relaxant activity in rat uterus contracted by histamine, since both preparations are rich in H₂-histamine receptors.     

Investigation of the prevalence of tetQ, tetX and tetX1 genes in Bacteroides strains with elevated tigecycline minimum inhibitory concentrations

In this study, the antibiotic susceptibilities to tigecycline and tetracycline of 35 selected Bacteroides fragilis group strains were determined by Etest, and the presence of tetQ, tetX, tetX1 and ermF genes was investigated by polymerase chain reaction (PCR). tetQ was detected in all 12 B. fragilis group isolates (100%) exhibiting elevated tigecycline minimum inhibitory concentrations (MICs) (≥8 μg/mL) as well as the 8 strains (100%) with a tigecycline MIC of 4 μg/mL, whilst tetX and tetX1 were present in 15% and 75% of these strains, respectively. All of these strains were fully resistant to tetracycline (MIC ≥ 16 μg/mL). On the other hand, amongst the group of strains with tigecycline MICs < 4 μg/mL (15 isolates), tetQ, tetX and tetX1 were found less frequently (73.3%, 13.3% and 46.7%, respectively). All but two strains harbouring the tetQ gene in this group were non-susceptible to tetracycline, with a MIC > 4 μg/mL. These data suggest that in most cases tigecycline overcomes the tetracycline resistance mechanisms frequently observed in Bacteroides strains. However, the presence of tetX and tetX1 genes in some of the strains exhibiting elevated MICs for tigecycline draws attention to the possible development and spread of resistance to this antibiotic agent amongst Bacteroides strains. The common occurrence of ermF, tetX, tetX1 and tetQ genes together predicted the presence of the CTnDOT-like Bacteroides conjugative transposon in this collection of Bacteroides strains.     

AMELIORIATION OF CHEMICALLY-INDUCED HEPATOCYTE INJURY BY CYCLOSPORINE A

Cyclosporine A, beside its current applications, possesses potential hepatoprotective effects. This study was directed to investigate the effect of Cyclosporine A pretreatment on hepatic injury due to carbon tetrachloride (CCl₄) and -galactosamine. Rats were injected by two successive doses of Cyclosporine A (5mgkg⁻¹day⁻¹). Six hours after the second dose, 1mlkg⁻¹of CCl₄was administered i.p. Effects associated with Cyclosporine A pretreatment were examined by using isolated hepatocytes and hepatocytes that were immobilized and continuously perfused. -Galactosamine (5m ) was added directly to the perfusion medium. After isolation, hepatocytes were examined histologically by light and electron microscopy, immobilized and perfused for further metabolic functional activity evaluation. Cyclosporine A pretreatmentin vivoproduced hepatoameliorative effects of various degrees which were statistically significant as manifested by: (1) an increased trypan blue exclusion after CCl₄; (2) an improved ureagenesis after CCl₄; (3) a reduction in the lipid droplets accumulation in the cytoplasm produced by CCl₄administration; (4) well preserved cytoplasmic organelles as mitochondria, endoplasmic reticulum ER, nuclear chromatin structures that were altered by CCl₄; and (5) an increased hepatocytes survival in the agarose gel matrix, reduction of LD leakage and improvement of ureagenesis after -galactosamine addition to the perfusion medium. The beneficial effect of Cyclosporine A pretreatment in modifying hepatotoxicity of chemical insults merits further studies.     

栝楼不同药用部位质量控制的研究进展

瓜蒌子、瓜蒌皮、瓜蒌、天花粉来源于栝楼的不同药用部位,4味药材均为常用的大宗药材,现行版《中国药典》对其制定的质量标准过于简单,无法科学合理地控制其质量。本文对瓜蒌子、瓜蒌皮、瓜蒌、天花粉安全性和有效组分的研究进行综述,明确了相关研究存在的问题并针对问题提出建议,为科学全面的药材及饮片标准的制定提供参考依据。     

鼻渊净胶囊的HPLC指纹图谱研究

目的 建立鼻渊净胶囊的高效液相色谱（HPLC）指纹图谱。方法 采用Agilent SB-C₁₈（4.6 mm×250 mm,5 μm）色谱柱,乙腈-水为流动相、以1.0 ml/min流速行梯度洗脱,检测波长210 nm,柱温30 ℃,洗脱时间为80 min。采用中药色谱指纹图谱相似度评价系统（2004A版）对检测出色谱进行指纹图谱相似度评价。结果 建立了鼻渊净胶囊的HPLC指纹图谱,确定了20个共有峰,15个峰归属到各药材,其中5个峰确认了化学成分;10批样品的指纹图谱的整体相似度与对照图谱比较,均在90%以上。结论 所建立的鼻渊净胶囊指纹图谱有助于从整体上控制该制剂的质量。