薄层扫描法测定冰片及含冰片中成药中龙脑,异龙脑的研究

本文采用硅胶G板,以石油醚;乙酸乙酯:氯仿(22:2:6)上行展开,5%磷钼酸乙醇液显色,对分离所得尤脑,异龙脑色斑进行薄层扫描定量,线性良好(γ=0.9995)。龙脑、异龙脑的平均回收率分别为99.34±2.4,100.0±1.9%用本法测定了数种天然冰片、合成冰片以及含冰片中成药中龙脑、异龙脑含量。对含冰片和薄荷脑的中成药,经改变溶剂系统,也能完全分离。所测含量均获得满意结果,并与毛细管气相色谱法进行了比较,结果相符。     

气相色谱法测定人服用速效救心丸后尿液中的冰片含量

目的：探讨气相色谱法(GC)测定健康志愿者含服速效救心丸后尿液中冰片含量。方法：直接取服药后的尿液样品，用乙醚 正己烷(1∶1)提取液萃取，萘为内标；色谱条件：HP4890D仪，HP 5石英弹性毛细管柱(15 m×0.53 mm，ID)，柱温75℃，进样口温度140℃，气化室温150℃，流速8.1 mL·min 1，氢离子火焰检测器(FID)。结果：冰片的最低检测浓度0.2 μg·mL 1，线性范围：0.6～36.0 μg·mL 1，线性关系良好；其中异龙脑、龙脑的日内及日间精密度平均分别为(8.93±0.67)%和(7.03±2.97)%，(7.37±1.93)%和(7.17±1.15)%；平均回收率分别为(107.6±9.4)%，(109.0±9.0)%。结论：该尿液预处理方法可行，GC法简便、灵敏、可靠，可用于人尿液中冰片的研究。     

气相色谱法测定健康人含服速效救心丸后冰片的血药浓度

目的 :用气相色谱法测定健康人含服速效救心丸后冰片 (龙脑、异龙脑)的血药浓度。方法 :采用HP -5石英弹性毛细管柱 ,柱温为85℃ ,汽化室温度为180℃ ,检测器温度为200℃ ,载气为氮气 ,萘为内标。结果 :冰片进样量在50～1000ng/ml范围内其峰面积与进样量呈良好线性关系 ,Y=—0 1273+0 0015X ,回收率为 (98 7±2 31) % ,RSD=2 76% (n=6)。健康人血清中冰片含量在15min左右达血药浓度高峰。结论 :建立的气相色谱法可靠、灵敏、简便 ,可较好地用于临床含冰片制剂的体内药代动力学研究     

血浆中立克命衍生化毛细管气相色谱法测定

该文研究了血浆中立克命的提取、衍生化和毛细管气相色谱分离测定的方法。其检测限为10~(-8)克;回收率为75.0±6.74×10~(-3)%;变异系数为0.90%(n=6)。本法简便、快速灵敏,可望用于临床立克命中毒者体内毒物分析。     

天然冰片(天然右旋龙脑)在眼科应用优于合成冰片

<正>天然冰片按旋光不同分天然右旋龙脑和天然左旋龙脑,眼科常用的是天然右旋龙脑;合成冰片含龙脑和异龙脑,《中国药典》(2015年版)收载了天然冰片(右旋龙脑)和合成冰片~([1])。天然冰片(d-Bormeo1)自古就是一种珍贵药材和名贵香料,为樟科植物樟Cinnamomum cam phora(L.)Presld的新鲜枝、叶经提取加工制成。梁(公元500年前后)以来历代本草多数以龙脑香命名,故亦称之龙脑香冰片。天然冰片广泛应用于食品、化妆品、医药等领域。云南     

气相色谱法测定赛胃安胶囊中冰片(龙脑与异龙脑)的含量

目的为了完善和提高赛胃安胶囊的产品质量,适应目前对含冰片中成药的质控要求。方法用气相色谱法建立以龙脑、异龙脑为对照品测定冰片的含量方法。色谱柱:A g ilent 1237032 DB-WAX 30m×0.32nm×0.25μm石英毛细管色谱柱,柱温:程序升温。结果龙脑、异龙脑在各自的浓度范围内线性关系良好。结论该方法可行,重复性好,能有效地控制该制剂的质量。     

手性毛细管柱气相色谱法测定复方牛黄消炎胶囊中冰片的含量

目的 建立手性毛细管柱气相色谱法同时测定复方牛黄消炎胶囊中异龙脑、左旋龙脑、右旋龙脑3个成分的含量.方法 采用CYCLO-SIL-B手性毛细管柱(30m×0.25mm,0.25μm),程序升温(初始温度120℃,保持12min,以20℃/min升温至最终温度200℃,保持5min),FID检测器温度220℃,进样口温度200℃,载气为高纯N2,进样量1.0μL,进样分流比5:1.结果 异龙脑、左旋龙脑、右旋龙脑质量浓度分别在3.000~150.0μg·mL-1(r=0.9999)、1.602~80.10μg·mL-1(r=1.0000)、3.143~157.2μg·mL-1(r=1.0000)范围内与峰面积线性关系良好;平均回收率(n=6)分别为99.3%(RSD=1.8%),102.6%(RSD=2.0%),96.2%(RSD=1.9%);不同厂家复方牛黄消炎胶囊中异龙脑、左旋龙脑、右旋龙脑3个主要成分的含量范围分别为2.18~5.38、2.39~3.47、1.64~5.48mg·g-1.结论 该方法 快速、准确,精密度良好,可用于复方牛黄消炎胶囊中冰片的含量测定.     

GC-MS法测定冰硼含片中冰片的含量

目的:建立以气相色谱-质谱联用技术测定冰硼含片中冰片含量的方法。方法:色谱柱为DB-5型石英毛细管(30m×0.32mm×0.25μm),样品用乙醚超声提取,采用选择离子监测(SIM)法定量。结果:冰片检测浓度在10.0~500.0μg.mL-1范围内与峰面积积分值呈良好的线性关系(r=0.999 9);平均加样回收率为98.55%,RSD=1.13%(n=6);最低检测限为10pg。结论:本方法简便、快速,结果准确,可用于冰硼含片的质量控制。     

气相色谱法测定复方蛇脂软膏中龙脑(冰片)的含量

目的为了完善和提高复方蛇脂软膏的产品质量,适应目前对含冰片中成药的质控要求。方法用气相色谱法建立以龙脑为对照品测定冰片的含量方法。结果测定得龙脑加样回收率为101．63％,RSD=0．9％。结论经研究建立了本品的龙脑(冰片)含量测定方法。     

手性毛细管柱气相色谱法测定冰硼散中冰片的含量

目的 建立手性毛细管柱气相色谱法同时测定冰硼散中异龙脑、左旋龙脑、右旋龙脑的含量.方法 采用气相色谱法、手性毛细管柱;柱温为120℃;进样口温度200℃;检测器温度220℃.结果 右旋龙脑在0.01～0.39 mg· mL-1与峰面积线性关系良好,r=0.999 9;左旋龙脑在0.01～0.38 mg·mL-1与峰面积线性关系良好,r=1.000 0;异龙脑在0.01～0.40 mg·mL-1与峰面积线性关系良好,r=1.000 0.结论 该方法快速,准确,精密度高,可测定以各种“冰片”投料生产的冰硼散中冰片的含量.     

TOXIC AND CARCINOGENIC EFFECTS OF PARENTERAL AND PERCUTANEOUS ATP AND ITS IRON COMPLEX

ABSTRACT

The long term effects of percutaneous, subcutaneous and intraperitoneal administration of sodium–ATP (NaATP) and ferric iron–ATP (FeATP) were studied on an animal model. Both compounds induce a generalized lymphoadenitis which in the case of FeATP led to lymphomas. The analytical study of the involved target tissues showed intracellular composition changes that result from the impairment of the cell membrane permeability. The morbidity and mortality rate were higher with FeATP which seems to be the result of two different, in intensity and duration, interactions with the cell plasma membrane. The influence of the changes in cellular calcium homeostasis, and its relationship with carcinogenesis and immuno response are discussed.     

苦参碱及氧化苦参碱的药代动力学与药效动力学

以QTc延长率为效应指标,用药代动力学-药效动力学结合模型对苦参碱、氧化苦参碱iv后在免体内的处置和效应动力学作定量分析,两药的血浓时程均符合二房室模型,两药的效应与效应室浓度之间的关系均符合S形E_max模型。两药彼此的药动学和药效学性质均有明显差异,但它们各自的劳动学和药效学性质在所用剂量范围内均为非剂量依赖性。     

HPLC和~1HNMR分析确定cis－A－和cis－B－羟甲芬太尼的组成和构型

羟甲芬太尼（１）是一个强效的镇痛剂和高亲和、高选择性的阿片μ受体激动剂。通过ＨＰＬＣ和１ＨＮＭＲ分析，ｃｉｓ－Ａ－ｌ被确定为由等量的ｃｉｓ－（＋）－（３Ｒ，４Ｓ，２＇Ｓ）－ｌ和：ｃｉｓ－（—）－（３Ｓ，４Ｒ，２＇Ｒ）－１组成的外消旋体，ｃｉｓ－Ｂ－ｌ被确定为由等量的ｃｉｓ－（—）－（３Ｒ，４Ｓ，２＇Ｒ）－１和ｃｉｓ－（＋）－（３Ｓ，４Ｒ，２＇Ｓ）－１组成的外消旋体。     

LIVER ALCOHOL AND ALDEHYDE DEHYDROGENASE: INHIBITION AND POTENTIATION BY HISTAMINE AGONISTS AND ANTAGONISTS

1. The in vitro effects of histamine, some other Hi- and H₂-receptor agonists and some antagonists were studied on the specific activities and kinetics of rat liver alcohol dehydrogenase (ADH), and cytoplasmic and mitochondrial liver aldehyde dehydrogenase (ALDH). 2. Histamine (H₁- and H₂-agonist) non-competitively inhibited ADH and ALDH, 2-(2-aminoethyl) pyridine (Hi-receptor agonist) non-competitively inhibited ADH. There were no changes of cytoplasmic and mitochondrial liver ALDH activities in the presence of 2-(2-aminoethyl) pyridine. 3. Betazole (H₂-receptor agonist) produced a competitive inhibition of mitochondrial ALDH but not of ADH or cytoplasmic ALDH. 4. Diphenhydramine (H₁-receptor antagonist) non-competitively inhibited ADH at a lower concentration. It stimulated mitochondrial ALDH activity without changes in cytoplasmic ALDH from control values. 5. Burimamide (H₂-receptor antagonist) produced a biphasic and dose-dependent stimulation and non-competitive inhibition of ADH and it non-competitively inhibited ALDH in both cytoplasmic and mitochondrial fractions. Metiamide (H₂-receptor antagonist) non-competitively inhibited all ADH and ALDH of both liver fraction studied. 6. It is concluded that liver ADH and ALDH activity can be altered by compounds which affect both Hi- and H₂-histamine receptors and that these compounds may cause an in vivo potentiation and/or reduction of the toxic effect of ethanol.     

冰毒吸食者焦虑抑郁情绪和自我概念的测评及相关分析

目的:了解冰毒吸食者焦虑抑郁情绪和自我概念状况,探讨二者之间的关系,为临床心理干预提供依据。方法:采用抑郁自评量表(SDS),焦虑自评量表(SAS)和田纳西自我概念量表(TSCS)对36例强制戒毒的冰毒吸食者(研究组)和36例健康人群(对照组)进行调查,将结果进行统计学处理分析。结果:(1)研究组SDS,SAS评分明显高于对照组,差别具有统计学意义(P<0.01);(2)TSCS评分比较,研究组除自我批评因子分高于对照组外,其余各因子分均低于对照组,差异具有统计学意义(P<0.01);(3)TSCS与SAS和SDS之间具有高度相关性(r=0.411-0.462,P<0.01)。结论:冰毒吸食者焦虑抑郁情绪明显,表现为消极的自我概念;焦虑抑郁情绪影响自我概念。临床治疗中应关注戒毒者负性情绪和自我概念,采取有效措施帮助他们消除负性情绪,树立积极的自我概念,促进心理康复。     

TOXICOKINETICS AND EFFECTS OF FIBROUS AND NONFIBROUS PARTICLES

Chronic inhalation of fibrous and nonfibrous particles by rats at high concentrations results in lung tumor formation if the particles are poorly soluble in the lung. Even rather benign nonfibrous particles such as TiO 2 produce this result. One significant change during a chronic inhalation exposure of poorly soluble particles of low cytotoxicity (PSP) is an impairment of normal clearance mechanisms in the alveolar region of the lung in rats, resulting in a continued buildup to high lung burdens accompanied by chronic alveolar inflammation, fibrosis, and mutational events. Since these are obviously high-dose effects, questions about their extrapolation to humans exposed to much lower concentrations have been raised. Results of key studies reported for chronic inhalation of PSP in rats indicate that mechanisms of PSP-induced lung tumors at high doses do not operate at low dose levels. Furthermore, the existence of two thresholds can be postulated: One is a dosimetric threshold for the endpoint alveolar macrophage-mediated clearance, which is related to lung particle overload. The other is a mechanistic threshold for the endpoint mutation, which is determined by the level of antioxidant defenses to counter-balance reactive oxidant species released by activated inflammatory cells. A no-observed-adverse-effect level (NOAEL) could therefore be based on avoiding alteration of the toxicokinetic of the particles such that the lung burdens stay below the dosimetric threshold. The suggestion that PSP-associated organic compounds (e.g., diesel particulate matter) contribute to the lung tumor responses in rats observed in chronic inhalation studies is not supported by experimental data from in vivo studies. It can be concluded that high-dose rat lung tumors due to PSP should not be used for low-dose extrapolations, and no significant contribution to human lung cancer risk can be predicted from levels of PSP below lung overload. With respect to the pulmonary toxicokinetics of inhaled fibrous particles, the biopersistence of long fibers (>20 µm) which cannot be phagocytized by alveolar macrophages is a key parameter related to long-term carcinogenic effects. Long fibers with a very low biopersistence should not be considered as carcinogenic. Since the clearance kinetics of fibers can generally be described by a biphasic or multiphasic pattern - fast initial and slow final phase - it is essential that the slow phase of the retention kinetics of fibers longer than 20 µm is considered in a biopersistence assay. Based on the results of such assay, fibers can be classified into one of two categories: a biopersistent fiber that cannot be dissolved in the lung within an acceptable time period; or a biosoluble fiber when even long nonphagocytizable fibers will be disappearing rapidly from the lung. However, in addition to biopersistence, it should be mandatory to evaluate fiber toxicity in an appropriate assay relative to a fiber whose long-term effects are well known. Moreover, for organic fibers it is likely that different rules may have to be established for characterization of their toxic and carcinogenic potential.     

顶头孢霉229与12的分生孢子及原生质体的形成和再生

头孢菌素产生菌顶头孢霉菌株229的沉没培养或斜面培养都可形成分生孢子,并可用普通滤纸将它们与菌丝及节孢子分开,但是它们成活率极低.这种成活的分生孢子的数量与培养基成分有关.菌丝培养基成分对制备顶头孢霉原生质体有显著影响.用一种MM培养基培养的菌丝,不经巯基化合物预处理,酶解(1%纤维素酶)3小时后,可得到大量原生质体.原生质体的再生频率为1.8～4.6%.与分生孢子形成的菌落相比,原生质体再生菌落的产抗生素能力显示出较大的变异性.本文还讨论了山梨醇与Nikkomycin对菌丝生长形态及原生质体形成的影响.     

珍珠母贝中糖胺聚糖的提取分离纯化

目的:对马氏珍珠母贝中提取、分离得到的糖胺聚糖(glycosam inog lycans,GAG)进行化学组分研究。方法:样品经还原、水解和乙酰化,采用气相色谱-质谱法定性测定。结果:测定出马氏珍珠母贝中经提取、分离得到的GAG中的3种主要成分,其骨架结构分别与(硫酸乙酰)肝素、(硫酸)软骨素和透明质酸相符。结论:马氏珍珠母贝中提取分离的糖胺聚糖中含有肝素、软骨素和透明质酸。