生牡蛎X射线衍射分析及指纹图谱的建立

目的:建立生牡蛎的X射线衍射指纹图谱,考察X射线衍射分析在生牡蛎质量检测与鉴别中的应用价值。方法:应用X射线衍射法对11批生牡蛎样品进行定性分析,比较其共有峰的夹角余弦和相关系数的相似度。结果:各生牡蛎样品X射线衍射共有峰的相似度均达到95%以上。结论:生牡蛎的X射线衍射分析方法专属性强、准确可靠,能全面、客观地反映其内在质量特征。     

中药材X-射线衍射图谱研究

为探讨中药材道地性的客观规律,以期建立相应的评估指标系统,本文选择常用中药材茜草类、贝母类、山药类三组样品,应用X-射线粉末衍射法进行图谱分析,获得了可用于标识中药材的衍射图形几何拓扑规律与图谱特征标记峰,由此观察到:不同产地茜草样品的相似性及其与欧茜草的差别;同属不同种贝母样品的相似性与差异;不同产地山药样品的相似性及与伪品的区别。本文结果预示着这一方法在揭示中药材道地性客观规律方面的广阔应用前景。     

X-射线粉末衍射法在药物研究和质量控制中的应用

随着新药评价标准的不断提高，要求原料药开发和仿制时重视对立体异构与晶型的研究；评价原料药的生物有效性研究中首先应予考虑的问题也是药物的多晶型。同一药物的不同晶型常引起疗效、生物利用度的不一致，在理化性质上体现为熔点、红外图谱、差热分析图谱以及X-射线衍射图谱等多方面的不同，从而在新药的开发和审批、药物的生产、质量控制、内外贸易等方面引发一系列问题。X-射线粉末衍射（XRD）法作为药物多晶型研究的主要手段，具有特异、准确、快速、操作简便的优点，正日益受到人们的重视，已广泛应用于药品的晶型分析，各国药典相继收载了这项技术。     

尼莫地平多晶型的研究

用不同有机溶剂重结晶制备了尼莫地平的两种晶型H和L,并通过红外光谱、X-射线粉末衍射、差热分析等方法得到证实。实验测定了尼莫地平两种晶型的溶解度曲线,并计算热力学数据。     

头孢曲松钠晶体结构与晶习预测的研究

差示扫描量热法(DSC)、傅立叶转换红外光谱(FT-IR)和X-射线粉末衍射(XRPD)研究表明实验室精制得到的头孢曲松钠晶体属单斜晶系,P21/c空间群。在Cerius2工作站SGIIRIX上应用能量最小化法确定了头孢曲松钠的晶体结构;基于BFDH、AE模型预测了头孢曲松钠晶体的晶习,其中AE模型预测的晶习与实际生长晶习相近,呈薄片状。实验定性考察了生长环境对头孢曲松钠晶习的影响。     

他唑巴坦中结晶水的研究

目的考察国产他唑巴坦中是否结合有结晶水。方法采用卡尔费休氏水分测定法、干燥失重、热重分析法、热差分析法、单晶X-射线衍射的方法对他唑巴坦中的水分进行研究。结果用不同的常规水分测定方法对同一批他唑巴坦测定的结果有明显的差异。结论国产他唑巴坦1分子结合有0.5分子结晶水,结晶水与他唑巴坦分子结合紧密。     

马来酸替加色罗的晶型研究

目的：研究马来酸替加色罗2种晶型的物理性质。方法：运用傅立叶变换红外光谱、拉曼光谱、热分析和粉末X-射线衍射法研究马来酸替加色罗的晶型。结果：运用不同的重结晶溶剂，马来酸替加色罗可形成2种晶型，这2种晶型的熔点一致，它们的DSC和TG曲线都相同。但他们的红外光谱、拉曼光谱和粉末X-射线衍射图谱均存在着差异。结论：红外光谱、拉曼光谱和粉末X-射线衍射图谱可作为鉴别马来酸替加色罗晶型的方法。     

牡蛎提取物抗肿瘤作用的实验研究

以每天０．２ｍｌ剂量的牡蛎提取物连续１０ｄ胃饲荷ＨＡＣ鼠肝癌的Ｂａｌｂ／ｃ小鼠，发现主因瘤而下降的指标明显回升，包括总Ｔ细胞数，Ｔ辅助细胞百分比，丝裂原诱发的淋巴细胞转化强度，和ＮＫ细胞的杀伤活性。瘤重亦较对照组明显减轻，宿主成活期处长。用相同剂量的牡蛎提取物胃饲长有人结肠癌的裸鼠共１５ｄ，发现肿瘤体积明显减少为对照的４４．６％。     

白木香酸晶体结构的研究

白木香酸(C₁₅H₂₄O₃)的晶体属单斜晶系,空间群C2,晶胞参数为:a=12.150(3),b=10.827(4),c=11.344(4),B=111.78(2)°,Z=4,理论密度Dc=1.208 gcm^-3。在“RIGAKU”衍射仪上收集强度数据;用直接法(MULTAN 80)解结构;全矩阵最小二乘修正结构,对2052个衍射点,最终R=0.060;差值Fourier综合确定了氢原子位置。     

福建牡蛎软体的化学成份研究

目的 对福建牡蛎(Ostres rivularis Gould)所含之无机元素，有毒物质及氨基酸等，进行研究检测。方法 用原子吸收分光光度法、等离子光谱法及氨基酸分析仪进行分析。结果 本品分别含有17种游离氨基酸与复合氨基酸；并含有铁、镁等宏量元素与锌、锰及铜等微量元素，砷、铅含量小于2ppm而汞到小于1ppb。结论 本品含有丰富的氨基酸及有益于人体健康的微量元素与宏量元素。     

感音神经性耳聋者的脑灰质结构基于体素形态学的研究

目的利用基于体素形态学技术分析听力正常人志愿者与感音神经性耳聋患者之间的脑灰质差异。方法分别对24例听力正常人及24例感音神经性耳聋人进行常规T2-WI与三维(3D)快速扰相梯度回波(fast spoiled gradient echo,FSPGR)采集脑结构图像。用VBM技术运算,然后观察两组之间的脑质差异并显示出差异脑区的MNI坐标及差异容积,然后对所得数据进行相应统计学分析。结果感音神经性耳聋组脑灰质增多的区域有(P<0.01,Cluster size=40):左侧颞上回、右侧颞上回、左侧额下回、左侧中央前回、左侧中央后回、左侧扣带回、左侧小脑半球、左侧顶下小叶、左侧屏状核、左侧小脑前叶、右侧小脑前叶、右侧小脑后叶、右侧额下回。结论感音神经性聋人在左、右侧颞上回灰质增多,提示其听觉中枢皮质有结构重组。     

广州市中学教师与工厂工人咽喉疾病的对比研究

目的：对比分析广州市中学教师与工厂工人的咽喉疾病的发生情况,为教师的咽喉疾病提供针对性预防和治疗措施。方法：对广州市某中学的273名教师及某工厂的261名工人进行了咽喉疾病发病率和病种的调查,主要通过临床体检、问卷调查和耳鼻咽喉专科体检,对比分析调查结果。结果：教师咽喉疾病发病率为34.6%,相比工人的9.2%,具有统计学意义（P〈0.05）。结论：教师是咽喉疾病的高发人群,应加强对教师咽喉疾病防治的关注程度。     

巴洛沙星含量测定的三种方法及比较

目的建立了巴洛沙星含量测定的最佳方法。方法试验分别采用了0.1mol／l盐酸溶液为溶剂的紫外分光光度法、流动相为0.05m01／l构橼酸溶液一乙腈（80：20）的高效液相色谱法及冰醋酸为滴定溶剂，高氯酸为滴定液的非水溶液滴定法，进行了巴洛沙星含量测定的方法学研究。结果三种方法所得数据基本一致，为巴洛沙星的含量测定的有效方法。结论对该三种方法进行精确性、重现性及适用性比较，非水溶液滴定法准确快速、重现性良好、操作简单、无特殊设备要求，更适合用于巴洛沙星的含量测定。     

Prenatal Tobacco Exposure and Brain Morphology: A Prospective Study in Young Children

It is well known that smoking during pregnancy can affect offspring health. Prenatal tobacco exposure has been associated with negative behavioral and cognitive outcomes in childhood, adolescence, and young adulthood. These associations between prenatal tobacco exposure and psychopathology in offspring could possibly be explained by the influence of prenatal tobacco exposure on brain development. In this prospective study, we investigated the association between prenatal tobacco exposure, behavioral and emotional functioning and brain morphology in young children. On the basis of age and gender, we matched 113 children prenatally exposed to tobacco with 113 unexposed controls. These children were part of a population-based study in the Netherlands, the Generation R Study, and were followed from pregnancy onward. Behavioral and emotional functioning was assessed at age 6 with the Child Behavior Checklist. We assessed brain morphology using magnetic resonance imaging techniques in children aged 6–8 years. Children exposed to tobacco throughout pregnancy have smaller total brain volumes and smaller cortical gray matter volumes. Continued prenatal tobacco exposure was associated with cortical thinning, primarily in the superior frontal, superior parietal, and precentral cortices. These children also demonstrated increased scores of affective problems. In addition, thickness of the precentral and superior frontal cortices was associated with affective problems. Importantly, brain development in offspring of mothers who quit smoking during pregnancy resembled that of nonexposed controls (no smaller brain volumes and no thinning of the cortex). Our findings suggest an association between continued prenatal tobacco exposure and brain structure and function in school-aged children.     

镉对大鼠睾丸生化毒作用的研究

镉2.5mg/kg腹腔染毒2天后,大鼠血镉和睾丸镉含量明显升高,同时血浆丙二醛含量和乳酸脱氢酶同工酶(LDH-X)活性亦显著增高。在睾丸匀浆及线粒体丙二醛含量明显升高的同时,睾丸匀浆的LDH-X则随之明显降低。光镜检查间质内明显出血,曲细精管生精细胞萎缩性变性,数量减少。推测镉可诱发睾丸生精细胞线粒体膜的脂质过氧化作用。电镜检查也证实,染毒大鼠精原细胞线粒体大量膨胀、破损。     

Differences in caffeine and paraxanthine metabolism between human and murine CYP1A2

For the characterisation of murine models of CYP1A2 mediated metabolism in humans we compared the metabolism of caffeine and paraxanthine in human liver microsomes (LM) (two samples) and in LM from CYP1A2-null and wild-type mice. Inhibition experiments were carried out with the quinolones norfloxacin and pefloxacin and the substrate, caffeine. Additionally, in vivo pharmacokinetics of paraxanthine was determined in CYP1A2-null and wild-type mice. All LM produced the primary metabolites of caffeine and paraxanthine. In human LM, the main metabolite of caffeine was paraxanthine (K(M) 0.4 and 0.5 mmol L(-1)). In wild-type and CYP1A2-null mice LM, the main caffeine metabolite was 1,3,7-trimethylurate, but formation was not saturable. Apparent K(M) for paraxanthine formation from caffeine in wild-type and CYP1A2-null murine LM were 0.2 and 4.9 mmol L(-1), respectively. The main metabolite of paraxanthine was 1-methylxanthine in human (K(M) 0.13 and 0.2 mmol L(-1)) and in wild-type mice LM (K(M) 0.53 mmol L(-1)). In CYP1A2-null murine LM, the main paraxanthine metabolite was 7-methylxanthine. The quinolones competitively inhibited caffeine metabolism in human but not in wild-type or CYP1A2-null murine LM. No obvious differences were seen for blood pharmacokinetics and urinary metabolite excretion of paraxanthine between CYP1A2-null and wild-type mice. Thus, for paraxanthine, norfloxacin and pefloxacin interaction with CYP1A2 there were clear differences between mice and man. Our results suggest that an interspecies comparison is required for the metabolism of individual xenobiotics interacting with CYP1A2 prior to the use of mice models to predict its toxicity and/or pharmacological activity in man.     

东北银莲花属植物花粉形态的研究

应用光学显微镜和扫描电镜,对东北银莲花属（Ａｎｅｍｏｎｅ）的６种药用植物花粉形态特征作了比较观察．６种植物花粉形态种间区别主要在于花粉粒的大小、孔沟的数目及形态、沟膜的形态、表面文饰的排列     

对鼻腔淋巴瘤形态学及免疫组化表型的研究

目的:鼻腔是结外常发生淋巴瘤的部位之一.为探讨鼻腔淋巴瘤的形态学改变及临床特点及临床预后.方法:应用免疫组化方法及临床随访对42例鼻腔恶性淋巴瘤进行了组织学类型及临床治疗方法和预后的研究.结果:发现鼻腔恶性淋巴瘤以NK/T细胞淋巴瘤为主(21例),其次是T细胞淋巴瘤(非特异型)(9例),以及其他类型,弥漫性大B细胞淋巴瘤(3例),粘膜相关淋巴瘤(3例),浆细胞肉瘤(1例),粒细胞肉瘤(2例).结论:鼻腔可发生的淋巴瘤种类较多,其生物学行为存在较大差异,各类淋巴瘤其免疫表型各有其特点,是病理诊断的重要依据和鉴别诊断要点,同时是临床治疗的前提.     

A Study to Compare Bioequivalence Approach Between FDA and EMA in a Highly Variable Drug: Pinaverium Bromide Film Tablets

The aim of this study is to investigate pharmacokinetic parameters of test and reference film tablet formulations of a highly variable drug, pinaverium bromide, under fasting conditions and to assess their bioequivalence in accordance with the FDA and EMA criteria. A randomised open-label, single oral dose, three-sequence, three-period, semi-replicated, cross-over trial was conducted with 36 healthy subjects. The intrasubject variability of reference products for C_max and AUC_0-tlast was found to be more than 50%. While bioequivalence was proven according to the FDA reference scaled average bioequivalence approach with only 36 subjects, more than 200 subjects are required to demonstrate bioequivalence in accordance with the EMA bioequivalence guideline. It is believed that the EMA bioequivalence criteria are too stringent for highly variable drugs whose intrasubject variability are more than 30% for both C_max and AUC_0-tlast and that in consequence the EMA ought to revise their bioequivalence guidelines for such drugs in the future.