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。     

X-射线粉末衍射技术在多晶型药物定量分析中的应用

X-射线粉末衍射技术（X-ray powder diffraction,PXRD）是研究药物多晶型的主要手段之一。药物在生产过程中有时会发生晶型的转变,只进行晶型的定性分析已经不能满足现代药物的质量控制要求。本文通过查阅中外文献,对PXRD在多晶型药物定量分析中的具体应用进行了综述。采用PXRD定量分析药物的多晶型状态,将使实际工艺中药物的多晶型现象得到更明确的阐述和更合理的控制,从而建立科学的质量控制体系和严格的药物质量标准。     

道地产区湖北应城石膏X-射线衍射专属特征峰的分析研究

摘 要 目的： 确定道地产区湖北应城石膏X-射线衍射专属特征峰。 方法: 应用X-射线衍射方法,对不同产地中药石膏进行指纹图谱分析,确定共有峰;并对道地产区湖北应城石膏的特征峰进行专属性鉴别。结果:获得不同产地石膏X-射线衍射指纹图谱,确定16个平均值共有峰;道地产区湖北应城产淡黄色纤维状石膏,其X-射线衍射图谱中具有两个专属特征峰,晶面间距（d）分别为1.68与1.51。 结论: 道地产区湖北应城石膏X-射线衍射专属特征峰的确定,可区别其他产地石膏,为进一步评价中药石膏的品质提供依据。     

褪黑素的抗肿瘤作用机制和化疗增敏作用研究现状

褪黑素(MLT)是由松果腺合成与分泌的神经内分泌活性物质,其以色氨酸为原料,经过羟化、脱羧及N-乙酰转移酶等的催化后而最终形成.MLT可迅速进入血液循环,分布到全身各部位发挥生理活性.现已证实,MLT除了可保证正常生物节律、调节内分泌腺的功能、抗应激和延缓衰老外,与肿瘤的发生、发展及治疗亦有着密切的关系[1].     

褪黑素的抗肿瘤作用机制和化疗增敏作用研究现状

褪黑素(MLT)是由松果腺合成与分泌的神经内分泌活性物质,其以色氨酸为原料,经过羟化、脱羧及N-乙酰转移酶等的催化后而最终形成。MLT可迅速进入血液循环,分布到全     

粉末X-射线衍射法测定阿托伐他汀钙片剂中晶型Ⅰ的含量

目的 应用粉末X-射线衍射技术对片剂中阿托伐他汀钙的晶型Ⅰ含量进行定量分析。方法 采用缩短扫描范围,降低扫描速度,提高步进扫描时间的精细扫描方法,建立了晶型Ⅰ含量测定的线性方程y=3179.3x-304.56（r=0.992 3）,并经方法学验证。结果 对2个规格6个批号片剂的晶型Ⅰ含量进行了测定,结果发现片剂中晶型Ⅰ含量有一定的变化。结论 本法操作简单,在辅料没有干扰的情况下可用于片剂中阿托伐他汀钙晶型Ⅰ含量的定量分析。     

厄贝沙坦多晶型X-射线粉末衍射定量分析

目的 建立厄贝沙坦晶型原料药的晶型含量分析方法,为药品晶型质量控制提供技术支撑.方法 采用X-射线粉末衍射法表征厄贝沙坦晶型A和晶型B.分别选取晶型A的特征衍射峰2θ=4.65°和晶型B的特征衍射峰2θ=-7.99°的峰面积比值为定量参数,建立标准曲线检测晶型B的含量.结果 晶型B在晶型A和晶型B混合物中含量为2％～5...     

X-射线粉末衍射法测定奥美拉唑钠环糊精包合片的包合率

目的：建立β-环糊精奥美拉唑钠包合片包合率的测定方法。方法：X-射线粉末衍射-加入标准法。结果和结论：该法可作为内控标准检测包合率。     

POTENTIATION OF THE NEGATIVE CHRONOTROPIC AND INOTROPIC EFFECTS OF ADENOSINE BY 2-PHENYLAMINOADENOSINE

1. Effects of 2-phenylaminoadenosine on SA nodal pacemaker activity and atrial contractility were studied, using eleven isolated, blood-perfused dog atrial preparations. The compounds were administered via the cannulated sinus node artery of the isolated atrium. 2. 2-Phenylaminoadenosine induced negative chronotropic and inotropic effects and was 100 times less potent than adenosine in this action. 3. The interaction between adenosine and 2-phenylaminoadenosine was studied. 2-Phenylaminoadenosine potentiated the effect of adenosine on atrial muscle, but not that of acetylcholine.     

POTENTIATION OF ACTH HYPERTENSION IN MAN WITH SALT LOADING

ACTH 1 mg/day for 5 days raises systolic blood pressure (SBP) in normotensive and hypertensive subjects on a fixed electrolyte intake of 100 mmol/day sodium (Na) and potassium (K) (Whitworth et al. 1983). The present study examined the effect of Na intake in the high normal range on the haemodynamic and metabolic responses to ACTH. ACTH administration on a 200-300 mmol Na intake increased SBP by 35 mmHg (s.e.m. = 11, n = 5) compared with the 22 mmHg (s.e.m. = 4, n = 12) rise seen on a 100 mmol Na intake in our previous study. These studies suggest that the effects of adrenocortical steroids on blood pressure in man may be magnified by increasing dietary Na intake.     

柱前手性衍生化反相高效液相色谱法拆分地佐西平对映异构体的研究

用乙酰葡萄糖异硫氰酸酯(GITC)作柱前手性衍生化试剂,以反相高效液相色谱法成功地拆分了地佐西平对映异构体。在此基础上建立了地佐西平对映异构体纯度和血药浓度测定方法。已用于测定右旋地佐西平的光学纯度和小鼠血药浓度。     

GITC柱前手性衍生化HPLC测定吡喹胺光学异构体纯度

以乙酰葡萄糖异硫氰酸酯(GITC)作柱前手性衍生化试剂,用反相高效液相色谱法成功地拆分了吡喹胺(1,3,4,6,7,11b-六氢-2H吡嗪[2,1-a]并异喹啉-4-酮)光学异构体。在此基础上建立了测定吡喹胺光学异构体纯度的方法,并已用于d-和l-吡喹胺纯度的测定。     

POTENTIATION OF AN EFFECT OF ALLOPURINOL ON PYRIMIDINE METABOLISM BY CHLOROTHIAZIDE IN MAN

SUMMARY 1. Treatment with allopurinol leads to increased excretion of the pyrimidine compounds orotic acid and orotidine, and to increased levels in erythrocytes of the enzymes orotate phosphoribosyltransferase and orotidylate decarboxylase.
2. The effects of allopurinol on pyrimidine metabolism are enhanced by concurrent treatment with chlorothiazide.
3. This interaction between allopurinol and chlorothiazide does not appear to give rise to any disadvantageous effects. Knowledge of such interactions could lead to more rational drug therapy.     

手性药物对映体的环糊精手性流动相、手性固定相HPLC法拆分

使用β-环糊精(CD)作为手性流动相添加剂或手性固定相,采用反相高效液相色谱法首次拆分了抗胆碱能药物盐酸戊乙奎醚、盐酸苯环壬酯和盐酸卡马特灵。结果表明,3个手性药物4对对映体完全达到基线分离。求得其包络常数、包络比和分离度,并结合其他结构类似的化合物,从结构—分离因子关系的角度研究了其拆分机理。详细研究了影响容量因子和分离度的各种因素。     

RP－HPLC手性流动相添加剂法分析尿中氧氟沙星对映体

以Ｌ－苯丙氨酸为配合剂，Ｃｕ２＋为配合离子，建立了一种简便的手性配合交换ＲＰ－ＨＰＬＣ拆分氧氟沙星对映体的方法，该法已用于人尿中氧氟沙星对映异构体的分析。     

SYNERGISTIC POTENTIATION BY CAPTOPRIL AND PROPRANOLOL OF BRADYKININ-INDUCED BRONCHOCONSTRICTION IN THE GUINEA-PIG

1. Captopril (30 or 100 micrograms/kg intravenous (i.v.] in anaesthetized artificially ventilated guinea-pigs potentiated bronchoconstrictor responses to bradykinin, but not those to histamine or the thromboxane A2-mimetic U46619. 2. Propranolol (5 mg/kg, i.v.) potentiated bradykinin-induced broncho-constriction. The potentiated responses were further augmented by captopril. 3.The captopril-potentiated responses to bradykinin were inhibited during cyclo-oxygenase inhibition with indomethacin. Bronchoconstrictor responses to bradykinin, but not those to histamine or U46619, were reduced after thromboxane synthase inhibition with dazoxiben. The thromboxane A2 antagonist AH23848 inhibited bronchoconstrictor responses to bradykinin, arachidonic acid or U46619 whereas it did not affect those to histamine. 4. A kininase I inhibitor DL-2-mercaptomethyl-3-guanidinoethyl thiopropanoic acid caused no change in bronchoconstriction caused by bradykinin and did not alter the potentiated responses occurring after captopril. 5. Thus, confirmation has been obtained that bradykinin causes broncho-constriction in the guinea-pig indirectly, by release of eicosanoids. Thromboxane A2 is likely to be the major eicosanoid released, since the bronchoconstrictor effect of bradykinin was blocked by indomethacin, dazoxiben and AH23848. The intensity of the bronchoconstriction appears dependent on sympathetic influences mediated by beta-adrenoceptors. Kininase I, in contrast to kininase II apparently has little role in terminating the effects of bradykinin in the lung.     

2型糖尿病患者骨密度的变化

本文采用了高精度的双能Ｘ线骨密度仪对３０例２型糖尿病男性患者和３０例年龄、性别和体重指数相匹配的非糖尿病健康者腰椎（Ｌ２～４）和股骨近端骨密度进行了检测，发现糖尿病患者腰椎和股骨近端骨密度明显降低（Ｐ＜０．０１～０．０５），同时对其骨密度的变化与年龄、糖尿病病程的关系进行了分析。提示老年糖尿病患者骨丢失率增加，且随着病程的延长骨量丢失以腰椎椎体为著。     

RP-HPLC手性流动相添加剂法分析尿中氧氟沙星对映体

以L-苯丙氨酸为配合剂,Cu²⁺为配合离子,建立了一种简便的手性配合交换RP-HPLC拆分氧氟沙星对映体的方法,该法已用于人尿中氧氟沙星对映异构体的分析。