HPLC法测定耆鹿逐痹胶囊中补骨脂素和异补骨脂素的含量

ＨＰＬＣ法测定耆鹿逐痹胶囊中补骨脂素、异补骨脂素的含量。补骨脂素１．０～６．０μｇ／ｍｌ范围内呈线性关系，回收率为１００．９％（ＲＳＤ＝２．０％）；异补骨脂素１．８～１０．８μｇ／ｍｌ范围内呈线性关系，回收率９９．１％（ＲＳＤ＝１．９％）。     

高效液相色谱法测定人血清中头孢呋辛浓度

作者建立了快速、简便测定人血清中头孢呋辛反相高效液相色谱法（ＨＰＬＣ法），采用５×２００ｍｍ不锈钢柱，内填１０μｍＹｗＧ－Ｃ＿１８Ｈ＿３７固定相，流动相甲醇：水：冰醋酸（２８：７１：１ｖ／ｖ），流速１．２ｍｌ／ｍｉｎ，以头孢噻肟为内标物，紫外检测波长２９０ｎｍ，用１０％三氯醋酸作蛋白沉淀剂，与血清之比为１：２（Ｖ／Ｖ）。头孢呋辛的日内平均相对回收率为１００．３４％±６．６０％，日间平均相对回收率为９９．６９％±６．３３％。头孢呋辛最低检测限为２ｎｇ，最低检测浓度为０．２μｇ／ｍｌ，在０．２５～１０μｇ／ｍｌ度范围内线性良好，相关系数ｒ＝０．９９９９。     

地高辛血药浓度监测结果分析

目的：为我院合理使用地高辛提出可靠依据。方法：用放射免疫测定法监列次心衰患者应用地高辛治疗过程中的血药浓度。结果：０．８～２．０ｎｇ／ｍｌ占４４．０５％;〈０．８ｎｇ／ｍｌ占３４．５２％;〉２．０ｎｇ／ｍｌ２１．４３％。绫血药浓度以０．８～２．０ｎｇ／ｍｌ为宜。     

高效液相色谱法测定人血清中盐酸马普替林的浓度

本文建立了反相高效液相色谱法测定人血清中马普替林浓度的方法。本法用ＺｏｒｂａｘＯＤＳＣ１８色谱柱，以甲醇－水－氨水（５ｍｏｌ／Ｌ）－１０％醋酸铵＝４００∶７５∶１０∶１为流动相，检测波长为２５４ｎｍ，流速０．８ｍｌ／ｍｉｎ，线性范围２０～２４００ｎｇ／ｍｌ（ｒ＝０．９９９７），平均回收率为９８．０％±３．９％，日内与日间的标准差分别为３．２％和４．９％     

高效液相色谱法测定痛特灵霜中双氯芬酸的含量

本文采用ＨＰＬＣ法，建立了痛特灵霜中双氯芬酸的含量测定方法。用地塞米松为内标，样品加超纯水超声振荡提取后，用０．４５μｍ滤膜滤过，进样１０μｌ，采用国产ＹＷＧ－Ｃ＿（１８）柱分离，甲醇：水：醋酸（８０：２０：２）的混合溶液为流动相，２７５ｎｍ波长处检测。样品保留时间为４．６３ｍｉｎ。标准曲线浓度在０．５～４０μｇ／ｍｌ范围内线性关系良好（ｒ＝０．９９９９）。最低检测浓度为０．１２５μｇ／ｍｌ。方法的绝对回收率平均为９８％（ｎ＝６），ＲＳＤ为１．８％。相对回收率平均为９９．８％（ｎ＝６），ＲＳＤ＝１．０％。日内ＲＳＤ为０．５％～１．８％，日间ＲＳＤ为０．８％～６．５％。测定三批样品，平均百分含量为９７．９９％。     

双氯芬酸钠对大鼠足跖肿胀的抑制作用及其与肿胀组织中药物浓度的关系

目的：观察双氯芬酸钠对鹿角菜所致大鼠足跖肿胀的抑制作用及其与肿胀组织和血浆中药物浓度的关系。方法：足跖皮下注射１ ％ 鹿角菜制备大鼠足跖肿胀模型,观察双氯芬酸钠对足跖肿胀的抑制作用,并采用高效液相色谱法测定该模型中足跖肿胀组织和血浆中的双氯芬酸钠浓度,分析其药动学特征。结果：灌胃给予双氯芬酸钠（１０ ｍｇ·ｋｇ － １） 对足跖浮肿的抑制率为３２ ％ ～５７ ％ ;消除相中双氯芬酸在足跖肿胀组织中的浓度高于血浆,消除较血浆缓慢, Ｔ１／２ 分别为３ ．４ ｈ 和１ ．５ ｈ ,消除速率常数 Ｋ 分别为０ ．２０６ ５ 和０ ．４７３ ３ ,注射鹿角菜后的 Ａ Ｕ Ｃ０ ～ Ｔｎ 分别为９ ．４７５ ５ μｇ·ｍｌ－ １·ｈ 和１ ．８３ μｇ·ｍｌ－ １·ｈ 。结论：双氯芬酸钠对大鼠足跖肿胀抑制作用的延长效应与药物在肿胀组织中蓄积相关。     

应用反相高效液相色谱法测定马钱子胶囊中马钱子碱的血药浓度

用反相高效液相色谱法测定了马钱子碱的血药浓度，流动相为甲醇与０．０１２５Ｍ磷酸二氢钠（ｐＨ＝５．６）检测波长为２６６ｎｍ，色谱柱为ＵｌｔｒａｓｐｈｅｒｅＴＭＯＤＳ柱，线性范围为０１～１０．０ｕｇ／ｍｌ，日内变异系数为１．９～２．５％，日间变异系数为３．９％～６．２％，最低检测限为０．０２ｕｇ。     

乌苯美司对体外人白细胞介素－2生成及受体表达的促进作用

乌苯美司（乌比美克）１０～１００μｇ／ｍｌ能促进人外周血淋巴细胞分泌ＩＬ－２；而０．０１～０．１μｇ／ｍｌ则能增强人外周血淋巴细胞表达ＩＬ－２受体以及对ＩＬ－２发生反应的能力；在０．０１～１００μｇ／ｍｌ范围内，乌苯美司对人血清中ＩＬ－２抑制物活性无明显影响。     

应用反相高效液相色谱法测定马线子胶囊中马钱子碱的血药浓度

用反相色效液相色谱法测定了马钱子碱的血药浓度，流动相为甲醇与０．０１２５Ｍ磷酸二氢钠（ｐＨ＝５．６）检测波长为２６６ｎｍ，色谱柱为Ｕｌｔｒａｓｐｈｅｒｅ＾ＴＭＯＤＳ柱，线性范围为０．１～１０．０ｕｇ／ｍｌ，日内变异系数为１．９～２．５％，日间变异系数为３．９％～６．２％，最低检测限为０．０２ｕｇ。     

新型双氯芬酸钠缓释片的人体相对生物利用度研究

８名健康男性志愿者单剂量交叉口服１００ｍｇ受试双氯芬酸钠缓释片、扶他林或ＶｏｌｔａｒｅｎＳＲ１００后,Ｔｍａｘ分别为２．４±１．０、２．１±０．５和４．４±１．８ｈ;Ｃｍａｘ分别为６０２．６±９２．８、３３３７．６±１０８８．２　７６１．０±３４２．０ｎｇ／ｍｌ;ＭＲＴ分别为１３．２±４．８、２．９±０．８和７．９±１．９ｈ;ＡＵＣ０分别为４８６６．２±６４４．６、５３１４．３±５３４．３和４８２９．１±５８２．８ｎｇ／（ｍｌ－１·ｈ）;双氯芬酸钠缓释片和ＶｏｌｔａｒｅｎＳＲ１００相对于扶他林的生物利用度分别为８８．３±１３．２％和８６．３±１２．６％。另８名志愿者交叉口服受试双氯芬酸钠缓释片（１００ｍｇ,ｐｄ）和扶他林（５０ｍｇ,ｂｉｄ〕,连服５天。Ｃｍａｘ分别为５９３．９±１３４．１、１２４７．８±５２７．５ｎｇ／ｍｌ,峰谷波动率（ＰＴＦ）分别为３．３±１．２、５．３±２．１。本研究将为新型双氯芬酸钠缓释片的临床应用提供依据。     

2005年北京地区海洛因毒品中稀释剂的分析

目的:对2005年收缴的"零包"海洛因毒品中的稀释剂进行分析。方法:准确称取可疑毒品适量,用SKF525做内标,用乙醇配制成1.0mg.kg-1的样品溶液,取1μl进行GC/MS分析。结果:在408份"零包"海洛因毒品中,检测出含有机稀释剂的323份,占79.2%。检测出的有机稀释剂是烟酰胺(231份,占总份数的56.6%)、咖啡因(135份,占总份数的33.1%)、扑热息痛(51份,占总份数的12.5%)、氨基比林(39份,占总份数的9.6%)、茶碱(37份,占总份数的9.1%)、非那西丁(29份,占总份数的7.1%)、脑复康(28份,占总份数的6.9%)、镇静催眠药(10份,占总份数的2.4%)、曲马朵及其它(10份,占总份数的2.4%)。结论:北京地区"零包"海洛因毒品中多数有有机稀释剂,且种类繁多。脑复康是一个新发现的稀释剂。     

PRESENCE OF CHOLINOCEPTORS IN MESENCEPHALIC RAPHE NUCLEI CONCERNED IN THERMOREGULATION IN RABBITS

1. The thermal effects of cholinomimetics and cholinoceptor blocking agents microinjected into mesencephalic nucleus raphe medianus (NRM) were investigated in rabbits to determine the nature and role of these cholinoceptors in thermoregulation. 2. Microinjection of cholinoceptor agonists, carbachol and pilocarpine, into NRM resulted in significant hyperthermia which could be blocked by local pretreatment with chlorisondamine (a nicotinic receptor blocker) as well as by ethybenztropine (a muscarinic receptor blocker). 3. Intracerebroventricular pretreatment with LM 5008 (serotonin reuptake blocker) significantly inhibited the carbachol-induced hyperthermia. 4. Both nicotinic and muscarinic cholinoceptors are present in mesencephalic NRM which may be involved in thermoregulation in rabbits. Activation of these cholinoceptors in NRM results in hyperthermia which seems to be due to an inhibition of a serotonin sensitive hypothalamic heat loss mechanism.     

CATECHOLAMINE INACTIVATION IN UTERINE TISSUES: CHANGES IN PREGNANCY IN THE RAT

1. In vitro metabolism of [3H]-(-)-noradrenaline (3H-NA), 0.2 mumol/l, was measured in rat endometrial and myometrial slices at different stages of gestation and compared with that in dioestrous rats. Metabolism of 3H-NA, 0.2 mumol/l, was measured in rat placental slices from day 14 of gestation onwards. 2. 3H-NA was metabolized mainly by deamination in rat myometrium, with [3H]-3,4-dihydroxyphenylethylene glycol, (3H-DOPEG) being the major metabolite. Cocaine, 30 mumol/l, inhibited 3H-DOPEG formation and the amount of 3H-NA remaining in the tissue. O-methylated metabolite formation was unaffected by cocaine. 3. O-methylation and deamination were equally active pathways for metabolizing 3H-NA in rat endometrium. O-methylation to [3H]-normetanephrine (3H-NMN) predominated in the placenta. In both tissues O-methylated metabolite formation was inhibited by 30 mumol/l cocaine. 4. In myometrium, metabolite formation per gram was constant in the first half of pregnancy and was similar to that in dioestrous animals. By day 17 of gestation, however, [3H]-O-methylated deaminated metabolites (3H-OMDA), comprising 3-methoxy, 4-hydroxy-phenylethylene glycol and vanillylmandelic acid, and 3H-NMN formation were less than in dioestrous animals. 5. Endometrial 3H-NMN and 3H-DOPEG formation per gram were higher in rats at day 5 of gestation than in dioestrous rats but metabolite formation per gram declined thereafter to reach values equal to (3H-DOPEG) or less than (3H-OMDA and 3H-NMN) those in dioestrous rats. 6. 3H-NMN and 3H-OMDA formation per gram decreased from day 14 to day 20 of gestation in rat placentae.(ABSTRACT TRUNCATED AT 250 WORDS)     

PRESSOR RESPONSIVENESS IN STEROID-INDUCED HYPERTENSION IN MAN

Pressor responsiveness to angiotensin II (AII) and phenylephrine (PE) was examined before and after 5 days of ACTH (1 mg, i.m., daily) or hydrocortisone (200 mg, orally, daily) in six normotensive men. Pulse pressure was higher prior to PE than AII infusion, presumably due to feeding. Systolic blood pressure (SBP) was increased by both ACTH and hydrocortisone treatment, but more by ACTH. There were no significant changes in AII pressor responsiveness with either ACTH or hydrocortisone. ACTH increased pressor responsiveness to PE at 1.35 and 2 micrograms/kg per min, and hydrocortisone at 0.6-2 micrograms/kg per min, with falls in pulse rate at 0.3-0.9 micrograms/kg per min. Changes in pressor responsiveness do not explain ACTH hypertension.     

HAEMODYNAMIC CHANGES IN ACTH-INDUCED HYPERTENSION IN SHEEP

1. ACTH (20 μg/kg per day) produced an elevation in blood pressure associated with an increase in cardiac output in conscious sheep, due in the first 72 h to a rise in heart rate. Stroke volume did not rise until the fourth day of ACTH treatment. 2. Calculated total peripheral resistance did not change. 3. Intravenous administration of acebutolol prior to and during ACTH administration did not modify the rise in blood pressure, but this was associated with a rise in total peripheral resistance. 4. These studies show that while ACTH-induced hypertension is usually associated with increased cardiac output, rather than total peripheral resistance it still occurs, but is associated with a rise in total peripheral resistance if the rise in cardiac output is prevented by /J-adrenoreceptor blockade.     

反式曲马朵在大鼠肝微粒体O-去甲基代谢中的立体选择性

目的研究反式曲马朵O-去甲基代谢的立体选择性.方法高效毛细管电泳法测定大鼠肝微粒体孵育液中反式曲马朵和O-去甲基曲马朵对映体的浓度,酶促动力学方法研究O-去甲基曲马朵对映体的生成.结果 (-)-O-去甲基曲马朵生成有较大的Vmax;反式曲马朵两对映体间存在相互作用,使(+)-O-去甲基曲马朵生成的Vmax明显减慢;奎宁及奎尼丁对(+)-O-去甲基曲马朵生成的抑制作用较强.结论反式曲马朵O-去甲基代谢有立体选择性,对映体间的相互作用及酶抑制剂使其立体选择性程度加强.     

INCREASE IN HAEMATOCRIT IN BORDERLINE HYPERTENSIVE MEN

1. Haematologic parameters were measured in untreated borderline hypertensive (BHT) men, and weight and age matched with normotensive men to determine whether previously described increased haematocrit (Hct) in established hypertension is evident in borderline hypertension. 2. Haematocrit was significantly increased in BHT men (mean 0.46, s.d. 0.032) compared with normotensive men (mean 0.43, s.d. 0.014) and correlated significantly with mean arterial pressure in this group (r = 0.67, P= 0.036) independent of weight. 3. The correlation of blood pressure with Hct in BHT men supports the concept that increased Hct may contribute to increased blood viscosity and thus to raised arterial pressure.     

国产阿克拉霉素A的体内外抗肿瘤作用

国产阿克拉霉素A(aclacinomycin;ACM-A)能明显抑制体外培养小鼠白血病P₃₈₈和人体胃癌SGC-7901细胞的生长。在0.01 μg/ml浓度时能抑制65.4%的克隆形成,ED₅₀为0.0085μg/ml。ACM-A对白血病小鼠有显著治疗作用,延长小鼠生命时间143%,并有半数小鼠获得治疗。对Ehrlich腹水癌和肉瘤-180也有较强的抑制作用,对肉瘤-180的作用与adriamycin相似。ACM-A主要抑制³H-TDR和。H-UR分别参人人体胃癌细胞的DNA和RNA;大剂量时对蛋白质合成也有影响。P₃₈₈细胞实验中证明ACM-A对DNA合成的抑制程度与adriamycin相似,低于daunomycin。     

藿胆丸薄层色谱鉴别方法的改进

本文对《中国药典》收载的藿胆丸的薄层鉴别（2）进行了改进，使操作过程简便、快速，同时减少了溶剂的用量，避免了高浓度碱液对玻璃器皿的损伤。