柳珊瑚酸的抗利尿作用

柳珊瑚酸(Sub)3.16mg/kg ig明显减少清醒大鼠的累积尿量,并提高尿Na~ ,K~ 浓度,给药24h作用仍然显著;Sub 0.4mg/kg iv也明显提高麻醉猫的尿Na~ ,K~ 浓度,但给药7h后作用不明显.     

茯苓对家兔利尿作用的观察

观察茯苓水煎醇沉液对兔的利尿作用。取雄性家兔24只随机均分Ⅳ组,兔称重全身麻醉后固定于手术台上,沿尿道口将导尿管插入膀胱内收集尿液,连续记录1h内排尿量。Ⅰ～Ⅳ组分别按0g/kg、0.5g/kg、1.5g/kg、2.5g/kg剂量耳缘静脉注射茯苓水煎醇沉液。结果:静注茯苓水煎醇沉液1.5g/kg、2.5g/kg剂量组利尿作用明显(P0.01),其中2.5g/kg剂量组在给药10min内尿量出现高峰。表明茯苓对兔具有明显的利尿作用,并且存在一定程度的正向量效关系。     

瑞马唑仑与丙泊酚在无痛胃肠镜患者中的麻醉比较

目的 探讨瑞马唑仑与丙泊酚用于无痛胃肠镜患者中的麻醉优势比较。方法 选取2021年10月至12月接受无痛胃肠镜检查的64例患者作为研究对象,随机分为对照组（P组）和实验组（R组）,两组均给予瑞芬太尼0.5ug/kg静脉注射后以0.05ug/kg/min持续静脉泵注,P组静脉注射丙泊酚1.5mg/kg,每5min追加0.3mg/kg,R组静脉注射瑞马唑仑0.2mg/kg,每5min追加0.05mg/kg。Ramsay镇静评分6分时开始进镜检查,若评分不足6分,间隔1min追加1次,直至评分达6分后开始内镜检查。记录给药前、给药后1min、2min、3min、5min及离室时收缩压、心率、呼吸频率、血氧饱和度;记录麻醉诱导起效时间、苏醒时间、离室时间;记录追加给药次数、补救给药次数、体动次数;记录注射痛、低氧血症、呼吸抑制、低血压、心动过缓、恶心、呕吐、眩晕发生情况。结果 R组诱导时间低于P组,离室时间高于P组,差异有统计学意义（P<0.05）;R组注射痛、低血压、呼吸抑制、心率减慢发生率均低于P组,差异有统计学意义（P<0.05）。R组T3、T5收缩压高于P组,差异有统计学意...     

胸腺肽聚乳酸微球的制备和体外释药研究

为了寻找适于多肽分子吸收,免疫学上"有效"、"安全",且服用方便的口服制剂,用W/O/W型乳化挥发法制备胸腺肽聚乳酸微球,正交实验方法优化了制备工艺.通过差热分析证明载药微球已较好形成,Lowry法测定药物的含量,计算微球的载药量、包封率及体外释药量.结果表明,所得微球平均粒径为13.8 μm,平均包封率为80.7%,前12 h的体外释药符合Higuchi方程,T1/2=295 min,在25℃和40℃分别放置90d,微球的粒径分布和剩余药量无显著变化.微球的载药量和包封率符合要求,释药半衰期长,具有良好的应用前景.     

阿霉素不同给药部位对兔心收缩功能的影响研究——湖北省教育厅科技计划项目《阿霉素静脉注射部位对兔心脏血流动力学的影响》成果介绍

目的探讨不同部位注射阿霉素对处于亚临床阶段兔心脏收缩功能的影响,为临床治疗安全提供依据。方法普通级大耳白兔50只注射阿霉素2.0 mg/kg·次×1次/周×4周,于末次给药后12周通过心室内插管的方法,记录手术完成后从不同部位给药前后兔左室压。于30 min后分别从耳缘静脉、颈外静脉注射阿霉素(耳缘组、颈外组)和生理盐水(空白组、对照组),比较给药前后的左室压力,观察心肝肺组织光镜下变化。结果颈外静脉较耳缘静脉给药后最大收缩速率减弱,左室舒张末期内压升高,P<0.001,有统计学意义;镜下示肺、肝组织淤血水肿的程度不同。结论从回心路径短的部位给药会使处于亚临床阶段的心脏收缩功能下降。     

药物在肝脏的首过效应和剂量调整

肝脏是人体内药物代谢的重要场所,经胃肠道吸收的药物,都要经过门静脉进入肝脏,因此某些在肝脏代谢或在肠壁代谢的药物经胃肠吸收而进入体循环的有效药量就将减少,药效降低,这种现象称为首过效应。而首过效应受到酶浓度及血液速度的影响,肝脏内酶浓度越高,血流速度越快,首过效应就越明显;首过效应越强,进入血中的药物就越少,药物半衰期(T_(1/2))相对较短。老年人肝脏血流减少40-45％,肝脏首过效应能力明显减弱,抗焦虑和抗抑郁药物等血药浓度明显升高,T_(1/2)相对延长。     

苦参碱对急性心衰猫心功能和血流动力学的影响

目的：研究苦参碱对急性心衰猫心功能和血流动力学的影响方法：以成巴比妥钠造成猫急性心衰模型,iv甘参碱20、40mg/kg,用多道生理记录仪和电磁流量计测定猫的心脏血流动力学参数．结果：苦参碱低、高剂量组均可使LVSP、±dp／dtmax、CO、CI、SI、LVWI显著增加,LVEDP、MAP、TPVR、HR显著下降;高剂量组作用强于低剂量组,给药后15min作用达峰值．结论：苦参碱对戊巴比妥钠诱发的心衰猫具有明显的正性肌力作用,负性频率作用,且能增强心脏舒缩功能,降低外周血管阻力,减轻心脏负荷．说明苦参碱有抗心衰作用．     

HPLC法测定大鼠静脉注射色胺酮的血药浓度及其药代动力学研究

目的:建立HPLC法测定静脉注射色胺酮后大鼠血浆中色胺酮的浓度,研究其在体内的药代动力学过程。方法:色谱条件:色谱柱Agilent 5 HC-C18 (250 mm×4.6 mm,5μm),流动相乙腈-水(53∶47,v∶v),流速1mL/min,紫外检测器检测波长251nm,柱温30℃。以4(3H)-喹唑酮为内标物。内标标准曲线法测定生物样品中色胺酮含量,研究其体内药代动力学。结果:色胺酮在0.06～2μg/mL线性关系良好(r=0.999 7);平均回收率大于85%,批内和批间的RSD均小于15%。大鼠静脉注射75 mg/kg的色胺酮后,其体内主要药动学参数t1/2α为0.133h,t1/2β为2.193h,AUC(0-t)为4.288mg/(L·h),MRT为1.934h。结论:试验结果表明本法操作简单,灵敏度高,重现性良好,结果准确可靠,可以用于色胺酮在大鼠体内的药代动力学参数研究。     

磺胺间甲氧嘧啶在家兔体内的药代动力学研究

分析了磺胺间甲氧嘧啶 (Sulfam onomethoxinum ,SMM)在 6只成年健康兔体内的药代动力学过程。结果表明 ,家兔静脉快速推注 114 mg/kg的 SMM,血药浓度 -时间曲线符合二室模型 ,其动力过程符合 C=7.80 6 e- 4.0 0 8t+2 7.5 99e- 0 .4 1 7t。药物动力参数 ,初始浓度 Cp0 为 35 .4 0 5 mg/dl;分布半衰期 t1 / 2α为 0 .2 0 8h;消除半衰期 t1 / 2β为 1.6 6 6h;表观分布容积 Vd为 3.978dl/kg;体清除率 CLB为 1.6 94 dl· kg- 1· h- 1 ;有效血药浓度维持时间 tcp为 4 .10 8h。提示 SMM在家兔体内为短效药物。     

苦参不同器官中的生物碱含量分析

[目的]探讨苦参不同器官中的生物碱含量,为该资源植物的合理应用提供依据.[方法]用薄层色谱法(TLC)分析测定了辽宁产苦参不同器官中苦参碱及氧化苦参碱含量.[结果]各类器官,除叶片外,氧化苦参碱含量均显著超过苦参碱含量;苦参碱含量以种子中的为最高,占干重的0.065%,其次为茎(0.034%)、根(0.016%)、叶(0.013%);氧化苦参碱含量以根最高,占干重的3.847%,其次为种子(1.982%)、茎(0.140%),叶中未检测到;粗老根(直径大于1 cm)与细嫩根(直径在0.5~1.0 cm)中的两种生物碱含量差别不大.[结论]达到一定生长年限后,生物碱积累不再有明显增加而趋于饱和;大部分器官中,氧化苦参碱含量高于苦参碱含量;种子及茎更适合作为苦参碱的提取器官.     

MITOCHONDRIAL DYSFUNCTION AT THE EARLY STAGE OF CISPLATIN-INDUCED ACUTE RENAL FAILURE IN RATS

ＩＮＴＲＯＤＵＣＴＩＯＮＣｉｓ ｄｉａｍｍｉｎｅｄｉｃｈｌｏｒｏｐｌａｔｉｎｕｍ (Ⅱ ) (Ｃｉｓ ｐｌａｔｉｎ)ｉｓａｗｉｄｅｌｙｕｓｅｄａｎｔｉｎｅｏｐｌａｓｔｉｃａｇｅｎｔｔｈａｔｈａｓｎｅｐｈｒｏｔｏｘｉｃｉｔｙａｓａｍａｊｏｒｄｏｓｅ ｌｉｍｉｔｉｎｇｓｉｄｅｅｆｆｅｃｔ.Ｔｈｅｍｏｓｔｃｏｍｍｏｎｆｏｒｍｏｆｃｉｓｐｌａｔｉｎ ｉｎ ｄｕｃｅｄｒｅｎａｌｔｏｘｉｃｉｔｙｉｓｎｏｎ ｏｌｉｇｕｒｉｃａｃｕｔｅｒｅｎａｌｆａｉｌｕｒｅ.Ｔｈｅｕｎｄｅｒｌｙｉｎｇｍｅｃｈａｎｉｓｍｏｆｔｈｉｓｒｅｎａ…     

固相萃取-UPLC—MS／MS测定食品中的黄曲霉毒素M1和B1

建立固相萃取与UPLC—MS／MS检测食品中黄曲霉毒素M1和黄曲霉毒素B1的方法。样品经乙腈提取和SPE小柱萃取净化,提取液经氮气吹干后,用50％甲醇水溶液定容。超高效液相色谱一串联质谱（UPLC—MS／MS）测定,采用电喷雾正离子（ESI＋）模式电离,多反应监测（MRM）模式检测。流动相为0．1％甲酸水溶液和甲醇,流速0．4ml／min,使用ZORBAX Eclipse XDB—C18色谱柱（100mm×3．0mm×1．8μm）为分析柱。黄曲霉毒素AFM1在0．1～50μg／kg范围内线性关系良好、黄曲霉毒素AFB1在0．1～10ug／kg范围内线性关系良好,相关系数均大于0．999;回收率在83．75％～97．8％之间;检出限AFMl为0．05μg／kg、AFBl0．02μg／kg。该法具有分析速度快,检测准确、灵敏度和回收率高等优点,适合食品中黄曲霉毒素M1、B1含量的检测。     

Midazolam in rabbits terminates dysrhythmias caused by intracerebroventricular ropivacaine

The current study was designed to investigate the mechanisms by which ropivacaine may act within the central nervous system (CNS) to produce cardiotoxicity. Eighty New Zealand rabbits were divided into four groups randomly. In Group 1, 20 rabbits received intracerebroventricular (icv) saline, and then received icv ropivacaine 30 min later. In Group 2, 20 rabbits received icv ropivacaine. Whenever dysrhythmias continued for more than 5 min, 0.1 ml saline was administered into the left cerebral ventricle. Ten minutes later, 0.1 ml midazolam was given into the left lateral ventricle. In Group 3, 20 rabbits received icv ropivacaine, and once the dysrhythmias developed, the inspired isoflurane concentration was increased from 0.75% to 1.50%. In Group 4, 20 animals received an intravenous (iv) phenylephrine infusion until dysrhythmias occurred. In Group 1, the rabbits did not develop dysrhythmias in response to icv saline, whereas dysrhythmias did develop in these animals after icv ropivacaine. In Group 2, icv saline had no effect on the dysrhythmias; however, icv midazolam terminated cardiac dysrhythmias. In Group 3, an increase in the concentration of the inspired isoflurane had no effect on dysrhythmias. In Group 4, icv midazolam had no effect on dysrhythmias in response to iv phenylephrine. Ropivacaine administered directly into the CNS is capable of producing cardiac dysrhythmias; midazolam terminated dysrhythmias presumably by potentiation of γ-aminobutyric acid (GABA) receptor activity. Our results suggest that ropivacaine produces some of its cardiotoxicity not only by the direct cardiotoxicity of the drug, but also by the CNS effects of ropivacaine.     

1%戊巴比妥钠对家兔体温的影响

60只家兔，在室温条件下用1％的戊巴比妥钠麻醉，连续观察麻醉前、麻醉后10min、20min、30min、60min、90min、120min七个时相点的肛温变化，结果发现麻醉后家兔的肛温显著降低，麻醉后60min左右，体温降至最低水平，并形成20min左右的低温稳定期，之后体温逐渐回升，提示麻醉后的家兔体温调节功能下降，从而降低相关实验的成功率及数据的准确性。     

Mitochondrial dysfunction at the early stage of cisplatin-induced acute renal failure in rats

The present study was undertaken to clarify the pathogenesis of cisplatin-induced acute renal failure at the early stage. Male Sprague-Dawley rats were given an intravenous administration of 10 mg/kg cisplatin. 0.9% saline was infused into them at a rate of 2 ml/h for 3 h, starting with a 2-ml bolus injection before cisplatin administration. 3 h following cisplatin administration, no evident morphological abnormalities were found by both light and electron microscopy; there were also no significant changes in GFR. Thirty min after cisplatin injection, urine sodium and potassium excretion increased by 56% and 260% those of the control animals, respectively. Apparent renal mitochondrial respiration dysfunction was observed in cisplatintreated rats 3 h later; the state 4 respiration increased by 100% and state 3 respiration, respiratory control ratio and carbonyl cyanide p-trifluoromethoxyphenyl hydrazone-uncoupled respiration decreased by 46%, 74% and 47% of the controls, respectively. The present data suggest that mitochondrial dysfunction may be a very early event in cisplatin-induced acute renal failure in rats.     

气相法测定氟马西尼中乙醇、乙醚、二氯甲烷残留量

建立顶空气相色谱法控制氟马西尼中有机溶剂乙醇、乙醚、二氯甲烷残留量的分析方法。方法：采用DB-624石英毛细管柱,FID离子化检测器,以90%的二甲亚砜水溶液为溶剂。结果：乙醇在12.60～75.60ug/ml（630ppm～3780ppm）的浓度范围内,r为0.9998乙醚在12.79～76.74ug/ml（639.5ppm～3837ppm）的浓度范围内,r为0.9999二氯甲烷在2.54～15.24ug/ml（127ppm～762ppm）的浓度范围内,r为0.9997,大于规定的0.99;定量限试验中,信噪比符合规定,能够达到定量检测及检出的要求;各浓度下的乙醇、乙醚、二氯甲烷平均回收率均在90%-110%范围内。结论：该方法专属性好,精密度、准确度都符合要求,方法可靠,可用于原料药氟马西尼中有机溶剂乙醇、乙醚、二氯甲烷的残留量的控制。     

Pharmacokinetic study with N-Ile1-Thr2-63-desulfato-r-hirudin in rabbits by means of bioassay

INTRODUCTION Hirudin, a naturally occurring polypeptide from salivary glands of medicinal leech (Hirudo Medici-nalis) and an important effective component of tradi-tional Chinese medicine Shui Zhi, has proven to be a highly selective direct thrombin inhibitor (Markwardt, 1994). Currently, in China recombinant-hirudin has been developed by DNA recombination technique and is undergoing extensive preclinical and clinical evaluation. Over the past decade, much effort in our lab was devote…     

Enhancing effect of natural borneol on the absorption of geniposide in rat via intranasal administration

Both geniposide (Ge) and natural borneol (NB) are bioactive substances derived from traditional Chinese herbs. The effect of NB on the pharmacokinetics of Ge in rat via intranasal administration was investigated. The concentrations of Ge in plasma were determined by reversed-phase high-performance liquid chromatography (HPLC) after intranasal administration of Ge (4 mg/kg) alone and combined with different doses (0.08, 0.8, and 8 mg/kg) of NB. The intravenous administration was given as a reference (4 mg/kg of Ge and 8 mg/kg of NB). Compared with the intravenous administration, the absolute bioavailability of Ge was 76.14% through intranasal administration combined with NB. Compared with the intranasal administration of Ge alone, Ge could be absorbed rapidly in the nasal cavity combined with NB; the peak time of Ge in the plasma became shorter (3–5 min vs. 40 min); the peak concentration became higher (1.32–4.25 μg/ml vs. 0.67 μg/ml); and, the relative bioavailability of Ge combined with NB was 90.3%–237.8%. The enhancing effect was attenuated as the dose of NB decreased. The results indicated that NB can accelerate the absorption of Ge dose-dependently in the nasal cavity.