一阶导数高速脉冲极谱法用于盐酸普鲁卡因的定量分析

研究了一阶导数高速脉冲极谱法,并运用于盐酸普鲁卡因及其注射制剂的定量分析。在-0.04 V(对 Ag/AgCl)处出现的良好导数峰,于1.0～6.0×10~(-4)mol/L 范围内,导数峰电流与浓度呈线性关系。检测限为3.0×10~(-8)mol/L。操作简便、快速、灵敏,结果准确。     

Chemical and statistical considerations in the determination of partition coefficients of weakly ionizable drugs and poisons

Equations have been developed that relate the concentration (or a parameter directly proportional to concentration, such as optical absorbance) of a weakly ionizable solute in a water-immiscible phase, in equilibrium with an aqueous phase, to the pH of the aqueous phase, the partition coefficient of the unionized solute and the phase volume ratio. These relationships have been used in the design of experimental methods for determining partition coefficients, which require measurement of solute concentration in only one phase. Data obtained in this way permit ready recognition of deviations from assumptions made in the development of the model; these assumptions include insolubility of the ionized solute in the water-immiscible phase and lack of interaction between buffer components and solute. Conditions for optimal liquid—liquid extraction of weakly ionizable solutes are more easily recognized. With these techniques, the negative logarithm of the acid dissociation constant (pK′_a) and the logarithm of the octanol—water partition coefficient (log P) have been measured for warfarin (pK′_a = 5.15 ± 0.04; log P = 2.82 ± 0.06), strychnine (pK′_a = 8.29 ± 0.02; log P = 2.23 ± 0.04), phenol (pK′_a = 9.88 ± 0.02; log P = 1.75 ± 0.05), procaine (pK′_a = 8.11 ± 0.04; log P = 1.10 ± 0.08), and ephedrine (pK′_a = 9.92 ± 0.01; log P = 1.65 ± 0.04) at 21°C.     

Stability-indicating determination of adrenaline in injections containing procaine

Adrenaline was determined in injections containing procaine in a 1000-fold excess by reversed-phase high-performance liquid chromatography using UV detection at 205 nm and aqueous sulphuric acid (100 μmol/l) as eluent. The relative standard deviation was 2.1%, and the method was selective in the presence of adrenaline degradation products. Changes of the capacity factor with pH and ionic strength of the eluent were studied, and a simple model is suggested to explain the retention data.     

普鲁卡因对缺氧心肌细胞的影响

目的 探讨普鲁卡因对心肌细胞缺氧损伤的影响。方法 将原代培养成活48h的大鼠乳鼠心肌细胞分为三组：A组为对照组（氰化钠造成心肌细胞内缺氧模型）,B组为Prol组（缺氧＋7．4mg／L普鲁卡因）,C组为Pro2组（缺氧＋14．8mg／L普鲁卡因）。比较三组心肌细胞形态学（倒置相差显微镜、透射电镜观察）的变化及吸光度A值的改变。结果 缺氧12h后,对照组细胞搏动功能变化明显,呈散在细胞搏动,而实验组搏动频率减慢。随着时间的延长,细胞形态学变化逐渐明显,对照组较实验组变化更显著。结论 普鲁卡因对培养心肌细胞缺氧损伤有一定的保护作用。     

国产盐酸氯普鲁卡因临床效应分析

目的 分析研究国产盐酸氯普卡因冻干粉与针剂分别应用于硬膜外麻醉、臂丛神经阻滞、局部浸润麻醉的效果。方法 采用随机双盲目的方法分组进行研究。硬膜外麻醉45例,分为3组（每组15例）：Ⅰ组1．7％利多卡因,Ⅱ组氯普鲁卡因粉剂稀释为3％,Ⅲ组3％氯普鲁卡因针剂;臂丛神经阻滞40例,分为4组（每组10例）;I组1．33％利多卡因,Ⅱ组2％普鲁卡因,Ⅲ组氯普鲁卡因粉剂稀释为2％,Ⅳ组2％氯普鲁卡因针刺;局部浸润麻醉30例（每例10例）分为3组：Ⅰ组1％普鲁卡因,Ⅱ组氯普鲁卡因粉剂稀释为1％,Ⅲ组1％氯普鲁卡因针剂。结果 硬膜外组中除Ⅲ组运动消失时间明显短于Ⅰ组外（P＜0．05）,其余指标无明显统计学差异;臂全神经阻滞组中,实验组疼痛恢复及运动恢复时间少于对照组I组,有统计学差异（P＜0．01）,实验组Ⅲ组疼痛及运动恢复时间均比对照组Ⅱ组长（P＜0．05）;局部浸润麻醉组中两实验组疼痛消失迅速,疼痛恢复时间均长于对照组,Ⅲ组短于Ⅱ组。结论 国产盐酸氯普鲁卡因麻醉起效迅速,性能稳定,粉剂比针剂更佳;作用维持时间介于盐酸普鲁卡因与利多卡因之间。     

普鲁卡因对豚鼠接触性湿疹模型的影响

目的：探讨普鲁卡因对豚鼠接触性湿疹模型的影响。方法：采用０．１％二硝基氯苯涂擦豚鼠耳部,激发接触性皮炎,每周１次,共４周,建立接触性湿疹模型,然后胜利腔注射普产因,每天１次共１４天,测人肿胀度、表皮朗格汉斯细胞数、真皮浸润细胞数。结果：普瞳因组明显地抑制豚亚急性／慢性湿疹。结论：普鲁卡因对湿疹具有治疗作用,其机制可能与朗格汉斯细胞减少有关。     

褶合光谱法用于盐酸普鲁卡因注射液中对氨基苯甲酸的限量检测

 目的:建立用褶合光谱法进行盐酸普鲁卡因注射液中对氨基苯甲酸(PABA)限量检测的方法。方法:选择褶合光谱波长范围为210～330 nm，间隔4 nm,以限量杂质三维褶合光谱差谱点域值为判据。结果:检测了5批样品，结果与中国药典规定的方法一致。结论:方法简便、灵敏、结果准确，适用于药物的杂质限量检测。     

维拉帕米-普鲁卡因合剂防治危重手术后急性呼吸窘迫综合征的临床观察

目的观察维拉帕米普鲁卡因合剂(维普合剂)防治危重患者手术后急性呼吸窘迫综合征(ARDS)的效果,探讨适宜推广应用防治ARDS的简便、实用、价廉方法。方法符合ARDS高危因素的各科危重手术患者150例,在常规基础综合治疗基础上随机分为3组:维普合剂组给予质量分数为5%的葡萄糖500ml+普鲁卡因1250mg+维拉帕米10mg;普鲁卡因组给予5%葡萄糖500ml+普鲁卡因1250mg;对照组仅给予5%葡萄糖500ml。3组均以0.5ml·h-1·kg-1持续静脉滴注,确诊急性肺损伤(ALI)或ARDS后,维普合剂组和普鲁卡因组的普鲁卡因和维拉帕米剂量均加倍,滴速不变。均应用金科威UT4000F持续无创监测血压(BP)、心电图(ECG)、脉搏血氧饱和度(SpO2)、呼吸及体温,间断测定动脉血气分析和外周血常规。依据全身炎症反应综合征(SIRS)、ALI与ARDS诊断标准确定诊断,并进行SIRS评分和急性生理学与慢性健康状况(APACHE)评分。结果维普合剂组、普鲁卡因组和对照组24hSIRS确诊数分别为11例、26例和42例,组间比较差异均有显著性(P均<0.01);术后72h3组ALI确诊数分别为4例、7例和19例,维普合剂组与普鲁卡因组组间比较差异无统计学意义,维普合剂组和普鲁卡因组与对照组比较差异均有显著性(P均<0.01);术后2周仅对照组有12例确诊ARDS,其中5例并发多器官功能衰竭后死亡,     

褶合光谱法用于盐酸普鲁卡因注射液中对氨基苯甲酸的限量检测

目的：建立用褶合光谱法进行盐酸普鲁卡因注射液中对氨基苯甲酸（ＰＡＢＡ）限量检测的方法。方法：选择褶合光谱波长范围为２１０～３３０ｎｍ，间隔４ｎｍ，以限量杂质三维褶合光谱差谱点域值为判据。结果：检测了５批样品，结果与中国药典规定的方法一致。结论：方法简便、灵敏、结果准确，适用于药物的杂质限量检测。     

In vivo comparison of the reinforcing and dopamine transporter effects of local anesthetics in rhesus monkeys

Dopaminergic mechanisms are thought to play a central role in the reinforcing effects of cocaine. Similar to cocaine, other local anesthetics bind to the dopamine transporter (DAT) and inhibit DA uptake in rodent and monkey brain. Additionally, local anesthetics are self-administered in rhesus monkeys, indicative of abuse liability. The present study examined the reinforcing and DAT effects of the local anesthetics dimethocaine, procaine and cocaine using in vivo techniques. Monkeys were trained to respond under a second-order schedule for i.v. cocaine administration (0.10 or 0.30 mg/kg/infusion). When responding was stable, dimethocaine (0.030-1.7 mg/kg/ infusion) or procaine (0.10-10 mg/kg/ infusion) was substituted for the cocaine training dose. Dimethocaine administration produced higher response rates compared with that of procaine, and was a more potent reinforcer. Drug effects on behavior were related to DAT occupancy in monkey striatum during neuroimaging with positron emission tomography (PET). DAT occupancy was determined by displacement of 8-(2-[(18)F]fluroethyl)2beta-carbomethoxy-3beta-(4-chlorophenyl)nortropane (FECNT). DAT occupancy was between 66 and 82% and <10-41% for doses of dimethocaine and procaine that maintained maximum response rates, respectively. Finally, in vivo microdialysis in awake subjects determined drug-induced changes in extracellular DA in the caudate nucleus. There was close correspondence between peak increases in DA and DAT occupancy. Overall, reinforcing effects were consistent with DAT effects determined with in vivo techniques. The results further support a role for the DAT in the abuse liability of local anesthetics.