2008年1—3月份医药商品进出口分析

2008年1～3月份，我国医药商品进出口总额为50．25亿美元，同比增长42．26％。其中：进口总额为20．75亿美元，同比增长39．80％，增长幅度为35．20个百分点；出口总额为29．49亿美元，同比增长43．98％，增长幅度为36．53个百分点，实现贸易顺差8．77亿美元。     

高效液相色谱波长切换法同时测定肿节风中多指标成分的含量

目的：建立肿节风药材中反丁烯二酸、异秦皮啶和落新妇苷的含量测定方法。方法：采用DiamonsilC18（200mm×4．6mm，5μm）柱，以乙腈为流动相A，以0．1％磷酸溶液为流动相B，梯度洗脱，检测波长分别切换为210，344nm，290nm。结果：反丁烯二酸在0．0710～1．4020μg范围内线性关系良好，平均回收率为103．0%，RSD为=1．1%；异嗪皮啶在0．071，6～0．716，0μg范围内线性关系良好，平均回收率为99．8％，RSD为1．9％。落新妇苷在0．0413～0．6195Mg范围内线性关系良好，平均回收率为99．5％，RSD为2．0％。结论：本方法简便、准确，重复性好，在同一色谱条件下可同时测定反丁烯二酸、异秦皮啶和落新妇苷的含量。     

高效液相色谱法测定茶碱麻黄碱片中茶碱与盐酸麻黄碱含量

目的用高效液相色谱（HPLC）法测定茶碱麻黄碱片中茶碱与盐酸麻黄碱的含量。方法采用Kromasil C18柱（150mm×4．6mm，5μm），流动相为0．05mol／L磷酸二氢钾溶液-甲醇-三乙胺（72：28：0．2），检测波长为215nm，流速为1．0mL／min，柱温为42℃。结果茶碱质量浓度的线性范围为22．34～111．7μg／mL，r=0．9999（n=6），平均回收率为99．85％，RSD为0．14％（n=9）；盐酸麻黄碱质量浓度的线性范围为5．17～25．86μg／mL，r=0．9997（n=6），平均回收率为99．25％，RSD为0．39％（n=9）。结论HPLC法简便易行，结果准确，重现性好。     

顶空气相色谱法测定匹伐他汀钙中有机溶剂残留量

目的建立以顶空进样测定匹伐他汀钙原料药中有机溶刑残留量的方法。方法以N，N-二甲基甲酰胺为溶剂，平衡温度为90℃，平衡时间为30min。采用DM-624毛细管柱（内涂6％氰丙基苯基硅氧烷和94％聚甲基硅氧烷），检测器为FID，载气为№，流速为5mL／min，分流比为3：1，顶空进样量为1．0mL。结果二氯甲烷、四氢呋喃、乙醇、正己烷、甲苯、环己烷和乙腈的质量浓度线性范围分别是12．2-304．8μg／mL，14．4—359．6μg／mL，101．1—2528μg／mL，5．8～145μg／mL，17．9—446．5μg／mL，77．8—1945μg／mL，8．1—203．3μg／mL；平均回收率分另4为98．0％，99．0％，98．2％，99．2％，98．5％。99．6％，97．5％。结论顶空气相色谱法简单，灵敏度高，测定结果准确，可用于匹伐他汀钙有机溶剂残留量的测定。     

复方呋喃西林滴鼻凝胶剂的制备

目的：制备复方呋喃西林滴鼻凝胶并对其含量进行测定。方法：以卡波姆-40为乳化剂，三乙醇胺调节pH，制备水溶性透明凝胶。用紫外分光光度法和旋光度法分别测定凝胶剂中呋喃西林和盐酸麻黄碱的含量。结果：制备的凝胶均匀细腻，稠度适宜。呋喃西林的平均含量为98．56％，RSD为1．24％。平均回收率为99．36％，RSD为0．83％，盐酸麻黄碱的平均含量为97．93％，RSD为1．32％。平均回收率为100．36％，RSD为0．67％。结论：该制剂性质稳定，容易吸收，无刺激性，使用方便，测定方法简单易行，快速准确。     

头孢他定正常人和烧伤患者的药代动力学研究

用高效液相色谱法研究了６例正常人和７例烧伤患者静滴头孢地定１ｇ后的临床药动学。结果显示，该药静滴后的药动学符合二室开放模型。正常人静滴后即刻平均血药浓度为１１４．１３±３３．５４μ／ｍｌ，消除相半衰期为１．８９±０．１５小时，表观分布容积为０．２３±０．０５Ｌ／ｋｇ，给药后２４小时尿中回收药量为８７．０２％，０～９．０小时为８３．９１％。烧伤患者静滴后即刻平均血药浓度与正常人接近，为１００．８５±１８，８５μｇ／ｍｌ，但消除相半衰期比正常人长，为２．９２±１．０４小时（ｐ＜０．０５），表现分布容积增大，为０．３８±０．１０Ｌ／ｋｇ（ｐ＜０．０１），给药后０～８小时尿回收药量略低于正常人，为７３．４２％（ｐ＜０．０５）。     

临床路径应用于肝部分切除患者健康教育的效果分析

目的探讨临床路径在肝部分切除术患者健康教育中的应用效果，为临床提供参考。方法选取肝部分切除术患者72例，通过随机数字表法将其分为观察组和对照组各36例，对照组采用传统的健康教育方法，观察组在临床路径的指导下实施健康教育。对比两组患者的住院情况，并通过自制的调查问卷，评估两组患者住院期间对健康教育知识的掌握情况。结果观察组术后卧床时间为（8．21±0．41）h，住院费用为（20197．54±6772．35）元，住院天数为（10．28±1．47）d；对照组术后卧床时间为（9．26±0．68）h，住院费用为（26732．61±7290．53）元，住院天数为（13．38±2．82）d，两组差异均有统计学意义（t=4．010、12．948、8．552，均P〈0．05）；观察组优的比例为77．78％，优良率为91．67％，对照组优的比例为33．33％，优良率为52．78％，两组差异均有统计学意义（x2=14．400、11．700，均P〈0．05）。结论临床路径能够提高肝部分切除术患者健康教育的效果，帮助患者更好掌握健康教育知识，提高手术的临床疗效。     

尼群地平微囊的研制及体外释放度的研究

本文采用明胶单凝聚法将尼群地平包成微囊，并对其包囊率、主药含量、稳定性、溶出度进行了实验研究，得出包囊率为81．43±2.08m为1．03±0．11，T50为41．90±2．03min，Td为59．7±z．12min，并与尼群地平片的溶出度进行比较，得出其片剂的m为0．95±0．23，T50为14．9±1．3min，Td为21．9±0．98min，将两者进行T检验，P＜0．001，有显著差异，表明尼群地平制成微囊后具有缓释，长效和稳定的作用。     

胃溃疡的不同手术方式风险及其疗效评价

目的探讨胃溃疡的不同手术方式的手术风险和治疗效果。方法选择177例胃溃疡患者作为研究对象，将其随机分为A组、B组和C组。A组采用Billroth Ⅰ式胃空肠吻合术，B组采用BillrothⅡ式胃空肠吻合术，C组采用Roux—en—Y胃空肠吻合术。结果显效率A组为49．2％，B组为45．8％，C组为47．5％，显效率A〉C〉B；总有效率A组为96．6％，B组为89．8％，C组为93．2％，总有效率A〉C〉B，组间比较，差异均无显著性（χ^2=0．136，P〉0．05．χ^2=2．145，P〉0．05）。1年复发率A组为3．4％，B组为16．9％，C组为6．8％，1年复发率B〉C〉A，组间比较，差异有显著性（χ^2=7．146，P〈0．05）；术后半年并发症率A组为5．1％，B组为22．0％，C组为8．5％，术后半年并发症率B〉C〉A，组间比较，差异有显著性（χ^2=9．077，P〈0．05）。结论Billroth Ⅰ式有效性和安全性最高，应该根据患者病情和身体耐受情况，进行综合考虑和评估，选择合适的手术方式；对于全身状况较好，病变进展稳定的患者，可在严密监测下适当提高手术指征，尽量实施Billroth Ⅰ式手术治疗。     

双波长分光光度法测定栓剂中甲硝唑,诺氟沙星的含量

本文采用双波长分光光度法同时测定栓剂中甲硝唑、诺氟沙星的含量；甲硝唑的测定波长为３１３．０ｎｍ，参比波长为２６１．５ｎｍ，诺氟沙星的测定波长为２８３．５ｎｍ，参比波长为３４０．５ｎｍ，甲硝唑的平均回４文率为１００．７４％，ＲＳＤ为０．７１％；诺氟沙星的平均回收率为１００．０５％，ＲＳＤ为０．６５％。该法快速、简便，结果准确，适用于该制剂质量控制。     

高乌甲素贴片释放度测定的研究

本文通过体内及体外实验观察了纳络酮对正常、缺血和再灌注心肌腺苷酸环化酶（AC）活性的影响。其结果表明：静脉注射纳络因（1mg．kg-1）可以明显降低缺血、再灌注心肌AC活性（P＜0．01，P＜0．05）；但纳络酮在体外对正常、缺血和再灌注心肌组织匀浆AC活性无明显抑制作用（P＞0．05）。提示：纳络酮本身对AC活性无直接抑制作用，它降低缺血、再灌注心肌AC活性可能与酶前调节有关。     

纳络酮对缺血再灌注心肌脂质过氧化物和钙含量的影响

利用大心肌缺血、再灌注模型，观察了纳络酮对缺血再藻注心肌脂质过氧化物（ＬＰＯ）、超氧化物歧化酶（ＳＯＤ）和钙含量的影响。结果表明：缺血、再灌注心肌ＬＰＯ和钙含量明显增加（Ｐ＜０．０５，Ｐ＜０．０１），再灌注心肌ＬＰＯ含量和钙含量明显高于缺血心肌（Ｐ＜０．０５，Ｐ＜０．０１），而缺血、再灌注心肌ＳＯＤ明显降低（Ｐ＜０．０１）；纳络用明显降低缺血、再灌注心肌ＬＰＯ和钙含量（Ｐ＜０．０５，Ｐ＜００１），但对ＳＯＤ的影响不明显（Ｐ＞０．０５）。提示：纳络酮抑制心肌缺血、再灌注时的脂质过氧化物反应，部份阻止细胞外钙跨膜内流，对心肌只响保护作用。     

迷走神经刺激预处理对急性心肌缺血大鼠心肌P物质和降钙素基因相关肽的影响

目的观察迷走神经刺激预处理对急性心肌缺血大鼠心肌组织缺血区和非缺血区P物质(SP)和降钙素基因相关肽(CGRP)表达的影响。方法健康成年雄性SD大鼠24只,体质量270~300g,随机分为3组,每组8只,假手术组(S组)、单纯冠状动脉结扎组(I组)和迷走神经刺激预处理冠状动脉结扎组(VS组)。S组大鼠开胸后在冠状动脉左前降支下穿线不结扎;Ⅰ组大鼠开胸后结扎冠状动脉左前降支;VS组大鼠实施迷走神经刺激30min后结扎冠状动脉左前降支。各组在手术后计时3h。采用免疫组织化学、酶免疫法和反转录-聚合酶链反应法从蛋白和基因水平观察各组大鼠缺血区和非缺血区心肌SP和CGRP的表达。结果Ⅰ组大鼠缺血区心肌SP/SP mRNA和CGRP/β-CGRP mRNA的水平较S组升高(P<0.05),VS组低于Ⅰ组(P<0.05),但仍高于S组(P<0.05)。非缺血区各组的变化趋势类同缺血区,但各扎闭冠状动脉组SP/SP mRNA和CGRP/β-CGRP mRNA的水平均低于相应组缺血区的水平(P<0.05)。结论迷走神经刺激预处理可降低急性心肌缺血大鼠心肌组织SP和CGRP的表达,提示迷走神经刺激预处理可能参与缺血心肌的保护。     

Beneficial effect of nipradilol (K-351) on acute myocardial ischemia. Study of the relationship between regional myocardial blood flow and energy metabolism

To examine the effects of nipradilol on ischemic myocardium, experiments were performed on regional myocardial blood flow (MBF) and energy metabolism in anesthetized, open-chest dogs. Nipradilol at a dose of 0.3 mg/kg was i.v.-administered 10 min after coronary ligation. MBFs at various sites, including ischemic and non-ischemic areas, were determined by the hydrogen gas clearance method. The levels of ATP and creatine phosphate (CP) at the site of MBF determination were measured 60 min after ligation, and mitochondrial function (RCI, QO2) in the ischemic and non-ischemic areas was determined. Following nipradilol administration, aortic pressure and heart rate were significantly lowered. In ischemic areas with MBF below 40 ml/min/100 g, nipradilol had no influence on MBF. However, the tissue level of ATP in nipradilol treated hearts was significantly higher as compared with untreated hearts. In the area of mild ischemia with MBF of 40-60 ml/min/100 g, nipradilol preserved the tissue ATP and CP levels in spite of a decrease in MBF. Moreover, an inhibition of the decrease in mitochondrial respiratory function was observed in ischemic areas with MBF below 20 ml/min/100 g. Thus, nipradilol administered following ischemia preserved ATP content and mitochondrial function in the ischemic myocardium with reduction of heart rate and aortic pressure. This suggests that nipradilol exerts a cardioprotective effect in acute ischemia. It seems that the cardioprotective effect is due to a decrease in myocardial oxygen demand and preservation of mitochondrial function.     

急性缺血对犬在体左心室内膜恢复性质的影响

目的探讨急性缺血对左心室内膜整体恢复性质的影响。方法健康犬10只,应用非接触球囊标测技术,同步记录在体阻断左前降支30 min前后心内膜各区域单极电图,测量激动恢复间期(ARI)和舒张间期(DI),计算恢复曲线斜率。结果正常供血状态下心肌内膜恢复曲线存在一定差异。从心尖部向心底部,曲线的斜率呈逐步下降的趋势,左心室内膜恢复曲线的斜率总体上<1。急性缺血后,缺血区恢复曲线变平;而在部分非缺血区(室间隔后部接近心底部及心室流出道附近)恢复曲线变陡峭,斜率显著升高,最大的曲线斜率>1,与缺血前比较差异有统计学意义(P<0.05)。结论急性缺血后,缺血与非缺血心肌的恢复性质均发生改变,部分非缺血心肌恢复曲线斜率显著增加。     

丹参酮、纳络酮对缺血再灌注心肌局部血流量的影响

目的：观察丹参酮、纳络酮对缺血再灌注心肌局部血流量的影响。方法：用结扎冠状动脉左前降支的方法复制犬心肌缺血再灌注模型，心肌局部血流量用氢气清除法测定。结果：丹参酮、纳络酮均能明显增加正常及部分再灌注心肌血流量，丹参酮主要增加缺血周围区血流量，纳络酮可增加缺血中心区及周围区血流量。结论：丹参酮、纳络酮均能缩小缺血区范围，纳络酮还能减轻缺血程度。     

Adrenergic influences on ischemic and reperfusion arrhythmias in a canine model with diminished collateral blood flow

To examine the role of adrenergic influences on genesis of ischemic and reperfusion arrhythmias, the left anterior descending coronary artery (LAD) was cannulated and perfused by a shunt from the left carotid artery in 38 open-chest pentobarbital-anesthetized dogs. Ischemia was produced by shunt occlusion and retrograde diversion of collateral flow from the LAD. The diverted blood was collected and returned to the animal by intravenous (i.v.) injection. The shunt was opened and the ischemic myocardium reperfused after 30 min of ischemia. Microsphere injections in six dogs during shunt occlusion and retrograde bleeding showed that blood flow to the ischemic zone was less than 1.5% of normal zone flow. The remaining 32 dogs were randomized into four treatment groups. Dogs (n = 8) were treated before shunt occlusion with either saline, nadolol (1 mg/kg), prazosin (0.2 mg/kg), or bilateral stellate transection. As compared with saline treatment, nadolol and stellate transection significantly reduced heart rate (HR), and prazosin significantly reduced mean arterial blood pressure (MAP) (p less than 0.05). However, none of the antiadrenergic interventions significantly reduced the number or frequency of ectopic beats during either the 1a or 1b phases of ischemia. None of the 32 dogs developed ventricular fibrillation (VF) during ischemia, but all dogs fibrillated within 30 s of reperfusion. The size of the ischemic zone ranged from 21 to 38% of the left ventricle, and there were no differences among the four treatment groups. The results suggest that when ischemia is severe, the adrenergic nervous system does not play a significant role in genesis of ischemic-induced ectopy or reperfusion-induced VF.     

Antiarrhythmic and electrophysiologic actions of clofilium in experimental canine models

Clofilium was studied in three experimental models. In non-ischemic and chronically infarcted canine hearts, clofilium (0.5-2 mg/kg) produced a dose-dependent increase in electrical ventricular fibrillation threshold (VFT), but prolonged the effective refractory period (ERP) of normal myocardium in only the non-ischemic heart. When chronically infarcted hearts were subjected to programmed electrical stimulation, 1 mg/kg of clofilium inhibited the re-induction of either ventricular tachycardia or ventricular fibrillation in 5 of 6 animals and slowed the rate of the induced tachycardia in the sixth. Clofilium, however, failed to alter ventricular refractory periods of normal myocardium at either twice diastolic threshold current (176 +/- 5 ms control vs. 187 +/- 9 ms post-clofilium, P greater than 0.05) or at 10 mA (134 +/- 6 ms control vs. 137 +/- 13 ms post-clofilium, P greater than 0.05). In addition, chronic administration of clofilium (2 mg/kg, i.v., followed by 1 mg/kg every 12 h) was ineffective in decreasing mortality in a canine model of sudden coronary death. Of 10 saline-treated conscious animals subjected to an electrically-induced intimal lesion of the left circumflex coronary artery in the presence of a previous ischemic insult, all 10 died suddenly of ventricular fibrillation within 173 +/- 45 min after current application. Under similar conditions, 7 clofilium-treated animals died suddenly within 249 +/- 88 min (P greater than 0.05) after current application while 3 animals survived (P greater than 0.10). Clofilium did, however, elevate the effective refractory period in these animals (150 +/- 3 ms saline-treated vs. 195 +/- 7 ms clofilium-treated). It is concluded from our data that there is little relationship between clofilium's electrophysiologic actions in normal myocardium and antiarrhythmic effects. Furthermore, simple prolongation of refractoriness in normal non-ischemic myocardium may be insufficient for the prevention of ventricular fibrillation which develops in response to a transient ischemic event superimposed on a chronically injured myocardium.     

The effect of cibenzoline on myocardial damages in dogs

The antiarrhythmic and cardioprotective effects of cibenzoline (4,5-dihydro-2-(2,2-diphenylcyclopropyl)-1H-imidazole) were investigated. Nineteen adult mongrel dogs were divided into 2 groups; in the control group, physiological saline (25 ml) was administered, and 20 min after, the left anterior descending coronary artery (LAD) was occluded for 2 h; in the cibenzoline group, cibenzoline (2 mg/kg), was administered 10 min before 2 h LAD occlusion. Blood pressure and appearance of arrhythmias were monitored throughout the experiment. Two h after occlusion, mitochondria were prepared from both ischemic and non-ischemic areas in each group, and their functions were measured polarographically. Fractionation of myocardial tissue from both ischemic and non-ischemic areas was performed, and activities of lysosomal enzymes (N-acetyl-beta-glucosaminidase and beta-glucuronidase) were measured in each fraction. Administration of cibenzoline significantly reduced the appearance of ventricular arrhythmias in association with ischemia. Cibenzoline did not change significantly blood pressure and heart rate. In the control group, mitochondrial dysfunction and leakage of lysosomal enzymes induced by 2 h occlusion were observed. Administration of cibenzoline maintained significantly mitochondrial function and prevented significantly leakage of lysosomal enzymes. These results indicated that cibenzoline has a cardioprotective as well as an antiarrhythmic effect on ischemic myocardium.     

Effect of a novel thromboxane A2 synthetase inhibitor on ischemia-induced mitochondrial dysfunction in canine hearts

This study was designed to determine the effect of sodium 6-(2-[1-(1H)-imidazolyl]methyl-4,5-dihydrobenzo[b] thiophene)carboxylate (RS-5186), a new thromboxane A2 (TXA2) synthetase inhibitor, on mitochondrial function and lysosomal integrity in ischemic myocardium. 17 anesthetized mongrel dogs were divided into 2 groups. In the control group (n = 11), the left anterior descending arteries (LAD) of the dogs were occluded for 2 h and physiological saline was infused until the end of the experiment. In the RS-5186 treated group (n = 6), 25 min prior to LAD occlusion, RS-5186, 10 mg/kg, was injected for 10 min. 2 h after occlusion, mitochondria were prepared from both ischemic and non-ischemic areas, which were confirmed by Evans' blue dye, and mitochondrial function (respiratory control index: RCI, and the rate of oxygen consumption in state III respiration: St.III O2) was measured polarographically with succinate as substrate. Fractionation of myocardial tissue from both ischemic and non-ischemic areas was also performed, and the activities of lysosomal enzymes (N-acetyl-beta-glucosaminidase: NAG, beta-glucuronidase: beta-gluc) of each fraction were measured. 2-h LAD occlusion induced a significant greater decrease in mitochondrial function from the ischemic area of the control group (RCI: 2.80 +/- 0.45, St.III O2: 133.5 +/- 35.6 natoms/mg protein/min) compared with those from the non-ischemic area (RCI: 4.49 +/- 0.46, St.III O2: 344.0 +/- 31.9).(ABSTRACT TRUNCATED AT 250 WORDS)