高效液相色谱法测定盐酸多巴酚丁胺注射液中盐酸多巴酚丁胺的含量

目的建立测定盐酸多巴酚丁胺注射液中盐酸多巴酚丁胺的含量的HPLC方法。方法采用ODS柱,流动相为乙腈-磷酸盐缓冲溶液（取磷酸铵2.75g,加水950ml,用磷酸调节pH值至2.4,补水至1000ml,摇匀）（梯度洗脱）;检测波长282nm,流速1.0ml/min,柱温30℃。结果盐酸多巴酚丁胺的在浓度93.4～934μg/ml与峰面积呈良好的线性关系,平均回收率为99.9%,RSD为0.11%。结论所建立的方法简便易行,准确可靠,可用于盐酸多巴酚丁胺注射液中盐酸多巴酚丁胺的含量测定。     

盐酸多巴酚丁胺葡萄糖注射液中盐酸多巴酚丁胺的HPLC测定

建立了HPLC法测定盐酸多巴酚丁胺葡萄糖注射液中盐酸多巴酚丁胺的含量.采用ODS柱,流动相为乙腈-磷酸盐缓冲溶液(((NH4)3PO4o3H2O)5.7g,加水1900ml,用磷酸调节pH值至2.4,补水至2000ml,摇匀)(梯度洗脱);检测波长284nm.盐酸多巴酚丁胺的线性范围为186～934 μg/ml,平均回收率为99.9%,RSD为0.11%.     

多巴酚丁胺早期干预喘憋性肺炎预防心衰临床探讨

目的：探讨多巴酚丁胺早期干预治疗喘憋性肺炎,预防心衰的疗效和安全性。方法：将喘憋性肺炎患儿随机分为治疗组46例、对照组43例进行临床分析。治疗组喘憋较重患儿用小剂量多巴酚丁胺2～5μg／（kg·min）≤10mg／次加5％葡萄糖50～100ml维持静脉滴注或微量泵控制,速度约12～20ml／h,维持静脉点滴3～5h。结果：治疗组无新增心衰病例,在喘憋消失、肺部体征消散、早期心衰纠正、总病程时间均短于对照组（P均〈0．01）;两组总有效率差异有显著性（P〈O．01）。结论：多巴酚丁胺可以改善心肺循环,早期干预心衰,未见不良反应。     

用3-甲基苯并噻唑啉-2-酮腙分光光度法测定盐酸多巴酚丁胺(Dobutamine)

本文报道用分光光度法测定盐酸多巴酚丁胺。用3-甲基苯并噻唑啉-2-酮腙(MBTH)作发色剂,在酸性介质中,本品和发色剂的混合水溶液加入硫酸铈(Ⅳ)铵,多巴酚丁胺反应生成桃红色,在510nm处有最大吸收系数(ε_(max)=1.5×10~4mol~(-1)cm~(-1));在4～20μg/ml浓度范围内符合比尔定律。     

多巴胺和多巴酚丁胺联合硝普钠治疗难治性心力衰竭临床观察

目的观察多巴胺、多巴酚丁胺、硝普钠联合治疗难治性心力衰竭（心衰）临床效果。方法选取难治性心衰住院患者100例,随机分为2组,均予强心利尿、扩血管等对症治疗,治疗组加用多巴胺、多巴酚丁胺、硝普钠联合治疗,多巴胺20～60mg,多巴酚丁胺30～60mg入5%葡萄糖溶液500ml静脉滴注,20滴/min,硝普钠25～50mg入5%葡萄糖溶液50ml,以25μg/min开始避光微量泵持续泵入,症状明显控制后逐渐减量,5～7d为1个疗程,在改用其他扩血管药物后停用。结果治疗组总有效率96.0%,对照组总有效率62.0%。治疗组有效率高于对照组（P〈0.05）。结论多巴胺、多巴酚丁胺、硝普钠联合治疗难治性心衰临床疗效佳,且不良反应少,缩短了住院时间,值得基层医院推广。     

盐酸多巴酚丁胺葡萄糖注射液制备工艺研究

目的：研究盐酸多巴酚丁胺葡萄糖注射液的制备工艺。方法：参考美国药典处方考察不同浓度的稳定剂、葡萄糖及盐酸多巴酚丁胺的吸附脱色，不同的灭菌条件及pH值。结果：制定了盐酸多巴酚丁胺葡萄糖注射液的处方与制备工艺。结论：制剂处方合理，工艺简便。     

HPLC法测定己酮可可碱葡萄糖注射液中5－羟甲基糠醛限量

目的采用HPLC法测定己酮可可碱葡萄糖注射液中5-羟甲基糠醛限量。方法ODSC18柱（250×4.6mm,5 μm）,以甲醇：水：三乙胺（50：50：0.1）为流动相,检测波长为284nm。结果回归方程A=4100.91＋53467.52C（r=0.999,n=5）,在浓度1μg/ml-20μg∥ml的范围内线性良好,加样回收率为99.89％,RSD=0.19％。结论本方法准确而灵敏,能有效地控制5-羟甲基糠醛的限量。     

国产微理注射泵持续泵入药物治疗难治性心力衰竭

目的：观察国产微量注射泵持续泵入硝普钠、小剂量多巴胺、多巴酚丁胺治疗难治性心力衰竭的疗效。方法：将硝普钠、多巴胺、多巴酚丁胺分别溶于生理盐水50mL中，采用国产微量注射泵持续泵入，硝普钠起始剂量12.5-25μg/min。结果：显效（心功能由Ⅳ级恢复至Ⅱ级以下）37例（84％），有效（心功能由Ⅳ级恢复至Ⅲ级）7例（16％）。结论：国产微量注射泵持续泵入硝普钠、小剂量多巴胺、多巴酚丁胺治疗难治性心力衰竭，即提高了疗效，又缩短了治疗时间，值得临床推广使用。     

小剂量多巴胺与多巴酚丁胺治疗顽固性心力衰竭的疗效

目的：观察顽固性心力衰竭用小剂量多巴胺与多巴酚丁胺治疗的疗效及安全性。方法：将36例顽固性心力衰竭随机分成对照组和治疗组，对照组在常规治疗基础上采用吸氧、利尿、血管紧张素转换酶抑制剂、地高辛治疗，治疗组在常规治疗基础上加用小剂量多巴胺（1～2μg/kg·min）与多巴酚丁胺注射液（1～2μg/kg＆·min）静点，连续用药5～7天。结果：治疗组心功能改善有效率为94.4%，优于对照组66.7%。结论：小剂量多巴胺与多巴酚丁胺能改善顽固性心力衰竭患者心功能，临床观察安全有效。     

多巴酚丁胺联合环磷腺苷治疗心力衰竭的临床观察

目的探讨多巴酚丁胺联合环磷腺苷对患心力衰竭的老年人的治疗方法及临床效果。方法选取2006～2009年在我院接受治疗的老年心力衰竭患者378例,随机分为3组,每组各126例,Ⅰ组为空白对照组,仅应用一般方法给予洋地黄制剂、利尿剂剂血管扩张剂治疗。Ⅱ组为对照组,单独应用多巴酚丁胺治疗。方法为多巴酚丁胺葡萄糖,以2.5～5.5μg/（kg·min）的速度静脉滴入,1次/d。Ⅲ组为观察组,应用多巴酚丁胺联合环磷腺苷治疗。其中多巴酚丁胺的用法用量与Ⅱ组相同;环磷腺苷的用法为针剂80mg,加入5%葡萄糖注射液250ml中,静脉滴入,1次/d。3组疗程均为10d。治疗前后分别观察各组患者心功能、血压、心率及血氧饱和度变化。结果Ⅱ、Ⅲ组患者应用多巴酚丁胺,左室收缩功能及舒张功能均有改善,但Ⅲ组左室收缩功能改善较Ⅰ、Ⅱ组显著。结论多巴酚丁胺联合环磷腺苷治疗老年心力衰竭临床疗效确切,且较单用多巴酚丁胺及传统的治疗方法更佳,值得临床推广应用。     

Synthesis,Cytotoxicity and Antileishmanial Activity of Some N-(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-amines

We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3) . Hydrolysis of the methyl ester adduct (5) yielded the free acid (6) . The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.     

Efficacy of gut lavage,hemodialysis, and hemoperfusion in the therapy of paraquat or diquat intoxication

Clinical and in vitro investigations were carried out to test the efficacy of gut lavage, hemodialysis, and hemoperfusion in the treatment of poisoning with paraquat or diquat. In a patient suffering from diquat intoxication 130 times more diquat was removed by gut lavage 30 h after ingestion than was removed by complete aspiration of the gastric contents.Determination of in vitro clearances for paraquat and diquat by hemodialysis showed that, at serum concentrations of 1–2 ppm, such as are frequently encountered in poisoning in man, toxicologically relevant quantities of herbicide cannot be removed from the body. At a concentration of 20 ppm, on the other hand, hemodialysis proved to be effective, the clearance being 70 ml/min at a blood flow rate of 100 ml/min. The efficacy of hemoperfusion with coated activated charcoal was on the whole better. Especially at concentrations around 1–2 ppm, the clearance values for hemoperfusion were some 5–7 times higher than those for hemodialysis.In a patient suffering from paraquat poisoning, both hemodialysis as well as hemoperfusion were carried out. The in vitro results could be confirmed: At serum concentrations of paraquat less than 1 ppm no clearance could be obtained by hemodialysis while by hemoperfusion with activated charcoal quite high clearance values were measured and the serum level dropped down to zero.

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Zusammenfassung Klinische Untersuchungen und Laboratoriumsversuche wurden durchgeführt, um die Wirksamkeit von Darmspülung, Hämodialyse und Hämoperfusion bei Paraquat- und Deiquat-Vergiftungen zu prüfen.Bei einem Patienten wurde 30 Std nach Deiquat-Aufnahme durch Darmspülung 130mal mehr Deiquat entfernt als durch vollständige Aspiration des Mageninhaltes. In vitro-Versuche ergaben, daß bei Blutserumkonzentrationen von 1–2 ppm, die bei Vergiftungen oft gemessen werden, durch Hämodialyse keine toxikologisch relevanten Paraquat- oder Deiquat-Mengen entfernt werden können. Dagegen erwies sich die Hämodialyse bei 20 ppm und einer Blutumlaufgeschwindigkeit von 100 ml/min mit einer Clearance von 70 ml/min als wirksam. Die Hämoperfusion mit beschicheter Aktivkohle war in diesen Versuchen aber eindeutig überlegen, denn insbesondere bei Konzentrationen um 1–2 ppm waren die Clearance-Werte 5–7mal höher als bei der Hämodialyse.Die in vitro-Ergebnisse wurden bei einem Patienten mit einer Paraquat-Vergiftung bestätigt: Bei Konzentrationen unter 1 ppm war die Hämodialyse wirkungslos, während durch Hämoperfusion relativ hohe Clearance-Werte erreicht wurden, so daß der Serumspiegel rasch unter die Nachweisgrenze abfiel.

     

In vitro studies on sterically stabilized liposomes (SL) as enzyme carriers in organophosphorus (OP) antagonism

This study describes a new approach for organophosphorous (OP) antidotal treatment by encapsulating an OP hydrolyzing enzyme, OPA anhydrolase (OPAA), within sterically stabilized liposomes. The recombinant OPAA enzyme was derived from Alteromonas strain JD6. It has broad substrate specificity to a wide range of OP compounds: DFP and the nerve agents, soman and sarin. Liposomes encapsulating OPAA (SL)* were made by mechanical dispersion method. Hydrolysis of DFP by (SL)* was measured by following an increase of fluoride ion concentration using a fluoride ion selective electrode. OPAA entrapped in the carrier liposomes rapidly hydrolyze DFP, with the rate of DFP hydrolysis directly proportional to the amount of (SL)* added to the solution. Liposomal carriers containing no enzyme did not hydrolyze DFP. The reaction was linear and the rate of hydrolysis was first order in the substrate. This enzyme carrier system serves as a biodegradable protective environment for the recombinant OP-metabolizing enzyme, OPAA, resulting in prolongation of enzymatic concentration in the body. These studies suggest that the protection of OP intoxication can be strikingly enhanced by adding OPAA encapsulated within (SL)* to pralidoxime and atropine.     

Lung disease and PKCs

The lung offers a rich opportunity for development of therapeutic strategies focused on isozymes of protein kinase C (PKCs). PKCs are important in many cellular responses in the lung, and existing therapies for pulmonary disorders are inadequate. The lung poses unique challenges as it interfaces with air and blood, contains a pulmonary and systemic circulation, and consists of many cell types. Key structures are bronchial and pulmonary vessels, branching airways, and distal air sacs defined by alveolar walls containing capillaries and interstitial space. The cellular composition of each vessel, airway, and alveolar wall is heterogeneous. Injurious environmental stimuli signal through PKCs and cause a variety of disorders. Edema formation and pulmonary hypertension (PHTN) result from derangements in endothelial, smooth muscle (SM), and/or adventitial fibroblast cell phenotype. Asthma, chronic obstructive pulmonary disease (COPD), and lung cancer are characterized by distinctive pathological changes in airway epithelial, SM, and mucous-generating cells. Acute and chronic pneumonitis and fibrosis occur in the alveolar space and interstitium with type 2 pneumocytes and interstitial fibroblasts/myofibroblasts playing a prominent role. At each site, inflammatory, immune, and vascular progenitor cells contribute to the injury and repair process. Many strategies have been used to investigate PKCs in lung injury. Isolated organ preparations and whole animal studies are powerful approaches especially when genetically engineered mice are used. More analysis of PKC isozymes in normal and diseased human lung tissue and cells is needed to complement this work. Since opposing or counter-regulatory effects of selected PKCs in the same cell or tissue have been found, it may be desirable to target more than one PKC isozyme and potentially in different directions. Because multiple signaling pathways contribute to the key cellular responses important in lung biology, therapeutic strategies targeting PKCs may be more effective if combined with inhibitors of other pathways for additive or synergistic effect. Mechanisms that regulate PKC activity, including phosphorylation and interaction with isozyme-specific binding proteins, are also potential therapeutic targets. Key isotypes of PKC involved in lung pathophysiology are summarized and current and evolving therapeutic approaches to target them are identified.     

Steroidal sapogenin contents in some domestic plants

In order to find out the values of the steroid resources for the future use. the compositions and contents of steroidal sapogenins from 13 domestic plants have been investigated. As a result,Dioscorea nipponica, D. quinqueloba andSmilax china were found to have large amount of diosgenin. And pennogenin inTrillium kamtschaticum andParis verticillata, yuccagenin inAllium fistulosum, hecogenin inAgave americana and neochlorogenin inSolanum nigum were appeared to be major steroidal sapogenins.