莪术油注射液和莪术油葡萄糖注射液含量测定中聚山梨酯80的影响分析

目的:研究聚山梨酯80对莪术油注射液和莪术油葡萄糖注射液含量测定结果的影响。方法:采用紫外分光光度法。结果:以不同来源、同一来源不同批号的聚山梨酯80为空白,对含量测定结果均有较大影响。同一来源不同用量、不同来源、同一来源不同批号的聚山梨酯80的紫外吸收特性均有较大差异。结论:建议对莪术油注射液和莪术油葡萄糖注射液中聚山梨酯80进行质量控制,并建议修改含量测定方法。     

HPLC法测定复方莪术油栓的含量

目的:建立复方莪术油栓中硝酸益康唑和牻牛儿酮的含量测定方法.方法:采用高效液相色谱法.结果:硝酸益康唑在0.02058～0.205 8 mg·mL-1范围内,牻牛儿酮峰在0.00799～0.079 92 mg·mL-1范围内,线性关系良好;平均回收率分别为97.9%和98.7%,RSD分别为1.5%与1.2%(n＝9).结论:所建方法简便、准确,适用于复方莪术油栓中硝酸益康唑和牻牛儿酮的含量测定.     

头孢唑啉钠与莪术油葡萄糖注射液配伍的稳定性实验研究

目的考察莪术油葡萄糖注射液与注射用头孢唑啉钠的配伍稳定性。方法通过观察色泽变化，测定微粒数、pH值、含量等，确定0，2，4，8h配伍液中莪术油及头孢唑啉钠的稳定性。结果在(20±5)℃条件下，8h内配伍液中莪术油及头孢唑啉钠的含量变化均在±4％以内，配伍液外观、微粒数及pH值均无明显改变。结论莪术油葡萄糖注射液与头孢唑啉钠可配伍使用。     

一次性塑料输液器对莪术油的吸附

目的 :考察输液过程中 ,塑料输液器对莪术油的吸附程度。方法 :用分光光度法测定模拟输液过程中莪术油的含量变化。结果 :证明在输液过程中 ,塑料输液器对莪术油有约 10 %以上的吸附。结论 :一次性塑料输液器对莪术油的吸附应引起临床应用的注意。     

莪术油葡萄糖注射液与维生素C的配伍稳定性

目的 :考察莪术油葡萄糖注射液 (简称莪葡液 )与维生素C的配伍稳定性。方法 :通过观察色泽变化 ,测定微粒、pH、含量等方法 ,确定 0 ,0 5 ,1,1 5 ,2 ,4h配伍液中莪术油及维生素C的稳定性。结果 :在 (2 0± 5 )℃室温下 ,1 5h内配伍液中莪术油及维生素C的含量变化均在± 10 %以内 ,溶液的外观性状、微粒数及pH值均无明显变化。结论 :莪葡液与维生素C配伍后1 5h内稳定。     

莪术油的最新研究进展

莪术油(zedoary turmeric oil)是从莪术干燥根茎中提取的挥发油,具有多种功能,人们对莪术油的研究越来越深入,本文通过查阅大量的参考文献资料,从植物的栽培、莪术油的提取、化学成分、含量测定、药理学、临床应用等几方面进行综述.     

莪术油脂质体的含量测定及方法应用

目的以莪术醇和莪术油的含量为指标,测定评价莪术油脂质体的质量。方法采用高效液相色谱法和分光光度法分别测定不同药脂比脂质体中莪术醇和莪术油的含量,并比较不同药脂比脂质体的包封率及产率。结果莪术油脂质体中莪术油的包封率大于莪术醇的包封率,但产率明显小于莪术醇的产率;莪术油中莪术醇所占比例均发生了变化,随着药脂比的减少,比例依次增大。结论该方法准确可靠,可对莪术油脂质体的质量控制提供参考。莪术油制备成脂质体后原来成分的组成比例发生了一定改变。     

紫外-可见分光光度法测定复方益康唑凝胶中莪术油的含量

目的:建立以紫外-可见分光光度法测定复方益康唑凝胶中莪术油含量的方法。方法:以无水乙醇提取凝胶中的莪术油后稀释至刻度,以香草醛硫酸溶液显色,于(520±2)nm波长处测定其与莪术醇的吸收度,并通过公式计算出莪术油的含量。结果:莪术醇检测浓度在0.051～0.255mg/ml范围内与吸收度线性关系良好(r=0.9999),平均回收率为99.8%(RSD=1.50%)。结论:本方法准确、可靠,可用于本品的含量测定与质量控制。     

莪术油质量控制及药理研究进展

目的 介绍近年来莪术油的化学成分和药理学研究情况。方法 查阅大量关于莪术油提取、含量测定和药理作用的文献,进行综合、分析和归纳。结果 莪术油提取方法有水蒸气蒸馏法、超临界流体萃取法、索氏提取法、微波提取法等;其主要有效成分含量测定有薄层扫描法、气相色谱法、气质联用色谱法、高效液相色谱法等;莪术油具有抗肿瘤、抗血栓、抗菌抗病毒、增强免疫等药理作用。结论 可以采用莪术油的主要有效成分——莪术醇、β-榄香烯、吉玛酮含量来判断药材的质量。     

莪术油质量控制及药理研究进展

目的介绍近年来莪术油的化学成分和药理学研究情况。方法查阅大量关于莪术油提取、含量测定和药理作用的文献,进行综合、分析和归纳。结果莪术油提取方法有水蒸气蒸馏法、超临界流体萃取法、索氏提取法、微波提取法等;其主要有效成分含量测定有薄层扫描法、气相色谱法、气质联用色谱法、高效液相色谱法等;莪术油具有抗肿瘤、抗血栓、抗菌抗病毒、增强免疫等药理作用。结论可以采用莪术油的主要有效成分——莪术醇、β-榄香烯、吉玛酮含量来判断药材的质量。     

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.