5%碳酸氢钠注射液和葡萄糖注射液配伍的稳定性考察

目的:考察5%碳酸氢钠注射液分别与5%葡萄糖注射液、10%葡萄糖注射液、葡萄糖氯化钠注射液配伍后溶液的稳定性。方法:将5%碳酸氢钠注射液分别与5%葡萄糖注射液、10%葡萄糖注射液、葡萄糖氯化钠注射液按照不同比例配伍后,在0、1、2、3、4、6、8h分别测定配伍溶液的pH值、284nm处吸光度、旋光度。结果:5%碳酸氢钠注射液和含糖注射液配伍后pH值随时间增加而升高,均超过含葡萄糖注射液的规定范围,葡萄糖含量未见下降,5-羟甲基糠醛含量未见增高,并且远低于规定限量。结论:5%碳酸氢钠注射液分别与5%葡萄糖注射液、10%葡萄糖注射液、葡萄糖氯化钠注射液配伍使用是合理的,但为了安全起见,配伍溶液最好在临用前配制并尽快使用。     

注射用地塞米松对头孢曲松注射液的稳定性影响分析

目的分析注射用地塞米松在5%葡萄糖溶液中对头孢曲松注射液的稳定性影响。方法配伍后6h的头孢曲松浓度变化应用高效液相色谱法(HPLC)测定,不溶性微粒含量用光阻法测定,观察配伍液的外观及检测配伍液的pH值。结果在室温的6h内,配伍液中头孢曲松的浓度、外现及pH值无明显变化,且不溶性微粒含量符合国家规定。结论室温时6h内,注射用地塞米松在5%葡萄糖溶液中对头孢曲松注射液稳定性无影响。     

温度对环磷酰胺注射液配制及配伍后稳定性的影响

目的考察温度对环磷酰胺(cyclophosphamide,CTX)注射液配制的影响及配伍后CTX在5种溶液中的稳定性。方法按临床常规给药剂量配制CTX注射液,放置于不同温度水浴(20,40,60℃),记录完全溶解所耗时间并测定溶解后的含量有否变化。将配伍后的溶液,于不同条件下(8和20℃避光,20,30℃)放置24 h,用高效液相色谱(HPLC)法测定配伍后不同时间点溶液中CTX的含量,同时观察外观性状、紫外吸收光谱和HPLC色谱图的变化。结果在40℃水浴温度条件下CTX溶解较快(≤15 min),且稳定性较好,而在20℃条件下完全溶解耗时太长(40~50min),在60℃条件下CTX溶解后含量下降明显(幅度约为15%);于8和20℃避光及20,30℃条件下放置,CTX与5种常用输液的配伍溶液在24 h内含量较稳定(RSD≤6%),其外观性状、紫外吸收光谱图在观察其间无明显变化,色谱图中除峰面积有变化外未见其他变化。结论CTX溶液配制以水浴温度40℃助溶为宜,配伍后CTX溶液在8和20℃避光及20,30℃条件下在观察的24 h内较稳定,以8和20℃避光保存最佳。     

维生素K1与维生素C等药物配伍的稳定性研究

目的研究维生素K1注射液与注射用维生素C(唯西)、注射用肌苷(奇方能)等在葡萄糖(葡萄糖氯化钠)注射液中配伍的稳定性;方法采用高效液相色谱法测定维生素K1注射液在葡萄糖(葡萄糖氯化钠)注射液中与注射用维生素C(唯西)、注射用肌苷(奇方能)等配伍前后溶液的含量,并观察配伍溶液的外观、pH值、微粒以及含量的变化。色谱柱:HypersilBOSC18柱(4.6mm×200mm,5μm);流动相:无水乙醇-乙醚(95:5);柱温:25℃;检测波长:254nm;流速:1.0ml/min;进样量:10μl。结果维生素K1注射液,在葡萄糖(葡萄糖氯化钠)注射液中与注射用维生素C(唯西)、注射用肌苷(奇方能)等配伍后,5h内溶液的含量、pH值、微粒等均产生明显的变化;结论维生素K1注射液在葡萄糖(葡萄糖氯化钠)注射液中与注射用维生素C(唯西)、注射用肌苷(奇方能)等配伍后,溶液的稳定性较差,维生素K1注射液不宜与注射用维生素C(唯西)等药物配伍。     

配制浓度对奥美拉唑滴注液稳定性的影响

目的探讨配置浓度对奥美拉唑滴注液稳定性的影响。方法使用氯化钠、葡萄糖注射液对奥美拉唑静脉滴注进行不同浓度的配制,使用高效液相色谱仪、p H仪对不同浓度的奥美拉唑滴注液稳定性进行分析。结果奥美拉唑经0.9%氯化钠溶液、5%葡萄糖溶液稀释后,经8h连续观察发现,不同组别滴注液的含量随时间的延长逐渐下降,但并未出现显著的变化,不同组别滴注液的p H随浓度增大逐渐降低,并随时间的延长逐渐降低,未发现有颜色上的变化发生。结论使用0.9%氯化钠溶液、5%葡萄糖溶液对奥美拉唑进行配制,浓度在0.08-0.8g/L范围内,时间在8h内,含量、p H值并未发生显著变化,稳定性较好。     

注射用加替沙星与美洛西林的配伍稳定性考察

目的:考察注射用加替沙星与美洛西林在0.9%氯化注射液和5%葡萄糖注射液中的配伍稳定性。方法:分别考察配伍液在室温(20±1)℃下放置8h内的外观、pH值变化,并用紫外双波长分光光度法测定其含量。结果:2药在0.9%氯化钠注射液中pH值和含量无显著变化,但在4h时配伍液出现极少量细微粉末状沉淀使溶液混浊;在5%葡萄糖注射液中加入美洛西林溶解后再加入加替沙星立即出现少量细微粉末状沉淀并使溶液混浊。结论:注射用加替沙星与美洛西林在0.9%氯化钠注射液中可以配伍使用,但宜在4h内滴注完毕;2药在5%葡萄糖注射液中不能配伍使用。     

温度对环磷酰胺注射液配制的影响及配伍后的稳定性

目的 考察温度对环磷酰胺(cyclophosphamide, CTX)注射液配制的影响及配伍后CTX在5种溶液中的稳定性。方法 按临床常规给药剂量配制CTX注射液，放置于不同温度水浴（20，40，60 ℃），记录完全溶解所耗时间并测定溶解后的含量有否变化。将配伍后的溶液，于不同条件下（8 和20 ℃避光，20，30 ℃）放置24 h，用高效液相色谱（HPLC）法测定配伍后不同时间点溶液中CTX的含量，同时观察外观性状、紫外吸收光谱和HPLC色谱图的变化。结果在40 ℃水浴温度条件下CTX溶解较快（≤15 min），且稳定性较好，而在20 ℃条件下完全溶解耗时太长（40～50 min），在60 ℃条件下CTX溶解后含量下降明显（幅度约为15%）；于8和20 ℃避光及20，30 ℃条件下放置，CTX与5种常用输液的配伍溶液在24 h内含量较稳定(RSD≤6%)，其外观性状、紫外吸收光谱图在观察其间无明显变化，色谱图中除峰面积有变化外未见其他变化。结论CTX溶液配制以水浴温度40 ℃助溶为宜，配伍后CTX溶液在8和20 ℃避光及20，30℃条件下在观察的24 h内较稳定，以8和20 ℃避光保存最佳.     

注射用埃索美拉唑钠与6种常用溶媒配伍的稳定性

摘要目的探讨注射用埃索美拉唑钠在6种常见溶媒中的稳定性,为临床合理配制提供参考依据。方法将注射用埃索美拉唑钠与100 mL的5%葡萄糖注射液、5%葡萄糖氯化钠注射液、10%葡萄糖注射液、0.9%氯化钠注射液、果糖注射液及木糖醇注射液配伍,测定溶液的pH,采用高效液相色谱法测定配伍液中埃索美拉唑钠的含量,定时观察溶液的颜色及澄明度。结果注射用埃索美拉唑钠标准曲线在0.05～1.60 mg·mL－1浓度范围内,线性关系良好（R2＝0.999 9）;与0.9%氯化钠注射液、木糖醇注射液配伍后,24 h内pH、澄明度及含量无明显变化;与10%葡萄糖注射液、5%葡萄糖注射液、5%葡萄糖氯化钠注射液配伍后分别在12,8,6 h内pH、澄明度及含量无明显变化,溶液稳定;与果糖注射液配伍后,pH、澄明度及含量均有明显变化。结论埃索美拉唑钠不宜与果糖配伍,宜与0.9%氯化钠注射液、木糖醇注射液配伍,若与10%葡萄糖注射液、5%葡萄糖注射液、5%葡萄糖氯化钠注射液配伍,应分别在12,8,6 h内滴注完。     

注射用比阿培南与5种输液配伍稳定性考察

目的建立HPLC法测定注射用比阿培南的含量,并考察其与0.9%氯化钠、5%葡萄糖、10%葡萄糖、葡萄糖氯化钠、复方氯化钠注射液配伍的稳定性。方法采用色谱柱Symmetry C18（4.6×150mm,5μm）、流动相为醋酸盐缓冲液∶乙腈（100∶3,v/v）、检测波长294nm;在25℃、室内自然光照射下观察配伍液的外观变化,同时监测配伍液pH值及比阿培南含量的变化。结果比阿培南线性范围0.01~1.0mg.mL-1,r=0.9998（n=8）;平均回收率99.57%,RSD 1.30%,最低定量限58ng.mL-1（S/N≥10）。在0.9%氯化钠注射液、5%葡萄糖注射液中10h,葡萄糖氯化钠注射液中8h,10%葡萄糖注射液中5h,比阿培南的含量变化均〈5%;在复方氯化钠注射液中,3h时比阿培南的含量即小于95%。5种配伍液pH值均略降低,但24h内皆未超出药典规定范围。葡萄糖氯化钠配伍液6h起,10%葡萄糖配伍液10h起,颜色开始逐渐变黄加深。结论在25°C室内自然光照射下,比阿培南可与除复方氯化钠以外的本文其他4种输液配伍使用,但须注意稳定时间有所差别。本文建立的HPLC法适用于比阿培南含量测定。     

注射用盐酸表柔比星与胰岛素在葡萄糖注射液中的配伍稳定性考察

目的:考察在葡萄糖溶液中表柔比星和胰岛素配伍的稳定性。方法:观察室温、避光24 h内表柔比星-胰岛素-5%葡萄糖配伍液的外观、pH、不溶性微粒的变化,采用高效液相色谱法考察配伍液中表柔比星、胰岛素含量的变化。结果:配伍液在24 h内无浑浊、沉淀、气体产生,颜色、pH、不溶性微粒数等无明显变化,表柔比星、胰岛素含量无明显变化。结论:在室温下避光放置24 h,表柔比星、胰岛素在5%的葡萄糖注射液中配伍稳定。     

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.     

Gender-related symptoms and correlates of alcohol dependence among men and women with a lifetime diagnosis of alcohol use disorders

This study explored gender-related symptoms and correlates of alcohol dependence in a crosssectional study of 150 men and 150 women with a lifetime diagnosis of alcohol use disorders (AUD). Participants were recruited in equal numbers from treatment settings, correctional centres and the general community. Standardized measures were used to determine participants' use of substances, history of psychiatric disorders and psychosocial stress, their sensation seeking and family history of substance use and mental health disorders. Multivariate analyses were used to detect patterns of variables associated with gender and the lifetime severity of AUD. Men had a longer history of severe AUD than women. Women had similar levels of alcohol dependence and medical and psychological sequelae as men, despite 6 fewer years of AUD. More women than men had a history of severe psychosocial stress, severe dependence on other substances and antecedent mental health problems, especially mood and anxiety disorders. There were differences in family history of alcohol-related problems approximating same-gender aggregation. The severity of a lifetime AUD was predicted by its earlier age at onset and the occurrence of other disorders, especially anxiety, among both men and women. The limitations in the generalizability of these findings due to sample idiosyncrasies are discussed.