氯霉素醋酸泼尼松龙滴眼液有效期的预测

目的:确定氯霉素醋酸泼尼松龙滴眼液(强氯滴眼液)有效期。方法:用HPLC法测定其含量,用光照法及初匀速法对强氯滴眼液稳定性进行考察。结果:强氯滴眼液中二成分经光照均有降解产物产生,其室温(20℃)有效期为12 d,冰箱保存(5℃)有效期37.5 d。结论:本制剂须冰箱保存并采用避光包装的条件下暂定有效期定为30 d。     

氯霉素滴眼液不同贮存条件下稳定性考察

目的:考察氯霉素滴眼液在不同贮存条件下的稳定性,并确定其有效期.方法:取供试品3批分别于(25±2)℃与(4±2)℃条件下贮存9个月,以HPLC法考察贮存期间氯霉素含量的变化情况.结果:两种贮存条件下,氯霉素含量均逐渐降低,且(25±2)℃条件下降低更为明显,有效期分别为4.71个月和24.04个月.结论:贮存温度显著影响氯霉素含量,氯霉素滴眼液宜低温贮存.     

高效液相色谱法测定氯霉素滴眼液含量及降解产物的控制

目的:采用高效液相色谱法分离测定氯霉素滴眼液的含量,并对其中降解产物二醇物进行控制.方法:固定相为KromasilC18色谱柱(4.6 mm×250 mm,5 μm);流动相为甲醇-乙腈-0.15%磷酸(1:2:7);流速为1.0 mL·min-1,检测波长为270 nm.结果:氯霉素的平均回收率为100.94%,RSD为0.49%,氯霉素二醇物的平均回收率为99.61%,RSD为0.97%.结论:本法可同时测定氯霉素滴眼液中氯霉素与氯霉素二醇物的含量,而且简便、快速、准确.     

人工泪液氯霉素滴眼液中防腐剂防腐效力的测定

目的测定人工泪液氯霉素滴眼液中防腐剂羟苯乙酯对大肠埃希菌、金黄色葡萄球菌、铜绿假单胞菌、白色念珠菌和黑曲霉菌的抑菌作用。方法采用微生物学方法和各时间间隔菌落计数表明防腐剂抑菌效果。结果人工泪液氯霉素滴眼液中防腐剂羟苯乙酯对霉菌的作用较强,对其他各菌作用符合标准。结论该方法可有效控制产品内在质量。     

0.5%马来酸右旋噻吗洛尔滴眼液的稳定性

目的 :研究马来酸右旋噻吗洛尔滴眼液的稳定性 ,并预测其室温贮存期。方法 :采用紫外分光光度法测定马来酸右旋噻吗洛尔滴眼液含量 ,以初匀速法预测其有效期。结果 :0 5 %马来酸右旋噻吗洛尔滴眼液在室温下 ,有效期仅70d ,而置于5℃冰箱中贮存 ,有效期可达1 2y。结论 :初匀速法预测药品有效期简便、省时、准确 ,适用于医院制剂稳定性研究。     

复方氯霉素滴眼液中有效成分含量的测定

目的:测定复方氯霉素滴眼液中氯霉素和地塞米松磷酸钠的含量.方法:采用一阶导数紫外分光光度法测定氯霉素含量,吸收度法测定氯霉素和地塞米松磷酸钠的总量以计算地塞米松磷酸钠的含量.结果:氯霉素在25.06～75.18 μg•mL 1浓度范围内线性关系良好,一阶导数光谱图307 nm处C＝1 393.510 5 D＋0.037 2,r＝0.999 9,氯霉素的回收率100.5%,RSD＝0.61%;零阶光谱图242 nm处C＝102.525 6 A－0.712 2,r＝0.999 9,计算出地塞米松磷酸钠的回收率99.0%,RSD＝0.53%.结论:采用本方法测定复方氯霉素滴眼液中有效成分的含量,简便易行,值得推广.     

一阶导数光谱法测定氯霉素滴眼液中氯霉素的含量

目的 建立氯霉素滴眼液中氯霉素的含量测定方法.方法 采用一阶导数分光光度法,样品不经分离处理直接测定氯霉素滴眼液中氯霉素的含量,检测波长为300 nm.结果 线性范围为8～64 mg·L-1,r=0.999 8,平均回收率为99.9%,RSD为1.2%.结论 本法可消除其他组分的干扰,简便易行,适合作为氯霉素滴眼液的质量控制.     

RP-HPLC 测定氯霉素滴眼液中氯霉素的含量

目的采用RP-HPLC测定氯霉素滴眼液中氯霉素的含量.方法用YWG-C18柱,甲醇-水-冰醋酸(70∶30∶0.2)为流动相,检测波长278 nm.结果氯霉素线性范围为12.5～100.0 μg*ml,r=0.9999,3种浓度的氯霉素的平均回收率为97.4%、97.8%和98.2%,RSD＝1.0%(n=6).结论该法准确、快速、简便,可用作氯霉素滴眼液中氯霉素的含量测定.     

氯霉素滴眼液质量稳定性的考察

目的促进氯霉素滴眼液质量稳定性的提高,保证人民用药安全有效。方法对本辖区内经营的氯霉素滴眼液进行抽样测定并分别置254nm和365nm的紫外光灯及40℃的温度下放置一定时间进行测定研究,采用《中国药典》2005年版二部氯霉素滴眼液项下的含量测定、有关物质检查的方法测定。结果抽验的氯霉素滴眼液不合格率为95.83%,主要不合格项目为氯霉素二醇物,经紫外光灯照射、40℃放置一定时间后,氯霉素的含量下降,氯霉素二醇物含量增加,对硝基苯甲醛受紫外光的影响较大而温度对其影响较小。结论①氯霉素滴眼液的储存条件应由20℃以下的阴凉处存放更改为冰箱内保存;②氯霉素滴眼液的处方工艺值得研究和改进。     

高效液相色谱法同时测定氯霉素地塞米松滴眼液两组分的含量

目的 :采用HPLC法测定氯霉素地塞米松滴眼液中氯霉素和地塞米松磷酸钠的含量。方法 :采用C18色谱柱 ,流动相为甲醇 0 .0 2 5mol·L- 1的磷酸二氢钠溶液 (4 8∶52V/V) ,检测波长为 2 40nm。结果 :氯霉素的线性范围为 75～ 1 75μg·ml- 1,r=0 .9994,回收率 99.6 6 %。RSD =1 .0 3%;地塞米松磷酸钠的线性范围为 1 5～ 35μg·ml- 1;r =0 .9992 ,回收率 1 0 4.2 4%。结论 :该方法简便、准确 ,可同时测定滴眼液中氯霉素和地塞米松磷酸钠的含量。     

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.     

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.     

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.     

Aquatic Insects and Trace Metals: Bioavailability,Bioaccumulation, and Toxicity

Abstract

The uptake of metals from food and water sources by insects is thought to be additive. For a given metal, the proportions taken up from water and food will depend both on the bioavailable concentration of the metal associated with each source and the mechanism and rate by which the metal enters the insect. Attempts to correlate insect trace metal concentrations with the trophic level of insects should be made with a knowledge of the feeding relationships of the individual taxa concerned. Pathways for the uptake of essential metals, such as copper and zinc, exist at the cellular level, and other nonessential metals, such as cadmium, also appear to enter via these routes. Within cells, trace metals can be bound to proteins or stored in granules. The internal distribution of metals among body tissues is very heterogeneous, and distribution patterns tend to be both metal and taxon specific. Trace metals associated with insects can be both bound on the surface of their chitinous exoskeleton and incorporated into body tissues. The quantities of trace meals accumulated by an individual reflect the net balance between the rate of metal influx from both dissolved and particulate sources and the rate of metal efflux from the organism. The toxicity of metals has been demonstrated at all levels of biological organization: cell, tissue, individual, population, and community. Much of the literature pertaining to the toxic effects of metals on aquatic insects is based on laboratory observations and, as such, it is difficult to extrapolate the data to insects in nature. The few experimental studies in nature suggest that trace metal contaminants can affect both the distribution and the abundance of aquatic insects. Insects have a largely unexploited potential as biomonitors of metal contamination in nature. A better understanding of the physico-chemical and biological mechanisms mediating trace metal bioavailability and exchange will facilitate the development of general predictive models relating trace metal concentrations in insects to those in their environment. Such models will facilitate the use of insects as contaminant biomonitors.