旋光法测定阿奇霉素及阿奇霉素片含量

目的 建立阿奇霉素及阿奇霉紊片含量测定方法.方法 以无水乙醇为溶剂,运用旋光法测定阿奇霉素及阿奇霉素片含量.结果 阿奇霉素在5.0～30mg/ml范围内浓度与旋光度呈良好线性关系,回归方程C=-37.6 21298.8x,r=0.9999,平均回收率99.9%,RSD为0.97%(n=9).结论 本法简便易行,结果准确,可作为阿奇霉素及阿奇霉素片的质控方法.     

HPLC法测定阿奇霉素分散片的含量

目的用高效液相色谱法测定阿奇霉素分散片的含量。方法以Hibar RT Pre-Packed柱为固定相,0.1mol.L-10.002M磷酸氢二铵溶液-异丙醇-乙腈(15∶25∶60,pH 9.2)为流动相,流速:1.0ml.min-1,紫外检测波长:210nm的条件下分离测定阿奇霉素分散片。结果阿奇霉素分散片在0.6~3mg.ml-1范围内,浓度与峰面积线性关系良好,r=0.9992,平均回收率为101.2%,RSD为0.8%。结论本法简便、迅速、灵敏度高、重现性好,可用于测定阿奇霉素分散片的含量。     

微生物比浊法测定口服阿奇霉素的效价含量

目的 建立以微生物比浊法测定口服阿奇霉素效价含量的方法.方法 采用比浊法测定阿奇霉素的含量,并对微生物比浊法、管碟法测定阿奇霉素效价的结果进行评价.结果 阿奇霉素的线性范围为0.4～1.32 u·mL-1(r=0.995 9),分散片与颗粒的平均回收率分别为100.11%,100.27%,方法重复性良好(RSD为0.4%),比浊法与管碟法测定结果一致.结论 微生物比浊法具有简便、精确、快速的特点,可以应用于该产品的质量控制.     

HPLC法同时测定阿奇霉素滴眼液中阿奇霉素及苯扎氯铵的含量

目的建立一种高效液相色谱法同时测定阿奇霉素滴眼液中阿奇霉素及苯扎氯铵的含量。方法采用十八烷基硅烷键合硅胶色谱柱(4.6 mm×150 mm,5μm),柱温30℃,以乙腈-磷酸盐缓冲液(取0.05 mol.L-1磷酸氢二钾溶液,用20%磷酸调节pH至8.2)(58∶42)为流动相;检测波长210 nm;流速:1.0 mL.min-1。结果阿奇霉素在1.002 8～5.014 0 mg.mL-1的浓度范围内,苯扎氯铵在6.15μg.mL-1～14.35μg.mL-1的浓度范围内均呈线性。阿奇霉素的平均回收率100.68%,RSD为0.50%(n=9);苯扎氯铵的平均回收率100.59%,RSD为0.92%(n=9)。阿奇霉素与苯扎氯铵的定量限分别为750 ng.mL-1、46 ng.mL-1,平均含量分别为106.94%及100.04%,RSD分别为0.94%及0.67%。仪器重复性RSD值均在2.0%以下。结论本方法简单、准确,可同时测定样品中阿奇霉素及苯扎氯铵的含量。     

阿奇霉素颗粒剂和片剂的人体相对生物利用度及生物等效性评价

目的研究阿奇霉素颗粒剂和片剂在健康人体内的药物动力学及相对生物利用度,为临床合理用药提供依据。方法采用三周期三交叉试验设计,利用建立的液相色谱-串联质谱法测定24名健康男性受试者口服含阿奇霉素0.5 g的阿奇霉素颗粒(受试制剂Ⅰ)、阿奇霉素片A(受试制剂Ⅱ)及阿奇霉素片B(参比制剂)后不同时刻血浆中阿奇霉素的质量浓度,同时绘制血药质量浓度-时间曲线并计算主要药物动力学参数。结果阿奇霉素颗粒、阿奇霉素片A、B血浆中阿奇霉素的tmax分别为(1.9±0.6)、(1.9±0.7)、(1.8±0.6)h,ρmax分别为(441.0±129.5)、(421.7±142.8)、(426.2±128.1)μg.L-1,t1/2分别为(48.0±10.7)、(44.8±8.0)、(45.6±9.8)h,AUC0-t分别为(4 564.6±1 312.0)、(4 743.1±1 616.1)、(4 654.6±1 489.4)μg.h.L-1,AUC0-∞分别为(5 224.6±1 529.7)、(5 373.4±1 854.7)、(5 278.7±1 675.9)μg.h.L-1。以AUC0-t计算,阿奇霉素颗粒剂及片剂的相对生物利用度分别为(99.7±14.0)%和(101.8±13.8)%。结论双单侧检验结果证明,阿奇霉素颗粒及阿奇霉素片A与阿奇霉素片B具有生物等效性。     

高效液相色谱法测定阿奇霉素的含量

目的:用高效液相色谱法测定阿奇霉素的含量.方法:以日本岛津CLC-CN柱为固定相,0.1 mol·L-1磷酸二氢钠-甲醇-乙腈(85∶7∶8)为流动相,在pH 3.0～3.5,流速:1 mL·min-1,柱温:40 ℃,紫外检测波长210 nm,灵敏度为0.08 AUFS的条件下分离测定阿奇霉素,并对方法进行了认证.结果:阿奇霉素与其杂质能完全分离,在100～1 000 mg·L-1范围内,浓度与峰面积线性关系良好,r=0.999 6(n=3).阿奇霉素的平均回收率为100.3%(n=9),日内RSD在0.35%～3.90%之间(n=9),日间RSD在0.35%～4.40%(n=9),重复进样精度RSD%在2%以下(n=5).在pH 3～9之间的溶液中及3%双氧水中,阿奇霉素在12 h内含量基本保持不变.结论:本法简便、迅速、灵敏度高及重现性好,可用于测定阿奇霉素的含量.     

猴头菌提取物颗粒减轻小儿阿奇霉素胃肠道反应的疗效观察

目的 探讨用猴头菌提取物颗粒减少与缓解小儿阿奇霉素胃肠道不良反应的作用.方法 将85例6～12岁使用阿奇霉素的患儿按照抽签法随机分为2组,其中治疗组42例,在使用阿奇霉素前30 min口服猴头菌提取物颗粒1.5～3.0 g/次,给予静脉滴注阿奇霉素10 mg/(kg·次),加维生素B6 100 mg/次,浓度1g/L,速度为100～125μg/(kg·min).对照组43例,只使用阿奇霉素加维生素B6静脉滴注,剂量、浓度、滴速均与治疗组相同,但不口服猴头菌提取物颗粒,连续治疗5 d.最后比较2组出现胃肠道不良反应的结果.结果 治疗组显效37例(88.1%),有效4例(9.5%),无效1例(2.4%).对照组则分别为10例(23.3%),24例(55.8%),9例(20.9%).结论 猴头菌提取物颗粒确能有效减轻与缓解阿奇霉素对胃肠道的不良反应,方便实用.     

阿奇霉素片颗粒湿法制粒的工艺研究

目的：探讨阿奇霉素片颗粒的成型工艺。方法采用湿法制粒制备阿奇霉素片颗粒,通过正交实验考察搅拌速度、切碎速度、pvp 浓度、搅拌时间四因素对阿奇霉素片颗粒成品率、水分的影响。结果优选的工艺为搅拌速度80r/ min,切碎速度400r/ min,pvp 浓度5%,搅拌时间13s。结论该工艺稳定可行,可在大生产中推广。     

微生物比浊法测定阿奇霉素颗粒的效价

目的 建立测定阿奇霉素颗粒效价的微生物比浊法.方法 分别采用微生物比浊法和管蝶法对阿奇霉素的含量进行测定和比较研究.结果 阿奇霉素的线性范围为1～10U·mL-1,r=0.9996,平均回收率为99.43%,RSD=0.3%.结论 微生物比浊法具有简便、精确、快速的特点,可以应用于该产品的质量控制.     

小儿阿奇霉素口腔崩解片中阿奇霉素含量的测定

目的测定阿奇霉素口腔崩解片中阿奇霉素的含量。方法依据2005版中国药典阿奇霉素片溶出度检查中的含量测定方法来测定。结果阿奇霉素在15.02～35.06μg·mL^-1的浓度范围内吸收度A和浓度C之间成线性相关,（r=0.9999）;平均回收率为99.9%（n=9）,RSD为0.31%。结论本法简便、准确,适合于本制剂质量控制的快速测定。     

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.     

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.     

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.     

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.