HPLC测定盐酸贝那普利片的含量

目的　测定盐酸贝那普利片中贝那普利的含量。方法　采用HPLC ,ZorbaxXDB -C18色谱柱 (5 μm ,4 .6mm× 15 0mm) ,柱温 2 5℃ ,流动相为 0 .0 75 %HAc -甲醇 (35∶6 5 ) ,流速 1.0ml·min-1;DAD检测波长 2 39nm。结果　贝那普利浓度在 0 .8～ 4 8g·ml-1范围内线性关系良好 ,最低检测浓度为 0 .4 μg·ml-1,日内RSD≤ 1.5 1% ,日间RSD≤ 1.6 9% (n =5 ) ,回收率 98.9%～99 .9% (n =5 )。结论　所用方法简便快速 ,准确可靠 ,可用于盐酸贝那普利片的含量测定。     

HPLC法同时测定复方诺氟沙星滴鼻液中的诺氟沙星和盐酸麻黄碱

目的　建立一种快速、准确的高效液相色谱法同时测定诺氟沙星 ( NOR)和盐酸麻黄碱 ( EPH)的含量。 方法　使用 C1 8色谱柱 ,流动相为乙腈— 0 .1%磷酸 ( 15 :85 V/V) ,检测波长为 2 5 6nm。结果 　样品测定在 9min内完成。诺氟沙星在 10～ 60μg· ml- 1 浓度范围内 ,r=0 .9999,RSD= 0 .46% ,平均回收率为 99.91% ;盐酸麻黄碱在 2 5～ 12 5 μg· ml- 1浓度范围内 ,r=0 .9992 ,RSD=0 .5 1% ,平均回收率为 10 0 .0 3%。 结论 　方法可快速准确地检测复方诺氟沙星滴鼻液中的诺氟沙星和盐酸麻黄碱含量     

导数分光光度法测定祛白酊中醋酸氢化可的松的含量

目的　建立祛白酊中醋酸氢化可的松的含量测定方法。方法 　应用导数分光光度法测定祛白酊中醋酸氢化可的松的含量。结果 　醋酸氢化可的松在 11～ 19μg· ml- 1呈良好的线性关系 ( r=0 .9996) ,其含量测定平均回收率 10 0 .9% ,RSD=0 .9% ( n=5 )。结论 　方法简便快速 ,结果准确可靠 ,可用于祛白酊中醋酸氢化可的松的含量测定     

高效液相色谱法测定鼻眼净滴鼻剂的含量

目的 :建立测定鼻眼净滴鼻剂中盐酸萘甲唑林含量的高效液相色谱法。方法 :采用HypersilBDSC18(5 μm ,4mm× 15 0mm)色谱柱 ,以甲醇 0 .0 5mol·L-1硫酸铵 (5 0∶5 0 )为流动相 ,紫外检测波长 2 81nm ,外标法定量。结果 :盐酸萘甲唑林浓度在 0 .5～ 2 0 μg·ml-1范围内呈线性关系 ,方法回收率为 99.2 % (n =6 ) ,RSD为 0 .5 %。结论 :此法避免了羟苯乙酯的干扰 ,灵敏度高 ,重现性好 ,结果准确 ,适用于该制剂的质量控制     

高效液相色谱法测定氯麻滴鼻液中氯霉素和盐酸麻黄碱的含量

目的 :建立测定氯麻滴鼻液中氯霉素和盐酸麻黄碱含量的高效液相色谱法。方法 :采用反相 μ Bondpak色谱柱 ,甲醇- 0 .0 2mol·L-1磷酸二氢钾 (5 5∶45 ,磷酸调 pH值3.5 )为流动相 ,检测波长 2 5 4nm。结果 :氯霉素和盐酸麻黄碱的线性范围分别为 2 0～ 12 0 μg·ml-1(r =0 .9998) ,80～ 480 μg·ml-1(r =0 .9998) ;加样回收率分别为 10 1.4% ,RSD =0 .5 %及 10 0 .8% ,RSD =0 .9% (n =5 ) ,日内RSD分别为 0 .9%和 0 .4% (n =5 ) ,日间RSD分别为 1.0 %和 0 .8% (n =4)。结论 :HPLC法可用于本制剂的含量测定和质量控制 ,方法简便、灵敏、结果准确     

RP-HPLC测定面醑Ⅱ号中甲硝唑和氯霉素的含量

目的　测定面醑Ⅱ号中甲硝唑、氯霉素两者的含量。方法　采用反相高效液相色谱法 ,NovaPakC18色谱柱 (3 9mm× 15 0mm ,4 μm) ,以氢化可的松为内标 ,甲醇 -乙腈 -水 (30∶2 0∶5 0 )为流动相 ;检测波长 2 6 1nm。 结果　一次进样可完成 2种不同化学性质组分的含量测定 ,甲硝唑在 9 6 0～ 4 8 0 0 μg·ml-1、氯霉素在 9 89～ 4 9 4 4 μg·ml-1浓度范围内 ,两组份内标峰面积的比值与其浓度呈良好的线性关系 ,平均回收率分别为 99 1% (RSD =1 6 3% ) ,10 0 9% (RSD =0 90 % )。结论　该方法简便 ,快速 ,准确 ,可作为日常质量控制手段     

HPLC法测定盐酸西替利嗪口服溶液中主成分及三种抑菌剂的含量

摘要：目的:建立HPLC法同时测定盐酸西替利嗪口服溶液中的药物主成分盐酸西替利嗪以及苯甲酸钠、羟苯甲酯和羟苯丙酯三种抑菌剂的含量。方法:采用月旭Ultimate XB-C18色谱柱（250 mm×4.6 mm,5μm）,以0.1 mol·L-1磷酸二氢钠溶液（用磷酸调节p H至3.7）-乙腈（65∶35）为流动相,柱温为35℃,检测波长为232 nm,进样量为20μl。结果:主成分盐酸西替利嗪及三种抑菌剂均得到较好的分离,盐酸西替利嗪在10.2～216.4μg·ml-1范围内线性关系良好（r=0.999 5）,平均回收率为99.8%（RSD=0.6%,n=9）;苯甲酸钠在10.60～211.60μg·ml-1范围内线性关系良好（r=0.999 5）,平均回收率为98.9%（RSD=0.5%,n=9）;羟苯甲酯在11.30～225.40μg·ml-1范围内线性关系良好（r=0.999 9）,平均回收率为98.5%（RSD=0.3%,n=9）;羟苯丙酯在1.30～24.90μg·ml-1范围内线性关系良好（r=0.999 5）,平均回收率为101.1%（RSD=0.5%,n=9）。结论:本法简便、快速,能够同时准确测定盐酸西替利嗪口服溶液中主成分和三种抑菌剂的含量。     

旋光法和紫外分光光度法测定卡地滴眼液含量

目的 :建立卡地滴眼液的含量测定方法。方法 :用旋光法测定卡地滴眼液中卡那霉素的含量 ,用紫外分光光度法测定卡地滴眼液中地塞米松磷酸钠的含量。结果 :在 1.0～ 5 .0mg·ml-1范围内旋光度与卡那霉素的浓度呈线性关系 (r =0 .9999) ,回收率平均为 99.3% ,RSD =0 .4 0 % (n =5 ) ;在 6～ 2 1μg·ml-1范围内吸收度与地塞米松磷酸钠的浓度呈线性关系 (r =0 .9998,n =6 ) ,回收率平均为 99.2 % ,RSD =0 .2 0 % (n =5 )。结论 :本法简便、快速、准确 ,适用于医院制剂的快速检验。     

高效液相色谱法同时测定滴鼻剂中三组分的含量

目的采用高效液相色谱(HPLC)法同时测定滴鼻剂中盐酸麻黄碱、盐酸苯海拉明、地塞米松磷酸钠的含量.方法采用C18色谱柱,流动相为甲醇-0.05 mol*L-1 KH2PO4-三乙胺(58∶42∶0.2),检测波长为221 nm.结果盐酸麻黄碱在1600～2400 mg*L-1浓度范围内线性关系良好(r=0.9994),回收率为99.8%,RSD为1.0%.盐酸苯海拉明80～120 mg*L-1浓度范围内线性关系良好(r=0.9996),回收率为101.0%,RSD为0.9%.地塞米松磷酸钠160～240 mg*L-1浓度范围内线性关系良好(r=0.9991),回收率为99.6%,RSD为0.8%.结论该方法可同时测定滴鼻剂中盐酸麻黄碱、盐酸苯海拉明、地塞米松磷酸钠.     

盐酸达克罗宁凝胶的制备与质量控制

目的 :研制盐酸达克罗宁凝胶剂 ,并制定合适的质量控制。方法 :以卡波姆 94 0为凝胶基质制备盐酸达克较宁凝胶剂 ,用一阶导数光度法进行含量测定。结果 :盐酸达克罗宁溶液在 2～ 16 μg·ml-1范围内 ,浓度C与振幅D有良好的线性关系 ,其回归方程为C =- 0 .0 2 6 1+1.0 70 1D(r =0 .9997) ,平均回收率为 99.8% ,RSD为 0 .5 % (n =6 )。结论 :盐酸达克罗宁凝胶制备工艺简单 ,用一阶导数光度法测定含量快捷、简便、准确。     

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.     

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.     

Alzheimer’s disease – current trends in basic and clinical research. Highlights from the 16th ECNP

Advances in the molecular biological knowledge of neuronal nicotinic acetylcholine receptors (nAChRs) have led to a growing interest by the pharmaceutical industry in the development of novel compounds that selectively modulate nAChR function. The ability of (-)-nicotine, an activator of nAChRs, to enhance attentional aspects of cognition in animals and humans, to exert neuroprotective and anxiolytic-like effects, and presumably to mediate the negative correlation between smoking and Alzheimer's (and Parkinson's) Disease, has focused interest on the potential therapeutic utility of modulators of nAChR function for treatment of some of the deficits associated with these progressive, neurodegenerative conditions. Numerous compounds are known which activate nAChRs and which might serve as lead compounds toward the development of such agents. The pharmacologic diversity of neuronal nAChR subtypes suggests the possibility of developing selective compounds which would have more favourable side-effect profiles than existing agents. This broader class of agents, collectively called cholinergic channel modulators (ChCMs), is anticipated to encompass compounds which would have more favourable side-effect profiles than existing agents, which generally exhibit low selectivity. This selectivity may be achieved by preferentially activating some subtypes of nAChRs (i.e., Cholinergic Channel Activators, ChCAs) or inhibiting the function of other subtypes (Cholinergic Channel Inhibitors, ChCIs). An overview of the biology of nAChRs and the rationale for the use of ChCMs for the treatment of dementia related to neurodegenerative diseases are presented, followed by a discussion of lead compounds and compounds under consideration for clinical evaluation.     

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.