复方酮康唑凝胶剂的研制方法研究

目的制备复方酮康唑凝胶并建立其质控方法。方法以卡波姆-940为凝胶基质,建立酸碱度、卫生学、含量测定等质控方法,并进行刺激性试验、高速离心试验、耐热耐寒试验和室温留样观察等。用高效液相色谱法,C18柱,甲醇-水(75∶25)为流动相,检测波长为240nm,流速1.0ml/min测定复方酮康唑凝胶中酮康唑的含量。结果该剂pH为6.5～7.0,卫生学检查符合规定,酮康唑在4.0～16.0μg/ml范围内,峰面积与浓度呈良好的线性关系(r=0.9999),平均回收率为99.51%,日内相对标准偏差(RSD)为0.86%,日间RSD为1.02%。结论复方酮康唑凝胶剂制备工艺简单,所得制剂质量可控,性质稳定,无刺激性,临床疗效可靠,可满足临床需要。     

复方积雪草苷凝胶的制备与质量控制

目的：制备复方积雪草苷凝胶,并建立其质量控制方法。方法：以卡波姆-940为凝胶的主要基质,建立酸碱度、卫生学、含量测定等质量控制方法,并进行刺激性实验、高速离心实验、耐热耐寒实验和室温留样观察等。采用高效液相色谱法,选用Hypersil ODS柱（ 250 mm×4.6 mm,5 μm）,甲醇-水（58∶42）为流动相,检测波长为205 nm,柱温为35 ℃,流速为1.0 mL?min-1,测定复方积雪草苷凝胶中积雪草苷的含量。结果：复方积雪草苷溶液pH值为6.5～7.0,卫生学检查符合规定,积雪草苷浓度在0.05～0.9 mg?mL-1范围内峰面积与浓度呈良好线性关系（r=0.999 7）,平均回收率为99.05%,RSD为0.62%。结论：该凝胶剂制备工艺简单,质量稳定,质量控制方法准确可靠。     

复方酮康唑散中酮康唑的含量测定

目的建立复方酮康唑散剂中酮康唑的含量测定方法。方法以无水乙醇作溶剂分次提取，采用紫外分光光度法测定酮康唑的含量。结果 酮康唑浓度在10～24 μg·mL 1范围内线性关系良好，线性回归方程为C＝34087A＋0699，r＝0999 9(n＝5)。平均回收率为9948%，RSD＝084%。结论该法可用于复方酮康唑散中酮康唑的质量控制。     

复方环丙沙星膜剂的制备与含量测定

［摘要］目的 制备复方环丙沙星膜剂并制定该制剂的含量测定方法。方法 以聚乙烯醇 124、羧甲基纤维素钠为成膜材料，制备复方环丙沙星膜剂。采用等吸收双波长紫外分光光度法进行含量测定。结果环丙沙星浓度测定的线性范围为4～9 μg· mL 1，r＝0.999 7（n=6），平均回收率98.06%，RSD为1.04%；替硝唑浓度测定的线性范围8～18 μg· mL 1，r＝0.998 9（n=6），平均回收率99.17%，RSD为0.82%。结论复方环丙沙星膜剂制备工艺可行，含量测定方法准确可靠，可达到质量控制的目的。     

盐酸左氧氟沙星凝胶剂的制备与质量控制

目的制备盐酸左氧氟沙星凝胶,并建立其质量控制方法.方法以0.5%卡波姆940为凝胶基质,采用高效液相色谱法测定制剂中盐酸左氧氟沙星的含量,并进行稳定性考察和皮肤刺激性试验.结果盐酸左氧氟沙星浓度在12.5～200 mg·L-1范围内线性关系良好,平均回收率为99.9%,RSD为0.02;制剂稳定性良好,对皮肤无刺激性.结论该制剂处方合理,制备工艺简便,质量控制方法简单、准确.     

复方盐酸苯海拉明凝胶的制备与质量控制

目的 研制复方盐酸苯海拉明凝胶,并建立其质量控制方法. 方法 以卡波姆作为凝胶基质,制备复方盐酸苯海拉明凝胶,采用高效液相色谱法进行含量测定. 结果 制备的凝胶均匀细腻,稳定性好;盐酸苯海拉明检测浓度在100～500 μg• mL^-1 范围内线性关系良好（r＝0.999 9）,平均回收率为100.41%,RSD＝0.87%;地塞米松磷酸钠检测浓度在10～50 μg•mL^-1范围内线性关系良好（r＝0.999 4）,平均回收率为100.96%,RSD＝1.15%. 结论 该凝胶制备工艺简单,质量稳定,质量控制方法准确可靠.     

复方酮康唑搽剂的制备和质量控制

目的:制备复方酮康唑搽剂,并制定质量控制标准。方法:以酮康唑、氧氟沙星为主药,制成复方酮康唑搽剂,用紫外分光光度法测定含量。结果:所制备的搽剂质量稳定,无刺激性,酮康唑、氧氟沙星平均回收率分别为100.67%、100.39%,RSD分别为0.86%、0.81%。结论:制剂工艺简单,含量测定操作方法简便,结果准确,适于医院制剂室生产。     

HPLC法同时测定复方酮康唑凝胶中酮康唑、硝酸咪康唑的含量

目的：建立同时测定复方酮康唑凝胶中酮康唑、硝酸咪康唑含量的方法。方法：采用HPLC法,色谱柱为HypersilBDSC18（416mm×200mm,5μm）;以0.5%醋酸铵溶液-0.2%三乙胺的甲醇溶液（20∶80）为流动相;流速为1.0ml·min-1;检测波长为230nm,柱温：30℃,进样量20μl。结果：酮康唑在5.1～510.0mg·L-1浓度范围内有良好的线性关系,r=0.9999。平均回收率为100.3%（RSD=0.38%,n=6）。硝酸咪康唑在5.0～500.0mg·L-1浓度范围内有良好的线性关系,r=0.9999,平均回收率=99.9%（RSD=0.79%,n=6）。结论：该方法能简便、快速、准确、灵敏地同时测定酮康唑、硝酸咪康唑的含量,可以用于复方酮康唑凝胶的质量控制。     

阿昔洛韦凝胶的研制与质量标准

目的研制阿昔洛韦凝胶.方法用卡波姆-940作凝胶基质,制备阿昔洛韦凝胶,建立酸碱度、卫生学、含量测定等质控方法,进行刺激性试验,光照试验,高速离心试验,耐热耐寒试验和自然室温留样考察.结果pH值6.5～7.0,卫生学检查符合规定,含量测定平均回收率100.2%～100.4%,RSD＜0.75%(n=5),且凝胶稳定无变化,无刺激性.结论制备该凝胶工艺简单,所得制剂质量可控,性质稳定,可满足临床用药需求.     

普卢利沙星凝胶的制备与质量控制

目的制备普卢利沙星凝胶剂，并建立其质量控制方法。方法以壳聚糖为凝胶基质，按药剂学原理制备普卢利沙星凝胶剂；采用高效液相色谱法测定制剂中普卢利沙星含量，并进行稳定性实验。结果普卢利沙星浓度在25～125 μg·mL 1范围内线性关系良好，平均回收率为100.55%，RSD=0.31%，制剂稳定性较好。结论该制剂制备工艺简单，质量控制方法可行，制剂质量稳定。     

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.     

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.