马来酸伊索拉啶口腔崩解片的研制

目的:研究马来酸伊索拉啶口腔崩解片的最佳处方和工艺。方法:选用微晶纤维素和低取代羟丙基纤维素作为崩解剂,通过湿法制粒压片制备,以体外崩解时间为指标,采用改进单纯形法优化处方,并测定体外和人体口腔内的崩解时间及体外溶出度等质量评价指标。结果:按照优选处方制得的口腔崩解片的体外崩解时间为(9.30±1.06)s,人体口腔内的崩解时间为(53.86±7.43)s,体外释放迅速,5 min之内释放近70%。结论:本研究所得的处方和工艺可以制备性能优良的伊索拉啶口腔崩解片。     

利培酮口腔崩解片的研制

目的研究利培酮口腔崩解片的最佳处方和制备工艺。方法选用微晶纤维素和交联羧甲基纤维素钠作为崩解剂,通过湿法制粒压片制备,以体外崩解时间为指标,正交试验优化处方,并测定体外崩解时间及口感等质量评价指标。结果优选处方的口腔崩解片的体外崩解时间为(18.26±0.1)s,口感佳。结论本研究所得的处方可以制备性能优良的利培酮口腔崩解片。     

辛伐他汀口腔崩解片的研制及质量评价

目的对辛伐他汀口腔崩解片的处方及制备工艺进行研究,并评价其质量.方法以体外崩解时间和口感为指标,采用正交试验筛选辛伐他汀口腔崩解片的处方.通过直接压片法制备,并测定体外崩解时间及溶出度等质量评价指标.结果优选处方的体外崩解时间为32s,口腔崩解时间为30s,30min的体外溶出度可达95%以上.结论本研究所得的处方和工艺可以制备质量优良的辛伐他汀口腔崩解片.     

银黄口腔崩解片的制备工艺研究及体外评价

目的:优选银黄口腔崩解片的处方和制备工艺。方法:采用单因素考察和星点设计-效应面法,以崩解时限为主要评价指标,优选最佳制备工艺和处方;采用体外溶出度实验考察制备的口崩片与普通片剂的溶出度差异。结果:经效应面法筛选出了最佳处方组合,以优选出的处方,制备3批银黄口崩片,片面光洁圆整、均匀无斑点,口感良好,片重差异在±5%以内,硬度在40N左右,体外崩解时间为(29±0.3)s,口腔内崩解时间为(28±0.5)s。体外溶出度实验表明,所制备的口崩片在15 min内累积溶出达到80%以上,30 min累积溶出达90%以上,明显优于普通片剂。结论:制备的银黄口腔崩解片达到设计要求,硬度适中,崩解迅速,口感良好,服用方便,工艺简单易行。     

阿司匹林口崩片的制备

目的用正交实验法优选阿司匹林口腔崩解片的最佳处方和制备工艺。方法以崩解时间为主要评价指标,选择最佳制备工艺及配方,通过单因素试验选取变量,进行正交试验设计,确定最优处方,通过粉末直接压片制备样品。结果以崩解时间为评价指标筛选出了最佳处方组合,制得3批阿司匹林口腔速崩片,片面光洁圆整、无斑点,崩解时间为21±3 s。结论制备的阿司匹林口腔崩解片崩解时间短、硬度适中、口感好,具备临床应用价值。     

盐酸普萘洛尔口腔崩解片的研制及其质量评价

目的研究盐酸普萘洛尔口腔崩解片的处方、制备工艺和质量评价。方法以崩解时限、外观为考察指标,采用正交设计试验,筛选盐酸普萘洛尔口腔崩解片处方。通过直接压片法制备样品,并测定体外崩解时间及溶出度等质量评价指标。结果所得片剂完整光洁,口感良好,能在15 s内崩解完全,2 min内体外溶出度超过98.45%。结论所用处方和工艺可制备质量优良的盐酸普萘洛尔口腔崩解片。     

多潘立酮口腔崩解片的处方优化及体外评价

目的:优化多潘立酮口腔崩解片的处方并评价其质量。方法:以直接粉末压片法制备多潘立酮口腔崩解片,采用HPLC法测定其含量,以崩解时限和体外溶出度为指标优化处方。结果:以6%的交联聚维酮作为崩解剂,制备的多潘立酮口腔崩解片外观圆整光洁,硬度为(3.3±0.8)kg/cm2,脆碎度<1%,体外崩解时限和口腔内崩解时限分别为(9.00±0.56),(17.00±2.00)s,15min的累积溶出度为(99.22±0.38)%。结论:按最优处方制备的多潘立酮口腔崩解片符合《中华人民共和国药典》2010年版的要求,质控方法准确可靠。     

盐酸异丙嗪口崩片的制备

目的 制备盐酸异丙嗪口崩片并评价其质量.方法 以片剂崩解时限为指标,采用正交试验筛选盐酸异丙嗪口腔崩解片的处方,同时考虑其口感,确定最优处方.通过粉末直接压片法制备,并测定体外崩解时限及溶出度等质量评价指标.结果 优选处方的体外崩解时限为28 s,口腔崩解时间为26 s,3 min的体外溶出度可达85％以上.结论 该处方和工艺可制备质量优良的盐酸异丙嗪口腔崩解片,方便患者服用.     

氯氮平口腔崩解片的制备及质量控制

目的制备氯氮平口腔崩解片并探讨其质量控制。方法考察填充剂微晶纤维素、甘露醇及崩解剂交联羧甲基纤维素钠的用量,以外观、口感及体外崩解时间为指标,通过正交试验优化处方,采用直接压片法制备口腔崩解片,并对其崩解时间、溶出度、含量进行检测。结果氯氮平口腔崩解片在30s内可完全崩解,2min溶出达90％以上,含量符合规定。结论处方设计合理,制备工艺可行,产品质量可控。     

苯甲酸利扎曲普坦口腔速崩片的制备

目的 制备苯甲酸利扎曲普坦口腔速崩片.方法 选用微晶纤维素(MCC)和低取代羟丙基纤维素(LHPC)作为崩解剂,通过粉末直接压片工艺制备口腔速崩片.考察速崩片的性质.结果 当MCC/LHPC的比例为9:1时,其体外崩解时间在20 s以内,体内崩解时间在30 s以内.结论 所制片剂口感良好,优化的工艺可以工业化生产.     

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.