甲氧苄氨嘧啶联合用药的研究及其不良反应防治

目的研究甲氧苄氨嘧啶联合用药的情况及其不良反应的防治,为甲氧苄氨嘧啶的临床合理应用提供参考。方法对近年来有关甲氧苄氨嘧啶的联合用药研究做系统检索,分类综述,总结已得成果,并结合临床实际调查找出存在问题,做出分析。结论使用甲氧苄氨嘧啶时应严格掌握适应症,谨慎联合用药,减少不良反应的发生。     

双波长倍增差法测定复方头孢氨苄胶囊的含量

复方头孢氨苄胶囊系头孢氨苄和甲氧苄氨嘧啶的复方制剂，应用双波长倍增差法［１］可同时测定二种组分的含量，且不用分离提取．此法简便、快速、准确．平均回收率为：头孢氨苄：９９．４３％；甲氧苄氨嘧啶：９９．９０％．     

双波长倍增差法测定复方头孢氨苄胶囊的含量

复方头孢氨苄胶囊系头孢氨苄和甲氧苄氨嘧啶的复方制剂，应用双波长倍增差法可同时测定二种组分的含量，且不用分离提取，此法简便、快速、准确、平均回收率为：头孢氨苄；９９．４３％；甲氧苄氧嘧啶：９９．９０％。     

增效黄连素胶囊的分光光度测定法

增效黄连素胶囊每粒中含盐酸黄连素0.1g,甲氧苄氨嘧啶0.05g。其含量测定方法,盐酸黄连素采用碘量法:甲氧苄氨嘧啶采用提取后分光光度法均颇为费时,本文根据文献(刘耀华、药学通报1985;20(11):     

薄层色谱法同时鉴别增效联磺片中磺胺甲基异噁唑、磺胺嘧啶与甲氧苄氨嘧啶

薄层色谱法同时鉴别增效联磺片中磺胺甲基异噁唑、磺胺嘧啶与甲氧苄氨嘧啶山东省威海市药品检验所２６４２００方彬吕凤莲姜瑛丛培军张宇增效联磺片为磺胺类抗菌消炎药的新型复方制剂，每片含磺胺甲基异唑２００ｍｇ、磺胺嘧啶２００ｍｇ、甲氧苄氨嘧啶８０ｍｇ，各地方...     

非水法测定复方新诺明片中甲氧苄氨嘧啶含量

复方新诺明片中甲氧苄氨嘧啶的含量测定,《天津市药品标准》(82年版)和《中国药典》(85年版)均采用紫外分光光度法,限于基层医院的仪器条件,不易开展;根据甲氧苄氨嘧啶在不同溶剂中的溶解度不同及其弱碱性,将该片剂中的甲氧节氨嘧啶萃取分离后以非水法测定含量,并做了回收试验,现介绍如下:     

增效牛黄喉症片中甲氧苄氨嘧啶的含量测定

增效牛黄喉症片中甲氧苄氨嘧啶的含量测定邱泽雨，秦天德辽宁省药品检验所沈阳１１００２３增效牛黄喉症片是由黄连、甲氧苄氨嘧啶等多种药物组成，用于急慢性咽喉炎、扁桃腺炎，临床效果很好，为了保证药品质量，我们采用薄层－紫外分光光度法，对增效牛黄喉症片中甲氧苄...     

HPLC-化学发光法测定Co.SMZ片中甲氧苄氨嘧啶的含量

在ＫＭｎＯ４－Ｈ＋一还原剂体系中研究了甲氧苄氨嘧啶的化学发光行为,以流动注射化学发光分析法联用ＨＰＬＣ,实现了复方磺胺甲■唑片中甲氧苄氨嘧啶的选择性测定。检出限为 ０．８４μｇ／ｍｌ, ＲＳＤ＝３． ６％,线性范围为：０．００３～１ｍｇ／ｍｌ。     

甲氧苄氨嘧啶对庆大霉素血药浓度及药动学参数的影响

本文用微生物法,在家兔身上分别测定了庆大霉素单独用药和庆大霉素联合甲氧苄氨嘧啶使用时的血药浓度,根据分析C-t曲线,符合一定模型,并计算庆大霉素药物动力学参数,结果发现:TMP使庆大霉素的ke、t1/2、vd、Cl和AUC~(0-∞)发生显著性变化。     

甲氧苄氨嘧啶片的溶出度研究

甲氧苄氨嘧啶片的溶出度研究安徽省马鞍山市药品检验所２４３０１１钱崇付，徐金霞甲氧苄氨嘧啶片（ＴＭＰ）为常用的抗菌增效剂，其生物利用度、疗效与体外溶出度具有密切关系。为全面考察本品质量，本文参照有关文献［１］进行溶出度研究。ｌ仪器与材料ＲＣ－３Ｂ型药物...     

双炔失碳酯—PVP共沉淀物的研究

本文用差示扫描量热法(DSC)筛选确定双炔失碳酯与PVP按1:7～1:9比例以溶剂法制得共沉淀物,其中已不存在双炔失碳酯晶体。用X射线衍射法研究了1:8共沉淀物,证明无双炔失碳酯的晶体衍射峰。经溶出速率测定结果20 min的药物溶出度1:8共沉淀物比原药约大38倍。用导数热重法(DTG)求得1:8共沉淀物与双炔失碳酯的热解动力学参数,其活化能分别为182.8和133.4 kJ/mol,1:8共沉淀物的热解稳定性明显大于原药。小鼠抗着床试验结果表明空白对照组着床数为4.8,53抗孕片(剂量10.6 mg/kg)组为0.9(P<0.05),1:8共沉淀物(剂量5 mg/kg)组为0.2(P<0.01),即1:8共沉淀物抗着床的有效剂量小于53抗孕片的一半。     

溶剂沉积法制备联苯双酯共沉淀物及其性能考察

本文采用溶剂沉积法制备了联苯双酯-PVP-增量物(buking substance)的共沉淀物。DTA分析表明,联苯双酯以非晶态存在于共沉淀物中。体外溶出实验指出,实验所用不同比例的PVP对溶出速度无明显影响(P>0.05),但溶剂不同,其共沉淀物的溶出速度有显著差异(P<0.05),共沉淀物溶出速度较纯药提高5倍。对由CCl_4引起小鼠SGPT升高的抑制作用,共沉淀物用量不到纯药的1/6,其抑制作用还显著地大于纯药(P<0.01).稳定性实验结果可见,本品具有较好的抗湿作用。     

氘代川芎嗪与川芎嗪药理作用比较(一)抗血栓及抗血小板作用

在川穹嗪(TMP)甲基上设计同位素开关(6D-TMP,12D-TMP),以试图减慢TMP氧化代谢,增强药效.对比研究TMP、6D-TMP、12D-TMP等对~(131)I、~(125)Ⅰ-双标记静脉血栓增长模型及血小板聚集的影响.结果表明6D-TMP、12D-TMP体内、体外抗血栓作用均大于TMP;血小板聚集实验表明,随着TMP、6D-TMP、12D-TMP给药剂量增加,三药在一定剂量范围均得良好量效关系,以其IC_(50).估算,12D-TMP与6D-TMP抑制血小板聚集作用强度分别约为TMP的2.67倍及1.27倍.大鼠体内实验亦表明,三药对ADP诱导的血小板聚集有抑制作用,12D-TMP作用最显著.提示对川芎嗪进行结构改造前景广阔.     

The protective effect of tetramethylpyrazine （TMP） against PC12 cells damages

AIM: To discover the protective effects of tetramethylpyrazine (TMP) against PC12 cells damages and explore its protective mechanisms. METHODS: We established three in vitro models to investigate the protective effects of TMP against the injuries. In both of glutamate and natrium azide-induced PC12 injuries, the action of TMP on the cell viability was measured by MTT assay. The LDH efflux was measured by the assay kit, production     

Microencapsulation of Solid Dispersions: Release of Griseofulvin from Griseofulvin:Phospholipid Coprecipitates in Microspheres

The preparation, characteristics, and behavior of microspheres of poly(L-lactic acid) (PLA) containing griseofulvin (Gris) or Gris:phospholipid coprecipitates are described. Microspheres were spherical and increased in size from 17 µm (empty) to 30 µm, containing 22% Gris. The release of coprecipitated Gris after 60 min from 146,000 MW PLA microspheres in pH 2.0 buffer at 37°C was twofold greater than that from microspheres containing pure Gris. Also, the release profile from pure Gris microspheres was 25% lower than its dissolution profile, whereas the dissolution and mi-crosphere release profiles of Gris coprecipitate were the same. Microspheres of Gris coprecipitate suspended in PEG 600 in hard gelatin capsules for 1 week released Gris at levels comparable to the dissolution of coprecipitate. Decreasing the MW of PLA substantially increased the release of Gris from microspheres of coprecipitate after 20 min but insignificantly from microspheres of pure Gris. These findings suggest that microsphere formulation offers some new opportunities in the development of solid dispersions which normally encounter processing difficulties.     

川芎嗪对脂多糖诱导大鼠肾小球系膜细胞增殖及细胞间粘附因子-1表达的影响

目的 :探讨川芎嗪对脂多糖诱导大鼠肾小球系膜细胞增殖及细胞间粘附因子 1表达的影响。方法 :体外培养大鼠肾小球系膜细胞 ,经脂多糖诱导后 ,分别应用噻唑蓝 (MTT)比色法和流式细胞术检测细胞增殖抑制率和细胞周期的变化 ,应用免疫细胞化学法检测细胞表面细胞间粘附因子 1的表达。结果 :川芎嗪呈剂量依赖性的抑制系膜细胞的增殖 ,并阻止细胞由G0 G1期进入S期 ;使系膜细胞间粘附因子 1的表达水平明显减少。结论 :川芎嗪能抑制大鼠肾小球系膜细胞增殖和降低细胞间粘附因子 1表达水平。     

Enhanced dissolution of furosemide by coprecipitating or cogrinding with crospovidone

To increase the dissolution rate of furosemide, cogrinding or coprecipitating of furosemide with crospovidone was carried out. The 1:2 (w/w) ground mixture of furosemide with crospovidone was prepared by cogrinding in a ceramic ball mill and the coprecipitate was prepared by the solvent method using methanol. The dissolution test was carried at 37±0.5°C and 150 rpm in simulated gastric fluids (pH 1.2). The dissolution rate of furosemide was rapid and markedly enhanced by cogrinding or coprecipitating with crospovidone. The X-ray diffraction, IR, DTA and TGA studies showed the physicochemical modifications of the furosemide from the ground mixture or the coprecipitate. Furosemide alone or furosemide contained within a physical mixture was crystalline in nature, whereas furosemide in the ground mixture or the coprecipitate was not crystalline even when preserved at room temperature for 1 year. An interaction, in the ground mixture or in the coprecipitate, such as an association between the functional groups of furosemide and crospovidone may have occurred at the molecular level, changed the thermal property and increased the dissolution of furosemide. The cogrinding or coprecipitating techniques with crospovidone provide a promising way to increase the dissolution rate of poorly soluble drugs.     

川芎嗪的猪口腔粘膜透过特性

目的:确定川芎嗪(TMP)在猪口腔粘膜的主要渗透途径并用体外方法研究药物浓度、供给池pH和TMP油水分配系数对药物透过性的影响.方法:采用在线流通扩散池法进行透过实验,并用Scientist~((R))软件对数据进行处理.结果:稳态流量随药物浓度呈线性增大;透过系数和油水分配系数均随pH的增大而增大,且经细胞内的透过系数 9.05 ×10~(-6)cm·s~(-1)远远大于经细胞间的透过系数 2.99 ×10~(-7)cm·s~(-1).结论:药物经猪口腔粘膜吸收是一个被动扩散过程;药物转运的主要通道为细胞内途径.     

Renal excretion of emtricitabine II. effect of trimethoprim on emtricitabine excretion: In vitro and in vivo studies

The potential interaction between the nucleoside analog emtricitabine (FTC) and trimethoprim (TMP) was assessed in the isolated perfused rat kidney (IPK) model and in vivo in rats. IPK experiments were performed with FTC alone (2 microg/mL) and in the presence of increasing concentrations of TMP (1-10 microg/mL). TMP inhibited FTC excretion in a concentration dependent manner. The IC(50) (TMP concentration associated with a 50% reduction in FTC excretion) was 1.86 +/- 0.37 microg/mL. The results were compared to whole animal studies in rats. Animals received an IV dose of FTC (1 mg/kg) with or without pretreatment with TMP (25 mg/kg). TMP coadministration significantly decreased FTC clearance (7.4 +/- 1.2 mL/min/kg to 2.7 +/- 0.53 mL/min/kg), and elimination half-life was significantly increased (58 +/- 12 min to 215 +/- 44 min). A good correlation was obtained between IPK findings and in vivo data, as FTC renal clearance was reduced approximately 60% in the presence of TMP in both studies. Based on this investigation, TMP would be expected to inhibit the renal excretion of FTC when the two compounds are coadministered, resulting in increased plasma exposure of FTC. However, the clinical significance of this finding remains to be elucidated.     

Trimethoprim/sulfamethoxazole does not affect the steady-state disposition of indinavir.

This study evaluates the safety and potential pharmacokinetic interaction between indinavir and trimethoprim/sulfamethoxazole (TMP/SMZ). In a randomized, three-period crossover fashion, 12 healthy adults received 1 week of indinavir sulfate 400 mg orally every 6 hours with placebo, TMP 160 mg/SMZ 800 mg orally every 12 hours with placebo, and indinavir sulfate with TMP/SMZ. Plasma indinavir, SMZ, and TMP concentrations were determined after the last dose of each treatment period. Concomitant administration resulted in a 17% decrease in geometric mean trough plasma indinavir concentrations (p = 0.032), an 18% increase in geometric mean AUC0-12 h and Cmax TMP values (p = 0.031 and 0.030, respectively), and a 5% increase in geometric mean AUC0-12 h SMZ values (p = 0.039). None of these effects was considered clinically significant. The combination of indinavir sulfate and TMP/SMZ is generally well tolerated, with no clinically significant pharmacokinetic interaction being noted.