HPLC法同时测定加替沙星和奥硝唑的含量

目的建立同时测定加替沙星及奥硝唑含量的高效液相色谱方法。方法分析柱为Hy-persil-ODSC18柱(250mm×4.6mm,5μm);流动相为0.02mol/L磷酸二氢钾缓冲液(含0.5%三乙胺,用磷酸调pH3.0):甲醇:乙腈(65:18:17);流速:1ml/min;加替沙星、奥硝唑检测波长分别为292nm、318nm;柱温为30℃,进样量20μl。结果加替沙星线性浓度范围为8.0～48.0μg/ml(r=0.9998),日内RSD≤0.52%,日间RSD≤0.92%,平均回收率100.53%;奥硝唑线性浓度范围为8.0～48.0μg/ml(r=0.9999),日内RSD≤0.35%,日间RSD≤0.71%,平均回收率100.56%。结论该方法简便、准确、灵敏,可用于同时测定加替沙星和奥硝唑两组分的含量。     

高效液相色谱荧光法测定加替沙星注射液的含量

目的　建立高效液相色谱荧光法测定加替沙星注射液的含量方法。方法　CLC ODS柱 (15mm× 6.0mm ,5 μm ) ,流动相 :0 .0 5mol/L枸橼酸 乙腈 (80∶2 0 ) ,三乙胺调 pH3 .0 ,流速 1mL·min-1,Ex =3 60nm ,Em =465nm ,样品稀释 10 0 0倍 ,进样10 μL。 结果　加替沙星在 4～ 3 2ng范围内线性关系良好 ,回收率 (99.98± 0 .0 6) % ,日内、日间RSD <2 %。 结论　该法简便、快速、准确 ,可用于测定加替沙星注射液的含量。     

加替沙星制剂中有关物质检查与含量测定的高效液相色谱法

目的　建立加替沙星制剂中加替沙星的含量及其有关物质测定的 RP- HPL C法。方法　采用Shimpack VP- ODS柱 (15 0 mm× 4 .6 mm,5 μm) ,流动相为 1%三乙胺 (磷酸调节 p H至 4 .5 ) -乙腈 (82∶ 18,体积比 ) ,检测波长 32 5 nm。结果　加替沙星在 2 .32～ 4 6 .4 8μg/ ml浓度范围内线性关系良好 ,日内及日间 RSD分别为 1.1%和 1.7%。平均回收率为 99.9% ,RSD为 0 .6 5 %。最低检测限为 0 .2 μg/ ml。结论　该方法简单 ,灵敏度高 ,结果准确 ,可用于加替沙星制剂的含量测定及有关物质检查。     

HPLC测定烧伤患者肾脏透析排出液中头孢噻肟钠的含量

目的　测定肾替代治疗的烧伤患者肾脏透析排出液中头孢噻肟钠的含量。方法　用HPLC ,μBondapak C18柱 ,流动相为甲醇 -醋酸钠 (0 0 2mol·L-1,pH 5 0 ) (30∶70 ) ,流速 1 2ml·min-1,检测波长 2 6 0nm。结果　在 1～ 10 0 μg·ml-1的范围内线性良好 ,r =0 9999;日内、日间RSD≤ 2 % ,平均回收率 10 0 2 %。结论　所用方法简便、快速、准确、可用于样品测定。     

高效液相色谱法同时测定复方苯甲酸软膏中两组分含量

目的 :建立以高效液相色谱法同时测定复方苯甲酸软膏中苯甲酸和水杨酸含量的方法。方法 :以HypersilODS为色谱柱 ,磷酸二氢钾溶液为流动相 -甲醇 (78∶22) ,检测波长为254nm。结果 :苯甲酸、水杨酸的线性范围分别为0 4～2 0mg/ml(r=0 9999)、0 2～1 0mg/ml(r=0 9999) ;回收率分别为98 74 % (RSD=0 55 % )、98 67 % (RSD=0 59 % ) ;日内相对标准差分别为0 56 %、0 73 % (n=5) ,日间相对标准差分别为0 75 %、0 82 % (n=5)。结论 :本法可用于复方苯甲酸软膏的含量测定和质量控制 ,且简便、快速、准确。     

RP-HPLC测定犬血浆中磷酸川芎嗪的浓度

目的　建立反相高效液相色谱法测定犬血浆中磷酸川芎嗪 (TMPP)的浓度。方法　采用RP -HPLC ,使用Shim -packCLC-ODSC18柱 (15 0mm× 6 .0mm ,5 μm) ,流动相为甲醇 -水 (6 2∶38) ,流速 1.0ml·min-1,检测波长 2 79nm ,用卡马西平乙腈内标液沉淀蛋白后进样。结果　血浆中磷酸川芎嗪的最低检测浓度为 0 .0 5 μg·ml-1,分析时仅需血浆 10 0 μl。标准曲线线性范围为 0 .2～ 5 0 μg·ml-1,r =0 .9999;TMPP 3种浓度血浆样品的回收率为 99.4 %～ 10 4 .4 % ,日内RSD≤ 4 .5 2 % ,日间RSD≤7.4 6 %。结论　所用方法灵敏、可靠 ,可用于磷酸川芎嗪及其制剂的药物动力学研究     

高效液相色谱法及紫外分光光度法测定替加色罗片的含量

目的 :建立替加色罗片剂含量测定的HPLC法和UV法。方法 :HPLC法———采用C18柱 ,流动相为乙腈∶1%十二烷基硫酸钠缓冲溶液 (含0 .95 %冰醋酸 ) =5 6∶4 4。流速 :2mL·min- 1。检测波长 :314nm。柱温 :4 0℃。UV法———在 314nm处测定替加色罗的吸收度。结果 :HPLC法在 0 .1～ 12 0mg·L- 1的范围内 ,将峰面积A与浓度C进行回归处理 ,A =2 8.93C - 14 .4 6 (r =0 .9999,n =6 ) ,日内RSD≤ 1.11% ,日间RSD≤ 3.0 9% ,回收率在 10 0 .4 2 %～ 10 3.82 %之间。UV法在 2～ 2 0mg·L- 1范围内线性良好 ,回归方程为A =5 4.2 8C +0 .0 14 8(r =0 .9998,n =7) ,日内RSD≤ 0 .70 % ,日间RSD≤ 0 .92 % ,回收率在 10 1.0 6 %～ 10 3.0 2 %之间。 2种方法测得 3批样品的标示量百分含量均在规定范围内 (90 %～ 110 % )。结论 :HPLC法和UV法均适用于替加色罗片剂的含量测定 ,由于UV法更简便易行 ,在对有关物质进行了较好控制的情况下 ,此法更为适用     

HPLC法测定大鼠肌肉中醋酸地塞米松含量

目的 :建立一种用于测定大鼠肌肉中醋酸地塞米松含量的HPLC法。方法 :固定相为ZorbaxXDB -C8柱 (15 0mm× 4 6mm ,5 μm) ,流动相为甲醇∶水 =6 5∶35 (V/V)。肌肉组织样品匀浆后用二氯甲烷提取 ,流动相溶解残留物 ,氢化可的松为内标 ,在 2 4 2nm处紫外检测。结果 :在 1 0 2 2～ 30 6 6 μg·g-1浓度范围内 ,醋酸地塞米松线性方程为Y =0 0 2 4 4 +0 0 12 1X(r =0 9998) ,日内RSD≤ 3 91% ,日间RSD≤ 7 4 7% ,回收率 >95 % ,最低检测限为 4 5ng·g-1。结论 :本方法能简单、快速、准确地测定大鼠肌肉中醋酸地塞米松的含量     

西洛他唑的高效液相色谱法测定及药动学研究

目的 :建立测定人血浆中西洛他唑含量的高效液相色谱 (HPLC)法 ,并研究西洛他唑片在健康人体内的药动学。方法 :色谱柱为HypersilC18柱(4 .6mm× 2 0 0mm ,5 μm) ,流动相为乙腈 水 (4 5∶5 5 ) ,流速 1.0ml·min-1,柱温 30℃ ,检测波长2 5 4nm ,西洛他唑血浆样品以 2mol·L-1NaOH 无水乙醚 (1∶4 )提取 ,以地西泮为内标。结果 :标准曲线线性范围 2 0～ 2 0 0 0 μg·L-1(r =0 .9999)。血浆中西洛他唑最低检测限为 10 μg·L-1。平均提取回收率为 80 .2 %± 3.6 % ,平均方法回收率为 97.0 %±3.8% ,日内RSD≤ 5 .8% ,日间RSD≤ 10 .1%。应用该法研究了 10例健康志愿者口服 10 0mg西洛他唑后的药动学 ;其体内过程符合二室模型 ,tmax为 3.5 8± 1.0 8h ,Cmax为 92 0± 2 30 μg·L-1,AUC0 -48为 11.0± 3.3mg·h-1·L-1。结论 :此法简便、快速 ,适用于药物分析 ,其药动学数据可为临床合理用药、新药研制及剂型改进提供理论依据     

烧伤患者肾脏透析排出液中头孢他啶的含量测定

目的 :测定烧伤患者肾脏透析排出液中头孢他啶的含量。方法 :采用高效液相色谱法 ,色谱柱 :μ Bondapak -C18 柱 ;流动相 :甲醇 -醋酸胺 (17∶83 ,V/V ) ;流速 :1 0ml/min ;检测波长 :254nm。结果 :头孢他啶在0 5～100μg/ml的范围内线性关系良好 ,r=0 9999 ;日内、日间RSD≤3 ,平均回收率100 30 %。结论 :本法简便、快速、准确     

Affective and Anxiety Disorders and Alcohol and Drug Dependence:

Depression and anxiety frequently coexist in patients with substance use disorders. This clinically-oriented article examiens the relationship between these conditions and emphasizes data showing that substances of abuse can cause signs and symptoms of both depression and anxiety. These substance-related syndromes appear to have a different course and prognosis than uncomplicated, independent anxiety and major depressive disorders, and clinicians should consider the role of alcohol and other drugs in all patients presenting with these complaints. The authors will also outline an approach for diagnosing and managing patients with the combination of a substance use and depressive or anxiety disorder.     

Synthesis and anti-nociceptive and anti-inflammatory effects of gaultherin and its analogs

The synthesis of gaultherin (1) and its analogs was carried out to provide 11 glycosides under phase-transfer catalytic conditions. The activities of all synthesized compounds were evaluated by nitric oxide production inhibitory assay in vitro. Methyl 2-O-(4-O-β-d-galactopyranosyl)-β-d-glucopyranosylbenzoate (5f) showed significantly anti-nociceptive and anti-inflammatory effects by the evaluation in vivo. Structure–activity relationships within these compounds were discussed.     

Modelling and simulation of variability and uncertainty in toxicokinetics and pharmacokinetics

Two important methodological issues within the framework of the variability and uncertainty analysis of toxicokinetic and pharmacokinetic systems are discussed: (i) modelling and simulation of the existing physiologic variability in a population; and (ii) modelling and simulation of variability and uncertainty when there is insufficient or not well defined (e.g. small sample, semiquantitative, qualitative and vague) information available. Physiologically based pharmacokinetic models are especially suited for separating and characterising the physiologic variability from the overall variability and uncertainty in the system. Monte Carlo sampling should draw from multivariate distributions, which reflect all levels of existing dependencies in the intact organism. The population characteristics should be taken into account. A fuzzy simulation approach is proposed to model variability and uncertainty when there is semiquantitative, qualitative and vague information about the model parameters and their statistical distributions cannot be defined reliably.     

成骨细胞的功能与损伤和骨质疏松的防治

骨质疏松是一种全身性骨骼疾病,导致骨折风险增加。成人的骨量通过破骨细胞的骨吸收和成骨细胞的骨形成作用来维持动态平衡,治疗骨质疏松症的理想策略是抑制破骨细胞的骨吸收和/或增强成骨细胞的骨形成功能。目前针对保护成骨细胞及增强其功能的骨质疏松疗法相对较少。因此,本文针对成骨细胞相关功能蛋白、各种细胞损伤机制（内质网应激、氧化应激、机械过载、微小RNA和长链非编码RNA的影响等）及骨质疏松的治疗与预防作一综述,以期为针对增强成骨细胞功能的骨质疏松治疗策略提供新思路。     

Self-stimulation and amphetamine: Tolerance to d and l isomers and cross tolerance to cocaine and methylphenidate

The effects of the d and l isomers of amphetamine on self-stimulation responding were tested following acute and chronic administration. Tolerance and post-drug depression of responding occurred in tests with both isomers, indicating no role for p-hydroxynorephedrine (PHN) which is one of the metabolites of d-amphetamine. In the second experiment, d-amphetamine, methylphenidate and cocaine all produced quantitatively and qualitatively similar effects on self-stimulation responding following acute administration. Following chronic administration of d-amphetamine, animals showed tolerance to all three drugs, indicating cross-tolerance among them. These data are consistent with an hypothesis that tolerance and post-drug depression following chronic amphetamine treatment are the result of decreases in postsynaptic receptor sensitivity, which would lead to a decreased effectiveness of all three drugs, regardless of their pre-synaptic mechanisms.     

益生菌与肿瘤防治

益生菌广泛存在于自然界中,通过维持宿主体内菌群平衡、影响肠屏障功能和调节免疫应答等作用,提高宿主健康水平,被公认为"肠道健康卫士".一些益生菌可以增强机体的免疫功能,抑制致癌物质,影响肿瘤细胞的基因表达,对肿瘤具有拮抗作用.大量研究表明,益生菌在未来的肿瘤防治中有很好的应用和发展前景.     

Acamprosate and naltrexone treatment effects on ethanol and sucrose seeking and intake in ethanol-dependent and nondependent rats

Rationale  Two pharmacotherapies are approved for treating alcohol craving (acamprosate and naltrexone), but both have shown mixed findings in animals and humans. Objectives  The present experiments utilized a “reinforcer blocking” approach (i.e., rats were able to consume ethanol during treatment) to better understand the efficacy of these treatments for ethanol seeking and drinking using ethanol-dependent and nondependent rats. Materials and methods  In “nondependent” experiments, drugs (acamprosate 50, 100, and 200 mg/kg; naltrexone 0.1, 0.3, and 1.0 mg/kg) were administered over 3-week periods prior to operant sessions with a low response requirement to gain access to reinforcers for 20 min. For “dependent” experiments, rats were made dependent in vapor/inhalation chambers. Results  Acamprosate and naltrexone had similar effects on intake in nondependent and dependent rats; neither drug was selective for ethanol over sucrose drinking. In nondependent animals, naltrexone was more efficacious at more doses than acamprosate, and acamprosate’s effects were limited to a dose that also had adverse effects on body weight. Both pharmacotherapies showed more selectivity when examining reinforcer seeking. In nondependent rats, acamprosate and naltrexone had response-attenuating effects in ethanol, but not sucrose, groups. In dependent animals, acamprosate had selective effects limited to a decrease in sucrose seeking. Naltrexone, however, selectively decreased ethanol-seeking in nondependent rats. Conclusions  The naltrexone-induced decreases in seeking suggested a change in incentive motivation which was selective for ethanol in nondependent rats. The “nondependent” paradigm may model early stages of “problem drinking” in humans, and the findings suggest that naltrexone could be a good intervention for this level of alcohol abuse and relapse prevention.     

Antiinfective and encrustation-inhibiting materials--myth and facts

Catheters, urethral and ureteral stents and other urological implants are frequently affected by encrustration and infection due to their permanent contact with urine. Indwelling urinary catheters provide a haven for microorganisms and thus require extensive monitoring. Several surface modification techniques have been proposed to improve the performance of devices including the immobilization of biomolecules, the incorporation of hydrophilic grafts to reduce protein adsorption, the creation of hydrophobic surfaces, the creation of microdomains to regulate cellular and protein adhesion, new polymers and antimicrobial coatings. Physico-chemical explanation to elucidate the mechanism of such encrustation or infection inhibiting materials is still not available. Our series of experiments showed a marked decrease of silver-activity in biological fluids which corresponds with the controversial clinical results obtained with silver coated urinary catheters. Rifampicin/minocycline coated catheters had very low activity against Gram-negative rods, enterococci and Candida spp., the main causing organisms of urinary catheter infection. Surface engineered materials and antimicrobial drug delivery systems will be the next generation of sophisticated urinary catheters and stents, if both efficacy as well as efficiency has been proved clinically.     

Alprazolam and lorazepam single and multiple-dose effects on psychomotor skills and sleep

Summary The effects of alprazolam 0.5 mg and lorazepam 2 mg on cognitive and psychomotor skills were assessed in twelve normal volunteer subjects in a randomised, double-blind, crossover design. Single and multiple dose effects were monitored using a battery of tests comprising critical flicker fusion threshold (CFFT), choice reaction time (CRT), simulated car tracking, and subjective ratings of perceived sedation (LARS) and of sleep behaviour (LSEQ). Compared with placebo baseline scores, treatment with lorazepam 2 mg (both single and multiple doses) resulted in a widespread impairment of CRT, tracking accuracy, and CFFT. Single doses of alprazolam 0.5 mg reduced CFFT with respect to the placebo baseline. Single and multiple dose treatment with both drugs resulted in subjective reports of sedation, a reduction of sleep onset latency, and improved sleep quality. Only lorazepam 2 mg significantly disrupted the integrity of behaviour on waking from sleep. These results suggest important pharmacodynamic differences between the two drugs in the doses used.