国产盐酸地芬尼多片与原研制剂的溶出曲线和有关物质比较研究

目的:通过测定国产盐酸地芬尼多片和原研制剂的有关物质和溶出度,评价国产仿制制剂与原研制剂的质量一致性.方法:参照《中华人民共和国药典》2015年版方法进行溶出试验,用pH 1.2盐酸溶液、pH 4.0醋酸盐溶液、pH 6.8磷酸盐溶液、水4种溶出介质测定溶出曲线,分析国产制剂与原研制剂的溶出曲线相似性.借助Gastro...     

多烯磷脂酰胆碱治疗抗结核药物所致肝损伤患者疗效及其对血清抗氧化应激指标的影响

目的 观察多烯磷脂酰胆碱治疗抗结核药物所致肝损伤患者的临床疗效及其对血清抗氧化应激指标的影响。方法 选取2018—2020年南平市建阳第一医院收治的抗结核药物所致肝损伤患者64例,采用随机数字表法分为对照组与观察组,各32例。对照组予以甘草酸二铵胶囊,观察组予以多烯磷脂酰胆碱胶囊。2组均连续治疗12周。比较2组临床疗效,治疗前后血清肝功能指标[丙氨酸氨基转移酶(ALT)、天冬氨酸氨基转移酶(AST)、总胆红素(TBiL)、直接胆红素(DBiL)]、血清炎性指标[白介素6(IL-6)、肿瘤坏死因子α(TNF-α)和白介素1β(IL-1β)]、血清抗氧化应激指标[血红素加氧酶(HO-1)、谷胱甘肽过氧化物酶(GSH-Px)与超氧化物歧化酶(SOD)],并观察2组不良反应发生率。结果 观察组总有效率为96.88%,高于对照组的81.25%(χ²=4.010,P=0.045)。治疗12周后,2组ALT、AST、TBiL、DBiL水平低于治疗前,且观察组低于对照组(P<0.01);2组IL-6、TNF-α、IL-1β水平低于治疗前,且观察组低于对照组(P<0.0...     

单剂量和多剂量口服西替伪麻缓释片的人体药动学

目的评价单剂量和多剂量口服西替伪麻缓释片的药动学特征.方法10名健康志愿者单剂量和多剂量口服西替伪麻缓释片后,用LC-MS/MS法同时测定血浆中盐酸西替利嗪和盐酸伪麻黄碱的浓度.结果盐酸西替利嗪和盐酸伪麻黄碱的主要药动学参数如下单剂量Cmax分别为(249.50±55.81)和(433.40±86.29)ng·mL-1,Tmax分别为(1.35±1.06)和(4.00±1.00)h,AUCO～t分别为(2 393.11±684.31)和(5 131.96±1 327.18)ng·h·mL-1;多剂量达稳态Cav分别为(199.91±59.03)和(366.73±126.78)ng·mL-1,Tmax分别为(1.35±1.08)和(3.95±0.60)h,AUCas分别为(2 398.90±708.32)和(4 400.72±1 521.38)ng·h·mL-1,DF分别为(112.35±23.22)%和(86.68±38.38)%.结论西替伪麻缓释片在中国健康人体内安全耐受性良好,盐酸伪麻黄碱具有缓释特征,多剂量给药后药物在体内无明显蓄积现象.     

肌酐和胆固醇试剂对总胆汁酸自动分析的影响

目的 探讨对总胆汁酸自动分析产生交叉污染的项目及解决方法.方法 (1)通过放大的手法,把肌酐和总胆固醇试剂加入混合血清测定其总胆汁酸,与加入蒸馏水的空白对照比较;(2)先测CR接着测TBA 10遍,CHO同CR;(3)先测CR后连续测10次TBA,看其影响至第几管,CHO同CR.结果 肌酐和总胆固醇试剂对总胆汁酸的检测有明显的影响,CR及CHO分别影响到第三及第六管.结论 对这些分析项目的设置不能随意,必须注意位置和程序的设置,必要时加强清洗.     

铁离子对环吡酮胺抑制犬小孢子菌的影响

目的:探索抗真菌药物环吡酮胺可能的作用机制。方法:利用微量液基稀释法和纸片扩散法,测定抗真菌药物环吡酮胺抑制犬小孢子菌时铁离子的作用。结果:所有受试菌株均表现为对环吡酮胺耐药。结论:铁离子参与了抗真菌药物环吡酮胺对犬小孢子菌的抑菌作用。     

延续性护理对首次单采血小板献血者持续献血意愿的影响分析

目的 分析延续性护理对首次单采血小板献血者持续献血意愿的影响.方法 选取2015年9月至2016年9月于本院献血的106例首次单采血小板献血者临床资料,根据护理方式不同,分设对照组(53例)与研究组(53例),对照组予以常规护理,研究组予以延续性护理,比对两组持续献血情况、生活方式变化情况以及献血反应发生情况.结果 研究组不再献血小板及持续献血率(0.00％、94.33％)较对照组(22.64％、32.07％)优,且作息紊乱及坚持运动率(5.66％、77.35％)较对照组(15.09％、24.52％)优,献血反应总发生率24.52％较对照组56.60％低(P＜0.05).结论 给予首次单采血小板献血者延续性护理可促使持续献血者增加,改善献血者生活方式,降低献血反应发生率,值得推广.     

Inhibition of voltage-gated K+ channels and Ca2+ channels by diphenidol

BackgroundAlthough diphenidol has long been deployed as an anti-emetic and anti-vertigo drug, its mechanism of action remains unclear. In particular, little is known as to how diphenidol affects neuronal ion channels. Recently, we showed that diphenidol blocked neuronal voltage-gated Na⁺ channels, causing spinal blockade of motor function, proprioception and nociception in rats. In this work, we investigated whether diphenidol could also affect voltage-gated K⁺ and Ca²⁺ channels.MethodsElectrophysiological experiments were performed to study ion channel activities in two neuronal cell lines, namely, neuroblastoma N2A cells and differentiated NG108-15 cells.ResultsDiphenidol inhibited voltage-gated K⁺ channels and Ca²⁺ channels, but did not affect store-operated Ca²⁺ channels.ConclusionDiphenidol is a non-specific inhibitor of voltage-gated ion channels in neuronal cells.     

Effect of 3'azidothymidine administered in drinking water or by continuous infusion on the development of MAIDS.

LP-BM5 MuLV infection of C57BL/6 mice induces a well characterized, lymphoproliferative, immunodeficiency disease (MAIDS), which is useful for evaluation of potential antiviral agents, because of the reproducibility of virological and clinical endpoints. This MAIDS retrovirus model was used to evaluate 3'azido-2,3'dideoxythymidine (AZT), using different doses, methods of administration and timing for initiation and continuation of therapy. AZT therapy 1 mg/ml in the drinking water given 30 days prior to virus challenge, and continued for 16 weeks, prevented LP-BM5 MuLV dissemination and disease in 13 of 15 treated mice. Efficacy was dose dependent for AZT concentrations of 1, 0.5, and 0.1 mg/ml in drinking water. One mg/ml AZT was most effective in preventing infection if therapy was begun within days prior to virus challenge or within the first four hours after virus inoculation. If treatment was initiated later, disease was delayed. Continuous infusion of AZT, 25 micrograms/h, was effective since virus was not detected in spleens of any mice during the 21 days of AZT treatment. However, after treatment was stopped treated mice became virus positive and disease progressed. Likewise, AZT administration at 1 mg/ml in the drinking water for only 21 days post virus inoculation (p.i.), was not sufficient to prevent virus dissemination or disease.     

大剂量呋塞米持续静脉输注与单次及分次静脉注射在难治性心力衰竭治疗中的疗效观察

目的探讨大剂量呋塞米强化利尿治疗效果及持续静脉输注与单次及分次静脉注射给药在难治性心力衰竭治疗中的疗效差异.方法收集难治性心力衰竭患者21例,给予600 mg·d-1呋塞米强化利尿治疗,观察其利尿效果和电解质、肾功能、神经内分泌因子变化,并采用随机交叉对照设计,对比持续静脉输注与单次及分次静脉注射的临床疗效差异和药动学差异.结果强化利尿患者由治疗前平均尿量(1 154±254)mL·d-1,增加至(2 517±366)mL·d-1,差异极显著,同时伴有血肌酐和肾素水平升高和血钾水平下降.持续静脉输注、分次及单次静脉注射的平均尿量分别为(2 808±415)mL·d-1,(2 473±388)mL·d-1和(2 269±434)mL·d-1,差异极显著.持续静脉输注组高水平血药浓度持续时间更长.结论大剂量呋塞米强化利尿可显著增加利尿效果,改善心脏功能,其中持续静脉输注组疗效显著优于分次静脉注射组和单次静脉注射组.其疗效优越可能与持续静脉输注组高水平血药浓度持续时间更长有关.     

产前地塞米松单疗程与多疗程对早产儿出生指标影响的比较

目的探讨产前应用单疗程及多疗程地塞米松对早产儿出生体重、头围、身长的影响。方法回顾性调查了2005-01～2007-01笔者所在医院产科≤孕34周出生的早产儿出生指标,按母亲产前应用地塞米松的疗程分为三组,进行统计学分析。结果出生体重方面,多疗程组平均体重明显小于单疗程组及未用激素组(P=0.001);单疗程组及未用组相比无显著性差异(P>0.05);头围方面,多疗程组明显低于单疗程及对照组,单疗程组同未用组相比无显著性差异;身长方面,三组无统计学差异(P>0.05)。结论产前多疗程应用地塞米松对早产儿出生指标产生负面影响。     

Antiestrogenic potentials of ortho-PCB congeners by single or complex exposure

Di-ortho PCB congeners 52, 138, 153 and 180, and the mono-ortho coplanar congener 118 have been detected as a complex mixture in human tissue in Korea. This study examined the antiestrogenic effects of samples exposed to single or combination treatment of the ortho-PCB congeners. In order to determined the combined toxicity, a sample mixture (M1, M2, M3, M4, and M5) was designed based on the ortho-PCB congeners found in Korean human tissue. With the exception of PCB 52, the ortho-PCB congeners (PCB 118, 138, 153, and 180) showed weak antiestrogenic activity. The antiestrogenic activity of di-ortho PCB congeners (PCB 138, 153, and 180) was induced by the depletion of endogenous E2 as well as through the ER-dependent pathway, whereas the antiestrogenic activity of mono-ortho PCB 118 was only induced through the depletion of endogenous E2. When the MCF7-BUS cells were treated with mixtures containing the no effective concentration (10(-6) M) of the PCB congeners, M3 (PCB 118 + PCB 138 + PCB 180) and M4 (PCB 118 + PCB 138) had an antiestrogenic effect but the other mixtures (M1; PCB 52 + PCB 118 + PCB 138 + PCB 180, M2; PCB 118 + PCB 138 + PCB 153 + PCB 180, M5; PCB 118 + PCB 180) did not. Although the mechanism for the interaction between the PCB congeners is not completely understood, it was presumed that exposure to a mixture of the PCB congeners might have synergistic effects on their antiestrogenicity through the ER-independent pathway.     

Effect of single or consecutive administration of T-2588 on hepatic-injured male rats

The present study was carried out to examine the effect of single or consecutive administration of T-2588 on liver of male rat injured by the administration of D-galactosamine X HCl. The T-2588 was orally given to hepatic-injured rats at doses of 125 mg/kg and 1,000 mg/kg singly or for consecutive 5 days. A 10 ml/kg dose of the vehicle was orally given to control rats. The results obtained were summarized below. Single administration of T-2588. Twenty-four hours after a single administration of T-2588, the liver taken from control rats apparently indicated galactosamine-induced hepatitis. No drug-related alterations were observed in hepatic functional test, liver weight and histological examinations at either dose of T-2588. Galactosamine-induced hepatitis was not affected by a single administration of T-2588. Consecutive administration of T-2588. Twenty-four hours after a 5-consecutive-day administration of T-2588, galactosamine-induced hepatitis in control rats was restored to the normal state. The cure of galactosamine-induced hepatitis was not affected by a 5-consecutive-day administration of T-2588. The hepatic aldehyde dehydrogenase activity in hepatic-injured rats was not affected by a 5-consecutive-day administration of T-2588.