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NVP-BEZ235逆转伯基特淋巴瘤RAJI细胞阿霉素耐药的研究
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作者 李纯团 朱雄鹏 +7 位作者 王少雄 彭群艺 郑艳 刘生全 卢旭东 王永彬 翁丹 王丹 《中国实验血液学杂志》 CAS CSCD 北大核心 2024年第2期476-482,共7页
目的:研究NVP-BEZ23对耐阿霉素细胞株RAJI/DOX的逆转耐药作用。方法:利用浓度梯度法诱导耐阿霉素细胞株RAJI/DOX;Western blot测定各组细胞Pgp、p-AKT、p-mTOR蛋白水平;MTT法检测细胞抑制率,SPSS软件测定IC50。结果:成功诱导出耐阿霉素... 目的:研究NVP-BEZ23对耐阿霉素细胞株RAJI/DOX的逆转耐药作用。方法:利用浓度梯度法诱导耐阿霉素细胞株RAJI/DOX;Western blot测定各组细胞Pgp、p-AKT、p-mTOR蛋白水平;MTT法检测细胞抑制率,SPSS软件测定IC50。结果:成功诱导出耐阿霉素细胞株RAJI/DOX。耐阿霉素细胞株RAJI/DOX中Pgp、p-AKT、p-mTOR蛋白水平高于亲本细胞RAJI。NVP-BEZ235可引起耐阿霉素细胞株RAJI/DOX中p-AKT、p-mTOR蛋白水平下降。NVP-BEZ235能够抑制耐阿霉素细胞株RAJI/DOX增殖,与阿霉素具有协同作用。结论:PI3K/AKT/mTOR通道在耐阿霉素伯基特淋巴瘤细胞中进一步活化;NVP-BEZ235通过抑制PI3K/AKT/mTOR信号通道活化,能够与阿霉素协同抑制伯基特淋巴瘤耐药细胞,逆转伯基特淋巴瘤耐药细胞对阿霉素的耐药性。 展开更多
关键词 nvp-BEZ235 伯基特淋巴瘤 阿霉素耐药 逆转
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NR2A特异性拮抗剂NVP-AAM077对大鼠海马空间学习和记忆能力的影响
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作者 郑峰 张子涵 +2 位作者 陈建州 金清华 肖斌 《中国药理学通报》 CAS CSCD 北大核心 2024年第8期1517-1522,共6页
目的基于经典水迷宫空间记忆行为范式,观察大鼠学习记忆前后N-甲基-D-天冬氨酸受体(N-methyl-D-aspartic acid receptor,NMDAR)2A亚单位(NR2A)变化,通过海马齿状回微量注射NVP-AAM077(NR2A拮抗剂)探讨其神经药理学作用及可能机制。方法... 目的基于经典水迷宫空间记忆行为范式,观察大鼠学习记忆前后N-甲基-D-天冬氨酸受体(N-methyl-D-aspartic acid receptor,NMDAR)2A亚单位(NR2A)变化,通过海马齿状回微量注射NVP-AAM077(NR2A拮抗剂)探讨其神经药理学作用及可能机制。方法3月龄♂SD大鼠随机分为行为学训练(Training)和未训练(Non-training)两大组,再分别分为对照和齿状回注射NVP-AAM077(NVP)组。Western blot检测齿状回的NR2A、p-eIF2α、ATF4和脑源性神经营养因子(brain-derived neurotrophic factor,BDNF)表达;向NVP组大鼠齿状回注射整合应激反应抑制剂ISRIB,观察齿状回的p-eIF2α水平、ATF4表达及空间记忆能力。结果与Non-training比较,行为学训练促进大鼠齿状回的NR2A和BDNF表达;Training-NVP大鼠齿状回的NR2A和BDNF表达明显减少,p-eIF2α和ATF4表达增加;ISRIB明显抑制ATF4表达,并翻转注射NVP引起的大鼠空间记忆损伤。结论齿状回注射NVP抑制NR2A通路激活并损害大鼠空间记忆,这种作用主要与海马整合应激反应有关。 展开更多
关键词 N-甲基-D-天冬氨酸受体2A亚基 nvp-AAM077 海马 齿状回 空间学习和记忆 整合应激反应
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Sustained heavy ethanol drinking affects CD4<sup>+</sup>cell counts in HIV-infected patients on stavudine (d4T), lamivudine (3TC) and nevirapine (NVP) treatment regimen during 9 months follow-up period
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作者 Godfrey S. Bbosa David B. Kyegombe +2 位作者 William W. Anokbonggo Apollo Mugisha Jasper Ogwal-Okeng 《Health》 2014年第5期432-441,共10页
Sustained heavy ethanol drinking is a common problem globally and ethanol is one of the most abused drugs among individuals of different socio-economic status including the HIV-infected patients on antiretroviral drug... Sustained heavy ethanol drinking is a common problem globally and ethanol is one of the most abused drugs among individuals of different socio-economic status including the HIV-infected patients on antiretroviral drugs. Ethanol is reward drug and a CNS depressant especially at high doses. The study determined the effect of sustained heavy ethanol drinking by HIV-infected patients on d4T/3TC/NVP regimen on CD4+ cell counts in Uganda using WHO AUDIT tool and chronic alcohol-use biomarkers. A case control study using repeated measures design with serial measurements model was used. The patients on stavudine (d4T) 30 mg, lamivudine (3TC) 150 mg and nevirapine (NVP) 200 mg and chronic alcohol use were recruited. A total of 41 patients (20 in alcohol group and 21 in control group) were screened for chronic alcohol use by WHO AUDIT tool and chronic alcohol use biomarkers. They were followed up for 9 months with blood sampling done at 3 months intervals. CD4+ cell count was determined using Facscalibur Flow Cytometer system. Results were then sorted by alcohol-use biomarkers (GGT, MCV and AST/ ALT ratio). Data were analysed using SAS 2003 version 9.1 statistical package with repeated measures fixed model and the means were compared using student t-test. The mean CD4+ cell counts in all the groups were lower than the reference ranges at baseline and gradually increased at 3, 6 and 9 months of follow-up. The mean CD4+ cell counts were higher in the control group as compared to the chronic alcohol use group in both WHO AUDIT tool group and chronic alcohol-use biomarkers group though there was no significant difference (p > 0.05). Chronic alcohol use slightly lowers CD4+ cell count in HIV-infected patients on d4T/3TC/NVP treatment regimen. 展开更多
关键词 SUSTAINED HEAVY ETHANOL DRINKING CD4+ Cell Counts HIV-Infected Patients d4T/3TC/nvp Drug Regimen
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单剂Nevirapine阻断HIV母婴传播:挑战与对策 被引量:2
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作者 曹玮 李太生 《中国艾滋病性病》 CAS 2007年第4期389-392,共4页
母婴传播(mother-to-child-transmission,MTCT)是新生儿HIV感染的主要来源。近年来,由于单剂非核苷类逆转录酶抑制剂Nevirapine(NVP)阻断方案应用于临床,极大地降低了由母婴传播所致的新生儿HIV感染率。尽管存在着病毒耐药性及其不可忽... 母婴传播(mother-to-child-transmission,MTCT)是新生儿HIV感染的主要来源。近年来,由于单剂非核苷类逆转录酶抑制剂Nevirapine(NVP)阻断方案应用于临床,极大地降低了由母婴传播所致的新生儿HIV感染率。尽管存在着病毒耐药性及其不可忽略的长期影响,这一效果肯定、经济简便的方案,在今后很长时期内仍将是发展中国家母婴阻断的首选方案。如何最大限度地避免由NVP耐药性引发的问题,已成了HIV母婴阻断研究的新焦点。该文将对单剂NVP引发的HIV耐药性相关突变、影响及其对策进行综述。 展开更多
关键词 艾滋病病毒 母婴传播 阻断 nevirapine(nvp) 耐药性
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利用NVP组分调控亲水增强型温敏性PNIPAAm共聚物
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作者 范晓光 雷景胜 +3 位作者 顾诗雅 冷旭 刘畅 杨磊 《材料导报》 CSCD 北大核心 2023年第15期230-236,共7页
聚N-异丙基丙烯酰胺(PNIPAAm)是目前在生物医药领域研究和应用最为广泛的一种温敏性聚合物。但PNIPAAm均聚物的温敏性能相对单一,且由其构建的终产物难以在较宽温度范围内通过改变温度发生整体体积或表面润湿性能转变,因此限制了其应用... 聚N-异丙基丙烯酰胺(PNIPAAm)是目前在生物医药领域研究和应用最为广泛的一种温敏性聚合物。但PNIPAAm均聚物的温敏性能相对单一,且由其构建的终产物难以在较宽温度范围内通过改变温度发生整体体积或表面润湿性能转变,因此限制了其应用范围。为了扩展PNIPAAm的应用领域,设计可以调控特别是提升PNIPAAm基材最低临界溶液温度(LCST)的温敏性聚合物十分必要。鉴于此,本研究将亲水性N-乙烯基吡咯烷酮(NVP)引入温敏性聚合物分子骨架,同时利用共聚物的反应基团将P(NIPAAm-co-NVP)共聚物聚合接枝于铂片表面从而形成共聚物膜。衰减全反射-傅里叶变换红外光谱(ATR-FTIR)、核磁共振氢谱(1H-NMR)和凝胶渗透色谱(GPC)的鉴定结果表明各单体间的共聚反应均按预定方案进行,且可显著提升NVP在聚合过程的参与率;动态光散射(DLS)和静态接触角数据、扫描电子显微镜(SEM)图像均证明可以利用NVP组分提升P(NIPAAm-co-NVP)共聚物的LCST,从而获得亲水增强型的温敏性共聚物膜,该膜可用于药物控制释放和非侵害性细胞收获等。 展开更多
关键词 聚N-异丙基丙烯酰胺(PNIPAAm) N-乙烯基吡咯烷酮(nvp) 最低临界溶液温度(LCST) 自由基聚合法 亲水性
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新型逆转录酶抑制剂Nevirapine的合成 被引量:1
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作者 徐晓晖 涂国刚 +2 位作者 麦曦 黄惠明 李少华 《江西化工》 2007年第2期60-62,共3页
艾滋病(AIDS)是严重威胁人类健康的传染性疾病,它是由HIV引发,特别是HIV-1。Nevirapine是一种新型的非核苷类逆转录酶抑制剂,该药与核苷类逆转录酶抑制剂或蛋白酶抑制剂合用可用于治疗艾滋病,单独用药可用于预防HIV感染和母婴传播。本... 艾滋病(AIDS)是严重威胁人类健康的传染性疾病,它是由HIV引发,特别是HIV-1。Nevirapine是一种新型的非核苷类逆转录酶抑制剂,该药与核苷类逆转录酶抑制剂或蛋白酶抑制剂合用可用于治疗艾滋病,单独用药可用于预防HIV感染和母婴传播。本文介绍了Nevirapine的作用机制,着重研究了Nevirapine的合成,并对其合成工艺进行了较为详尽的考察和改进,简化了工艺,提高了收率。以4-甲基-3-硝基-2-羟基吡啶为起始原料,共经六步反应得到Nevirapine,反应总收率为38%。并确证其结构。 展开更多
关键词 抗HIV药物 nevirapine 合成 非核苷类逆转录酶抑制剂 艾滋病 药物治疗 药理学
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Nevirapine induces apoptosis in liver(HepG2) cells 被引量:1
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作者 Jeerang Wongtrakul Atchara Paemanee +6 位作者 Phitchayapak Wintachai Chutima Thepparit Sittiruk Roytrakul Thananya Thongtan Kanokwan Janphen Khuanchai Supparatpinyo Duncan R.Smith 《Asian Pacific Journal of Tropical Medicine》 SCIE CAS 2016年第6期531-536,共6页
Objective: To generate insights into the mechanism of NVP induced hepatotoxicity. Methods: Liver(HepG2) cells were cultured with various concentrations of NVP. This cell line was chosen because it has low expression o... Objective: To generate insights into the mechanism of NVP induced hepatotoxicity. Methods: Liver(HepG2) cells were cultured with various concentrations of NVP. This cell line was chosen because it has low expression of cytochrome P450, allowing evaluation of the effects of NVP rather than specific metabolites. Cytotoxicity was determined using a proliferation assay and cell numbers were monitored using trypan blue exclusion assay for long term culture experiments and apoptosis induction was determined by morphological and biochemical investigation. Results: HepG2 cells treated with the highest concentration of NVP tested(819 μM) initially showed a rounded morphology and all cells had died by week three of exposure. Nuclear condensation and fragmentation, increased Annexin V/propidium iodide staining and caspase 9 activation all supported the induction of apoptosis in HepG2 cells in response to NVP treatment. Conclusions: There is a clear induction of apoptosis in response to NVP which suggests that NVP has significant cytotoxicity, over and above any cytotoxicity of metabolites and may contribute directly to patient hepatotoxicity. 展开更多
关键词 nevirapine APOPTOSIS HEPATOTOXICITY CYTOTOXICITY
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PI3Ks新型抑制剂NVP-BEZ235对食管鳞癌的抑制作用 被引量:1
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作者 姚佳仪 王斯琦 +6 位作者 钱玉兰 孙晓鸣 马赛 杨薇 郭冰 杨中 查良英 《中国药业》 CAS 2023年第9期28-32,共5页
目的探讨磷脂酰肌醇3-激酶(PI3Ks)新型抑制剂NVP-BEZ235(Dactolisib)对食管鳞癌体内外模型的抑制作用,为食管鳞癌的靶向治疗提供参考。方法采用免疫印迹(Western blot)法检测食管鳞癌细胞系中磷脂酰肌醇3-激酶调节亚基p85α(PI3K-p85α... 目的探讨磷脂酰肌醇3-激酶(PI3Ks)新型抑制剂NVP-BEZ235(Dactolisib)对食管鳞癌体内外模型的抑制作用,为食管鳞癌的靶向治疗提供参考。方法采用免疫印迹(Western blot)法检测食管鳞癌细胞系中磷脂酰肌醇3-激酶调节亚基p85α(PI3K-p85α)蛋白的表达情况;对食管鳞癌的细胞系分别给予0,1,4,8,16,32,64,128 nmol/L浓度的NVP-BEZ235,采用MTT法检测生长情况,计算细胞生存率及半数抑制浓度(IC50);对PI3K-p85α高表达及低表达的食管鳞癌细胞系分别予10 nmol/L NVP-BEZ235,观察细胞集落形成情况;建立裸鼠皮下移植瘤模型,评估NVP-BEZ235的体内治疗效果。结果PI3K-p85α高表达的食管鳞癌细胞系KYSE30,KYSE70,KYSE510,TE1对NVP-BEZ235更敏感,IC50分别为4.92,5.43,4.76,7.78 nmol/L;而PI3K-p85α低表达的细胞系KYSE150,KYSE180,KYSE270,KYSE450对NVP-BEZ235的敏感度较低,IC50分别为13.21,18.44,20.37,48.45 nmol/L。加入10 nmol/L NVP-BEZ235进行的集落形成实验结果相似,KYSE30,KYSE70,KYSE510,TE1的集落数目少于KYSE150,KYSE180,KYSE270,KYSE450的集落数目。在裸鼠皮下移植瘤模型中,较低浓度(10 mg/kg)的NVP-BEZ235即可抑制食管鳞癌皮下移植瘤的生长。结论NVP-BEZ235对食管鳞癌细胞系和裸鼠移植瘤都有明显的抑制作用,在PI3K-p85α高表达的食管鳞癌细胞系中抑制效果更明显,在食管鳞癌中具有一定靶向性,可为后期的临床试验提供参考。 展开更多
关键词 食管鳞癌 nvp-BEZ235 磷脂酰肌醇3-激酶调节亚基p85α 靶向治疗
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P(NVP-DVB)的改性及其检测水中双酚A的应用 被引量:1
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作者 张金颐 崔阳 +3 位作者 何柳 张有来 孟祥太 张舜光 《精细化工》 EI CAS CSCD 北大核心 2023年第1期75-86,共12页
为提高水中双酚A(BPA)检测的准确性,采用两步法制备胺功能化聚(N-乙烯吡咯烷酮-二乙烯苯)[P(NVP-DVB)]吸附剂。采用SEM、FTIR、BET、TGA和水接触角测试对两步反应中的样品进行表征,并将胺功能化P(NVP-DVB)用于水中BPA检测。通过优化实... 为提高水中双酚A(BPA)检测的准确性,采用两步法制备胺功能化聚(N-乙烯吡咯烷酮-二乙烯苯)[P(NVP-DVB)]吸附剂。采用SEM、FTIR、BET、TGA和水接触角测试对两步反应中的样品进行表征,并将胺功能化P(NVP-DVB)用于水中BPA检测。通过优化实验得到氯甲基化反应的最佳条件为:以多聚甲醛[(CH_(2)O)n]和盐酸为氯化试剂,Zn Cl_(2)为催化剂,n(HCl)∶n[(CH_(2)O)n]∶n(Zn Cl_(2))=1∶1∶1,反应温度为80℃,氯化时间为3 h,在该条件下制得中间体[P(NVP-DVB-CH2Cl)]氯含量可达11.14%;以苯胺为胺化试剂对P(NVP-DVB-CH2Cl)进行接枝改性制得的P(NVP-DVB-苯胺),其平均孔径为8.59 nm,比表面积为590.36 m^(2)/g,热失重率为70.66%,其对水中BPA的回收效果最好,回收率为99.65%,相对标准偏差为1.96%,其在模拟水样和实际水样中应用效果均较好,且回收率比商业吸附剂提高了近32%。 展开更多
关键词 P(nvp-DVB) 氯甲基化 胺功能化 双酚A 固相萃取 回收率 功能材料
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抗艾滋病药奈韦拉平(nevirapine)能阻止HIV病毒母婴传播 被引量:1
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《中国新药杂志》 CAS CSCD 北大核心 2004年第8期746-746,共1页
关键词 抗艾滋病药 奈韦拉平 nevirapine HIV病毒 母婴传播
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Immunological responses of HIV/AIDS patients treated with Nevirapine versus Efavirenz based highly active anti-retroviral therapy in Addis Ababa, Ethiopia: A retrospective cohort study
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作者 Zemedu Mehamed Tirfe Tekabe Abdosh Ahmed +2 位作者 Negga Baraki Tedla Mesfin Kote Debere Andamlak Gizaw Alamdo 《Health》 2013年第9期1502-1508,共7页
Background: There are two approved non-nucleoside reverse transcriptase inhibitor antiretroviral drugs;namely Nevirapine (NVP) and Efavirenz (EFV). Nevirapine and EFV have comparable clinical efficacy when administere... Background: There are two approved non-nucleoside reverse transcriptase inhibitor antiretroviral drugs;namely Nevirapine (NVP) and Efavirenz (EFV). Nevirapine and EFV have comparable clinical efficacy when administered in combination regimens. But there is a lack of recent evidence showing the effect of NVP and EFV-based ARTs on immunological responses in HIV infected individuals in Ethiopia in general and Addis Ababa in particular. Methods: Retrospective cohort study design was used to compare immunological response rate of NVP and EFV based HAART regimen in Addis Ababa. Four hundred ninety two HIV infected patients who started HAART in ten selected health facilities were included in the study. Rate of immunologic response was examined at the 6th, 12th, 18th, and 24th months of follow-up period. The time required to get immunological response was analyzed by Kaplan-Meier survival curve. Adjusted hazard ratio was calculated with a 95% confidence interval by Cox proportional hazards model to determine the rate of immunological response. To ascertain the association, bivariate and multi variable Cox proportional hazard model was used. Statistical significance was considered with two sides P-value of 0.05. Results: The mean CD4 count ranged between 132.2 cell/μl at baseline and 302.3 cell/μl at the end of the follow-up period. This change was significant at 95% of CI but did not show significant differences among the comparison group. The median time to get immunological response was 18 (75% percental 12) months. At the end of the follow-up period, 73.2% (76.6% for NVP and 69.8% for EVF P-value 0.13) of the study population had immunological response. Conclusion: As a conclusion, there was a robust and sustained CD4 response and the effect of NVP and EFV based ART on change of mean CD4 count and immunological response was comparable and effective. Initiation of ART with high baseline CD4 count, in combination of IPT and with either NVP or EFV based NNTI was recommended. 展开更多
关键词 EFAVIRENZ nevirapine IMMUNOLOGICAL Response Rate Mean CD4 COUNT
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Evaluation of Adherence to Nevirapine for Prevention of Mother-to-Child Transmission amongst Infants of HIV Positive Mothers in the First 6 Weeks of Life in Lagos Nigeria
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作者 Obiyo Nwaiwu Folasade A. Olatunde +2 位作者 Nkechinyere E. Harrison Margaret O. Ilomuanya Oludaisi A. Oduniyi 《World Journal of AIDS》 2019年第2期70-84,共15页
Background: Over 90% of infection in children is acquired through mother to child transmission (MTCT). Nevirapine’s efficacy, safety and affordable cost make it the most preferred non-nucleoside reverse transcriptase... Background: Over 90% of infection in children is acquired through mother to child transmission (MTCT). Nevirapine’s efficacy, safety and affordable cost make it the most preferred non-nucleoside reverse transcriptase inhibitor (NNRTI) for paediatric prophylactic use in resource limited settings. There are very few studies on pediatric adherence to antiretroviral prophylaxis, especially in very young infants. The objective of the study was to evaluate the adherence to nevirapine for prevention of mother to child transmission (PMTCT) amongst infants of HIV positive mothers in the first 6 weeks of life. Methods: This was a questionnaire based prospective cross-sectional multicenter study initiated in July 2015 and concluded in December 2017. The study was carried out at the Aids Prevention in Nigeria (APIN/HIV) human immunodeficiency paediatric clinics of the Lagos University Teaching Hospital (LUTH), Idi-Araba, Lagos State, 68 Nigerian Army Reference Hospital Yaba (68NARHY) Lagos, Nigeria and the Holy Family Catholic Hospital, Festac Town, Amuwo Odofin, Lagos State. Nevirapine adherence, in infants of 0 - 6 weeks was measured by maternal verbal reports. Results: Eighty-one (81) infants receiving nevirapine within the age of 0 - 6 weeks completed the study. Majority of the infants started treatment at birth (32%) and after 4 weeks (31%). 54% of the 81 respondents do not miss or skip their doses while 46% of respondents skip doses. Majority of the respondents 18 (49%) missed their doses for 24 - 48 hours while 25% missed their doses because they were away from home and 23% ran out of pills. 85.2% took ≥95% of the prescribed medications (good or high adherence ), 8.2% took 80% - 95% of doses (moderate adherence) while 6.2% took 0.05). Conclusions: The adherence rates found in this study are comparable to other studies in developing countries. But these rates are still low for good clinical outcomes. Different levels of adherence were documented with the majority having good or high adherence. Not all of the infants started treatment at birth and Institutional delivery should be encouraged to improve early initiation of prophylaxis. The finding of patients with low adherence rates among the study population calls for intensification of counselling on adherence and should continue to be an integral part of prevention of mother to child transmission. Improved access to antiretroviral agents and improved care delivery systems are important. 展开更多
关键词 ADHERENCE INFANTS ANTIRETROVIRAL Prophylaxis Maternal/Caregiver Verbal Reports nevirapine Six Weeks
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Prediction of Dermal Permeability Coefficient of Nevirapine—Effect of Cosolvents, Anionic, Nonionic and Cationic Surfactants
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作者 Chika J. Mbah Theophilus C. Onyekaba Agatha O. Uwakwe 《Pharmacology & Pharmacy》 2016年第7期283-289,共7页
Transdermal drug delivery not only has contributed immensely to medical practice, but has enjoyed enormous interest in the field of cosmetic and pharmaceutical industries. Nevirapine, a non‐nucleoside reverse transcr... Transdermal drug delivery not only has contributed immensely to medical practice, but has enjoyed enormous interest in the field of cosmetic and pharmaceutical industries. Nevirapine, a non‐nucleoside reverse transcriptase inhibitor (NNRTI) is used clinically for the treatment of HIV‐ 1 infection. The aim of the present study is to investigate the influence of cosolvents (glycerol, propylene glycol, ethanol, polyethylene glycol 400) and surfactants (polysorbate 20, polysorbate 80, sodium lauryl sulfate, sodium cholate and cetrimide) on the dermal permeability coefficient of nevirapine by utilizing established and recognized mathematical model that employs partition coefficient as one of its molecular descriptors. The partition coefficient of nevirapine is determined in chloroform-water system at room temperature using the shake flask method. The results show that all the cosolvents used in this study decrease the partition coefficient of nevirapine. The same decrease in the partition coefficient of nevirapine is observed with all the surfactants investigated. The order of dermal enhancement potential of the vehicles studied based on the predicted permeability coefficient is glycerol > propylene glycol > ethanol > polyethylene glycol 400 for the cosolvents while tween 20 > tween 80 > sodium lauryl sulfate > sodium cholate > cetrimide for the surfactants. The maximum predicted flux through skin was obtained by multiplying the predicted permeability coefficient and the drug aqueous solubility. As the rate of penetration into the skin is quantitatively assessed by the use of permeability coefficient, the findings suggest that for dermal formulation of nevirapine, glycerol and tween 20 are the most preferred vehicles out of the vehicles investigated. Furthermore, the results of the correlation coefficients obtained by plotting permeability coefficient or maximum predicted flux, versus logarithm partition coefficient indicate that permeability coefficient can be a more reliable parameter to predict transdermal absorption of nevirapine than flux. 展开更多
关键词 COSOLVENTS SURFACTANTS Partition Coefficient Dermal Permeability Coefficient nevirapine
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Identification, Isolation and Characterization of Unknown Acid Degradation Product of Nevirapine
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作者 Vasudev Pottabathini Vijayacharan Gugulothu +1 位作者 Muralidharan Kaliyaperumal Satyanarayana Battu 《American Journal of Analytical Chemistry》 2016年第9期663-678,共17页
A Novel stability indicating RP-UPLC chromatographic method was developed for analysis of Nevirapine in pharmaceutical formulations. The developed RP-UPLC method is superior in technology to conventional RP-HPLC with ... A Novel stability indicating RP-UPLC chromatographic method was developed for analysis of Nevirapine in pharmaceutical formulations. The developed RP-UPLC method is superior in technology to conventional RP-HPLC with respect to speed, resolution, solvent consumption and cost of analysis. Nevirapine was subjected to the stress conditions like acid, base, thermal, oxidative and photolytic degradation. Nevirapine was found to degrade significantly in acid and thermal degradation. In acid degradation relative retention time with 0.42 is found as unknown impurity. New impurity was identified, isolated using mass based auto purification system and characterized by <sup>1</sup>H NMR (<sup>1</sup>D and <sup>2</sup>D) and HRMS experiments. Isolated impurity was showing molecular weight of 244.10, molecular formula C<sub>12</sub>H<sub>12</sub>N<sub>4</sub>O<sub>2</sub> and its name as 2-(3-Amino-4-methylpyridin-2-ylamino)nicotinic acid. The calibration graph was linear and the method showed less deviation in accuracy results. The test solution was found to be stable for 20 days when stored in the refrigerator between 2°C to 8°C. The developed RP-UPLC method was validated and meets the requirements delineated by the International Conference on Harmonization (ICH) guidelines. The intra-day and inter-day variation was less than 1%. The method was reproducible and selective for the estimation of Nevirapine. Because the method could effectively separate the drug from its degradation products, it can be employed as a stability-indicating method. 展开更多
关键词 nevirapine Method Development Validation Forced Degradation Unknown Impurity ISOLATION Characterization NMR HRMS
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Development, Validation and Application of a Spectrofluorimetric Method for the Quantification of Nevirapine in Pharmaceutical Formulations Tablets and Suspensions
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作者 Lucien Murhula Namegabe Aladin Ombeni Mahano Serigne Omar Sarr 《American Journal of Analytical Chemistry》 2022年第6期206-227,共22页
The development of the spectrofluorimetric method can be considered a promising alternative that is relatively less expensive and sufficiently reliable. In the current literature, no method for the analysis of nevirap... The development of the spectrofluorimetric method can be considered a promising alternative that is relatively less expensive and sufficiently reliable. In the current literature, no method for the analysis of nevirapine by spectro-fluorimetric has been reported. The proposed method is based on the transformation of naturally non-fluorescent nevirapine into a fluorescent derivative after chemical synthesis. Maximum excitation and emission wavelengths are 290 nm and 357 nm respectively. The analytical performance of the method demonstrates linearity in the concentration range 1.5 × 10<sup>-2</sup> and 13.5 × 10<sup>-2</sup> μg/mL with a correlation coefficient (r) greater than 0.999. The detection (LOD) and quantification (LOQ) limits found are 1.97 × 10<sup>-3</sup> μg/mL and 5.48 × 10<sup>-3</sup> μg/mL respectively. Recovery is achieved with 99.9% and 100.3% trueness, intra-day precision with a coefficient of variation of repeatability (CVr) of 0.99% and inter-day precision with a coefficient of variation of precision (CVR) of 1.7%. The method has been successfully applied in the analysis of 10 batches of nevirapine tablets and suspensions. 展开更多
关键词 Spectrofluorimetric Method Validation nevirapine Sodium Hypochlorite
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Evaluation of Nevirapine Release Kinetics from Polycaprolactone Hybrids
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作者 Mariana S. S. B. Monteiro Jackeline Lunz +1 位作者 Pedro J. Sebastião Maria Inês Bruno Tavares 《Materials Sciences and Applications》 2016年第11期680-701,共22页
The Nevirapine (NVP)/Polycaprolactone (PCL)/Nanoparticles hybrids systems have been developed as a potential platform for drug delivery, by solvent cast, as thin films. NVP, an antiretroviral drug, was included within... The Nevirapine (NVP)/Polycaprolactone (PCL)/Nanoparticles hybrids systems have been developed as a potential platform for drug delivery, by solvent cast, as thin films. NVP, an antiretroviral drug, was included within PCL matrix containing three types of nanoparticles: an organoclay layered silicate Viscogel S7&reg;(3% w/w), hydrophilic silica oxide particles Aerosil&reg;A20 (0.25% w/w) and titanium dioxide particles (0.25% w/w). These systems were characterized by X-ray diffraction (XRD), Fourier-transform infrared spectroscopy (FTIR), low-field nuclear magnetic resonance (NMR), ultraviolet-visible spectroscopy (UV), in-vitro dissolution testing and drug release mechanism kinetics. The PCL crystallization was affected by NVP incorporation, modifying its semi-crystalline structure to a less ordered structure. When nanoparticles and NVP were added, the T<sub>1</sub>H values increased, for PCL, PCL/S7, PCL/ SiO<sub>2</sub> and PCL/TiO<sub>2</sub> hybrids, suggesting that its addition produced a new material, with less molecular mobility, due to the new intermolecular interactions formation. It can consider a structure formation among the PCL chains, nanoparticles and NVP, with strong forces in the PCL/SiO<sub>2</sub>/NVP system. The amount of NVP included was around 1.5 ± 0.03 mg/cm<sup>2</sup>. In the in-vitro dissolution test, the PCL/SiO<sub>2</sub>/NVP system released the smallest amount of drug and this result could be attributed to the strong intermolecular interaction between the drug and the PCL/SiO<sub>2</sub> system. Higuchi’s model was the mathematical model chosen to treat the release data, since this model presented the highest coefficient correlation (r) value. The drug release probably occur by diffusion through the matrix pores, thus, these materials are suitable for sustained release of NVP. 展开更多
关键词 POLYCAPROLACTONE nevirapine HYBRIDS Modified Release
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Nevirapine可降低HIV的母婴传播
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作者 菲琳 《国外医学情报》 2001年第8期36-36,共1页
在南非德班市召开的第十三届国际AIDS大会为非洲国家预防HIV感染带来了极大的希望。许多国家的试验研究人员报道说,他们采用给母亲和新生儿投用Nevirapine这一简便而廉价的治疗方案获得了成功。南非产时Nevirapine试验(SAINT)结果证实Ne... 在南非德班市召开的第十三届国际AIDS大会为非洲国家预防HIV感染带来了极大的希望。许多国家的试验研究人员报道说,他们采用给母亲和新生儿投用Nevirapine这一简便而廉价的治疗方案获得了成功。南非产时Nevirapine试验(SAINT)结果证实Nevirapine在减少HIV母-婴传播方面是安全而有效的。 展开更多
关键词 艾滋病病毒 母婴传播 预防 nevirapine
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NVP、α-P蒸馏残渣综合利用——裂解工艺应用
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作者 杨国庆 马文锐 《化工设计通讯》 CAS 2023年第2期66-68,共3页
介绍了NVP、α-P蒸馏残渣来源以及成分分析,利用低温裂解工艺进行综合利用,裂解产物得到合理利用和处置,并分析了生产应用状况。结果表明,效果稳定、良好,既节约了资源,又保护了环境,消除了相关安全隐患。
关键词 nvp、α-P蒸馏残渣 裂解工艺 综合利用
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辐射接枝共聚物XG-g-NVP溶胀性能及其对苯酚吸附特性的研究 被引量:5
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作者 李咏富 哈益明 +2 位作者 陶乐仁 李彦杰 王锋 《核农学报》 CAS CSCD 北大核心 2011年第1期97-104,共8页
采用共辐射接枝法制备黄原胶-N-乙烯基吡咯烷酮接枝共聚物(XG-g-NVP),研究其溶胀性能及对苯酚的吸附性能。研究表明,XG-g-NVP在接枝率为623%时溶胀性能和吸附苯酚的能力最强,分别为62.1和0.76g/g。红外分析显示,XG-g-NVP与苯酚通过氢键... 采用共辐射接枝法制备黄原胶-N-乙烯基吡咯烷酮接枝共聚物(XG-g-NVP),研究其溶胀性能及对苯酚的吸附性能。研究表明,XG-g-NVP在接枝率为623%时溶胀性能和吸附苯酚的能力最强,分别为62.1和0.76g/g。红外分析显示,XG-g-NVP与苯酚通过氢键相结合。XG-g-NVP对苯酚吸附符合Freundlich等温吸附方程。298K下,XG-g-NVP吸附苯酚的自由能(ΔG)为-2.586kJ/mol,表明其对苯酚的吸附是物理吸附,可自发进行。因此,XG-g-NVP可作为苯酚废水处理的一种高效吸附剂。 展开更多
关键词 辐射接枝 黄原胶 N-乙烯基吡咯烷酮(nvp) 吸附苯酚
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P(AM-DAAM-NVP)三元共聚物的耐温抗盐性能研究 被引量:8
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作者 张玉平 叶彦春 +1 位作者 郭燕文 张军良 《精细化工》 EI CAS CSCD 北大核心 2006年第5期494-496,共3页
以丙烯酰胺(AM)、双丙酮丙烯酰胺(DAAM)、N-乙烯基-2-吡咯烷酮(NVP)为原料,采用水溶液聚合法合成了三元共聚物P(AM-DAAM-NVP),表征了其红外光谱特征;研究了它的热稳定性能和其溶液的特性黏数随温度的变化。结果表明,当m(AM)∶m(DAAM)∶m... 以丙烯酰胺(AM)、双丙酮丙烯酰胺(DAAM)、N-乙烯基-2-吡咯烷酮(NVP)为原料,采用水溶液聚合法合成了三元共聚物P(AM-DAAM-NVP),表征了其红外光谱特征;研究了它的热稳定性能和其溶液的特性黏数随温度的变化。结果表明,当m(AM)∶m(DAAM)∶m(NVP)=7.5∶2.0∶1.5,w(引发剂)=0.4%,聚合反应温度60℃时,得到的三元共聚物的半分解温度(T1/2)为390℃,比聚丙烯酰胺提高了14.3%;它在350℃时的失重速率(K350)为1.0%/m in,较聚丙烯酰胺的K350(1.43%/m in)下降了30.1%,耐热抗盐性能优于聚丙烯酰胺(PAM);该三元共聚物黏度保留值(B.R)均大于0.75,最大可达0.97,远大于相同条件下的聚丙烯酰胺黏度保留值(最大为0.55)。 展开更多
关键词 P(AM—DAAM—nvp)三元共聚物 耐热抗盐性 特性黏数 聚丙烯酰胺
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