Cefuroxime Axetil (CA) a widely used cephalosporin antibiotic displays low aqueous solubility and high membrane penetrability. This results in its solubility driven variable and/or low oral bioavailability and therape...Cefuroxime Axetil (CA) a widely used cephalosporin antibiotic displays low aqueous solubility and high membrane penetrability. This results in its solubility driven variable and/or low oral bioavailability and therapeutic efficacy as a major drawback. Thus, most of the goal of our study was to increase the solubility as well as dissolution rate of CA using the simple and cost-effective solid dispersion (SD) method. At first, the SD formulations of CA were prepared at various weight ratios of Carplex-67 and PEG-4000 by solvent evaporation technique. These new formulations were then subjected to an in-vitro drug release performance study and tested for physicochemical characterization to distinguish the thermal behavior, crystallinity, interactions phenomena, and surface morphology. Among the formulated Cefuroxime Axetil Solid Dispersion (CSD), CSD-8 which contained CA, Carplex-67, and PEG-4000 at the weight ratio 1:3:2, respectively showed the most significant (p in-vitro dissolution in water, Gastric Simulated Fluid (GSF), and Intestinal Simulated Fluid (ISF). This study also showed a significant (p < 0.001) increase in drug release compared to the marketed product. Therefore, it is supposed to be a promising alternative to conventional antimicrobial therapy.展开更多
Mesoporous Ce0.5Zr0.5O2 mixed oxide with high specific surface area was synthesized under basic condition in the presence of non-ionic surfactant PEG-4000. The effect of synthesis conditions, such as synthesis tempera...Mesoporous Ce0.5Zr0.5O2 mixed oxide with high specific surface area was synthesized under basic condition in the presence of non-ionic surfactant PEG-4000. The effect of synthesis conditions, such as synthesis temperature and the molar ratio of PEG-4000/（[ Ce] ＋ [ Zr] ）, on specific surface area were investigated. The products were characterized by transmission electron microscopy, powder X-ray diffraction, and nitrogen adsorption-desorption measurements, respectively. The results showed that synthesis temperature and the molar ratio of PEG-4000/（[ Ce] ＋ [ Zr] ） had great influence on specific surface area. Under the optimum synthesis conditions, the prepared Ce0.5Zr0.5O2 mixed oxide presented cubic fluorite-type structure and possessed high surface area of 148.6 m2·g^-1 with wormlike pores.展开更多
Fenofibrate (FF) is an anti-hyperlipidaemic drug belonging to BCS class-II (low solubility, high permeability). Its bioavailability is limited by the dissolution rate. This study was aimed to enhance the rate of disso...Fenofibrate (FF) is an anti-hyperlipidaemic drug belonging to BCS class-II (low solubility, high permeability). Its bioavailability is limited by the dissolution rate. This study was aimed to enhance the rate of dissolution of poorly water soluble drug, FF. Initially, solid dispersions of fenofibrate (SDFs) were formulated with Carplex-80 or PEG-4000 or in combination at various weight ratios and were subjected to dissolution study. On the basis of drug release at various time intervals, the formulation producing maximum drug concentration was evaluated physicochemically using differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), Fourier-transform infrared spectroscopy (FTIR), and scanning electron microscopy (SEM). It was observed that the peak drug concentration was obtained at 120 min of dissolution by formulation SDF-7, which contains a mixture of Carplex-80 and PEG-4000 at weight ratio 1:5:6 of FF:PEG-4000:Carplex-80, respectively. Thus, the extent of drug release by SDF-7 was maximized by 2.5-fold than that of pure FF. Physicochemical characterization revealed the reason for this increased drug release as a conversion of crystalline FF to amorphous form and ensured the chemical compatibility among FF and carriers. The results specified the significant improvement of FF release using solid dispersion technique.展开更多
目的评价聚乙二醇（PEG）4000治疗〈8岁儿童便秘的安全性和有效性。方法计算机检索PubMed、EMBASE、Cochrane图书馆、中国知网和维普数据库,检索起止时间为1981年1月1日至2016年4月1日,获得PEG4000治疗〈8岁儿童便秘的RCT文献,评估纳入...目的评价聚乙二醇（PEG）4000治疗〈8岁儿童便秘的安全性和有效性。方法计算机检索PubMed、EMBASE、Cochrane图书馆、中国知网和维普数据库,检索起止时间为1981年1月1日至2016年4月1日,获得PEG4000治疗〈8岁儿童便秘的RCT文献,评估纳入文献的偏倚风险。评估PEG4000治疗期间的安全性和疗效指标。采用Rev Man 5.0软件行Meta分析。结果 4篇RCT文献进入系统评价,共纳入344例〈8岁便秘患儿,观察时间为2-12周,PEG4000与乳果糖、氧化镁和PEG-电解质对照的文献分别为2、1和1篇。4篇文献均描述了随机序列的产生、分配隐藏和受试者的脱落或失访,3篇文献采用双盲法。因对照组和结局指标不同行描述性分析,14篇文献PEG4000治疗期间均未观察到严重不良事件,1篇文献显示PEG4000组治疗12周至少1项血生化指标异常的比例与治疗前基线数据差异无统计学意义（35/39 vs 31/39）,1篇文献显示腹泻发生率低于氧化镁对照组（2/46 vs 12/43）,1篇文献显示恶心发生率低于PEG-电解质对照组（1/49 vs 9/42）。21篇文献显示用药后4周每天大便次数PEG4000组与乳果糖对照组差值为0.36次（95%CI：0.16-0.56次）,1篇文献显示用药后12周每周大便次数PEG4000组和乳果糖对照组相近（8.5 vs 11.5次）。治疗4周后好转率率PEG4000组优于氧化镁对照组（42/46 vs 28/43,P=0.003）;治疗4周后每周大便次数PEG4000组优于PEG-电解质对照组,（9.2±3.2）vs（7.8±2.4）次,P=0.025。结论现有临床证据表明,PEG4000治疗〈8岁儿童便秘的安全性和疗效较好。展开更多
文摘Cefuroxime Axetil (CA) a widely used cephalosporin antibiotic displays low aqueous solubility and high membrane penetrability. This results in its solubility driven variable and/or low oral bioavailability and therapeutic efficacy as a major drawback. Thus, most of the goal of our study was to increase the solubility as well as dissolution rate of CA using the simple and cost-effective solid dispersion (SD) method. At first, the SD formulations of CA were prepared at various weight ratios of Carplex-67 and PEG-4000 by solvent evaporation technique. These new formulations were then subjected to an in-vitro drug release performance study and tested for physicochemical characterization to distinguish the thermal behavior, crystallinity, interactions phenomena, and surface morphology. Among the formulated Cefuroxime Axetil Solid Dispersion (CSD), CSD-8 which contained CA, Carplex-67, and PEG-4000 at the weight ratio 1:3:2, respectively showed the most significant (p in-vitro dissolution in water, Gastric Simulated Fluid (GSF), and Intestinal Simulated Fluid (ISF). This study also showed a significant (p < 0.001) increase in drug release compared to the marketed product. Therefore, it is supposed to be a promising alternative to conventional antimicrobial therapy.
基金Project Supported by Open Fund of Key Laboratory of Catalysis Materials and Science of Hubei Province (CHCL0501)
文摘Mesoporous Ce0.5Zr0.5O2 mixed oxide with high specific surface area was synthesized under basic condition in the presence of non-ionic surfactant PEG-4000. The effect of synthesis conditions, such as synthesis temperature and the molar ratio of PEG-4000/（[ Ce] ＋ [ Zr] ）, on specific surface area were investigated. The products were characterized by transmission electron microscopy, powder X-ray diffraction, and nitrogen adsorption-desorption measurements, respectively. The results showed that synthesis temperature and the molar ratio of PEG-4000/（[ Ce] ＋ [ Zr] ） had great influence on specific surface area. Under the optimum synthesis conditions, the prepared Ce0.5Zr0.5O2 mixed oxide presented cubic fluorite-type structure and possessed high surface area of 148.6 m2·g^-1 with wormlike pores.
文摘Fenofibrate (FF) is an anti-hyperlipidaemic drug belonging to BCS class-II (low solubility, high permeability). Its bioavailability is limited by the dissolution rate. This study was aimed to enhance the rate of dissolution of poorly water soluble drug, FF. Initially, solid dispersions of fenofibrate (SDFs) were formulated with Carplex-80 or PEG-4000 or in combination at various weight ratios and were subjected to dissolution study. On the basis of drug release at various time intervals, the formulation producing maximum drug concentration was evaluated physicochemically using differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), Fourier-transform infrared spectroscopy (FTIR), and scanning electron microscopy (SEM). It was observed that the peak drug concentration was obtained at 120 min of dissolution by formulation SDF-7, which contains a mixture of Carplex-80 and PEG-4000 at weight ratio 1:5:6 of FF:PEG-4000:Carplex-80, respectively. Thus, the extent of drug release by SDF-7 was maximized by 2.5-fold than that of pure FF. Physicochemical characterization revealed the reason for this increased drug release as a conversion of crystalline FF to amorphous form and ensured the chemical compatibility among FF and carriers. The results specified the significant improvement of FF release using solid dispersion technique.
文摘目的评价聚乙二醇（PEG）4000治疗〈8岁儿童便秘的安全性和有效性。方法计算机检索PubMed、EMBASE、Cochrane图书馆、中国知网和维普数据库,检索起止时间为1981年1月1日至2016年4月1日,获得PEG4000治疗〈8岁儿童便秘的RCT文献,评估纳入文献的偏倚风险。评估PEG4000治疗期间的安全性和疗效指标。采用Rev Man 5.0软件行Meta分析。结果 4篇RCT文献进入系统评价,共纳入344例〈8岁便秘患儿,观察时间为2-12周,PEG4000与乳果糖、氧化镁和PEG-电解质对照的文献分别为2、1和1篇。4篇文献均描述了随机序列的产生、分配隐藏和受试者的脱落或失访,3篇文献采用双盲法。因对照组和结局指标不同行描述性分析,14篇文献PEG4000治疗期间均未观察到严重不良事件,1篇文献显示PEG4000组治疗12周至少1项血生化指标异常的比例与治疗前基线数据差异无统计学意义（35/39 vs 31/39）,1篇文献显示腹泻发生率低于氧化镁对照组（2/46 vs 12/43）,1篇文献显示恶心发生率低于PEG-电解质对照组（1/49 vs 9/42）。21篇文献显示用药后4周每天大便次数PEG4000组与乳果糖对照组差值为0.36次（95%CI：0.16-0.56次）,1篇文献显示用药后12周每周大便次数PEG4000组和乳果糖对照组相近（8.5 vs 11.5次）。治疗4周后好转率率PEG4000组优于氧化镁对照组（42/46 vs 28/43,P=0.003）;治疗4周后每周大便次数PEG4000组优于PEG-电解质对照组,（9.2±3.2）vs（7.8±2.4）次,P=0.025。结论现有临床证据表明,PEG4000治疗〈8岁儿童便秘的安全性和疗效较好。
