The aim of present study was to measure and correlate the solubility of poorly water-soluble flavonoid diosmin in water, ethanol, isopropyl alcohol(IPA), polyethylene glycol-400(PEG-400) and β-cyclodextrin(β-CD) aqu...The aim of present study was to measure and correlate the solubility of poorly water-soluble flavonoid diosmin in water, ethanol, isopropyl alcohol(IPA), polyethylene glycol-400(PEG-400) and β-cyclodextrin(β-CD) aqueous solution(0.02 mol·L-1). The solubility of diosmin was measured using the shake flask method from(298.15 to333.15) K at atmospheric pressure. The experimental solubilities of diosmin were regressed by the modified Apelblat model with a relative deviation in the range of 0.048% to 5.940%. The correlation coefficients were observed in the range of 0.9957 to 0.9995. The solubility of diosmin was found to be increased with temperature in all sample matrices investigated. The mole fraction solubility of diosmin was found to be higher in β-CD aqueous solution and PEG-400 as compared to water, ethanol and IPA. Based on solubility data of present study, diosmin was considered as practically insoluble in water, insoluble in ethanol & IPA and soluble in PEG-400 and β-CD aqueous solution.展开更多
OBJECTIVE:The present study was undertaken to evaluate the effect of diosmin in diabetic neuropathy in type 2 diabetic rats.METHODS:Type 2 diabetes was induced in male Sprague-Dawley rats by single intraperitoneal inj...OBJECTIVE:The present study was undertaken to evaluate the effect of diosmin in diabetic neuropathy in type 2 diabetic rats.METHODS:Type 2 diabetes was induced in male Sprague-Dawley rats by single intraperitoneal injection of streptozotocin(35 mg/kg) and high-fat diet.Four weeks after the confirmation of diabetes,diabetic rats were treated with diosmin(50 and 100 mg/kg,p.o.) for next 4 weeks.Rats were evaluated for biochemical,behavioral and oxidative stress parameters.Eddy's hot plate and tail immersion test were performed on 6th,7th,8th,9th and 10th weeks of experiment to assess thermal hyperalgesia and cold allodynia respectively.Further,the walking function test was performed for assessing the motor responses at the end of the treatment schedule.RESULTS:Rats were fed with high-fat diet throughout the experiment schedule and administration of low-dose streptozotocin induced significant elevation in blood glucose level and insulin resistance which was confirmed by oral glucose tolerance test.Treatment with diosmin at doses of 50 and 100 mg/kg significantly restored the reduced body weight,elevated blood sugar and lipid profiles.Further the dose-dependent improvement was observed in thermal hyperalgesia,cold allodynia and walking function in diabetic rats treated with diosmin.Elevated levels of malondialdehyde,and nitric oxide and decreased glutathione levels and superoxide dismutase activity in diabetic rats were restored significantly after the 4 weeks of diosmin treatment.CONCLUSION:Diosmin has shown beneficial effect in preventing the progression of early diabetic neuropathy in rats.展开更多
目的:系统评价地奥司明治疗腰椎间盘突出症(LDH)的有效性。方法:计算机检索中国知网(CNKI)、万方数据库(Wangfang)、维普中文科技期刊数据库(VIP)、中国生物医学文献数据库(SinoMed)、Cochrane library、PubMed、Embase、Web of scienc...目的:系统评价地奥司明治疗腰椎间盘突出症(LDH)的有效性。方法:计算机检索中国知网(CNKI)、万方数据库(Wangfang)、维普中文科技期刊数据库(VIP)、中国生物医学文献数据库(SinoMed)、Cochrane library、PubMed、Embase、Web of science数据库,检索时间均从建库至2022年6月。收集地奥司明(试验组)对比甘露醇+地塞米松(对照组)治疗LDH的随机对照试验(RCT)。根据纳入与排除标准,由2位研究人员采用计算机独立进行文献筛选、数据提取和质量评价。采用RevMan 5.4软件进行Meta分析,采用Stata15软件进行敏感性分析。结果:共纳入5项RCT,共计878例患者,其中试验组479例,对照组399例。Meta分析结果显示,试验组视觉模拟量表(VAS)评分低于对照组[MD=-0.43,95%CI(-0.74,-0.12),P=0.006],而在治疗初期(3天),两组比较无统计学差异[MD=-0.12,95%CI(-1.32,1.07),P=0.84];试验组日本骨科协会(JOA)评分高于对照组[MD=3.10,95%CI(1.88,4.33),P<0.000 01];在治疗总有效率方面,两组比较无统计学差异[RR=1.01,95%CI(0.96,1.06),P=0.76]。敏感性分析结果显示,上述结果基本稳定。结论:现有临床证据表明,与甘露醇+地塞米松相比,地奥司明治疗LDH的疗效较好,可降低LDH患者VAS评分和改善腰椎功能,且治疗总有效率相当。展开更多
目的:建立测定人血浆中地奥司明苷元浓度的液相色谱-串连质谱检测法,并研究地奥司明片在健康人体内的药物动力学特征。方法:用LC/MS/MS法测定,色谱柱为CAPCELL PAK UG120柱,流动相为乙腈-0.1%甲酸溶液(80:20,v/v),流速0.6 ml·min^(...目的:建立测定人血浆中地奥司明苷元浓度的液相色谱-串连质谱检测法,并研究地奥司明片在健康人体内的药物动力学特征。方法:用LC/MS/MS法测定,色谱柱为CAPCELL PAK UG120柱,流动相为乙腈-0.1%甲酸溶液(80:20,v/v),流速0.6 ml·min^(-1),柱温为24℃,对12名健康志愿者口服地奥司明片后不同时间点的血药浓度进行测定,并用统计矩法计算药动学参数。结果:地奥司明片中地奥司明苷元在健康受试者体内的主要药动学参数t_(max)为(12.1±0.9)h,C_(max)为(8.88±2.69)ng·ml^(-1),t_(1/2)为(11.9±2.5)h,AUC_(0-48h)为(183±55)ng·h·ml^(-1),AUC_(0-∞)为(200±61)ng·h·ml^(-1)。结论:本方法具有良好的准确性、精密度和较高的灵敏度、简便快速,能满足地奥司明的血药浓度测定和药动学研究。展开更多
基金supported by the Deanship of Scientific Research, Salman Bin Abdulaziz University, Al-Kharj, Saudi Arabia (47H/1433)
文摘The aim of present study was to measure and correlate the solubility of poorly water-soluble flavonoid diosmin in water, ethanol, isopropyl alcohol(IPA), polyethylene glycol-400(PEG-400) and β-cyclodextrin(β-CD) aqueous solution(0.02 mol·L-1). The solubility of diosmin was measured using the shake flask method from(298.15 to333.15) K at atmospheric pressure. The experimental solubilities of diosmin were regressed by the modified Apelblat model with a relative deviation in the range of 0.048% to 5.940%. The correlation coefficients were observed in the range of 0.9957 to 0.9995. The solubility of diosmin was found to be increased with temperature in all sample matrices investigated. The mole fraction solubility of diosmin was found to be higher in β-CD aqueous solution and PEG-400 as compared to water, ethanol and IPA. Based on solubility data of present study, diosmin was considered as practically insoluble in water, insoluble in ethanol & IPA and soluble in PEG-400 and β-CD aqueous solution.
文摘OBJECTIVE:The present study was undertaken to evaluate the effect of diosmin in diabetic neuropathy in type 2 diabetic rats.METHODS:Type 2 diabetes was induced in male Sprague-Dawley rats by single intraperitoneal injection of streptozotocin(35 mg/kg) and high-fat diet.Four weeks after the confirmation of diabetes,diabetic rats were treated with diosmin(50 and 100 mg/kg,p.o.) for next 4 weeks.Rats were evaluated for biochemical,behavioral and oxidative stress parameters.Eddy's hot plate and tail immersion test were performed on 6th,7th,8th,9th and 10th weeks of experiment to assess thermal hyperalgesia and cold allodynia respectively.Further,the walking function test was performed for assessing the motor responses at the end of the treatment schedule.RESULTS:Rats were fed with high-fat diet throughout the experiment schedule and administration of low-dose streptozotocin induced significant elevation in blood glucose level and insulin resistance which was confirmed by oral glucose tolerance test.Treatment with diosmin at doses of 50 and 100 mg/kg significantly restored the reduced body weight,elevated blood sugar and lipid profiles.Further the dose-dependent improvement was observed in thermal hyperalgesia,cold allodynia and walking function in diabetic rats treated with diosmin.Elevated levels of malondialdehyde,and nitric oxide and decreased glutathione levels and superoxide dismutase activity in diabetic rats were restored significantly after the 4 weeks of diosmin treatment.CONCLUSION:Diosmin has shown beneficial effect in preventing the progression of early diabetic neuropathy in rats.
文摘目的:建立测定人血浆中地奥司明苷元浓度的液相色谱-串连质谱检测法,并研究地奥司明片在健康人体内的药物动力学特征。方法:用LC/MS/MS法测定,色谱柱为CAPCELL PAK UG120柱,流动相为乙腈-0.1%甲酸溶液(80:20,v/v),流速0.6 ml·min^(-1),柱温为24℃,对12名健康志愿者口服地奥司明片后不同时间点的血药浓度进行测定,并用统计矩法计算药动学参数。结果:地奥司明片中地奥司明苷元在健康受试者体内的主要药动学参数t_(max)为(12.1±0.9)h,C_(max)为(8.88±2.69)ng·ml^(-1),t_(1/2)为(11.9±2.5)h,AUC_(0-48h)为(183±55)ng·h·ml^(-1),AUC_(0-∞)为(200±61)ng·h·ml^(-1)。结论:本方法具有良好的准确性、精密度和较高的灵敏度、简便快速,能满足地奥司明的血药浓度测定和药动学研究。
