Aim To prepare a self-emulsifying microemulsion of 9-nitrocamptothecin （9-NC ME） for intravenous injection and investi- gation of its pharmacokinetic profiles in normal SD rats. Methods 9-NC ME was optimized in term...Aim To prepare a self-emulsifying microemulsion of 9-nitrocamptothecin （9-NC ME） for intravenous injection and investi- gation of its pharmacokinetic profiles in normal SD rats. Methods 9-NC ME was optimized in terms of droplet size and lack of drug precipitation following aqueous dilution using a pseudo-ternary phase diagram. Physicochemical properties of 9-NC ME were evaluated. 9-NC ME was intravenously administered via tail vein in healthy rats. Results A stable microemulsion was formulated consisted of soybean oil as oil phase, EPC/Tween-80 as emulsifier, and anhydrous ethanol as co-emulsifier. The droplets of the microemulsion were spherical shape with mean diameter of 38.3 ± 4.0 nm after 1：20 dilution with 5% glucose injection. The pharmacokinetic parameters of 9-NC ME after intravenous administration in rats were t1/2 of 0.97 ± 0.14 h, A UC0-8 of 372.77 ±49.62 ng·h·mL^-1 and MRT of 1.40 ± 0.21 h which were 1.4-fold, 1.65-fold, and 1.4-fold more than those of 9-NC solution （P〈0.01）. Conclusion The results suggested that 9-NC ME was a promising drug delivery system and it was expected to provide a novel 9-NC injection for cancer patients.展开更多
目的通过研究缺氧缺血性脑病(HIE)新生儿血清神经纤维轻链(NF-L)、水通道蛋白9(AQP9)、纤维蛋白原样蛋白2(FGL2)水平的变化,分析三者与新生儿行为神经评估(NABA)评分的相关性。方法选取2022年1月~2024年7月山西省儿童医院收治的203例HI...目的通过研究缺氧缺血性脑病(HIE)新生儿血清神经纤维轻链(NF-L)、水通道蛋白9(AQP9)、纤维蛋白原样蛋白2(FGL2)水平的变化,分析三者与新生儿行为神经评估(NABA)评分的相关性。方法选取2022年1月~2024年7月山西省儿童医院收治的203例HIE患儿为研究组,根据病情程度分为轻度组(n=63)、中度组(n=81)和重度组(n=59),另选同期的健康新生儿203例为对照组,酶联免疫吸附试验(ELISA)检测血清NF-L、AQP9、FGL2水平,收集分析一般临床资料。受试者操作特征(ROC)曲线分析NF-L、AQP9、FGL2及NABA评分对新生儿重度HIE的诊断价值;Pearson法分析血清NF-L、AQP9、FGL2与NABA评分的相关性。结果与对照组相比,研究组血清NF-L(14.78±1.67ng/ml vs 10.65±1.21ng/ml)、AQP9(61.82±6.29pg/ml vs 42.62±4.31pg/ml)、FGL2(189.69±20.26ng/ml vs 132.51±14.84ng/ml)水平显著升高,差异具有统计学意义(t=28.533、35.877、32.440,均P<0.05);中度组、重度组血清NF-L(14.68±1.67ng/ml、18.62±2.03ng/ml),AQP9(63.51±6.44pg/ml、69.63±7.03pg/ml),FGL2(195.68±20.84ng/ml、210.65±22.36ng/ml)水平显著高于轻度组(11.32±1.33ng/ml、52.32±5.41pg/ml、162.35±17.55ng/ml),NABA(34.89±3.51分、29.88±3.43分)评分显著低于轻度组(36.54±1.52分),差异具有统计学意义(t_(中度组)=4.616~16.729,t_(重度组)=17.276~33.701,均P<0.05);NF-L、AQP9、FGL2与NABA评分均呈负相关(r=-0.432、-0.421、-0.402,均P<0.05);NF-L、AQP9、FGL2、NABA联合诊断患儿重度病情的曲线下面积(AUC)显著高于各项单独诊断,差异具有统计学意义(Z=2.066~3.307,均P<0.05)。结论HIE患儿血清NF-L、AQP9、FGL2水平显著升高,与NABA评分相关,可能成为评估HIE患儿病情的标志物。展开更多
目的探究血清网膜素-1(Omentin-1)、补体/C1q肿瘤坏死因子相关蛋白9(CTRP-9)水平与急性脑梗死(ACI)神经功能康复的相关性。方法选取2022年11月至2024年2月于该院治疗的ACI患者106例作为研究组,其中包括ACI神经功能康复良好患者62例(良好...目的探究血清网膜素-1(Omentin-1)、补体/C1q肿瘤坏死因子相关蛋白9(CTRP-9)水平与急性脑梗死(ACI)神经功能康复的相关性。方法选取2022年11月至2024年2月于该院治疗的ACI患者106例作为研究组,其中包括ACI神经功能康复良好患者62例(良好组)和康复不良患者44例(不良组)。采用酶联免疫吸附试验检测所有研究对象的血清Omentin-1、CTRP-9水平;采用Spearman相关性分析血清Omentin-1、CTRP-9水平与ACI患者入院时的美国国立卫生研究院卒中量表(NIHSS)评分及脑梗死体积的相关性;采用多因素Logistic回归分析ACI患者神经功能康复不良的影响因素;采用受试者工作特征(ROC)曲线分析血清Omentin-1、CTRP-9水平对ACI患者神经功能康复不良的诊断价值。结果良好组血清Omentin-1、CTRP-9水平明显高于不良组(P<0.05),入院时NIHSS评分、脑梗死面积和发病90 d时改良Rankin量表(mRS)评分明显低于不良组(P<0.05);Spearman相关性分析显示,血清Omentin-1、CTRP-9水平与90 d mRS评分呈负相关(r=-0.648,-0.573,均P<0.001);多因素Logistic回归分析结果显示,90 d mRS评分是ACI患者神经功能康复不良的危险因素(P<0.05),血清Omentin-1、CTRP-9水平是ACI患者神经功能康复不良的保护因素(P<0.05);ROC曲线分析结果显示,血清Omentin-1、CTRP-9水平诊断ACI患者神经功能康复不良的曲线下面积(AUC)为0.843、0.828,二者联合诊断的AUC为0.937,明显大于二者单独诊断(Z_(二者联合-Omentin-1)=2.321,P=0.020;Z_(二者联合-CTRP-9)=2.532,P=0.011)。结论ACI神经功能康复不良患者血清Omentin-1、CTRP-9水平明显降低,且Omentin-1、CTRP-9水平与90 d mRS评分呈负相关,与神经功能康复情况密切相关。展开更多
基金National Natural Science Foundation of China (GrantNo.30430760)the 985 projects (Phase II) of the State Key Labo-ratory of Natural and Biomimetic Drugs (Peking University, China).
文摘Aim To prepare a self-emulsifying microemulsion of 9-nitrocamptothecin （9-NC ME） for intravenous injection and investi- gation of its pharmacokinetic profiles in normal SD rats. Methods 9-NC ME was optimized in terms of droplet size and lack of drug precipitation following aqueous dilution using a pseudo-ternary phase diagram. Physicochemical properties of 9-NC ME were evaluated. 9-NC ME was intravenously administered via tail vein in healthy rats. Results A stable microemulsion was formulated consisted of soybean oil as oil phase, EPC/Tween-80 as emulsifier, and anhydrous ethanol as co-emulsifier. The droplets of the microemulsion were spherical shape with mean diameter of 38.3 ± 4.0 nm after 1：20 dilution with 5% glucose injection. The pharmacokinetic parameters of 9-NC ME after intravenous administration in rats were t1/2 of 0.97 ± 0.14 h, A UC0-8 of 372.77 ±49.62 ng·h·mL^-1 and MRT of 1.40 ± 0.21 h which were 1.4-fold, 1.65-fold, and 1.4-fold more than those of 9-NC solution （P〈0.01）. Conclusion The results suggested that 9-NC ME was a promising drug delivery system and it was expected to provide a novel 9-NC injection for cancer patients.
文摘目的通过研究缺氧缺血性脑病(HIE)新生儿血清神经纤维轻链(NF-L)、水通道蛋白9(AQP9)、纤维蛋白原样蛋白2(FGL2)水平的变化,分析三者与新生儿行为神经评估(NABA)评分的相关性。方法选取2022年1月~2024年7月山西省儿童医院收治的203例HIE患儿为研究组,根据病情程度分为轻度组(n=63)、中度组(n=81)和重度组(n=59),另选同期的健康新生儿203例为对照组,酶联免疫吸附试验(ELISA)检测血清NF-L、AQP9、FGL2水平,收集分析一般临床资料。受试者操作特征(ROC)曲线分析NF-L、AQP9、FGL2及NABA评分对新生儿重度HIE的诊断价值;Pearson法分析血清NF-L、AQP9、FGL2与NABA评分的相关性。结果与对照组相比,研究组血清NF-L(14.78±1.67ng/ml vs 10.65±1.21ng/ml)、AQP9(61.82±6.29pg/ml vs 42.62±4.31pg/ml)、FGL2(189.69±20.26ng/ml vs 132.51±14.84ng/ml)水平显著升高,差异具有统计学意义(t=28.533、35.877、32.440,均P<0.05);中度组、重度组血清NF-L(14.68±1.67ng/ml、18.62±2.03ng/ml),AQP9(63.51±6.44pg/ml、69.63±7.03pg/ml),FGL2(195.68±20.84ng/ml、210.65±22.36ng/ml)水平显著高于轻度组(11.32±1.33ng/ml、52.32±5.41pg/ml、162.35±17.55ng/ml),NABA(34.89±3.51分、29.88±3.43分)评分显著低于轻度组(36.54±1.52分),差异具有统计学意义(t_(中度组)=4.616~16.729,t_(重度组)=17.276~33.701,均P<0.05);NF-L、AQP9、FGL2与NABA评分均呈负相关(r=-0.432、-0.421、-0.402,均P<0.05);NF-L、AQP9、FGL2、NABA联合诊断患儿重度病情的曲线下面积(AUC)显著高于各项单独诊断,差异具有统计学意义(Z=2.066~3.307,均P<0.05)。结论HIE患儿血清NF-L、AQP9、FGL2水平显著升高,与NABA评分相关,可能成为评估HIE患儿病情的标志物。
文摘目的探究血清网膜素-1(Omentin-1)、补体/C1q肿瘤坏死因子相关蛋白9(CTRP-9)水平与急性脑梗死(ACI)神经功能康复的相关性。方法选取2022年11月至2024年2月于该院治疗的ACI患者106例作为研究组,其中包括ACI神经功能康复良好患者62例(良好组)和康复不良患者44例(不良组)。采用酶联免疫吸附试验检测所有研究对象的血清Omentin-1、CTRP-9水平;采用Spearman相关性分析血清Omentin-1、CTRP-9水平与ACI患者入院时的美国国立卫生研究院卒中量表(NIHSS)评分及脑梗死体积的相关性;采用多因素Logistic回归分析ACI患者神经功能康复不良的影响因素;采用受试者工作特征(ROC)曲线分析血清Omentin-1、CTRP-9水平对ACI患者神经功能康复不良的诊断价值。结果良好组血清Omentin-1、CTRP-9水平明显高于不良组(P<0.05),入院时NIHSS评分、脑梗死面积和发病90 d时改良Rankin量表(mRS)评分明显低于不良组(P<0.05);Spearman相关性分析显示,血清Omentin-1、CTRP-9水平与90 d mRS评分呈负相关(r=-0.648,-0.573,均P<0.001);多因素Logistic回归分析结果显示,90 d mRS评分是ACI患者神经功能康复不良的危险因素(P<0.05),血清Omentin-1、CTRP-9水平是ACI患者神经功能康复不良的保护因素(P<0.05);ROC曲线分析结果显示,血清Omentin-1、CTRP-9水平诊断ACI患者神经功能康复不良的曲线下面积(AUC)为0.843、0.828,二者联合诊断的AUC为0.937,明显大于二者单独诊断(Z_(二者联合-Omentin-1)=2.321,P=0.020;Z_(二者联合-CTRP-9)=2.532,P=0.011)。结论ACI神经功能康复不良患者血清Omentin-1、CTRP-9水平明显降低,且Omentin-1、CTRP-9水平与90 d mRS评分呈负相关,与神经功能康复情况密切相关。
