The inclusion complexes of poorly water-soluble cephalosporin, cefuroxime axetil(CFA), were prepared with β-cyclodextrin(βCD) with or without addition of L-arginine(ARG) to improve its physicochemical properties. We...The inclusion complexes of poorly water-soluble cephalosporin, cefuroxime axetil(CFA), were prepared with β-cyclodextrin(βCD) with or without addition of L-arginine(ARG) to improve its physicochemical properties. We also investigated the effect of ARG on complexation efficiency(CE) of βCD towards CFA in an aqueous medium through phase solubility behaviour according to Higuchi and Connors. Although phase solubility studies showed AL(linear) type of solubility curve in presence and absence of ARG, the CE and association constant(Ks) of βCD towards CFA were significantly promoted in presence of ARG,justifying its use as a ternary component. The solid systems of CFA with βCD were obtained by spray drying technique with or without incorporation of ARG and characterized by differential scanning calorimetry(DSC), X-ray powder diffractometry(XRPD), scanning electron microscopy(SEM), and saturation solubility and dissolution studies. The molecular modeling studies provided a better insight into geometry and inclusion mode of CFA inside βCD cavity. The solubility and dissolution rate of CFA were significantly improved upon complexation with βCD as compared to CFA alone. However, ternary system incorporated with ARG performed better than binary system in physicochemical evaluation. In conclusion, ARG could be exploited as a ternary component to improve the physicochemical properties of CFA via βCD complexation.展开更多
Objective To investigate the effects of low dosage of β-elemene on the radiosensitivity of rabbit VX2 renal transplant carcinoma model. Methods We took the rabbit VX2 renal transplant carcinoma as the model. Experime...Objective To investigate the effects of low dosage of β-elemene on the radiosensitivity of rabbit VX2 renal transplant carcinoma model. Methods We took the rabbit VX2 renal transplant carcinoma as the model. Experimental rabbits were divided into three groups: the control group, the radiation group, and the radiation +β-elemene (radiosensitivity) group. The change of tumor was observed by Spiral CT and B ultrasound to compare its regrowth period. The tumor was measured by light microscopy and electron microscopy. Results The tumor in radiosensitivity group was restrained obviously and the sensitization enhancement ratio (SER) of β-elemene was 1.89. Different apoptosis was observed under transmission electron microscopy. Conclusion Low dosage β-elemene can enhance the radiosensitivity of rabbit VX2 renal transplant carcinoma model and induce the apoptosis of tumor cells, but the mechanism needs further study. It promotes apoptosis in mechanisms in vitro.展开更多
Ursolic acid(UA) and oleanolic acid(OA) are insoluble drugs. The objective of this study was to encapsulate them into β-cyclodextrin(β-CD) and compare the solubility and intermolecular force of β-CD with the two is...Ursolic acid(UA) and oleanolic acid(OA) are insoluble drugs. The objective of this study was to encapsulate them into β-cyclodextrin(β-CD) and compare the solubility and intermolecular force of β-CD with the two isomeric triterpenic acids. The host-guest interaction was explored in liquid and solid state by ultraviolet-visible absorption,1H NMR, phase solubility analysis, and differential scanning calorimetry, X-ray powder diffractometry, and molecular modeling studies. Both experimental and theoretical studies revealed that β-CD formed 1: 1 water soluble inclusion complexes and the complexation process was naturally favorable. In addition, the overall results suggested that ring E with a carboxyl group of the drug was encapsulated into the hydrophobic CD nanocavity. Therefore, a clear different inclusion behavior was observed, and UA exhibited better affinity to β-CD compared with OA in various media due to little steric interference, which was beneficial to form stable inclusion complex with β-CD and increase its water solubility effectively.展开更多
为提高近红外光谱法测定初烤烟叶中β-胡萝卜素和叶黄素含量的准确性和稳定性,采用随机蛙跳(Random Frog,RF)筛选特征波长建立上述指标的偏最小二乘(Partial Least Squares,PLS)近红外模型,结合模型内部交互验证结果确定最优建模波长数...为提高近红外光谱法测定初烤烟叶中β-胡萝卜素和叶黄素含量的准确性和稳定性,采用随机蛙跳(Random Frog,RF)筛选特征波长建立上述指标的偏最小二乘(Partial Least Squares,PLS)近红外模型,结合模型内部交互验证结果确定最优建模波长数和主成分数,并对最优模型的准确性和稳定性进行内外部评价。结果表明:相较于全波长(1298个波长)建模,利用RF筛选出的181个和216个特征波长建模,模型的决定系数(R2)由0.7718和0.8677分别提高至0.9511和0.9587,校正均方根误差(RMSEC)由3.362μg/g和4.930μg/g分别降低至1.556μg/g和2.756μg/g,交互验证均方根误差(RMSECV)由3.304μg/g和4.836μg/g分别降低至1.529μg/g和2.703μg/g;模型外部预测集(样品数=50)的预测平均相对误差分别由11.80%和9.62%降低至5.48%和5.49%。采用RF筛选特征波长能有效提升初烤烟叶β-胡萝卜素和叶黄素含量近红外模型的准确性和稳定性,可为初烤烟叶质量评价提供理论参考。展开更多
文摘The inclusion complexes of poorly water-soluble cephalosporin, cefuroxime axetil(CFA), were prepared with β-cyclodextrin(βCD) with or without addition of L-arginine(ARG) to improve its physicochemical properties. We also investigated the effect of ARG on complexation efficiency(CE) of βCD towards CFA in an aqueous medium through phase solubility behaviour according to Higuchi and Connors. Although phase solubility studies showed AL(linear) type of solubility curve in presence and absence of ARG, the CE and association constant(Ks) of βCD towards CFA were significantly promoted in presence of ARG,justifying its use as a ternary component. The solid systems of CFA with βCD were obtained by spray drying technique with or without incorporation of ARG and characterized by differential scanning calorimetry(DSC), X-ray powder diffractometry(XRPD), scanning electron microscopy(SEM), and saturation solubility and dissolution studies. The molecular modeling studies provided a better insight into geometry and inclusion mode of CFA inside βCD cavity. The solubility and dissolution rate of CFA were significantly improved upon complexation with βCD as compared to CFA alone. However, ternary system incorporated with ARG performed better than binary system in physicochemical evaluation. In conclusion, ARG could be exploited as a ternary component to improve the physicochemical properties of CFA via βCD complexation.
基金This work was supported by the National Natural Science Foundation of China (No30371831)
文摘Objective To investigate the effects of low dosage of β-elemene on the radiosensitivity of rabbit VX2 renal transplant carcinoma model. Methods We took the rabbit VX2 renal transplant carcinoma as the model. Experimental rabbits were divided into three groups: the control group, the radiation group, and the radiation +β-elemene (radiosensitivity) group. The change of tumor was observed by Spiral CT and B ultrasound to compare its regrowth period. The tumor was measured by light microscopy and electron microscopy. Results The tumor in radiosensitivity group was restrained obviously and the sensitization enhancement ratio (SER) of β-elemene was 1.89. Different apoptosis was observed under transmission electron microscopy. Conclusion Low dosage β-elemene can enhance the radiosensitivity of rabbit VX2 renal transplant carcinoma model and induce the apoptosis of tumor cells, but the mechanism needs further study. It promotes apoptosis in mechanisms in vitro.
基金supported by grants from the National Natural Science Foundation of China (21303086)the Natural Science Foundation of Jiangsu Province (BK20130884)the Research Fund for Doctoral Program of Higher Education (20123234120012)
文摘Ursolic acid(UA) and oleanolic acid(OA) are insoluble drugs. The objective of this study was to encapsulate them into β-cyclodextrin(β-CD) and compare the solubility and intermolecular force of β-CD with the two isomeric triterpenic acids. The host-guest interaction was explored in liquid and solid state by ultraviolet-visible absorption,1H NMR, phase solubility analysis, and differential scanning calorimetry, X-ray powder diffractometry, and molecular modeling studies. Both experimental and theoretical studies revealed that β-CD formed 1: 1 water soluble inclusion complexes and the complexation process was naturally favorable. In addition, the overall results suggested that ring E with a carboxyl group of the drug was encapsulated into the hydrophobic CD nanocavity. Therefore, a clear different inclusion behavior was observed, and UA exhibited better affinity to β-CD compared with OA in various media due to little steric interference, which was beneficial to form stable inclusion complex with β-CD and increase its water solubility effectively.
文摘为提高近红外光谱法测定初烤烟叶中β-胡萝卜素和叶黄素含量的准确性和稳定性,采用随机蛙跳(Random Frog,RF)筛选特征波长建立上述指标的偏最小二乘(Partial Least Squares,PLS)近红外模型,结合模型内部交互验证结果确定最优建模波长数和主成分数,并对最优模型的准确性和稳定性进行内外部评价。结果表明:相较于全波长(1298个波长)建模,利用RF筛选出的181个和216个特征波长建模,模型的决定系数(R2)由0.7718和0.8677分别提高至0.9511和0.9587,校正均方根误差(RMSEC)由3.362μg/g和4.930μg/g分别降低至1.556μg/g和2.756μg/g,交互验证均方根误差(RMSECV)由3.304μg/g和4.836μg/g分别降低至1.529μg/g和2.703μg/g;模型外部预测集(样品数=50)的预测平均相对误差分别由11.80%和9.62%降低至5.48%和5.49%。采用RF筛选特征波长能有效提升初烤烟叶β-胡萝卜素和叶黄素含量近红外模型的准确性和稳定性,可为初烤烟叶质量评价提供理论参考。
