Aim To improve the dissolution rate and bioavailability of silybin. Methods Sustained-release silybin microspheres were prepared by the spherical crystallization technique with soliddispersing and release-retarding po...Aim To improve the dissolution rate and bioavailability of silybin. Methods Sustained-release silybin microspheres were prepared by the spherical crystallization technique with soliddispersing and release-retarding polymers. A differential scanning calorimeter and an X-ray diffractometer were used to investigate the dispersion state of silybin in the microspheres. The shape, surface morphology, and internal structure of the microspheres were observed using a scanning electron microscope. Characterization of the microspheres, such as average diameter, size distribution and bulk density of the microspheres was investigated. Results The particle size of the microspheres was determined mainly by the agitation speed. The dissolution rate of silybin from microspheres was enhanced by increasing the amount of the dispersing agents, and sustained by the retarding agents. The release rate of microspheres was controlled by adjusting the combination ratio of the dispersing agents to the retarding agents. The resuits of X-ray diffraction and differential scanning calorimetry analysis indicated that silybin was highly dispersed in the microspheres in amorphous state. The release profiles and content did not change after a three-month accelerated stability test at 40 ℃ and 75% relative humidity. Conclusion Sustained-release silybin microspheres with a solid dispersion structure were prepared successfully in one step by a spherical crystallization technique combined with solid dispersion technique. The preparation process is simple, reproducible and inexpensive. The method is efficient for designing sustained-release microspheres with water-insoluble drugs.展开更多
目的以羟丙基甲基纤维素(HPMC)为载体、西沙必利为模型药物制备固体分散体,以此来提高药物在水中的溶解度和体外释放速度。方法利用溶剂挥发法,分别用乙醇和0.1 mol·L-1HCl将药物和载体溶解,使药物均匀分散在载体中,再减压除去溶...目的以羟丙基甲基纤维素(HPMC)为载体、西沙必利为模型药物制备固体分散体,以此来提高药物在水中的溶解度和体外释放速度。方法利用溶剂挥发法,分别用乙醇和0.1 mol·L-1HCl将药物和载体溶解,使药物均匀分散在载体中,再减压除去溶剂得到固体分散体。结果当载体与药物的比例为4:1时,X射线衍射实验表明药物的晶体峰已经消失。与西沙必利的原药相比,固体分散体中药物在水、人工胃液和人工肠液中的溶解度分别提高了339.43%、232.62%和217.95%。体外药物释放结果表明,当以水和人工胃液为介质时,用固体分散体制备的缓释片的药物释放速度要快于用原料药制备的缓释片。结论羟丙基甲基纤维素(HPMC E 5-LV)作为载体材料可以和西沙必利形成固体分散体,并提高了药物的溶解度和体外释药速度。展开更多
Solid dispersion is an established concept for drug solubility and bioavailability enhancement but strongly dependent on the choice of an appropriate carrier and preparation technique[1,2].Ternary solid dispersion is ...Solid dispersion is an established concept for drug solubility and bioavailability enhancement but strongly dependent on the choice of an appropriate carrier and preparation technique[1,2].Ternary solid dispersion is one of the promising methods to increase the solubility of poorly-water soluble drug.The present work was conducted to increase the solubility of manidipine hydrochloride(MDP)using ternary solid dispersion prepared by melting and then solidifying at low temperature.The effect of cooling technique on the physicochemical properties of the developed system was investigated.展开更多
文摘Aim To improve the dissolution rate and bioavailability of silybin. Methods Sustained-release silybin microspheres were prepared by the spherical crystallization technique with soliddispersing and release-retarding polymers. A differential scanning calorimeter and an X-ray diffractometer were used to investigate the dispersion state of silybin in the microspheres. The shape, surface morphology, and internal structure of the microspheres were observed using a scanning electron microscope. Characterization of the microspheres, such as average diameter, size distribution and bulk density of the microspheres was investigated. Results The particle size of the microspheres was determined mainly by the agitation speed. The dissolution rate of silybin from microspheres was enhanced by increasing the amount of the dispersing agents, and sustained by the retarding agents. The release rate of microspheres was controlled by adjusting the combination ratio of the dispersing agents to the retarding agents. The resuits of X-ray diffraction and differential scanning calorimetry analysis indicated that silybin was highly dispersed in the microspheres in amorphous state. The release profiles and content did not change after a three-month accelerated stability test at 40 ℃ and 75% relative humidity. Conclusion Sustained-release silybin microspheres with a solid dispersion structure were prepared successfully in one step by a spherical crystallization technique combined with solid dispersion technique. The preparation process is simple, reproducible and inexpensive. The method is efficient for designing sustained-release microspheres with water-insoluble drugs.
文摘目的以羟丙基甲基纤维素(HPMC)为载体、西沙必利为模型药物制备固体分散体,以此来提高药物在水中的溶解度和体外释放速度。方法利用溶剂挥发法,分别用乙醇和0.1 mol·L-1HCl将药物和载体溶解,使药物均匀分散在载体中,再减压除去溶剂得到固体分散体。结果当载体与药物的比例为4:1时,X射线衍射实验表明药物的晶体峰已经消失。与西沙必利的原药相比,固体分散体中药物在水、人工胃液和人工肠液中的溶解度分别提高了339.43%、232.62%和217.95%。体外药物释放结果表明,当以水和人工胃液为介质时,用固体分散体制备的缓释片的药物释放速度要快于用原料药制备的缓释片。结论羟丙基甲基纤维素(HPMC E 5-LV)作为载体材料可以和西沙必利形成固体分散体,并提高了药物的溶解度和体外释药速度。
文摘Solid dispersion is an established concept for drug solubility and bioavailability enhancement but strongly dependent on the choice of an appropriate carrier and preparation technique[1,2].Ternary solid dispersion is one of the promising methods to increase the solubility of poorly-water soluble drug.The present work was conducted to increase the solubility of manidipine hydrochloride(MDP)using ternary solid dispersion prepared by melting and then solidifying at low temperature.The effect of cooling technique on the physicochemical properties of the developed system was investigated.
