【摘要】 以头孢羟氨苄-水+乙醇-二氧化碳系统为研究对象,利用超临界流体膨胀减压过程成功制备出了水溶性药物头孢羟氨苄的超细微粒,测定了混合器压力和温度、进液速率、溶液浓度对微粒形态、粒径和粒径分布的影响.实验结果表明:选用水+乙醇做溶剂,在适合的操作参数下可制备出粒径在1～3μm适于吸入式给药的头孢羟氨苄超细微粒,且大部分微粒形态呈完整的球形;各因素对微粒粒径及粒径分布均有不同程度的影响,其中混合器压力影响最明显;微粒粒径及粒径分布可通过改变操作参数进行控制.最佳的操作参数为混合器压力14MPa、温度60℃、溶液浓度4mg/mL、进液速率3mL/min,在此条件下,可获得最小粒径和粒径分布的水溶性超细微粒.更多还原

【Abstract】 Cefadroxil(CD) microparticles were successfully prepared from CD-water+ethanol-CO2 mix-solution by the supercritical fluid expansion depressurization(SFED) process.The influences of the operation parameters,including the pressure and temperature in the mixing vessel,the feed solution rate and the solution concentration on the particle morphology,size and size distribution,were investigated.The experimental results show that CD microparticles with the diameter range of 1-3 μm which is suitable for inhalation delivery can be prepared by using water+ethanol as original solvent under some adapted operation conditions and most of them are well-defined spherical.Different parameters make different influences on the particle diameter and diameter distributions; the pressure in the mixing vessel is the most effective factor among these parameters.The particle characteristics can be controlled by adjusting operation conditions and the optimal operation parameters for preparing CD microparticles are as follows: The pressure is 14 MPa,temperature is 60 ℃,the solution concentration is 4 mg/mL and the feed solution rate is 3 mL/min.The particles with the minimum diameter and narrowest diameter distributions can be obtained under this condition.更多还原