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目的制备可通过肺部吸入方式给药的硫酸沙丁胺醇缓释微球。方法以透明质酸为载体材料,采用乳化溶剂挥发法制备硫酸沙丁胺醇的透明质酸微球,以微球的体积平均直径为指标考察不同工艺和处方因素的影响,并对优化处方的微球进行体外释放评价。结果经优化,得到的最佳制备工艺和处方为:透明质酸质量浓度为6 g·L~(-1),油相为含质量分数1.0%Span80的蓖麻油,药物与载体的质量比为1∶1,内外相的质量比为1∶10,匀质转速为1.2×104 r·min~(-1),超声功率为500 W。制备得到的最优硫酸沙丁胺醇微球,粒径较小,平均粒径为(4.75±2.56)μm;粒径分布较窄,跨距为1.55±0.09;表面粗糙;其体外释放行为表现出一定的缓释效果。结论透明质酸的质量浓度、乳化方式、超声功率是影响微球粒径的重要因素,透明质酸的性质对微球的体外释放行为有显著影响。
Objective To prepare salbutamol sulfate microspheres for pulmonary inhalation. Methods Hyaluronic acid microspheres were prepared by emulsifying solvent evaporation method using hyaluronic acid as carrier material. The effects of different techniques and prescription factors were investigated by taking the average diameter of microspheres as an index. Microspheres Evaluation of in vitro release. Results The optimal preparation process and prescription were as follows: the mass concentration of hyaluronic acid was 6 g · L -1, the oil phase was castor oil containing 1.0% Span 80, the mass ratio of drug to carrier was 1: 1, the mass ratio of inner and outer phase is 1:10, the speed of homogenization is 1.2 × 104 r · min -1, and the ultrasonic power is 500W. The prepared salbutamol sulphate microspheres had a smaller particle size and a mean particle size of (4.75 ± 2.56) μm, a narrow particle size distribution with a span of 1.55 ± 0.09 and a rough surface. The in vitro release behavior of salbutamol microspheres showed a certain Slow release effect. Conclusion The hyaluronic acid concentration, emulsification mode and ultrasonic power are important factors affecting the particle size of microspheres. The properties of hyaluronic acid have a significant effect on the in vitro release behavior of microspheres.