甲砜霉素纳米粒的研制及表征

Development and physicochemical characterization of thiamphenicol nanoparticles

采用乳化溶剂挥发法制备一种可以有效降低粒径、提高药物水溶性的甲砜霉素纳米粒。以甲砜霉素纳米粒混悬液粒径大小为主要考察指标,利用单因素试验优化处方及工艺,并对纳米粒进行理化表征。结果显示,最佳制备条件为:油相与水相的体积比为1∶5,聚乙烯吡咯烷酮K30的浓度为1‰,在6000 r/min转速下匀浆5 min,在700 bar均质压力下循环7次,甘露醇为冻干保护剂。在最佳条件下制得的甲砜霉素纳米粒的平均粒径为225.5±30.5 nm,PDI平均值为0.260±0.02,载药量为(75.52±2.87)%,溶解度为9.69±0.78 mg/m L。表征结果显示,甲砜霉素纳米粒呈长棒状,粒径分布均一,化学结构没有变化,晶型结构发生了改变,可能以无定型状态存在。本研究为甲砜霉素的增溶方法供了一种新思路。

Emulsion solvent evaporation method was used to prepare the thiamphenicol nanoparticles that can evidently reduce particle size and improve the water solubility of the drug.Taking the size of the thiamphenicol nanoparticle suspension as the main investigation index,the prescription and process were optimized by single factor test analysis,and the physicochemical properties of the nanoparticles were characterized.The results showed that the optimal condition was:the volume ratio of the oil phase to the aqueous phase was 1∶5,the concentration of polyvinylpyrrolidone K30 was 1‰,the homogenization time was 5 min at the speed of 6000 r/min,the cycle was 7 times at the homogeneous pressure of 700 bar,and mannitol was the lyophilized protector.The average size of thiamphenicol nanoparticles prepared under the best conditions was 225.5±30.5 nm,the average PDI was 0.260±0.02,the thiamphenicol content was(75.52±2.87)%,and its solubility was 9.69±0.78 mg/m L.The characterization results showed that the thiamphenicol nanoparticles were long rod-shaped,uniformly distributed,and the chemical structure did not change,but the crystalline structure changed,and may exist in an amorphous state.The study provides a new idea to the solubilization study of thiamphenicol.