罗哌卡因乳酸羟基乙酸共聚物微球的制备及体外释药研究

Preparation and in Vitro Release of Poly(lactide-co-glycolide) Microspheres Loaded with Ropivacaine

目的:优化罗哌卡因乳酸羟基乙酸共聚物微球制备工艺,并考察其粉粒学特征和体外释药特性。方法:以乳酸羟基乙酸共聚物为载体,采用W/O/W乳剂-扩散溶剂挥发法制备微球,以微球的粒径、药物包封率、载药量及微球形态等重要粉粒学特征为考察指标,通过正交分析试验优化微球制备工艺,并进行体外释药研究。结果:以优化处方制备的制剂,外观光滑圆整,平均粒径为(2.525±0.047)μm,粒径在1.8～5.0μm的占总数的80%以上,载药量(6.067±0.312)%,包封率(58.05±1.169)%。其体外释药曲线可用Higuchi方程拟合,192h累积释药率达82%,t1/2=60.16h。结论:罗哌卡因乳酸羟基乙酸共聚物微球具有明显的缓释性。

OBJECTIVE： To optimize the preparation technology of poly（lactide-co-glycolide） （PLGA） microspheres loaded with ropivacaine （ROP- PLGA-MS） and study their powder particle characteristics and in vitro release characteristics. METHODS： ROP- PLGA- MS was prepared with PLGA as carriers using the water- in- oil- in- water（W/ O/ W） emulsion solvent evaporation method. The micromeritic characteristics of ROP- PLGA- MS, such as the particle size, loading and entrapment efficiency were taken as indexes for evaluation, and the preparation technology was optimized by orthogonal design. Its dissolution characteristics in vitro were studied. RESULTS： The prepared microspheres were spherical with smooth surfaces, with an average particle size of （2.525±0.047） μm and over 80% falling in the range of 1.8-5.0 μm. The encap- sulation efficiency was （ 58.05 ± 1.169） % and the drug loading efficiency was （6.067 ± 0.312） %. The in vitro release curves of ropivacaine microspheres could be fitted with Higuchi equation. The accumulated release percentage of which was 82 % in 192 h, and t 1/2 = 60.16 h. CONCLUSION ： ROP - PLGA - MS has obvious sustained release.