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采用超临界CO2抗溶剂法制备具有缓释效果的布洛芬/乙基纤维素(EC)-聚乙烯醇吡咯烷酮(PVP)复合微粒。以载药量为主要评价指标,采用正交试验设计优选布洛芬/EC-PVP复合微粒的制备工艺,并对优选的工艺组合进行了包封率、粒径分布、电镜分析、红外光谱(IR)、差示扫描量热法(DSC)以及体外溶出等实验分析。正交试验得到的优选工艺为:结晶温度40℃,结晶压力12 MPa,PVP质量浓度4 mg.mL/1,动态CO2流出速度3.5 L.min?1。此工艺条件下,制备得到的复合微粒的载药量和包封率分别为12.14%和52.21%,平均粒径为27.621μm;IR与DSC分析表明PVP与EC可能发生了络合反应;体外溶出实验表明布洛芬/EC-PVP复合微粒具有良好的缓释效果。实验表明,超临界CO2抗溶剂法可制备具有缓释效果的布洛芬/EC-PVP复合微粒。
The supercritical CO2 antisolvent method was used to prepare ibuprofen / ethyl cellulose (EC) -polyvinyl pyrrolidone (PVP) composite particles with sustained release effect. The drug loading was taken as the main evaluation index. The orthogonal experiment was adopted to optimize the preparation process of ibuprofen / EC-PVP composite particles. The optimal combination of process parameters including entrapment efficiency, particle size distribution, electron microscopy, IR), differential scanning calorimetry (DSC) and in vitro dissolution experiments. The optimum conditions of orthogonal experiment were as follows: the crystallization temperature was 40 ℃, the crystallization pressure was 12 MPa, the mass concentration of PVP was 4 mg.mL -1 and the dynamic CO2 efflux rate was 3.5 L.min -1. Under these conditions, the drug loading and entrapment efficiency of the prepared composite particles were 12.14% and 52.21%, respectively, and the average particle size was 27.621 μm. IR and DSC analysis showed that the complexation reaction between PVP and EC might occur. Experiments show that ibuprofen / EC-PVP composite particles have a good sustained-release effect. Experiments show that supercritical CO2 anti-solvent method can be prepared with sustained-release effect of ibuprofen / EC-PVP composite particles.