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目的 在本实验中 ,以生物可降解和生物相容性良好的聚乳酸 (PLA)或乳酸 -乙醇酸共聚物 (PLGA)为载体材料制备含有雌二醇药物的缓释微球 ,考察在制备过程中水溶性更强的四氢呋喃的加入对微球性质的影响。方法 以乙酸乙酯和四氢呋喃为有机溶剂、采用乳化 -溶剂萃取法制备含药微球 ,分别从成球性、粒径、包封率和体外释药等方面 ,进行制备工艺研究以及微球相关性质的研究。结果 在乙酸乙酯中加入四氢呋喃 ,使包封率降低 ,但在乙酸乙酯体积比大于 5 0 %时 ,增加四氢呋喃的用量对包封率无明显影响。相同条件下 ,在考察范围内 ,粒径随四氢呋喃用量比例的增大而增大 ,而载体的性质和微球含药量是影响微球释药的主要因素。结论 尽管在制备过程中的油相中加入了水溶性更强的四氢呋喃 ,但是通过控制制备工艺和条件 ,仍然可以得到球形态好、有适当粒径分布范围、载药量高并且突释程度小的雌二醇生物可降解缓释微球
OBJECTIVE In this experiment, sustained release microspheres containing estradiol drug were prepared with polylactic acid (PLA) or lactic acid-glycolic acid copolymer (PLGA) with good biodegradability and biocompatibility. The influence of the more water-soluble tetrahydrofuran in the process on the properties of the microspheres. Methods The drug-containing microspheres were prepared by emulsification-solvent extraction using ethyl acetate and tetrahydrofuran as organic solvents. The preparation techniques and microsphere-related properties of the drug-containing microspheres were discussed respectively from the aspects of spheroidization, particle size, entrapment efficiency and drug release in vitro Nature of the study. As a result, tetrahydrofuran was added to the ethyl acetate to reduce the entrapment efficiency. However, when the volume ratio of ethyl acetate was more than 50%, the amount of tetrahydrofuran added had no significant effect on the entrapment efficiency. Under the same conditions, the particle size increased with the increase of the proportion of tetrahydrofuran in the study area, and the nature of the carrier and the content of the microspheres were the main factors affecting the release of microspheres. Conclusions Although the more water-soluble tetrahydrofuran was added to the oil phase during the preparation process, by controlling the preparation process and conditions, it is still possible to obtain good spherical morphology, suitable particle size distribution, high drug loading, and low degree of burst Of estradiol biodegradable sustained-release microspheres