广东药学院学报
廣東藥學院學報
엄동약학원학보
ACADEMIC JOURNAL OF GUANGDONG COLLEGE OF PHARMACY
2014年
6期
675-678
,共4页
利福平%聚乳酸-羟基乙酸共聚物%多孔微球%理化特性%体外释放
利福平%聚乳痠-羥基乙痠共聚物%多孔微毬%理化特性%體外釋放
리복평%취유산-간기을산공취물%다공미구%이화특성%체외석방
rifampicin%PLGA%porous microspheres%physicochemical characteristics%release in vitro
目的:制备多孔利福平/聚乳酸-羟基乙酸共聚物( PLGA)微球,并考察其理化特性和体外释放行为。方法以PLGA为载体,NH4 HCO3为致孔剂,改良乳化溶剂扩散法制备多孔利福平微球,扫描电镜观察微球的形态,测定微球的空气动力学直径,HPLC法测定微球的载药量和包封率,并考察微球的体外释放行为。结果多孔利福平/PLGA微球为多孔状,粒径和孔道大小随NH4 HCO3的量的增加而相应增大,空气动力学直径在1~5μm范围内,载药量和包封率分别约为5%和60%,体外累积释放率24 h可达60%左右。结论多孔微球具有适宜的吸入特性,或可成为递送利福平的新载体。
目的:製備多孔利福平/聚乳痠-羥基乙痠共聚物( PLGA)微毬,併攷察其理化特性和體外釋放行為。方法以PLGA為載體,NH4 HCO3為緻孔劑,改良乳化溶劑擴散法製備多孔利福平微毬,掃描電鏡觀察微毬的形態,測定微毬的空氣動力學直徑,HPLC法測定微毬的載藥量和包封率,併攷察微毬的體外釋放行為。結果多孔利福平/PLGA微毬為多孔狀,粒徑和孔道大小隨NH4 HCO3的量的增加而相應增大,空氣動力學直徑在1~5μm範圍內,載藥量和包封率分彆約為5%和60%,體外纍積釋放率24 h可達60%左右。結論多孔微毬具有適宜的吸入特性,或可成為遞送利福平的新載體。
목적:제비다공리복평/취유산-간기을산공취물( PLGA)미구,병고찰기이화특성화체외석방행위。방법이PLGA위재체,NH4 HCO3위치공제,개량유화용제확산법제비다공리복평미구,소묘전경관찰미구적형태,측정미구적공기동역학직경,HPLC법측정미구적재약량화포봉솔,병고찰미구적체외석방행위。결과다공리복평/PLGA미구위다공상,립경화공도대소수NH4 HCO3적량적증가이상응증대,공기동역학직경재1~5μm범위내,재약량화포봉솔분별약위5%화60%,체외루적석방솔24 h가체60%좌우。결론다공미구구유괄의적흡입특성,혹가성위체송리복평적신재체。
Objective To prepare the porous rifampicin-loaded poly ( lactic-co-glycolic acid ) ( PLGA ) microspheres and investigate the physicochemical characteristics and drug release in vitro of the microspheres. Methods Porous microparticles were prepared from PLGA by modified emulsion solvent-extraction method with ammonium bicarbonate as the porogen. The morphology of the microspheres was examined by scanning electron microscope and the mass median aerodynamic diameter were calculated. Drug loading and encapsulation efficiency were determined by high performance liquid chromatography and the in vitro release behavior of microspheres were investigated. Results Microspheres were porous, and the particle size and pore size increased as the porogen concentration increased. The aerodynamic diameter was within 1-5 μm. The drug loading and encapsulation efficiency in the porous PLGA microparticles were about 5% and 60%, respectively, and the in vitro drug release from porous microspheres was faster than that from non-porous microspheres, approximately 60% in 24 h. Conclusion Porous PLGA microspheres were suitable for inhalation, they could be a new drug carrier for rifampicin.