安徽医药
安徽醫藥
안휘의약
ANHUI MEDICAL AND PHARMACEUTICAL JOURNAL
2015年
7期
1241-1244,1245
,共5页
利福平%肺部给药%多孔微球%聚乳酸-羟基乙酸共聚物
利福平%肺部給藥%多孔微毬%聚乳痠-羥基乙痠共聚物
리복평%폐부급약%다공미구%취유산-간기을산공취물
rifampicin%pulmonary drug delivery%porous microsphere%PLGA
目的:以利福平为模型药物,研究多孔聚乳酸—羟基乙酸共聚物(poly(lactic-co-glycolic acid),PLGA)微球的最佳制备工艺。方法乳化溶剂扩散法制备多孔微球,采用扫描电镜观察微球形态,HPLC 法测定微球包封率。通过单因素考察实验,筛选影响微球形态和包封率的主要因素并优选条件。结果制备过程中 PLGA 种类、PLGA 浓度、致孔剂浓度、均质速度、外水相 PVA 浓度等影响微球的粒径、多孔结构和包封率。按优化工艺制备的微球平均粒径为8.6μm,密度为0.1 g·cm -3,易于吸入并提高肺部的沉积率。结论低密度多孔微球具有适宜的吸入特性和肺部沉积率,或可成为递送抗结核药物的新载体。
目的:以利福平為模型藥物,研究多孔聚乳痠—羥基乙痠共聚物(poly(lactic-co-glycolic acid),PLGA)微毬的最佳製備工藝。方法乳化溶劑擴散法製備多孔微毬,採用掃描電鏡觀察微毬形態,HPLC 法測定微毬包封率。通過單因素攷察實驗,篩選影響微毬形態和包封率的主要因素併優選條件。結果製備過程中 PLGA 種類、PLGA 濃度、緻孔劑濃度、均質速度、外水相 PVA 濃度等影響微毬的粒徑、多孔結構和包封率。按優化工藝製備的微毬平均粒徑為8.6μm,密度為0.1 g·cm -3,易于吸入併提高肺部的沉積率。結論低密度多孔微毬具有適宜的吸入特性和肺部沉積率,或可成為遞送抗結覈藥物的新載體。
목적:이리복평위모형약물,연구다공취유산—간기을산공취물(poly(lactic-co-glycolic acid),PLGA)미구적최가제비공예。방법유화용제확산법제비다공미구,채용소묘전경관찰미구형태,HPLC 법측정미구포봉솔。통과단인소고찰실험,사선영향미구형태화포봉솔적주요인소병우선조건。결과제비과정중 PLGA 충류、PLGA 농도、치공제농도、균질속도、외수상 PVA 농도등영향미구적립경、다공결구화포봉솔。안우화공예제비적미구평균립경위8.6μm,밀도위0.1 g·cm -3,역우흡입병제고폐부적침적솔。결론저밀도다공미구구유괄의적흡입특성화폐부침적솔,혹가성위체송항결핵약물적신재체。
Objective To study and optimize the preparation process of porous rifampicin-loaded PLGA microspheres.Methods Por-ous microparticles were prepared by double emulsion solvent-extraction method.The morphology of the microspheres was examined by scanning electron microscope and the encapsulation efficiency was determined by high performance liquid chromatography.Through sin-gle factor selecting experiment,the major factors affecting the morphology and encapsulation efficiency of microspheres were investigated and optimized.Results The particle size,porous structure and encapsulation efficiency of the microspheres were influenced by the PL-GA type,PLGA concentration,porogenic agent concentration,homogeneous velocity and PVA concentration.Microspheres prepared by optimized process had an average particle diameter of 8.6 μm,and density of 0.1g·cm -3 ,which could be easily inhaled.Conclusion Low density porous microspheres with good inhalation characteristics and higher pulmonary deposition could be a new drug delivery carrier for anti-tuberculosis drugs.