首次以利福喷丁为模型药物、聚己内酯为载体材料,制备了用于长效抑制骨结核生长的利福喷丁聚己内酯缓释微球,观察其理化特性和体外释放性能.采用O/W乳化溶剂挥发法制备载利福喷丁聚己内酯微球,系统考察了投药量、聚乙烯醇的浓度、乳化速度对微球形貌、粒径、载药量扣包封率的影响.通过对制备工艺的优化,得到最佳制备条件是乳化速度300 r·min-1,投药量20 mg,聚乙烯醇的浓度2％.所制备的载利福喷丁聚己内酯微球圆整,表面有微孔,大小分布均匀,粒径分布较窄,平均粒径为(27.249±0.256) μm、载药量(3.098±0.011)％、包封率(34.078±0.123)％.实验结果表明:聚己内酯是负载利福喷丁的一种理想控释材料.
参考文献
| [1] | Avnesh Kumari;Sudesh Kumar Yadav;Subhash C. Yadav .Biodegradable polymeric nanoparticles based drug delivery systems[J].Colloids and Surfaces, B. Biointerfaces,2010(1):1-18. |
| [2] | Sinha VR;Bansal K;Kaushik R;Kumria R;Trehan A .Poly-epsilon-caprolactone microspheres and nanospheres: an overview.[J].International Journal of Pharmaceutics,2004(1):1-23. |
| [3] | Pitt G;Gratzl M;Kimmel G et al.Aliphatic polyesters Ⅱ.The degradation of poly (DL-lactide),poly (ε-caprolactone),and their copolymers in vivo[J].BIOMATERIALS,1981,2(04):215. |
| [4] | Sun HF;Mei L;Song CX;Cui XM;Wang PY .The in vivo degradation, absorption and excretion of PCL-based implant[J].Biomaterials,2006(9):1735-1740. |
| [5] | Sterling TR;Villarino ME;Borisov AS;Shang N;Gordin F;Bliven Sizemore E;Hackman J;Hamilton CD;Menzies D;Kerrigan A;Weis SE;Weiner M;Wing D;Conde MB;Bozeman L;Horsburgh CR Jr;Chaisson RE .Three months of rifapentine and isoniazid for latent tuberculosis infection.[J].The New England journal of medicine,2011(23):2155-2166. |
| [6] | O'Donnell P B;McGinity J W .Preparation of microspheres by the solvent evaporation technique[J].Advanced Drug Delivery Reviews,1997,28(01):25. |
| [7] | 李良,李国明,黎茂荣,容品加.利福平/聚乳酸微球的制备研究[J].华南师范大学学报(自然科学版),2003(03):102-107. |
| [8] | Gasparini G;Kosvintsev SR;Stillwell MT;Holdich RG .Preparation and characterization of PLGA particles for subcutaneous controlled drug release by membrane emulsification[J].Colloids and Surfaces, B. Biointerfaces,2008(2):199-207. |
| [9] | 罗培培,左奕,孙斌,黄棣,蒋电明,李玉宝.载异烟肼聚己内酯微球的制备及其性质研究[J].功能材料,2011(08):1410-1414. |
| [10] | Hombreiro Pérez M;Zinutti C;Lamprecht A et al.The preparation and evaluation of poly (ε-caprolactone) microparticles containing both a lipophilic and a hydrophilic drug[J].Journal of Controlled Release,2000,65(03):429. |
| [11] | Ki-Seok Kim;Soo-Jin Park .Characterization and release behaviors of porous PCL/Eudragit RS microcapsules containing tulobuterol[J].Colloids and Surfaces, B. Biointerfaces,2010(2):404-409. |
| [12] | Jameela S;Suma N;Jayakrishnan A .Protein release from poly (ε-caprolactone) microspheres prepared by melt encapsulation and solvent evaporation techniques:A comparative study[J].J Biomater Sci:Polym Ed,1997,8(06):457. |
| [13] | Santos CA;Freedman BD;Ghosn S;Jacob JS;Scarpulla M;Mathiowitz E .Evaluation of anhydride oligomers within polymer microsphere blends and their impact on bioadhesion and drug delivery in vitro.[J].Biomaterials,2003(20):3571-3583. |
上一张
下一张
上一张
下一张
计量
- 下载量()
- 访问量()
文章评分
- 您的评分：
-
10%
-
20%
-
30%
-
40%
-
50%