肺靶向地塞米松微球的制备及体外释药.pdfVIP

2006 26 5 Chin Hosp Pharm J, 2006 May, Vol 26, No. 5 515 陶兆武, 徐启勇, 叶燕青, 彭平, 汪自然 (, 43 00 71) [ ] :研究水溶性药物地塞米松磷酸钠肺靶向 球制备工艺的优化:以油/ 水型乳化-溶剂挥发法制备 球,考 察 球的性质及肺靶向性维持其他条件不变, 内相中加入甲醇和改变外相中氯化钠的加入量后, 考察 球的载药量变化 :所制的 球的平均粒径为( 8. 37 4. 0) m突释性好, 最初0 .5 h 释药量达48 .28% 各器官石蜡切片中, 肺组织中有 较多 球嵌顿随着内相中加入甲醇和外相中加入氯化钠, 球载药量提高: 地塞米松 球有良好的肺靶向性采用 油/ 水型乳化-溶剂挥发法制备水溶性地塞米松 球时, 内相中加入甲醇和外相中加入氯化钠有助于提高 球的载药量 [ ] 地塞米松磷酸钠;聚乳酸-聚乙醇酸共聚物; 球;肺靶向 [ ] R965. 1 [ ] A [ ] 1001-52 13( 2006) 05-0515-03 Preparation and in vit ro characterization of microspheres containing dexamethasone sodium phosphate TAO Zhao-wu, X Qi-yong, YE Yan-qing, Peng-ping,WANG Zhi-ran (T he Zhongnan Hospital of Wuhan n-i versity, Hubei Wuhan 43 00 71, China) ABSTRACT:OBJECTIVE To optimize the preparation technique of microspheres containing dexamethasone sodium phosphate. ETHODS M icrospheres were prepared by O/ W emulsification-evaporation method. Characterizations of microspheres were investigation. Effects of adding methanol in inner phase and sodium chloride in external phase on drug loading were investiga- tion. RESULTS T he average particle sizewas ( 8. 3 4 .0) m. In the in v itr o release test, the burst stagewas notable. Drug released near 4 8. 28% in the initial 0. 5 h. Many microspheres in the lung could be observed in the paraffin section. Methanol in inner phase and sodium chloride in external phase could increase the drug loading. CONCLUSION Lung could be targeted by these microspheres. The drug loading can be enhanced-by using O/ W emulsification-evaporation medhad, and adding methanol in inner phase and sodium chloride in external phase. KEY WORDS:dexamethasone sodium phosphate; PLGA; microsphere; lung targeted (dexamethasone sodium phos- 178 8() ; ( [ 1] ) ; phate, DSP) , 2 DSP 2. 1 O/ W - , DSP , , [3] DSP