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1、离校化学工程学报Journal of Chemical Engineering of Chinese UniversitiesM 231 W2009年2月No. I WI 23Feb. 2009文章编号：1003-9015(2009)01-0099-06反溶剂重结晶法制备布地奈德超细颗粒及其肺部给药体外评价胡蚌婷，乐 at降立川，沈志刖，陈建峰(北京化工大学纳米材料先进创备技术与应用科学教育部重点实验室，北京100029)摘 要：利用反溶刊重结晶法对平臥药布地奈进行f超细赖粒的制备研究当以甲諄为移刊.水为反溶剂时.分别 粤察了甲諄水为体积比.混合莊度和干燥方式对产岛平均粒径和收率的彫响结杲表明
2、.当布地余佛甲醉溶液与水的 体枳比为1:7.搅持转逮高于SOOOr.min-1时.浆料中可得到平均长径3 pm.短径2pm.厚度200 nm的桶關形片状頰 札并且一次收率为96.02%将此布地奈箒浆料通过真空干燥和喷雾干燥氐产品均可保持浆料中颗料的大小与形貌. 而经喷雾冷冻二燥后则变为10-20 pm左右的球形颤粒FT4R和XRD分析显示.与原料药和气潦粉碎冷品相比.反 溶刊更结品制得的布地奈键的化学结构与晶型均无改变.此外.经辭部给药体外评价.桶H1形片状颗粒具有最优的沉 枳分布.FPF值高达60%以上，分别比故料囲和气流粉碎簡品提高了 9倍和1.5倍.关健词：布地亲德；反溶剂超细粉体*肿部
3、给药中图分类号* TQ467.95: R944.7文繊标识码：APreparation of Budesonide Ultra-fine Particles by Antisolvent Recrystallization andtheir in vitro Evaluation for Pulmonary DeliveryHU Ting-ting. LE Yuan, JIANG Li-chuan. SHEN Zhi-gang, CHEN Jian-feng(Key Lab for Nanomaterials, Ministry of Education, Beijing University
4、 of Chemical Technology,Beijing 100029, China)Abstract: The budesonide ultra-fine particles were prepared by antisolvent recrystallization for pulmonary delivery. Methanol was used to form the budesonide solution, and the water was chosen as the antisolvcnt to induce precipitation. The main factors
5、aflecting the particle size of the precipitates were investigated; they are the volume ratio of methanol to water, the stirring speed and the drying methods. The results indicate that the elliptic flaky particles with average 3 pm in length, 2 pm in width and 200 nm in thickness were obtained from t
6、he slurry when the ratio of methanol to water is 1：7 and the stirring speed is over 5000 r min"1; and the recovery of the recrystallization process can be up to 96.02%. The size and morphology of the particles in the slurry do not change after vacuum drying or spray drying. However, the spray-f
7、reeze dried particles have spherical shape with 10-20 pm in diameter. As assessed by FT-IR and XRD, all the as-prepared budesonide dry powders have the same chemical structure and crystal form as the raw material and jet-milled budesonide In vitro evaluations with an Aerolizer inhaler and a multi-st
8、age liquid impinger show that the flaky particles have better aerosol performance because their FPF value (fine particle fraction) could be over 60%, which is 9 times and 1.5 times higher than that of raw material and jet-milled budesonide, respectively.Key words: budesonide; antisolvent recrystallization; ultra-fine particle; pulmonary delivery1前 s近5年.布地奈德(budesonide)-直位居我国平喘药市场的第一位。由于肺部给药是治疗哮喘的最佳牧MBM： 2008X)1.21； 订200S4646.鼻舎项目：0Q« “S63- iftM2006AA030202)i北京術科技韓星计划(20078022).作着窗介，M(I98O)江苏齐卅人.北京化I：大沪上生通讯联系人&陈建峰.E-maUi chenj(nwl bact.educn