二丙酸倍氯米松缓释微囊在豚鼠体内释药浓度的测定  

Determination of BDP level from Slow Released Nanocapsule of BDP in vivo Healthy Guineapigs

作　　者：林芳[1] 孙铭[1] 肖琅[1] 周立波[1] 

机构地区：[1]天津市第三中心医院

出　　处：《生物医学工程与临床》2002年第4期191-192,202,共3页Biomedical Engineering and Clinical Medicine

基　　金：国家自然科学基金资助;编号 39970 71 2

摘　　要：目的　了解BDP -PLGA纳米缓释微囊体内释药情况。方法　采用超声乳化法和去溶剂固化法 ,制备BDP -PLGA纳米缓释微囊 ;健康豚鼠气管插管后 ,喷雾给予BDP纳米缓释微囊悬液 ,不同时间点取血及肺组织 ,HPLC法测定血浆及肺组织匀浆BDP浓度。结果　肺组织匀浆中 ,BDP普通制剂组BDP峰浓度出现在 8h左右 ,然后较快下降 ;纳米微囊组 ,给药后 0 .5～ 1.0h有一个相对的爆破释放 ,8h左右达峰浓度 ,12h开始BDP浓度明显高于普通制剂组 ,并维持相当高浓度的平台期 (至 72h)。血浆中普通制剂组和纳米微囊组BDP浓度均未测出。结论　吸入给药后 ,肺组织中BDP纳米微囊制剂表现良好的缓释性且局部药物浓度明显高于血浆 。Objective To study the releasing characteristics of beclomethasone dipropionate(BDP) from slow released polylactale-polyglycolic acid(PLGA) nanocapsule in vivo. Methods The slow released BDP-PLGA nanocapsule were prepared by ultrasound emulsification and dissolvent volatilization. The conventional prepared BDP or BDP-PLGA nanocapsule suspension were sprayed. Through tracheal intubation in devided groups of guineapigs,their blood and lung tissue samples were collected at different time-points,then BDP levels were determined by high performance liquid chromatography (HPLC). Results The peak concentration of BDP was found at about 8 hours and descended rapidly in lung tissue homogenates in conventional BDP group after administration of drug inhalation. But there was a relatively rapid burst releasing in 0.5～1.0 h after administration of BDP-PLGA nanocapsules, the peak level of BDP in lung tissue sample was occurred at about 8 h, followed by a high plateau up to 72 h. Compared with BDP-PLGA nanocapsule group, the BDP level in conventional BDP group was obviously lower since 12 h after inhalation of drug. The BDP concentration was not detected in both conventional and nanocapsule BDP groups. Conclusion After inhalation of drug, the good releasing characteristics of BDP-PLGA nanocapsule preparation is presented in lung tissue and local BDP level is significantly higher than that in blood plasma. Thus the BDP-PLGA nanocapsule is suitable for long term inhalation therapy.

关 键 词：糖皮质激素 二丙酸倍氯米松 缓释微囊 豚鼠 释药浓度 测定 

分 类 号：R965[医药卫生—药理学]