摘要
采用热熔挤出法,选用聚氧化乙烯(PEO)、乙基纤维素(EC)、羟丙甲基纤维素(HPMC)为载体制备了布洛芬缓释制剂,并比较其释药速率。在三种载体中添加不同辅料,比较对药物释放的调节作用;应用差式扫描量热法、电镜法对热熔挤出制剂与相应压制片剂进行比较,并与释放曲线进行比照。结果表明,三种载体制备的热熔挤出制剂,均对药物有缓释作用,其中药物从EC载体中释放最慢。在不同载体系统中添加相同辅料微晶纤维素(MCC)时,对药物的释放有不同调节作用,在PEO和HPMC系统中,药物12h时释放度提高近20%,且HPMC/MCC载体系统可达到较理想的药物释放;但MCC对EC系统的药物释放影响不大。在同一PEO载体系统中添加不同辅料时对释药速率产生的影响也不同;由差式扫描量热图谱、电镜、释放曲线结果,推测药物在热熔挤出制剂中的分散程度比在压片制剂中高。
Polyethylene oxide （PEO）, ethyl cellulose （EC） and hydroxypropyl methyl cellulose （HPMC） have been employed as carriers in hot-melt extrusion （HME） in order to fabricate sustained-release systems for ibuprofen. The effects of the different carriers and different excipients on the rate of drug release were studied. Scanning electron microscopy （SEM） was used to examine cross sections of the extrudates and directly compressed （DC） tablets. All three carriers （PEO, EC and HPMC） sustained the rate of IBP release from extrudates. EC gave the slowest drug release, with only 20 % being released in 12 h. The effect of adding microcrystalline celluose （MCC） as an excipient was different for the three carrier systems： the release rate was increased by nearly 20% in 12 h for PEO/MCC/IBP and HPMC/MCC/IBP, but there was little change in the case of EC/MCC/IBP. The rate of IBP release was increased by adding agar, low-substituted hydroxypropyl cellulose （L-HPC） or MCC as excipients to the PEO based system, while xanthan gum （XG） had the opposite effect on drug release. The DSC, SEM and release profile date all confirm that, there was a high distribution of the drug in the extrudates.
出处
《北京化工大学学报（自然科学版）》
EI
CAS
CSCD
北大核心
2008年第2期68-72,共5页
Journal of Beijing University of Chemical Technology(Natural Science Edition)
关键词
热熔挤出技术
布洛芬
缓释制剂
药物释放
hot-melt extrusion
ibuprofen
sustained-release dosage form
drug release
