摘要
目的:制备茶碱脉冲栓剂并评价其体外释药性质。方法:以处方基质中泊洛沙姆、羧甲基纤维素钠(CMC-Na)、聚乙二醇6000(PEG6000)、PEG400的不同用量为因素,以释药时滞及累积释药率为指标采用单因素法筛选栓剂处方组成,并考察填充不同内容物(茶碱原料、茶碱-PVP物理混合物和茶碱-PVP固体分散体)的栓剂的累积释药率。结果:较优基质处方组成为70%泊洛沙姆、6%CMC-Na、12%PEG6000、12%PEG400,其体外释药时滞为4h,90min累积释药率为85%以上;3种填充不同内容物的栓剂累积释药率分别为58.8%、65.8%、91%。结论:所制茶碱脉冲栓剂具有较好的脉冲释药作用。
OBJECTIVE： To prepare theophylline pulsed suppository（TPS） and evaluate its in vitro release characteristics. METHODS： The formulation of TPS was optimized using single factor method taking the amount of base materials including poloxamer, CMC-Na, PEG 6000 and PEG 400 as factors with lag time of drug release and the accumulative drug release rate served as indexes. The accumulative drug release rates of the TPS prepared with different fillers （crude drug of theopylline, theopylline- PVP physical mixture, and the theopylline- PVP solid dispersion） were investigated. RESULTS： The optimal formulation was as follows： 70% poloxamer, 6% CMC-Na, 12% PEG 6000, 12% PEG 400; its lag time of in vitro drug release was about 4 hours and its accumulative drug release rate at 90 min reached more than 85%. The accumulative drug release rates of the suppository prepared with 3 different fillers were 58.8%, 65.8% and 91%, respectively. CONCLUSION： The prepared TPS showed satisfactory pulsed release efficacy.
出处
《中国药房》
CAS
CSCD
北大核心
2009年第28期2206-2208,共3页
China Pharmacy
关键词
茶碱
脉冲栓剂
制备
处方
体外释药
Theophylline
Pulsed suppository
Preparation
Formulation
In vitro drug release
