盐酸地尔硫延迟起释型缓释片的研制  

PREPARATION OF DILTIAZEM HYDROCHLORIDE DELAYED-ONSET, SUSTAINED RELEASE TABLET

作　　者：张宁[1] 朱家壁[1] 

机构地区：[1]中国药科大学中昆制剂研究所,江苏南京210009

出　　处：《药学学报》2002年第9期724-727,共4页Acta Pharmaceutica Sinica

摘　　要：目的　制备盐酸地尔硫 (diltiazamhydrochloride,DIL)延迟起释型缓释片 ,解析释药机制 ,并考察外衣层组成对药物释放的影响。方法　用干压包衣技术制备盐酸地尔硫的延缓片 ,用释药时滞 (Tlag)及释药速率常数 (k)将各因素 (外衣层中的HPMC用量和粘度 ,PVPK30用量、EC粘度及压片压力 )对药物的释放效果进行评价。结果HPMC用量或粘度增大 ,Tlag延长 ,k减慢 ;PVPK30用量增大 ,Tlag减短 ,k加快 ;在一定范围内EC粘度及压片压力波动对释药行为无影响。结论　延缓片中药物主要是通过溶蚀机制释放 ,外衣层的溶蚀速率是决定释药时滞的关键因素。AIM To prepare diltiazem hydrochloride delayed onset, sustained release tablet, whi ch can not only provide the delay in release start, but also the constant releas e rate after a lag time. To analyze release mechanism and investigate the effect of outershell compositions on release behavior. METHODS The delayed onset, sustained release tablets were prepared by dry compression coated technology. The release profiles of uncoated cores and press coated tabl ets were compared. Two parameters, time lag ( T lag ) and release rate ( k ), were used to evaluate the influence of factors, such as the amount of hy droxypropylmethylcellulose (HPMC) and poly vinyl pyrrolidinone (PVP) K30, the viscosity of ethylcellulose (EC) and HPMC, and the compression load on diltazam hydrochloride (DIL) release. Higuchi equation and Peppa's equation were used to analyze release mechanism. RESULTS With the increase of HPMC amount or HPMC viscosity, T lag was prolonged and k was decreased; With the increase of PVP K30 amount, T lag wa s shortened and k was increased; EC viscosity and compression load above cer tain degree showed no effect on DIL release. CONCLUSION The drug release from delayed release tablet is controlled by erosion mechanism , T lag is determined by the erosion rate of outer shell.

关 键 词：盐酸地尔硫ZHUO 延迟起释剂缓释片 干压包衣技术 释药机制 释放度 影响因素 

分 类 号：R944.9[医药卫生—药剂学]