Design and evaluation of nicorandil extended-release tablet  

作　　者：Ju-Young Kim Chun-Woong Park Beom-Jin Lee Eun-Seok Park Yun-Seok Rhee 

机构地区：[1]College of Pharmacy,Woosuk University,Wanju-gun 565-701,Republic of Korea [2]College of Pharmacy,Chungbuk National University,Cheongju 361-763,Republic of Korea [3]College of Pharmacy,Ajou University,Suwon 443-749,Republic of Korea [4]School of Pharmacy,Sungkyunkwan University,Suwon 440-746,Republic of Korea [5]College of Pharmacy and Research Institute of Pharmaceutical Sciences,Gyeongsang National University,Jinju 660-701,Republic of Korea

出　　处：《Asian Journal of Pharmaceutical Sciences》2015年第2期108-113,共6页亚洲药物制剂科学（英文）

基　　金：supported by the Basic Science Research Program through the National Research Foundation of Korea(NRF)funded by the Korean Ministry of Education,Science and Technology(NRF-2012R1A1A1013210);by a grant of the Korean Health Technology R&D Project,Ministry of Health,Welfare&Family Affairs,Republic of Korea(A092018).

摘　　要：The aim of this study was to design and evaluate extended-release formulations of a model drug,nicorandil,in order to achieve the desired steady-state plasma concentration of drug in vivo.Simulation was employed to estimate optimum dissolution and absorption rate of nicorandil.The dissolution test was employed using pH 1.2,4.0,6.8 buffer solution,or water,to measure the in vitro release behaviors of nicorandil formulations.A single dose(15 mg)of each formulation was orally administered to four beagle dogs under fasted conditions,and the pharmacokinetic parameters were calculated.The in vitro/in vivo relationship of the extended-release formulation was confirmed using in vitro dissolution profiles and plasma concentrations of drug in beagle dogs.Nicorandil was released completely within 30 min from the immediate-release tablets and released for 24 h from the extended-release tablets.The nicorandil plasma concentration could be modified by adjusting the drug release rate from the extended-release formulation.The release rate of nicorandil was the rate-limiting step in the overall absorption of drug from the extendedrelease formulations.These results highlight the potential of a nicorandil extended-release formulation in the treatment of angina pectoris.

关 键 词：NICORANDIL In vitro In vivo PHARMACOKINETIC EXTENDED-RELEASE 

分 类 号：R96[医药卫生—药理学]