山东化工
山東化工
산동화공
Shandong Chemical Industry
2015年
22期
109-111
,共3页
王洁%孙杨%金刚%于世华%刘治刚
王潔%孫楊%金剛%于世華%劉治剛
왕길%손양%금강%우세화%류치강
碱性调节剂%硝苯地平%固体分散体%体外溶出度
堿性調節劑%硝苯地平%固體分散體%體外溶齣度
감성조절제%초분지평%고체분산체%체외용출도
alkalizer%nifedipine%solid dispersion%in vitro dissolution
目的:采用溶剂-冷冻干燥法制备硝苯地平(nifedipine, NF)速释固体分散体(SD)来提高其体外溶出度,并通过添加碱性调节剂来调节溶出微环境的 pH 值,进一步提高 SD 中药物的溶出速率。方法:以原料药在各辅料水溶液的溶解度及固体分散体的体外溶出度为指标,从聚乙烯吡咯烷酮 K30(PVPK30)、羟丙甲基纤维素(HPMC)、泊洛沙姆407(Poloxamer 407)中筛选最优载体及其比例,并添加适量的碳酸钠( Na2 CO3)来进一步调节溶出速率。结果:当以 PVPK30为载体,Na2 CO3为碱性调节剂,且 NF:PVPK30:Na2 CO3=30mg:150mg:9mg 时,制备的 SD 中药物的溶出速率显著提高,在2h 内累积溶出度百分率可达84%。
目的:採用溶劑-冷凍榦燥法製備硝苯地平(nifedipine, NF)速釋固體分散體(SD)來提高其體外溶齣度,併通過添加堿性調節劑來調節溶齣微環境的 pH 值,進一步提高 SD 中藥物的溶齣速率。方法:以原料藥在各輔料水溶液的溶解度及固體分散體的體外溶齣度為指標,從聚乙烯吡咯烷酮 K30(PVPK30)、羥丙甲基纖維素(HPMC)、泊洛沙姆407(Poloxamer 407)中篩選最優載體及其比例,併添加適量的碳痠鈉( Na2 CO3)來進一步調節溶齣速率。結果:噹以 PVPK30為載體,Na2 CO3為堿性調節劑,且 NF:PVPK30:Na2 CO3=30mg:150mg:9mg 時,製備的 SD 中藥物的溶齣速率顯著提高,在2h 內纍積溶齣度百分率可達84%。
목적:채용용제-냉동간조법제비초분지평(nifedipine, NF)속석고체분산체(SD)래제고기체외용출도,병통과첨가감성조절제래조절용출미배경적 pH 치,진일보제고 SD 중약물적용출속솔。방법:이원료약재각보료수용액적용해도급고체분산체적체외용출도위지표,종취을희필각완동 K30(PVPK30)、간병갑기섬유소(HPMC)、박락사모407(Poloxamer 407)중사선최우재체급기비례,병첨가괄량적탄산납( Na2 CO3)래진일보조절용출속솔。결과:당이 PVPK30위재체,Na2 CO3위감성조절제,차 NF:PVPK30:Na2 CO3=30mg:150mg:9mg 시,제비적 SD 중약물적용출속솔현저제고,재2h 내루적용출도백분솔가체84%。
OBJECTIVE: Prepare the solid dispersions (SD) of nifedipine (NF) by the solvent -freeze drying method to improve the dissolution rate of the drug .The dissolution rate has been further improved by the alkalizer to modifier the PH . METHODS: The solid dispersions of NF have been prepared with polyvinyl pyrrolidone (PVPk30), hydroxypropyl methyl cellulose (HPMC), poloxamer407 and sodium carbonate (Na2 CO3 ), respectively.The optimal carrier were chose from the solubility and dissolution test, then the dissolution rate of the drug has been further improved by the Na 2 CO3 . CONCLUSION: The dissolution rate improved to the 84% during 2hours, when used PVPk30 as the carrier, Na2 CO3 as the alkalizer and the ratio of NF: PVPk30: Na2 CO3 was 30mg: 150mg: 9mg in this solid dispersion system .