上海医科大学学报
上海醫科大學學報
상해의과대학학보
JOURNAL OF SHANGHAI MEDICAL UNIVERSITY
2000年
3期
178-180
,共3页
金昔陆%陈滨凌%吴卫江%顾铮%江明华%张智波%董纪昌
金昔陸%陳濱凌%吳衛江%顧錚%江明華%張智波%董紀昌
금석륙%진빈릉%오위강%고쟁%강명화%장지파%동기창
磷酸川芎嗪%缓释骨架片%羟丙甲纤维素%生物利用度
燐痠川芎嗪%緩釋骨架片%羥丙甲纖維素%生物利用度
린산천궁진%완석골가편%간병갑섬유소%생물이용도
tetramethylpyrazine phosphate%sustained-release tablet%hydroxypropylmethylcellulose%bioavailability
目的 以羟丙甲纤维素(HPMC)为骨架材料制备持续释药12h的磷酸川芎嗪缓释片。方法 分别采用中国药典1995年版溶出度测定法第2法及高效液相色谱法测定缓释片的体外释放度及兔体内生物利用度。结果 缓释片体外1h释药20%左右,12h释药85%以上,12 h内释药平稳,释药曲线符合Higuchi方程,体外释药受HPMC类型、黏度、用量影响较大。缓释片与市售常释片相比,兔体内峰浓度降低,达峰时间延迟,平均滞留时间延长,吸收程度生物等效。结论 缓释片体内外缓释效果良好,并具有良好的体内外相关性。
目的 以羥丙甲纖維素(HPMC)為骨架材料製備持續釋藥12h的燐痠川芎嗪緩釋片。方法 分彆採用中國藥典1995年版溶齣度測定法第2法及高效液相色譜法測定緩釋片的體外釋放度及兔體內生物利用度。結果 緩釋片體外1h釋藥20%左右,12h釋藥85%以上,12 h內釋藥平穩,釋藥麯線符閤Higuchi方程,體外釋藥受HPMC類型、黏度、用量影響較大。緩釋片與市售常釋片相比,兔體內峰濃度降低,達峰時間延遲,平均滯留時間延長,吸收程度生物等效。結論 緩釋片體內外緩釋效果良好,併具有良好的體內外相關性。
목적 이간병갑섬유소(HPMC)위골가재료제비지속석약12h적린산천궁진완석편。방법 분별채용중국약전1995년판용출도측정법제2법급고효액상색보법측정완석편적체외석방도급토체내생물이용도。결과 완석편체외1h석약20%좌우,12h석약85%이상,12 h내석약평은,석약곡선부합Higuchi방정,체외석약수HPMC류형、점도、용량영향교대。완석편여시수상석편상비,토체내봉농도강저,체봉시간연지,평균체류시간연장,흡수정도생물등효。결론 완석편체내외완석효과량호,병구유량호적체내외상관성。
Purpose To prepare the sustained-release tablet of tetramethylpyrazine phosphate with hydroxypropylmethylcelluose(HPMC) as matrix material. Methods The paddle method and the HPLC method were erspectively used determined the cumulative drug released in vitro and the serum concentration in vivo. Results The cumulative drug released in the first hour was about 20%, while in 12 hours it was above 85%. Drug release behavior can be best described by Higuchi equation, and the release rate decreased as the viscosity and/or the amount of HPMC increased. Compared with the market tablet on the rabbits, the sustained release tablet had the decreased peak concentration (P < 0.05 ); the prolonged peak time and mean residence time (P< 0.05). Conclusions The matrix tablet was a good sustained-release dosage form and it had a good in vitro-in vivo correlation.