摘要
双氯灭痛（ＤＣ－Ｎａ）控释小丸的制备，成丸百分率受种粒中乳糖／淀粉比例、粘合剂溶液粘度及种粒在包衣锅中滚动时间的影响；小丸的园整度与粘合剂溶液的表面张力显著相关；包衣液组成及浓度，小丸大小分布范围对包衣中粘连影响较大。６名健康自愿者多剂量口服ＤＣ－Ｎａ控释小丸（ＣＲＰ）及普通片（ＣＴ），比较最低血浆浓度，说明ｄ３已达稳态。稳态时两者之间血浆药物浓度波动指数（ＦＩ）存在显著差异（Ｐ＜０．０５），而稳态时一个给药间隔内血浆药物浓度一时间曲线下的面积（ＡＵＣ）无显著差异（Ｐ＞０．０５），相对生物利用度为８６％。
The yield of pellets obtained in preparing diclofenac sedium( DC-Na)controlledrelease pellets was affected by the lactose/starch ratio of the feed granules,viscosity of the bindingsolution and residence time in the rolling pot.The pellet shape was found to be correlated with surfacetension of the binding solution,The concentration and composition of the coating solution and pelletsize distribution were responsible for the agglutination in coating. The controlled release pellets(CRP)and commercial tablets(CT)of DC Na were administrated orally to healthy volunteers by multiple-dose,The steady-state condition, based on trough plasma concentration on day 3～5,was achieved onday 3;A great difference in plasma drug concentration fluctuation index(FI) between CRP(0.476±0. 0484)and CT(0. 935±0. 092)was observed(P<0.05)during steady-state.The area underthe plasma drug concentration-time curve for a 0～12 h interval(AUC)on day 5 of CRP(6. 493±0. 4169μg·h· ml-1) and CT(7.551±0. 4745 μg·h· ml-1) was shown to be not significantlydifferent(P>0.05).The relative bioavailabilitv in the human was about 86%.
出处
《药学学报》
CAS
CSCD
北大核心
1996年第3期209-213,共5页
Acta Pharmaceutica Sinica
