PDF(Pubmed)
Abstract：
This study aims to evaluate and determine the correlation between in vitro release and in vivo pharmacokinetics of two extended-release dosage forms of Cilostazol. In vitro release profiles for two dosage forms, tablet and capsule, were analyzed under physiologically mimicked medium conditions using the paddle and basket USP release apparatus. A single-dose, two-period crossover study design in beagle dogs was applied for the pharmacokinetic study. The fed and fast effects were considered for evaluation. Pseudo gastric release medium transfer setup study from pH 1.2 to pH 6.8 (+0.5% SLS) and pH 1.2 to pH 6.8 (+1.0% SLS) demonstrated that Pletaal® SR 200 mg capsules have higher drug release rates than Cilostan® CR 200 mg tablets. Similarly, in vivo study showed Cilostazol concentration in plasma and AUC was lower under the fast state than the fed state. The ratio of least squared geometric mean values, Cmax, AUC0-t, and AUC0-inf of Cilostazol were 2.53-fold, 2.89-fold, and 2.87-fold higher for Pletaal® SR 200 mg capsules compared with Cilostan® CR 200 mg tablets, respectively. Correlation of in vitro/in vivo data indicated that Pletal® SR 200 mg capsules have better release and pharmacodynamic effect than Cilostan® CR 200 mg tablets.
摘要：
本研究旨在评估和确定两种西洛他唑缓释剂型的体外释放与体内药代动力学之间的相关性。两种剂型的体外释放曲线，片剂和胶囊，在生理模拟的培养基条件下使用桨和篮式USP释放装置进行分析。单剂量,本研究采用比格犬的两期交叉研究设计进行药代动力学研究.考虑了饲喂和快速效果进行评估。从pH1.2到pH6.8(+0.5%SLS)和pH1.2到pH6.8(+1.0%SLS)的伪胃释放介质转移设置研究表明,Pletaal®SR200mg胶囊具有比Cilostan®CR200mg片剂更高的药物释放速率。同样，体内研究显示，快速状态下血浆中西洛他唑的浓度和AUC低于进食状态。最小二乘几何平均值之比，Cmax,AUC0-t,西洛他唑的AUC0-inf为2.53倍，2.89折，与Cilostan®CR200mg片剂相比，Pletaal®SR200mg胶囊高2.87倍，分别。体外/体内数据的相关性表明，Pletal®SR200mg胶囊比Cilostan®CR200mg片剂具有更好的释放和药效学效果。
