在体外/体外对应两种延长释放型西洛斯塔的配方
Kyoung Ah Min1, Na Young Kim2,3, Min Jeong Jin2,3
1College of Pharmacy and Inje Institute of Pharmaceutical Sciences and Research, Inje University, 197 Injero, Gimhae 50834, Gyeongnam, Republic of Korea.
与Cilostan® CR 200 mg片相比,Pletaal® SR 200 mg囊显示出更优异的药物释放和药物动力学特征. 这表明囊配方的体内性能和治疗潜力更好.
科学领域:
- 药理学 药理学是指药理学的学科.
- 制药科学 制药科学
- 药物输送系统 药物输送系统
背景情况:
- 延长释放剂型的目的是提供持续的药物水平.
- 了解体外-体内相关性对于剂型开发至关重要.
- 奇洛斯塔 (cilostazol) 用于间歇性听症.
研究的目的:
- 为了将体外药物释放与两种延长释放西洛斯塔配方体体内的体内药理学相关联.
- 为了比较Pletaal® SR 200毫克囊和Cilostan® CR 200毫克片的性能.
- 为了评估食与禁食状态对西洛斯塔的药理动力学的影响.
主要方法:
- 在实验室药物释放研究中,在模拟的胃介质中使用USP和篮子装置.
- 使用单剂量,两期交叉设计在 beagle 狗体内生物药理学评估.
- 在食和禁食条件下分析血度,Cmax,AUC0-t和AUC0-inf.
主要成果:
- 在体外,Pletaal® SR 200 mg囊的药物释放率明显高于Cilostan® CR 200 mg片.
- 在体内研究显示,与禁食状态相比,在养状态下,基洛斯塔的血度和AUC值更高.
- 与Cilostan® CR 200 mg片相比,Pletaal® SR 200 mg囊的Cmax高出2.53倍,AUC0-t高出2.89倍,AUC0-inf高出2.87倍.
结论:
- 与Cilostan® CR 200 mg片相比,Pletaal® SR 200 mg囊在体外释放特征和体内药物动力学性能优越.
- 食状态增强了基洛斯塔的吸收,影响了其药理动力学特征.
- 在体外和体内相关性支持Pletaal® SR 200 mg囊的增强治疗潜力.
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