帕利哌酮缓释片的制备及体内外评价

发布时间：2019-01-07 16:24

【摘要】：目的:制备帕利哌酮缓释片,并对其在Beagle犬体内的药动学进行评价。方法:首先制备含有帕利哌酮的缓释片芯,再将其通过压制包衣的手段包埋在同样含有帕利哌酮的缓释材料中,压片制得。采用单因素试验和星点设计-效应面法,以自研缓释片和原研制剂(芮达~汶)在pH6.8磷酸盐缓冲液(PBS)中释放行为的相似性为评价指标,优化自制缓释片的处方;以Beagle犬为模型,考察了自制缓释片和原研制剂的体内药动学行为,采用液-质联用(LC-MS/MS)法测定血浆中帕利哌酮浓度,并采用非房室模型计算两制剂的药动学参数。结果:优化后的自制缓释片与原研制剂在pH6.8磷酸盐缓冲液中的释放行为相似(相似因子大于50),自研缓释片与原研制剂的Cmax为(76.79±67.88)ng·mL-1和(76.86±59.80)ng·mL-1,AUC(0→∞)为(1 643.92±1 307.79)ng·mL-1·h和(1 652.33±1 249.45)ng·mL-1·h,提示两制剂相似。结论:通过压制包衣制备帕利哌酮缓释片可实现与原研制剂(芮达~汶)达到一致的目的。
[Abstract]:Aim: to prepare Pariperidone sustained-release tablets and evaluate its pharmacokinetics in Beagle dogs. Methods: firstly, the sustained release tablets containing Pariperidone were prepared, and then the tablets were prepared by pressing and embedding them in the same sustained-release materials containing Pariperidone. Single factor test and star design-effect surface method were used to optimize the formulation of self-made sustained-release tablets based on the similarity of release behavior between the self-developed sustained-release tablets and the original preparation (Ruida Wen) in pH6.8 phosphate buffer (PBS). The pharmacokinetic behavior of sustained release tablets and probiotics in Beagle dogs was investigated. The plasma concentration of peridol was determined by liquid-mass spectrometry (LC-MS/MS), and the pharmacokinetic parameters of the two preparations were calculated by non-atrioventricular model. Results: the release behavior of the optimized sustained-release tablets was similar to that of the original preparation in pH6.8 phosphate buffer (similarity factor > 50). The Cmax of self-made sustained-release tablets and original preparations were (76.79 卤67.88) ng mL-1 and (76.86 卤59.80) ng mL-1,. AUC (0 ~ 鈭，

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