盐酸帕罗西汀肠溶缓释片的研制及体内外评价

发布时间：2018-05-19 17:56

  本文选题：盐酸帕罗西汀 + 肠溶缓释片　； 参考：《中国医药工业杂志》2017年06期

【摘要】：采用PVP K30的水溶液为黏合剂,应用流化床一步制粒技术,分别制备含药层颗粒与基座层颗粒,再压制双层缓释片,最后对素片进行肠溶包衣得盐酸帕罗西汀肠溶缓释片。以参比制剂(Paxil CR)为对照,分别考察在pH 1.0盐酸、pH 7.5 Tris盐缓冲液、pH 6.0磷酸盐缓冲液和水中的释放行为,以相似因子(f_2)评判二者体外释放行为的相似性。在4种介质中二者释放行为均相似的前提下(f_250),建立了Beagle犬体内分析方法,进一步探究自制肠溶缓释片与参比制剂的体内药动学特征,经过双周期交叉口服给予Beagle犬盐酸帕罗西汀肠溶缓释片后,自制品的部分药代参数如下:t_(max)(5.38±3.25)h,c_(max)(5.57±3.81)ng/ml,t_(1/2)(3.59±2.31)h,AUC_0→t(38.34±30.07)ng·ml~(-1)·h,MRT_0→∞(7.51±2.97)h;参比制剂的参数如下:t_(max)(6.75±7.15)h,c_(max)(5.84±6.74)ng/ml,t_(1/2)(3.94±2.67)h,AUC_0→t(35.48±39.45)ng·ml~(-1)·h,MRT_0→∞(7.65±3.64)h,自制品的c_(max)值为参比制剂相应参数的121.90%;二者主要药代动力学参数t_(max)、c_(max)、AUC_0→t经对数转换后无统计学差异(P0.05),自制肠溶缓释片的相对生物利用度为125.13%(几何均值)。
[Abstract]:Using aqueous solution of PVP K30 as binder, the pellets of drug-containing layer and base layer were prepared by fluidized bed granulation technology, and then double-layer sustained release tablets were pressed. Finally, paroxetine hydrochloride enteric-soluble sustained-release tablets were coated with enteric-coated tablets. The release behavior of Paxil CR1 in pH 1. 0 Tris salt buffer pH 6. 0 phosphate buffer and water was investigated, and the similarity of in vitro release behavior was evaluated by similarity factor. Based on the similar release behavior of both of the four mediums, a method for the in vivo analysis of Beagle dogs was established, and the pharmacokinetic characteristics of enteric sustained-release tablets and reference preparations were further investigated. After Beagle dog was given paroxetine hydrochloride enteric-soluble sustained-release tablets, 鑷�鍒跺搧鐨勯儴鍒嗚嵂浠ｅ弬鏁板�備笅:t_(max)(5.38卤3.25)h,c_(max)(5.57卤3.81)ng/ml,t_(1/2)(3.59卤2.31)h,AUC_0鈫抰(38.34卤30.07)ng路ml~(-1)路h,MRT_0鈫掆垶(7.51卤2.97)h;鍙傛瘮鍒跺墏鐨勫弬鏁板�備福�

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