本文選題：鹽酸帕羅西汀 + 腸溶緩釋片�。� 參考：《中國醫(yī)藥工業(yè)雜志》2017年06期

【摘要】：采用PVP K30的水溶液為黏合劑,應(yīng)用流化床一步制粒技術(shù),分別制備含藥層顆粒與基座層顆粒,再壓制雙層緩釋片,最后對素片進(jìn)行腸溶包衣得鹽酸帕羅西汀腸溶緩釋片。以參比制劑(Paxil CR)為對照,分別考察在pH 1.0鹽酸、pH 7.5 Tris鹽緩沖液、pH 6.0磷酸鹽緩沖液和水中的釋放行為,以相似因子(f_2)評判二者體外釋放行為的相似性。在4種介質(zhì)中二者釋放行為均相似的前提下(f_250),建立了Beagle犬體內(nèi)分析方法,進(jìn)一步探究自制腸溶緩釋片與參比制劑的體內(nèi)藥動學(xué)特征,經(jīng)過雙周期交叉口服給予Beagle犬鹽酸帕羅西汀腸溶緩釋片后,自制品的部分藥代參數(shù)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;參比制劑的參數(shù)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)值為參比制劑相應(yīng)參數(shù)的121.90%;二者主要藥代動力學(xué)參數(shù)t_(max)、c_(max)、AUC_0→t經(jīng)對數(shù)轉(zhuǎn)換后無統(tǒng)計學(xué)差異(P0.05),自制腸溶緩釋片的相對生物利用度為125.13%(幾何均值)。
[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埗鍝佺殑閮ㄥ垎鑽唬鍙傛暟濡備笅:t_(max)(5.38鹵3.25)h,c_(max)(5.57鹵3.81)ng/ml,t_(1/2)(3.59鹵2.31)h,AUC_0鈫抰(38.34鹵30.07)ng路ml~(-1)路h,MRT_0鈫掆垶(7.51鹵2.97)h;鍙傛瘮鍒跺墏鐨勫弬鏁板涓，

本文編號：1911086