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不同阿司匹林制剂的体内-体外相关性

In vivo-in vitro correlations with various aspirin formulations.

作者信息

Alcorn G J, Lücker P W, Procaccini R L, Ritschel W A

机构信息

Division of Pharmaceutics and Drug Delivery Systems, University of Cincinnati, OH.

出版信息

Methods Find Exp Clin Pharmacol. 1987 Nov;9(11):761-7.

PMID:3448453
Abstract

In vivo evaluation of gastric irritation as determined by gastric transmural potential difference (GPD) and in vitro characterization of four formulations have been made. The four formulations were: (A) highly buffered, (B) cytoprotective, (C) microencapsulated and (D) a plain tablet. The GPD results showed C to be much less irritating than A or D, and slightly less-irritating than B. The release from all formulations was well represented by dissolution efficiency (DE%) and mean time of dissolution. When correlation coefficients were calculated, significant relationships were found between DE% and the GPD parameters area under the baseline (AUB) and the Reiz Index (RI), and between the mean time of dissolution and the GPD parameters AUB, mean potential drop (MD) and RI.

摘要

已通过胃跨壁电位差(GPD)对胃刺激性进行了体内评估,并对四种制剂进行了体外特性分析。这四种制剂分别为:(A)高缓冲型、(B)细胞保护型、(C)微囊化型和(D)普通片剂。GPD结果显示,C的刺激性远小于A或D,且比B的刺激性略小。所有制剂的释放情况均可用溶出效率(DE%)和平均溶出时间很好地表示。计算相关系数时,发现DE%与GPD参数基线以下面积(AUB)和刺激指数(RI)之间,以及平均溶出时间与GPD参数AUB、平均电位降(MD)和RI之间存在显著关系。

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