Laboratory of Galenic Pharmacy, Faculty of Pharmacy of Monastir, University of Monastir, 5000 Monastir, Tunisia.
J Pharm Pharm Sci. 2011;14(1):117-27. doi: 10.18433/j3gc7r.
Oral drug administration remains the most common and most convenient way used in clinical therapy. The availability of a simple, rapid, economic and reproducible in vitro method to assess the rate, extent and mechanism of intestinal drug absorption is a very helpful tool. The purpose of this study was to compare the performance of Sartorius SM 16750 Absorption Simulator apparatus to Everted Gut Sac (EGS) technique in terms of predicting drug permeability.
Permeation studies across these two in vitro models were performed with six drugs selected across the Biopharmaceutics Classification System (BCS) categories: tramadol (class I of BCS), doxycycline (class I of BCS), diclofenac (class II of BCS), clopidogrel (class II of BCS), metformin (class III of BCS) and chlorothiazide (class IV of BCS).
Apparent permeability coefficient (Papp) and diffusion profiles obtained with EGS and Sartorius SM 16750 apparatus were similar for diclofenac and metformin, whereas, we noticed significant differences (p ≤ 0.05), for tramadol, doxycycline, clopidogrel and chlorothiazide.
Compared to Everted Gut Sac model, Sartorius SM 16750 absorption simulator apparatus seems to have limited application for the assessment of intestinal drug absorption since it does not take into consideration the involvement of others processes than the passive transcellular pathway as mechanism of drug absorption.
口服给药仍然是临床治疗中最常用和最方便的方式。拥有一种简单、快速、经济且可重现的体外方法来评估肠道药物吸收的速率、程度和机制是非常有帮助的。本研究的目的是比较 Sartorius SM 16750 吸收模拟器设备与外翻肠囊 (EGS) 技术在预测药物渗透性方面的性能。
通过体外模型进行了六种药物的渗透研究，这些药物选自生物药剂学分类系统 (BCS) 类别：曲马多（BCS 类别 I）、多西环素（BCS 类别 I）、双氯芬酸（BCS 类别 II）、氯吡格雷（BCS 类别 II）、二甲双胍（BCS 类别 III）和氯噻嗪（BCS 类别 IV）。
EGS 和 Sartorius SM 16750 仪器获得的表观渗透系数 (Papp) 和扩散曲线在双氯芬酸和二甲双胍方面相似，而我们注意到曲马多、多西环素、氯吡格雷和氯噻嗪存在显著差异 (p ≤ 0.05)。
与外翻肠囊模型相比，Sartorius SM 16750 吸收模拟器设备似乎对评估肠道药物吸收的应用有限，因为它没有考虑到除被动跨细胞途径以外的其他过程作为药物吸收的机制。
