去铁氧胺自纳米乳化给药系统(SNEDDs)的组分分配

Alaa Alghananim, Y. Özalp, B. Mesut, Y. Özsoy, S. Güngör
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摘要

铁asirox (DFR)是一种口服三叉状铁螯合剂,可有效降低输铁依赖性贫血患者体内铁含量[1]。它是一种高度亲脂分子(log P: 3.52),被列为BCS II类原料药[2]。自纳米乳化给药系统(snedd)是由药物、油和亲水表面活性剂以及助表面活性剂/助溶剂组成的各向同性混合物。近年来,snedd在提高亲脂分子的溶解度从而提高其口服生物利用度方面受到越来越多的关注。在SNEDDs配方中选择适当的成分对于开发成功的配方至关重要。本工作的目的是选择和筛选合适的组分,以优化DFR负载的snedd配方。为此,制备了不同的snedd配方,并构建了伪三元相图。2. 材料与方法
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Assigning the components of a Self-Nanoemulsifying Drug Delivery System (SNEDDs) of Deferasirox
Deferasirox (DFR) is an oral tridentate iron chelator effective for reduction of body iron in ironoverloaded patients with transfusion-dependent anemias [1]. It is a highly lipophilic molecule (log P: 3.52) which is classified as BCS Class II drug substance [2]. Self-nanoemulsifying drug delivery systems (SNEDDs) are isotropic mixtures of drug, oil and hydrophilic surfactants and co-surfactant/co-solvents. In recent years, SNEDDs gained more attention in the solubility enhancement of lipophilic molecule hence enhancing their oral bioavailability. The selection of appropriate components in the SNEDDs formulation is crucial for development of a successful formulation. The goal of this work is to select and to screen appropriate components for the optimization of DFR loaded SNEDDs formulations. In this respect, different SNEDDs formulations were prepared and pseudo-ternary phase diagrams were constructed. 2. Materials and Methods
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