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首页> 美国卫生研究院文献>Springer Open Choice >Surface Dissolution UV Imaging for Investigation of Dissolution of Poorly Soluble Drugs and Their Amorphous Formulation
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Surface Dissolution UV Imaging for Investigation of Dissolution of Poorly Soluble Drugs and Their Amorphous Formulation

机译：表面溶解紫外成像技术用于研究难溶性药物及其无定形制剂的溶解度

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The aim of this study is to investigate the dissolution properties of poorly soluble drugs from their pure form and their amorphous formulation under physiological relevant conditions for oral administration based on surface dissolution ultraviolet (UV) imaging. Dissolution of two poorly soluble drugs (cefuroxime axetil and itraconazole) and their amorphous formulations (Zinnat® and Sporanox®) was studied with the Sirius Surface Dissolution Imager (SDI). Media simulating the fasted state conditions (compendial and biorelevant) with sequential media/flow rate change were used. The dissolution mechanism of cefuroxime axetil in simulated gastric fluid (SGF), fasted state simulated gastric fluid (FaSSGF) and simulated intestinal fluid (SIF) is predominantly swelling as opposed to the convective flow in fasted state simulated intestinal fluid (FaSSIF-V1), attributed to the effect of mixed micelles. For the itraconazole compact in biorelevant media, a clear upward diffusion of the dissolved itraconazole into the bulk buffer solution is observed. Dissolution of itraconazole from the Sporanox® compact is affected by the polyethylene glycol (PEG) gelling layer and hydroxypropyl methylcellulose (HPMC) matrix, and a steady diffusional dissolution pattern is revealed. A visual representation and a quantitative assessment of dissolution properties of poorly soluble compounds and their amorphous formulation can be obtained with the use of surface dissolution imaging under in vivo relevant conditions.
机译：这项研究的目的是基于表面溶解紫外（UV）成像技术，研究难溶性药物的纯净形式和无定形制剂在生理相关条件下的口服口服溶出特性。使用Sirius表面溶出成像仪（SDI）研究了两种难溶药物（头孢呋辛酯和伊曲康唑）及其无定形制剂（Zinnat ®和Sporanox ®）的溶出度。使用了模拟禁食状态条件（肠道菌群和生物相关）以及连续的培养基/流速变化的培养基。头孢呋辛酯在模拟胃液（SGF），禁食状态模拟胃液（FaSSGF）和模拟肠液（SIF）中的溶解机理主要是溶胀，与禁食状态模拟肠液（FaSSIF-V1）中的对流流动相反，归因于混合胶束的作用。对于在生物相关介质中的伊曲康唑压块，观察到溶解的伊曲康唑向本体缓冲液的明显向上扩散。伊曲康唑从Sporanox ®压块中的溶解受聚乙二醇（PEG）胶凝层和羟丙基甲基纤维素（HPMC）基质的影响，显示出稳定的扩散溶解模式。可以通过在体内相关条件下使用表面溶出显像来获得弱溶性化合物及其无定形制剂溶出特性的视觉表示和定量评估。

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