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首页> 外文期刊>Applied Magnetic Resonance >Real-Time in Vitro Drug Dissolution Studies of Tablets Using Volume-Localized NMR (MRS)
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Real-Time in Vitro Drug Dissolution Studies of Tablets Using Volume-Localized NMR (MRS)

机译：使用体积局部核磁共振（MRS）进行片剂的实时体外药物溶解研究

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An approach to measure in vitro drug dissolution rates employing spatially resolved nuclear magnetic resonance (NMR) is reported, as a complement to standard United States Pharmacopeia protocols. Measurements are performed under conditions that mimic the physiological (pH 1, temperature 37° C). In order to register realistic dissolution rates, the sample is stirred in the magnetic field, employing a setup that is described. While the stirrer in the sample cell does degrade spectral resolution even in volume-localized mode, it proves possible nevertheless to acquire ‘high resolution’ information. Measurements are performed employing ‘point resolved spectroscopy’ (PRESS) by tracking drug concentration in a selected voxel in the dissolution medium as a function of time. The dissolution of the tablets in vitro follows first-order kinetics under the non-sink conditions of these experiments, the measured rate constants reflecting characteristic differences in dissolution rates of different formulations. We supplement this study with diffusion-weighted imaging of water ingress into the tablets, confirming the trends.
机译：报道了一种使用空间分辨核磁共振（NMR）测量体外药物溶解速率的方法，作为对美国药典标准规程的补充。在模拟生理条件（pH 1，温度37°C）的条件下进行测量。为了记录实际的溶出度，使用所述装置在磁场中搅拌样品。尽管样品池中的搅拌器即使在体积定位模式下也确实会降低光谱分辨率，但事实证明仍然有可能获得“高分辨率”信息。通过跟踪溶出介质中所选体素中药物浓度随时间的变化，采用“点分辨光谱法”（PRESS）进行测量。在这些实验的非沉没条件下，片剂的体外溶出遵循一级动力学，测得的速率常数反映了不同制剂溶出速率的特征差异。我们用扩散加权成像的水进入片剂补充了这项研究，确认了趋势。

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