Laboratory of Pharmaceutical Technology, School of Pharmacy and Pharmaceutical Sciences, University of Toyama, 2630 Sugitani, Toyama-shi, Toyama 930-0194, Japan.
Laboratory of Pharmaceutical Technology, School of Pharmacy and Pharmaceutical Sciences, University of Toyama, 2630 Sugitani, Toyama-shi, Toyama 930-0194, Japan; Formulation Development Department, Development & Planning Division, Nichi-Iko Pharmaceutical Co., Ltd., 205-1 Shimoumezawa, Namerikawa-shi, Toyama 936-0857, Japan.
J Pharm Sci. 2024 Mar;113(3):680-687. doi: 10.1016/j.xphs.2023.08.021. Epub 2023 Sep 1.
This study examined the usefulness of H T relaxation measurements for evaluating the homogeneity of amorphous solid dispersion (ASD). Indomethacin and polyvinylpyrrolidone were used to prepare two kinds of ASDs. One was inhomogeneous ASD (ASD) prepared by a melt-quenching method, and the other was homogeneous ASD (ASD) prepared by a solvent evaporation method. The T relaxation was measured by the time-domain NMR (TD-NMR) technique using a low-field NMR system. Curve-fitting analysis of T relaxation plots was conducted using the Akaike information criterion. This fitting analysis revealed that the T relaxation of ASD and ASD was biphasic and monophasic, respectively. ASD and ASD were inhomogeneous and homogeneous on a nanometer scale, respectively, considering the spin diffusion of H nuclei. These T results were consistent with the Raman mapping of ASDs. From the fitting analysis of H T relaxation, we conclude that TD-NMR is a promising technique for evaluating ASD homogeneity.
本研究考察了 H T 弛豫测量在评估无定形固体分散体 (ASD) 均匀性中的有用性。使用吲哚美辛和聚乙烯吡咯烷酮制备了两种 ASD。一种是由熔融淬火法制备的不均匀 ASD（ASD），另一种是由溶剂蒸发法制备的均匀 ASD（ASD）。T 弛豫通过使用低场 NMR 系统的时域 NMR（TD-NMR）技术进行测量。使用赤池信息量准则对 T 弛豫曲线进行拟合分析。该拟合分析表明，ASD 和 ASD 的 T 弛豫分别为两相和单相。考虑到 H 核的自旋扩散，ASD 和 ASD 在纳米尺度上分别是不均匀和均匀的。这些 T 结果与 ASDs 的拉曼映射一致。从 H T 弛豫的拟合分析中，我们得出结论，TD-NMR 是评估 ASD 均匀性的一种很有前途的技术。
