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无溶剂球磨过程中从 α-甘氨酸合成 γ 相和无定形固体分散体的甘氨酸。

Synthesis of γ Phase and Amorphous Solid Dispersion of Glycine from α-Glycine During the Solvent-Free Ball Milling Process.

机构信息

School of Resources and Chemical Engineering, Sanming University, Sanming 365004, Fujian, China.

School of Resources and Chemical Engineering, Sanming University, Sanming 365004, Fujian, China.

出版信息

J Pharm Sci. 2021 Sep;110(9):3171-3175. doi: 10.1016/j.xphs.2021.06.023. Epub 2021 Jun 14.

Abstract

Nano α-glycine crystals, γ-glycine crystals, and amorphous solid dispersion (ASD) of glycine were prepared through solvent-free ball milling of commercial α-glycine. The solid-state polymorph conversion of glycine from α to γ was completely realized by ball milling with 0.2 wt.% NaCl for 1 h or by ball milling with 0.02 wt.% NaCl for 1 h with subsequent storage for one week. The ASD of glycine was prepared by ball milling α-glycine with an equal amount of CaCl for 1 h. We studied the effect of inorganic salt types and their concentrations on the extent of polymorph conversion and amorphization of glycine in our experiments. This solvent-free ball milling method could be used for the synthesis of polymorphs and amorphous phase of drugs and other organic materials.

摘要

纳米 α-甘氨酸晶体、γ-甘氨酸晶体和甘氨酸无定形固体分散体(ASD)是通过商业 α-甘氨酸的无溶剂球磨制备的。通过 0.2wt.%NaCl 球磨 1 小时或 0.02wt.%NaCl 球磨 1 小时并随后储存一周,甘氨酸的固相反转化从 α 完全转化为 γ。甘氨酸的 ASD 是通过将 α-甘氨酸与等摩尔量的 CaCl 球磨 1 小时制备的。我们研究了无机盐类型及其浓度对甘氨酸在实验中多晶型转化和非晶化程度的影响。这种无溶剂球磨方法可用于合成药物和其他有机材料的多晶型物和非晶相。

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