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通过电喷雾和溶剂蒸发制备的布洛芬-异烟酰胺共晶的固态表征。

Solid-state characterization of ibuprofen-isonicotinamide cocrystals prepared by electrospraying and solvent evaporation.

机构信息

Department of Pharmaceutics, School of Pharmacy, Urmia University of Medical Sciences, Urmia, Iran.

Pharmaceutical Analysis Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.

出版信息

Ther Deliv. 2023 Feb;14(2):121-138. doi: 10.4155/tde-2022-0072. Epub 2023 Apr 26.

Abstract

Electrospraying (ELS) was used to prepare micronized ibuprofen-isonicotinamide cocrystal (IBU-INA-ELS) and its properties were compared with the solvent evaporated cocrystal (IBU-INA-SE). Solid-state characterization of crystalline phase, production yield, particle size, powder flow, wettability, solution mediated phase transformation (SMPT), and dissolution rate were measured. The ELS produced phase pure particles of IBU-INA with a size of 1.46 μm and yield of 72.3%. This cocrystal improved the intrinsic dissolution rate and powder dissolution rate of IBU by 3.6- and 1.7-fold, respectively. Our experiments showed that the dissolution of IBU-INA was affected by particle size, solubility, SMPT and wettability. ELS produced micronized cocrystals for improving dissolution of ibuprofen with a high yield in a single step and mild conditions.

摘要

电喷雾(ELS)被用于制备微米级布洛芬-异烟酰胺共晶(IBU-INA-ELS),并将其性质与溶剂蒸发共晶(IBU-INA-SE)进行了比较。对结晶相、产率、粒径、粉末流动、润湿性、溶液介导的相转变(SMPT)和溶解速率进行了固态特性表征。ELS 生产出了尺寸为 1.46μm、产率为 72.3%的 IBU-INA 纯相颗粒。该共晶将 IBU 的固有溶解速率和粉末溶解速率分别提高了 3.6 倍和 1.7 倍。我们的实验表明,IBU-INA 的溶解受到粒径、溶解度、SMPT 和润湿性的影响。ELS 一步法、温和条件下高产率制备微米级共晶以提高布洛芬的溶解速率。

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