Solid-State Insight Into the Action of a Pharmaceutical Solvate: Structural, Thermal, and Dissolution Analysis of Indinavir Sulfate Ethanolate.

Chengcheng Zhang, Kortney M Kersten, Jeff W Kampf, Adam J Matzger

Journal of pharmaceutical sciences 2018 Oct

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The crystal structure of indinavir sulfate, a pharmaceutical administered as an ethanol solvate, is presented, revealing a unique channel/ionic solvate structure to be characteristic of the compound. The properties of the material with regard to thermal treatment and water adsorption follow closely from the structure. The in situ amorphization of the pharmaceutical upon contacting liquid water is observed and highlights the unique dissolution enhancement of marketing the crystalline solvate dosage. Through survey of published crystal structures, an ambiguous sulfate/bisulfate ionization state is also observed in the crystal, which challenges the general understanding of the pharmaceutical. This study provides a solid-state insight into the function of a special multicomponent crystalline pharmaceutical form. Copyright © 2018 American Pharmacists Association®. Published by Elsevier Inc. All rights reserved.

Citation

Chengcheng Zhang, Kortney M Kersten, Jeff W Kampf, Adam J Matzger. Solid-State Insight Into the Action of a Pharmaceutical Solvate: Structural, Thermal, and Dissolution Analysis of Indinavir Sulfate Ethanolate. Journal of pharmaceutical sciences. 2018 Oct;107(10):2731-2734