Literature DB >> 29960024

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

Chengcheng Zhang1, Kortney M Kersten1, Jeff W Kampf1, Adam J Matzger2.   

Abstract

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.

Entities:  

Keywords:  amorphism; crystal structure; desolvation; salts; solvates

Mesh:

Substances:

Year:  2018        PMID: 29960024      PMCID: PMC6170162          DOI: 10.1016/j.xphs.2018.06.020

Source DB:  PubMed          Journal:  J Pharm Sci        ISSN: 0022-3549            Impact factor:   3.534


  8 in total

1.  The Cambridge Structural Database: a quarter of a million crystal structures and rising.

Authors:  Frank H Allen
Journal:  Acta Crystallogr B       Date:  2002-05-29

2.  The hydrogen bond in the solid state.

Authors:  Thomas Steiner
Journal:  Angew Chem Int Ed Engl       Date:  2002-01-04       Impact factor: 15.336

3.  Applications of thermal analysis in the pharmaceutical industry.

Authors:  D Giron
Journal:  J Pharm Biomed Anal       Date:  1986       Impact factor: 3.935

4.  The salt-cocrystal continuum: the influence of crystal structure on ionization state.

Authors:  Scott L Childs; G Patrick Stahly; Aeri Park
Journal:  Mol Pharm       Date:  2007-04-27       Impact factor: 4.939

5.  Three isostructural solvates of finasteride and their solid-state characterization.

Authors:  Nate Schultheiss; Jared P Smit; Jason A Hanko
Journal:  Eur J Pharm Sci       Date:  2009-10-03       Impact factor: 4.384

Review 6.  The integration of medicinal chemistry, drug metabolism, and pharmaceutical research and development in drug discovery and development. The story of Crixivan, an HIV protease inhibitor.

Authors:  J H Lin; D Ostovic; J P Vacca
Journal:  Pharm Biotechnol       Date:  1998

7.  Solid-state acid-base interactions in complexes of heterocyclic bases with dicarboxylic acids: crystallography, hydrogen bond analysis, and 15N NMR spectroscopy.

Authors:  Z Jane Li; Yuriy Abramov; Jon Bordner; Jason Leonard; Ales Medek; Andrew V Trask
Journal:  J Am Chem Soc       Date:  2006-06-28       Impact factor: 15.419

8.  Characterisation and evaluation of pharmaceutical solvates of Atorvastatin calcium by thermoanalytical and spectroscopic studies.

Authors:  Renu Chadha; Astha Kuhad; Poonam Arora; Shyam Kishor
Journal:  Chem Cent J       Date:  2012-10-06       Impact factor: 4.215

  8 in total
  1 in total

1.  Far-Infrared Spectroscopy as a Probe for Polymorph Discrimination.

Authors:  Kuthuru Suresh; Jeffrey S Ashe; Adam J Matzger
Journal:  J Pharm Sci       Date:  2018-12-30       Impact factor: 3.534

  1 in total

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