The dissolution and solid-state behaviours of coground ibuprofen-glucosamine HCl

Hiba Al-Hamidi, Kofi Asare-Addo, Sandip Desai, Mike Kitson, Ali Nokhodchi

Research output: Contribution to journalArticle

Abstract

The cogrinding technique is one of most effective methods for improving the dissolution of poorly water-soluble drugs and it is superior to other approaches from an economical as well as an environmental standpoint, as the technique does not require any toxic organic solvents. Present work explores the role of d-glucosamine HCl (GL) as a potential excipient to improve dissolution of a low melting point drug, ibuprofen (Ibu), using physical mixtures and coground formulations. The dissolution of the poorly soluble drug has been improved by changing the ratio of Ibu:GL and also grinding time. The results also showed that although GL can enhance the solubility of Ibu, it also reduces pH around the Ibu particles which led to poor dissolution performance when the concentration of GL is high. The effect of GL on the solubility of Ibu could be misleading if the pH of the final solution was not measured. Grinding reduced the particle size of GL significantly but in case of Ibu it was less effective. Solid state analysis (XRPD, DSC, and FT-IR) showed that ibuprofen is stable under grinding conditions, but the presence of high concentration of GL in samples subjected to high grinding times caused changes in FT-IR spectrum of Ibu which could be due to intermolecular hydrogen bond or esterification between the carboxylic acid group in the ibuprofen and hydroxyl group in the GL.

Original languageEnglish
Pages (from-to)1682-1692
Number of pages11
JournalDrug Development and Industrial Pharmacy
Volume41
Issue number10
DOIs
Publication statusPublished - 2015

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Ibuprofen
Glucosamine
Dissolution
Solubility
Pharmaceutical Preparations
Esterification
Excipients
Poisons
Carboxylic Acids
Particle Size
Hydroxyl Radical
Organic solvents
Freezing
Melting point
Hydrogen
Hydrogen bonds
Particle size
Water

Cite this

Al-Hamidi, Hiba ; Asare-Addo, Kofi ; Desai, Sandip ; Kitson, Mike ; Nokhodchi, Ali. / The dissolution and solid-state behaviours of coground ibuprofen-glucosamine HCl. In: Drug Development and Industrial Pharmacy. 2015 ; Vol. 41, No. 10. pp. 1682-1692.
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The dissolution and solid-state behaviours of coground ibuprofen-glucosamine HCl. / Al-Hamidi, Hiba; Asare-Addo, Kofi; Desai, Sandip; Kitson, Mike; Nokhodchi, Ali.

In: Drug Development and Industrial Pharmacy, Vol. 41, No. 10, 2015, p. 1682-1692.

Research output: Contribution to journalArticle

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