Surface dissolution UV imaging for investigation of dissolution of poorly soluble drugs and their amorphous formulation

Chiau Ming Long, Kin Tang, Hitesh Chokshi, Nikoletta Fotaki

Research output: Contribution to journalArticle

6 Citations (Scopus)
35 Downloads (Pure)

Abstract

The aim of this study is to investigate the dissolution properties of poorly soluble drugs from their pure form and their amorphous formulation under physiological relevant conditions for oral administration based on surface dissolution ultraviolet (UV) imaging. Dissolution of two poorly soluble drugs (cefuroxime axetil and itraconazole) and their amorphous formulations (Zinnat® and Sporanox®) was studied with the Sirius Surface Dissolution Imager (SDI). Media simulating the fasted state conditions (compendial and biorelevant) with sequential media/flow rate change were used. The dissolution mechanism of cefuroxime axetil in simulated gastric fluid (SGF), fasted state simulated gastric fluid (FaSSGF) and simulated intestinal fluid (SIF) is predominantly swelling as opposed to the convective flow in fasted state simulated intestinal fluid (FaSSIF-V1), attributed to the effect of mixed micelles. For the itraconazole compact in biorelevant media, a clear upward diffusion of the dissolved itraconazole into the bulk buffer solution is observed. Dissolution of itraconazole from the Sporanox® compact is affected by the polyethylene glycol (PEG) gelling layer and hydroxypropyl methylcellulose (HPMC) matrix, and a steady diffusional dissolution pattern is revealed. A visual representation and a quantitative assessment of dissolution properties of poorly soluble compounds and their amorphous formulation can be obtained with the use of surface dissolution imaging under in vivo relevant conditions.
Original languageEnglish
Article number113
Pages (from-to)1-12
Number of pages12
JournalAAPS PharmSciTech
Volume20
Issue number3
Early online date13 Feb 2019
DOIs
Publication statusPublished - 1 Apr 2019

Keywords

  • UV imaging
  • amorphous formulation
  • biorelevant dissolution
  • intrinsic dissolution
  • poorly soluble drugs
  • surface dissolution
  • Anti-Bacterial Agents/chemistry
  • Cefuroxime/analogs & derivatives
  • Solubility
  • Antifungal Agents/chemistry
  • Spectrophotometry, Ultraviolet/methods
  • Micelles
  • Surface Properties
  • Drug Compounding
  • Body Fluids
  • Itraconazole/chemistry

ASJC Scopus subject areas

  • Pharmaceutical Science

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