Moringa coagulant as a stabilizer for amorphous solids: Part I

AAPS PharmSciTech. 2012 Jun;13(2):400-10. doi: 10.1208/s12249-012-9755-x. Epub 2012 Feb 23.

Abstract

Stabilization of amorphous state is a focal area for formulators to reap benefits related with solubility and consequently bioavailability of poorly soluble drugs. In the present work, an attempt has been made to explore the potential of moringa coagulant as an amorphous state stabilizer by investigating its role in stabilization of spray-dried (amorphous) ibuprofen, meloxicam and felodipine. Thermal studies like glass forming ability, glass transition temperature, hot stage microscopy and DSC were carried out for understanding thermodynamic stabilization of drugs. PXRD and dissolution studies were performed to support contribution of moringa coagulant. Studies showed that hydrogen bonding and electrostatic interactions between drug and moringa coagulant are responsible for amorphous state stabilization as explored by ATR-FTIR and molecular docking. Especially, H-bonding was found to be predominant mechanism for drug stabilization. Therein, arginine (basic amino acid in coagulant) exhibited various interactions and played important role in stabilization of aforesaid amorphous drugs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Arginine / chemistry
  • Calorimetry, Differential Scanning
  • Chemistry, Pharmaceutical
  • Coagulants / chemistry*
  • Coagulants / isolation & purification
  • Crystallography, X-Ray
  • Drug Stability
  • Excipients / chemistry*
  • Excipients / isolation & purification
  • Felodipine / chemistry*
  • Hydrogen Bonding
  • Ibuprofen / chemistry*
  • Kinetics
  • Meloxicam
  • Microscopy
  • Models, Molecular
  • Molecular Structure
  • Moringa oleifera / chemistry*
  • Plant Proteins / chemistry*
  • Plant Proteins / isolation & purification
  • Solubility
  • Spectroscopy, Fourier Transform Infrared
  • Technology, Pharmaceutical / methods
  • Thiazines / chemistry*
  • Thiazoles / chemistry*
  • Transition Temperature
  • X-Ray Diffraction

Substances

  • Coagulants
  • Excipients
  • Plant Proteins
  • Thiazines
  • Thiazoles
  • Arginine
  • Felodipine
  • Meloxicam
  • Ibuprofen