A novel carrier for the formulation of amorphous solid dispersion and solubility enhancement of poor water soluble drugs

Share
  • février 8, 2021
  • 2 minutes of read time

A novel carrier for the formulation of amorphous solid dispersion and solubility enhancement of poor water soluble drugs

Maëla Choimet 1, Sandra Lefebvre1, Laurène Haurie 2, Suénia de Paiva Lacerda 2, Maria-Inês Ré 2

12th World Meeting on Pharmaceutics, Biopharmaceutics & Pharmaceutical Technology, 2021

Hot melt extrusion (HME) is a widely used process in different sectors of application. This technology consists in extruding two o more components at high temperatures and under mechanical mixing. For pharmaceutical applications, the aim of this technology is to obtain an amorphous solid dispersion (ASD), which is defined as a dispersion of one or more active ingredients in an inert support, or polymeric matrix, in the solid state. ASD offers the advantages of higher solubility and dissolution rate, and better compression characteristics compared to the corresponding native crystalline active principle ingredient (API). The aim of this work was to study the possibility to use a functional excipient, a polysorbate 80 adsorbed on magnesium aluminometasilicate (Sepitrap™ 80), as a carrier for HME and to evaluate its capability to improve the solubility of indomethacin, (1-(4-Chlorobenzoyl)-5 -methoxy-2-methyl-1H-indole-3-acetic acid), a poor water soluble drug. Several works have studied its (pure) amorphization, the stability of the amorphous phase and recrystallization conditions [1-7]. Sepitrap™ 80 is a microencapsulated powder solubilizer designed to simplify the manufacture of drugs in oral solid forms. It is obtained by adsorption of the solubilizer in liquid form on a porous support. This study was carried out in order to develop ASD with SepitrapTM 80 via HME and to compare their functional properties (solubility, dissolution kinetics) to those of commercialized indomethacin, and of a physical mixture of indomethacin with Sepitrap™ 80.

1 - Seppic, 50 boulevard National - CS 90020 - 92257 La Garenne Colombes, France,

2 - Université de Toulouse, IMT Mines Albi, CNRS UMR 5302, Plateforme Gala/Centre RAPSODEE, Campus Jarlard, 81013 Albi, France