• Home
  • Search Results
  • Spontaneous crystalline-to-amorphous phase transformation of organic or medicinal compounds in the presence of porous media, part 1: thermodynamics of spontaneous amorphization.

Spontaneous crystalline-to-amorphous phase transformation of organic or medicinal compounds in the presence of porous media, part 1: thermodynamics of spontaneous amorphization.

Journal of pharmaceutical sciences (2011-02-22)
Ken K Qian, Robin H Bogner
ABSTRACT

Spontaneous crystalline-to-amorphous phase transformation of organic or medicinal molecules in the presence of mesoporous materials has been observed, for which pathway was suggested to be via the vapor phase, that is, sublimation of the crystalline molecules followed by adsorption on the porous media. The objective of this paper is to rigorously evaluate this amorphization pathway and to study the thermodynamics of spontaneous amorphization. Mesoporous silicon dioxide (SiO(2)) was used as a model system. Physical mixtures of SiO(2) and crystalline compounds were prepared and stored at 0% relative humidity (RH) and 40 °C. Loss of crystallinity of the model compounds was confirmed using powder X-ray diffraction and polarized light microscopy. Adsorption chamber was set up, in which naphthalene and SiO(2) were stored, without physical contact, under reduced pressure at 0% RH and 40 °C. Data confirmed that the rate and extent of sublimation and adsorption of naphthalene were significant for amorphization to occur on a pharmaceutically relevant timescale. Furthermore, a thermodynamic model has been developed to explain spontaneous amorphization. This unique phase transformation phenomenon can be a simple and effective method to improve the aqueous solubility and bioavailability of poorly soluble drug molecules.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Decahydronaphthalene, mixture of cis + trans, anhydrous, ≥99%
Sigma-Aldrich
Decahydronaphthalene, mixture of cis + trans, reagent grade, 98%
Sigma-Aldrich
cis-Decahydronaphthalene, 99%
Sigma-Aldrich
trans-Decahydronaphthalene, 99%

Social Media

LinkedIn icon
Twitter icon
Facebook Icon
Instagram Icon

MilliporeSigma

Research. Development. Production.

We are a leading supplier to the global Life Science industry with solutions and services for research, biotechnology development and production, and pharmaceutical drug therapy development and production.

© 2021 Merck KGaA, Darmstadt, Germany and/or its affiliates. All Rights Reserved.

Reproduction of any materials from the site is strictly forbidden without permission.