Emerging trends in the stabilization of amorphous drugs

Riikka Laitinen, Korbinian Löbmann, Clare J. Strachan, Holger Grohganz, Thomas Rades

Research output: Contribution to journalJournal articleResearchpeer-review

362 Citations (Scopus)

Abstract

The number of active pharmaceutical substances having high therapeutic potential but low water solubility is constantly increasing, making it difficult to formulate these compounds as oral dosage forms. The solubility and dissolution rate, and thus potentially the bioavailability, of these poorly water-soluble drugs can be increased by the formation of stabilized amorphous forms. Currently, formulation as solid polymer dispersions is the preferred method to enhance drug dissolution and to stabilize the amorphous form of a drug. The purpose of this review is to highlight emerging alternative methods to amorphous polymer dispersions for stabilizing the amorphous form of drugs. First, an overview of the properties and stabilization mechanisms of amorphous forms is provided. Subsequently, formulation approaches such as the preparation of co-amorphous small-molecule mixtures and the use of mesoporous silicon and silica-based carriers are presented as potential means to increase the stability of amorphous pharmaceuticals.
Original languageEnglish
JournalInternational Journal of Pharmaceutics
Volume453
Issue number1
Pages (from-to)65-79
Number of pages15
ISSN0378-5173
DOIs
Publication statusPublished - 30 Aug 2013

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