title: Emerging trends in the stabilization of amorphous drugs.
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.
authors.affiliation: School of Pharmacy, University of Otago, P.O. Box 913, Dunedin 9054, New Zealand. riikka.laitinen@otago.ac.nz
authors.forename: Riikka
authors.initials: R
authors.lastname: Laitinen
authors.forename: Korbinian
authors.initials: K
authors.lastname: Löbmann
authors.forename: Clare J
authors.initials: CJ
authors.lastname: Strachan
authors.forename: Holger
authors.initials: H
authors.lastname: Grohganz
authors.forename: Thomas
authors.initials: T
authors.lastname: Rades
mesh_terms: D002626:Chemistry, Pharmaceutical / Q000379:methods*; D004355:Drug Stability; D004364:Pharmaceutical Preparations / Q000737:chemistry*; D011108:Polymers / Q000737:chemistry; D012825:Silicon / Q000737:chemistry; D012822:Silicon Dioxide / Q000737:chemistry; D012995:Solubility
chemical_list: D004364:Pharmaceutical Preparations; D011108:Polymers; D012822:Silicon Dioxide; D012825:Silicon