Abstract
Amorphous solid dispersion drug delivery systems (ASD DDS) were proved to be efficient for the enhancement of solubility and bioavailability of poorly water-soluble drugs. One of the major keys for successful preparation of ASD is the selection of appropriate excipients, mostly polymers, which have a crucial role in improving drug solubility and its physical stability. Even though, excipients should be chemically inert, there is some evidence that polymers can affect the thermal stability of active pharmaceutical ingredients (API). The thermal stability of a drug is closely related to the shelf-life of pharmaceutical products and therefore it is a matter of high pharmaceutical relevance. An overview of thermal stability of amorphous solids is provided in this paper. Evaluation of thermal stability of amorphous solid dispersion is perceived from the physicochemical perspective, from a kinetic (motions) and thermodynamic (energy) point of view, focusing on activation energy and fragility, as well all other relevant parameters for ASD design, with a glance on computational kinetic analysis of solid-state decomposition.
Highlights
Physical instability is mostly related to the mobility of molecules, due to temperature increment, while chemical instability is related to energy flow which can induce thermal decomposition of drugs
An overview of thermal stability provided here highlights its intrinsic characteristic connected with drug stability, both chemical and physical
Thermal stability is important for the thermal behavior of drug, thermal decomposition of drug and its products, compatibility/incompatibility between active pharmaceutical ingredients (API) and excipients, and solubility potential and its shelf-life, which are the most important challenges in the drug development
Summary
Thermal stability is a characteristic of a material to retain its structure and properties when exposed to higher temperatures. Physical instability is mostly related to the mobility of molecules, due to temperature increment, while chemical instability is related to energy (heat) flow which can induce thermal decomposition of drugs. These changes might lead to a decreased pharmacological activity and shortened shelf life of drugs. The onset temperature of degradation that goes in favor of the thermal behavior of drug can be determined [3]; Second, we can get insight into the mechanism of thermal decomposition of drugs and potential degradants (i.e., the relationship between the molecular structure and thermal stability) [7]; Third, understanding of compatibility/incompatibility between drug and excipients is revealed [8]; Fourth, we learn about its solubility potential [9]; information on handling/storage of drugs, shelf-life, and usage can be provided [10]. This paper provides an overview of the quantitative meaning of thermal stability considering kinetics and thermodynamics factors relevant to predict and control stability and, the shelf life of amorphous solid dispersions
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