Abstract：
:Supersaturated drug delivery systems are commonly used to address the problems of poor aqueous solubility posed by most of the active pharmaceutical ingredients (APIs). However, the supersaturated systems are highly unstable due to their high free energy levels and demonstrate a tendency to precipitate. Understanding the crystallization tendency based on the mechanisms of crystallization, that is nucleation and crystal growth, is imperative to design formulation strategies and select appropriate precipitation inhibitors. This study aims to provide a classification system, based on both the nucleation and crystal growth tendency in the solution state of 60 APIs and nutraceuticals (in absence of polymer) from their desupersaturation profiles monitored by UV-Visible spectroscopy. The APIs and nutraceuticals are divided into four classes based on their induction time (tind) and crystal growth rate as fast nucleators-fast crystal growth (class I), fast nucleators-slow crystal growth (class II), slow nucleators-fast crystal growth (class III) and slow nucleators-slow crystal growth (class IV). Most of the molecules fall in the class I and class IV. An easy-to-use protocol for nucleation and crystal growth studies has been optimized. This protocol will find application to assess the crystallization tendency of the molecules in the preliminary screening stages, enabling appropriate formulation strategies to inhibit crystallization.
journal_name
Drug Deliv Transl Resjournal_title
Drug delivery and translational researchauthors
Rathi S,Chavan RB,Shastri NRdoi
10.1007/s13346-019-00663-wsubject
Has Abstractpub_date
2020-02-01 00:00:00pages
70-82issue
1eissn
2190-393Xissn
2190-3948pii
10.1007/s13346-019-00663-wjournal_volume
10pub_type
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