Adsorption of Polyvinylpyrrolidone and its Impact on Maintenance of Aqueous Supersaturation of Indomethacin via Crystal Growth Inhibition

Approaches to increase mechanistic understanding and aid in the selection of precipitation inhibitors for supersaturating formulations – a PEARRL review

“…Further, the isotherms demonstrated that the adsorption capacity for PVP was directly proportional to PVP molecular weight. These model predictions were then validated experimentally, with PVP significantly outperforming N‐vinylpyrrolidone in the inhibition of indomethacin precipitation, with increasing molecular weight of PVP also correlating to a higher degree of sustained supersaturation …”

“…One of the most extensive studies on the use of adsorption and crystallisation models was carried out by Patel et al . They studied the precipitation behaviour of indomethacin in the presence of PIs.…”

The interplay of dissolution, solution crystallization and solid-state transformation of amorphous indomethacin in aqueous solution

“…Crystal-growth kinetics from solution were e.g. studied by the group of Taylor ( Alonzo et al, 2010 ; Abbou Oucherif et al, 2013 ; Alonzo et al, 2012 ; Schram et al, 2016 ; Patel and Anderson (2014) ; Patel and Anderson (2015) ) and Cheng et al (2019) , for a variety of APIs. Kinetic effects of hydroxypropylmethycellulose (HPMC) and polyvinylpyrrolidone (PVP) were observed consistently.…”

Role of Polymeric Excipients in the Stabilization of Olanzapine when Exposed to Aqueous Environments

“…Phase transformation of an API is of pharmaceutical interest because such transformations may change the physical and chemical properties of the drug with an impact on its dissolution and bioavailability [2]. The hydrate formation in wet masses takes place via solvent-mediated transformations (SMT) involving three different steps: (1) dissolution of the anhydrate phase in the solvent used for the wet massing of the powders; (2) nucleation of the hydrate species and (3) growth of the hydrate phase [3,4]. Inhibiting one of these stages could be advantageous to maintaining the original crystal form of the API and avoiding a product containing a mixture of solid-state forms.…”

“…The addition of other excipients to the formulation (e.g., polymers) may reduce the amount of water needed for the powder to agglomerate. Furthermore, polymers are known to inhibit the nucleation and/or growth of hydrated pharmaceutical crystals in aqueous slurries [3,4]. For instance, polyvinylpyrrolidone (PVP) has been demonstrated to inhibit the growth rate of sulfathiazole and indomethacin in solutions [3].…”