Impact of Surfactant and Surfactant-Polymer Interaction on Desupersaturation of Clotrimazole.

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ID: 66461
2019
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Abstract
The impact of surfactants on supersaturation of clotrimazole solutions was systematically evaluated. Four clinically relevant surfactants, sodium dodecyl sulfate, vitamin E TPGS, Tween 80, and docusate sodium were studied. The induction time for nucleation and rate of desupersaturation were determined at a supersaturation ratio of 90% amorphous solubility. Measurement was also performed in the presence of predissolved hydroxypropyl methylcellulose acetate succinate to study the effect of surfactant-polymer interaction on desupersaturation. The 4 surfactants showed varied effects on desupersaturation. From supersaturation maintenance perspective, in the presence of hydroxypropyl methylcellulose acetate succinate, the rank order for the 4 surfactants was found to be: docusate sodium > vitamin E TPGS > sodium dodecyl sulfate > Tween 80. Given the importance of maintaining supersaturation and varied effect of surfactants on nucleation kinetics and desupersaturation rate, a careful examination of active pharmaceutical ingredient, polymer and surfactant interaction on an individual basis is recommended for selecting an appropriate surfactant for use in amorphous solid dispersion formulation.
Reference Key
zhang2019impactjournal Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Zhang, Wei;Hate, Siddhi S;Russell, David J;Hou, Hao Helen;Nagapudi, Karthik;
Journal journal of pharmaceutical sciences
Year 2019
DOI
S0022-3549(19)30369-7
URL
Keywords
Crystallization formulation supersaturation preformulation amorphous solid dispersion(s) (asd) surfactant(s)

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