The effect of surfactants on the dissolution behavior of amorphous formulations

The optimal design of oral amorphous formulations benefits from the use of excipients to maintain drug supersaturation and thus ensure adequate absorption during intestinal transit. The use of surfactants for the maintenance of supersaturation in amorphous formulations has not been investigated in detail. The main aim of this study was to investigate the effect of surfactant on the dissolution behavior of neat amorphous drug and binary polymer based solid dispersion. Indomethacin was used as the model drug and the surfactants studied were polysorbate 80 and poloxamer 407. The presence of surfactants (alone or in combination with polymers) in the buffer was detrimental to the dissolution of neat amorphous indomethacin, suggesting that the surfactants promoted the crystallization of neat amorphous indomethacin.

Key words: Amorphous; Crystallization; Dissolution; Indomethacin; Polymer; Solid dispersion; Supersaturation; Surfactant

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