Solid state behavior of progesterone and its release from Neusilin US2 based liquisolid compacts

Abstract

The aim of present work was to investigate the role of liquisolid technique in improving dissolution of high dose Progesterone. Progesterone-PEG 400 dispersions were prepared and evaluated for technological properties, and further formulated into liquisolid tablets using Neusilin US2 and Syloid 244 FP as a carrier and coat respectively. Due to polymorphic behavior of Progesterone, liquisolid tablets were investigated by XRPD, DSC and SEM, whereas, improvement in dissolution was studied by in vitro technique. Results of liquid load factor and liquid retention potential demonstrated a role of Neusilin US2 and Syloid 244 FP as a superior carrier and coat material respectively. Both excipients enabled incorporation of higher amount of liquid medication and high Progesterone loading (50 mg). Acceptable flowability and compressibility of liquisolids were noted, uncompromising tablettability and tablet size. Noteworthy findings of XRPD and DSC suggested polymorphic transition of Progesterone from stable α to metastable β form in liquisolid formulation having high liquid medication. Consequently, superior dissolution profiles for liquisolid tablets, compared to conventional tablet were noted. Hence, it can be concluded that, liquisolid tablets of high dose progesterone were successfully formulated using Neusilin US2 and Syloid 244 FP. Besides improved dissolution, polymorphic transition was also revealed for Progesterone.

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