The role of SeDeM for characterizing the active substance and polyvinyilpyrrolidone eliminating metastable forms in an oral lyophilizate-A preformulation study.

Flórez Borges, Paloma; García-Montoya, Encarna; Pérez-Lozano, Pilar; Jo, Enric; Miñarro, Montserrat; Manich, Albert; Suñé-Negre, Josep Maria · PLoS One · 2018

basic_science · Level V

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Abstract

A preformulation study of an oral lyophilisate with cetirizine dihydrochloride (CTZ) as active ingredient, mannitol and PVP K30 as bulking agents is presented. CTZ shown a humidity content of 0.150% and a spontaneous hygroscopicity of 0.200% (both determined by SeDeM diagram), demonstrating an adequate stability behavior in solid form. A design of experiments (DoE) performed with both mannitol and PVP K30, followed by a simple factorial design (32) has determined the optimum combination of excipients and CTZ, and showed that a higher proportion of PVP K30 was able to prevent metastable forms generated by mannitol.

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