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AAPS PharmSciTech ; 25(5): 127, 2024 Jun 06.
Artigo em Inglês | MEDLINE | ID: mdl-38844724

RESUMO

The success of obtaining solid dispersions for solubility improvement invariably depends on the miscibility of the drug and polymeric carriers. This study aimed to categorize and select polymeric carriers via the classical group contribution method using the multivariate analysis of the calculated solubility parameter of RX-HCl. The total, partial, and derivate parameters for RX-HCl were calculated. The data were compared with the results of excipients (N = 36), and a hierarchical clustering analysis was further performed. Solid dispersions of selected polymers in different drug loads were produced using solvent casting and characterized via X-ray diffraction, infrared spectroscopy and scanning electron microscopy. RX-HCl presented a Hansen solubility parameter (HSP) of 23.52 MPa1/2. The exploratory analysis of HSP and relative energy difference (RED) elicited a classification for miscible (n = 11), partially miscible (n = 15), and immiscible (n = 10) combinations. The experimental validation followed by a principal component regression exhibited a significant correlation between the crystallinity reduction and calculated parameters, whereas the spectroscopic evaluation highlighted the hydrogen-bonding contribution towards amorphization. The systematic approach presented a high discrimination ability, contributing to optimal excipient selection for the obtention of solid solutions of RX-HCl.


Assuntos
Química Farmacêutica , Excipientes , Polímeros , Cloridrato de Raloxifeno , Solubilidade , Difração de Raios X , Polímeros/química , Excipientes/química , Cloridrato de Raloxifeno/química , Análise Multivariada , Difração de Raios X/métodos , Química Farmacêutica/métodos , Portadores de Fármacos/química , Composição de Medicamentos/métodos , Microscopia Eletrônica de Varredura/métodos , Ligação de Hidrogênio , Cristalização/métodos
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