Study of the preparation, characterization, and solubility of lidocaine complexed with 5-sulfosalicylic acid dihydrate.
Drug Dev Ind Pharm
; 50(7): 628-638, 2024 Jul.
Article
em En
| MEDLINE
| ID: mdl-39030701
ABSTRACT
OBJECTIVE:
This study was to prepare solid dispersions of lidocaine (Lid) with 5-sulfosalicylic acid dihydrate (SSA) by freeze-drying (freeze-dried [FD] Lid/SSA = 1/1) and to evaluate their physical properties.METHODS:
Here, we evaluated the physicochemical properties and solubility of solid dispersions of Lid and SSA prepared by freeze-drying (freeze-dried [FD] Lid/SSA = 1/1).RESULTS:
Differential scanning calorimetry measurements showed that after freeze-drying, the endothermic peak due to Lid melting, the dehydration peak, and the endothermic peak due to SSA melting disappeared. Powder X-ray diffraction results showed that the characteristic Lid and SSA peaks disappeared after freeze-drying, indicating a halo pattern. The near-infrared spectroscopy results suggested that Lid-derived -NH and -CH groups and the Lid-derived -OH and -CH groups from the SSA peak shifted and broadened after freeze-drying, suggesting their involvement in complex formation through Lid/SSA intermolecular interactions. Nuclear Overhauser effect spectroscopy-nuclear magnetic resonance (NMR) measurements showed a cross-peak due to the interaction between the Lid-derived -CH group and the SSA-derived -OH group, suggesting hydrogen bonding. Diffusion-ordered spectroscopy NMR measurements showed that the diffusion coefficients of Lid and SSA aggregated in FD Lid/SSA, suggesting a change in Lid dispersibility in the solvent owing to the formation of a complex with SSA. The solubility of FD Lid/SSA was approximately 88 mg/mL (â¼20-fold higher than that of Lid).CONCLUSIONS:
These findings suggest that complex formation occurred in FD Lid/SSA; this enhanced the solubility of this dispersion.Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Solubilidade
/
Varredura Diferencial de Calorimetria
/
Salicilatos
/
Liofilização
/
Lidocaína
Idioma:
En
Revista:
Drug Dev Ind Pharm
Ano de publicação:
2024
Tipo de documento:
Article
País de afiliação:
Japão
País de publicação:
Reino Unido