Bioavailability Enhancement of BCS Class II Raloxifene Hydrochloride by Inclusion Complex and Solid Dispersion Techniques.
Zhongguo Ying Yong Sheng Li Xue Za Zhi
; 40: e20240002, 2024 Jun 12.
Article
em En
| MEDLINE
| ID: mdl-38862271
ABSTRACT
OBJECTIVE:
Raloxifene hydrochloride (RLX) is used extensively in the treatment of osteoporosis, only 2% of RLX's bioavailability remains after a significant first pass metabolism. Besides coming from BCS class II, RLX is not very soluble in water. Thus, the goal of the current study was to improve RLX solubility by creating an inclusion complex using ß cyclodextrin (ß-CD) as a carrier and solid dispersion with Poloxamer 407.METHODS:
Inclusion complex and solid dispersion were made using a variety of techniques, including kneading, co-precipitation, and physical mixing and solid dispersion using different drug to carrier ratios (11, 12 and 13).RESULTS:
Inclusion complex made using the co-precipitation method had shown 9-fold improvements in water solubility when compared with plain RLX. In order to assess the optimized complex's compatibility, thermal analysis, and crystallinity, X-ray diffraction, differential scanning calorimetry, and Fourier transform infrared spectroscopy were used. The XRD and DSC study's results indicated that RLX changed from a crystalline to an amorphous state. IC-6 exhibits effective water solubility based on the outcome. However, upon comparison of the two techniques, the ß-CD complexation method shown an impressive rise in drug solubility when compared to solid dispersion.Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Solubilidade
/
Disponibilidade Biológica
/
Cloridrato de Raloxifeno
/
Beta-Ciclodextrinas
Limite:
Animals
Idioma:
En
Revista:
Zhongguo Ying Yong Sheng Li Xue Za Zhi
Assunto da revista:
FISIOLOGIA
Ano de publicação:
2024
Tipo de documento:
Article
País de afiliação:
Índia