[Preparation of salvianolic acid B, tanshinone â
¡_A, and glycyrrhetinic acid lipid emulsion and its protective effect against acute liver injury induced by acetaminophen].
Zhongguo Zhong Yao Za Zhi
; 47(17): 4634-4642, 2022 Sep.
Article
em Zh
| MEDLINE
| ID: mdl-36164869
ABSTRACT
Salvianolic acid B(Sal B), tanshinone â
¡_A(TSN â
¡_A), and glycyrrhetinic acid(GA) lipid emulsion(GTS-LE) was prepared by the high-speed dispersion method combined with ultrasonic emulsification.The preparation process of the emulsion was optimized by single-factor method and D-optimal method with appearance, centrifugal stability, and particle size of the emulsion as evalua-tion indexes, followed by verification.In vitro release of Sal B, TSN â
¡_A, and GA in GTS-LE was performed by reverse dialysis.In vivo pharmacokinetic evaluation was carried out in mice.The acute liver injury model was induced by acetaminophen.The effect of oral GTS-LE on the acute liver injury was investigated by serum liver function indexes and pathological changes in liver tissues of mice.The results showed that under the optimal preparation process, the average particle size of GTS-LE was(145.4±9.25) nm and the Zeta potential was(-33.6±1.45) mV.The drug-loading efficiencies of Sal B, TSN â
¡_A, and GA in GTS-LE were above 95%, and the drug release in vitro conformed to the Higuchi equation.The pharmacokinetic results showed that the C_(max) of Sal B, TSN â
¡_A, and GA in GTS-LE was 3.128, 2.7, and 2.85 times that of the GTS-S group, and AUC_(0-t) of Sal B, TSN â
¡_A, and GA in GTS-LE was 3.09, 2.23, and 1.9 times that of the GTS-S group.After intragastric administration of GTS-LE, the activities of alanine aminotransferase and aspartate aminotransferase were significantly inhibited, the content of malondialdehyde was reduced, and the structure of hepatocytes recovered to normal.In conclusion, GTS-LE can delay the release of Sal B and promote the release of TSN â
¡_A and GA.The encapsulation of three drug components in the emulsion can improve the oral bioavailability to varying degrees and can effectively prevent the acute liver injury caused by acetaminophen.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Benzofuranos
/
Abietanos
/
Depsídeos
/
Doença Hepática Induzida por Substâncias e Drogas
/
Antipiréticos
/
Ácido Glicirretínico
/
Acetaminofen
Tipo de estudo:
Prognostic_studies
Limite:
Animals
Idioma:
Zh
Ano de publicação:
2022
Tipo de documento:
Article