Study on in vitro dissolution and in vivo pharmacokinetics of Luteolin solid dispersion
- VernacularTitle:木犀草素固体分散体的体外溶出度和体内药动学研究
- Author:
Ziting HUANG
1
;
Mengyan WANG
1
;
Jinhua CHANG
1
;
Pei LIU
1
;
Ruxing WANG
1
;
Xigang LIU
1
Author Information
1. Institute of Chinese Materia Medica，Chengde Medical University，Hebei Chengde 067000，China
- Publication Type:Journal Article
- Keywords:
luteolin;
solid dispersion;
UPLC-MS/MS;
pharmacokinetics;
dissolution;
bioavailability
- From:
China Pharmacy
2024;35(10):1215-1219
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE To explore in vitro dissolution and in vivo pharmacokinetics of Luteolin solid dispersion in Beagle dogs. METHODS The dissolution of Luteolin solid dispersion was investigated according to the second method （paddle method） of the “dissolution determination method” in the 2020 edition of Chinese Pharmacopoeia （Part Ⅳ）. UPLC-MS/MS method was established to determine the concentration of luteolin in the plasma of Beagle dogs. Twelve Beagle dogs were randomly divided into luteolin group and Luteolin solid dispersion group， with 6 dogs in each group. They were given relevant medicine orally at the dose of 10 mg/kg luteolin. Blood was collected before medication （0 h）， at 5， 10， 15， 30， 45 min and 1， 2， 4， 6， 8， 10， 12， 24， 48 h after administration. After protein precipitation with acetonitrile， the blood concentration of luteolin in Beagle dogs was determined by UPLC-MS/MS and the major pharmacokinetic parameters were calculated with non-compartmental models by using DAS 3.2.8 pharmacokinetic software. RESULTS The dissolutions of Luteolin solid dispersion in purified water and 0.1% sodium dodecyl sulfate solution was significantly higher than those of luteolin； the dissolution rate reached 95% in 0.1% sodium dodecyl sulfate solution for 120 minutes. The peak concentration （cmax） of luteolin in the Luteolin solid dispersion group of Beagle dogs was 5.62 times higher than the luteolin group， and the relative bioavailability was 348%. Compared with luteolin group， cmax and the area under the drug time curve of luteolin in the Luteolin solid dispersion group of Beagle dogs were significantly increased， while the apparent distribution volume was significantly reduced （P＜0.05）. CONCLUSIONS Luteolin solid dispersion can improve in vitro dissolution and bioavailability of luteolin in Beagle dogs.
