中国药房2024，Vol.35Issue(10)：1215-1219,5.DOI:10.6039/j.issn.1001-0408.2024.10.11
木犀草素固体分散体的体外溶出度和体内药动学研究
Study on in vitro dissolution and in vivo pharmacokinetics of Luteolin solid dispersion
摘要
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.关键词
木犀草素/固体分散体/UPLC-MS/MS法/药动学/溶出度/生物利用度Key words
luteolin/solid dispersion/UPLC-MS/MS/pharmacokinetics/dissolution/bioavailability分类
医药卫生引用本文复制引用
黄子婷,王梦颜,常金花,刘沛,王汝兴,刘喜纲..木犀草素固体分散体的体外溶出度和体内药动学研究[J].中国药房,2024,35(10):1215-1219,5.基金项目
河北省高等学校科学研究项目(No.ZD2022-121) （No.ZD2022-121）
承德医学院自然科学研究计划项目(No.202010) （No.202010）
