白藜芦醇/羟丙基-β-环糊精/壳聚糖缓释微球的体外释放度及其在大鼠体内药动学的考察
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篇名: | 白藜芦醇/羟丙基-β-环糊精/壳聚糖缓释微球的体外释放度及其在大鼠体内药动学的考察 |
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摘要: | 目的:考察白藜芦醇/羟丙基-β-环糊精/壳聚糖缓释微球(RES/HP-β-CD/Chitosan)的体外释放度及其在大鼠体内的药动学。方法:采用桨法考察RES原料药、RES/HP-β-CD包合物(RES/HP-β-CD)和RES/HP-β-CD/Chitosan在水中12 h内的体外释放度。比较灌胃给予大鼠RES原料药、RES/HP-β-CD和RES/HP-β-CD/Chitosan后720 min内的药动学特征。结果:与RES原料药比较,RES/HP-β-CD的体外释放度明显增加,120 min的累积释放度为87%;与RES/HP-β-CD比较,RES/HP-β-CD/Chitosan的体外释放明显减缓,释放时间明显延长,12 h的累积释放度为72%。RES原料药、RES/HP-β-CD、RES/HP-β-CD/Chitosan在大鼠体内的药动学参数cmax分别为473.3、2 492.2、590.5 ng/mL,t1/2分别为2.6、0.5、4.6 h,AUC0-12 h分别为514.7、824.6、2 778.5 ng·h/mL。与RES原料药比较,RES/HP-β-CD和RES/HP-β-CD/Chitosan的相对生物利用度分别为172.5%和540.0%。结论:RES/HP-β-CD/Chitosan具有良好的缓释作用,且生物利用度明显高于RES原料药和RES/HP-β-CD。 |
ABSTRACT: | OBJECTIVE: To investigate in vitro release rate and in vivo pharmacokinetics of Resveratrol/hydroxypropyl-β- cyclodextrin/chitosan sustained-release pellets (RES/HP-β-CD/Chitosan) in rats. METHODS: In vitro release rate of RES raw materials, RES-HP-β-CD complexes (RES/HP-β-CD) and RES/HP-β-CD/Chitosan in water within 12 h were investigated by paddle method. The pharmacokinetic characteristics of RES raw materials, RES/HP-β-CD and RES/HP-β-CD/Chitosan were compared within 720 min after intragastric administration. RESULTS: Compared with RES raw materials, in vitro release rate of RES/HP-β-CD was increased significantly, and 120 min accumulative release rate reached 87%. Compared with RES/HP-β-CD, in vitro release rate of RES/HP-β-CD/Chitosan were relieved significantly; release time prolonged significantly; 12 h accumulative release rate was 72%. The pharmacokinetic parameters of RES raw materials, RES/HP-β-CD and RES/HP-β-CD/Chitosan included that cmax were 473.3, 2 492.2, 590.5 ng/mL; t1/2 were 2.6, 0.5, 4.6 h; AUC0-12 h were 514.7, 824.6, 2 778.5 ng·h/mL. Compared with RES raw materials, relative bioavailability of RES/HP-β-CD and RES/HP-β-CD/Chitosan were 172.5% and 540.0%. CONCLUSIONS: RES/HP-β-CD/Chitosan shows good sustained-release effect, and its bioavailability is significantly higher than that of RES raw materials, RES/HP-β-CD. |
期刊: | 2019年第30卷第19期 |
作者: | 于琛琛,张纯刚,尹丽,周旖璇,程岚,康廷国 |
AUTHORS: | YU Chenchen,ZHANG Chungang,YIN Li,ZHOU Yixuan,CHENG Lan,KANG Tingguo |
关键字: | 白藜芦醇;羟丙基-β-环糊精;壳聚糖;释放度;药动学;大鼠 |
KEYWORDS: | Resveratrol; Hydroxypropyl-β-cyclodextrin; Chitosan; Release rate; Pharmacokinetics; Rats |
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