摘要
该研究旨在初步考察复合红花籽油(Complex Safflower Seed Oil,CSSO)的肠吸收特性.采用肠襻吸收模型结合药代动力学,通过计算液相色谱测定的α-亚麻酸(α-Linolenic Acid,ALA)和亚油酸(Linoleic Acid,LA)浓度,计算吸收参数M(吸收药量)、P(累计吸收率)、Ka(吸收速率常数),t1/2(吸收半衰期)以及药动学参数,考察CSSO的药物浓度、pH值条件及吸收促进剂对其吸收的影响,以及在动物体内不同给药剂量CSSO的吸收速度与吸收程度,以此来阐明CSSO的吸收特性.由在体肠吸收实验可知,高浓度CSSO中ALA和LA的M(ALA:23.77 mg,LA:42.27 mg)和P(ALA:94.92%;LA:91.89%)最高,且均随着浓度的升高而增加,pH值为8.0时CSSO中ALA和LA的M(ALA:24.19 mg;LA:43.38 mg)和P(ALA:96.60%;LA:94.295%)最高,吸收促进剂对CSSO的吸收无影响.由药代动力学实验可知,CSSO吸收速度较快,在 1～2 h即可达到峰浓度,在2.604～5.208 g/kg内生物利用度较高.结果表明,CSSO的吸收特性为具有浓度(剂量)依赖性且以被动扩散方式在大鼠体内吸收,为不饱和脂肪酸制剂的开发提供理论基础.
Abstract
In this study,the intestinal absorption characteristics of compound safflower seed oil(CSSO)were preliminarily investigated.The absorption parameters M(absorbed drug dose),P(cumulative absorption rate),Ka(absorption rate constant),t1/2(absorption half-life)and pharmacokinetic parameters were calculated via the analysis of α-linolenic acid(ALA)and linoleic acid(LA)concentrations by liquid chromatography using an intestinal loop absorption model in combination with pharmacokinetics.The effects of drug concentration,pH value and absorption enhancers on the absorption of CSSO were investigated,as well as the absorption rate and extent of CSSO at different doses administered in animals,in order to elucidate the absorption characteristics of CSSO.The in vivo intestinal absorption experiments revealed that the M(ALA:23.77 mg,LA:42.27 mg)and P(ALA:94.92%;LA:91.89%)of ALA and LA in high concentrations of CSSO were the highest,and both increased with an elevated concentration:The M(ALA:24.19 mg;LA:43.38 mg)and P(ALA:96.60%;LA:94.295%)in CSSO were the highest at pH 8.0.The absorption enhancers had no effect on the absorption of CSSO.The pharmacokinetic experiments revealed that CSSO was absorbed rapidly,reaching the peak concentration within 1～2 h.The bioavailability was relatively high in the range of 2.604～5.208 g/kg.The results showed that the absorption characteristics of CSSO was concentration(dose)-dependent and CSSO was absorbed in a passive diffusion in rats,providing a theoretical basis for the development of unsaturated fatty acid preparations.
基金项目
国家自然科学基金项目(31960475)
新疆农业大学研究生科研创新项目(XJAUGRI2022014)
国家科技期刊平台
NSTL
万方数据