Intestinal Loop Method Combined with Pharmacokinetics for the Investigation on the Absorption Characteristics of Compound Safflower Seed Oil
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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.
