Pharmacokinetics study of a supersaturatable self-microemulsifying drug delivery system for ellagic acid by UHPLC-Q-TOF-MS.

IF 1.8 4区 医学 Q3 PHARMACOLOGY & PHARMACY
Jinglong Wang, Liqun Fan, Lihua Zhang, Dandan Zheng, Yingzi Wang, Xiao Sun, Yonghui Ji
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引用次数: 0

Abstract

To evaluate the bioavailability of ellagic acid loaded super-saturatable self-microemulsifying drug delivery system (S-SMEDDS), its pharmacokinetic properties were studied in rats with an ultra-high performance liquid chromatography-quadrupole time-of-flight tandem mass spectrometry. The plasma samples were treated by solid-phase extraction method, and gallic acid was used as the internal standard when determining the concentration of ellagic acid. Results showed that the established analytical method was sensitive and accurate, which is applicable to the pharmacokinetic study of ellagic acid. The drug was found to be absorbed rapidly in vivo, and the plasma concentration-time curve showed double peaks, indicating that ellagic acid were reabsorbed by entero-hepatic circulation after oral administration. Compared with ellagic acid suspension, the apparent clearance of ellagic acid-loaded S-SMEDDS and SMEDDS reduced significantly, and the AUC 0~t of them were 4.7 and 5.8-fold increase, respectively. Therefore, the bioavailability of ellagic acid-loaded S-SMEDDS was higher than that of the suspension and SMEDDS.

UHPLC-Q-TOF-MS研究鞣花酸过饱和自微乳化给药体系的药动学。
为评价载花藻酸超饱和自微乳化给药系统(S-SMEDDS)的生物利用度,采用超高效液相色谱-四极杆飞行时间串联质谱法研究其在大鼠体内的药动学特性。血浆样品采用固相萃取法处理,以没食子酸为内标测定鞣花酸浓度。结果表明,所建立的分析方法灵敏、准确,可用于鞣花酸的药动学研究。体内吸收快,血药浓度-时间曲线呈双峰,说明鞣花酸经口服后经肠肝循环重吸收。与鞣花酸悬浮液相比,载鞣花酸S-SMEDDS和SMEDDS的表观清除率显著降低,AUC 0~t分别提高4.7倍和5.8倍。因此,载鞣花酸S-SMEDDS的生物利用度高于悬浮液和SMEDDS。
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来源期刊
Acta Pharmaceutica
Acta Pharmaceutica PHARMACOLOGY & PHARMACY-
CiteScore
5.20
自引率
3.60%
发文量
20
审稿时长
>12 weeks
期刊介绍: AP is an international, multidisciplinary journal devoted to pharmaceutical and allied sciences and contains articles predominantly on core biomedical and health subjects. The aim of AP is to increase the impact of pharmaceutical research in academia, industry and laboratories. With strong emphasis on quality and originality, AP publishes reports from the discovery of a drug up to clinical practice. Topics covered are: analytics, biochemistry, biopharmaceutics, biotechnology, cell biology, cell cultures, clinical pharmacy, drug design, drug delivery, drug disposition, drug stability, gene technology, medicine (including diagnostics and therapy), medicinal chemistry, metabolism, molecular modeling, pharmacology (clinical and animal), peptide and protein chemistry, pharmacognosy, pharmacoepidemiology, pharmacoeconomics, pharmacodynamics and pharmacokinetics, protein design, radiopharmaceuticals, and toxicology.
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