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口服不同脂质体制剂后,葛根素经淋巴管转运至意识性淋巴管插管大鼠体内。

Lymphatic transport of puerarin occurs after oral administration of different lipid-based formulations to unconscious lymph duct-cannulated rats.

机构信息

Department of Pharmaceutics, Anhui University of Chinese Medicine , Anhui Province , China .

出版信息

Pharm Dev Technol. 2014 Sep;19(6):743-7. doi: 10.3109/10837450.2013.829093. Epub 2013 Aug 27.

Abstract

This study investigated the potential of targeted intestinal lymphatic transport of puerarin via a lipid formulation approach. Three formulations of PEG nanoemulsion, nanosuspension and an oil suspension containing puerarin were examined with the lymph-cannulated anaesthetized rat model. Plasma and lymph samples were analyzed by HPLC. Lymph triglyceride was measured using an enzymatic colorimetric technique. After 8 h, the total administered dose accumulated in the thoracic lymph duct was analyze. Nanoemulsion, nanosuspension and oil suspension was 0.065 ± 0.006%, 0.137 ± 0.018%, 0.021 ± 0.002% of the administered dose, respectively. In nanoemulsion, nanosuspension and oil suspension group, the systemic bioavailability of oral puerarin was 11%, 16% and 11% for lymph-cannulated rats, 41%, 67% and 18% for control rats. Absorption into the intestinal lymph should thus contribute to ∼30%, 51% and 7% of the systemic bioavailable puerarin. This data indicated that lipid-based nano drug formulation produced higher lymph concentrations of puerarin than oil suspension. The nanosuspension formulation may be considerable in terms of increased local concentrations in lymphoid tissue.

摘要

本研究通过脂质体制剂方法探讨了葛根素靶向肠道淋巴转运的潜力。采用淋巴插管麻醉大鼠模型,考察了三种 PEG 纳米乳、纳米混悬液和含葛根素的油混悬液制剂。采用 HPLC 法分析血浆和淋巴样品,用酶比色法测定淋巴甘油三酯。8 小时后,分析胸导管中累积的总给药剂量。纳米乳、纳米混悬液和油混悬液的给药剂量分别为 0.065±0.006%、0.137±0.018%和 0.021±0.002%。在纳米乳、纳米混悬液和油混悬液组中,淋巴插管大鼠口服葛根素的系统生物利用度分别为 11%、16%和 11%,而对照组大鼠分别为 41%、67%和 18%。因此,肠道淋巴吸收约占系统生物利用葛根素的 30%、51%和 7%。这些数据表明,基于脂质的纳米药物制剂可使葛根素在淋巴中的浓度高于油混悬液。纳米混悬剂制剂在增加淋巴组织中的局部浓度方面可能具有重要意义。

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