目的 考察聚乙二醇琥珀酸酯1000(TPGS 1000)与Soluplus对人参皂苷CK在Caco-2细胞模型上转运的影响。方法 采用Caco-2 细胞模型研究不同浓度的聚乙二醇琥珀酸酯1000与Soluplus对人参皂苷CK细胞转运行为的影响,以超高压液相色谱法(UPLC)测定细胞样品溶液中人参皂苷CK的浓度,计算表观渗透系数(Papp)与外排比率。结果 当人参皂苷CK与聚乙二醇琥珀酸酯1000或Soluplus质量比例分别为1∶1、1∶3和1∶9时,人参皂苷CK吸收显著增加,外排显著降低,外排比率也随之显著下降(P<0.05);在相同比例条件下,聚乙二醇琥珀酸酯1000对人参皂苷CK的促吸收效果和抑制外排效果均优于Soluplus(P<0.05)。结论 在Caco-2细胞模型上,聚乙二醇琥珀酸酯1000与Soluplus均可显著促进人参皂苷CK的吸收,有希望应用于CK制剂的开发中。
Abstract
OBJECTIVE To examine the effects of TPGS 1000 and Soluplus on the transport of ginsenoside CK in Caco-2 cell model. METHODS The effects of TPGS 1000 and Soluplus at different concentrations on ginsenoside CK were evaluated by using Caco-2 cell model. The concentration of ginsenoside CK in cell was examined by ultra high pressure liquid chromatography (UPLC) method. The apparent permeability coefficient (Papp) and the efflux ratio were calculated. RESULTS When the proportion of ginsenoside CK to TPGS 1000 or Soluplus was 1∶1, 1∶3, and 1∶9, the absorption of ginsenoside CK significantly increased. The efflux and efflux ratio both decreased significantly(P<0.05). TPGS 1000 had more significant promotion effect on the transport of ginsenoside CK than the same dose of soluplus at the same ratio (P<0.05). CONCLUSION In Caco-2 cell model, both TPGS 1000 and Soluplus can significantly promote the absorption of ginsenoside CK.
关键词
人参皂苷CK /
Caco-2 细胞模型 /
聚乙二醇琥珀酸酯1000 /
Soluplus /
肠道吸收
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Key words
ginsenoside CK /
Caco-2 cell model /
TPGS 1000 /
soluplus /
intestinal absorption
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中图分类号:
R944
R965
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参考文献
[1] LEE J, LEE E, KIM D, et al. Studies on absorption, distribution and metabolism of ginseng in humans after oral administration[J]. J Ethnopharmacol, 2009,122(1):143-148.
[2] GAN C W, CHIEN S, FENG S S. Nanomedicine: Enhancement of chemotherapeutical efficacy of docetaxel by using a biodegradable nanoparticle formulation[J]. Curr Pharm Design, 2010,16:2308-2320.
[3] ZHANG Z, FENG S S. Self-assembled nanoparticles of poly(lactide) - Vitamin E TPGS copolymers for oral chemotherapy[J]. Int J Pharm, 2006,324(2): 191-198.
[4] LINN M, COLLNOT E M, DJURIC D, et al. Soluplus as an effective absorption enhancer of poorly soluble drugs in vitro and in vivo[J]. Eur J Pharm Sci, 2012, 45(3):336-343.
[5] ZHANG M, LI H, LANG B, et al. Formulation and delivery of improved amorphous fenofibrate solid dispersions prepared by thin film freezing[J]. Eur J Pharm Biopharm, 2012, 82(3): 534-544.
[6] WU M, DENG M Y, GUO R, et al .Transport characteristics and absorption promoting methods of bergenin across Caco-2 cell monolayer model[J]. Chin Pharm J(中国药学杂志), 2013,48(13): 1083-1087.
[7] ZHENG N N, WU L H, TANG J L. Advance in application of D-α-tocopherol polyethyleneglycol succinate in the field of pharmaceutics[J]. Chin Pharm J (中国药学杂志), 2014,49(16):1373-1376.
[8] KRASAVAGE W J, TERHAAR C J. D-alpha-tocopheryl polyethylene glycol 1000 succinate. Acute toxicity, subchronic feeding, reproduction and teralogic studies in the rat[J]. J Agric Food Chem, 1977,25(2):273-278.
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脚注
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基金
国家自然科学基金资助项目(81403119)
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