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体外脂解模型在脂质制剂评价中的研究进展

吴慧仪 龙晓英

吴慧仪, 龙晓英. 体外脂解模型在脂质制剂评价中的研究进展[J]. 药学实践与服务, 2017, 35(6): 481-484,489. doi: 10.3969/j.issn.1006-0111.2017.06.001
引用本文: 吴慧仪, 龙晓英. 体外脂解模型在脂质制剂评价中的研究进展[J]. 药学实践与服务, 2017, 35(6): 481-484,489. doi: 10.3969/j.issn.1006-0111.2017.06.001
WU Huiyi, LONG Xiaoying. Research progress on in vitro lipolysis model for the evaluation of lipid formulations[J]. Journal of Pharmaceutical Practice and Service, 2017, 35(6): 481-484,489. doi: 10.3969/j.issn.1006-0111.2017.06.001
Citation: WU Huiyi, LONG Xiaoying. Research progress on in vitro lipolysis model for the evaluation of lipid formulations[J]. Journal of Pharmaceutical Practice and Service, 2017, 35(6): 481-484,489. doi: 10.3969/j.issn.1006-0111.2017.06.001

体外脂解模型在脂质制剂评价中的研究进展

doi: 10.3969/j.issn.1006-0111.2017.06.001
基金项目: 国家自然科学基金资助项目(81373361);广东省自然基金资助项目(S2013020012980)

Research progress on in vitro lipolysis model for the evaluation of lipid formulations

  • 摘要: 体外脂解模型能模拟体内胃肠道生理环境,较好地反映脂质制剂口服后在人体肠道的性质,是一种具有应用前景的筛选和评价口服脂质制剂的新方法。综述脂质制剂的特性、胃肠道消化过程、体外脂解模型的应用及脂解液表征方法的研究进展,为脂解模型在脂质制剂口服吸收机制及体内外相关性研究中的深入应用提供依据。
  • [1] Pouton CW. Formulation of poorly water-soluble drugs for oral administration:Physicochemical and physiological issues and the lipid formulation classification system[J]. Eur J Pharm Sci, 2006, 29(3-4):278-287.
    [2] Porter CJ, Pouton CW, Cuine JF, et al. Enhancing intestinal drug solubilisation using lipid-based delivery systems[J]. Adv Drug Deliv Rev, 2008, 60(6):673-691.
    [3] Pouton CW. Lipid formulations for oral administration of drugs:non-emulsifying, self-emulsifying and self-microemulsifying' drug delivery systems[J]. Eur J Pharm Sci, 2000, 11(Suppl 2):S93-98.
    [4] Carri re F. Impact of gastrointestinal lipolysis on oral lipid-based formulations and bioavailability of lipophilic drugs[J]. Biochimie. 2016, 125:297-305.
    [5] Kalantzi L, Persson E, Polentarutti B, et al. Canine intestinal contents vs. simulated media for the assessment of solubility of two weak bases in the human small intestinal contents[J]. Pharm Res, 2006, 23(6):1373-1381.
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    [9] Nordskog BK, Phan CT, Nutting DF, et al. An examination of the factors affecting intestinal lymphatic transport of dietary lipids[J]. Adv Drug Deliv Rev, 2001, 50(1-2):21-44.
    [10] Mattson FH, Benedict JH, Martin JB, et al. Intermediates formed during the digestion of triglycerides[J]. J Nutr, 1952, 48(3):335-344.
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    [14] Zangenberg NH, Mullertz A, Kristensen HG, et al. A dynamic in vitro lipolysis model.Ⅱ:evaluation of the model[J]. Eur J Pharm Sci, 2001, 14(3):237-244.
    [15] Porter CJ, Trevaskis NL, Charman WN. Lipids and lipid-based formulations:Optimizing the oral delivery of lipophilic drugs[J]. Nat Rev Drug Discov, 2007, 6(3):231-248.
    [16] Fatouros DG, Müllertz A. In vitro lipid digestion models in design of drug delivery systems for enhancing oral bioavailability[J]. Expert Opin Drug Metab Toxicol, 2008, 4(1):65-76.
    [17] 曾棋平, 张晶, 刘志宏, 等. 脂解模型在脂质给药系统体外评价中的应用研究进展[J]. 药学实践杂志, 2014, 32(2):85-87.
    [18] Dening TJ, Rao S, Thomas N, et al. Montmorillonite-lipid hybrid carriers for ionizable and neutral poorly water-soluble drugs:Formulation, characterization and in vitro lipolysis studies[J]. Int J Pharm, 2017, 526(1):95-105.
    [19] Kazi M, Al-Qarni H, Alanazi FK. Development of oral solid self-emulsifying lipid formulations of risperidone with improved in vitro dissolution and digestion[J]. Eur J Pharm Biopharm, 2017, 114:239-249.
    [20] 林婉婷, 龙晓英, 吴慧仪, 等. 灰黄霉素纳米乳体外脂解过程中药物动态分布研究[J]. 中国药学杂志, 2015, 50(6):512-520.
    [21] Xiao L, Yi T, Liu Y, et al. The in vitro lipolysis of lipid-based drug delivery systems:A newly identified relationship between drug release and liquid crystalline phase[J]. Biomed Res Int, 2016,2016:2364317.
    [22] Siqueira SD, M llertz A, Gr eser K, et al. Influence of drug load and physical form of cinnarizine in new SNEDDS dosing regimens:in vivo and in vitro evaluations[J]. AAPS J. 2017, 19(2):587-594.
    [23] Tanaka Y, Hara T, Waki R, et al. Regional differences in the components of luminal water from rat gastrointestinal tract and comparison with other species[J]. J Pharm Pharm Sci, 2012, 15(4):510-518.
    [24] Fatouros DG, Bergenstahl B, Mullertz A. Morphological observations on a lipid-based drug delivery system during in vitro digestion[J]. Eur J Pharm Sci, 2007, 31(2):85-94.
    [25] Roshan GD, Aagaard AE, Pedersen JS, et al. Experimental Set-up with flow-through cell with SAXS studies of in-situ degradation of drug formulations under gastro-intestinal mimicking conditions[R]. 13th International Conference of Small Angle Scattering, Kyoto:2006.
    [26] Sassene PJ, Knopp MM, Hesselkilde JZ, et al. Precipitation of a poorly soluble model drug during in vitro lipolysis:characterization and dissolution of the precipitate[J]. J Pharm Sci, 2010, 99(12):4982-4991.
    [27] Fernandez S, Jannin V, Chevrier S, et al. In vitro digestion of the self-emulsifying lipid excipient Labrasol by gastrointestinal lipases and influence of its colloidal structure on lipolysis rate[J]. Pharm Res, 2013, 30(12):3077-3087.
  • [1] 王耀振, 徐灿, 吕顺莉, 田泾, 张东炜.  钾离子竞争性酸阻滞剂的药学特征研究进展 . 药学实践与服务, 2024, 42(7): 1-7. doi: 10.12206/j.issn.2097-2024.202306040
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出版历程
  • 收稿日期:  2017-04-07
  • 修回日期:  2017-09-04

体外脂解模型在脂质制剂评价中的研究进展

doi: 10.3969/j.issn.1006-0111.2017.06.001
    基金项目:  国家自然科学基金资助项目(81373361);广东省自然基金资助项目(S2013020012980)

摘要: 体外脂解模型能模拟体内胃肠道生理环境,较好地反映脂质制剂口服后在人体肠道的性质,是一种具有应用前景的筛选和评价口服脂质制剂的新方法。综述脂质制剂的特性、胃肠道消化过程、体外脂解模型的应用及脂解液表征方法的研究进展,为脂解模型在脂质制剂口服吸收机制及体内外相关性研究中的深入应用提供依据。

English Abstract

吴慧仪, 龙晓英. 体外脂解模型在脂质制剂评价中的研究进展[J]. 药学实践与服务, 2017, 35(6): 481-484,489. doi: 10.3969/j.issn.1006-0111.2017.06.001
引用本文: 吴慧仪, 龙晓英. 体外脂解模型在脂质制剂评价中的研究进展[J]. 药学实践与服务, 2017, 35(6): 481-484,489. doi: 10.3969/j.issn.1006-0111.2017.06.001
WU Huiyi, LONG Xiaoying. Research progress on in vitro lipolysis model for the evaluation of lipid formulations[J]. Journal of Pharmaceutical Practice and Service, 2017, 35(6): 481-484,489. doi: 10.3969/j.issn.1006-0111.2017.06.001
Citation: WU Huiyi, LONG Xiaoying. Research progress on in vitro lipolysis model for the evaluation of lipid formulations[J]. Journal of Pharmaceutical Practice and Service, 2017, 35(6): 481-484,489. doi: 10.3969/j.issn.1006-0111.2017.06.001
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