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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.
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    [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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    [7] Lowe ME. The triglyceride lipases of the pancreas[J]. J Lipid Res, 2002, 43(12):2007-2016.
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    [10] Mattson FH, Benedict JH, Martin JB, et al. Intermediates formed during the digestion of triglycerides[J]. J Nutr, 1952, 48(3):335-344.
    [11] Naylor LJ, Bakatselou V, Dressman JB. Comparison of the mechanism of dissolution of hydrocortisone in simple and mixed micelle systems[J]. Pharm Res, 1993, 10(6):865-870.
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    [13] Mu H, Hoy CE. The digestion of dietary triacylglycerols[J]. Prog Lipid Res, 2004, 43(2):105-133.
    [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.
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    [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.
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    [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.
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  • 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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