氟苯尼考磷脂复合物的制备及对氟苯尼考在大鼠小肠吸收的影响
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- 英文论文题名：Development of Florfenicol Phospholipid Complex and its Effect on Florfenicol Absorption in Rat Small Intestinal
- 论文作者：符华林 ; 刘梦娇 ; 刘梦喜 ; 凡国庆
- 英文论文作者：FU Hualin ; LIU Mengjiao ; LIU Mengxi ; FAN Guoqing ; Innovative Engineering Research Center of Veterinary Pharmaceutics ; Department of Pharmacy ; College of Veterinary Medicine ; Sichuan Agricultural University
- 年：2016
- 作者机构：四川农业大学动物医学院药学系兽药创新制剂工程技术研究中心;
- 论文关键词：氟苯尼考 ; 磷脂复合物 ; 外翻肠囊法 ; 在体肠灌流法
- 英文论文关键词：florfenicol ; phospholipid complex ; everted gut sac ; one-way intestinal perfusion model
- 会议召开时间：2016-09-18
- 会议录名称：中国畜牧兽医学会动物药品学分会第五届全国会员代表大会暨2016年学术年会论文集
- 语种：中文
- 分类号：S859.79
- 学会代码：ZGXJ
- 会议名称：中国畜牧兽医学会动物药品学分会第五届全国会员代表大会暨2016年学术年会
- 会议地点：中国四川成都
- 主办单位：中国畜牧兽医学会动物药品学分会
- 学会名称：中国畜牧兽医学会
- 页数：6
- 文件大小：463k
- 原文格式：O
- 会议级别：全国
摘要
采用溶剂挥发法制备氟苯尼考磷脂复合物,并用平衡法测定氟苯尼考及其磷脂复合物的溶解度和脂水分配系数,采用离体外翻肠囊法研究氟苯尼考及其磷脂复合物在不同肠段的吸收情况,同时采用大鼠单向在体肠灌流法重点考察氟苯尼考及其磷脂复合物在十二指肠的吸收差异。结果显示氟苯尼考磷脂复合物较氟苯尼考原药的溶解度提高了36.14%,脂水分配系数降低了47.62%,且在大鼠小肠各段的促进吸收率大小表现为十二指肠>回肠>空肠。氟苯尼考磷脂复合物在十二指肠的表观吸收系数(P_(app))、有效渗透系数(P_(eff))和吸收速率常数(K_a)较氟苯尼考原药分别增加了121.93%、109.48%和90.83%。结果表明氟苯尼考磷脂复合物可以促进氟苯尼考在大鼠小肠中的吸收。
Solvent evaporation method was used to prepare florfenicol phospholipid complex,and the solubility and lipid water partition coefficient of the florfenicol and its phospholipid complex were measured by using the balance method.In addition,the everted gut sac method was adopted to investigate the absorption of florfenicol and its phospholipid in different intestine.Meanwhile,one-way intestinal perfusion model was applied to highly investigate the difference of absorption of florfenicol and its phospholipid complex in the duodenum.Results show that the solubility of florfenicol phospholipid complex increased 36.14%,lipid water partition coefficient reduced 47.62%compared with florfenicol,moreover,the promote absorption rate in rat small intestine was:duodenum > ileum > jejunum.Beside,compared with florfenicol,the apparent absorption coefficient(p_(opp)),effective permeability coefficient(P_(eff)) and absorption rate constant(K_a) of the duodenum of florfenicol phospholipid complex increased121.93%,109.48%and 90.83%,respectively.Results suggest that florfenicol phospholipid complex can promote florfenicol absorption in the rat small intestine.
Solvent evaporation method was used to prepare florfenicol phospholipid complex,and the solubility and lipid water partition coefficient of the florfenicol and its phospholipid complex were measured by using the balance method.In addition,the everted gut sac method was adopted to investigate the absorption of florfenicol and its phospholipid in different intestine.Meanwhile,one-way intestinal perfusion model was applied to highly investigate the difference of absorption of florfenicol and its phospholipid complex in the duodenum.Results show that the solubility of florfenicol phospholipid complex increased 36.14%,lipid water partition coefficient reduced 47.62%compared with florfenicol,moreover,the promote absorption rate in rat small intestine was:duodenum > ileum > jejunum.Beside,compared with florfenicol,the apparent absorption coefficient(p_(opp)),effective permeability coefficient(P_(eff)) and absorption rate constant(K_a) of the duodenum of florfenicol phospholipid complex increased121.93%,109.48%and 90.83%,respectively.Results suggest that florfenicol phospholipid complex can promote florfenicol absorption in the rat small intestine.
引文
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[15]高秀蓉,蒋学华,杜青青.基于Caco-2细胞模型研究蝙蝠葛碱的跨膜吸收机制[J].中国实验方剂学杂志.2012(15):139-143.
[16]Sangsen Y,Wiwattanawongsa K,Likhitwitayawuid K,et al.Influence of surfactants in self-microemulsifying formulations on enhancing oral bioavailability of oxyresveratrol:Studies in Caco-2 cells and in vivo[J].International Journal of Pharmaceutics.2016,498(1-2):294-303.
[2]李仲谨,田晓静,杨威.氟苯尼考淀粉微球的制备及缓释性能的研究[J].食品工业科技.2011(02):205-207.
[3]魏海涛,方秋华,曾振灵,等.氟苯尼考药剂学研究进展[J].中国兽药杂志.2010(07):44-46.
[4]刘九生.氟苯尼考的研究进展及临床应用[J].兽医导刊.2008(04):31-34.
[5]刘洋,赵修华,祖元刚,等.氟苯尼考PEG 6000固体分散体的无溶剂熔融法制备与分析[J].中国兽药杂志.2012(04):40-43.
[6]孙秀漫,杜俊楠,刘光辉,等.采用外翻肠囊法研究枇杷叶紫珠中毛蕊花糖苷的肠吸收特性[J].中成药.2013(09):1888-1891.
[7]黄嗣航,龙晓英,袁飞,等.酚红法和改良重量法分别研究葛根素的大鼠在体肠吸收机制[J].广东药学院学报.2012(06):603-607.
[8]王大为,张基,李沛,等.在体肠灌流模型研究灵仙新苷的大鼠肠吸收特性[J].中国新药杂志.2012(07):800-803.
[9]黄嗣航,龙晓英,袁飞,等.盐酸小檗碱的溶解度及油水分配系数与大鼠在体肠吸收之间的相关性研究[J].中国现代应用药学.2012(03):233-238.
[10]Rathore R,Jain J P,Srivastava A,et al.Simultaneous determination of hydrazinocurcumin and phenol red in samples from rat intestinal permeability studies:HPLC method development and validation[J].Journal of Pharmaceutical and Biomedical Analysis.2008,46(2):374-380.
[11]Sugano K.Fraction of a dose absorbed estimation for structurally diverse low solubility compounds[J].International Journal of Pharmaceutics.2011,405(1-2):79-89.
[12]陈新民,李俊松,李文,等.五味子有效成分的大鼠在体单向灌流肠吸收[J].药学学报.2010(05):652-658.
[13]Muir A H,Robb R,Mclaren M,et al.The use of Ginkgo biloba in Raynaud's disease:a double-blind placebo-controlled trial[J].Vascular Medicine.2002,7(4):265-267.
[14]陈晓艳,刘扬,张玮,等.去甲基斑蝥素纳米粒大鼠体肠吸收动力学研究[J].抗感染药学.2009(03):149-152.
[15]高秀蓉,蒋学华,杜青青.基于Caco-2细胞模型研究蝙蝠葛碱的跨膜吸收机制[J].中国实验方剂学杂志.2012(15):139-143.
[16]Sangsen Y,Wiwattanawongsa K,Likhitwitayawuid K,et al.Influence of surfactants in self-microemulsifying formulations on enhancing oral bioavailability of oxyresveratrol:Studies in Caco-2 cells and in vivo[J].International Journal of Pharmaceutics.2016,498(1-2):294-303.