丹参提取物磷脂复合物的制备及在体肠吸收研究
|
摘要
目的:制备丹参提取物磷脂复合物(DTPLC)并对其基本性质进行考察,研究丹参提取物磷脂复合物在大鼠各个肠段的吸收情况。方法:以甲醇为反应溶剂,加入丹参提取物(DT)与大豆磷脂,搅拌至澄清,减压干燥,得到粉末状磷脂复合物;采用UV、IR等手段考察DTPLC的理化性质;测量计算DTPLC的平衡溶解度和油水分配系数;对比DT与DTPLC的肠吸收差异,明确DTPLC在大鼠肠段的吸收部位、药物浓度与吸收速率。结果:研究表明,DTPLC是以非共价键结合,未形成新的化合物;DTPLC的表观溶解度和油水分配系数均有不同程度提高;与DT相比,DTPLC的吸收参数均大于DT,且DTPLC在大鼠回肠的吸收参数最高;对于不同质量浓度的DTPLC吸收情况显示,吸收参数变化不明显,不具有统计学差异。结论:DTPLC的形成并未产生新的吸收峰,而对其脂溶性有了明显改善,DTPLC的吸收均较提取物效果明显提高。
Objective:To prepare phospholipid complex of Salvia miltiorrhiza extract(DTPLC)and inspect its physicochemical properties,and to study the absorption of Salvia miltiorrhiza extract phospholipid complex in different intestinal segments of rats.Methods:Using methanol as the reaction solvent,Salvia miltiorrhiza extract and phospholipid were resolved into the medium,when the organic solvent was clear,phospholipid complex was obtained by vacuum drying;The physicochemical properties of DTPLC were studied by UV and IR;The equilibrium solubility and oil-water distribution coefficient of DTPLC were measured and calculated;The differences in intestinal absorption between DT and DTPLC were compared,and the absorption site,drug concentration and absorption rate of DTPLC in the intestine segment of rats were determined.Results:DTPLC was combined by non-covalent-bonded,not forming a new compound,the apparent solubility and oil-water distribution coefficients of DTPLC were effectively enhanced.Compared with the DT,the absorption parameters of DTPLC were greater than DT,and DTPLC had the highest absorption parameters in ileum of rats.The absorption of DTPLC at different concentrations showed that the absorption parameters did not change significantly,and there were no statistical differences.Conclusion:The formation of DTPLC does not produce new absorption peaks,but its liposoluble property is improved significantly.The absorption of DTPLC is better than that of the extract.
Objective:To prepare phospholipid complex of Salvia miltiorrhiza extract(DTPLC)and inspect its physicochemical properties,and to study the absorption of Salvia miltiorrhiza extract phospholipid complex in different intestinal segments of rats.Methods:Using methanol as the reaction solvent,Salvia miltiorrhiza extract and phospholipid were resolved into the medium,when the organic solvent was clear,phospholipid complex was obtained by vacuum drying;The physicochemical properties of DTPLC were studied by UV and IR;The equilibrium solubility and oil-water distribution coefficient of DTPLC were measured and calculated;The differences in intestinal absorption between DT and DTPLC were compared,and the absorption site,drug concentration and absorption rate of DTPLC in the intestine segment of rats were determined.Results:DTPLC was combined by non-covalent-bonded,not forming a new compound,the apparent solubility and oil-water distribution coefficients of DTPLC were effectively enhanced.Compared with the DT,the absorption parameters of DTPLC were greater than DT,and DTPLC had the highest absorption parameters in ileum of rats.The absorption of DTPLC at different concentrations showed that the absorption parameters did not change significantly,and there were no statistical differences.Conclusion:The formation of DTPLC does not produce new absorption peaks,but its liposoluble property is improved significantly.The absorption of DTPLC is better than that of the extract.
引文
[1] 国家药典委员会.中华人民共和国药典[S].一部.北京:中国医药科技出版社,2015:678.
[2] 张聪,韩晓锦.丹参药材-中间体-丹参片的HPLC指纹图谱及其相关性研究[J].中成药,2010,32(10):1656-1662.
[3] 巫剑锋,邱佩斯,陈彦雯,等.丹参提取物固体分散体的制备与溶出特性[J].中国医院药学杂志,2010,30(11):900-905.
[4] Lin R,Wang WR,Liu JT,et al.Protective effect of tanshinone ⅡA on human umbilical vein endothelial cell injured by hydrogen peroxide and its mechanism[J].J Ethnopharmacol,2006,108(2):217-222.
[5] 李素春,刘建平,曾昭征,等.丹参酮ⅡA溶解渗透性以及常用辅料对其增溶促渗的研究[J].时珍国医国药,2008,19(7):1724-1726.
[6] Hao HP,Wang GJ,Cui N,et al.Pharmacokinetics,absorption and tissue distribution of tanshinone ⅡA solid[J].Planta Med,2006,72(14):1311-1317.
[7] Kim CK,Cho YJ,Gao ZG.Preparation and evaluation of salvianolic acid B microemulsions for oral delivery[J].J Control Release,2001,70:149-155.
[8] 孙静,史亚军,张小飞,等.丹参片提取物磷脂复合物的制备及初步吸收评价[J].中药材,2017,40(1):164-166.
[9] 郁丹红,贾晓斌.相似性分析用于丹参二萜醌组分平衡溶解度和油水分配系数的研究[J].中国中药杂志,2013,38(12):1860-1864.
[10] 邢建国,谢敏,王新春,等.天山雪莲提取物平衡溶解度和表观油水分配系数的测定[J].中国医院药学杂志,2013,33(1):26-28.
[11] 唐灿.中药肠吸收动力学的研究-灯盏花素肠吸收动力学的研究[D].成都:成都中医药大学,2004.
[12] 周冬菊,赵会英,杨英禄.大鼠小肠对葛根素吸收的动力学研究[J].北京化工大学学报,2006,33(5):106-109.
[13] 徐术,刘忠良,胡晋红.药物肠吸收的实验研究方法概述[J].中国药房,2009,20(16):1266-1268.
[14] 李凌军,李季,娄华伟.天钩降压胶囊中黄芩苷大鼠在体肠吸收研究[J].中国中药杂志,2013,38(6):894-898.
[15] 焦放,侯子言,尹登科,等.黄连水煎液中固体微粒对小檗碱在体肠吸收特性的影响研究[J].中草药,2016,47(8):1357-1360.
[2] 张聪,韩晓锦.丹参药材-中间体-丹参片的HPLC指纹图谱及其相关性研究[J].中成药,2010,32(10):1656-1662.
[3] 巫剑锋,邱佩斯,陈彦雯,等.丹参提取物固体分散体的制备与溶出特性[J].中国医院药学杂志,2010,30(11):900-905.
[4] Lin R,Wang WR,Liu JT,et al.Protective effect of tanshinone ⅡA on human umbilical vein endothelial cell injured by hydrogen peroxide and its mechanism[J].J Ethnopharmacol,2006,108(2):217-222.
[5] 李素春,刘建平,曾昭征,等.丹参酮ⅡA溶解渗透性以及常用辅料对其增溶促渗的研究[J].时珍国医国药,2008,19(7):1724-1726.
[6] Hao HP,Wang GJ,Cui N,et al.Pharmacokinetics,absorption and tissue distribution of tanshinone ⅡA solid[J].Planta Med,2006,72(14):1311-1317.
[7] Kim CK,Cho YJ,Gao ZG.Preparation and evaluation of salvianolic acid B microemulsions for oral delivery[J].J Control Release,2001,70:149-155.
[8] 孙静,史亚军,张小飞,等.丹参片提取物磷脂复合物的制备及初步吸收评价[J].中药材,2017,40(1):164-166.
[9] 郁丹红,贾晓斌.相似性分析用于丹参二萜醌组分平衡溶解度和油水分配系数的研究[J].中国中药杂志,2013,38(12):1860-1864.
[10] 邢建国,谢敏,王新春,等.天山雪莲提取物平衡溶解度和表观油水分配系数的测定[J].中国医院药学杂志,2013,33(1):26-28.
[11] 唐灿.中药肠吸收动力学的研究-灯盏花素肠吸收动力学的研究[D].成都:成都中医药大学,2004.
[12] 周冬菊,赵会英,杨英禄.大鼠小肠对葛根素吸收的动力学研究[J].北京化工大学学报,2006,33(5):106-109.
[13] 徐术,刘忠良,胡晋红.药物肠吸收的实验研究方法概述[J].中国药房,2009,20(16):1266-1268.
[14] 李凌军,李季,娄华伟.天钩降压胶囊中黄芩苷大鼠在体肠吸收研究[J].中国中药杂志,2013,38(6):894-898.
[15] 焦放,侯子言,尹登科,等.黄连水煎液中固体微粒对小檗碱在体肠吸收特性的影响研究[J].中草药,2016,47(8):1357-1360.