Abstract:Objective To measure and analyze the oil-water partition coefficients and intestinal absorption characteristics of deoxyandrographolide in rats. Methods The shaking method and rat intestinal perfusion model in vivo was used. Oil-water partition coefficient, chemical and biological stability were measured by UPLC, and contents in intestinal perfusate and bile were determined. Results Oil water partition coefficient Log P=1.45±0.12 of deoxyandrographolide in the HBSS (pH 6.5), and its chemical and biological stability were well. In the perfusion model, the absorption of deoxyandrographolide in duodenum, jejunum, ileum and colon were 30.29%, 28.39%, 22.04% and 34.63%. On the other hand, deoxyandrographolide was excreted by bile with 0.146% of total prefused amount of deoxyandrographolide. Conclusion Deoxyandrographolide in various intestinal segments of rats are absorbed, but there is no significant difference on absorption rate in different intestinal segments.
伍治中1 叶玲2. 去氧穿心莲内酯的大鼠肠吸收特征研究[J]. 中国医药导报, 2017, 14(16): 8-11.
WU Zhizhong1 YE Ling2. Study on the intestinal absorption characteristics of deoxydeoxyandrographolide in rats. 中国医药导报, 2017, 14(16): 8-11.
[1] 吕巧,涂国刚,王嘉琦,等.穿心莲内酯的研究进展及临床应用[J].南昌大学学报,2013,53(1):83-86.
[2] Rollinger JM,Schyschka L. Neoandrographolide from Andrographis paniculata as a Potential Natural Chemosensitizer [J]. Planta Medica,2015,76(15):1698-1700.
[3] Fau-Takano F. Suppression of NO production in activated macrophages in vitro and ex vivo by neoandrographolide isolated from Andrographis paniculata [J]. Biol Pharm Bull,2014,25(16):1169-1174.
[4] 华素,李园园,赵军利.穿心莲提取物中穿心莲内酯和脱水穿心莲内酯大鼠肠吸收特性研究[J].中草药,2014,45(21):25-29.
[5] 廖琼峰,姚媛,谢智勇.穿心莲内酯在Caco-2细胞单层模型中的吸收机制[J].中草药,2011,42(7):1363-1366.
[6] 颜隆,朱建平.中药剂型理论的现代药物动力学诠释[J].世界中西医结合杂志,2015,10(2):262-267.
[7] 莫李立,王素军.口服药物吸收模型的研究进展[J].广东药学院学报,2011,27(1):123-134.
[8] 张字城,李新,李琳琳.动物肠吸收模型在药物研发中的应用[J].医学综述,2015,21(5):775-778.
[9] Tak?觃cs-Novak K,Avdeef A. Interlaboratory study of log P determination by shake-flask and potentiometric methods [J]. J Pharm Biomed Anal,1996,14(11):1405-1413.
[10] Kataoka,Itsubata,Masaoka,et al. In vitro discussion/permeation system to predict the oral absorption of poorly water-soluble drugs:effect of food and dose strength on it [J]. Bio Pharm Bull,2011,34(3):401-407.
[11] 王明娟,何风艳,郑笑为.消炎利胆片中穿心莲内酯、脱水穿心莲内酯及其总量测定能力验证项目的结果分析[J].中国药事,2014,28(9):981.
[12] Ye L,Liang FG. Oral bioavailability and intestinal disposition of dehydroandrographolide in rats [J]. J South Med Univ,012,32(8):1074-1080.
[13] 李兴平,李东晓,邓文龙.脱水穿心莲内酯、穿心莲内酯的鼠胃肠吸收研[J].中药药理与临床,2011,27(1):14-15.
[14] Wang Y,Chen YH,Xu H,et al. Analgesic effects of glycoproteins from Panax ginseng root in mice [J]. J Ethnopharmacol,2013,148(3):946-960.
[15] Escribano E,Sala XG,Salamanca J,et al. Single-pass intestinal perfusion to establish the intestinal permeability of model drugs in mouse [J]. Int J Pharm,2012,436(2):472-477.
[16] Ye L,Wang T,Tang L,et al. Poor oral bioavailability of a promising anticancer agent andrographolide is due to extensive metabolism and efflux by P-glycoprotein [J]. Pharm Sci,2011,100(11):5007-5017.
[17] 叶玲,梁福贵,杨晓珊,等.脱水穿心莲内酯在大鼠体内的口服生物利用度和肠道处置[J].南方医科大学学报,2012,32(8):1074-1081.
[18] 张红星.穿心莲叶含量对药材质量影响的研究[J].中国现代药物应用,2015,9(5):265-266.
[19] Tremblay YD,Lamarche D,Chever P,et al. Characterization of the ability of coagulase- negative staphylococci isolated from the milk of Canadian farms to form biofilms [J]. J Dairy Sci,2013,96(1):234-236.
[20] Ma Y,Sun S,Peng CK. Applications of dynamical complexity theory in traditional Chinese medicine [J]. Front Med,2014,8(3):279-284.