|
|
Study on the intestinal absorption characteristics of deoxydeoxyandrographolide in rats |
WU Zhizhong1 YE Ling2 |
1.Department of Pharmacy, Shenzhen Shahe Hospital, Guangdong Province, Shenzhen 518053, China;
2.College of Pharmacy, Southern Medical University, Guangdong Province, Guangzhou 510000, China |
|
|
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.
|
|
|
|
|
[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. |
|
|
|