ABSORPTION OF A VASOPRESSIN ANALOG, 1-DEAMINO-8-D-ARGININE-VASOPRESSIN (DDAVP), IN A HUMAN INTESTINAL EPITHELIAL-CELL LINE, CACO-2

被引:45
作者
LUNDIN, S [1 ]
ARTURSSON, P [1 ]
机构
[1] BIOMED CTR,DEPT PHARMACEUT,S-75123 UPPSALA,SWEDEN
关键词
Cell culture; Drug absorption; Enzymatic degradation; Intestine; Vasopressin;
D O I
10.1016/0378-5173(90)90267-8
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The intestinal absorption of the metabolically stable vasopressin analogue dDAVP was studied in human intestinal epithelial (CaCO-2) cells grown on permeable supports. The parent peptide arginine-vasopressin (AVP) was used as a control peptide. Both peptides displayed linear kinetics and were absorbed at very slow rates across CaCO-2 monolayers. The apparent permeability coefficients were in the range of 4-14 × 10-8 cm/s. No degradation of dDAVP and AVP was observed during the incubation period. The absorption of dDAVP was concentration independent, indicating that the transport was mediated by a passive permeation. The low permeability coefficients indicate that the absorption rate across CaCO-2 monolayers is similar to that of colonic epithelium in vivo. © 1990.
引用
收藏
页码:181 / 186
页数:6
相关论文
共 23 条
[1]   EPITHELIAL TRANSPORT OF DRUGS IN CELL-CULTURE .1. A MODEL FOR STUDYING THE PASSIVE DIFFUSION OF DRUGS OVER INTESTINAL ABSORPTIVE (CACO-2) CELLS [J].
ARTURSSON, P .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1990, 79 (06) :476-482
[3]   THE TRANSPORT OF VITAMIN-B12 THROUGH POLARIZED MONOLAYERS OF CACO-2 CELLS [J].
DIX, CJ ;
HASSAN, IF ;
OBRAY, HY ;
SHAH, R ;
WILSON, G .
GASTROENTEROLOGY, 1990, 98 (05) :1272-1279
[4]   127 CULTURED HUMAN TUMOR-CELL LINES PRODUCING TUMORS IN NUDE MICE [J].
FOGH, J ;
FOGH, JM ;
ORFEO, T .
JNCI-JOURNAL OF THE NATIONAL CANCER INSTITUTE, 1977, 59 (01) :221-226
[5]  
HIDALGO IJ, 1989, GASTROENTEROLOGY, V96, P736
[6]   MECHANISMS OF POLYETHYLENE GLYCOL-400 PERMEABILITY OF PERFUSED RAT INTESTINE [J].
KRUGLIAK, P ;
HOLLANDER, D ;
MA, TY ;
TRAN, D ;
DADUFALZA, VD ;
KATZ, KD ;
LE, K .
GASTROENTEROLOGY, 1989, 97 (05) :1164-1170
[7]  
KUBIAK TM, 1989, DRUG METAB DISPOS, V17, P393
[8]   A NEW EXTRACTION OF ARGININE VASOPRESSIN FROM BLOOD - THE USE OF OCTADECASILYL-SILICA [J].
LAROCHELLE, FT ;
NORTH, WG ;
STERN, P .
PFLUGERS ARCHIV-EUROPEAN JOURNAL OF PHYSIOLOGY, 1980, 387 (01) :79-81
[9]   USE OF 3 SPECIFIC RADIOIMMUNOASSAYS IN MEASURING NEUROHYPOPHYSEAL HORMONE CONTENT AND PLASMA-CONCENTRATIONS OF VASOPRESSIN, OXYTOCIN AND DDAVP IN RATS AFTER PROLONGED INFUSION OF DDAVP [J].
LUNDIN, S ;
MELIN, P ;
VILHARDT, H .
EXPERIENTIA, 1985, 41 (07) :933-935
[10]   ABSORPTION OF 1-DEAMINO-8-D-ARGININE VASOPRESSIN FROM DIFFERENT REGIONS OF THE GASTROINTESTINAL-TRACT IN RABBITS [J].
LUNDIN, S ;
VILHARDT, H .
ACTA ENDOCRINOLOGICA, 1986, 112 (03) :457-460