COMPETITIVE-INHIBITION BETWEEN FOLIC-ACID AND METHOTREXATE FOR TRANSPORT CARRIER IN THE RAT SMALL-INTESTINE

被引：15

作者：

CHUNGI, VS ^{[1
]}

BOURNE, DWA ^{[1
]}

DITTERT, LW ^{[1
]}

机构：

[1] UNIV KENTUCKY,COLL PHARM,LEXINGTON,KY 40506

来源：

JOURNAL OF PHARMACEUTICAL SCIENCES | 1979年 / 68卷 / 12期

关键词：

Antineoplastic agents—methotrexate; absorption; rat small intestine; competitive inhibition by folic acid; Folic acid—absorption; competitive inhibition by methotrexate; Intestinal absorption—folic acid; methotrexate; competitive inhibition; rats; Methotrexate—absorption;

D O I：

10.1002/jps.2600681225

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Folic acid absorption from the lumen of the rat small intestine in situ obeyed Michaelis‐Menten kinetics. The values of Vmax and Km for absorption were 4.63 × 10−7 M/min and 1.21 × 10−6 M, respectively. Folic acid and methotrexate were mutual competitive inhibitors of absorption. Their Ki values were 1.28 × 10−6 and 1.9 × 10−5 M, respectively. Copyright © 1979 Wiley‐Liss, Inc., A Wiley Company

引用

页码：1552 / 1553

页数：2

共 14 条

[1] CHELLO PL, 1977, CANCER RES, V37, P4297
[2] DRUG ABSORPTION .8. KINETICS OF GI ABSORPTION OF METHOTREXATE
CHUNGI, VS
BOURNE, DWA
DITTERT, LW
[J]. JOURNAL OF PHARMACEUTICAL SCIENCES, 1978, 67 (04) : 560 - 561
[3] THE DETERMINATION OF ENZYME INHIBITOR CONSTANTS
DIXON, M
[J]. BIOCHEMICAL JOURNAL, 1953, 55 (01) : 170 - 171
[4] DIXON M, 1959, ENZYMES, P24
[5] DRUG ABSORPTION .I. AN IN SITU RAT GUT TECHNIQUE YIELDING REALISTIC ABSORPTION RATES
DOLUISIO, JT
BILLUPS, NF
DITTERT, LW
SUGITA, ET
SWINTOSKY, JV
[J]. JOURNAL OF PHARMACEUTICAL SCIENCES, 1969, 58 (10) : 1196 - +
[6] JEJUNAL UPTAKE OF TRITIATED FOLIC-ACID IN RAT STUDIED BY INVIVO PERFUSION
HALSTED, CH
BHANTHUMNAVIN, K
MEZEY, E
[J]. JOURNAL OF NUTRITION, 1974, 104 (12) : 1674 - 1680
[7] HEPNER GW, 1969, BRIT J HAEMATOL, V16, P241
[8] PLASMA-LEVELS OF METHOTREXATE IN CANCER-PATIENTS AS STUDIED BY AN IMPROVED SPECTROPHOTOFLUOROMETRIC METHOD
KINKADE, JM
VOGLER, WR
DAYTON, PG
[J]. BIOCHEMICAL MEDICINE, 1974, 10 (04): : 337 - 350
[9] KRAKOFF IH, 1971, DRILLS PHARMACOLOGY, P1595
[10] The determination of enzyme dissociation constants
Lineweaver, H
Burk, D
[J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1934, 56 : 658 - 666

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