Online citations, reference lists, and bibliographies.
← Back to Search

Carrier Mediated Transport Of Amino Acids, Small Peptides, And Their Drug Analogs

P. Sinko, M. Hu, G. Amidon
Published 1987 · Chemistry

Cite This
Download PDF
Analyze on Scholarcy
Share
Abstract The oral absorption of amino acids, small peptides and their analogs has been studied in rats using single pass intestinal perfusion. The experimental data was analyzed using a modified boundary layer method permitting the calculation of intrinsic membrane absorption parameters. Cefatrizine, l -Dopa, α-methyldopa, and l -PHE demonstrated concentration dependent absorption. Furthermore, the absorption of the amino acid analog, l -Dopa, was significantly inhibited by l -Leucine. Cefatrizine absorption was significantly inhibited by the peptide PHE-PHE (20 mM whereas the amino acid l -PHE (100 mM) did not inhibit its absorption. The results clearly demonstrate that l -Dopa and α-methyldopa oral absorption occurs via the amino acid pathway, while cefatrizine absorption occurs via the peptide pathway. These results indicate that nutrient pathways may function as a possible route for the oral delivery of selected drugs.
This paper references
10.1085/JGP.56.6.673
Characteristics of the Amino Acid Transport System in the Mucosal Border of Rabbit Ileum
J. J. Hajjar (1970)
10.1042/CS0580221
Influx of glycylsarcosine and L-lysyl-L-lysine into hamster jejunum in vitro.
E. Taylor (1980)
10.1152/PHYSREV.1975.55.4.537
Intestinal absorption of peptides.
D. M. Matthews (1975)
10.1111/j.2042-7158.1986.tb04588.x
Concentration and pH dependency of α‐methyldopa absorption in rat intestine
G. Amidon (1986)
10.1172/JCI106724
Intestinal transport of dipeptides in man: relative importance of hydrolysis and intact absorption
Adibi Sa (1971)
Absorption of protein digestion products.
G. Wiseman (1974)
10.1016/S0022-5193(88)80123-1
Determination of intrinsic membrane transport parameters from perfused intestine experiments: a boundary layer approach to estimating the aqueous and unbiased membrane permeabilities.
D. C. Johnson (1988)
10.1042/CS0560015
Influx of two dipeptides, glycylsarcosine and L-glutamyl-L-glutamic acid, into hamster jejunum in vitro.
D. Matthews (1979)
10.3109/00365528309181626
Passage of molecules through the wall of the gastrointestinal tract. Measurement of intestinal permeability to polyethylene glycols in the 634-1338 dalton range (PEG 1000).
C. Tagesson (1983)
10.1085/JGP.64.4.443
Structure-Affinity Relationships of Substrates for the Neutral Amino Acid Transport System in Rabbit Ileum
Robert L. Preston (1974)
10.1016/0005-2736(76)90164-4
Mucosal and serosal fluxes of alanine in rabbit ileum.
G. Danisi (1976)
10.1248/BPB1978.1.262
CARRIER-MEDIATED TRANSPORT SYSTEMS FOR AMINOPENICIL-LINS IN RAT SMALL INTESTINE
T. Kimura (1978)
10.1016/S0016-5085(19)32196-1
Measurements of intestinal permeability using low molecular weight polyethylene glycols (PEG 400). I. Chemical analysis and biological properties of PEG 400.
V. Chadwick (1977)
Intestinal absorption of amino acids
S. Dibella (1960)
10.1042/BJ1290001
The metabolism of 14 C-labelled -methyldopa in normal and hypertensive human subjects.
W. Au (1972)
10.1016/S0016-5085(19)32197-3
Measurements of intestinal permeability using low molecular weight polyethylene glycols (PEG 400). II. Application to normal and abnormal permeability states in man and animals.
V. Chadwick (1977)
10.3109/00365527809181758
Passage of molecules through the wall of the gastrointestinal tract. I. A simple experimental model.
C. Tagesson (1978)
10.1042/BJ1460133
Studies on a wide-spectrum intestinal dipeptide uptake system in the monkey and in the human.
M. Das (1975)
10.1016/0378-5173(86)90077-3
Binding of antibiotics to rat intestinal mucin
J. Niibuchi (1986)
10.1248/BPB1978.7.452
Intestinal absorption mechanism of amino-beta-lactam antibiotics. III. Kinetics of carrier-mediated transport across the rat small intestine in situ.
E. Nakashima (1984)
10.1248/BPB1978.6.246
Characterization of aminocephalosporin transport across rat small intestine.
T. Kimura (1983)



This paper is referenced by
10.1111/J.1365-2125.1993.TB05691.X
The effect of L-leucine on the absorption of levodopa, studied by regional jejunal perfusion in man.
H. Lennernäs (1993)
10.1023/A:1018923618747
Comparison of the Transport Characteristics of D- and L-Methionine in a Human Intestinal Epithelial Model (Caco-2) and in a Perfused Rat Intestinal Model
L. Zheng (2004)
10.1002/BDD.2510120903
Partially competitive inhibition of intestinal baclofen absorption by beta‐alanine, a nonessential dietary aminoacid
A. Polache (1991)
Pharmacokinetics and allometric scaling of antimalarial drugs
Senarathna Mudiyanselage Dona Kalyani Ganga Senarathna (2015)
10.1016/0928-0987(96)00161-3
Transport mechanism of the α1-antagonist alfuzosin and its enantiomers in rat intestine: in vitro studies
A. Haddouche (1996)
10.1016/j.nano.2014.02.014
Intestinal absorption of insulin nanoparticles: contribution of M cells.
M. A. Lopes (2014)
10.1007/978-1-4757-9021-4_1
Predicting Oral Drug Absorption in Humans: A Macroscopic Mass Balance Approach for Passive and Carrier-Mediated Compounds
D. Oh (1991)
10.1111/j.2042-7158.1995.tb06731.x
The Influence of Uptake from the Gastrointestinal Tract and First‐pass Effect on Oral Bioavailability of (Z)‐alkyloxyimino Penicillins
L. Mizen (1995)
10.1023/A:1011573831444
Time-Dependent Oral Absorption Models
Kazutaka Higaki (2004)
10.2165/00063030-200822040-00002
Strategies Toward the Improved Oral Delivery of Insulin Nanoparticles via Gastrointestinal Uptake and Translocation
Camile B. Woitiski (2012)
10.1016/j.jcis.2009.04.001
Preparation of an amphiphilic triblock copolymer with pH- and thermo-responsiveness and self-assembled micelles applied to drug release.
Tianhong Qu (2009)
10.1021/JS9504346
Interaction of taurine on baclofen intestinal absorption: a nonlinear mathematical treatment using differential equations to describe kinetic inhibition models.
M. J. Moll‐Navarro (1996)
10.1016/S0928-0987(99)00032-9
Chitosans as absorption enhancers of poorly absorbable drugs. 3: Influence of mucus on absorption enhancement.
N. G. Schipper (1999)
10.1016/S1367-5931(00)00228-3
Prediction of pharmacokinetic properties using experimental approaches during early drug discovery.
P. Chaturvedi (2001)
10.1007/BF03402027
Tumor-targeting, Systemically Delivered Antisense HER-2 Chemosensitizes Human Breast Cancer Xenografts Irrespective of HER-2 Levels
A. Rait (2002)
10.1201/9780203912072.SECB
Ocular Delivery and Therapeutics of Proteins and Peptides
Surajit Dey (2003)
10.2165/00063030-200519030-00003
Oral Delivery of Peptide Drugs
J. Hamman (2012)
10.1016/0928-0987(94)90063-9
Gastrointestinal absorption mechanisms: a comparison between animal and human models
H. Lennernäs (1994)
10.1007/978-1-4615-3314-6_7
Food-associated intoxicants.
J. L. Hall (1988)
10.1016/0169-409X(95)00129-U
The intestinal peptide carrier: A potential transport system for small peptide derived drugs
E. Walter (1996)
10.1038/sj.gt.3302304
A sterically stabilized immunolipoplex for systemic administration of a therapeutic gene
W. Yu (2004)
10.1002/BDD.2510160705
Influence of leucine on intestinal baclofen absorption as a model compound of neutral α‐aminoacids
T. Cercós-Fortea (1995)
10.1007/978-3-642-61015-8_2
Drug Interactions in the Gastrointestinal Tract and Their Impact on Drug Absorption and Systemic Availability: A Mechanistic Review
E. Lipka (1996)
10.1023/A:1016207525186
Comparison of Intestinal Permeabilities Determined in Multiple in Vitro and inSitu Models: Relationship to Absorption in Humans
B. Stewart (2004)
10.1080/15533174.2013.776604
Synthesis, Characterization, and Antimicrobial Activities of New N-(2-hydroxy-1-naphthalidene)-amino Acid (L-Tyrosine, L-Arginine, and L-Lysine) Schiff Bases and Their Manganese(III) Complexes
İffet Şakiyan (2014)
Semantic Scholar Logo Some data provided by SemanticScholar