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Titre du document / Document title

Oral bioavailability of proteolytic enzymes

Auteur(s) / Author(s)

KOLAC C. (1) ; STREICHHAN P. (2) ; LEHR C.-M. (1) ;

Affiliation(s) du ou des auteurs / Author(s) Affiliation(s)

(1) University of the Saarland, Dept. of Biopharmaceutics and Pharmaceutical Technology, Saarbrücken, ALLEMAGNE
(2) Mucos Pharma GmbH, Geretsried, ALLEMAGNE

Résumé / Abstract

The oral bioavailability of proteolytic enzymes such as e.g. trypsin, chymotrypsin, papain and bromelain has been discussed since their introduction as anti-inflammatory, anti-edematose and immunostimulating agents. The controversy about oral enzyme absorption has not yet been solved, because in the blood proteolytic enzymes bind to antiproteinases and therefore are difficult to quantify with immunological, enzymic and radiochemical methods. Therefore, the amounts of enzymes absorbed in vivo tend to be underestimated (immunological, enzymic methods) or overestimated (radiochemical methods). Quantification as an objective parameter, however, is pivotal for any bioavailability study. Regardless of these analytical difficulties it is presently accepted that proteolytic enzymes when orally administered to man can be detected in the blood plasma, at least to some extent, in their intact, biologically active form. What, however, is still unknown, is the mechanism by which the large molecules cross the intestinal barrier. Using Caco-2 monolayers as a model, some progress was made to better understand this phenomenon. The proteolytic enzymes trypsin, chymotrypsin, papain and bromelain decreased the transepithelial electrical resistance and simultaneously increased the transport of fluorescent marker substances, which normally are not transported across the Caco-2 monolayer. Mucin, albumin and fetal calf serum influence differently the behaviour of these enzymes thus indicating different mechanisms of action for the enzymes. The results suggest that proteolytic enzymes are able to increase the permeability of the mucosal epithelium and, hence, facilitate their own absorption by a mechanism of self-enhanced paracellular diffusion.

Revue / Journal Title

European journal of pharmaceutics and biopharmaceutics    ISSN  0939-6411 

Source / Source

1996, vol. 42, no4, pp. 222-232 (68 ref.)

Langue / Language

Anglais
Revue : Anglais

Editeur / Publisher

Elsevier, Amsterdam, PAYS-BAS  (1991) (Revue)

Mots-clés anglais / English Keywords

Trypsin

;

Chymotrypsin

;

Papain

;

Stem bromelain

;

Antiinflammatory agent

;

Bioavailability

;

Oral administration

;

Pharmacokinetics

;

Animal

;

Human

;

Absorption

;

Serine endopeptidases

;

Proteinases

;

Hydrolases

;

Enzyme

;

Cysteine endopeptidases

;

Mots-clés français / French Keywords

Trypsin

;

Chymotrypsin

;

Papain

;

Stem bromelain

;

Antiinflammatoire

;

Biodisponibilité

;

Voie orale

;

Pharmacocinétique

;

Animal

;

Homme

;

Absorption

;

Serine endopeptidases

;

Proteinases

;

Hydrolases

;

Enzyme

;

Cysteine endopeptidases

;

Mots-clés espagnols / Spanish Keywords

Trypsin

;

Chymotrypsin

;

Papain

;

Stem bromelain

;

Antiinflamatorio

;

Biodisponibilidad

;

Vía oral

;

Farmacocinética

;

Animal

;

Hombre

;

Absorción

;

Serine endopeptidases

;

Proteinases

;

Hydrolases

;

Enzima

;

Cysteine endopeptidases

;

Localisation / Location

INIST-CNRS, Cote INIST : 17483, 35400006405295.0010

Nº notice refdoc (ud4) : 3191444



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