Enhanced delivery of ketobemidone through porcine buccal mucosa in vitro via more lipophilic ester prodrugs

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Standard

Enhanced delivery of ketobemidone through porcine buccal mucosa in vitro via more lipophilic ester prodrugs. / Hansen, L.B.; Christrup, Lona Louring; Bundgaard, H.

I: International Journal of Pharmaceutics, Bind 88, Nr. 1-3, 01.01.1992, s. 237-242.

Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt

Harvard

Hansen, LB, Christrup, LL & Bundgaard, H 1992, 'Enhanced delivery of ketobemidone through porcine buccal mucosa in vitro via more lipophilic ester prodrugs', International Journal of Pharmaceutics, bind 88, nr. 1-3, s. 237-242. https://doi.org/10.1016/0378-5173(92)90321-R

APA

Hansen, L. B., Christrup, L. L., & Bundgaard, H. (1992). Enhanced delivery of ketobemidone through porcine buccal mucosa in vitro via more lipophilic ester prodrugs. International Journal of Pharmaceutics, 88(1-3), 237-242. https://doi.org/10.1016/0378-5173(92)90321-R

Vancouver

Hansen LB, Christrup LL, Bundgaard H. Enhanced delivery of ketobemidone through porcine buccal mucosa in vitro via more lipophilic ester prodrugs. International Journal of Pharmaceutics. 1992 jan. 1;88(1-3):237-242. https://doi.org/10.1016/0378-5173(92)90321-R

Author

Hansen, L.B. ; Christrup, Lona Louring ; Bundgaard, H. / Enhanced delivery of ketobemidone through porcine buccal mucosa in vitro via more lipophilic ester prodrugs. I: International Journal of Pharmaceutics. 1992 ; Bind 88, Nr. 1-3. s. 237-242.

Bibtex

@article{8dde7d3ef5404fc78888f347b326dce8,
title = "Enhanced delivery of ketobemidone through porcine buccal mucosa in vitro via more lipophilic ester prodrugs",
abstract = "The in vitro penetration of ketobemidone and various ester prodrugs through porcine buccal mucosa in a modified Ussing chamber was investigated in order to support the selection of a prodrug derivative with optimal buccal absorption. The nine esters studied included carboxylic acid and carbonate esters formed at the phenolic hydroxy group of ketobemidone. The esters were all rapidly hydrolyzed to the parent drug in a porcine buccal epithelial homogenate and only free ketobemidone was detected in the receptor compartment of the Ussing chamber. All the ester prodrugs showed enhanced rates of permeation relative to ketobemidone, the permeability coefficients being 3-30-times higher than that of ketobemidone. The permeability coefficients increased with increasing lipophilicity, expressed in terms of octanol-buffer (pH 7.4) partition coefficients (P), up to log P values of about 1.5 whereupon a plateau or a slight decrease occurred. No toxic effects of ketobemidone or the prodrugs on the buccal membrane were observed as judged from monitoring of the electrical properties of the membrane.",
author = "L.B. Hansen and Christrup, {Lona Louring} and H. Bundgaard",
year = "1992",
month = jan,
day = "1",
doi = "10.1016/0378-5173(92)90321-R",
language = "English",
volume = "88",
pages = "237--242",
journal = "International Journal of Pharmaceutics",
issn = "0378-5173",
publisher = "Elsevier",
number = "1-3",

}

RIS

TY - JOUR

T1 - Enhanced delivery of ketobemidone through porcine buccal mucosa in vitro via more lipophilic ester prodrugs

AU - Hansen, L.B.

AU - Christrup, Lona Louring

AU - Bundgaard, H.

PY - 1992/1/1

Y1 - 1992/1/1

N2 - The in vitro penetration of ketobemidone and various ester prodrugs through porcine buccal mucosa in a modified Ussing chamber was investigated in order to support the selection of a prodrug derivative with optimal buccal absorption. The nine esters studied included carboxylic acid and carbonate esters formed at the phenolic hydroxy group of ketobemidone. The esters were all rapidly hydrolyzed to the parent drug in a porcine buccal epithelial homogenate and only free ketobemidone was detected in the receptor compartment of the Ussing chamber. All the ester prodrugs showed enhanced rates of permeation relative to ketobemidone, the permeability coefficients being 3-30-times higher than that of ketobemidone. The permeability coefficients increased with increasing lipophilicity, expressed in terms of octanol-buffer (pH 7.4) partition coefficients (P), up to log P values of about 1.5 whereupon a plateau or a slight decrease occurred. No toxic effects of ketobemidone or the prodrugs on the buccal membrane were observed as judged from monitoring of the electrical properties of the membrane.

AB - The in vitro penetration of ketobemidone and various ester prodrugs through porcine buccal mucosa in a modified Ussing chamber was investigated in order to support the selection of a prodrug derivative with optimal buccal absorption. The nine esters studied included carboxylic acid and carbonate esters formed at the phenolic hydroxy group of ketobemidone. The esters were all rapidly hydrolyzed to the parent drug in a porcine buccal epithelial homogenate and only free ketobemidone was detected in the receptor compartment of the Ussing chamber. All the ester prodrugs showed enhanced rates of permeation relative to ketobemidone, the permeability coefficients being 3-30-times higher than that of ketobemidone. The permeability coefficients increased with increasing lipophilicity, expressed in terms of octanol-buffer (pH 7.4) partition coefficients (P), up to log P values of about 1.5 whereupon a plateau or a slight decrease occurred. No toxic effects of ketobemidone or the prodrugs on the buccal membrane were observed as judged from monitoring of the electrical properties of the membrane.

UR - http://www.scopus.com/inward/record.url?scp=0026618801&partnerID=8YFLogxK

U2 - 10.1016/0378-5173(92)90321-R

DO - 10.1016/0378-5173(92)90321-R

M3 - Journal article

AN - SCOPUS:0026618801

VL - 88

SP - 237

EP - 242

JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

SN - 0378-5173

IS - 1-3

ER -

ID: 46100843