Buccal absorption of ketobemidone and various ester prodrugs in the rat

Research output: Contribution to journal › Journal article › Research › peer-review

Standard

Buccal absorption of ketobemidone and various ester prodrugs in the rat. / Hansen, L.B.; Jorgensen, A.; Rasmussen, S.N.; Christrup, Lona Louring; Bundgaard, H.

In: International Journal of Pharmaceutics, Vol. 88, No. 1-3, 01.01.1992, p. 243-250.

Research output: Contribution to journal › Journal article › Research › peer-review

Harvard

Hansen, LB, Jorgensen, A, Rasmussen, SN, Christrup, LL & Bundgaard, H 1992, 'Buccal absorption of ketobemidone and various ester prodrugs in the rat', International Journal of Pharmaceutics, vol. 88, no. 1-3, pp. 243-250. https://doi.org/10.1016/0378-5173(92)90322-S

APA

Hansen, L. B., Jorgensen, A., Rasmussen, S. N., Christrup, L. L., & Bundgaard, H. (1992). Buccal absorption of ketobemidone and various ester prodrugs in the rat. International Journal of Pharmaceutics, 88(1-3), 243-250. https://doi.org/10.1016/0378-5173(92)90322-S

Vancouver

Hansen LB, Jorgensen A, Rasmussen SN, Christrup LL, Bundgaard H. Buccal absorption of ketobemidone and various ester prodrugs in the rat. International Journal of Pharmaceutics. 1992 Jan 1;88(1-3):243-250. https://doi.org/10.1016/0378-5173(92)90322-S

Author

Hansen, L.B. ; Jorgensen, A. ; Rasmussen, S.N. ; Christrup, Lona Louring ; Bundgaard, H. / Buccal absorption of ketobemidone and various ester prodrugs in the rat. In: International Journal of Pharmaceutics. 1992 ; Vol. 88, No. 1-3. pp. 243-250.

Bibtex

@article{6ced9d947289427ebea26bdd9a236907,
title = "Buccal absorption of ketobemidone and various ester prodrugs in the rat",
abstract = "The buccal absorption of ketobemidone, a strong narcotic analgesic, and various carboxylate and carbonate ester prodrugs was studied in rats. The compounds were administered in the form of aqueous solutions of pH 7.4. The absolute bioavailability of ketobemidone following buccal dosing was 26% whereas the bioavailability of ketobemidone following buccal administration of the prodrugs ranged from 37 to 98%. The highest bioavailability was obtained with the ethyl carbonate ester. An apparent parabolic correlation between bioavailability and lipophilicity of the compounds was seen. All esters were rapidly hydrolyzed to ketobemidone after both buccal and intravenous administration. The acute toxicity of the esters after i.v. administration to mice and rats was similar to that of the parent drug. It is concluded that esterification of the phenolic hydroxyl group in ketobemidone to give a more lipophilic prodrug may be a useful approach to improve the buccal delivery of this analgesic.",
author = "L.B. Hansen and A. Jorgensen and S.N. Rasmussen and Christrup, {Lona Louring} and H. Bundgaard",
year = "1992",
month = jan,
day = "1",
doi = "10.1016/0378-5173(92)90322-S",
language = "English",
volume = "88",
pages = "243--250",
journal = "International Journal of Pharmaceutics",
issn = "0378-5173",
publisher = "Elsevier",
number = "1-3",

}

RIS

TY - JOUR

T1 - Buccal absorption of ketobemidone and various ester prodrugs in the rat

AU - Hansen, L.B.

AU - Jorgensen, A.

AU - Rasmussen, S.N.

AU - Christrup, Lona Louring

AU - Bundgaard, H.

PY - 1992/1/1

Y1 - 1992/1/1

N2 - The buccal absorption of ketobemidone, a strong narcotic analgesic, and various carboxylate and carbonate ester prodrugs was studied in rats. The compounds were administered in the form of aqueous solutions of pH 7.4. The absolute bioavailability of ketobemidone following buccal dosing was 26% whereas the bioavailability of ketobemidone following buccal administration of the prodrugs ranged from 37 to 98%. The highest bioavailability was obtained with the ethyl carbonate ester. An apparent parabolic correlation between bioavailability and lipophilicity of the compounds was seen. All esters were rapidly hydrolyzed to ketobemidone after both buccal and intravenous administration. The acute toxicity of the esters after i.v. administration to mice and rats was similar to that of the parent drug. It is concluded that esterification of the phenolic hydroxyl group in ketobemidone to give a more lipophilic prodrug may be a useful approach to improve the buccal delivery of this analgesic.

AB - The buccal absorption of ketobemidone, a strong narcotic analgesic, and various carboxylate and carbonate ester prodrugs was studied in rats. The compounds were administered in the form of aqueous solutions of pH 7.4. The absolute bioavailability of ketobemidone following buccal dosing was 26% whereas the bioavailability of ketobemidone following buccal administration of the prodrugs ranged from 37 to 98%. The highest bioavailability was obtained with the ethyl carbonate ester. An apparent parabolic correlation between bioavailability and lipophilicity of the compounds was seen. All esters were rapidly hydrolyzed to ketobemidone after both buccal and intravenous administration. The acute toxicity of the esters after i.v. administration to mice and rats was similar to that of the parent drug. It is concluded that esterification of the phenolic hydroxyl group in ketobemidone to give a more lipophilic prodrug may be a useful approach to improve the buccal delivery of this analgesic.

UR - http://www.scopus.com/inward/record.url?scp=0026678205&partnerID=8YFLogxK

U2 - 10.1016/0378-5173(92)90322-S

DO - 10.1016/0378-5173(92)90322-S

M3 - Journal article

AN - SCOPUS:0026678205

VL - 88

SP - 243

EP - 250

JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

SN - 0378-5173

IS - 1-3

ER -

ID: 46100865