Saliva-catalyzed hydrolysis of a ketobemidone ester prodrug: Factors influencing human salivary esterase activity

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

Standard

Saliva-catalyzed hydrolysis of a ketobemidone ester prodrug : Factors influencing human salivary esterase activity. / Hansen, L.B.; Christrup, Lona Louring; Bundgaard, H.

In: International Journal of Pharmaceutics, Vol. 88, No. 1-3, 01.01.1992, p. 221-227.

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

Harvard

Hansen, LB, Christrup, LL & Bundgaard, H 1992, 'Saliva-catalyzed hydrolysis of a ketobemidone ester prodrug: Factors influencing human salivary esterase activity', International Journal of Pharmaceutics, vol. 88, no. 1-3, pp. 221-227. https://doi.org/10.1016/0378-5173(92)90319-W

APA

Hansen, L. B., Christrup, L. L., & Bundgaard, H. (1992). Saliva-catalyzed hydrolysis of a ketobemidone ester prodrug: Factors influencing human salivary esterase activity. International Journal of Pharmaceutics, 88(1-3), 221-227. https://doi.org/10.1016/0378-5173(92)90319-W

Vancouver

Hansen LB, Christrup LL, Bundgaard H. Saliva-catalyzed hydrolysis of a ketobemidone ester prodrug: Factors influencing human salivary esterase activity. International Journal of Pharmaceutics. 1992 Jan 1;88(1-3):221-227. https://doi.org/10.1016/0378-5173(92)90319-W

Author

Hansen, L.B. ; Christrup, Lona Louring ; Bundgaard, H. / Saliva-catalyzed hydrolysis of a ketobemidone ester prodrug : Factors influencing human salivary esterase activity. In: International Journal of Pharmaceutics. 1992 ; Vol. 88, No. 1-3. pp. 221-227.

Bibtex

@article{7c8b98adda124461aa7f0f45697c6db5,
title = "Saliva-catalyzed hydrolysis of a ketobemidone ester prodrug: Factors influencing human salivary esterase activity",
abstract = "Saliva enzyme-catalysed hydrolysis of ester prodrugs or drugs containing sensitive ester groups may be a limiting factor for the buccal absorption of such compounds. Using the isopropyl carbonate ester of ketobemidone as a model substance of a hydrolysis-sensitive prodrug the esterase activity of human saliva has been characterized as a function of various factors. The esterase activity was found to decrease rapidly upon storage of the saliva at 37°C. The activity increased with increasing pH in the range 4.5-7.4 and with increasing salivation flow rate up to a rate of 0.9 ml min. Under resting conditions, the flow rate was about 0.2 ml min which implied a greatly decreased esterase activity. The activity was highest after fasting and decreased after intake of a meal. The intraindividual variation in the saliva esterase activity was small whereas a larger interindividual variation was found.",
author = "L.B. Hansen and Christrup, {Lona Louring} and H. Bundgaard",
year = "1992",
month = jan,
day = "1",
doi = "10.1016/0378-5173(92)90319-W",
language = "English",
volume = "88",
pages = "221--227",
journal = "International Journal of Pharmaceutics",
issn = "0378-5173",
publisher = "Elsevier",
number = "1-3",

}

RIS

TY - JOUR

T1 - Saliva-catalyzed hydrolysis of a ketobemidone ester prodrug

T2 - Factors influencing human salivary esterase activity

AU - Hansen, L.B.

AU - Christrup, Lona Louring

AU - Bundgaard, H.

PY - 1992/1/1

Y1 - 1992/1/1

N2 - Saliva enzyme-catalysed hydrolysis of ester prodrugs or drugs containing sensitive ester groups may be a limiting factor for the buccal absorption of such compounds. Using the isopropyl carbonate ester of ketobemidone as a model substance of a hydrolysis-sensitive prodrug the esterase activity of human saliva has been characterized as a function of various factors. The esterase activity was found to decrease rapidly upon storage of the saliva at 37°C. The activity increased with increasing pH in the range 4.5-7.4 and with increasing salivation flow rate up to a rate of 0.9 ml min. Under resting conditions, the flow rate was about 0.2 ml min which implied a greatly decreased esterase activity. The activity was highest after fasting and decreased after intake of a meal. The intraindividual variation in the saliva esterase activity was small whereas a larger interindividual variation was found.

AB - Saliva enzyme-catalysed hydrolysis of ester prodrugs or drugs containing sensitive ester groups may be a limiting factor for the buccal absorption of such compounds. Using the isopropyl carbonate ester of ketobemidone as a model substance of a hydrolysis-sensitive prodrug the esterase activity of human saliva has been characterized as a function of various factors. The esterase activity was found to decrease rapidly upon storage of the saliva at 37°C. The activity increased with increasing pH in the range 4.5-7.4 and with increasing salivation flow rate up to a rate of 0.9 ml min. Under resting conditions, the flow rate was about 0.2 ml min which implied a greatly decreased esterase activity. The activity was highest after fasting and decreased after intake of a meal. The intraindividual variation in the saliva esterase activity was small whereas a larger interindividual variation was found.

UR - http://www.scopus.com/inward/record.url?scp=0026727250&partnerID=8YFLogxK

U2 - 10.1016/0378-5173(92)90319-W

DO - 10.1016/0378-5173(92)90319-W

M3 - Journal article

AN - SCOPUS:0026727250

VL - 88

SP - 221

EP - 227

JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

SN - 0378-5173

IS - 1-3

ER -

ID: 46100821