Saliva-catalyzed hydrolysis of a ketobemidone ester prodrug: Factors influencing human salivary esterase activity
Research output: Contribution to journal › Journal article › Research › peer-review
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.
Original language | English |
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Journal | International Journal of Pharmaceutics |
Volume | 88 |
Issue number | 1-3 |
Pages (from-to) | 221-227 |
Number of pages | 7 |
ISSN | 0378-5173 |
DOIs | |
Publication status | Published - 1 Jan 1992 |
Links
- https://www.sciencedirect.com/science/article/pii/037851739290319W
Final published version
ID: 46100821