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

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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.
OriginalsprogEngelsk
TidsskriftInternational Journal of Pharmaceutics
Vol/bind88
Udgave nummer1-3
Sider (fra-til)221-227
Antal sider7
ISSN0378-5173
DOI
StatusUdgivet - 1 jan. 1992

ID: 46100821