IN VITRO IRREVERSIBLE BINDING AND DEGRADATION OF (R)- AND (S)-KETOPROFEN GLUCURONIDES TO PLASMA PROTEINS
This study describes the in vitro degradation studies of the diastereomeric ketoprofen glucuronides, under physiological conditions (pH 7.4, 37°C, (R)-ketoprofen glucuronide t½ = 30 min, (S)-ketoprofen glucuronide t½ = 70 min) and the irreversible binding of diastereomeric ketoprofen glucuronides (1...
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| Main Authors: | , |
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| Format: | Book |
| Published: |
Universiti Sains Malaysia,
2007-01-01T00:00:00Z.
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| Online Access: | Connect to this object online. |
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| Summary: | This study describes the in vitro degradation studies of the diastereomeric ketoprofen glucuronides, under physiological conditions (pH 7.4, 37°C, (R)-ketoprofen glucuronide t½ = 30 min, (S)-ketoprofen glucuronide t½ = 70 min) and the irreversible binding of diastereomeric ketoprofen glucuronides (15 μg/ml) to human serum albumin (HSA) (289 μM) and human plasma under physiological conditions (pH 7.4, 37ºC). The (R)-ketoprofen glucuronide irreversibly bound to a greater extent in both human plasma and human serum albumin. This is the reverse to that found in previous studies. These findings further support the hypothesis that faster degradation of 1-O-acyl glucuronide (in this case the (R)-diastereomer) is associated with a greater extent of irreversible binding. |
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| Item Description: | 1675-7319 1985-8396 |