Pharmacology Resveratrol

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1 pharmacology

1.1 pharmacodynamics
1.2 pharmacokinetics

1.2.1 metabolism







pharmacology
pharmacodynamics

although in vitro studies indicate resveratrol activates sirtuin 1 , pgc-1α, , affects functioning of mitochondria, other research disputes effect.


in cells treated resveratrol, increase observed in action of mnsod (sod2) , in gper activity.


pharmacokinetics

one way of administering resveratrol in humans may buccal delivery, without swallowing, direct absorption through tissues on inside of mouth. when 1 milligram of resveratrol in 50 ml 50% alcohol/ water solution retained in mouth 1 minute before swallowing, 37 ng/ml of free resveratrol measured in plasma 2 minutes later. level of unchanged resveratrol in blood can achieved 250 mg of resveratrol taken in pill form. however, viability of buccal delivery method called question due low aqueous solubility of molecule. drug absorbed transmucosally must in free-form or dissolved. resveratrol fits criteria oral transmucosal dosing, except caveat. low aqueous solubility limits amount can absorbed through buccal mucosa. resveratrol attempted taken buccally expected pass through mucous membrane of mouth , absorbed oral dose, however, need explore buccal delivery in future pharmaceutical formulations expressed.


while 70% of orally administered resveratrol absorbed, oral bioavailability approximately 0.5% due extensive hepatic glucuronidation , sulfation. resveratrol given in proprietary formulation srt-501 (3 or 5 g), developed sirtris pharmaceuticals, reached 5 8 times higher blood levels. these levels did approach concentration necessary exert effects shown in animal models , in vitro experiments.


in rats, less 5% of oral dose observed free resveratrol in blood plasma. there hypothesis resveratrol wine have higher bioavailability resveratrol pill.


in human study involving oral administration of 500 mg on 13 weeks, resveratrol detected in cerebrospinal fluid, indicating had crossed blood-brain barrier.


metabolism

resveratrol gets extensively metabolized in body, liver , lungs major sites of metabolism.








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