EFFECT OF AQUEOUS EXTRACT OF CRYPTOLEPIS SANGUINOLENTA ON PHARMACOKINETICS OF ARTESUNATE
Journal Title: International Journal of Pharmaceutical Sciences and Drug Research - Year 2011, Vol 3, Issue 4
Abstract
The aim of this study is to investigate the effect of aqueous extract of Cryptolepis sanguinolenta on the pharmacokinetics of the antimalarial; artesumate in male Sprague-Dawley rats. Reconstituted freeze dried Cryptolepis sanguinolenta was administered in drinking water at the therapeutic dose of 36 g/kg body weight for two (2) weeks, followed by a single oral dose of artesunate (150 mg/kg body weight). The Concentration - Time course; Maximum Whole Blood Concentration, Cmax; Time for the Maximum Concentration, Tmax; Bioavailability; Elimination Rate Constant; Half- life; Clearance; Volume of Distribution and Absorption Rate Constant were measured. Results indicated that about 80% of dihydroartemisinin was recovered during extraction suggesting that the extraction procedure was effective. The elimination rate constant and clearance of dihydroartemisinin the most potent metabolite of artesunate increased by 233.3% and 62.1% respectively in rats which received concurrent administration of Cryptolepis sanguinolenta compared to control (artesunate only). This resulted in significant decrease (p < 0.05) in the Bioavailability (40.1%), Volume of Distribution (68.1%) and Half-life (52.1%) of dihydroartemesinin. The findings therefore, showed that Cryptolepis sanguinolenta could cause sub-therapeutic blood levels of dihydroartemisinin of artesunate leading to decreased effectiveness and possibly drug resistance as a result of herb-drug interactions. Thus, in clinical practice, patients should be advised on the serious implication of using Cryptolepis sanguinolenta and artesunate together.
Authors and Affiliations
Sakyiamah M M, Ocloo A, Adjimani J P, Sittie A
Keywords
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