Effect of dehusked Garcinia kola seeds on the overall pharmacokinetics of quinine in healthy Nigerian volunteers

Abstract

We investigated the effect of concurrent ingestion of Garcinia kola seed on the pharmacokinetics of quinine. In a randomized crossover study, 24 healthy Nigerian volunteers were assigned into 2 groups (A and B; n = 12 per group) on the basis of G. kola dose orally ingested. Each subject received 600 mg quinine sulfate before and after ingesting 12.5 g of G. kola once daily for 7 days (group A) or 12.5 g twice daily for 6 days and once on the seventh day (group B). Blood samples were collected and analyzed for plasma quinine and its metabolite (3-hydroxyquinine) using a validated high performance liquid chromatography method. Concurrent administration of quinine with G. kola reduced quinine tmax by 48% (group A), mean Cmax by 19% and 26% in groups A and B, respectively, and slight reduction in mean AUC0- ∞ of quinine in both groups. 3-hydroxyquinine Cmax also reduced by 29% and 32%; AUC0-∞ by 13% and 9%, respectively. The point estimates of the T/R ratio of the geometric means for all Cmax obtained and only the AUC0-∞ at a higher dose of G. kola were outside the 80%-125% bioequivalence range. In conclusion, an herb-drug interaction was noted with concurrent quinine and G. kola administration.

Keywords: 3-hydroxyquinine; Garcinia kola; drug-herb interactions; pharmacokinetics; quinine.

Figure 1

Mean plasma concentration versus time profiles for quinine and 3-hydroxyquinine following single oral administration of 600mg dose of quinine sulphate tablet to 12 volunteers before and after each volunteer received G. kola (12.5 g) once daily for 7 days (Group A)

Figure 2

Mean plasma concentration versus time profiles for quinine and 3-hydroxyquinine following single oral administration of 600mg dose of quinine sulphate tablet to 12 volunteers before and after each volunteer received G. kola (12.5 g) twice daily for 6 days and once on day 7 (Group B)