Improved oral bioavailability of artemisinin through inclusion complexation with β- and γ-cyclodextrins

The bioavailability of β- and γ-cyclodextrin artemisinin complexes was evaluated in comparison with a normal commercially available preparation, Artemisinin 250 ®. Twelve healthy male volunteers participated in the study conducted according to a three-way crossover design. The bioavailability was co...

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Bibliographic Details
Published in:International journal of pharmaceutics 2001-10, Vol.227 (1), p.177-185
Main Authors: Wong, J.W, Yuen, K.H
Format: Article
Language:English
Subjects:
Adult
Antimalarials - pharmacokinetics
Area Under Curve
Artemisinin
Artemisinins
Bioavailability
Biological Availability
Cross-Over Studies
Cyclodextrins - pharmacology
Drug Interactions
Gastrointestinal Transit
Half-Life
Humans
Male
Metabolic Clearance Rate
Sesquiterpenes - pharmacokinetics
β-cyclodextrins
γ-cyclodextrins
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Summary:The bioavailability of β- and γ-cyclodextrin artemisinin complexes was evaluated in comparison with a normal commercially available preparation, Artemisinin 250 ®. Twelve healthy male volunteers participated in the study conducted according to a three-way crossover design. The bioavailability was compared using the parameters, total area under the plasma level–time curve (AUC 0–∝), peak plasma concentration ( C max), and time to reach peak plasma concentration ( T max). A statistically significant difference was observed between the values of the complexes and Artemisinin 250 ® for the three parameters. However, no statistically significant difference was observed between the values of the β- and γ-cyclodextrin complexes. Moreover, the 90% confidence interval for the ratio of the AUC 0–∝ values of the β-cyclodextrin complex over those of Artemisinin 250 ® was estimated to be between 1.51–2.04, while that of C max was between 1.73–2.93. For the γ-cyclodextrin complex, the respective intervals were 1.30–1.76 and 1.43–2.43. These findings indicated that the β- and γ-cyclodextrin complexes had a much higher rate and extent of bioavailability compared to Artemisinin 250 ®. In addition, the absorption of artemisinin was observed to be poor and negligible when the preparations started to arrive in the colon. This could be attributed to poor dissolution of artemisinin in the semi-solid faecal matter in the lower part of the gastrointestinal tract.
ISSN:0378-5173
1873-3476
DOI:10.1016/S0378-5173(01)00796-7