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A Preliminary Pharmacokinetic Study of Betulin, the Main Pentacyclic Triterpene from Extract of Outer Bark of Birch (Betulae alba cortex)

Carl Gustav Carus-Institut, Am Eichhof 30, D-75223 Niefern-Öschlbronn, Germany
Betulin-Institut, Blumenstrasse 24, D-64297 Darmstadt, Germany
Author to whom correspondence should be addressed.
Molecules 2008, 13(12), 3224-3235;
Received: 31 October 2008 / Revised: 10 December 2008 / Accepted: 17 December 2008 / Published: 18 December 2008
(This article belongs to the Special Issue Triterpenes and Triterpenoids 2013)
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During the last two decades triterpenes have attracted attention because of their pharmacological potential. Triterpene extract (TE) from outer bark of birch consisting mainly of betulin is able to form an oleogel which was successfully tested in the treatment of actinic keratosis. Some aspects of TE in vitro pharmacology are already known. Now we show preliminary pharmacokinetics of betulin and results of a subchronic toxicity study of TE in rats and dogs. Because of poor aqueous solubility of the TE-triterpenes (< 0.1 μg/mL respectively), for pharmacokinetic studies it was suspended in sesame oil (rats, i.p.) and PEG 400 / 0.9 % NaCl (dogs, s.c.). I.p. administered, betulin, the main component of TE, shows time dependency over a period of 4 h and reaches a dose-independent serum level of 0.13 μg/mL. Dose dependency was observed with s.c. administration. At 300 mg/kg a maximum plasma concentration of 0.33 μg/mL betulin was detected after 28 daily applications. The subchronic toxicity study showed no toxicity of TE in rats (i.p.) and dogs (s.c.). In conclusion, triterpene extract from birch bark is safe, its betulin is bioavailable and in addition to published triterpene biological activities TE provides high potential for further pharmaceutical and pharmacological research. View Full-Text
Keywords: Triterpene extract; Betulin; Preliminary pharmacokinetics; Subchronic toxicity Triterpene extract; Betulin; Preliminary pharmacokinetics; Subchronic toxicity

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Jäger, S.; Laszczyk, M.N.; Scheffler, A. A Preliminary Pharmacokinetic Study of Betulin, the Main Pentacyclic Triterpene from Extract of Outer Bark of Birch (Betulae alba cortex). Molecules 2008, 13, 3224-3235.

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