A Preliminary Pharmacokinetic Study of Betulin, the Main Pentacyclic Triterpene from Extract of Outer Bark of Birch (Betulae alba cortex)
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 T...
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| Format: | Article |
| Language: | English |
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MDPI AG
2008-12-01
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| Series: | Molecules |
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| Online Access: | http://www.mdpi.com/1420-3049/13/12/3224/ |
| _version_ | 1829138666070474752 |
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| author | Melanie N. Laszczyk Armin Scheffler Sebastian Jäger |
| author_facet | Melanie N. Laszczyk Armin Scheffler Sebastian Jäger |
| author_sort | Melanie N. Laszczyk |
| collection | DOAJ |
| description | 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. |
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| id | doaj.art-0996617471944214a6065a4e3f919f27 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-12-14T19:21:33Z |
| publishDate | 2008-12-01 |
| publisher | MDPI AG |
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| series | Molecules |
| spelling | doaj.art-0996617471944214a6065a4e3f919f272022-12-21T22:50:18ZengMDPI AGMolecules1420-30492008-12-0113123224323510.3390/molecules13123224A Preliminary Pharmacokinetic Study of Betulin, the Main Pentacyclic Triterpene from Extract of Outer Bark of Birch (Betulae alba cortex)Melanie N. LaszczykArmin SchefflerSebastian JägerDuring 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.http://www.mdpi.com/1420-3049/13/12/3224/Triterpene extractBetulinPreliminary pharmacokineticsSubchronic toxicity |
| spellingShingle | Melanie N. Laszczyk Armin Scheffler Sebastian Jäger A Preliminary Pharmacokinetic Study of Betulin, the Main Pentacyclic Triterpene from Extract of Outer Bark of Birch (Betulae alba cortex) Molecules Triterpene extract Betulin Preliminary pharmacokinetics Subchronic toxicity |
| title | A Preliminary Pharmacokinetic Study of Betulin, the Main Pentacyclic Triterpene from Extract of Outer Bark of Birch (Betulae alba cortex) |
| title_full | A Preliminary Pharmacokinetic Study of Betulin, the Main Pentacyclic Triterpene from Extract of Outer Bark of Birch (Betulae alba cortex) |
| title_fullStr | A Preliminary Pharmacokinetic Study of Betulin, the Main Pentacyclic Triterpene from Extract of Outer Bark of Birch (Betulae alba cortex) |
| title_full_unstemmed | A Preliminary Pharmacokinetic Study of Betulin, the Main Pentacyclic Triterpene from Extract of Outer Bark of Birch (Betulae alba cortex) |
| title_short | A Preliminary Pharmacokinetic Study of Betulin, the Main Pentacyclic Triterpene from Extract of Outer Bark of Birch (Betulae alba cortex) |
| title_sort | preliminary pharmacokinetic study of betulin the main pentacyclic triterpene from extract of outer bark of birch betulae alba cortex |
| topic | Triterpene extract Betulin Preliminary pharmacokinetics Subchronic toxicity |
| url | http://www.mdpi.com/1420-3049/13/12/3224/ |
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