Influence of pharmaceutical quality on the bioavailability of active components from Ginkgo biloba preparations.
To be effective, herbal medicinal products are expected to meet comparable standards concerning the assessment of efficacy, safety and biopharmaceutical quality as chemically defined synthetic drugs as food supplements. However, these requirements are often not fulfilled, particularly regarding the characterization of biopharmaceutical properties such as in-vitro dissolution and in-vivo bioavailability. With respect to the relevance of biopharmaceutical quality of herbal medicinal products, two different Ginkgo biloba brands (test product: Ginkgo biloba capsules; reference product: Ginkgold) were analysed for dissolution rates and bioavailability of the most relevant active ingredients. Dissolution rates at pH 1 and 4.5 were determined according to the USP 23. The relative bioavailability of ginkgolide A, ginkgolide B and bilobalide was investigated after single oral administration of 120 mg Ginkgo biloba extract as tablets or capsules. Bioavailability data (area under the curve and peak concentration in plasma) were clearly different and did not show bioequivalence of test and reference products. The slow in-vitro dissolution of the test product resulted in a large decrease in bioavailability. These results indicate for the first time that the pharmaceutical properties of a herbal medicinal product have a significant impact on the rate and extent of drug absorption, and very likely on efficacy in humans.
Kressmann
S
S
Department of Pharmacology, University of Frankfurt, Marie-Curie-Str. 9, 60439 Frankfurt/Main, Germany.
Biber
A
A
Wonnemann
M
M
Schug
B
B
Blume
H H
HH
Müller
W E
WE
D000284:Administration, Oral; D000328:Adult; D019540:Area Under Curve; D001682:Biological Availability; D003517:Cyclopentanes / Q000097:blood; D004224:Diterpenes; D005663:Furans / Q000097:blood; D008401:Gas Chromatography-Mass Spectrometry; D020441:Ginkgo biloba / Q000737:chemistry*; D046934:Ginkgolides; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007783:Lactones / Q000097:blood; D008297:Male; D008875:Middle Aged; D010936:Plant Extracts / Q000737:chemistry / Q000493:pharmacokinetics*; D012995:Solubility; D013678:Technology, Pharmaceutical; D013810:Therapeutic Equivalency
D003517:Cyclopentanes; D004224:Diterpenes; D005663:Furans; D046934:Ginkgolides; D007783:Lactones; D010936:Plant Extracts; C045856:ginkgolide B; C073710:bilobalide