Schrödter A, Loew D, Schwankl W, Rietbrock N
Institut für Klinische Pharmakologie des Klinikums, Johann Wolfgang von Goethe-Universität, Frankfurt/Main.
Arzneimittelforschung. 1998 Sep;48(9):905-10.
The bioavailability under steady state conditions of a standard, slow-release horse chestnut seed extract (HCSE)-containing product was compared with that of an analogous, fast-release test preparation (Noricaven novo) in a prospective, randomised, double-blind study in a double cross-over design. The serum concentration of beta-escin (CAS 6805-41-0) was measured by radioimmunoassay. In addition, the biopharmaceutical properties of the HCSEs present in the products were investigated, the amount and composition of the active ingredient, escin, being analysed with a validated HPLC method. The pharmacokinetics of this study were compared with the corresponding data of a similar investigation carried out under analogous conditions concerning study design, analytical methods and reference preparation. Comparison of the similar studies revealed differences in characteristic pharmakokinetic values of beta-escin in terms of a shift of the concentration time curves as could be demonstrated for the reference product. The total amounts of escin in the two products investigated did not differ significantly. However, quantitative and qualitative differences were detected in the constituents of the two different extract preparations. It is concluded that the high specificity of the validated beta-escin radioimmunoassay leads to analytical imprecision due to the variable constituents of the extract preparations used. It is necessary to test whether this problem can be solved using an analytical approach, which is specific for each extract.
在一项采用双交叉设计的前瞻性、随机、双盲研究中，将一种标准的含缓释七叶树籽提取物（HCSE）产品在稳态条件下的生物利用度与一种类似的速释试验制剂（Noricaven novo）进行了比较。通过放射免疫分析法测定β-七叶皂苷（CAS 6805-41-0）的血清浓度。此外，还研究了产品中HCSE的生物药剂学性质，采用经过验证的高效液相色谱法分析活性成分七叶皂苷的含量和组成。将本研究的药代动力学与在类似条件下进行的关于研究设计、分析方法和参比制剂的类似研究的相应数据进行了比较。类似研究的比较显示，就浓度-时间曲线的位移而言，β-七叶皂苷的特征药代动力学值存在差异，这在参比产品中得到了证实。所研究的两种产品中七叶皂苷的总量没有显著差异。然而，在两种不同提取物制剂的成分中检测到了定量和定性的差异。得出的结论是，由于所用提取物制剂的成分可变，经过验证的β-七叶皂苷放射免疫分析法的高特异性导致分析不精确。有必要测试是否可以使用针对每种提取物的分析方法来解决这个问题。
