Characterization of overall biopharmaceutical properties of traditional Chinese medicine components based on identification of representational components / 中国中药杂志

Preformulation research, an in-depth research for pharmacological and pharmaceutical properties of raw materials, has been widely used in the field of chemical drugs. Although traditional Chinese medicine components (TCMCs) are the basic units in Chinese medicine preparation, the properties characterization of these components is still in an exploratory stage, because empiricism and blindness are still present in the development of the Chinese medicine preparations. TCMCs, a complex multi-component system, is very difficult to be analyzed in details. Herein, a research idea is put forward for the characterization of overall properties by using representative compositions. Firstly, various composition groups were set up for screening the representative components by in vitro and in vivo efficacy evaluation according to the original proportion. Then the equilibrium solubility, oil/water (O/W) partition coefficient and apparent permeability coefficient of the representative components were detected. Subsequently, the similarity assessment and discrete analysis were performed for the subdivision of TCMCs. The overall properties of TCMCs were fitted by mass fraction or efficacy contribution of each representative component, so as to characterize the overall properties of components/sub-components.

Study on biopharmaceutical properties of active fraction from Xiangfu Siwu Decoction by composite phospholipid liposome-based artificial skin membrane / 中草药

Objective: To evaluate the feasibility of the application of composite phospholipid liposome-based artificial skin membrane (CPLASM) for measuring biopharmaceutical properties of active fraction extracted from Xiangfu Siwu Decoction (XSD) via transdermal administration. Methods: The HPLC method was established for the determination of active ingredients (ferulic acid, tetrahydrocolumbamine, tetrahydropalmatine, senkyunolide I, and senkyunolide H) in active fraction of XSD. The oil/water partition coefficient values of these active ingredients were measured. The CPLASM was prepared to determine the in vitro permeability parameters of active fraction of XSD. The obtained parameters were further compared with those obtained by porcine ear skin. Results: The oil-water partition coefficients of ferulic acid, tetrahydrocolumbamine, tetrahydropalmatine, senkyunolide I, and senkyunolide H in active fraction of XSD (pH 5.5) were measured to be 1.220 ± 0.280, 0.670 ± 0.085, 0.920 ± 0.110, 1.040 ± 0.092, 1.030 ± 0.093 (n = 3), respectively. The permeability parameters of the active ingredients through porcine ear skin and CPLASM indicated a significant correlation (r > 0.9). Compared with the classical oil-water partition coefficients, the 6 h- cumulative permeation ratio of five active ingredients through CPLASM can be characterized as effectively predicting permeability parameters through porcine ear skin. Conclusion: The biopharmaceutical properties of active fractions from Chinese material medica can be effectively characterized by the application of CPLASM for the determination of in vitro permeability parameters of active ingredients.