1.Quality Evaluation and Suggestions on Pharmacopoeia Standard of Eucommiae Folium
Ping WANG ; Shaojia LIANG ; Wenwen ZHANG ; Weihong FENG ; Hong YI ; Chun LI ; Fengqian GUO ; Qin SI ; Dejing FU ; Man GONG ; Zhengtao WANG ; Hongchu ZHENG ; Xiaoqian LIU ; Zhimin WANG
Chinese Journal of Experimental Traditional Medical Formulae 2023;29(2):10-17
ObjectiveTo establish a quantitative analysis multi-components by single marker method (QAMS) for five main components (aucubin, geniposidic acid, chlorogenic acid, asperuloside and rutin) in Eucommiae Folium, to verify its feasibility and applicability in the determination of Eucommiae Folium, so as to provide a scientific basis for the development of quality standard of this herb. MethodHigh performance liquid chromatography was performed on a Welch Boltmatetm™ C18 column (4.6 mm×100 mm, 2.7 μm) with methanol (A)-0.2% phosphoric acid aqueous solution (B) as the mobile phase for gradient elution (0-8 min, 3%A; 8-10 min, 3%-11%A; 10-26 min, 11%A; 26-27 min, 11%-25%A; 27-60 min, 25%-32%A), the column temperature was set at 30 ℃, the flow rate was 0.6 mL·min-1, the detection wavelengths were at 210 nm and 254 nm. Chlorogenic acid was used as an internal reference to establish the relative correction factors (f) between it and the other four components, and the contents of the five components in 14 batches of Eucommiae Folium were determined by QAMS and external standard method (ESM), respectively. ResultThe f values of chlorogenic acid to aucubin, geniposidic acid, asperuloside and rutin were 3.13, 1.45, 2.64 and 0.56, respectively. Repeatability was good under different experimental conditions, relative standard deviation (RSD) was <5.0%. The contents of aucubin, geniposidic acid, chlorogenic acid, asperuloside and rutin in 14 batches of Eucommiae Folium were 1.340-28.975, 0.252-36.086, 10.016-27.443, 1.396-8.646, 0.533-1.766 mg·g-1, respectively. There were no significant difference between content results of QAMS and that of ESM (RSD<5.0%). ConclusionQAMS established with chlorogenic acid as the internal reference can be used to determine the contents of five components in Eucommiae Folium, and this method is simple and accurate. After comprehensive evaluation, the quality standard of Eucommiae Folium in subsequent editions of Chinese Pharmacopoeia is suggested that three main active components, chlorogenic acid, aucubin and geniposidic acid, are selected as quality markers, and their content limits are recommended not less than 1.5%, 1.0% and 1.0%, respectively. This quality standard draft can avoid the potential quality risk due to poor specificity and low content limit of the index component (chlorogenic acid) in the previous editions of Chinese Pharmacopoeia.
2.Preparation and in Vitro Evaluation of Matrine Lipid-based Cubic Liquid Crystalline Nanoparticle Gels
Qin SI ; Huimin GAO ; Chun LI ; Zhimin WANG ; Shuo SHEN ; Lihua YAN ; Fengqian GUO ; Dinghua XIANG ; Ping WANG ; Dejing FU ; Xiaoqian LIU ; Hong YI
Chinese Journal of Experimental Traditional Medical Formulae 2023;29(2):27-36
ObjectiveTo prepare matrine lipid-based cubic liquid crystalline nanoparticle (MAT-LLCN) gels and investigate its in vitro release and transdermal absorption behavior. MethodTaking entrapment efficiency as the index, the optimal formulation of MAT-LLCN was screened by extreme vertex mixture method based on the optimal ratio of glycerol monooleate (GMO) to poloxamer 407 (P407), and its drug loading was investigated. MAT-LLCN gels was prepared by mixing MAT-LLCN with pre-swelled carbomer 940 as the gel matrix. The structure of MAT-lipid-based cubic liquid crystalline (LLC) was characterized by polarized light microscopy (PLM) and small angle X-ray scattering (SAXS). The in vitro release and transdermal absorption properties of MAT-LLCN gels and MAT ordinary gels were compared by modified Franz diffusion cell method, skin structure changes caused by them were observed by hematoxylin-eosin (HE) staining. ResultThe optimal formulation of MAT-LLCN gels was 5.5% of GMO-P407 (9∶1), 1%-6% of MAT, 0.6% of carbomer 940, adding water to sufficient amount. The prepared MAT-LLC was confirmed as body-centered (Im3m) LLC. The in vitro release behavior of MAT-LLCN gels was in accordance with the Weibull equation (R2=0.954 0), and the release mechanism was the Fick diffusion. In vitro transdermal test showed that all the parameters of MAT-LLCN gels were higher than those of MAT ordinary gels (P<0.05), including cumulative release rate, steady-state release rate and the amount of drug retention in skin. HE staining results showed that MAT-LLCN gels could loose the cellular arrangement of skin stratum corneum, and maintain the stability of the cell structure of the dermis. ConclusionThe prepared MAT-LLCN gels can accelerate the transdermal drug transport and form drug storage in the dermis by rapidly opening the skin stratum corneum barrier, suggesting that LLC has good application prospects in the field of transdermal drug delivery.