RESUMEN
To explore the quality consistency evaluation method for multi-component traditional Chinese medicine and establish a dissolution evaluation method suitable for the characteristics of multi-component Chinese patent medicine, this study discussed the characteristics and advantages of the flow-through cell method in the dissolution evaluation of Chinese patent medicine by comparing the impact of the small cup method and the flow-through cell method on the dissolution behavior of water-soluble and lipid-soluble major active components of Danshen Tablets. Dissolution tests were performed using the small cup method as described in the 2020 edition of the Chinese Pharmacopoeia and the newly introduced flow-through cell method(closed-loop method) with water solution containing 0.5% SDS as dissolution medium. Cumulative dissolution curves of the water-soluble component salvianolic acid B and the lipid-soluble component tanshinone Ⅱ_A in Danshen Tablets were plotted, and fitting and similarity analysis of the dissolution models was conducted to identify the characteristics and advantages of the flow-through cell method. For the small cup method, 150 mL of water containing 0.5% SDS was used as the dissolution medium, with a rotation speed of 75 r·min~(-1) and a temperature of(37±0.5) ℃, and 3 mL of samples were taken at 15, 30 min, 1, 2, and 4 h, with fresh dissolution medium added at the same temperature and volume. For the flow-through cell method, a closed-loop system was used. Danshen Tablets were placed in the flow-through cell with approximately 6.7 g of glass beads, and 150 mL of water containing 0.5% SDS was used as the dissolution medium. The flow rate was set at 20 mL·min~(-1), and the temperature and sampling were the same as the small cup method. The results showed that compared with the small cup method, the flow-through cell method had stronger discriminative power and higher sensitivity in distinguishing the dissolution behavior of the two components, and could better reflect the differences in formulation quality, especially for water-insoluble lipid-soluble components. Given that there were no essential differences in the in vitro release kinetics between the two methods, the flow-through cell method could not only replace the traditional small cup method but also better guide the formulation development and identify quality issues of formulations.
Asunto(s)
Salvia miltiorrhiza , Medicina Tradicional China , Comprimidos , Agua , Lípidos , SolubilidadRESUMEN
Objective::To investigate the pharmacodynamics of volatile oil in couplet medicines of Moslae Herba and Pogostemonis Herba, to establish a method for simultaneous determination of three essential ingredients (thymol, carvacrol and patchouli alcohol) in volatile oil of the couplet medicines by gas chromatography (GC), to optimize the preparation process of β-cyclodextrin (β-CD) inclusion complex of volatile oil in the couplet medicines and to confirm the formation of the inclusion complex. Method::An in vitro inflammatory response model was established by hyaluronidase activity inhibition test in order to detect the anti-inflammatory activity of the volatile oil. Also, the antioxidant activity of the volatile oil was assessed by 1, 1-diphenyl-2-trinitrophenylhydrazine (DPPH) free radical scavenging method. The inclusion of volatile oil in couplet medicines of Moslae Herba and Pogostemonis Herba was prepared by scaturated aqueous solution method, colloid milling method and grinding method, respectively. GC was used to determine the contents of thymol, carvacrol and patchouli alcohol in volatile oil for optimizing extraction and inclusion processes of volatile oil. Scanning electron microscope, infrared spectroscopy, thermal differential analysis, and X-ray diffraction (XRD) were used to verify the formation of the inclusion complex. Result::The volatile oil not only inhibited hyaluronidase activity to a certain extent, but also eliminated DPPH and increased with the increase of concentration. There was a good linear relationship between the peak area and concentration of thymol, carvacrol and patchouli alcohol at 0.021 3-0.426, 0.020 04-0.400 8, 0.022 6-0.452 g·L-1 (R2>0.999), respectively. Their recoveries were 99.59%(RSD 1.6%), 100.15%(RSD 1.5%), 100.70%(RSD 1.4%), respectively. The colloid milling method was optimized, and the formation of the inclusion complex was verified by the aforementioned methods. Conclusion::The volatile oil in couplet medicines of Moslae Herba and Pogostemonis Herba has certain anti-inflammatory activity and anti-oxidation ability. The colloid milling method was the best inclusion process for the volatile oil. The established GC has the advantages of simple, sensitive, accurate, reliable and reproducible, which can meet the requirements of simultaneous determination of thymol, carvacrol and patchouli alcohol in the inclusion complex.
RESUMEN
Ginger juice， a commonly used adjuvant for Chinese materia medica， is applied in processing of multiple Chinese herbal decoction pieces. Because of the raw materials and preparation process of ginger juice， it is difficult to be preserved for a long time， and the dosage of ginger juice in the processing can not be determined base on its content of main compositions. Ginger juice from different sources is hard to achieve consistent effect during the processing of traditional Chinese herbal decoction pieces. Based on the previous studies， the freeze drying of ginger juice under different shelf temperatures and vacuum degrees were studied， and the optimized freeze drying condition of ginger juice was determined. The content determination method for 6-gingerol， 8-gingerol， 10-gingerol and 6-shagaol in ginger juice and redissolved ginger juice was established. The content changes of 6-gingerol， 8-gingerol， 10-gingerol， 6-gingerol， 6-shagaol， volatile oil and total phenol were studied through the drying process and 30 days preservation period. The results showed that the freeze drying time of ginger juice was shortened after process optimization; the compositions basically remained unchanged after freeze drying， and there was no significant changes in the total phenol content and gingerol content， but the volatile oil content was significantly decreased(<0.05). Within 30 days， the contents of gingerol， total phenol， and volatile oil were on the decline as a whole. This study has preliminarily proved the feasibility of freeze-drying process of ginger juice as an adjuvant for Chinese medicine processing.