The Pharmaceutical Study Of Xingsiang Tuerfeng Total Phenolic Acid Dispersible Tablet

Ainsliaea fragrans Champ. is one of traditional Chinese medicines. And its whole plant is considered as the treatment of clearing heat and reinforcing deficiency, cooling blood to stop blooding, removing dampness and promoting detoxication, dispelling wind and so on in folk. The research on A. fragrans Champ. indicated that chlorogenic acid and isochlorogenic acid are its important anti-inflammatory activity components using modern pharmacology. In this work, Xingxiang Tuerfeng total phenolic acid (XXTEF-TPA) is extracted utilizing macroporous adsorption resin, one of advanced separation techniques in phytochemistry. In view of the low biological availability of traditional preparation, dispersible table is prepared with XXTEF-TPA substances, which will provide corresponding foundation for exploitation and research of pharmacodynamic action of A. fragrans Champ..Objective:1. XXTEF-TPA was extracted using separation technique of macroporous adsorption resin, and the content of total phenolic acid would be increased to above 50%.2. To research preparation technology of XXTEF-TPA dispersible tablet.3. To establish quality standard of XXTEF-TPA dispersible tablet.Methods:1. According to the content of XXTEF-TPA, extraction process was optimized using the orthogonal experimental design and the optimal conditions were determined on the basis of range analysis.2. Single-factor experiments were applied to determine the optimal preparation technology of XXTEF-TPA dispersible tablet in terms of disintegration time.3. Through the research of methodology, the quality evaluation system of XXTEF-TPA dispersible tablet and substances was established. The content of XXTEF-TPA was determined using UV spectral analysis and the content of 4,5-dicaffeoyl-quinic acid was determined by HPLC. To ensure the quality of XXTEF-TPA substances and dispersible tablets, the quality standard of medical material was also researched.4. To investigate the stability of three batchs of prescription, the remained specimens were observed at room temperature.Results:1. The optimized extraction conditions of XXTEF-TPA: the soaking time of medical material: 1h; the pH of the adsorptive solution is 1; the ratio of the weight of medical material and the volume of adsorptive solution is 1:5; the ratio of the weight of macroporous adsorption resin and the volume of elutriant is 1:6.2. The preparation technology of XXTEF-TPA dispersible tablet: XXTEF-TPA extractive 150g (30%) Microcrystalline cellulose 290g (57%) Sodium starch glycolate 35g (7%) Polyvinyl polypyrroidone 25g (5%) Colloidal silicon dioxide 5g (1%) 95% Ethanol the right amount Number of preparation 1000 tablets The method of preparation: Based on recipe, XXTEF-TPA extractive, MCC, CMS-Na and PVPP was weighed, and 95% ethanol is added at the right amount. The above mixture was stirred with high speed and was granulated as pellet shape. The moisture pellets were dried in oven at 60℃, then were screened with 60 mesh screen. After addition of micropowder silica gel, the tablets were finally prepared in a medicinal tablet machine.3. 4,5-Dicaffeoyl-quinic acid was used as reference substance, and the absorbability of XXTEF-TPA solution was determined at 328nm using the method of UV spectral analysis. Based on the standard curve, the content of XXTEF-TPA should not be lower than 50~80% and the content of XXTEF-TPA dispersible tablet should not be lower than 50~80mg. The content of 4,5-dicaffeoyl-quinic acid in XXTEF-TPA should not be lower than 0.02, and the content of 4,5-dicaffeoyl-quinic acid in XXTEF-TPA dispersible tablet should not be lower than 5mg.To control the quality of XXTEF-TPA extractive, the quality standard established by Jiangxi Province was modified by the addition of two methods as follows: (1)the content of XXTEF-TPA of medical material was determined by UV spectral analysis; (2)the content of 4,5-dicaffeoyl-quinic acid of medical material was determined using HPLC analysis. 4. Through observing the remained specimens, the appearance of three-batch prescription had no obvious change within three months. And the content of the prescription had no obvious reduction. The preliminary prescription stability experiment indicated that the quality of the dispersible tablet is steady.Conclusion:The research results were shown as follows: the preparation of the XXTEF-TPA dispersible tablets was proved to be feasible, and drug quality was steady and controllable. The study goals of this work were achieved. The achievement of the work provided both the foundation for further study of A. fragrans Champ and the reference for solid preparation of traditional Chinese medicine.