Study On Active Components And Preparation Technology Of Compound Traditional Chinese Medicine Tou-nao-qing Dropping Pills

As one of the most common chronic disease, migraine has seriously threatened patients’ life. Traditional Chinese medicines(TCMs) such as Erigeron breviscapus, Ligusticum chuanxiong Hort, Lamiophlomis rotata(Benth.) are usually used to treat migraine. However, the clinical dosage forms of the drugs are traditional capsule, granules and injection. The low bioavailability, inconvenience and slow action combine with the dosage form limits their application. As a new dosage form of TCM, dropping pills displays the effects of efficacy enhancing, toxicity reducing, stable and reliable in quality and overcomes the disadvantages mentioned above. In this work, modern technology was used to concentrate the effective ingredients of the medicinal materials based on the research on their chemical composition, and to improve dissolution rate of the constituents as well as the bioavailability of the drug. Compound Tou- nao-qing dropping pills(C TDPs) in solid dispersion state were made. The detailed works are as follows:The main components of Erigeron breviscapus(EB), flavonoids and caffeate, were analyzed by High performance liquid chromatography-Diode array detector(HPLC-DAD). The ethyl acetate extracts were separated and purified with polyamide and silica gel column chromatography methods, their properties were identified by the physicochemical features and spectral data(UV、IR、MS and NMR). There were five components in ethyl acetate extracts, and two of them, i.e. scutellarin(EB-1) and 1,5-dicaffeoyl quinic acid(EB-5), were analyzed in this work.Pharmacological properties of th extracts from C TDP were verified with animal experiments in order to determine an optimum extracting process. The results showed that the extracting technology using alcohol as the extracting agent is the optimum one. The content of scutellarin in the extracts was selected as the index and the optimum extracting condition with alcohol was determined by orthogonal experiments: totally twenty-six times amount of 70% alcohol as compared with the raw material was used to extract the active components under refluxing condition through three times, 1 h for each time. With the content of scutellarin and caffeates in the extracts as indexes, High performance liquid chromatography(HPLC) and Ultraviolet spectrophotometry(US) were used to choose the purification technology parameters including the concentration and pH value of solution, stirring method, extraction solution. The optimum purification conditions were determined as: concentration of extract was 0.5 g crude drug /mL(solution), pH 6.5 with magnetic stirring, and the extraction solvent was n-butanol saturated with water.The preparation conditions of CTDPs based on solid dispersion technology were optimized with both single factor and orthogonal design experiment. The optimum preparation condition was found to be: the ratio of drugs to matrix was 1 : 2.5 and that for PEG 4000 to PEG 6000 was 0.5 : 1.5, temperature of drug fluids was 75 ℃. The preparation technology is proved to be stable and reasonable. The constituents in CTDPs’ were found to be in the dispersion state, which indicated that the extracts of compound drugs formed solid dispersion system.