Study On Preparation And Quality Control For Fuke Suppository

Fuke suppository derived from the innovative development of YinYanJing lotion, is a complex preparation of traditional Chinese medicine, which consists of 9 herbal Medicines as Phellodendron chinense Schneid., Coptis chinensis Franch., Sophora flavescens Ait., Stemona sessilifolia (Miq.) Miq., Forsythia suspensa (Thunb.) Vahl,Cnidium monnieri.(L.) Cuss., Kochia scoparia (L.)Schrad., Gentianarigescens Franch., Taraxacum mongolicum Hand Mazz.. It has the function of clearing Heat and expelling Miasma anti-inflammatory and analgesic, killing parasites to relieve itching and reducing swelling and ease pain, so it can be mainly used for the treatment on colpomycosis, trichomonas vaginitis, bacterial vaginosis, cervicitis, pruritus vulvae and eczema, and it can be used as an adjunctive therapy for gonorrhea.According to the the physiochemical property of the effective components from the Yinyanjing prescription, we designed an initial technological process in first place. And we compared the anti—inflammatory effect of the extract which was made by the pre-estabished process and the Yinyanjing lotion, the extract showed a more significant activity of anti-inflammatory effect than lotion. This indicated that the new preparation can bring about the improvement of pesticide effect in this study.The preparation of Fuke suppository was researched in this study on the basis of the physiochemical property of the effective components which were from the Yinyanjing prescription, and the optimized technological process and conditions of the Fuke suppository were obtained through the study. The results of three batchs produces suggest that the preparation procedure of the suppository is reasonable and practical. Morever, the results of quality control study show that quality of the suppository is controllable, and property is stable.The processes and results are as follows: 1. Preparation technologyThe herbs in this prescription were divided into two groups according to the physiochemical property of the effective components. Using single factor and orthogonal design to optimize the alcohol extraction technology. The extraction rate of berberine hydrochloride, oxymatrin, matrine and total solid rate were used as indices of appraisal. The optimum conditions for the alcohol extraction of Fuke Suppository were as follows:adding 12 times of 70% alcohol, and extracting for 1 h each time, totally extracting twice. Regarding the total solid rate and the extraction rate of gentiamarin as indexes, the optimum technical parameters of the water extracting technology was obtained by adopting orthogonal designs, as follows:adding 12 times water to the original crude materials,being fried and boiled three times and for 1 h each timeThe influence of concentration on the retention rates of berberine hydrochloride, oxymatrin, matrine and gentiamarin was studied. The optimum conditions for concentration of Fuke Suppository were as follows:film vacuum evaporation was used for concentration of alcohol extraction, the vacuum was controlled in -0.05～-0.06Mpa, and the relative density of concentrate was about 1.13. Water extraction and ethanol concentrate was mixed for film vacuum concentration. The vacuum in this process was -0.09 Mpa, and the relative density of the final thick paste was about 1.38Spray drying and vacuum microwave drying were compared in this study. The results show that wall sticking was serious when there was no added excipients in the spray drying.By contrast, vacuum microwave drying is convenient and efficient. The optimum conditions for drying was as follows:containing material was finalized 1.5 Kg/KW, vacuum was -0.08～-0.09MPa, maximum temperature was 90℃.When it comes to molding process, the SUPPOCIRE NCX semi-synthetic glyceride fatty acids was used as substrate. The substrate was melting to about three-quarters at 65℃, and stop heating, continue stirring until the temperature dropped to 60℃, added peppermint oil. Extract powder were added to the above matrix, stiring well. The substrate's temperature was about 50℃before injection molding, then injected to the suppository mold (mold temperature of about 15℃), cooling about 30min before scraping the overflow part, the process was finished.The total transfer rates of matrine and oxymatrine, berberine and gentiopicroside of three batchs suppositories were 80%,82% and 94% respectively. The results of three batchs produces suggest that the preparation procedure of the suppository is reasonable and practical.2. Quality controlThe methods of TLC identification for Phellodendron chinense Schneid., Coptis chinensis Franch., Sophora flavescens Ait., Stemona sessilifolia (Miq.) Miq.,Forsythia suspensa (Thunb.) Vahl,Cnidium monnieri (L.) Cuss., Kochia scoparia (L.)Schrad., Gentianarigescens Franch., Taraxacum mongolicum Hand Mazz.. in the preparation were established. The methodology of HPLC determining matrine and oxymatrine, berberine and gentiopicroside's content of the preparation was investigated systematically.