| "Fuzilizhongwan" is an effective Traditional Chinese Medicine Compound Recipe(TCMCR) with strengthening the spleen and warming the stomach composed of five components - "fuzi" (black Aconiti), " danshen " (root of Codonopsis pilosula), " gancao " (root of Glycyrrhiza uralensis), "baizhu" (rhizoma of Atractylodes macrocephala Koidz), "ganjiang" (rhizoma Zingiberis).The main action of Fuzilizhong pill is to cure the diseases of asthenia-cold of the spleen and stomach, cold-type pain of the stomach and abdomen, vomiting and diarrhea,coldness of limbs due to the cold symptom of spleen and stomach. The study tries to change traditional dosage form which is swallowed uneasily, mildewed easily with frequent oral dose and listed in the first section of the 2000's edition of pharmacopoeia into two new preparations of traditional Chinese medicine(TCM)-effervescent controlled osmotic pump tablet and sustained tabletIt is very difficult for traditional dosage forms to satisfy the requirements of small dosage, small toxicities and side-effects, and sustained or controlled release. The difficulties can be solved by developing TCM new dosage forms which have been a key subject to development of TCM.In this paper, active parts of Fuzilizhong prescription were selected as model drug, on the basis of which effervescent controlled osmotic pump tablet and sustained tablet were made and release theory of effervescent controlled osmotic pump tablet was disclosed primarily. Herein, patent for sustained and controlled release tablets of Fuzilizhong was applied for.Model drug was composed of two parts, one extract powder extracted from fuzi, danshen and gancao, the other p-cyclodextrin inclusion included by p-cyclodextrin and mixed essential oil which was distilled from baizhu and ganjiang. According to the optimal results of orthogonal design experiment on extract process of fuzi, danshen and gancao, extract powder was obtained by treating mixture liquid through macroporous resin with 75% alcohol as eluent and then evaporating the extract with vacuum after the mixture of three crude herbs was boiled with water and then precipitated with alcohol. Herein, an active constituent liquiritin was isolated from extract powder by column chromalography method. As to essential oil, natural borneol was determined by using gas chromatography-mass spectrum skill.At the aspect of preparation process, based on physicochemical properties of model drug and relevant results confirmed by in vitro analysis methods, active parts and osmotic promoting agents were uniformly mixed to be suitable-tableted powders and then directly compressed to form tablet core using single-punch tableting machine. After coated with coating fluid to prepare a semipermeable membrane, mechanically punched an appropriate orifice on the membrane surface and finally coated ahydroxypropylmethylcellulose (HPMC) moistureproof membrane, effervescent controlled osmotic pump tablets were then made, namely, extract powder 14g, essential oil inclusion 2.3g, sodium chloride 2.1g, mannitol 0.7g, sodium hydrogen carbonate 0.14g, HPMC 0.7g and magnesium stearate 0.06g. During the research of single factor influence, selection for osmotic promoting agent was studied emphatically,including determination of effervescent agent sodium hydrogen carbonate and its addition quantity, determination of HPMC and its addition quantity and so on, through which optimal formulation was given. In addition, study on process of essential oil inclusion, preparation for coating fluid, effect factor to the tablet membrane, such as membrane orifice, membrane thickness, membrane weight and so on, and the dissolution medium on the drug release behavior were investigated, which indicated that the optimal formulation had a good zero order release characteristics in 14 hours.Fuzilizhong sustained release tablet was prepared by using HPMC as main matrix material. After single factor investigation for other excipient was done, appropriate HPMC was determined and optimal formulation was got The study on the...
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