The Research Of Sustained-release Pellets Of Bioactive Extract From Lysimachia Clethroides Duby

It is necessary to realize the modernization of Chinese traditional medicine to meet the request of the development of times. The modernization of preparation is the premise and base of the modernization of Chinese traditional medicine. In this paper, to adapt the need of clinic, Lysimachia clethroides Duby, the drug of anti-tumor, was selected as the model drug. On base of new method, new technology, new supplements and equipment, a new Chinese traditional medicinal sustained-release preparation was developed, which was accorded with the characteristics of Chinese traditional medicine. To assure the safety, therapeutic, efficiency, stability of the drug, strict quality standard was established, so the preparation could exert action and characteristics in preventing and curing diseases more efficiently.Ultraviolet spectrophotometry method was developed for assaying during the study of content determination of the drug and release rate of the pellets. The method was accurate, liable, convenient and rapid, which meet the requirement of measurement. In the pre-formulation researches, the physicochemical properties of material drug were investigated, which were connected closely with pharmaceutic form design . The solubility of the drug in different buffer were increased while the apparent oil-water partition coefficient (Papp) decreased with the increase of pH value .In addition, the extract was stable when exposed to light,high temperature.Extract total flavone from Lysimachia clethroides Duby through ethanol solution. Based on the studies of the influence factors,orthogonal test was used to optimize the extract conditions. The optimized extraction technics was to use 80% alcohol, 3times, 12 quantity and 2 hour per time. Then Three kinds of macro porous adsorbents were used to study adsorption performance for total flavone. The result showed that AB-8 was a kind of good adsorption resin for total flavone. In addition, the optimum conditions were filtered as follows: concentration of total flavone of liquid samples was 10 mg/mL, pH was 5.07, and fluid velocity was 1.0 mL/min, eluted by 40% alcohol at flow speed of 1.5 mL/min, total flavone in ZE4 reached 25.5%.The absorption sites and the absorption kinetics were studied from various intestinal segments ligation using in situ perfusion method in rats. The research demonstrated that rutin was absorbed in the varied intestinal segments and mostly absorbed in jejunum .The mechanism of the gastrointestinal absorption of rutin was passive diffusion.The process included the preparation of prompt-release pellets and coating of the pellets. HPC as dilute agent and water as adhesive agent ,the prompt-release pellets were prepared by the method of extrusion-spheronization. A fluid bed spray processor was adopted for coating the pellets. Using EC as coating material, the thesis screened the coating process parameters. The coating process variables were determined and controlled . The pellets was produced by with 90% alcohol and by filtration of a series of poreforming agent PEG6000( 12%), talc( 20%) , coating level( 5%) and curing time(24h).The description of dissolution profiles suggested that among the kinetics, the first-order became the most appropriate model to describe. The stability of the coated pellets was monitored. The results showed the coated pellets were stable under high temperature, high humidity, strong light.Choosing rutin as standard sample, HPLC with UV detection was applied to analysis the plasma sample in dogs. The methods are accurate, liable, convenient and rapid, which meet the requirement of measurement.Pharmacokinetic studies of sustained-release and prompt-release capsule in dogs were performed based on determination of plasma concentration of drugs. The results showed, compared with prompt-release capsule, plasma concentration of sustained-release capsule was relatively stable, Tmax was postponed and Cmax was lowered and the mean residence time (MRT) was prolonged.The correlation study showed that a good relationship between in vivo and in vitro was built.