| Oral colon-specific drug delivery system (OCDDS) has gained much interest during the past decade.Two important therapeutic applications which can be found for OCDDS are the treatment of local disorders of the colon and the delivery of protein and peptide drugs via the oral route.Compared with western medicine,Chinese medicine has better curative effects,less adverse reactions and lower recurrence rate,but the laggard dosage forms restrict its function.Thus the research on oral colon-specific target delivery system for ulcerous colonitis in TCM is very important and urgent.In this thesis,Berberine Hydrocholride was selected as the model drug to prepare a colon-specific delivery system for pH-dependent and time-contolled coated tablets with acrylic resin water dispersion coating technique to treat chronic ulcerative colitis because of the high content,more extensive basic researches and good curative effects.Orthogonal design was used for studying the effect of alcohol concentration,volume,extraction time andtimes on the content of berberinel .The optimum extraction process is as follows: 8 times of 50 % alcohol,extracted for 4 times,each time for 2 hours.This extraction process is workable and reproducible,and can provide theoretic support for mass extraction of the alkaloids from Rhizoma Coptidis.New direct compression excipient was chosen.The formulation was optimized based on the Single-factor design.To liquidity and pressure are good 20% of anhydrous lactose as a filler,using 0.5% magnesium stearate as a lubricant and 3% sodium carboxymethyl starch (CMS-Na) for the collapse of agents,the prescription Process of preparation of the colon-coated tablets of the tablet core in line with quality requirements, and good stability. Berberine Hydrocholride colon-specific targeting coated tablets were prepared by a sugar coater,with multi-layer coating technology,using HPMC as sealing-coat layer,Eudragit L30D-55/S100 as enteric-dissolved layer,and EudragitRL30D/RS30D as sustained-release layer,using triethyl citrate as plasticizer and talc powder as antisticking agent.An optimal prescription was obtained by orthogonal design.The drug dissolusion rate in vitro was studied in simulating gastrointestinal circumstances.The result of orthogonal experiment showed that combination of Eudragit L30D-55/S100 was 1:5,coating weight was 5%;combination of Eudragit RL30D/RS was 1:2,coating weight was 2%,were the optimal formulation.There was no drug released in 0.1moL·L-1 hydrochloric acid solution for 2 hours.In pH6.8 phosphate buffer,dissolution rate was less than 10% for 3 hours.In pH7.5 phosphate buffer,the coated tablets showed sustained-release behavior,over 80% of the drug would be released to colon region for 12 hours.To establish the quality standards of Berberine Hydrocholride colon-specific targeting coated tablets.Huanglian was indentified by TLC,and Berberine Hydrocholride was determined by HPLC. Berberine Hydrocholride could be detected by TLC.Berberine Hydrocholride had a good liner relationshipin the range of 1.00～40.00μg/mL (r =0.99989) .The average recovery was 100.22%with RSD of 1.85%.The method is simple andaccurate witha strong specificity,and can be used for quality control of Berberine Hydrocholride colon-specific targeting coated tablets.
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