Study On Technology And The Pharmacokinetics Of Coptis Chinensis Colon-Specific Targeting Preparation

Oral colon targeted drug delivery system is a research hotspot in recent years.It is a targeted drug release in colon targeting agents,so as to achieve local or systemic therapeutic effect.In this thesis,according to the gastrointestinal tract pH and transit time characteristics,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.Hope that oral agents in the stomach and small intestine after the non-absorption,in colon-specific drug release to improve the colon partial lesion of the drug concentration,thereby enhancing the efficacy of the treatment of ulcerative colitis.Reference to the use of alcohol on the extraction of parts coptis chinensis effectively refined to direct compression lactose,magnesium stearate,and sodium carboxymethyl starch as additives,on the whole parts coptis chinensis effective direct compression of powder,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 Eudragit RL30D/RS30D as sustained-release layer,usingtriethyl 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 3%;combination of Eudragit RL30D:RS30D 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. The results show that the colon-coated tablets in the body of the average delay of 5 hours,plasma concentration reached its peak in eight hours, colon-coated tablets of the AUC is not only the core coated tablets of 30.1%, Cmax was not their core coated tablets of 22.1%,Thus it is demonstrated that the colon-specific coated tablets reduce the systemic absorption of syringopicroside and release drug into the ileum and colon.