Enzyme Touch-type Compound Berberine Hydrochloride Colon Skeleton Coated Tablets Preparation And Quality Standards

ObjectiveTo establish a suitable preparation method,as well as the evaluation method in vivo and in vitro and quality standard of the Enzyme-controlled Colon-Specific drugs by studying the suitability of the model drug of different dosage forms.The model drug was made by berberine and extract of Aucklandiae.Methods(1)Determine the content of the berberine by HPLC.(2) Establish a suitable evaluation method in vitro and dissolution medium according to the pharmacopoeia and the optimized condition.(3) The colon-specific coating matrix tablets are prepared by coating matrix tablets core,which was compressed by mixing drugs,the matrix materials of pectin and guar gum,with Enteric layer.The preparation process is screened according to the results of the topsis method and the drug release property is evaluated by dissolution rate in vitro.(4)Evaluated the condition of drugs releasing in dogs by microdialysis and determined influencing factors and the berberine recovery rate in vitro.(5) Determined the Berberine content in each gastrointestinal segment after oral administration by rats.Finished the preliminary evaluation in vivo of preparation.(6) Established the quality standard of compound berberine Coating matrix tablet.(7) Preliminarily studied the adhesion of the core tablets.Results(1) Methodological study shows that the testing condition of HPLC was feasible. (2)The dissolution medium was pH5.8 PBS(The content of pectinase andβ-mannanase was 0.5mg per ml).(3) The drug released less than 20%in artificial intestinal juice in 5 hours and close to 80%in artificial colon circumstance in 6 hours on the condition of pectin and guar gum are even and enteric layer increases 3.8%.(4) In the same flow,the recovery rate was independent of the content;In the same condition,the recovery rate was similar using osmosis and reversed osmosis method; In the same content,the recovery rate index decreased as the flow increased.(5) After the tablets were administered to rats,Berberine released mostly in caecum and colon but barely in stomach and small intestine.Under the effect of enzyme produced by flora in caecum and colon,the drug released faster than in the small intestine condition.(6)TLC qualitative distinction and quality specification of berberine were established.(7)The adhesion of the core tablets was indicated.ConclusionThe preparation technology of compound berberine Enzyme-controlled Colon-Specific tablet,the evaluation method in vivo and in vitro and quality standard were established.The study achieved its expected purpose.