ABSTRACT
<p><b>OBJECTIVE</b>Taking Chinese compound medicine Yuchangning as a research model, prepared the pH and time dependent Yuchangning tablets for colon-specific delivery (PT-YT-CSD), and evaluated the releasing property in vitro.</p><p><b>METHOD</b>The coating prescription is filtered by the release extent of matrine and oxymatrine in vitro and the wicking rate of the tablet, which including the category and proportion of film forming agent and porogen, the sort and dosage of fluidizing agent, the increment of weight after coating and so on. The releasing property of the preparation is evaluated by the dissolution tests in vitro through measuring the content of matrine and oxymatrine content.</p><p><b>RESULT</b>The preparation method of the PYTCSD: After prepared plain tablets, the 95% alcoholic solution of EC and Eudragit II are mixed in a 7:3 EC: Eudragit II ratio and then added in DEP up to 10% of the coating amount, reduced the alcohol concentration to 4% by diluting with ethonal. Tablet was coated by the alcohol solution and the weight of the plain tablet was increased by 3%. The dissolution tests in vitro indicated that matrine and oxymatrine were not dissolved in the simulated gastric juice after 2 h. The accumulative quantities of matrine and oxymatrine were less than 10% in the simulated intestinal juice after 4 h. The quantities of matrine and oxymatrine are 75.7% and 76.8% in the simulated colon juice after 1 h.</p><p><b>CONCLUSION</b>The PYTCSD was prepared and the preparation could fulfil the aim of delivering in the specific colon in vitro.</p>
Subject(s)
Alkaloids , Astragalus propinquus , Chemistry , Cellulose , Colon , Metabolism , Delayed-Action Preparations , Drug Combinations , Drug Compounding , Drug Delivery Systems , Drugs, Chinese Herbal , Pharmacokinetics , Hydrogen-Ion Concentration , Intestinal Absorption , Plants, Medicinal , Chemistry , Polymethacrylic Acids , Quinolizines , Sophora , Chemistry , Tablets, Enteric-CoatedABSTRACT
<p><b>OBJECTIVE</b>To prepare coated micro-pellets of pH-dependent and enzyme-dependent kangfuxin colon targeting delivery system, to make them go to colon, then release, educe partial effect.</p><p><b>METHOD</b>We eploy pan-pill to prepare simple pellets, and prepare tunicatus pellets with fluidized bed coating. We investigated the preparation and parameter of pellets, so, we bolting the best shaping and tunicatus artwork.</p><p><b>RESULT</b>The ingredients for preparing the micro-pellets are 125% starch +2% CMC-Na, and add 30% ethanol to be binder, pellets were coated with Eudragit S100 to prepare ph-dependent and pectin-HPMC to prepare enzyme-dependent colon targeting micro-pellets.</p><p><b>CONCLUSION</b>We get two micro-pellets of pH-dependent and enzyme-dependent kangfuxin colon targeting.</p>
Subject(s)
Animals , Colon , Metabolism , Delayed-Action Preparations , Drug Carriers , Drug Compounding , Methods , Drug Delivery Systems , Hydrogen-Ion Concentration , Hypromellose Derivatives , Materia Medica , Metabolism , Methylcellulose , Pectins , Periplaneta , Chemistry , Polymethacrylic AcidsABSTRACT
<p><b>OBJECTIVE</b>To evaluate the release in fixed position of pH-dependent and enzyme-dependent Kangfuxin colon targeting capsules in vivo and in vitro.</p><p><b>METHOD</b>The dissolution was tested in vitro and X-ray radiography was used for the evaluation in vivo.</p><p><b>RESULT</b>After two hours pH-dependent colon targeting in man-made colon fluid, medicine release in fixed position on the whole, colon loc-release. Add enzyme into man-made colon, when enzyme-dependent colon targeting in it, then medicine release quickly, mainly release in fixed position; The conveying time in vivo of pH-dependent and enzyme-dependent capsules have big individuality difference. In the experiment, disintegration is stabilize among individuales, between 2.0-3.5 hours.</p><p><b>CONCLUSION</b>Kangfuxin colon targeting capsules of two principles all release in fixed position to achieve the goal.</p>