Study Of Helicid Bioadhesive Sustain-release Tablet And Evaluation Of Relativity In Vivo And In Vitro

The paper discussed the consideration and method to produce the sustained-release tablet using traditional Chinese medicine -Helicid (HD) as the model drug under the principles of biopharmaceutics and pharmacokinetics. Bioadhesion and sustained-release techniques were employed to prepare sustained-release tablet which could release twelve hours continuously in vitro using A and B as bioadhesive materials, C as compression aid, magnesium stearate as lubricant.In the study of adhesive force determination in vitro and its influence factors, a self-made apparatus was used to determine the adhesive force and screen prescription. The results of influence factors exploration showed that low dropping rate had little influence but the cohesive force increased with the enhance of dropping rate; cohesive force was incorporation with the pressing time; pressure had significant influence on the cohesive force. The adhesive force between biohesive preparation and intestinal mucous membrane increased linearly in a definite range of pressure, and the two cohesive forces both were 50g when the pressure were 100g and 120g.In the study of prescription screening and technique modifying, the dissolubility in water and adhesive force to small intestine of HD were employed as indices. Single-factor and orthogonal test were used to screen the category and amount of addendum. The dissolution experiment showed that under the dissolution conditions the accumulated dissolubility of HD in the sustained-release tablets at 2h, 6h, 10h were 20～40%, 50～70%, >75% respectively. The sustained-release tablets after modification had good dissolution recovery and the technique was stable.According to the sustained-release and control-release preparation guidance in the second part of "Chinese Pharmacopoeia" 2000 edition (appendix XIXD) and requirements of tablet items (appendix IIA), the identification method of HD...