The Pharmaceutics Study Of Longyagantai Sustained-release Tablets

Based on original longyagantai capsule, longyagantai sustained release tablets is newdrug project of second research development.the raw material longyagantai capsules comefrom Chinese herbal extract of aralia elata in Heilongjiang province,main components areocleanolic acid,which is the basic components of aralia elata and obtained byextaction,separation,refine of aralia elata,(OA content≥90%), longyagantai capsules haveliver protection detoxification function which had been used clinically for the treatment offatty liver, alcoholic liver,jaundice hepatitis,chronic defer and other liver dieases.Purpose:Aiming at the physicochemical properties of active ingredient-oleanolic acid. it is madeskeleton type Chinese sustained release tablets by using molding excipient and modernpharmaceutical means. Method: In this project, the prescription process of suatained releasetablets of oleanolic acid (basic component in arelia elata), influence factor in vitro releaseand quality standards were studied. In the Study of the sustained-release tablets formulation,several significant factors of suatained release tablets were obtained, such as content ofHPMC, Viscosity, ratio of microcrystalline cellulose and lactose as bulking agent, the type ofgranulation adhesive, according to preliminary screening of literatures and test results. Theinvestigation method was optimized by orthogonal design for4factors above. according totake cumulative release rate in vitro as evaluation Index, the best process route and thecomposition of prescription preparations were determined On the basis of prescriptioncomposition of sustained-release tablets, tablet size and hardness,the releasemedium,pH,rotate speed and other factors are respectively investigated for preparedsustained release tablets,,which have effect on the release rate in vitro of Oleanic acidsustained-release tablets. Release conditions: medium is0.5%sodium dodecylsulfate(Phosphates adjusted pH=7.0±0.1).Rotate speed is100rpm,method is Rotating basketmethod.By relevant requirements of the China pharmacopoeia2010edition volumeⅠ(appendix), we studied character,identification,inspection,content determining and otheraspects. to longyagantai sustained release tablets. Content and release is determined byHPLC,and to which methodology validation is carried.Result: we established qualitystandard of longyagantai sustained release tablets and Formulated quality standard draft.Releasing regularity in vitro is fitted equations,which consistent with higuichequation,12-hour cumulative release rate reach up to90%, it mean having a good releaseproperties. release mechanism in vitro studies have shown that the release mechanism of thesustained-release tablets is synergy among corrosion and diffusion, mainlycorrosi.Conclusion: it is made skeleton type Chinese sustained release tablets by usingmolding excipient and modern pharmaceutical means.Compared with the original capsuleformulation,which can improve the pharmacokinetic properties in vivo and avoid excessiveplasma concentration, reduce drug toxicities, improve patient compliance and otheradvantages.it is particularly suitable for longer course strong defer and other chronic dieases.