Study On Compand RGNa-MH Sustained-Release Tablets

In this thesis, the sustained-release material is HPMC K 100 M. It is granulated by the wet processing and the core of MH sustained-release tablets are made by the technics of pressing. RGNa as ordinary coating material is added in the coating solution and then coat the core of MH sustained-release tablets by the ordinary film coating technology to fabricate RGNa fast-release layer. The preparation methods, influencing factors of MH sustained-release tablets core and RGNa fast-release layer, stability of finished products and so on are inverstigated comprehensively and deeply. The results show that the property of the sustained-release tablets is stable, the part of the fast-release releases rapidly and the part of the sustained- release releases stable and lasting.The HPLC determination methods were established separately for MH and RGNa content, the release (dissolution), the related substances and content uniformity. The results show that the repeatability is good, the result is accurate, it is not affected by excipients and it is fit for in vitro control.Before the formulation study, regard the materials properties, content of RGNa and MH, related substances and so on as the quality index. We research the compatibility between main medicine RGNa and MH, among RGNa, MH and relevant excipients. Results show that compatibility between RGNa and MH is good and the excipients can be used in the study.Regarding release rate as judging the principle, we research the types and specifications of sustained-release matrix materials, the types and concentration of adhesive agents, the amount of lubricant, the method of granulation, the adding ways of HPMC and the pressure of tablets. On the basis of the research results, we adopted the orthogonal test L9 (34) to screen the formulation. The sustained-release tablets core was prepared with HPMC K100M as basic matrix materials of MH, microcrystalline cellulose as filling agent, magnesium stearate as lubricant,5% HPMC E5 and 70% ethanol as adhensive materia1. The core release well and it is total up to the requirement of releasing for 12 hours. Experiments show that it has obvious sustained-release characteristic in vitro, the released rule accords with Higuchi equation and the curve of release and square root of time is nearly linear.The core of MH sustained-release tablets are coated again, that is coating an ordinary film containing RGNa on its outer layer to fabricate RGNa fast-release layer. We have researched and screened the coating materials, the type and concentration of the coating solvent, the concentration of coating solution, the spray pressure of spray gun, temperature and blowing rate of coating, rotating speed of coating pan, RGNa size, increased weight, etc. which affect this technology. Ultimately we determine to use opadry as the coating material and the technology when the weight of film has increased 3% to obtain the RGNa fast-release layer.We also have studied the dissolution in vitro and content uniformity of RGNa in final tablets. The Results show that the RGNa of compound sustained-release tablets can be dissolved desired in 25 minutes and it's content uniformity satisfied the demand. Further experiments show that the outer ordinary film has no effect on the release of the core of MH sustained-release tablets.In the study of stability, using the content, release (or dissolution), and other related substances of MH and RGNa as the detecting index respectively, we have studied the stability of compound RGNa-MH sustained-release tablets under the conditions of high temperature, high humidity, strong slight, acceleration and long-term experiments. The results show that each detecting index of tablets is accord with the No. 0 month, the content of main drug RGNa and MH has no decrease and the related substances haven't increased obviously in the process of storage, the release and dissolution of the product performance well, which shows the stability of the product is fine.