Preparation of Compound Danshen Sustained-release Capsula by multiparticulate time-controlled release technology

Objective To prepare Compound Danshen Sustained-release Capsula by using multiparticulate time-controlled release technology.Methods Compound Danshen pellets were prepared with the refined medicinal materials.Then,compound Danshen coat-loaded pellets were prepared in a fluid-bed coater.The coating material of swelling layer was 3% low-substituted hydroxypropylcellulose,2% hydroxypropylmethylcellulose,and 1% sodium dodecyl sulphate.The coating load of swelling layer was 12%.The coating material of controlled layer was 2% ethylcellulose in 90% alcohol solution,mixture of 2% micronization talc and 0.2% diethyl phthalate.Finally,Compound Danshen Sustained-release Capsula was developed by encapsulating the six kinds of coated pellets whose coating load were 0%,8%,16%,20%,24%,and 26% at equivalent ratio in hard gelatin capsule.Results After formulation and coating load of swelling layer were fixed,the coated pellets would release active compositions in the different times expectably through regulating coating level of controlled layer.Several kinds of coated pellets whose controlled layer had different coating load were mixed and encapsulated into Compound Danshen Sustained-release Capsula.In the dissolution medium,the various kinds of coated pellets could release active compositions in accordance with time and show a characteristic of sustained-releasing as a whole.Under the simulated gastrointestinal pH conditions,the in vitro release tests of Compound Danshen Sustained-release Capsula was carried out.The value of similarity factor(f2) of salvianolic acid B and notoginseng saponin,salvianolic acid B and borneol,notoginseng saponin and borneol was 66.9,69.0,and 58.0,respectively.The release profiles of various compositions from Compound Danshen Sustained-release Capsula showed obvious sustained-release characteristic and no significant difference between them.Conclusion The results indicated that the multiparticulate time-controlled release technology made it possible that various components with extremely different physicochemical properties in sustained-release formulations of traditional Chinese medicinal compound recipe could get to release synchronously while sustained-releasing.That complies with the organic whole conception of compound compatibility of traditional Chinese medicinal compound recipe.