Study On The Sustained-release Capsules Of Ibuprofen

Objective:Use different process to prepare ibuprofen suatained-release capsule,and create the assay method of the release rates in vitro and injection of it,investigate the in vitro release rates of different ibuprofen sustained-release capsules,thus f2 factor was calculated to compare their similarity with Fenbid.The releasing mechanism of sustained-release capsule was primarily studied.Methods:Extrusion-spheronization technique was introduced to prepare ibuprofen sustained-release capsule,MCC was used as filling substance.Yield,particle size and particle size distribution,the roundness and releasing degree in vitro were used as indicators to evaluate pellets quality.To determine the prescription and process parameters by the single factor investigated,then orthogonal design were used to optimize the experiment technology.Ibuprofen sustained-release pellets were prepared in a centrifugal granulation by powder layer technology with stearic acid as blocker,talcum powder as flow aid agent,PVP ethanol solution as adhesive agent,optimize the prescription.Adjust the instrument parameters to determine the best process.A fluid-bed spray processor was adopted for preparing pellets.To determine the process parameters by the single factor investigation.Single factor screening was used to initially identify the prescription.The prescription was excellently screened with L9(34)orthogonal design,and three influencing factors such as EC,HPMC and triethyl citrate were selected,each factor take three levels.The releasing rate of each prescription in vitro was determined and analyzed so as to choose the best.A UV-HPLC method was developed to determine in the in vitro release and content.Determine release rate of ibuprofen sustained-release capsules prepared by different methods and Fenbid in different rotation speed and different release medium,release curve was used to fit different equation,f2 factor was calculated to compare their similarity with Fenbid.Explore the mechanism of drug release in pH 6.0 PBS.Result:Identify ibuprofen sustained-release capsules prescription and best technology of different methods,cumulative release percentage of the three kind of capsules are all in line with the requirements.UV-HPLC method was developed to determine the releasing degree in vitro.The concentration of ibuprofen and AUC were linear over the range of 19.96?g·mL-1-399.20?g·mL-1.The inter-day RSD was 0.06%(n=6).The mean absolute recoverie is 100.62%(n=9).The stability of the different solution within 24 hrs is acceptable which showed this method was accurate,reliable and reproducible.The similarity factor comparison results indicated that sustained-release capsules made by fluidized bed method had the highest similarity.The releasing mechanism of ibuprofen sustained-release capsule in pH6.0 phosphate buffer was primarily studied.The release model fitting results show that,the release curves of ibuprofen sustained-release capsule prepared by the three methods and Fenbid best meet the first-order equation.Ritger-Peppas model fitting results show that n values are all between 0.43 and 0.85,and the mechanism of drug release are diffusion combining the skeleton dissolution mechanism.Conclusion:The ibuprofen sustained-release capsules prepared by fluid-bed spray processor have high similarity with Fenbid.This assay method is sensitive,accurate,simple and feasible.