Study On The Preparation And Quality Standards Of Radix Linderae Floating Sustation Release Tablet

Floating drug delivery system is one of the approaches to increase the retention time of an oral dosage from in the stomach.FDDS have a bulk density lower than gastric fluids and thus remain buoyancy in the stomach without affecting the gastric emptying rate for a prolonged period of time.This study use linderalactone、linderane、isolinderalactone as the model drug,HPMC as the main hydrophilic matrix, octadecanol as bleaching agent,NaHCO3 as gas-generating agent,PVP as porogeneous compound,MCC as diluent to regulat weights of tablets.At the basis of pre-experiments,we find the impact of floating and release factors, use orthogonal design to optimize the prescription,which have ideal buoyancy and drug release characteristics.From the results of release mechanism,we can find the release of radix linderae floating tablets can finely fitted with zero-order release equation,which was indicated that the drug was released by diffusion and corrcosion mechanism according to Peppas equation(0.45<n<0.89).According to the stability study of Radix Lindeare,this agent should avoid of humidity and high temperature,otherwise the buoyancy will be affected. 1. Study of prepation(1) Study of conconte technology:with the content of linderalactone、linderane、isolinderalactone as evaluating indexes,we deal the data with the normalization and combination score method,the optimum conconte technology confirmed by the contradistinction investigations and orthogonal design was:add 20g vinegar per 100g of the Radix Lindeare,put 60min,baking 120min at 60℃.(2) Study of the traction:Use the extraction content of linderalactone、linderaneand extracting ratio as evaluating indexes, deal the data with the normalization and combination score method,the optimum alcohol extraction confirmed by the contradistinction investigations and orthogonal design was:30min of soaking,2 times of refluxing with 70% alcohol,8/6 times of alcohol-adding amount and 1.5/1.0 hours of refluxing time respectively.(3) Study of the concentration and desiccation:Accoding to the comparison test,we choose the changed content of linderalactone、linderaneand after concentrate and desiccat as evaluating indexes,determine the physic liquor was decompression concentrated at 60℃,the vacuity was-0.08MPa.The best desiccation technology was 60℃,0.08MPa.(4) Study of the preparation process:Use the floating performance and vitro release performance as the evaluating indexes to charge the type and amount of the accessories,through direct observation and orthogonal design,we sure the best preparation process was whole-powder Compression,the hardness keep with the range of 3-4kg,use 400ml 0.1mol/L hydrochloric acid solution with 0.5%SDS as the release excitatory transmitter.The optimized prescription is:main drug:HPMC(K15M):Octadecanol:NaHCO3:PVPK30:MCC=25%:30%:15%:5%:20 %.2 Study of quality standardsUse Thin-layer chromatography to identify Radix Linderea,and use HPLC to determine the content of linderalactone、linderane、isolinderalactone,then do the methodology research. The average recovery rate of linderalactone was 99.13%, RSD was 1.22%; the average recovery rate of linderane was 99.88%, RSD was 0.99%; the average recovery rate of isolinderalactone was 98.66%, RSD was 1.22%. The result indicate that this method was simply and reliable and can be applied for quality control.