Pharmaceutical Research On Enteric Sustained-resease Tablets Of PNS

Panax notoginseng saponins?PNS?has a good effect in the treatment of cardiovascular diseases.However,duo to the drugs are easily destroyed by gastric acid environment after oral administration,which leading to low bioavailability,frequent medication,poor compliance of patients by injection and prone to allergies.Pharmacological studies have show that PNS has a better absorption in the small intestine.In this study,the active ingredients of Panax notoginseng were prepared into HPMC enteric sustained-release tablets,which play a sustained-release effect in the small intestine to avoid the destruction of gastric acid environment and improve the bioavailability of drugs.This study mainly includes the following three parts:1 Study on the preparation Technology of PNS Extract?1?Extraction Technology Taking the total saponin as the evaluation index.The optimum extraction conditions were as follows:adding 8 times the amount of 70%ethanol,90?water bath reflux extraction 3 times and 2 h for each time.?2?Purification Technology Taking the adsorption-resolving rate of total saponins as the evaluation index.The optimum extraction conditions were as follows:resin type D101,sample solution concentration was 0.5 g?raw dose?/ml,adsorption rate was 2 BV/h,sample volume was 2 BV,diameter ratio was 1:7,followed by eluting with 3 BV water and 3 BV 30%ethanol respectively and then eluting with 5BV 75%ethanol at a rate of 2 BV/h.The eluate was collected.?3?Decolorization Technology Taking the total saponin transfer rate and purity as evaluation indexes.The optimum decolorization conditions were as follows:resin type D941,sample solution concentration was 0.2 g?raw dose?/ml,sample flow rate was 1 BV/h,sample volume was 10 BV,when the durg liquids were flushed with resin surface,eluted with 3 BV water and then collected and combined the effluent and the water-washing.?4?Dry Technology Taking the effective contents of total saponins and the status of the extracts after drying as the evaluation indexs.The advantages of the three methods of blast drying,vacuum decompression drying and spray drying were investigated.Finally,the drying method was adopted by vacuum decompression drying at 60°C.?5?Quality evaluation According to Chinese Pharmacopoeia 2015 edition PNS was texted,The results of the checks were in line with the related provisions ofChinese Pharmacopoeia.2 Study on the preparation technology of PNS enteric sustained-release tablets?1?Preparation of sustained release tablets Taking the cumulative release of total saponins as evaluation indexe.The type and the amount of carrier materials,fillers,wetting agents,lubricants were investigated and the optimum conditions were as follows:taken certain PNS powders,HPMC_K15M15M and MCC,the ratio of PNS:HPMC_K15M:MCC was 100:51:92?m:m:m?,mixed up and sprayed with 95%ethanol to prepare soft material,granulated,dried,whole grain and then adding 0.8%magnesium stearate equivalent to the weight of the granules,mixed and compressed.?2?Preparation of coated tablets Taking the cumulative release of total saponins as evaluation indexe.the optimum conditions were as follows:used HP-55,talc as the coating prescription solution,the weight of the coating is about 8%of the sustained-release tablet,after the coating is finished,dried the tablet.3 Study on the quality standard and stability of PNS enteric sustained-release tabletsTo investigate the traits,identification,routine examination and determination of the total saponins of Panax notoginseng,and to establish the quality standard of the total saponin enteric-coated sustained-release tablets.At the same time,the stability and long-term stability of Panax notoginseng saponin enteric sustained-release tablets were observed for 6 months.As a result,the stability of the preparation was better.