Preparation And Research Of Kaempferol Microporous Osmotic Pump Tablet

Objective: Kaempferol(KAE),also known as kaempferol,kaempferol,kaempferol,etc.,is a widespread flavonoid active ingredient found in various natural plants,and a large number of pharmacological studies have now shown that kaempferol has anti-inflammatory,antioxidant,antidepressant,anticonvulsant,anticancer,antidementia,protection of ischemic brain tissue and prevention of cardiovascular disease and other clinical pharmacological activities,but its contained phenolic hydroxyl group causes it to be relatively sensitive to the surrounding environment,instable.In addition,kaempferol has poor water solubility and low oral bioavailability,so the method of multiple administrations is used to maintain a stable and effective blood drug concentration,but repeated administration easily leads to fluctuation of the blood drug concentration,poor compliance of patients,at the same time,the body kidney,heart and other important organs will be damaged.These characteristics of kaempferol severely limit its further development and utilization,therefore,improving the bioavailability of kaempferol is very important for its clinical promotion and practical application,and will also provide a whole new and effective means of medicine for the treatment of diseases such as cardiovascular diseases.Osmotic pump tablets are a typical representative of sustained-release formulations,which release at a uniform constant rate in the body,and this release behavior will hardly be affected by gastrointestinal p H,contents,and other factors,so it is very suitable for the preparation of drugs with poor solubility,so osmotic pump tablets are one of the first choice in oral biologically controlled release formulations.The microporous osmotic pump sheet is a type of osmotic pump sheet which is prepared by pressing the chip core with the master drug,excipients and permeation enhancers and coating the controlled release film containing porogen,in the medium,water enters the chip core by dissolving the formed micropores with porogen,the master drug and permeation enhancer are dissolved to form osmotic pressure,and finally,the drug is released through the micropores of the controlled release film.Because the microporous osmotic pump tablets do not need to make holes in the coated membrane,the preparation process is simple,and because of the poor water solubility of kaempferol,a part of the weakly basic excipients will be added to the prescription of the chip core in the hope of increasing the solubility of kaempferol and enhancing its bioavailability to improve its release after preparation into the microporous osmotic pump tablets.Methods: Based on pre prescription research,this study firstly conducted a single factor examination of prescribing and process.Lactose,compressible starch,sodium chloride,hydroxypropyl methylcellulose(HPMC),povidone K30(PVP K30)sodium dodecyl sulfate were used as chip materials;Microwell osmotic pump controlled release tablets of kaempferol were prepared by using acetone solution of diethyl phthalate(DEP),cellulose acetate(CA),polyethylene glycol(PEG-400)as coating liquid.Through single factor examination,the drug release degree was used as an index study and screened to optimize the prescription.Results: The best prescription of chip core was: kaempferol(18%),Na Cl(15%)and lactose(30%)mixed as osmotic enhancers,compressible starch(1%),HPMC(27%),SDS(2%),and pvpk30(7%).The coating liquid was the best prescription: the coating weight gain was 4% of the chip core,the amount of porogen PEG-400 was40%,and the amount of plasticizer dep was 30%.The cumulative release rate of this pump chip for 12 h reached more than 85%.Conclusion: Kaempferol microporous osmotic pump tablets the preparation of kaempferol microporous osmotic pump tablets is simple,effective and reproducible,and the prepared kaempferol microporous osmotic pump tablets can achieve the expected controlled release effect.