Synthesis And Bioavailability Of Novel Anti-inflammatory Drugs Ibuprofen Ester Nanoparticles

Traditional non-steroidal anti-inflammatory drugs inhibit both COX-1 and COX-2,but have side effects ongastrointestinal and renal.COX-2 selective inhibitors can prevent or reduce toxic side effects on the gastrointestinal tract while exerting anti-inflammatory and analgesic effects.The carrier molecule is chemically linked to the poorly soluble prodrug to increase the drug's selectivity for the purpose of increasing drug absorption,and is also referred to as the carrier prodrug.The non-steroidal anti-inflammatory drug is designed as an ester carrier,and the drug-soluble preparations are developed in different ways by utilizing the characteristics of fat-soluble property,thereby expanding the route of administration of the drug.The poorly soluble modified fat-soluble carrier is one of the improved pharmaceutical preparations,which can increase the solubility of the poorly soluble drug in vegetable oil,and can be made into an intravenous liposome or a nano-microemulsion.Ibuprofen has antipyretic and analgesic effects.It is currently the most widely used non-steroidal anti-inflammatory drug in the world.Ibuprofen lacks selectivity for COX-1 and COX-2,and long-term use may cause various gastrointestinal irritation symptoms,which may cause renal failure.Therefore,the development of new ibuprofen sustained release drugs,improve and reduce its toxic side effects,and achieve the key technology independent intellectual property rights is the inevitable demand for the industrialization of the drug.This paper is based on the above defects of ibuprofen and modified it into ethyl esters.Ibuprofen ester was dissolved in vegetable oil to explore the process technology for preparing intravenously injectable ibuprofen ester nanolipid microsphere emulsion.The pharmacokinetic behavior of the relevant drugs in animals and humans was comprehensively investigated by experiments of intravenous and oral administration of animals(dogs)and computer simulations.Predict the pharmacokinetic behavior of related drugs in the human body,and investigate the absorption and distribution characteristics of drugs in the human body.It lays a good foundation for the application of ibuprofen.The pharmacokinetic behavior of related drugs in animals and humans was comprehensively investigated by the results of intravenous and oral administration of animals(dogs)and computer simulations.Bioavailability studies include:(1)aggregation and analysis of kinetic measurements of dog veins and oral ibuprofen and its esters;(2)modeling with software GastroPlus to simulate the drug-related intravenous and oral administration in dogs The behavior was compared with the measured results;(3)Using software GastroPlus to predict the pharmacokinetic behavior of related drugs in the human body based on the drug model of the dog,and to investigate the absorption and distribution characteristics of the three drugs in the human body.