Study Of Aspirin Enteric Sustained-release Tablets

Objective: Aspirin is an application of the historic non-steroidalanti-inflammatory drugs, in recent years it is becoming the treatment ofthromboembolic disease drug of choice. When human blood platelets are activated,intracellular calcium ion concentration increased, the cell membrane phospholipidswill release arachidonic acid, arachidonic acid, respectively, in the role ofcyclooxygenase converted to thromboxane A2and prostacyclin, and aspirin Byacetylation inactivation of cyclooxygenase, thereby enabling the decreased productionof thromboxane A2, and thus inhibit platelet aggregation, reduce the incidence ofblood vessel blockage, effectively preventing thrombosis purposes, commonly used incoronary heart attack caused by blood clots (AMI) and angina; cerebral stroke causedby cerebral embolism; pulmonary embolism caused by pulmonary embolism,pulmonary heart disease; limb arterial embolism caused by pain or necrosis, limbvenous thrombosis due to local edema and pain. However, large doses of aspirin couldeasily lead to gastrointestinal side effects, such as stomach ulcers, gastrointestinalbleeding or perforation. Dosage forms are to be altered, thereby reducing theoccurrence of adverse reactions and prolong half-life drugs, slow release, so that largefluctuations in plasma concentration does not occur in a long time, to improveefficacy, to better improve the bioavailability.In this paper, the process of preparationand quality standards of Aspirin enteric sustained-release tablets processes werestudied. Methods: In this paper, the prescription of Aspirin enteric sustained-releasetablets were screened by Release experiments, Uniform Design formμlation has beenoptimized to filter out the best prescription, expand the amount of prescriptions to100times, conducted pilot experiments to verify the feasibility of prescription andreasonable. Quality standards inspection for Aspirin enteric sustained-release tabletswere investigated by UV-visible spectrophotometer measured release, methodologystudy conducted by high performance liquid chromatography. Finally, we study thestability of the Aspirin enteric sustained-release tablets, including the factors studyunder high temperature, high hμmidity conditions, And accelerated testing of sixmonths and12months of long-term trials, examining their appearance, and releasechanges in content. Resμlts: The best prescription: aspirin25g, starch9g, SDS0.75g,microcrystalline cellμlose2g, HPMC（K15M）5.25g, talcμm powder1g,3%PVPalcohol solution amount. The pilot test resμlts show the prescription in line withnational standards. Examine the resμlts of Aspirin enteric sustained-release tabletsquality standard, confirming that the process is feasible, with good reproducibility.The resμlt of the stability of the Aspirin enteric sustained-release tablets showed nosignificant changes in quality and stability of the process for the preparation ofAspirin enteric sustained-release tablets. Conclusion: By selecting the optimal prescription paper materials ratio, obtained better in vitro release Aspirin entericsustained-release tablets, thus reducing the adverse gastrointestinal reactionssimμltaneously improve its bioavailability, while reducing the nμmber of medication,the drug slow release, reaching a steady state plasma concentration, improve clinicaleffect of aspirin enteric-coated sustained release tablets, improved patient compliance.