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Studys Of Nimodipine Sustained-release Tablets

Posted on:2014-02-01Degree:MasterType:Thesis
Country:ChinaCandidate:L C MaoFull Text:PDF
GTID:2231330395997141Subject:Medicinal chemistry
Abstract/Summary:PDF Full Text Request
Nimodipine is a polar second generation pyridine calcium antagonist, in recent years isthe preferred drug for treatment of hypertension,it can reduce the fragility of red bloodcell and blood viscosity,inhibition of platelet aggregation anti-thrombotic.In suitabledosage,selective cerebral vascular expansion, no effect on peripheral vascular.Since it hardlyaffect peripheral vascular, commonly used on curing cerebrovascular disease.It can be usedeffectively in prevention and treatment of cerebral vasospasm caused by subarachnoidhemorrhage which caused by cerebral ischemia damage.However, based on first pass effectof hepar, its short half-life, the low bioavailability (5%~10%) and poor patient compliance,we need to adopt new technology to improve the bioavailability and decrease reaction time.In this paper, the prescription of nimodipine sustained-release tablets were screened,including the preparation of nimodipine solid dispersion, the carrier and its usage in the hotmelt extrusion process, sustained-release tablets release blocker nimodipinethe use ofsodium carboxymethyl cellulose (CMC-NA), methyl cellulose (MC), ethyl cellulose (EC),hydroxypropyl cellulose (HPC) and hydroxypropyl methylcellulose (HPMC) were measuredas a blocker, release, and ultimately determine the HPMC sustained release tablets blocker, and to determine the amount of prescription screening.Uniform Design formulation has beenoptimized to filter out the best prescription: Nimodipine50mg, PVP50mg HPMC120mg,compressible starch70mg magnesium stearate0.18mg.Uniform Design formulation hasbeen optimized to filter out the best prescription: Nimodipine50mg, PVP50mgHPMC120mg, compressible starch70mg magnesium stearate0.18mg.Studies on the quality standard of Nimodipine sustained-release tablets, includingsustained-release tablets assay, accessories interference experiment, precision inspection,reproducible experimental method recovery experiments and the release.UV-visiblespectrophotometer to determine the release, including the release of the uniform experiment,the experimental results show that between batches, batch process reproducibility.Using highperformance liquid chromatography method studies confirm that the detection method isfeasible, with good reproducibility.Finally, we study the stability of the sustained release tablets,The influencing factorsExperimental results show that Nimodipine Sustained-Release Tablets in high temperature,high humidity conditions no significant change in character, content and release of thepreparations,And accelerated testing of six months and12months of long-term trials,experimental results, the project examined the indicators are relatively stable, various targets are qualified, indicate the mass stabilization of Nimodipine tablet.In this thesis, by selecting the optimal ratio of accessories prescription, combined withhot-melt extrusion technique to obtain better sustained release tablets in vitrorelease.Thereby enhancing the bioavailability of a drug, while reducing the number ofmedication to improve the clinical effect of nimodipine preparation, to reduce adverse drugreactions, and improved patient compliance.
Keywords/Search Tags:Nimodipine, sustained release tablets, the solid dispersion, the release, the quality standard
PDF Full Text Request
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