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Study On Strychine Solid Lipid Nanoparticles Medicine System

Posted on:2017-05-02Degree:MasterType:Thesis
Country:ChinaCandidate:X Y GuoFull Text:PDF
GTID:2284330482477725Subject:Pharmaceutical
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Strychnine is one of the main active ingredients of the drying mature seed of Strychons nux-vanica L. With the function of exciting spinal cord and nerve center, improving the skeletal tension, anti-tumor, etc. It is mainly used for barbital poisoning rescues, diseases as amblyopia, hemiplegia, etc. The weakness of high toxicity, narrow therapeutic range, poor solubility, short half-life period, speedy metabolism and so on severely limits its clinical application. The main purpose of this study is the adoption of appropriate drug can slow down the speed of strychnine drugs’release and metabolism, effectively prolong the time of drug action to improve therapeutic effect and increase drug safety.Solid lipid nanoparticle (SLN) colloidal drug delivery system with the particle size of 10-1000 nm, function of sustained-release effect and advantages of good biocompatibility, stability, targeting etc, and a higher value of application and research.The emulsion-evaporation prepared SLN is adopted in this experiment. A high performance liquid chromatography (HPLC) analysis method is established to determine the drug’s envelopment rate with a high sensitivity, good reproducibility conforming to the requirements of the methodology. After the optimization of single factor investigation and orthogonal processing, it has selected the optimal technology, contents and storage in prescription, namely the F-68’s concentration of 0.3%,drug/monoglyceride’s proportion of 1:10,monoglycerides/lecithin ratio of 1:2 and the monoglyceride’s quality of 30mg. Physical-chemical investigation on optimized Strychnine SLN has been done. It shows a relatively smooth appearance of a complete sphere by transmission electron microscope (TEM) observation. The measured average particle size is (137.2±3.2) nm, polydispersity index (PDI) is 0.44±0.01,Zeta potential is (-38.9±1.8) mV, and envelopment rate was (72.8±0.8)%.Dynamic membrane method is adopted to simulate the internal environment human body and investigate the release characteristic of strychnine SLN. The release curve of strychnine SLN accords with the Higuchi kinetic equation:Q = 15.826+8.837t1/2(R=0.9837), the external releasing accords with the first-order kinetics equation:In(100-Q)=-0.1084t+4.5274(R=0.9957).It is achieved from the experiment that the strychnine SLN has a sustained-release function. Discovered simultaneously in the study of mice group division, it shows that strychnine SLN is targeted to the liver organ, and has a sustained-release effect comparing to the strychnine solution groups.This study has not only improved the bioavailability of strychnine, reduced the toxic side effect, but also enabled it to slow release and target, formed the foundation of new strychnine dosage’s research laid the foundation, and provided new idea for practice.
Keywords/Search Tags:Strychnine, Solid lipid nanoparticles, Preparation, in vitro release, Tissue distribution
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