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Research on Chitosan-based Drug-releasing Materials

Author: LuoHuaLi
Tutor: LuZaiJun
School: Shandong University
Course: Polymer Chemistry and Physics
Keywords: Chitosan Release Polyvinyl alcohol Polyacrylic acid Levofloxacin Sodium salicylate
CLC: TQ460.4
Type: Master's thesis
Year: 2007
Downloads: 631
Quote: 4
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Chitosan is a naturally occurring single basic polysaccharide, nontoxic, biodegradable in vivo, chitosan is chitin through alkaline hydrolysis or after removal of part of acetyl product of glucosamine glycans. Compared chitin chitosan, chitin by chemical treatment has been off the acetyl group, can be dissolved in acid, easily absorbed and used, chitosan applied research and development in today's domestic and foreign substances chitin research, development Trends. By controlling the release rate of drug release formulations to achieve the desired concentration in human blood, reducing the frequency of administration, adverse reactions reduce the body, increase efficacy, is the development direction of pharmaceutical preparations. Natural polymers such as chitosan release carrier substrate, the relative synthetic material, not only can regulate a stable plasma therapeutic concentrations, reducing the frequency of administration, reducing the strong stimulating effect on the gastrointestinal tract, and can participate in the body's natural metabolism, does not accumulate in the body. This study is carried out of drug selection Ofloxacin hydrochloride and sodium salicylate, the former is a third-generation fluoroquinolones, a variety of gram-negative and positive bacteria have antibacterial activity, half-life of six hours, while the latter has anti-fungal, antipyretic, analgesic, anti-rheumatic effect for the active treatment of rheumatism and rheumatoid arthritis. In this study, the main material of chitosan as a carrier, respectively inverse suspension crosslinking method, the application of an amine aldehyde condensation, aldol condensation principle and chemical polymerization techniques, were prepared by the drug release microspheres of chitosan and chitosan and polyvinyl alcohol physical blending the drug release microspheres of chitosan crosslinked polyvinyl alcohol drug release microspheres containing chitosan - polyacrylic acid - polyethylene glycol ternary complex sustained release microspheres obtained The main contents and results are as follows: 1, through inverse suspension crosslinked chitosan microspheres were prepared and levofloxacin drug-loaded microspheres, using scanning electron microscopy, microscope, IR, UV spectrophotometer and drug dissolution tester right drug-loaded chitosan microspheres and microspheres were characterized discussed acetic acid concentration, concentration of chitosan, chitosan deacetylation degree, emulsifier, oil-water ratio, crosslinking density, reaction time, stirring, drug / substrate ratio on the microsphere average particle size and particle size distribution, drug concentration, sustained performance can be obtained microsphere size, 20 ~ 200μm, rounded surface, dispersion of up to 0.3, levofloxacin chitosan Sugar microsphere drug loading capacity of up to 17%, 12hr cumulative release in vitro dissolution was up 52%; Chitosan Microspheres sodium salicylate drug loading of 21.6%, the release curve showed a good linear relationship, sustainable release 8hr drugs more and has excellent sustained release delivery characteristics bowel. 2 to chitosan and polyvinyl acetate solution as the aqueous phase containing the emulsifier liquid paraffin as the oil phase, were used at room temperature modification methods (physical blending) Preparation of drug-loaded microspheres modified Ⅰ and high-temperature acid-catalyzed methods (chemical crosslinking) Preparation of drug-loaded microspheres Ⅱ. By infrared spectroscopy, microscopy, ultraviolet spectrophotometer and drug dissolution instrument, such as the materials of construction and application performance characterization results showed that chitosan / PVA composite microspheres Ⅰ average particle size of 1 ~ 20μm, drug loading 13% , LVFX 12hr vitro cumulative release 80%; chitosan / PVA composite microspheres Ⅱ average particle size of 1.69μm, drug content 17.1%, LVFX vitro 6hr almost completely released. 3, with emulsifier-containing liquid paraffin as the oil phase, with chitosan / polyethylene glycol acetate solution as the aqueous phase by chemical glutaraldehyde crosslinked chitosan, chitosan inverse suspension polymerization / Polyethylene glycol salicylate drug-loaded microspheres. By infrared spectroscopy, microscopy, ultraviolet spectrophotometer and drug dissolution instrument, such as the materials of construction and application performance characterization results showed that the average particle size of microspheres 60.0μm, dispersion 0.52 2.61% drug loading capacity. 4, the use of chemical polymerization and physical blending two methods chitosan / polyacrylic acid / polyethylene glycol blends containing three yuan SA microspheres. By infrared spectroscopy, microscopy, ultraviolet spectrophotometer and drug dissolution instrument, such as the materials of construction and application performance characterization results show that chemical polymerization method microsphere average diameter 16.1μm, amounted to 3.8% drug loading, physical blending method as obtained microsphere size 8.76μm, drug loading capacity of 3.0%.

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