葛根总黄酮缓释制剂研究
摘要画眉鸟的叫声
针对葛根黄酮的溶解性差和其生物利用度低的问题,本研究通过对葛根黄酮采用生物粘附材料,制备胃内滞留型的缓释制剂,以提高葛根黄酮的生物利用度。同时在葛根黄酮生物粘附性胃滞留剂的基础上通过加入漂浮剂也对漂浮和生物粘附协同型的胃内滞留系统进行了考查。
本研究以羟丙基甲基纤维素(HPMC)与卡波姆(CP)为骨架粘附材料,乳糖为致孔剂,同时选用硬脂酸镁为润滑剂,分别采用湿法制粒压片和直接粉末压片的方法制备葛根总黄酮缓释骨架粘附片。采用桨法测定其溶出度检测试验,以葛根素为检测对象,考察了HPMC用量,CP用量,乳糖用量以及三者之间的比例关系对葛根总黄酮缓释骨架粘附片释放度的影响,同时本实验也考查了压力的影响。
另外,本研究在葛根总黄酮缓释骨架粘附片缓释配方的基础上通过加入适量比例的柠檬酸和碳酸氢钠,采用以上两种压片方法,制备了漂浮-生物粘附协同型制剂,并对其释放效果进行了考查。
白敬亭国籍HPMCCP作为缓释制剂的制备材料,均可以延缓葛根黄酮药物的释放,其中CP的缓释效果较强,当两者联合应用于葛根黄酮时,通过调整二者之间的比例,可以达到更好的缓释效果,本研究中当葛根黄酮、HPMC十大童装品牌排名、 CP、乳糖的比例为100:90:21.3:73.7和100:60:45:73.7时,药剂在12小时内可以达到较好的缓释效果和较高的累积释放度张筱雨人体艺术集(可以达到88.9%)。研究发现乳糖在葛根黄酮的药物制备中作为致孔剂可以促进主药的释放,同时制片时压力的大小也对释放度有影响。泡腾性漂浮材料的加入有效促进了药物的漂浮性,使药物达到较好的缓释效果。
关键词 葛根总黄酮,缓释制剂 ,胃滞留系统,体外溶出实验
STUDIES ON THE SUSTAINED-RELEASE FOR-MULATIONS OF GEGEN TOTAL FLAVONOIDS
ABSTRACT
   
To improve the poor solubility and low bioavailability of Gegen flavonoids, this study prep
ared stomach-stranded sustained-release formulations with bioadhesive materials. Based on stomach-stranded sustained-release formulations, by joining the floating-materials, the study test collaborative floating-bioadhesive stomach-stranded system.
We choose HPMC and CP as matrix adhesive materials, lactose as to pore agent, and magnesium as lubricant. Respectively with wet granulation compression way and pressed powder directly way, we chose propeller law as dissolution-testing way and puerarin as detected target, to test the effect of HPMC dosage, CP dosage, lactose dosage and the ratio between the three factors on drug release. At the same time this experiment has also examined the effects of pressure on drug release.
    In addition, by joining citric acid and sodium bicarbonate in stomach-stranded sustained-release formulations related above, this study tested the effect of collaborative floating-bioadhesive system on dug release.
    As matrix adhesive materials, HPMC and CP could keep release of Gegen flavonoids. In test, we found the effect of CP is stronger. When two materials were joined, we found d
rugs were able to keep drugs release better at proper ratio of two materials. In study, we found when the ratio of Gegen flavonoidsHPMCCP喔喔喔、lactose were 100:90:21.3:73.7 and 100:60:45:73.7, drug could keep better release and reach higher release rate in 12h.(88.9%) At the same time we found the lactose could improve the release of drug and the compression had important effect on the release of drug. In test, floating-materials could keep drug floating, and made drug get better release.
KEY WORDS: Gegen flavonoids, sustained-release formulations, stomach-stranded system, dissolution test in vitro
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第1章 前 言    1
§1.1 葛根黄酮的理化性质与药理作用    1
§1.1.1 葛根总黄酮的理化性质    1
§1.1.2 葛根药理作用的研究    1
§1.2 目前已经开发的葛根黄酮类产品    2
§1.3 葛根黄酮的临床研究    3
§1.4 目前缓控释制剂的主要研究    3
§1.4.1 缓控释制剂的定义与类型    3
§1.4.2 胃内滞留给药系统    4
叛逆者剧情§1.5 目前葛根黄酮缓控释制剂产品研究    7
§1.5.1 葛根素的固体分散体    7
§1.5.2 葛根黄酮口服微丸制剂    7
§1.5.3 葛根总黄酮生物粘附片    7
§1.5.4 葛根黄酮缓释胶囊    8
§1.5.5 葛根总黄酮骨架缓释片    8
§1.5.6 葛根黄酮 EC-PEG载药系统    8