江西农业大学学报
江西農業大學學報
강서농업대학학보
ACTA AGRICULTURAE UNIVERSITATIS JIANGXIENSIS
2014年
2期
413-417
,共5页
鲍光明%梅天笑%袁厚群%黄爱平%王小莺%钱晶晶%肖雪菲%李丽金%陈宇
鮑光明%梅天笑%袁厚群%黃愛平%王小鶯%錢晶晶%肖雪菲%李麗金%陳宇
포광명%매천소%원후군%황애평%왕소앵%전정정%초설비%리려금%진우
淀粉-氧氟沙星偶联物%接入率%体外释放%前药
澱粉-氧氟沙星偶聯物%接入率%體外釋放%前藥
정분-양불사성우련물%접입솔%체외석방%전약
starch-ofloxacin conjugation%drug-loading ratio%in vitro release%prodrug
以淀粉和氧氟沙星为原料,合成了淀粉支载的氧氟沙星高分子前药,用核磁共振氢谱对其结构进行了结构表征、紫外分光光度计测定了氧氟沙星的接入率,并在人工胃液和人工肠液中进行了体外释放研究。结果清楚显示氧氟沙星成功接入到淀粉分子上,该高分子前药在不同介质的体外释放中均呈现零级缓慢释药,与氧氟沙星相比较,其作用时间明显增长,可以有效减缓药物成分的释放,控制血药浓度,有望大大减轻药物对胃粘膜和肠的刺激作用,并解决氧氟沙星的味苦及难溶等问题。
以澱粉和氧氟沙星為原料,閤成瞭澱粉支載的氧氟沙星高分子前藥,用覈磁共振氫譜對其結構進行瞭結構錶徵、紫外分光光度計測定瞭氧氟沙星的接入率,併在人工胃液和人工腸液中進行瞭體外釋放研究。結果清楚顯示氧氟沙星成功接入到澱粉分子上,該高分子前藥在不同介質的體外釋放中均呈現零級緩慢釋藥,與氧氟沙星相比較,其作用時間明顯增長,可以有效減緩藥物成分的釋放,控製血藥濃度,有望大大減輕藥物對胃粘膜和腸的刺激作用,併解決氧氟沙星的味苦及難溶等問題。
이정분화양불사성위원료,합성료정분지재적양불사성고분자전약,용핵자공진경보대기결구진행료결구표정、자외분광광도계측정료양불사성적접입솔,병재인공위액화인공장액중진행료체외석방연구。결과청초현시양불사성성공접입도정분분자상,해고분자전약재불동개질적체외석방중균정현령급완만석약,여양불사성상비교,기작용시간명현증장,가이유효감완약물성분적석방,공제혈약농도,유망대대감경약물대위점막화장적자격작용,병해결양불사성적미고급난용등문제。
In order to obtain a sustained-release nicotinic acid ,starch-nicotinic acid conjugation was syn-thesized by coupling between starch and nicotinyl chloride .Its structure was characterized with FTIR and 1H-NMR.The drug-loading ratio of the product was measured by ultraviolet spectrophotometer .And in vitro drug release investigation was carried out in artificial gastric juice and artificial intestinal juice .The results clearly showed that nicotinic acid was coupled with the starch molecule successfully and the drug release rate of the conjugatation was nearly zero order without abrupt release .Compared with nicotinic acid , the effective thera-peutic time of the polymer prodrug was prolonged .So it may lead to less side-effect and relieving stimulation on gastrointestinal tract .