盐酸雷尼替丁胃内滞留漂浮型缓释片研制以及犬体内药物动力学  被引量:1

Pharmacokinetic study of ranitidine hydrochloride remaining-floating sustained release tablet in stomach

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作  者:马勇[1] 陈国广[1] 韦萍[1] 屠锡德[2] 蔺胜照[1] 

机构地区:[1]南京工业大学制药与生命科学学院,江苏南京210009 [2]中国药科大学药剂学教研室,江苏南京210009

出  处:《南京工业大学学报(自然科学版)》2005年第5期54-57,共4页Journal of Nanjing Tech University(Natural Science Edition)

摘  要:制备了24 h盐酸雷尼替丁胃内滞留漂浮型缓释片(RH RFSRT)。以水凝胶骨架作为胃内滞留漂浮型缓释片材料处方,研究了制剂体外释放度,漂浮性能以及对制剂在犬体内的药物动力学进行了初步研究。实验结果表明:RH RFSRT的累积释放百分率符合H iguch i方程;体内药物动力学参数为AUC=25 571.691 ng.h/mL,MRT=5.2 h,mρax=5 867.98 ng/mL,相对生物利用度为178.16%。该制剂制备工艺简单,质量稳定,可以延长体内滞留时间并能提高生物利用度。To prepare 24 h ranitidine hydrochloride remaining-floating sustained-release tablet (RH-RFSRT) in stomach. The tables were prepared by the use of HPMC as gel matrix. In vitro release rate and floating capability were observed to evaluate the formulation. Preliminary in vivo evaluation was carried out in dogs. The accumulation rates of RH-RFSRT were conformed to the Higuchi equation. The values of pharmacokinetics: AUC = 25 571. 691 h · ng/mL,MRT=5.2 h, Pmax =5 867. 98 ng/mL. Relative bioavailability of RH-RFSRT was 178.16%. The technology of preparation of RH is simple, its quality is stable and release rates are sustained. RH-RFSRT is capable of remaining floating on gastric fluid, which contribute to its prolonged the gastric resident time, and has an enhanced bioavailability and sustained action as compared with the capsule of RH.

关 键 词:盐酸雷尼替丁 胃内滞留漂浮型缓释片 药物动力学 

分 类 号:R944.4[医药卫生—药剂学]

 

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