大鼠奥昔布宁片剂口服给药与凝胶剂经皮给药吸收与组织分布研究(英文)  

Study on absorption and distribution of oxybutynin oral tablet and transdermal gel in rats

作　　者：温清[1] 冯堃[2] 郭瑞臣[3] 

机构地区：[1]济南市中心医院药学部 [2]山东中医药大学第二附属医院药学部 [3]山东大学齐鲁医院临床药理研究所

出　　处：《中国临床药理学与治疗学》2006年第5期586-589,共4页Chinese Journal of Clinical Pharmacology and Therapeutics

摘　　要：目的:考察口服和外用给药奥昔布宁在大鼠体内的吸收和分布。方法:48只大鼠随机分为两组:一组外用给予单剂0 .1 g奥昔布宁自制凝胶(2 mg OXY) ,一组给予单剂0 .5 mg普通片剂。收集血样、膀胱和肝脏样本,采用高效液相色谱-质谱法测定奥昔布宁浓度。结果:凝胶剂外用给药奥昔布宁膀胱组织浓度为血浆的800倍,而口服给药为70倍。奥昔布宁凝胶剂半衰期延长为5 .99 h,而口服给药为2 .18 h。结论:奥昔布宁凝胶剂半衰期延长,作用部位膀胱组织浓度高,与片剂相比具有明显的优势。AIM： To study the absorption and distribution characteristics of oxybutynin （OXY） oral tablet and transdermal gel. METHODS： A single dose of 0.1 g OXY transdermal gel （2 mg OXY） was applied to abdominal area about 4 cm^2 and 0.5 mg immediate-release tablet was orally given to 48 rats in a randomized, open-label, control design test. The plasma, bladder and liver tissue were collected, disposed and analyzed and OXY pharmacokinetic parameters were calculated and evaluated. RESULTS： The Cmax of OXY transdermal gel and oral tablets in bladder are approximately 800 and 70 times higher than those in plasma. The plasma half life of OXY gel delayed 5.99 h, tablets 2.18 h. CONCLUSION： OXY gel show better pharmacokinetic properties, characterized with long half life and high target organ concentrations than those of tablets.

关 键 词：奥昔布宁 凝胶 药代动力学 高效液相-质谱 大鼠 

分 类 号：R969[医药卫生—药理学]