噻吗心安经皮吸收制剂的体内生物利用度  

THE BIOAVAILABILITY OF TRANSDERMAL THERAPEUTIC SYSTEM OF TIMOLOL

作　　者：冀学芳[1] 平其能[1] 刘国杰[1] 于顺廷[1] 

机构地区：[1]中国药科大学药剂研究室

出　　处：《药学学报》1993年第8期609-613,共5页Acta Pharmaceutica Sinica

摘　　要：噻吗心安经皮吸收制剂选用PVA-0486作为骨架材料,由4层(背衬层、含药膜层、压敏胶层、保护层)组成。建立了HPLC方法检测血浆中噻吗心安的含量,以Zorbax ODS柱分离,流动相为乙腈—水—磷酸—三乙胺,在294 nm处检测,采用外标法峰面积定量。用本法对9名健康志愿者进行了噻吗心安贴剂和噻吗心安片剂的血药浓度测定,结果表明:噻吗心安贴剂贴用4 h开始达到治疗浓度,可持续32 h,血浓稳定,人体内为一室模型、零级吸收。A matrix-type transdermal therapeutic system of timolol (TTS-timolol) was well prepared. The patch consisted of backing membrane layer, timolol reservoir layer, pressure sensitive adhesive layer and protective layer. A sensitive and reliable HPLC-UV method for the determination of plasma level of timolol in healthy volunteers was developed. Effective therapeutic plasma level of timolol (4 ng/ml) was attained 4 h after application of the timolol patches and was maintained within 32 h while the patch was removed at 24 h. The pharmacokinetic behavior of this transdermal therapeutic system (TTS)-timolol in human showed zero order absorption and well fitted to a one compartment model. The pharmacokinetic parameters are: T_(max)= 18. 8h; C_(max)= 11.2 ng/ml; AUC= 265. 7 ng/ml·h; V_(ss)=120. 0L; K=0. 084 h_(-1). In comparison with the results of oral administration of timolol tablets, TTS-timolol possesses some advantages: stable plasma level, long effective time and convenient administration.

关 键 词：噻吗心安 生物利用度 高效液相色 

分 类 号：R972.4[医药卫生—药品]