摘要
目的：研究国产噻氯匹定片剂与进口同种产品的生物利用度及其药动学特性。方法：８名健康成年受试者，男女各半，随机交叉分组试验法分别按每１２ｈｐｏ２５０ｍｇ国产和进口噻氯匹定连续５个剂量。采用作者建立的ＨＰＬＣ测定血药浓度。结果：国产和进口片剂的动力学参数：ｃｍａｘ（ｓｓ）分别为２．０８±１．２４ｍｇ／Ｌ和１．６６±０．３７ｍｇ／Ｌ，Ｔｍａｘ分别为０．９７±０．４２ｈ和１．２２±０．３８ｈ，β分别为０．０８８±０．０２６ｈ－１和０．０８０±０．０４０ｈ－１，表观分布容积Ｖｄ／Ｆ分别为７３．６０±２１．５０Ｌ和９１．９６±２９．８０Ｌ，吸收速率常数Ｋ０１分别为５．１９２±５．４８９ｈ－１和５．８５１±５．８３２ｈ－１；稳态后梯形法求得的ＡＵＣ（４８～６０ｈ）分别为６．３２±１．２１（ｈ·ｍｇ）／Ｌ和６．２４±１．８０（ｈ·ｍｇ）／Ｌ。结论：两种片剂的药动学参数无统计学差异（Ｐ＞０．０５）。与进口片剂相比，国产片剂的平均相对生物利用度为９９．９７％±２６．５１％。
OBJECTIVE:Pharmacokineticsandbioavailabilityofdomesticandimportedticlopidinetabletswerecomparedinhealthyvolunteersafteroraladministration.METHODS:Eighthealthyvolunteersweregivenoraly500mgtabletstwiceadayfor5doses.Thebloodsampleswerecolectedafterthe5thdoseandticlopidinelevelsweredeterminedbyHPLC.ThePCNONLINsoftware(v.4.2)andnon-compartmentmodelanalysiswereusedforthecalculationofpharmacokineticsandrelative-bioavailability,respectively.RESULTS:Thepharmacokineticpa-rametersofdomesticandimportedtabletswereTmax=0.97±0.43hand1.22±0.38h,cmax(ss)=2.08±1.241mg/Land1.66±0.37mg/L,T1/2(β)=8.53±2.55hand12.18±8.08h,β=0.088±0.026h-1and0.080±0.040h-1,theVd/Fwere73.60±21.50Land91.96±29.80L,respectively.TheAUCτcalculatedbythetrapezoidalrulewas6.19±1.49(h·mg)/Land6.36±1.39(h·mg)/L,respectively.AndtheFofdomesticvsimportedwas99.97±26.51%.CONCLUSION:Therewasnosignificantdiference(P>0.05)betweendomesticandimportedticlopidinetabletsinthephamacokineticbehaviorandbioavailabilitiesinhumans.
出处
《中国药学杂志》
CAS
CSCD
北大核心
1996年第9期542-545,共4页
Chinese Pharmaceutical Journal
