154 中国临床药理学杂志 26 2 2010M2(9124) SScientificField中枢神经系统的药代动力学参数及其意义Pharmacokinetic parametersand itssignificances in centralnervoussysteml: 2008- 11- 09: 2009- 03- 30Te:( 1973- ),3,pV3,1VY50YT:,q,pV3=Te:l (0731) 5292121E-mai:l Li53HD medmail1 com1 cn刘艺平,李焕德(2vS=D04S, 410011)LIU Y-iping, LIHuan-de(Clinical Pharmacy Reseach Institute,The X iangya Second Hospital, CentraSouth University, Changsha 410011,China)K1:7pVE0w*dbdw*d0+: PSa=bq(K in, CLin, )abq(Kout, CLout)aT1/2eq, ina|s1(% ID/g)a7/s(Kp,Kp, uKp,uu),0V4s(Vu, brain )7=0(T1/2,brain)b, PSN0YV7p?a=bq(K in, CLin, )abq(K out, CLout )aT1/2eq, inaT1/2,brain0w*d=;% ID/gaKp,uuN0v7;Vu, brainN07=s+b1oM:7p;0ms|:R96911; R311 DSM: BcI|: 1001- 6821(2009)02- 0154- 03Abstract: It is popularly accept that blood- brain barrier affects drugtransportand distribution. Pharmacokinetic parameterswillhelp us pre-dict thepharmacologicalaction, drug- interactions and adversereaction.This article reviewed themajor pharmacokinetic parameters in centralnervous system, such asPS product(permeability surface areaproduct),K inorCLin ( influx clearance into thebrain),KoutorCLout(efflux clearancefrom thebrain), T1/2eq, in( intrinsicbrain equilibrium half- life),% ID/g(percentof injected dose per gram brain), K p, uu ( unbound brain/un-bound plasma concentration ratio at steady state), Vu, brain (apparent vo-lumeofdistribution in brain), T1/2, brain (half time in brain). These pa-rametersdescribe the aspects ofblood- brain permeability and the rateand extentofbrain drugdelivery.Keywords: centralnervous system; pharmacokineticparameter0rT0ifb01z34,Air0i=HWb7p(blood- brain barrier, BBB)BZ?Et(3a)v7,7=;76BZ9E0b0,7Fi,0iiasah+V 1b1 8VYi0130TAYVBBB, BBBYihqb3 T1/2eq, inls0a,aoa&1?yw?T;7Btvs0,54YVBBBb0CNSBbT1/2eq, in7=0r0i50%HWbT1/2eq, in= Vb ln2PS fu, brain(1), Vb7F3, fu, brain0sbBBBYia07F,%0rHWbPSv,5sv(Fql); Tl,0CNSrbBZ,0T 1bKp, uu, brain= PS+ CLuptakePS+CLefflux+ CLbulk +CLmetabolism(3), CLuptake|q, CLeffluxaCLbulkaCLmetabolismsY,aqhqbKp, uuVN0BBB,V0.MT(?3CNSMT)bMTvl?IK p, uu,BBB?3,5Kp, uu1,7WA( ISF)iM,i?3MTBb,rq,Kp, uu,MTBvbK p, uu = 015,5ISF0iKvV9F2;Kp, uu = 011,0i5V9F10b6 07Fs(Vu, brain)9Vu, brain0s,BLX,7F0ISF0i1,07FTM7MbT07L%,OF, Vu, brain012mL# g - 1,V3,KlbTVu, brain= 018mL# g- 1,7,5V0(s7F;TVu, brain 018mL g-1,V0FT,vs0%=bVu, brainQ07Fsf;H9Q07Ffb7 07=(T1/2, brain)156 中国临床药理学杂志 26 2 2010M2(9124) T1/2, brain7=0,bq0s%b7=0hy0h,58=%7=;7=0hA0h,7=|;Y&0,y78=Bs,7=0&0hYlbBHW0,8=0i,709Y0b,M7=0,?h7=0;M70;6BZ,TV=%ISF,A08,5V7=0b7=0w*07=|aashV,+7=0,w*d014,d05r,0MT#0Q?3bID: 1 de BenedictisFM, de BenedictisD, CanonicaGW1 New oralH1antihistamines in children: facts and unmeet needs J1 Allergy,2008; 63: 1395- 14041 2 EnnisSR, BetzAL1 Sucrose permeability of theblood- retinalandblood- brainbarriers1 Effectsofdiabetes, hypertonic