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Effects of different preparation technologies on concentrations of puerarin and catalpol in plasma and brain of rats after oral administration

不同制剂技术对葛根素、梓醇口服吸收入脑的影响



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Efectsofdiferentpreparationtechnologiesonconcentrationsofpuerarinand
catalpolinplasmaandbrainofratsafteroraladministration
TANGDandan1,ZHANGJiao1,WANGJirui1,ZHANGJifen1,XUXiaoyu1,2
(1ColegeofPharmaceuticalSciences,SouthwestUniversity,Chongqing400716,China;
2ChongqingEngineeringResearchCenterforPharmacologicalEvaluation,Chongqing400716,China)
[Abstract] Tocomparetheefectsofdiferentpreparationtechnologiesontheconcentrationsofpuerarinandcatalpolinplasmaand
brainofratsafteroraladministration,inordertolayanexperimentalbasisfordevelopingneworalZigepreparationsThenanocrystal,
selfmicroemulsions(tween80andCremophorRH40asemulsifiers)andinclusioncomplexofHPβCDcontainingpuerarinandcatal
polwerepreparedTheconcentrationsofpuerarinandcatalpolinplasmaandbrainofratsafteroraladministrationweredeterminedby
HPLCMS/MSmethodThepharmacokineticparametersandbraintargetindexwerecomparedTheresultsshowedthatpreparation
technologieshaddiferentinfluencesontheconcentrationsofpuerarinandcatalpolinplasmaandbrainTheselfmicroemulsion
(tween80)couldsignificantlyincreasetheoralabsorptionofpuerarinthanothertechnologies(P<005),andinclusioncomplex
couldremarkablyincreasetheoralabsorptionofcatalpolthannanocrystal(P<001)Forpuerarin,thebraintargetingindexofinclu
sioncomplexwasthehighest(P<005);butforcatalpol,thebraintargetingindexofinclusioncomplexandselfmicroemulsionswere
bothhigherthannanocrystal(P<005)Theselfmicroemulsion(tween80)hadthehighestAUCbrainofpuerarinthanothergroups
(P<001);theinclusioncomplexhadthehighestAUCbrainforcatalpol,buttherewasnosignificantdiferencecomparedwithselfmi
croemulsionsInconclusion,theselfmicroemulsion(tween80)technologycouldincreasetheamountofpuerarinandcatalpolin
brain,andwasexpectedtobeusedinneworalZigepreparations
[Keywords] puerarin;catalpol;nanocrystal;selfmicroemulsion;inclusioncomplex;braintargetingindex
doi:10.4268/cjcmm20160529
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AUC0~∞/mg·L
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Cmax/mg·L-1 269±118 284±0395 201±0462 111±0377
Tmax/h 133±0577 0833±0204 0667±0129 0958±0102
t1/2/h 214±113 435±128 715±232 520±165
MRT0~t/h 341±117 421±0372 393±0724 373±104
MRT0~∞/h 411±127 638±151 990±306 791±224
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AUC0~t/mg·L-1·h-1 129±0418 220±0329 128±0237 149±0299
AUC0~∞/mg·L
-1·h-1 157±0632 288±0437 144±0269 161±0354
Cmax/mg·L-1 0220±00908 0463±00558 0347±00506 0209±0115
Tmax/h 113±0595 0850±0224 0850±0137 0750±0177
t1/2/h 430±163 571±103 314±0879 223±0497
MRT0~t/h 445±0458 440±0411 362±0867 395±0990
MRT0~∞/h 675±206 817±163 493±119 463±110
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,Š¹= 01g·kg-1


~}íîÈ{
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AUC0~t/mg·L-1·h-1 321±529 361±134 416±125 482±934
AUC0~∞/mg·L
-1·h-1 318±618 406±137 464±153 491±949
Cmax/mg·L-1 120±358 109±578 156±513 383±779
Tmax/h 0875±0144 100±0524 0850±0224 0500±0102
t1/2/h 170±0407 359±132 357±0737 157±0147
MRT0~t/h 251±00983 409±0549 374±0493 141±0144
MRT0~∞/h 292±0386 565±179 507±110 156±0203
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,Š¹= 01g·kg-1


~}íîÈ{
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AUC0~t/mg·L-1·h-1 0542±0158 0952±0151 0964±0229 152±0531
AUC0~∞/mg·L
-1·h-1 0605±0183 135±0416 127±0327 166±0514
Cmax/mg·L-1 0209±0115 0296±00642 0262±00559 0631±0194
Tmax/h 100±00102 0800±0112 0650±0224 0708±0274
t1/2/h 388±109 442±145 498±0949 315±0808
MRT0~t/h 399±0531 288±0294 381±0812 291±0696
MRT0~∞/h 541±114 605±205 694±107 402±0948
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rameters(珋x±s,n=8)
{× }”ì ~Ð
01g·kg-1


~}íîÈ
174±189 180±0312
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