口服给药的介绍.docxVIP

口服给药的介绍

口服给药的介绍

Fororaladministration,themostcommonroute,absorptionreferstothetransportofdrugsacrossmembranesoftheepithelialcellsintheGItract.AbsorptionafteroraladministrationisconfoundedbydifferencesinluminalpHalongtheGItract,surfaceareaperluminalvolume,bloodperfusion,thepresenceofbileandmucus,andthenatureofepithelialmembranes.Acidsareabsorbedfasterintheintestinethaninthestomach,apparentlycontradictingthehypothesisthatun-ionizeddrugmorereadilycrossesmembranes.However,theapparentcontradictionisexplainedbythelargersurfaceareaandgreaterpermeabilityofthemembranesinthesmallintestine.

口服是最常用的给药途径，其吸收涉及药物通过胃肠道上皮细胞膜的转运。由于给药时相关环境条件的不同，如胃肠道管腔内pH及单位腔道容积的表面积，组织血流灌注情况，胆汁和粘液的存在以及上皮细胞膜的性质等，口服给药的吸收也有差异。酸性药物在肠中的吸收较胃中快，这显然与非解离药物更易透过细胞膜这一假设相矛盾。然而，这种明显的矛盾却可以从小肠具有很大的表面积和小肠细胞膜具有较大的通透性中得到答案。

Theoralmucosahasathinepitheliumandarichvascularitythatfavorsabsorption,butcontactisusuallytoobrief,evenfordrugsinsolution,forappreciableabsorptiontooccur.Adrugplacedbetweenthegumsandcheek(buccaladministration)orunderthetongue(sublingualadministration)isretainedlongersothatabsorptionismorecomplete.

口腔粘膜上皮很薄，血管丰富，有利于药物吸收。但是，接触的时间太短暂，即使是溶液剂也来不及等到明显的吸收发生。把一种药物置于齿龈和面颊之间(颊部给药)或置于舌下(舌下给药)则可保留较长时间，使吸收更加完全。

Thestomachhasarelativelylargeepithelialsurface,butbecauseithasathickmucouslayerandthetimethatthedrugremainsthereisusuallyrelativelyshort,absorptionislimited.Absorptionofvirtuallyalldrugsisfasterfromthesmallintestinethanfromthestomach.Therefore,gastricemptyingistherate-limitingstep.Food,especiallyfattyfoods,slowsgastricemptying(andtherateofdrugabsorption),explainingwhysomedrugsshouldbetakenonanemptystomachwhenarapidonsetofactionisdesired.Foodmayenhancetheextentofabsorptionforpoorlysolubledrugs(eg,griseofulvin),reduceitfordrugsdegradedinthestom