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首页> 外文期刊>Journal of pharmaceutical sciences. >Modulation of ganciclovir intestinal absorption in presence of absorption enhancers.
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Modulation of ganciclovir intestinal absorption in presence of absorption enhancers.

机译：在吸收促进剂存在下更昔洛韦肠道吸收的调节。

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The purpose of this investigation was to study the influences of absorption enhancers in increasing oral bioavailability of Ganciclovir (GAN) by assessing the transepithelial permeation across cell monolayers in vitro and bioavailability in rats in vivo. The permeation of GAN across Caco-2 and MDCK cell monolayers in the absence/presence of dimethyl-beta-cyclodextrin (DMbetaCD), chitosan hydrochloride (CH), sodium lauryl sulphate (SLS), and their combinations was studied for a 2-h period. GAN was administered to rats in absence/presence of absorption enhancers and drug contents in plasma were estimated. We found that the apparent permeability coefficient (Papp) of GAN in absence of absorption enhancers (control) were 0.261 +/- 0.072 x 10(-6) and 0.486 +/- 0.063 x 10(-6) cm/s in Caco-2 and MDCK cell monolayers, respectively, whereas in the presence of DMbetaCD, CH, SLS, and their combinations, Papp of GAN increased by 5- to 25-fold and 7- to 33-fold as compared to control in Caco-2 and MDCK cell monolayers, respectively. However, in rats, the maximum enhancement in bioavailability of GAN during coadministration of these absorption enhancers was only fivefold compared to GAN control. To conclude, the absorption enhancers-DMbetaCD, CH, SLS, and their combinations demonstrated significant improvement in transepithelial permeation and bioavailability of GAN.
机译：这项研究的目的是通过评估体外跨细胞单层的上皮渗透和体内大鼠的生物利用度，研究吸收促进剂对更昔洛韦（GAN）口服生物利用度的影响。在不存在/存在二甲基-β-环糊精（DMbetaCD），壳聚糖盐酸盐（CH），月桂基硫酸钠（SLS）及其组合的情况下，研究了GAN跨Caco-2和MDCK细胞单层的渗透情况，研究了2小时期。在不存在/不存在吸收促进剂的情况下，将GAN给药于大鼠，并估算血浆中的药物含量。我们发现，在无吸收促进剂（对照）的情况下，GAN的表观渗透系数（Papp）在Caco-中为0.261 +/- 0.072 x 10（-6）和0.486 +/- 0.063 x 10（-6）cm / s。分别是2和MDCK细胞单层，而在DMbetaCD，CH，SLS及其组合的存在下，与Caco-2和Caco-2中的对照相比，GAN的Papp增加了5至25倍和7至33倍。 MDCK细胞分别为单层。然而，在大鼠中，与GAN对照相比，这些吸收促进剂共同给药期间GAN的最大生物利用度提高只有五倍。总之，吸收促进剂-DMbetaCD，CH，SLS及其组合在GAN的跨上皮渗透和生物利用度方面显示出显着改善。

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