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首页> 外文期刊>European journal of pharmaceutical sciences >Intestinal absorption and intestinal lymphatic transport of sirolimus from self-microemulsifying drug delivery systems assessed using the single-pass intestinal perfusion (SPIP) technique and a chylomicron flow blocking approach: linear correlation with oral bioavailabilities in rats.
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Intestinal absorption and intestinal lymphatic transport of sirolimus from self-microemulsifying drug delivery systems assessed using the single-pass intestinal perfusion (SPIP) technique and a chylomicron flow blocking approach: linear correlation with oral bioavailabilities in rats.

机译：西罗莫司从自微乳化药物递送系统的肠道吸收和肠道淋巴运输，使用单次肠道灌注（SPIP）技术和乳糜微粒流阻滞方法进行评估：与大鼠口服生物利用度呈线性相关。

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This work aims to investigate the impact of different amount of oil or surfactant included in self-microemulsifying drug delivery systems on the intestinal lymphatic transport of sirolimus using the single-pass intestinal perfusion (SPIP) technique and a chylomicron flow blocking approach. Male Sprague-Dawley rats were pretreated intraperitoneally with 3.0mg/kg cycloheximide or saline. One hour later, single-pass intestinal perfusion experiments in jejunum and ileum and in vivo bioavailability studies were carried out to calculate the effective permeability coefficient and pharmacokinetic parameters, respectively. Drug absorption from oil-free formulation was mostly via the portal blood. In contrast, for the SMEDDS formulations containing >/=25% MCT, the lymphatic transport of sirolimus was a major contributor to oral bioavailability. The formulation including more content of oil presented higher lymphatic transport of drug and further exhibited the increased oral bioavailability. Besides, distal ileum presented much more lymphatic transport of drug compared to proximal jejunum. Furthermore, even though the smaller droplet size of resultant microemulsions and more surfactant content also can positively influence the intestinal absorption of drug, their influences on the drug intestinal lymphatic transport were relatively weaker than that of more oil content. In addition, there was a high linear correlation between the AUC values and the mean of P(eff) values in jejunum and ileum.
机译：这项工作旨在研究使用单程肠灌注（SPIP）技术和乳糜微粒阻滞方法，在自微乳化药物递送系统中包含的不同量的油或表面活性剂对西罗莫司的肠淋巴运输的影响。将雄性Sprague-Dawley大鼠腹膜内用3.0mg / kg环己酰亚胺或生理盐水预处理。一小时后，进行了空肠和回肠单次肠道灌注实验以及体内生物利用度研究，分别计算了有效渗透系数和药代动力学参数。无油配方的药物吸收主要是通过门静脉血。相反，对于含有≥25％MCT的SMEDDS制剂，西罗莫司的淋巴转运是口服生物利用度的主要贡献者。包含更高含量油的制剂表现出更高的药物淋巴转运性，并且进一步表现出更高的口服生物利用度。此外，与空肠近端相比，回肠远端呈现出更多的淋巴转运药物。此外，即使所得微乳液的液滴尺寸较小和表面活性剂含量较高也可以积极影响药物的肠道吸收，但它们对药物肠道淋巴运输的影响却比含油量更高的影响相对较弱。另外，空肠和回肠中的AUC值与P（eff）值的平均值之间存在高度线性相关。

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