Faculty of Pharmaceutical Sciences , Setsunan University , 45-1 Nagaotoge-Cho , Hirakata , Osaka 573-0101 , Japan.
Mol Pharm. 2020 Jan 6;17(1):212-218. doi: 10.1021/acs.molpharmaceut.9b00900. Epub 2019 Dec 6.
The present study sought to demonstrate the effect of dietary intake of medium-chain triacylglycerides (MCTs) on the intestinal absorption of a poorly permeable compound of intermediate molecular weight (FITC-dextran 4000 [FD-4]). As a model of MCTs, C-C fatty acid triacylglyceride (COCONAD ML) was mainly used, and the dose strength of each triglyceride was set with consideration of the dietary ingestion dose (12.5 mg/rat). When FD-4 with MCTs dispersed in fasted state simulated intestinal fluid containing surfactants was administered into the rat jejunum, the intestinal absorption of FD-4 was significantly higher than when administered with a similar solution with or without corn oil (long-chain triglycerides). The effects of pretreatment by MCT lipolysis, inhibition of endogenous lipases, and different dose timings of MCTs and FD-4 on the intestinal absorption of FD-4 indicated that medium-chain fatty acids, such as caprylic acid and capric acid, released from MCTs by lipolysis in the small intestine significantly enhanced the intestinal absorption of FD-4, but the effect was transient. In addition, a similar effect was observed when MCTs were dispersed in soymilk, although large interindividual variation was detected. These findings suggested that dietary intake of MCTs might affect the intestinal absorption of poorly permeable compounds.
本研究旨在探讨中链三酰甘油（MCT）的膳食摄入对一种中等分子量（FITC-葡聚糖 4000[FD-4]）的透壁化合物的肠道吸收的影响。作为 MCT 的模型，主要使用 C-C 脂肪酸三酰甘油（COCONAD ML），并考虑到膳食摄入剂量（12.5mg/大鼠），设定了每种甘油三酯的剂量强度。当 FD-4 与含有表面活性剂的禁食状态模拟肠液中的 MCT 分散体被给予大鼠空肠时，FD-4 的肠道吸收明显高于给予具有或不具有玉米油（长链甘油三酯）的类似溶液时。MCT 脂解预处理、内源性脂肪酶抑制以及 MCT 和 FD-4 的不同剂量时间对 FD-4 肠道吸收的影响表明，从小肠脂解释放的中链脂肪酸，如辛酸和癸酸，显著增强了 FD-4 的肠道吸收，但这种作用是短暂的。此外，当 MCT 分散在豆浆中时也观察到类似的效果，尽管检测到个体间存在较大差异。这些发现表明，MCT 的膳食摄入可能会影响透壁化合物的肠道吸收。
