Phosphorylated tocopherols are a new class of lipid excipients that have demonstrated potential in pharmaceutical applications. Their ability to solubilise poorly water soluble drugs indicates their potential utility in improving bioavailability of drugs where solubility limits their bioavailability. In this study a commercial mixture of phosphorylated tocopherols, TPM was combined with medium chain triglyceride (MCT) as a formulation for CoQ₁₀, and in vitro and in vivo performance compared to the effect of addition of alternative tocopherol-based excipients. In in vitro digestion experiments, CoQ₁₀ was poorly solubilised in the digesting MCT as anticipated. Addition of TPM facilitated the enhanced solubilisation of CoQ₁₀ as did vitamin E TPGS (TPGS). Other tocopherol derivatives (tocopherol acetate, tocopherol) were less effective at solubilising the active during the digestion process. The trends in in vitro solubilisation were conserved in the in vivo bioavailability of CoQ₁₀ after oral administration to rats, with TPM and TPGS formulations providing approximately double the exposure of MCT alone, while the addition of the other tocopherol derivatives reduced the overall exposure. Collectively, the results indicate potential of TPM as a new solubilising excipient for use in oral drug delivery for poorly water soluble drugs.

磷酸化的生育酚是一类新的脂质赋形剂，在药物应用中已显示出潜力。它们溶解水溶性差的药物的能力表明，在溶解度限制其生物利用度的情况下，它们在改善药物生物利用度方面的潜在效用。在这项研究中，将磷酸化生育酚的商业混合物TPM与中链甘油三酸酯（MCT）结合制成CoQ ₁₀制剂，与添加基于生育酚的替代性赋形剂的效果相比，其在体外和体内的性能更佳。在体外消化实验中，辅酶Q ₁₀如预期的那样，其在消化MCT中的溶解度很差。与维生素E TPGS（TPGS）一样，TPM的添加促进了辅酶Q _10的增溶。在消化过程中，其他生育酚衍生物（生育酚乙酸酯，生育酚）在溶解活性物质方面效果较差。口服给药于大鼠后，辅酶Q _10的体内生物利用度保持了体外增溶的趋势，TPM和TPGS配方仅提供MCT的暴露量约为一倍，而其他生育酚衍生物的添加降低了总暴露量。总的来说，结果表明TPM作为一种新的增溶性赋形剂，可用于水溶性差的药物的口服药物递送。