Two gabapentin-
chenodeoxycholic acid complexes were synthesized by coupling gabapentin to
chenodeoxycholic acid. Two monoanionic conjugates were hAsBT ligands, which had high affinity and high bearing capacity, and could be used as gabapentin use of prescription. Bile acid is the only oral effective small molecule liver targeting vector, which can be used with sodium-dependent cholic acid transporter (hAs-BT) on human small intestinal cells and sodium ion-taurocholic acid transport peptide (NTCP) specific binding, by liver cells specific absorption; as endogenous natural ligands, bile acids have good biocompatibility, suitable for use as a liver targeting drug carrier.
In recent years, bile acid as the carrier of liver-targeted drugs have a lot of research reports. Cytotoxic antitumor agents Fluorouracil can not selectively act on the lesion site and has serious side effects. A series of fluorouracil-cholic acid conjugates were prepared by bridging the fluorouracil derivative N-hydroxymethylfluorouracil with a series of alkanedioic acid compounds in the presence of a series of alkanedioic acid compounds, in which the conjugate of succinic acid as a bridge was rapidly Hydrolysis releases free fluorouracil. Further in vivo analysis showed that the half-life of the coupling drug was prolonged compared with that of the free drug. After oral administration of the drug, the concentration of fluorouracil increased significantly at each time point. Ara-cytarabine is an effective drug against acute myeloid leukemia, but its plasma half-life is short, the elimination rate is fast.