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Huperzine A (Hup-A) is a poorly water-soluble drug with low oral bioavailability.A self-microemulsifying drug delivery system (SMEDDS) was used to enhance the oral bioavailability and lymphatic uptake and transport of Hup-A.A single-pass intestinal perfusion (SPIP) technique and a chylomicron flow-blocking approach were used to study its intestinal absorption,mesenteric lymph node distribution and intestinal lymphatic uptake.The value of the area under the plasma concentration-time curve (AUC) of Hup-A SMEDDS was significantly higher than that of a Hup-A suspension (P<0.01).The absorption rate constant (Ka) and the apparent permeability coefficient (Papp) for Hup-A in different parts of the intestine suggested a passive transport mechanism,and the values of Ka and Papp of Hup-A SMEDDS in the ileum were much higher than those in other intestinal segments.The determination of Hup-A concentration in mesenteric lymph nodes can be used to explain the intestinal lymphatic absorption of Hup-A SMEDDS.For Hup-A SMEDDS,the values of AUC and maximum plasma concentration (Cmax) of the blocking model were significantly lower than those of the control model (P<0.05).The proportion of lymphatic transport of Hup-A SMEDDS and Hup-A suspension were about 40% and 5%,respectively,suggesting that SMEDDS can significantly improve the intestinal lymphatic uptake and transport of Hup-A.