Self-microemulsifying drug delivery system for improving the bioavailability of huperzine A by lymphatic uptake

作     者：Fang Li Rongfeng Hu Bin Wang Yun Gui Gang Cheng Song Gao Lei Ye Jihui Tang 

作者机构：Anhui University of Chinese MedicineHefei 230038China National Chinese Medicinal Materials Products Quality Supervision and Inspection Center(Anhui)Bozhou 236800China Key Laboratory of Xin'an Medicine Ministry of EducationHefei 230038China Anhui“115”Xin'an Traditional Chinese Medical Research&Development Innovation TeamHefei 230038China Anhui Province Key Laboratory of R&D of Chinese MedicineHefei 230038China School of PharmacyAnhui Medical UniversityHefei 230022China 

出 版 物：《Acta Pharmaceutica Sinica B》 (药学学报（英文版）)

年 卷 期：2017年第7卷第3期

页      面：353-360页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 1006[医学-中西医结合] 1004[医学-公共卫生与预防医学(可授医学、理学学位)] 1001[医学-基础医学(可授医学、理学学位)] 10[医学] 100602[医学-中西医结合临床] 

基　　金：supported by the National Natural Science Foundation of China(Grant Nos.81274100 81573615) Natural Science Foundation of Anhui Province of China(Grant No.1408085QH189) Key Project for the Excellent Higher Education of Anhui Province of China(Grant No.2013SQRL019ZD) Research Project for the Science and Technology of Bozhou city of China(Grant No.BK2015005) 

主　　题：Huperzine A Self-microemulsion Drug delivery systems SMEDDS Bioavailability Single-pass intestinal perfusion Lymphatic transport 

摘      要：Huperzine A(Hup-A) is a poorly water-soluble drug with low oral bioavailability. A selfmicroemulsifying 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(K_a) and the apparent permeability coefficient(P_(app)) for Hup-A in different parts of the intestine suggested a passive transport mechanism, and the values of K_a and P_(app) 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(C_(max)) of the blocking model were significantly lower than those of the control model(P0.05). 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.