Formulation development and evaluation of gastroretentive floating beads with Brucea javanica oil using ionotropic gelation technology  

作　　者：ZHANG Yue ZHANG Xi-Tong ZHANG Qi WANG Bing ZHANG Tong 

机构地区：[1]Experiment Center for Teaching and Learning, Shanghai University of Traditional Chinese Medicine [2]School of Pharmacy, Shanghai University of Traditional Chinese Medicine

出　　处：《Chinese Journal of Natural Medicines》2018年第4期293-301,共9页中国天然药物（英文版）

基　　金：supported by the National Natural Science Foundation of China(No.81303233);Foundation of Shanghai Science and Technology Committee(No.13401900300);Shanghai Municipal Commission of Health and Family Planning(No.20124074)

摘　　要：In the present study, a gastric retention floating system for Brucea javanica oil, composed of alginate and carrageenan, was prepared using ionotropic gelation. Parameters for floatability, drug load, encapsulation efficiency, bead morphology, in vitro release, and in vivo gastric retention were evaluated. The optimized formulation via Box–Behnken design consisted of 1.7% alginate(W/V), 1.02% carrageenan(W/V), 1.4% CaCO_3(W/V), and a gelling bath of pH 0.8. The alginate–carrageenan–Brucea javanica oil beads had a porous structure and exhibited up to 24 h of in vitro floatability with a load capacity of 45%–55% and an encapsulation efficiency of 70%–80%. A 6-h sustained release was observed in vitro. The beads had a prolonged gastric retention(> 60% at 6 h) in fasted rats, compared to non-floating beads(15% at 6 h), as measured by gamma scintigraphy with single-photon emission tomography/computed tomography(SPET/CT). In conclusion, the alginate–carrageenan–Brucea javanica oil system showed enhanced oil encapsulation efficiency, excellent floating and gastric retention abilities, and a favorable release behavior.In the present study, a gastric retention floating system for Brucea javanica oil, composed of alginate and carrageenan, was prepared using ionotropic gelation. Parameters for floatability, drug load, encapsulation efficiency, bead morphology, in vitro release, and in vivo gastric retention were evaluated. The optimized formulation via Box–Behnken design consisted of 1.7% alginate（W/V）, 1.02% carrageenan（W/V）, 1.4% CaCO_3（W/V）, and a gelling bath of pH 0.8. The alginate–carrageenan–Brucea javanica oil beads had a porous structure and exhibited up to 24 h of in vitro floatability with a load capacity of 45%–55% and an encapsulation efficiency of 70%–80%. A 6-h sustained release was observed in vitro. The beads had a prolonged gastric retention（ 60% at 6 h） in fasted rats, compared to non-floating beads（15% at 6 h）, as measured by gamma scintigraphy with single-photon emission tomography/computed tomography（SPET/CT）. In conclusion, the alginate–carrageenan–Brucea javanica oil system showed enhanced oil encapsulation efficiency, excellent floating and gastric retention abilities, and a favorable release behavior.

关 键 词：Brucea javanica oil SIMAROUBACEAE Alginate–carrageenan beads Gastric retention Box–Behnken design SPET/CT 

分 类 号：R944[医药卫生—药剂学]