YAN Min-jia, LI Xiao-fang, WU Chao-qun, et al. Preparation and Evaluation of Andrographolide Supersaturatable Self-microemulsifying Drug Delivery System[J]. Chinese journal of experimental traditional medical formulae, 2018, 24(10): 8-14.
YAN Min-jia, LI Xiao-fang, WU Chao-qun, et al. Preparation and Evaluation of Andrographolide Supersaturatable Self-microemulsifying Drug Delivery System[J]. Chinese journal of experimental traditional medical formulae, 2018, 24(10): 8-14. DOI: 10.13422/j.cnki.syfjx.20181003.
Objective: To prepare supersaturatable self-microemulsifying drug delivery system of andrographolide for increasing its solubility and bioavailability. Method: Based on results of solubility test and pseudo-ternary phase diagrams
the formulation of self-microemulsifying drug delivery system was optimized by simplex lattice method with degree of average particle size
polydispersity index and emulsifying time as indexes;and the best supersaturated inhibitor was screened out by means of crystallization
particle size
polydispersity index
self-emulsifying time and dissolution rate of andrographolide. Result: The optimum formulation of andrographolide supersaturated self-microemulsion was ethyl oleate
polysorbate-80
polyethylene glycol 400 and hydroxypropyl methylcellulose K4M in the ration of 20:35:45:1.After emulsification
average particle size
polydispersity index
Zeta potential
emulsifying time and the cumulative dissolution rate at 1 hour of andrographolide supersaturatable drug delivery system were (29.26±0.56) nm
0.19±0.02
(-10.23±2.34) mV
(62.39±2.03) s and 91%
respectively. Conclusion: The hydroxypropyl methylcellulose K4M can obviously inhibit the crystallization time and increase the stability of the self-microemulsion;compared with the ordinary self-microemulsion
supersaturated self-microemulsion can improve the dissolution of andrographolide obviously
and the bioavailability of andrographolide is improved.