Perspectives & Review
LI Hui, WU Xiaoqiang, FANG Liang
Based on the phase solubility determination results of clonidine in different cyclodextrin derivatives,
methyl-β-cyclodextrin was screened out because of the high inclusion efficiency. Then the inclusion complexes with the
inclusion ratio of methyl-β-cyclodextrin to clonidine of 1 ∶ 1 were prepared by rotary evaporation method. The drug
loading and encapsulation rates of the inclusion complexes were (13.45±0.22)% and (88.78±0.56)% , respectively. After
that, the orodispersible films based on the obtained inclusion complexes were prepared by cast coating method. The formulation
compositions were optimized by single factor tests, and the results were as follows: PVA 5-88(80% ), inclusion
complex(4% ), 1,2-propylene glycol(10% ), and low-substituted hydroxypropyl cellulose(10% ). The quality attributes
of the optimized films were determined. The results showed that the thickness, water content, surface pH value, tensile
strength and elongation at break of the self-made films were (91.72±1.74)μm, 4.71% , 6.75±0.09, (62.44±3.19)N/mm2,
and (107.15±7.02)% , respectively. Finally, the taste masking effect was evaluated by the electronic tongue techniques.
The results showed that the taste masking effect of the inclusion complex was better than that of aspartame. In conclusion,
cyclodextrin inclusion technology can significantly mask the bitterness of a drug.