Résumé
OBJECTIVE： To prepare Magnolol nano-crystal suspension （MAG-NS）， and to conduct quality evaluation. METHODS： The preparation technology of MAG-NS was optimized by central composite design-response surface methodology with OD value of particle size and polydispersity coefficient as evaluation indexes， using volume ratio of organic phase to water phase， ratio of excipient to drug， concentration of magnolol as factors and conduct validation tests. The quality of MAG-NS prepared optimal technology was evaluated. RESULTS： Optimized technology included that the volume ratio of organic phase to water phase was 1 ∶ 5， mass ratio of excipient to drug was 4 ∶ 1， concentration of magnolol was 2 mg/mL. In 3 times of validation tests， average OD value was 0.940 0 （RSD＝0.08％）， relative error of which to predicted value 0.977 7 was 3.86％. magnolol nano-crystals of MAG-NS prepared by the optimal technology were spherical， uniform in size， smooth in surface， with particle size of （34.88±0.33） nm， polydispersity coefficient of 0.032±0.001 and drug loading amount of （17.83±0.92）％. CONCLUSIONS： Established preparation method is simple and feasible. Prepared MAG-NS is in line with quality requirements. It can provide reference for further development and utilization of MAG-NS.
Résumé
OBJECTIVE: To prepare coenzyme Q10-γ-cyclodextrin nano-crystal suspension using high pressure homogeneous combining freeze-drying method, optimize the preparation technology, and evaluate the quality of the product. METHODS: Encapsulation efficiency and mean particle size of inclusion complex were used as indicators, and response surface method was performed for optimizing preparation process and formulations. The stability and transdermal performance in vitro of the inclusion complexes were investigated. RESULTS: The optimal technical parameters were as follows; the mass ratio of γ-cyclodextrin and drug, 7.76:1; ultrasonic temperature, 40℃; ultrasonic time, 28.33 min; homogeneous pressure, 40 MPa. Under such conditons, an average encapsulation efficiency of 48.39% and average particle size of 324 nm were obtained for the nano-crystal suspension. The transdermal experiment in vitro showed that the infiltration rate of inclusion was 5.68 μg·cm-2·h-1. CONCLUSION: The preparation method is simple and feasible. The product quality is stable. Moreover, it is easy to manufacture.