非诺贝特纳米混悬液冻干粉的制备及评价

Preparation and Evaluation of Fenofibrate Nanosuspension

目的研究非诺贝特纳米混悬液的制备方法。方法采用泡腾法联合旋转蒸发制备非诺贝特纳米混悬液及其冻干制剂。通过单因素分析法考察非诺贝特纳米混悬液影响因素,优化非诺贝特纳米混悬液处方,并对其体外性质进行考察。结果马尔文粒度分布仪测得,制备的非诺贝特纳米混悬液平均粒径为(262.2±3.875)nm,多分散系数(PDI)为(0.069±0.004),Zeta电位为(-28.4±6.95)mV,以PEG 6000为冻干保护剂制备的纳米混悬剂冻干粉复溶后平均粒径为(567.4±9.686)nm,PDI为(0.128±0.098)。非诺贝特纳米混悬液的体外溶出度与原料药相比显著提高,5min内其体外溶出量为原料药的37倍,2h时其体外溶出量为原料药的3倍。结论通过泡腾法制备纳米混悬液冻干粉,显著改善了非诺贝特的溶出速率。

Objective To seek a new method to prepare fenofibrate nanosuspension.Methods Fenofibrate nanosuspension was prepared using the effervescent-vacuum rotary evaporation method for in situ nanoamorphization（ISN）and was lyophilized to obtain dry powder.Single factor analysis was used to investigate the influence of factors on the response and optimize the formulation of fenofibrate nanosuspension.Results The mean size of the prepared fenofibrate nanosuspension and the reconstituted freeze-dried powder detected by a Malvern laser particle size analyzer was（262.2±3.875）and（567.4±9.686）nm respectively,while the polydispersion index（PDI）and Zeta potential of the fenofibrate nanosuspension were（0.069±0.004）and（-28.4±6.95）mV respectively.Fenofibrate nanosuspension improved the dissolution rate of fenofibrate,and the dissolution quantity of fenofibrate nanosuspension in 5 min was 37 times that of the bulk drug.Conclusion Fenofibrate nanosuspension prepared with this effervescent-vacuum rotary evaporation method has the advantage of low-cost,easy-production,low-toxicity,fewer side effects and homogeneous distribution of mean size.This fenofibrate nanosuspension can obviously improve the physicochemical property of fenofibrate and its dissolution rate.