Preparation of Altrenogest Solid Dispersions by Freeze-drying
The aim of this study was to prepare altrenogest(ALT)solid dispersion,improve the solubility and bioavailability of altrenogest,and provide a reference for its application in actual production.ALT solid dispersion was prepared by freeze-drying method with polyvinyl pyrrolidone k30(PVPK30)as the drug carrier and tert-butanol as the lyophilized solvent.X-ray diffraction(XRD),simultaneous thermal analysis(TG-DSC),Fourier transform infrared spectroscopy(FT-IR),scanning electron microscopy(SEM)and other methods were used to characterize the properties.The results showed that the optimal preparation process of tetraene estrone solid dispersion was as follows:drug loading ratio of 1∶8,tert-butanol concentration of 50％,and ultrasonic time of 60 min.The equilibrium solubility of the solid dispersion in pH 5.0 buffer was 5.91 times that of the active pharmaceutical ingredient(API),3.65 times that of the 1∶8 mixture,the cumulative dissolution rate of the solid dispersion in vitro for 6 h was 89.09％,and the cumulative dissolution rates of the ALT active ingredient and the physical mixture were 32.94％and 28.93％.In summary,the solid dispersion prepared by this method can effectively improve the solubility of altrenogest API.
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