倍他米松固体分散体的制备工艺优化与应用研究OA

Betamethasone(BMS)is a long-acting glucocorticoid drug,currently mainly used for treat-ing active rheumatism,rheumatoid arthritis,lupus erythematosus,etc.Due to its low solubility and poor oral efficacy,its bioavailability is relatively low,severely restricting its application as an oral formulation.This paper uses the solvent evaporation method to prepare BMS solid dispersions to increase its solubility,dissolution rate,and bioavailability.Hydrophilic polymers such as polyvinyl pyrrolidone,hydroxypropyl methylcellulose,and polyethylene glycol were selected as carrier materi-als to prepare the solid dispersions.The dissolution rate and cumulative dissolution rate were used as evaluation indicators,and single-factor screening,combined carrier screening,and orthogonal experi-ments were carried out for prescription screening and preparation process optimization.The BMS solid dispersions were characterized by scanning electron microscopy,powder X-ray diffraction,differen-tial scanning calorimetry,and Fourier transform infrared spectroscopy.The in vivo pharmacokinetic experiments of BMS raw material and solid dispersion in rats were conducted to evaluate the absorption,distribution,metabolism,and excretion process of BMS in rats.The results showed that the BMS solid dispersions could significantly increase the dissolution and absorption in both in vivo and in vitro conditions.Among them,BMS-PVP K13-18(1∶3),with a magnetic stirring time of 4 hours,a rotary evapora-tion temperature of 65 ℃,and a drying time of 24 hours,had the best effect,with a relative bioavail-ability of 554.9％.Therefore,the BMS solid dispersions prepared by the solvent evaporation method can significantly improve the solubility and dissolution rate,providing new ideas and methods for the new formulation of BMS.