洛索洛芬钠透皮贴剂的研制

Preparation of Loxoprofen Sodium Transdermal Patches

采用苯乙烯-异戊二烯-苯乙烯(SIS)的嵌段共聚物为基质,以液体石蜡作为载体分散剂、氢化石油树脂为增黏剂、N-甲基吡咯烷酮(NMP)为增溶剂、薄荷醇为促渗剂、枸橼酸为酸度调节剂及丁基化羟基甲苯(BHT)为抗氧剂制备了洛索洛芬钠透皮贴剂,并通过正交试验设计优化了处方工艺。所得优化处方为:SIS的质量分数为27%,液体石蜡为33%,氢化石油树脂为26%,枸橼酸为1.2%,薄荷醇为5.67%,NMP与BHT为0.85%。照优化处方制备的洛索洛芬钠贴剂质量稳定,透皮效果与参比制剂(Loxonin■)性能相当(24 h单位面积累积透过量可达72.69μg),且黏附性能良好。

This study used styrene-isoprene-styrene(SIS)block copolymer as the matrix,liquid paraffin as carrier dispersant,hydrogenated petroleum resin as the tackifier,N-methyl pyrrolidone(NMP)as solubilizer,menthol as the penetration enhancer,citric acid as the acidity regulator and butylated hydroxytoluene(BHT)as the antioxidant to prepare loxoprofen sodium(1)transdermal patches.The preparation process was optimized by orthogonal design.The optimized formulation compositons of the patch were as follows:the mass fraction of SIS was 27%,liquid paraffin was 33%,hydrogenated petroleum resin was 26%,citric acid was 1.2%,menthol was 5.67%,and both NMP and BHT were 0.85%.The quality of 1 patch prepared according to the optimal formulation was stable,and the adhesive property was good.Its transdermal effect was equivalent to the reference preparation(the permeability per unit area at 24 h reached 72.69μg).