双氯芬酸钠透皮控释制剂的研究(1)
【摘 要】 目的：探讨不同双氯芬酸钠透皮控释制剂对药物的影响。方法：采用正交设计实验，考察双氯芬酸钠制备过程中乙醇含量、磷脂浓度、柔性辅料的用量及超声处理时间等对包封率的影响；采用正交设计实验，考察丙烯酸树脂为主要成分、琥珀酸为交联剂、柠檬酸三乙酯为增塑剂制对体外透皮率和体外释药性的影响；采用健康大鼠进行药动学实验，研究双氯芬酸钠醇质体在大鼠体内的药动学特征和生物利用度。结果：乙醇含量(A)、磷脂浓度(B)、柔性辅料(D)的用量及超声处理时间(C)四个影响因素对透皮控释贴剂包封率的综合影响效果为B>A>C>D，根据评分，得最佳处方为：A3B2C2D1；得出的最优处方组成为：双氯芬酸钠醇脂质体溶液含量10%、丙烯酸树脂Ⅳ号0.4g，柠檬酸三乙酯0.25g，琥珀酸0.052g，氮酮含量5%；计算得出双氯芬酸钠透皮控释贴剂的相对生物利用度为167.20%，说明采用本研究优化后工艺制备的双氯芬酸钠透皮控释贴剂具有较高的生物利用度。结论：双氯芬酸钠应用醇质体制成透皮控释制剂，透皮吸收的效果好，控释作用显著，相对生物利用度高。
【关键词】 双氯芬酸钠 醇质体 经皮给药系统 相对生物利用度 包封率
Study of diclofenac sodium transdermal drug delivery
Su Ruizhen， Xu Yuehong
School of pharmaceutical sciences， Sun Yat-Sen University， Guangzhou 510006， China
【Abstract】 Objective： To investigate the effects of different diclofenac transdermal drug delivery system for the drug. Methods： The orthogonal design of experiments， study the influence of diclofenac sodium encapsulation efficiency of the manufacturing process of ethanol content， phospholipid concentration， the amount of flexible materials and ultrasonic treatment time； the main component of the orthogonal design experiments， investigate acrylic resin， amber acid as crosslinking agent， triethyl citrate plasticizer made as affecting in vitro and in vitro release rate of penetration； and the adoption of healthy rats， pharmacokinetic experiments， research ethosomes drug diclofenac in rats pharmacokinetic characteristics and bioavailability. Results： The ethanol content (A)， phospholipid concentration (B)， flexible materials (D) in an amount and sonication time (C) four factors on Transdermal patch encapsulation efficiency of the combined effect of the effect of B> A > C> D， according to the score， get the best prescription is： A3B2C2D1； optimal formulation obtained composition： solution of diclofenac sodium liposomes alcohol content of 10 percent， an acrylic resin Ⅳ No. 0.4g， 0.25g triethylcitrate ， succinic acid 0.052g， nitrogen ketone content of 5%； relative bioavailability calculated Transdermal diclofenac patch was 167.20%， indicating that after this study to optimize the use of controlled-release transdermal diclofenac patch preparation process has higher bioavailability. Conclusion： The application ethosomes diclofenac sodium transdermal drug delivery system into a transdermal absorption effect， controlled release significant effect on the relative bioavailability.
【Key words】 diclofenac sodium； ethosomes； transdermal delivery system； relative bioavailability； encapsulation efficiency, 百拇医药(苏瑞真 徐月红)
【关键词】 双氯芬酸钠 醇质体 经皮给药系统 相对生物利用度 包封率
Study of diclofenac sodium transdermal drug delivery
Su Ruizhen， Xu Yuehong
School of pharmaceutical sciences， Sun Yat-Sen University， Guangzhou 510006， China
【Abstract】 Objective： To investigate the effects of different diclofenac transdermal drug delivery system for the drug. Methods： The orthogonal design of experiments， study the influence of diclofenac sodium encapsulation efficiency of the manufacturing process of ethanol content， phospholipid concentration， the amount of flexible materials and ultrasonic treatment time； the main component of the orthogonal design experiments， investigate acrylic resin， amber acid as crosslinking agent， triethyl citrate plasticizer made as affecting in vitro and in vitro release rate of penetration； and the adoption of healthy rats， pharmacokinetic experiments， research ethosomes drug diclofenac in rats pharmacokinetic characteristics and bioavailability. Results： The ethanol content (A)， phospholipid concentration (B)， flexible materials (D) in an amount and sonication time (C) four factors on Transdermal patch encapsulation efficiency of the combined effect of the effect of B> A > C> D， according to the score， get the best prescription is： A3B2C2D1； optimal formulation obtained composition： solution of diclofenac sodium liposomes alcohol content of 10 percent， an acrylic resin Ⅳ No. 0.4g， 0.25g triethylcitrate ， succinic acid 0.052g， nitrogen ketone content of 5%； relative bioavailability calculated Transdermal diclofenac patch was 167.20%， indicating that after this study to optimize the use of controlled-release transdermal diclofenac patch preparation process has higher bioavailability. Conclusion： The application ethosomes diclofenac sodium transdermal drug delivery system into a transdermal absorption effect， controlled release significant effect on the relative bioavailability.
【Key words】 diclofenac sodium； ethosomes； transdermal delivery system； relative bioavailability； encapsulation efficiency, 百拇医药(苏瑞真 徐月红)