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设计制备了以泊洛沙姆407/188为主要基质,卡波姆、氯化钠为添加剂,月桂酸二乙醇酰胺为增溶剂的双氯芬酸钠缓释液体栓,以凝胶温度、凝胶强度、生物黏附力和体外释放度为考察指标进行体外评价;测定双氯芬酸钠缓释液体栓在犬体内的血药浓度,进行体内筛选.采用3p97软件计算液体栓相关药动学参数,进行体内释药特性研究.加入0.9%月桂酸二乙醇酰胺使双氯芬酸钠增溶2.3倍.缓释液体栓体外释放符合零级模式,R2>0.9,释药时限大于6h;体内药物释放出现血药平台,具有良好的体内外相关性;体内过程为一室模型,t1/2(Ke)=5.553 3h,t1/2(Ka)=0.357 4h,cmax=7 712ng.mL-1,AUC0→∞=72 029ng.h.mL-1,MRT=7.61h.所制备的双氯芬酸钠缓释液体栓具有稳定的缓控释特性.
The diclofenac sodium sustained-release liquid suppository with poloxamer 407/188 as matrix, carbomer, sodium chloride as additive and lauric acid diethanolamide as solubilizer was designed and prepared. The gel temperature, gel strength, Bioadhesive force and in vitro release were evaluated in vitro.Determined the plasma concentration of diclofenac sodium sustained-release liquid suppository in dogs and screened in vivo.The pharmacokinetic parameters of liquid suppository were calculated by 3p97 software, Study. Add 0.9% lauric acid diethanolamide to make diclofenac sodium 2.3 times. Sustained-release liquid in vitro release consistent with the zero-order mode, R2> 0.9, release time is greater than 6h; drug release blood drug platform appears to have good In vivo and in vitro, the in vivo process was a one-compartment model with t1 / 2 (Ke) = 5.553 3h, t1 / 2 (Ka) = 0.357 4h, cmax = 7 712ng.mL-1 and AUC0 → ∞ = 72 029ng.h. mL-1, MRT = 7.61h. The diclofenac sodium sustained-release liquid suppository has stable and controlled release characteristics.