HONG CHUNXUE, SHU YI, CAO YU, et al. Preparation and Properties of Thermosensitive Diclofenac Sodium Sustained-Release Liquid Suppository in vitro and in vivo Correlation. [J]. 2012, 58(4): 281-285.
HONG CHUNXUE, SHU YI, CAO YU, et al. Preparation and Properties of Thermosensitive Diclofenac Sodium Sustained-Release Liquid Suppository in vitro and in vivo Correlation. [J]. 2012, 58(4): 281-285. DOI: 10.14188/j.1671-8836.2012.04.001.
According to the thermosensitive gel properties the thermosensitive diclofenac sodium sustained-release liquid suppository with poloxamer 407/188 was designed and prepared.The physicochemical properties such as gelation temperature
gel strength
bioadhesive force and the drug release of diclofenac sodium liquid suppositories in vitro were studied.Lauric diethanolamide 0.9% increased the solubility of diclofenac sodium in liquid suppository by 130%.The drug absorption in vivo was performed in Beagle dogs.The 3p97 program was used to calculate the pharmacokinetic parameters of liquid suppository.Drug release pattern in vitro was best described by zero-order kinetics and in vivo profile was demonstrated to fit one compartment model.The pharmacokinetic parameters were: t1/2(Ke)=5.553 3 h
t1/2(Ka)=0.357 40 h
cmax=7 712 ng·mL-1
AUC0→∞=72 029 ng·h·mL-1
MRT=7.61 h.which showed this preparation has the characteristic of sustained releasing.
关键词
双氯芬酸钠缓释液体栓体内外相关性药代动力学
Keywords
diclofenac sodium sustained-release liquid suppositoryin vitro and in vivo correlationpharmacokinetics