摘要
目的以市售甘草酸二铵肠溶胶囊为参比制剂,考察自制甘草酸磷脂复合物自乳化胶囊在Beagle犬体内的相对生物利用度。方法 Beagle犬6只,自身交叉对照、单剂量灌胃甘草酸磷脂复合物自乳化胶囊或市售肠溶胶囊。采用HPLC测定血浆中的甘草酸浓度,DAS 2.0程序拟合药代动力学数据。结果参比制剂和受试制剂主要的药动学参数:Tmax分别为(6.00±0.000)h,(2.917±0.585)h;Cmax分别为(12.756±1.075)mg·L-1,(17.751±1.604)mg·L-1;AUC0-t分别为(150.894±22.850)mg·h·L-1,(211.196±40.880)mg·h·L-1;AUC0-∞分别为(159.39±21.862)mg·h·L-1,(221.287±42.164)mg·h·L-1,甘草酸磷脂复合物自乳化制剂相对生物利用度(F%)为139.76%。结论 Beagle犬体内甘草酸的药动学规律均符合一级吸收二室模型,与市售胶囊剂相比,自乳化制剂的Cmax、AUC0-t,AUC0-∞均高于肠溶胶囊,表明自乳化制剂能显著提高药物的生物利用度,初步达到了设计要求。
OBJECTIVE To compare the pharmacokinetics between glycyrrhizic acid phospholipid complex self emulsifying preparation（T） and glycyrrhizic acid diammonium enteric coated capsule（R） in dogs. METHODS Six Beagle dogs were given orally T and R, with a single dose of 50 mg·kg^-1 glycyrrhizic acid in self crossover study. The plasma concentration of glycyrrhizic acid was assayed by HPLC and the pharmacokinetic parameters were calculated with DAS2.0 program. RESULTS Tmax for R and T were （6.00±0.000）h and （2.917±0.585）h; Cmax for R and T were （12.756±1.075）mg·L^-1 and （17.751±1.604）mg·L^-1, respectively; AUC0- ∞ were （150.894±22.850）mg·h·L^-1 and （211.196J±40.880）mg·h·L^-1; AUC0-∞ were （159.39±21.862）mg·h·L^-1 and （221.287±42.164）mg·h·L^-1; the relative bioavailability ofT was 139.76%. CONCLUSIONS The pharmacokinetics of glycyrrhizic acid in dogs accorded with the two compartment models and with the first-order absorption after T or R administration orally, Cmax, AUC0-t and AUC0-∞ of T were all higher than those of R, and T had a higher bioavailabilitv, which reached the object of this task.
出处
《中国现代应用药学》
CAS
CSCD
2014年第3期310-312,共3页
Chinese Journal of Modern Applied Pharmacy
基金
浙江省中医药管理局重点项目(2009ZA014)
关键词
甘草酸磷脂复合物
自乳化制剂
高效液相色谱
药动学
glycyrrhizic acid phospholipid complex
self emulsifying preparation
HPLC
pharmacokinetics
