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引用本文:赵亚,李松龙,茹仁萍,梅笑冰,王琦.甘草酸磷脂复合物自乳化胶囊与肠溶胶囊的药动学比较[J].中国现代应用药学,2014,31(3):310-312.
ZHAO Ya,LI Songlong,RU Renping,MEI Xiaobing,WANG Qi.Comparison of the Pharmacokinetics Between Glycyrrhizic Acid Phospholipid Complex Self Emulsifying Capsule and Enteric Coated Capsule[J].Chin J Mod Appl Pharm(中国现代应用药学),2014,31(3):310-312.
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甘草酸磷脂复合物自乳化胶囊与肠溶胶囊的药动学比较
赵亚, 李松龙, 茹仁萍, 梅笑冰, 王琦
杭州市西溪医院药剂科,杭州 310023
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。
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
DOI:
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基金项目:浙江省中医药管理局重点项目(2009ZA014)
Comparison of the Pharmacokinetics Between Glycyrrhizic Acid Phospholipid Complex Self Emulsifying Capsule and Enteric Coated Capsule
ZHAO Ya, LI Songlong, RU Renping, MEI Xiaobing, WANG Qi
Department of Pharmacy, Hangzhou Xixi Hospital, Hangzhou 310023, China
Abstract:
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-t were (150.894±22.850)mg·h·L-1 and (211.196±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 of T 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 bioavailability, which reached the object of this task.
Key words:  glycyrrhizic acid phospholipid complex  self emulsifying preparation  HPLC  pharmacokinetics
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