甘草酸磷脂复合物自乳化胶囊与肠溶胶囊的药动学 - 中国现代应用药学.pdf

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 中图分类号：R943 文献标志码：A 文章编号：1007-7693(2014)03-0310-03 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 wa