国产与进口地塞米松棕榈酸酯注射液的人体生物等效性研究  

Bioequivalence of Domestic and Foreign Dexamethasone Palmitate Injection in Healthy Volunteers

作　　者：朱艳荣[1] 周伦[1] 丁莉坤[1] 赵培西[1] 常瑛[1] 冯娟[1] 王婧雯[1] 文爱东[1] 

机构地区：[1]第四军医大学西京医院药剂科,西安市710032

出　　处：《中国药房》2011年第34期3204-3206,共3页China Pharmacy

摘　　要：目的:研究国产与进口地塞米松棕榈酸酯注射液在健康志愿者体内的药动学特征及其生物等效性。方法:采用标准二阶段交叉设计自身对照试验方法,将20例受试者随机分为2组,交叉单剂量静脉注射1mL(4mg)地塞米松棕榈酸酯注射液国产制剂(受试制剂)与进口制剂(参比制剂)后取血样,以液-质联用(LC-MS)法测定给药后0～24h间血浆中地塞米松棕榈酸酯及其代谢物地塞米松的浓度,并计算其药动学参数。结果:受试制剂与参比制剂血浆中地塞米松棕榈酸酯主要药动学参数分别为:tmax(0.12±0.04)、(0.14±0.06)h,cmax(528.59±80.50)、(577.13±96.11)ng·mL-1,t1/2(1.20±0.17)、(1.29±0.25)h,AUC0～8h(845.09±141.99)、(868.86±160.99)ng·h·mL-1;地塞米松的主要药动学参数:tmax(1.65±0.40)、(1.55±0.43)h,cmax(36.87±7.74)、(35.70±6.27)ng·mL-1,t1/2(4.97±1.34)、(5.22±1.28)h,AUC0～24h(247.40±59.78)、(228.62±59.59n)ng·h·mL-1。结论:国产与进口2种地塞米松棕榈酸酯注射液具有人体生物等效性。OBJECTIVE ： To study the pharmacokinetic characteristics and bioequivalence of domestic and foreign Dexamethasone palmitate injection in healthy volunteers. METHODS： In two-step cross design self-controlled trial, 20 healthy volunteers were randomly divided into 2 groups, and then received a single dose of domestic Dexamethasone palmitate injection 1 mL （4 mg） （test preparation） and foreign injection （reference preparation） with intravenous administration. The blood samples were collected after administration. The pharmacokinetic parameters were calculated after the plasma concentrations of dexamethasone palmitate and its metabolite 0-24 h after administration were determined by LC-MS. RESULTS： The main pharmacokinetic parameters of dexamethasone palmitate in test preparation vs. reference preparation were as follows： try（0.12 ± 0.04） h vs. （0.14 ± 0.06） h; Cmax（528.59 ± 80.50） ng.mL^-1 vs. （577.13 ± 96.11） ng.mL^-1; t1/2（1.20 ± 0.17） h vs. （1.29 ± 0.25） h; AUC0-sh（845.09 ± 141.99） ng-h.mL^-1 vs. （868.86 ± 160.99） ng· h·mL^-1. The main pharmacokinetic parameters of dexamethasone in test preparation vs. reference preparation were as follows： tmax （ 1.65 ± 0.40） h vs.（1.55 ± 0.43） h;Cmax（36.87 ±7.74） ng·mL^-1 vs. （35.70 ± 6.27） ng·mL^-1; t1/2（4.97 ± 1.34） h vs.（5.22 ± 1.28）h;AUC0-2h （247.40 ±59.78 ）ng. h·mL^-1 vs. （228.62 ±59.59）ng· h· mL^-1. CONCLUSION： Domestic and foreign Dexamethasone palmitate injections are bioequivalent in healthy volunteers.

关 键 词：地塞米松棕榈酸酯 地塞米松 液.质联用法 生物等效性 药动学 

分 类 号：R969.1[医药卫生—药理学] R977.1[医药卫生—药学]