摘要
目的 研究健康受试者单剂量和多剂量口服硫酸沙丁胺醇缓释胶囊的人体生物利用度和药代动力学。方法 以英国Glaxo公司生产的硫酸沙丁胺醇控释片为参比制剂 ,HPLC UV法测定 2 0名健康男性志愿受试者按交叉试验单剂量和多剂量口服硫酸沙丁胺醇缓释胶囊和控释片后血浆中沙丁胺醇的浓度。结果 单剂量服用硫酸沙丁胺醇缓释胶囊和控释片后 ,二者的Cmax,Tmax和T1/2 均无显著性差异 ,缓释胶囊的相对生物利用度为 99 6 8%±10 2 7%。多剂量给药达稳态时 ,缓释胶囊和控释片的Cssmax,Cssmin,波动度 (DF) ,均无显著性差异。结论 两种制剂具有生物等效性 。
AIM To study the pharmacokinetics and relative bioavailability of a sustained release capsule (SRC) of albuterol in 20 healthy male volunteers in a randomized 2 way cross over study by taking a controlled release tablet (CRT) of albuterol as reference preparation. METHODS A simple and sensitive HPLC method with UV detection was developed to determine the plasma albuterol concentration and the pharmacokinetic parameters of the two formulations. Two one sided tests and analysis of variance were performed to evaluate the bioequivalence of the two formulations. RESULTS After a single oral dose in healthy volunteers, the C max , T max and AUC were of no significant difference between SRC and CRT ( P >0 05). The relative bioavailability of SRC was found to be 98 98%. Following multiple dosing, the mean steady state C ss max values were (12 94±3 35) ng·mL -1 and (12 60±3 36) ng·mL -1 , mean C ss min values were (5 84±1 34) ng·mL -1 and (6 16±1 33) ng·mL -1 , degrees of fluctuation (DF) were 0 82 and 0 76 for SRC and CRT, respectively. No significant difference was found between them. CONCLUSION The two preparations were bioequivalent and the new sustained release capsule exhibited good sustained release property as the reference.
出处
《药学学报》
CAS
CSCD
北大核心
2000年第9期683-687,共5页
Acta Pharmaceutica Sinica
关键词
硫酸沙丁胺醇
药物动力学
生物利用度
缓释胶囊
albuterol sulfate
pharmacokinetics
bioavailability
high performance liquid chromatography
