摘要
目的:研究单剂量po赖氨匹林(LA)胶囊和来比林散(LA散)后,水杨酸在血浆中的药物动力学与相对生物利用度.方法:采用反相高效液相色谱法测定10名志愿受试者单剂量po1000mg LA胶囊和4000mgLA散后,血浆中水杨酸浓度变化情况;计算药物动力学参数与相对生物利用度,并以配对t检验与双单侧t检验进行统计分析.结果:LA胶囊和LA散以水杨酸计的AUC分别是(251.81±33.58)和(255.12±44.76)mg·h/L;达峰时间分别是(3.52±0.50)和(0.97±0.4)h,峰浓度分别是(39.69±3.58)和(48.14±3.99)mg/L.配对t检验与双单侧t检验结果均表明:po1000mg LA胶囊后,以水杨酸计药-时曲线下面积与po 4000mg LA散相比无显著性差异(P>0.05);峰浓度、达峰时间以水杨酸计有显著性差异(P<0.05).结论:以AUC_(0-∝)为指标,LA囊和LA散为生物等效制剂.以LA散为标准参比制剂,LA胶囊以水杨酸计的相对生物利用度为(99.97±9.84)%.但两种制剂的t_(max)与C_(max)差异提示临床应用时应予注意.
AIM: To study the pharmacokinetics and relative bioavailability of lysine aspirin capsule. METHODS: Salicylic acid was determined after a single oral dose of lysine aspirin capsule and LAIBILIN(pulvis aspirin-dl-lysine)were given to 10 volunteers in an open randomized cross-over test. Salicylic acid concentration in serum was assayed by reversed phase high-performance liguid chromatography (RP-HPLC) method. RESULTS: After taking a single oral dose of 1000mg lysine aspirin capsule and 4 000mg LAIBILIN,the AUC0-∞ of salicylic acid of the two formulations were(251.81?3.58)and (255.12+44.76)(mg·h)/L;tmaxwere (3.52+0.50) and (0.97+0.4)h,cmsxwere (39.69+3.58)and(48.14+3.99) mg/L respectively. The bioavailability of lysine aspirin capsule computing as salicylic acid was (99. 97+9. 84)% relatively to LAIBILIN. CONCLUSION: The result of statistical analysis showed that there were no significant differences of the AUC0-∞ of salicylic acid between the two formulations (P>0. 05),but there were significant differences of tmax and cmax between the two formulations (P<0. 05),Lysine aspirin capsule was bioequivalent to LAIBILIN indicating as AUC0-∞ of salicyic acid.
出处
《中国临床药学杂志》
CAS
1998年第2期63-66,共4页
Chinese Journal of Clinical Pharmacy
关键词
赖氨匹林
药物动力学
生物利用度
lysine aspirin capsule
pharmacokinetics
bioavailability
