摘要
目的 阐明西替利嗪伪麻黄碱缓释胶囊中的伪麻黄碱是否具有缓释特征。方法 采用双周期随机交叉试验设计,分别给予12名男性健康受试者试验制剂西替利嗪伪麻黄碱缓释胶囊1粒(含盐酸伪麻黄碱120mg·粒^-1)或参比制剂氨酚伪麻4粒(含盐酸伪麻黄碱30nag·粒^-1),采用LC/MS/MS法测定伪麻黄碱的血药浓度。结果 参比制剂氨酚伪麻片和试验制剂西替利嗪伪麻黄碱缓释胶囊的主要药物动力学参数AUC0-24、AUC0-∞、Cmax、MRT、t1/2α、t1/2β和tmax均数±标准差)分别为:(2545.0±779.5)和(2687.4±643.2)ng·h·mL^-1;(2684.4±765.2)和(2844.7±663.8)ng·h·mL^-1;(418.5±130.5)和(276.2±79.4)ng·mL^-1;(6.6±0.7)和(8.0±0.7)h;(0.2±0.2)和(4.9±1.2)h;(10.2±1.1)和(9.8±1.O)h;(1.4±0.5)和(4.9±1.2)h。方差分析表明试验制剂的改‰、MRT均〉参比制剂(P〈0.05)。非参检验结果表明参比制剂中伪麻黄碱的tmax显著短于试验制剂(U=4.199,P〈0.001)。结论 江苏豪森药业股份有限公司生产的西替利嗪伪麻黄碱缓释胶囊中伪麻黄碱具有缓释特征。
Objective To explore the pharmacokinetics of pseudoephedrine in cetirizine and pseudoephedrine sustained-release capsules. Methods A single oral dose of 120 nag pseudoephedrine from in cetirizine and pseudoephedrine sustained-release capsules (CPSRC) or from paraeetamol and pserdoephedrine hydrochloride tablets (PPT) was given to 12 healthy male volunteers in an open randomized two way crossover design. The plasma concentration of pseudoephedrine was determined by HPLC/ MS/ MS. Results The main pharmacokinetie parameters AUC0-24 , AUC0-∞, Cmax, MRT, t1/2α, t1/2β and tmax of the pseudoephedrine in the PPT and the CPSRC were (2 545.0± 779. 5) and (2 687.4 ± 643. 2) ng . h . mL^-1 , (2 683.4 ± 765.2) and (2 844.7±663.8) ng.h.mL^-1, (418.5±130.5) and (276.2±79.4) ng.mL^-1, (6.6±0.7) and (8.0± 0. 7) h, (0. 2±0. 2) and (4. 9±1.2) h, (10. 2±1.1) and (9.8±1.0) h, and (1.4±0. 5) and (4. 9±1.2) h, respectively. Both t1/2α and MRT pserdoephedrine in the CPSRC were larger than those in the PPT analyzed by ANOVA (P〈 0. 05). tmax was shorter than that of pserdoephedrine in CPSRC according to Nonparametric Test (U=4. 199, P〈 0. 001). Conclusion Pseudoephedrine in cetirizine and pseudoephedrine sustained-release capsules is sustained.
出处
《中南药学》
CAS
2007年第4期317-320,共4页
Central South Pharmacy