非索非那定胶囊体外溶出度及在犬体内药动学评价  

In Vitro Release Behavior of Fexofenadine Capsules and its Pharmacokinetic Studies in Beagle Dogs

作　　者：袁春平[1] 彭可垄[2] 区淑蕴[2] 尹春萍[2] 

机构地区：[1]广东环球制药有限公司,佛山528303 [2]华中科技大学同济医学院药学院,武汉430030

出　　处：《医药导报》2011年第9期1141-1144,共4页Herald of Medicine

摘　　要：目的评价非索非那定胶囊的体外溶出度,建立犬血浆中非索非那定的液质联用(LC-MS/MS)测定法,并研究其在犬体内的药动学特性。方法采用大杯法在4种不同介质中测定非索非那定溶出度;6只比格(Beagle)犬分别单剂量灌胃给予非索非那定胶囊或非索非那定片各120 mg,采用LC-MS/MS法测定血浆非索非那定浓度,使用DAS2.1.1程序进行药动学参数计算。结果两种制剂体外溶出度良好;非索非那定胶囊剂及片剂的浓度-时间曲线下面积(AUC0-t)分别为(20.00±7.48)及(16.42±9.37)mg.L-1.h,AUC0-∞分别为(20.30±8.08)及(16.68±9.44)mg.L-1.h,半衰期(t1/2)分别为(3.10±1.60)及(4.54±2.03)h,达峰时间(tmax)分别为(1.58±0.49)及(1.67±0.68)h,峰浓度(Cmax)分别为(4.24±1.69)及(3.68±1.89)mg.L-1。结论非索非那定胶囊和片剂在体外有相似溶出度,两种制剂的主要药动学参数无明显差异,预示临床有相同疗效。Objective To evaluate in vitro release behavior of fexofenadine capsules, establish a LC-MS/MS method for the content determination of fexofenadine and study its pharmacokinetics in Beagle dogs. Methods The release behavior was evaluated by using a cup method in four media; a LC-MS/MS method was used to determine drug concentration after a single dose of administration of tablets or capsules in six dogs ; pharmacokinetic parameters were calculated with the DAS2.1.1 program. Results The two preparations showed good release behavior ; the AUC0-t of fexofenadiue capsules and tablets were （20.00±7.48）and （16.42±9.37） mg · L^-1 · h, AUC0-∞ were （20.30±8.08）and （16.68±9.44） mg · L^-1 · h, t1/2 were （3.10±1.60） and （4.54±2.03）h, tmax were （1.58±0.49）and （1.67±0.68） h, and C were （4.24±1.69）and （3.68±1.89） mg· L^-1, respectively. Conclusion The capsules and tablets of fexofenadine present similar release behavior in vitro. No obvious difference has been found between the main pharmacokinetic parameters of them, which suggests they would have the same therapeutic efficacy.

关 键 词：非索非那定 溶出度 药动学 液质联用 

分 类 号：R971.9[医药卫生—药品] R965[医药卫生—药学]