摘要
目的:研究洛伐他汀缓释片在Beagle犬体内的药动学特征及其口服相对生物利用度。方法:Beagle 犬12条随机分为2组,分别单次口服洛伐他汀缓释片和普通片备60 mg,用RP-HPLC法检测血药浓度。药动学参数用3P97软件分析。结果:洛伐他汀缓释片和普通片的tmax分别为(2.7±5 0.8)和(2.8±1.0)h,cmax分别为(137±43)和(176±59)μg·L-1,t1/2分别为(11±4)和(10±5)h;AUC0-(?)分别为(956±146)和(1 005± 147)μg·h·L-1。以AUC0-(?)计算,与普通片相比,洛伐他汀缓释片的相对生物利用度为(95±6)%。洛伐他汀缓释片和普通片AUC0-(?)对数比值的90%可信限为81.6%-112.2%。结论:洛伐他汀缓释片具有一定缓释特性,与普通片相比具有生物等效性。
AIM: To study the oral correlative bioequivalence and pharmacokinetics of lovastatin sustained release tablets in Beagle dogs. METHODS: Twelve Beagle dogs were randomized divided into two groups:A, subjects administered with a single 60 mg oral dose of lovastatin sustained-release tablets and B, lovastatin generic tablets. Plasma lovastatin levels were determined by a reversed-phase HPLC method. The pharmacokinetic parameters were calculated by 3P97 software. RESULTS:The comparison of pharmacokinetic parameters between the two preparations ( lovastatin sustained-release tablets, lovastatin generic tablets) were as follow, tmax,cmax, t1/2 and AUC0-4 were(2.7 ± s 0.8) h, (137 ± 43)μg·L^-1, (11 ± 4) h,and (956 ±146) μg·h·L^-1 for lovastatin sustained-release tablets (group A) vs (2.8±1.0) h,(176 ± 59) μg·L^-1, (10 ± 5) h ,and (1 005 ± 147) μg·h·L^-1respectively for lovastatin generic tablets(group B). Relative bioavailability of the former was (95 ±6) %.The 90 % confidence interval calculated from log-transformed values was 81.6 %~112.2 % for logarithm ratio of AUC0-4 in two groups. CONCLUSION: Lovastatin sustained-release tablets shows prolonged-action characteristics and possesses bioequivalence with lovastatin generic tablets.
出处
《中国新药与临床杂志》
CAS
CSCD
北大核心
2006年第2期107-110,共4页
Chinese Journal of New Drugs and Clinical Remedies
关键词
洛伐他汀
迟效制剂
色谱法
高压液相
药动学
生物利用度
生物等效性
lovastatin
delayed-action preparations
chromatography, high pressure liquid
pharmacokinetics
biological availability
bioequivalence