硝基安定的药代动力学研究  

STUDY ON PHARMACOKINETICS OF CHLONAZEPAN

作　　者：邹雄[1] 王艳君[1] 周瑞海[1] 刘少平 周文[1] 

机构地区：[1]山东医科大学附属医院中心实验室

出　　处：《山东医科大学学报》1998年第2期170-175,共6页Acta Academiae Medicinae Shandong

基　　金：山东省科委资助

摘　　要：为研究硝基安定的药代动力学参数，测定了正常健康服药者５例，正在服药并达到稳态浓度的癫痫患者２０例的间隔血药浓度。采用高压液相色谱仪外标法定量测定，所获数据利用药代动力学程序包处理，先用半对数法确定模式，再由残数法获得初步数据，最后用线性拟合法获得参数，拟合精度Ｅ０为０．００００１。２０例患者中，２例拟合失败，余１８例中，选择拟合相关系数ｒ和相关指数ＣⅠ均大于０．９的７例，求其各参数的平均值，主要结果为：一级吸收速率常数Ｋａ为６．４３７±９．３１６ｍｇ／Ｌ；分布半衰期Ｔ１／２ａ为１．０１７±０．７４０ｈ，分布相速率常数Ａ为０．５００±０．４０５，消除半衰期Ｔ１／２β为３．０４２±１．６６４ｈ，消除速率常数Ｋ为０．２８８±０．１２４，中央室分布容积和生物利用度比值ＶＣ／Ｆ为２３４５．４７±１０３７，每公斤体重中央室分布容积和生物利用度比值ＶＣ／（Ｆ．Ｋｇ）为４９．１９±１６．４３，达峰时间Ｔｐｋ２．２４２±０．７０４ｈ。上述有关参数及患者初始浓度Ｃｏ经“给药方案程序”运算，计算出３ｄ内最高浓度和患者实测最高浓度相比较，１８例中除２例外，相关系数ｒ＝０．７１１，Ｐ＜０．０１，相关公式为实测浓度（ｎｇ／ｍｌ）＝计算?In order to set the pharmacokinetics parameters of chlonazepan,five healthy volunteers(male 2,female 3,age 20￣45y)and twenty patiants with epilepsy(male 11,female 9,age 3￣59y)took chlonazepan orally.Serum concentration of chlonazepan was measured by HPLC before drug administration and at 1,1.5,2,3,4 h after administration.The results were analysised in the phamacokinetics management program(PKBP N1).Chlonazepan was confirmed in onecompartment model by log regression method.The results showed parameters of chlonazepan in patients were as follows:K absorbance:6.437±9.316,T1/2 α:1.017±0.740h,A:0.500±0.405,eliminant half time(T1/2β):3.042±1.664h,T peak:2.242±0.704h,VC/F:2345.47±1037,VC/(F.Kg):49.19±16.43.The maximum concentration was calculated by PKBP Ν1 compared with true maximum concentration,the r was 0.711 ( P <0.01).According to the parameters and primary serum concentration of chlozapen,the best treatment program can be established.

关 键 词：硝基安定 药代动力学 癫痫 

分 类 号：R971.3[医药卫生—药品] R742.105[医药卫生—药学]