盐酸地尔硫上（艹）下（卓）控释胶囊的药代动力学和生物利用度

 目的 以盐酸地尔硫上（艹）下（卓）普通片为参比制剂，研究盐酸地尔硫上（艹）下（卓）控释胶囊的药代动力学性质和相对生物利用度。方法 采用自身对照法，健康志愿受试者分别单剂量和多剂量口服盐酸地尔硫上（艹）下（卓）控释胶囊与普通片，采用反相高效液相色谱法测定地尔硫上（艹）下（卓）血药浓度变化情况，3P87药代动力学程序进行处理。结果 单剂量 po 60 mg盐酸地尔硫上（艹）下（卓）控释胶囊与普通片的AUCo→τ分别为(637.56±106.18) h·μg·L^-1和(597.39±117.60) h·μg·L^-1，t_max分别为(59.5±8.0)μg·L^-1和(99.7±8.2) μg·L^-1，t_max分别为(4.5±0.5) h和(3.0±0.3) h，t_1/2分别为(5.9±1.1) h和(5.3±0.7) h，相对生物利用度为(106.39±12.53)%。多剂量 po 盐酸地尔硫上（艹）下（卓）控释胶囊(每次60 mg，每日2次)与盐酸地尔硫上（艹）下（卓）普通片每次30 mg，每日3次达稳态后，AUCo→τ分别为(620.35±73.75) h·μg·L^-1和(303.90±54.53) h·μg·L^-1，c^ss_max分别是(79.0±7.6)μg·L^-1与(73.3±12.6) μg·L^-1，c^ss_min分别是(33.1±5.5)μg·L^-1与(23.9±5.7)μg·L^-1，c_ss分别为(51.7±6.2)μg·L^-1和(38.0±6.8)μg·L^-1，t_max分别为(3.4±0.5)h与(1.7±0.2) h，波动度(DF)分别是(0.89±0.11)与(1.30±0.16)，相对生物利用度为(102.06±11.46)%。以配对 t 检验与双单侧 t 检验对上述参数进行统计分析，两种制剂的 AUC 无显著性差异(P＞0.05)，而其它参数均有显著性差异(P＜0.05)。结论 两种制剂具生物等效性；盐酸地尔硫上（艹）下（卓）控释胶囊具有显著的控释特征。

The pharmacokinetics and relative bioavailability of diltiazem hydrochloride controlled-release capsule in healthy volunteers

OBJECTIVE To study the pharmacokinetics and relative bioavailability of diltiazem hydrochloride controlled-release (DTZ-CR) capsule in healthy male volunteers.METHODS Diltiazem tablet was used as the refereace.A crossover self-control study of single and multiple dose was conducted on 12 healthy volunteers.Plasma concentrations were determined by HPLC.RESULTS The pharmacokinetic parameters after a single dose of 60 mg DTZ-CR capsule were: AUC_0→τ=(637.56±106.18) h·μg·L^-1,c_max=(59.5±8.0) μg·L^-1，t_max(4.5±0.5) h,t_1/2=(5.9±1.1) h,respectively.The relative bioavailability was (106.39±12.53)%.The degree of fluctuation for steady state of multipledoses was (0.89±0.11) μg·L^-1，which were significantly lower than that of the reference tablet.CONCLUSION The two formulations were of bioequivalence and DTZ-CR capsule had marked characteristics of controlled release.