目的：制备异烟肼缓释胶囊，评价人体内药动学、生物利用度及患者体内血药浓度。方法：乙基纤维素为载体，相分离凝聚法制微囊，转篮法测释放特性；紫外光度法测10名志愿者单剂量po400mg异烟肼缓释胶囊与普通片后血药浓度，数据经MCP₈₆药动学程序处理。结果：体外释药：普通片T₅₀=0.032h；缓释胶囊：T₅₀=1h，释药10h以上。普通片c_max=11.12μg·ml^-1,t_max=1.41h,K:0.201h^-1;36h血药浓度：0μg·ml^-1。缓释胶囊:c_max=4.99μg·ml^-1,t_max=1.80h,K=0.03·h^-1,36h血药浓度：1.63μg·ml^{-1。配对与双侧ｔ检验结果表明：两者除t_max无显著性差异外，c_max及消除速率常数(k)均有显著性差异(P<0.01)。患者体内血药浓度：普通片与缓释胶囊分别为：1.5h时：(8.24±2.60)μg·ml-1,(3.69±0.51)μg·ml-1;36h:0μg·ml-1,2.09μg·ml-1。结论：该缓释胶囊处方合理、工艺简单，适用于工业化生产，可为结核患者临床防治提供一个新剂型。}

OBJECTIVE: To prepare and study the pharmacokinetics and release bioavailability in olunteers and concentrations in plasma in patients. METHODS: Ethylcellulose was used matrix in phase separationcoacervation for preparation of microencapsulation. The release experiments were performed in a rotating shaker. The isoniazid concentration in plasma was determined by spectrophotometrical method following a single oral dose of sustainedrelease cupsule and ordinary tablet respectively given to 10 volunteers in a open randomized crossover test. MCP₈₆was used to process main pharmacokinetic parameters. RESULTS: The sustainedrelease of capsule and ordinary teblet in vitro, T₅₀was 1 h and 0.032 h respectively. The drug in sustainedrelease capsule was sustained release over 10 h. The main parameters in body: ordinary tablets: c_max=11.12 μg·ml^-1, t_{max=1.41 h, K=0.201 h^-1; sustained release capsule: cmax.=4.99 μg·ml^-1, tmax=1.80 h, K=0.03 h^-1. The concentration of blood at 36 h was (0±0)μg·ml^-1and 1.63 μg·ml^-1,.respectively. Except tmax, there was significant difference between the two fomulations (P<0.01). The concentration of blood in patient at 1.5 h and 36 h. ordinary tablet and sustainedrelease capsule respectively were (8.24±2.60)μg·ml^-1, (0±0)μg·ml^-1and (3.69±0.86)μg·ml^-1, (2.09±0.56)μg·ml^-1. CONCLUSION: The sustainedrelease capsule will play an important part in prevention and treatment of tuberculosis as the result of its reasonable formulation and simple technology.}