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目的探讨异烟肼植入剂的制备工艺和体内释放特性。研究异烟肼植入剂在家兔体内的药动学,并与异烟肼普通片进行比较。方法以高分子材料乳酸-乙醇酸共聚物(PLGA)作为基质,采用压模成型法制备异烟肼植入剂。用RP-HPLC测定8只家兔植入异烟肼植入剂后不同时间血浆和组织样品中的异烟肼浓度,并与口服异烟肼普通片比较,通过3P97计算药动学参数。结果 25%的载药量,以丙酮做溶剂制备的植入剂在55 d后,累积释药量达85%以上;在家兔体内可连续释药55 d以上,病灶部位的药物浓度始终高于最低抑菌浓度(0.02μg·mL-1),体内其他组织脏器的浓度明显低于口服给药。结论异烟肼植入剂可以有效的延长体内释药时间、降低全身分布的目的。
Objective To investigate the preparation process and in vivo release characteristics of isoniazid implants. The pharmacokinetics of isoniazid in rabbits was studied and compared with isoniazid tablets. Methods Injecting isoniazid as an implants by using PLGA as matrix. The concentrations of isoniazid in plasma and tissue samples at different time points were measured by RP-HPLC in 8 rabbits after inoculation with isoniazid. The pharmacokinetic parameters were calculated by 3P97 compared with oral isoniazid tablets. Results The drug release rate of 25% was better than 85% after 55 days. The sustained-release rate was above 55 days in rabbits and the drug concentration in the lesion site was always high At the lowest inhibitory concentration (0.02μg · mL-1), the concentration of other organs in the body was significantly lower than that of oral administration. Conclusion Isoniazid injections can effectively prolong the release time in vivo and reduce the systemic distribution.