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(0.02 μgmL-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。
Abstract
OBJECTIVE To prepare isoniazid (INH) implant and evaluate the release behavior in rabbits and compare the pharmacokinetic characteristics and bioavailability of INH implant and INH tablets in rabbits. METHODS Poly (lactic-co-glycolic) acid (PLGA) was chosen as base material, and compression molding forming was used to prepare the INH implant. The concentrations of INH in plasma and organs of 8 rabbits after administrating the INH implant and tablets at different time were determined by RP-HPLC. The pharmacokinetic parameters were computed by software 3P97. RESUTLS The accumulative release percentage of INH from the implant with a drug loading of 25% using acetone as solvent was more than 85% after 55 d. The concentrations at focus were always higher than the MIC of INH (0.02 μgmL-1), while the concentrations at other tissues were less than those after oral administration. CONCLUSION The prepared INH implant possesses extended-release property in vivo and can decrease the system distribution of INH.
关键词
异烟肼植入剂 /
制备 /
体外释放 /
体内释放
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Key words
isoniazid implant /
preparation /
in vitro release /
in vivo release
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中图分类号：
R944
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参考文献
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