人工骨异烟肼体外及家兔体内释放度研究

Dissolution of isonizide in isonizide-hydroxylapatite ceramic composites in vitro and in rabbits

目的：了解蜂蜡为阻滞剂包裹的异烟肼－人工骨（ＩＮＨ－ＰＨＡ－ｗａｘ）与未包裹蜂蜡的异烟肼－人工骨（ＩＮＨ－ＰＨＡ）体外及家兔体内的释放度。方法：用ＲＰ－ＨＰＬＣ在不同时间分别测定体外及植入家兔体内的包裹或未包裹蜂蜡的异烟肼－人工骨中异烟肼的浓度。结果：包裹１５％蜂蜡ＩＮＨ－ＰＨＡ－ｗａｘ，体外２０ｄ释药６６％；包裹２５％蜂蜡ＩＮＨ－ＰＨＡ－ｗａｘ，２０６释药２２％；未包裹蜂蜡ＩＮＨ－ＰＨＡ，６ｄ释药９７％。包裹２５％蜂蜡ＩＮＨ－ＰＨＡ－ｗａｘ植入家兔体内，可持续释药达２４０ｄ，而未包裹蜂蜡ＩＮＨ－ＰＨＡ持续释药仅６０ｄ。结论：ＩＮＨ－ＰＨＡ－ｗａｘ可有效地控制药物的释放，对治疗骨结核可能是一有效植入式缓释剂。

OBJECTIVE:To study the dissolution of isonizide(INH)in isonizide-hydroxylapatite ceramic composites (INH-PHA)encapsulated with the wax as a ratardant(INH-PHA-wax)and INH-PHA without the wax in vitro and in rabbits.METHOD:The concentration of INHin vitro and vivo at different times was determined by reversed HPLC respectively.RESULTS:66%of INH in INH-PHA-wax encapsulated with 1 5%wax was released in vitro at the 20th day,22%in INH-PHA-wax with 25%wax at the 20th day,97%in INH-PHA(without wax)at the sixth day. Releasing of INH maintained for 240 days in INH-PHA-wax encapsulated with 25%wax in rabbits,but only for 60 days in INH-PHA without wax.CONCLUSION: Releasing of INH could be controlled with INHPHA-wax.It may be an effective implanting sustained biomaterial to treat bone tuberculosis.