Jeanes C W, Schaefer O, Eidus L
Can Med Assoc J. 1973 Sep 15;109(6):483-7.
Two groups of tuberculosis patients, phenotyped as either slow or fast inactivators of isoniazid, participated in a preliminary bioavailability study of a new INH-matrix preparation with sustained action. The absorption, excretion and metabolic patterns of the new form were compared with those of standard INH tablets in both sets of patients, using a crossover technique.The INH-matrix was more slowly absorbed by both slow and fast inctivators. When the latter were treated with 30 mg./kg. of the matrix formulation the blood levels attained were comparable with those observed in slow acetylators treated with 10 mg./kg. normal INH. Although this dose is three times that normally recommended with standard INH, blood levels remained within safe limits owing to the drug's slow release from the matrix.
两组经表型鉴定为异烟肼慢灭活剂或快灭活剂的肺结核患者参与了一种新型具有持续作用的异烟肼基质制剂的初步生物利用度研究。采用交叉技术,在两组患者中比较了这种新剂型与标准异烟肼片剂的吸收、排泄和代谢模式。异烟肼基质在慢灭活剂和快灭活剂体内的吸收均较慢。当快灭活剂接受30毫克/千克的基质制剂治疗时,所达到的血药浓度与接受10毫克/千克标准异烟肼治疗的慢乙酰化者所观察到的血药浓度相当。尽管该剂量是标准异烟肼通常推荐剂量的三倍,但由于药物从基质中缓慢释放,血药浓度仍保持在安全范围内。