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[小分子免疫调节剂甲砜霉素甘氨酸酯的基础与临床研究]

[Fundamental and clinical studies on forphenicinol, a small-molecular immunomodulator].

作者信息

Ishibashi T, Takamoto M, Shinoda A, Sugiyama K

出版信息

Jpn J Antibiot. 1984 Feb;37(2):185-97.

PMID:6737689
Abstract

Forphenicinol , a small-molecular immunomodulator, was orally administered to 10 long-term hospitalized patients with decreased pulmonary function, mainly, due to obsolete tuberculosis. The patients were grouped equally into 2, the first group received 50 mg of forphenicinol /day for 4 weeks and the second group received forphenicinol for a total period of 1 year, according to the following dose-schedule; 100 mg/day for the first 2 months, 400 mg/day for the next 6 months and 200 mg/day for the last 4 months. Investigations were made on the serum levels and safety of forphenicinol in all of these patients. The results of the investigations were as follows. Peak levels of forphenicinol were attained, in most cases, 2 hours after the administration and the average peak levels on the 14th day were 1.37 micrograms/ml for the dose of 50 mg/day, 5.02 micrograms/ml for 100 mg/day, 7.49 micrograms/ml for 200 mg/day and 15.02 micrograms/ml for 400 mg/day. There was no difference between the serum peak levels on the 1st and 14th days, in the patients who received forphenicinol at the dose of 50 or 100 mg/day. This finding led us to conclude that forphenicinol may not be accumulated in the body when it is administered repeatedly. Neither any side effects nor any abnormal values in the laboratory analysis of samples were observed for forphenicinol . The following improvement were observed, in the patients who received forphenicinol on a long-term basis (1 year); diminution of thick-walled cavity in 1 patient with atypical mycobacteriosis and in another patient with drug-resistant Mycobacterium tuberculosis, negative sputum culture for bacteria was observed during this whole period of forphenicinol treatment.

摘要

对苯尼考醇是一种小分子免疫调节剂,对10名长期住院、主要因陈旧性肺结核导致肺功能下降的患者进行了口服给药。患者被平均分为两组,第一组每天服用50毫克对苯尼考醇,持续4周,第二组根据以下剂量方案总共服用对苯尼考醇1年:前2个月每天100毫克,接下来6个月每天400毫克,最后4个月每天200毫克。对所有这些患者进行了对苯尼考醇的血清水平和安全性调查。调查结果如下。在大多数情况下,对苯尼考醇在给药后2小时达到峰值水平,第14天的平均峰值水平分别为:每天50毫克剂量时为1.37微克/毫升,每天100毫克时为5.02微克/毫升,每天200毫克时为7.49微克/毫升,每天400毫克时为15.02微克/毫升。在每天服用50或100毫克对苯尼考醇的患者中,第1天和第14天的血清峰值水平没有差异。这一发现使我们得出结论,反复给药时对苯尼考醇可能不会在体内蓄积。未观察到对苯尼考醇有任何副作用或实验室样本分析中的异常值。在长期(1年)接受对苯尼考醇治疗的患者中观察到以下改善情况:1例非典型分枝杆菌病患者和另1例耐多药结核分枝杆菌患者的厚壁空洞缩小,在整个对苯尼考醇治疗期间痰培养细菌呈阴性。

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1
[Fundamental and clinical studies on forphenicinol, a small-molecular immunomodulator].[小分子免疫调节剂甲砜霉素甘氨酸酯的基础与临床研究]
Jpn J Antibiot. 1984 Feb;37(2):185-97.
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Changes in the immunological parameters after a single dose of forphenicinol, a new small molecular immunomodifier.新型小分子免疫调节剂福苯尼醇单次给药后免疫参数的变化。
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Simple determination of forphenicinol in human plasma and erythrocytes by HPLC with native fluorescence detection.采用高效液相色谱法结合天然荧光检测法简单测定人血浆和红细胞中的甲砜霉素甘氨酸酯。
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