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新型抗生素磷霉素吸收、分布与排泄的实验研究。II. 磷霉素钙盐口服制剂在犬体内的吸收(作者译)

[Experimental studies on absorption, distribution and excretion of a new antibiotic, fosfomycin. II. Absorption of oral preparations of fosfomycin calcium salt in dogs (author's transl)].

作者信息

Fujita M, Tomo N, Abe M, Hosoi K, Sató T

出版信息

Jpn J Antibiot. 1975 Jun;28(3):314-9.

PMID:1152285
Abstract

To establish the best usage and dosage of fosfomycin granule and capsules which had been prepared based on our fundamental experiences as described in the first report, absorption of calcium salt contained in both preparations was evaluated using dogs as test animals. (1) Granule containing the calcium salt equivalent to 200 mg of fosfomycin free acid per g showed almost the same absorption as the bulk (fosfomycin calcium), having no disadvantage due to processing. (2) Capsules containing the calcium salt equivalent to 250 mg and 500 mg of the free acid per capsule showed slightly more retarded absorption than the bulk, probably due to some inevitable factors such as disintegration rate of capsules and dispersion rate of the calcium salt. But, once dispersed, the calcium salt in capsules was well absorbed as well as the bulk material. (3) Gastrointestinal absorption of granule and the capsule contents was almost the same. (4) Simultaneous administration of capsules and water improved the absorption efficiency. Though administration after feeding caused somewhat retarded absorption of the drug, the serum levels were rather well sustained with a slight drop but sufficiency of absorption, suggesting better clinical advantages than in the fasted animals. (5) Fosfomycin calcium salt in both preparations was well absorbed in the test animals through gastrointestinal tract as well as the bulk calcium salt, without any possible disadvantage caused by processing. In addition, the absorption efficiency was improved by giving with water or meal to the animals.

摘要

为确定基于首份报告中所述的基础经验所制备的磷霉素颗粒剂和胶囊剂的最佳用法和用量,以犬作为试验动物评估了这两种制剂中所含钙盐的吸收情况。(1) 每克含相当于200毫克磷霉素游离酸钙盐的颗粒剂,其吸收情况与原料药(磷霉素钙)几乎相同,不存在因加工而产生的劣势。(2) 每粒含相当于250毫克和500毫克游离酸钙盐的胶囊剂,其吸收比原料药稍显滞后,这可能是由于某些不可避免的因素,如胶囊的崩解速率和钙盐的分散速率。但是,一旦分散,胶囊中的钙盐与原料药一样能被很好地吸收。(3) 颗粒剂和胶囊内容物的胃肠道吸收情况几乎相同。(4) 同时服用胶囊和水可提高吸收效率。虽然进食后给药会使药物吸收稍有延迟,但血清水平维持得相当好,虽有轻微下降但吸收充分,这表明与空腹动物相比具有更好的临床优势。(5) 两种制剂中的磷霉素钙盐在试验动物的胃肠道中与原料药钙盐一样能被很好地吸收,不存在任何因加工而可能产生的劣势。此外,给动物喂水或进食可提高吸收效率。

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