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氨苄西林和阿莫西林在信鸽(家鸽)体内片剂、胶囊剂及长效制剂的生物利用度和药代动力学

Bioavailability and pharmacokinetics of ampicillin and amoxycillin from tablets, capsules and long-acting preparations in the homing pigeon (Columba livia).

作者信息

Dorrestein G M, van Gogh H, Rinzema J D, Buitelaar M N

出版信息

J Vet Pharmacol Ther. 1986 Dec;9(4):394-401. doi: 10.1111/j.1365-2885.1986.tb00060.x.

Abstract

Three ampicillin and three amoxycillin formulations (tablets and capsules, administered orally, and oily suspensions, injected intramuscularly (i.m.) and subcutaneously (s.c.] were studied in twenty adult homing pigeons (Columba livia). Bioavailability, pharmacokinetics and recovery were determined for each product and administration route. A standard dose of 50 mg/pigeon or 100 mg/kg was used in each study. The mean availability calculated for each of these preparations was 7% for ampicillin anhydrate tablets, 22% for amoxycillin trihydrate tablets, 17% for ampicillin trihydrate capsules, 67% for amoxycillin trihydrate capsules, 46% for ampicillin oily suspension i.m., 67% for amoxycillin oily suspension i.m. and 43% for amoxycillin oily suspension s.c. The blood concentration-time curves for the tablets were very scattered, which was far less the case for the capsules. The maximum blood concentration (Cmax) for amoxycillin was twice as high as for ampicillin. The Cmax resulting from the oily suspensions administered i.m. were low (4.35 +/- 1.05 and 5.04 +/- 1.36 mg/l, for ampicillin and amoxycillin, respectively). The Tmax for ampicillin was 10 h and for amoxycillin it was 0.9 h after administration. Both curves showed biphasic absorption, the initial peak representing an absorption and a distribution phase and the second part reflecting the 'depot-nature' of the drug. After the s.c. administration of the amoxycillin oily suspension the same pattern was found, but the Cmax, which was found at 2.13 +/- 1.03 h after administration, was low (2.81 +/- 0.68 mg/l).(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

在20只成年归巢鸽(家鸽)身上研究了三种氨苄西林制剂和三种阿莫西林制剂(片剂和胶囊,口服给药,以及油性混悬液,肌肉注射和皮下注射)。测定了每种产品和给药途径的生物利用度、药代动力学和回收率。每项研究均使用50 mg/只鸽子或100 mg/kg的标准剂量。这些制剂中,无水氨苄西林片剂的平均生物利用度为7%,三水阿莫西林片剂为22%,三水氨苄西林胶囊为17%,三水阿莫西林胶囊为67%,氨苄西林油性混悬液肌肉注射为46%,阿莫西林油性混悬液肌肉注射为67%,阿莫西林油性混悬液皮下注射为43%。片剂的血药浓度-时间曲线非常分散,而胶囊的情况则远非如此。阿莫西林的最大血药浓度(Cmax)是氨苄西林的两倍。肌肉注射油性混悬液产生的Cmax较低(氨苄西林和阿莫西林分别为4.35±1.05和5.04±1.36 mg/l)。氨苄西林给药后的达峰时间(Tmax)为10小时,阿莫西林为0.9小时。两条曲线均显示双相吸收,初始峰代表吸收和分布阶段,第二部分反映药物的“贮库性质”。皮下注射阿莫西林油性混悬液后也发现了相同的模式,但给药后2.13±1.03小时出现的Cmax较低(2.81±0.68 mg/l)。(摘要截短于250字)

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