不同给药途径头孢氨苄速释和缓释对骆驼的药动学研究

Q1 Pharmacology, Toxicology and Pharmaceutics Advances in Pharmacological Sciences Pub Date : 2016-03-09 DOI:10.1155/2016/4621039
V. Kreil, L. Ambros, A. Prados, L. Tarragona, A. Monfrinotti, G. Bramuglia, M. Rebuelto
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引用次数: 3

摘要

我们研究了两种不同的头孢氨苄制剂通过静脉注射(IV)、肌肉注射(IM)和皮下注射(SC)途径给羊驼的药代动力学,头孢氨苄对羊驼分离的大肠杆菌和葡萄球菌的最低抑制浓度(MIC),并应用PK/PD建模方法,以便提出该物种的有效剂量建议。6只大羊羊立即(10mg /kg,静脉注射,IM和SC)和持续(8mg /kg IM, SC)释放头孢氨苄。采用非室室法计算药代动力学参数。与静脉注射和IM给药相比,即刻释放SC给药产生更长的消除半衰期(分别为1.3±0.2和0.6±0.1和0.6±0.1 h,分别为1.3±0.2和0.6±0.1 h),平均吸收时间比IM给药高(1.7±0.5和0.6±0.4 h)。制剂和给药途径的绝对生物利用度均在72-89%之间。头孢氨苄对葡萄球菌和大肠杆菌的MIC90值分别为1.0和8.0 μg/mL。我们的研究结果表明,速释制剂(10 mg/kg)对治疗葡萄球菌感染有效,每8小时(IM)或12小时(SC)给药一次,而缓释制剂(8 mg/kg)则需要每12或24小时分别给药一次。
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Pharmacokinetics of Immediate and Sustained Release Cephalexin Administered by Different Routes to Llamas (Lama glama)
We investigate the pharmacokinetics of two different cephalexin formulations administered to llamas by the intravenous (IV), intramuscular (IM), and subcutaneous (SC) routes, the minimum inhibitory concentration (MIC) of cephalexin against some Escherichia coli and staphylococci isolated from llamas, and we apply the PK/PD modelling approach, so that effective dosage recommendations for this species could be made. Six llamas received immediate (10 mg/kg, IV, IM, and SC) and sustained (8 mg/kg IM, SC) release cephalexin. Pharmacokinetic parameters were calculated by noncompartmental approach. Immediate release SC administration produced a significantly longer elimination half-life as compared with the IV and IM administration (1.3 ± 0.2 versus 0.6 ± 0.1 and 0.6 ± 0.1 h, resp.) and higher mean absorption time as compared with the IM administration (1.7 ± 0.5 versus 0.6 ± 0.4 h). Absolute bioavailability was in the range of 72–89% for both formulations and routes of administration. Cephalexin MIC90 values against staphylococci and E. coli were 1.0 and 8.0 μg/mL, respectively. Our results show that the immediate release formulation (10 mg/kg) would be effective for treating staphylococcal infections administered every 8 h (IM) or 12 h (SC), whereas the sustained release formulation (8 mg/kg) would require the IM or SC administration every 12 or 24 h, respectively.
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来源期刊
Advances in Pharmacological Sciences
Advances in Pharmacological Sciences PHARMACOLOGY & PHARMACY-
CiteScore
6.40
自引率
0.00%
发文量
0
审稿时长
14 weeks
期刊介绍: Advances in Pharmacological and Pharmaceutical Sciences is a peer-reviewed, Open Access journal that publishes original research articles, review articles, and clinical studies in all areas of experimental and clinical pharmacology, pharmaceutics, medicinal chemistry and drug delivery. Topics covered by the journal include, but are not limited to: -Biochemical pharmacology, drug mechanism of action, pharmacodynamics, pharmacogenetics, pharmacokinetics, and toxicology. -The design and preparation of new drugs, and their safety and efficacy in humans, including descriptions of drug dosage forms. -All areas of medicinal chemistry, such as drug discovery, design and synthesis. -Basic biology of drug and gene delivery through to application and development of these principles, through therapeutic delivery and targeting. Areas covered include bioavailability, controlled release, microcapsules, novel drug delivery systems, personalized drug delivery, and techniques for passing biological barriers.
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