Penetration of amoxycillin into the respiratory tract tissues and secretions in pigs

Agersø, Henrik; Friis, Christian

doi:10.1016/s0034-5288(98)90133-3

Cited by 29 publications

(43 citation statements)

References 29 publications

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“…This is consistent with the results of Fernandez et al [111] where flip-flop pharmacokinetics was observed following im. injection of amoxicillin trihydrate suspension in sheep, horses [112,113] and pigs [114]. …”

Section: Drug Examplesmentioning

confidence: 99%

Flip-flop Pharmacokinetics – Delivering a Reversal of Disposition: Challenges and Opportunities During Drug Development

Yáñez

Remsberg

Sayre

et al. 2011

Therapeutic Delivery

189

108

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Flip-flop pharmacokinetics is a phenomenon often encountered with extravascularly administered drugs. Occurrence of flip-flop spans preclinical to human studies. The purpose of this article is to analyze both the pharmacokinetic interpretation errors and opportunities underlying the presence of flip-flop pharmacokinetics during drug development. Flip-flop occurs when the rate of absorption is slower than the rate of elimination. If it is not recognized, it can create difficulties in the acquisition and interpretation of pharmacokinetic parameters. When flip-flop is expected or discovered, a longer duration of sampling may be necessary in order to avoid overestimation of fraction of dose absorbed. Common culprits of flip-flop disposition are modified dosage formulations; however, formulation characteristics such as the drug chemical entities themselves or the incorporated excipients can also cause the phenomenon. Yet another contributing factor is the physiological makeup of the extravascular site of administration. In this article, these causes of flip-flop pharmacokinetics are discussed with incorporation of relevant examples and the implications for drug development outlined.

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Section: Drug Examplesmentioning

confidence: 99%

Flip-flop Pharmacokinetics – Delivering a Reversal of Disposition: Challenges and Opportunities During Drug Development

Yáñez

Remsberg

Sayre

et al. 2011

Therapeutic Delivery

189

108

View full text Add to dashboard Cite

show abstract

“…The oral bioavailability of AMOX in pigs ranges from 28% to 33% and the drug freely distributes to lymph nodes and to both bronchial secretions and mucous. [25,26] We report encapsulation of the amoxicillin anion into the interlayer space of layered zinc hydroxide through an ion-exchange method which is very simple. In this work, we investigated the antibacterial properties and drug release of the resulting AMOX-LZH nanocomposite.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, characterisation and sustained release properties of layered zinc hydroxide intercalated with amoxicillin trihydrate

Nabipour

Sadr

Thomas

2015

Journal of Experimental Nanoscience

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The intercalation of amoxicillin trihydrate (AMOX) into layered zinc hydroxide (LZH) has been achieved via ion-exchange method. The resulted nanocomposite (AMOX-LZH) has been thoroughly characterised by a number of techniques including powder X-ray diffraction (PXRD), FT-IR spectroscopy, TGA/DTG analysis and scanning electron microscopy (SEM). The PXRD results showed that the gallery height of LZH was expanded from 9.57 to 11.97 A , indicating that the AMOX anions were successfully intercalated into the interlayer space of LZHs. The increased thermal stability of nanocomposite was confirmed by TGA/ DTG analyses. Improved antibacterial activity and minimum inhibitory concentration of AMOX-LZH nanocomposite was evaluated against Grampositive bacteria Staphylococcus aureus, Klebsiella pneumonia and Gram-negative Escherichia coli using the disk diffusion technique. The sustained release of amoxicillin drug from the AMOX-LZH nanocomposite was also verified.

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“…Therefore, FOS may be useful in the treatment of lung infections caused by facultative intracellular microorganisms. However, it is well-known that the pathophysiological changes induced by inflammation that occur in the lungs of infected pigs (dilation of the capillaries and increased vascular supply to the infected region) may influence the antibiotic pharmacokinetics in the respiratory tract of swines (Baggot, 1977;Agerso and Friis, 1998). Thus, additional studies on FOS pharmacokinetics should be carried out in diseased pigs.…”

Section: Discussionmentioning

confidence: 99%

Intracellular Concentrations of Fosfomycin in Alveolar Macrophages from Weaning Piglets

Pérez¹,

Soraci²,

Martínez³

et al. 2015

Research J. of Veterinary Sciences

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At weaning, piglets are more susceptible to infectious diseases, being respiratory syndromes one of the most frequent conditions. Fosfomycin is indicated for the treatment of a variety of porcine bacterial pathogens, with MIC 90 ranging between 0.25-0.50 µg mLG 1 . Fosfomycin exhibits a time-dependent killing. Thus, killing of bacteria occurs when its concentrations remain constantly above the MIC. Fosfomycin concentrations in respiratory cells and epithelial lining fluid of pigs have already been studied. Although, fosfomycin showed clinical efficacy in the treatment of pulmonary diseases, concentrations in alveolar macrophages (biophase for facultative and obligate intracellular microorganisms) have not been established in any species. The present study determined the intracellular concentrations of disodium fosfomycin in alveolar macrophages after a single IM dose of 15 mg kgG 1 in the gluteal muscle. Concentrations ranged from 0.14-1.52 µg mLG 1 , being lower than those found in epithelial lining fluid (49.03%) and respiratory cells (54.48%). The C max was 1.52 µg mLG 1 and T max was 4 h. Concentrations exceeded the MIC 90 for most pathogens of importance in pig production for up to six hours (T>MIC = 6 h). Therefore, fosfomycin may be useful in the treatment of lung infections caused by facultative intracellular microorganisms.

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Penetration of amoxycillin into the respiratory tract tissues and secretions in pigs

Cited by 29 publications

References 29 publications

Flip-flop Pharmacokinetics – Delivering a Reversal of Disposition: Challenges and Opportunities During Drug Development

Flip-flop Pharmacokinetics – Delivering a Reversal of Disposition: Challenges and Opportunities During Drug Development

Synthesis, characterisation and sustained release properties of layered zinc hydroxide intercalated with amoxicillin trihydrate

Intracellular Concentrations of Fosfomycin in Alveolar Macrophages from Weaning Piglets

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