Cefotaxime pharmacokinetics after oral application in the form of 3α,7α-dihydroxy-12-keto-5β-cholanate microvesicles in rat

Goločorbin-Kon, Svetlana; Mikov, Momir; Arafat, M. Tarik; Lepojević, Žika; Mikov, Ivan; Sahman-Zaimovic, Majda; Tomić, Z.

doi:10.1007/bf03191381

Cited by 15 publications

(10 citation statements)

References 40 publications

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“…The level of significance between the groups was assessed with the Student's t-test for small independent samples using Excel software package (Microsoft Office 2007) 6 . All data are expressed as a mean ± standard deviation (SD).…”

Section: Discussionmentioning

confidence: 99%

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Influence of the Sodium Salt of 3α,7α-Dihydroxy-12-Oxo-5β-Cholanate on Antimicrobial Activity of Ampicillin In Vitro

Suvajdžić

Gigov²,

Rašković

et al. 2016

Acta Scientiae. Vet.

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Background: Multiple resistances to antibiotics are an emergent problem worldwide. Scientists intensively search for new substances with the antimicrobial potential or the mode to restore the activity of old-generation antibiotics. Ampicillin is the antibiotic with the expanded range of antimicrobial activity, but its use has decreased due to the poor absorption and highly developed resistance. In vivo studies showed that ampicillin has better absorption and bioavailability if combined with bile acid salts. The aim of this study was to examine antimicrobial effects of ampicillin alone and its combination with semisynthetic monoketocholic acid salt (MKH) in vitro.Materials, Methods & Results: In this study, commercial preparation of ampicillin and sodium salt of 3α,7α-dihydroxy-12oxo-5β-cholanate were used. Their effects were evaluated on Escherichia coli (E. coli), Enterococcus faecalis (E. faecalis) and Enterococcus faecium (E. faecium), obtained from urine specimens of dogs with clinically manifested cystitis. The first two investigated strains were ampicillin-sensitive, while E. faecium was resistant to ampicillin. Modified macrodilution method according to Clinical and Laboratory Standards Institute Guidelines (M7-A8) was performed. Bacterial suspension equivalent to 0.5 McFarland was prepared in saline, compared to the standard (Biomerieux) ad oculi. The density was checked spectrophotometrically at a wavelength of 625 nm and adjusted if necessary to the desired absorbance from 0.08 to 0.1. The resultant suspension was diluted 1:100 and inoculated in test tubes. Number of bacteria was counted on Petri plates using dilutions from 10-3 to 10-7 in order to obtain valid and countable plates. One hundred microliters of appropriate dilutions were aseptically plated in triplicate onto nutrient agar. Plates were incubated on 37°C for 72 h, under aerobic conditions. The number of colony forming units (CFU) was determined by direct counting. As a valid for enumeration, we took plates with 30 to 300 CFU. Percentage of killed bacteria for ampicillin was from 69.33-95.19% for E. coli, 87.1296.92% for E. faecalis and 7.20-33.30% for E. faecium. Ampicillin applied in the combination with MKH killed 99.99% to 100% of E. coli, 94.59% to 99.91% of E. faecalis and 31.73% to 64.76% of E. faecium. Mean percentage of killed bacteria for ampicillin was 81.93% for E. coli, 91.64% for E. faecalis, and 18.13% for E. faecium, while in combination with MKH percentage was 99.96% for E. coli, 98.23% for E. faecalis and 47.54% for E. faecium.Discussion: Results are presented as pharmacological minimal inhibitory concentration (MIC) values. Ampicillin was applied at the concentration higher than the therapeutic one, which could explain high MIC values for E. coli and E. faecalis. The combination of ampicillin with MKH showed the best improvement of antimicrobial effect on E. faecium (Δ = 29.41%), isolate that was resistant to ampicillin when applied alone. In all the investigated isolates, the combinations with MKH were more effective than ampicillin administered alone. It seems that MKH demonstrates a synergistic antimicrobial activity with ampicillin in vitro, which considerably decreases MIC values for all investigated isolates. These results implicate that MKH could restore the previous activity of ampicillin against some bacteria, which could be a significant benefit for clinical practice.

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Section: Discussionmentioning

confidence: 99%

“…Co-administration of ampicillin with bile acids protects normal intestinal flora [22]. Several in vivo studies showed better absorption and higher bioavailability of antibiotics if applied in the combination with bile acid salts [6,16,22,27].…”

Section: Introductionmentioning

confidence: 99%

Influence of the Sodium Salt of 3α,7α-Dihydroxy-12-Oxo-5β-Cholanate on Antimicrobial Activity of Ampicillin In Vitro

Suvajdžić

Gigov²,

Rašković

et al. 2016

Acta Scientiae. Vet.

Self Cite

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“…The active ingredient does not differ in the brand name drug and generic drug, other excipients, may be different and they may have contraindicated effect 10 . Since a wide variety of excipients are used in the drug formulation [11][12][13] . Therefore differences in excipients between brand name drugs and their generic versions can cause adverse drug reactions 14 even with rational drug use.…”

Section: Introduction:-mentioning

confidence: 99%

Evaluation of Anticancer Generic Drugs and Branded Drugs

D¹,

Prasanthi²,

S³

et al. 2018

IRJPS

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Cancer is a group of diseases involving abnormal cell growth with the potential to invade or spread to other body parts. Till now we have many drugs for the treatment of cancer which are available in branded and generic versions. In the present research, we studied about the difference between the branded and generic drugs in terms of their cost effectiveness, adverse effects, drug interactions, contraindications of the drugs used for cancer. we have collected the data from various retail pharmacies, authorized web sources and from up to date software. In our research we identified that the generic drugs shows huge variation in terms of cost effectiveness, adverse reactions, drug interactions & contraindications when compared with the branded one. This information provides us to choose better therapeutic approach towards cancer treatment.

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“…Considering the obvious drawbacks of drug administration by injection and potential side effects of high oral dosages, enhancing the oral bioavailability of CEF is a significant model study. Studies on oral bioavailability enhancement of BCS Class III cephalosporin antibiotics are limited in literature (16)(17)(18)(19).…”

Section: Introductionmentioning

confidence: 99%

Nanosized Liposomes Containing Bile Salt: A Vesicular Nanocarrier for Enhancing Oral Bioavailability of BCS Class III Drug

et al. 2017

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-PURPOSE: Liposomes have been studied as a colloidal carrier in drug delivery systems, especially for oral administration. However, their low structural integrity in the gut is still a major shortcoming. Membrane disruptive effects of physiological bile salts in the small intestine result in premature drug release prior to intestinal absorption. Thus, we analyzed the stabilizing effect of sodium deoxycholate when incorporated into nano-sized liposomes. METHOD: Cefotaxime-loaded liposomes were prepared with different sodium deoxycholate concentrations (3.75-30 mM) by rotary film evaporation followed by nanosize reduction. The physical integrity of liposomes was evaluated by monitoring cefotaxime leakage, particle sizes in different simulated physiological media. The oral bioavailability and pharmacokinetics of cefotaxime was assessed in rats (n = 6 per group) after single dose of drug-encapsulated in liposomes containing bile salt, drug in conventional liposomes, and cefotaxime solution (oral and intravenous). RESULTS: Simulated gastric fluid with low pH showed less effect on the stability of liposomes in comparison to media containing physiological bile salts. Liposomes containing 15 mM sodium deoxycholate were most stable in size and retained the majority of encapsulated cefotaxime even in fed state of simulated intestinal fluid being the most destructive media. Pharmacokinetics data showed an increase in Cmax and AUC0-inf in the following order: cefotaxime solution < conventional liposomes < liposomes made with bile salts. The total oral bioavailability of cefotaxime in liposomes containing bile salt was found to be 5-times higher compared to cefotaxime solution and twice as much as in conventional liposomes. CONCLUSION: Incorporation of bile salts, initially used as membrane permeation enhancer, also acted as a stabilizer against physiological bile salts. The nanosized liposomes containing sodium deoxycholate were able to reduce the leakage of encapsulated cefotaxime in the gut due to the improved vesicle stability and to enhance the oral bioavailability of acid-labile drugs up to 5-fold.

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Cefotaxime pharmacokinetics after oral application in the form of 3α,7α-dihydroxy-12-keto-5β-cholanate microvesicles in rat

Cited by 15 publications

References 40 publications

Influence of the Sodium Salt of 3α,7α-Dihydroxy-12-Oxo-5β-Cholanate on Antimicrobial Activity of Ampicillin In Vitro

Influence of the Sodium Salt of 3α,7α-Dihydroxy-12-Oxo-5β-Cholanate on Antimicrobial Activity of Ampicillin In Vitro

Evaluation of Anticancer Generic Drugs and Branded Drugs

Nanosized Liposomes Containing Bile Salt: A Vesicular Nanocarrier for Enhancing Oral Bioavailability of BCS Class III Drug

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