Ciprofloxacin permeability and its active secretion through rat small intestine in vitro

Žakelj, Simon; Šturm, Katja; Kristl, Albin

doi:10.1016/j.ijpharm.2006.02.004

Cited by 47 publications

(35 citation statements)

References 28 publications

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“…The octanolwater partition coefficient (logP) value for this compound is Ϫ1.08, suggesting moderately hydrophilic properties, which would serve to reduce lipid partitioning and passive transcellular absorptive permeability (Zhao et al, 2002). In agreement with this assessment, ciprofloxacin has been classified as a low-permeability compound (Volpe, 2004;Zakelj et al, 2006). In vivo it displays variable oral bioavailability of between 50 and 80% (Sörgel et al, 1989a).…”

Section: Introductionmentioning

confidence: 76%

“…Given the ambiguous evidence reported in previous publications (Rodríguez-Ibáñez et al, 2006;Zakelj et al, 2006), it was interesting to note that regional differences in secretory flux and permeability do exist. Net secretion of ciprofloxacin peaked in the ileum, suggesting higher active transport in this region.…”

Section: Haslam Et Almentioning

confidence: 95%

“…Active secretion of ciprofloxacin was observed in rat small intestinal tissue mounted in Ussing chambers, with higher secretory flux being observed in distal than in proximal small intestine (Zakelj et al, 2006). However, Rodríguez-Ibáñez et al (2006) demonstrated no regional variation in absorptive ciprofloxacin permeability in the rat using the in situ gut loop technique.…”

Section: Introductionmentioning

confidence: 91%

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Intestinal Ciprofloxacin Efflux: The Role of Breast Cancer Resistance Protein (ABCG2)

Haslam¹,

Wright²,

O’Reilly³

et al. 2011

Drug Metab Dispos

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ABSTRACT:Intestinal secretory movement of the fluoroquinolone antibiotic, ciprofloxacin, may limit its oral bioavailability. Active ATP-binding cassette ( , and verapamil as ABC-selective inhibitors. In addition, the regional variation in secretory capacity was investigated using male Han Wistar rat intestine mounted in Ussing chambers, and the first indicative measurements of ciprofloxacin transport by ex vivo human jejunum were made. Active, Ko143-sensitive ciprofloxacin secretion was observed in bcrp1-MDCKII cell layers, but in low-passage (BCRP-expressing) Caco-2 cell layers only a 54% fraction was Ko143-sensitive. Ciprofloxacin accumulation was lower in MRP4-HEK293 cells than in the parent line, indicating that ciprofloxacin is also a substrate for this transporter. Ciprofloxacin secretion by Caco-2 cell layers was not inhibited by MK571. Secretory flux showed marked regional variability in the rat intestine, increasing from the duodenum to peak in the ileum. Ciprofloxacin secretion was present in human jejunum and was reduced by Ko143 but showed marked interindividual variability. Ciprofloxacin is a substrate for human and rodent BCRP. An additional pathway for ciprofloxacin secretion exists in Caco-2 cells, which is unlikely to be MRP(4)-mediated. BCRP is likely to be the dominant transport mechanism for ciprofloxacin efflux in both rat and human jejunum.

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Section: Introductionmentioning

confidence: 76%

Section: Haslam Et Almentioning

confidence: 95%

Section: Introductionmentioning

confidence: 91%

See 1 more Smart Citation

Intestinal Ciprofloxacin Efflux: The Role of Breast Cancer Resistance Protein (ABCG2)

Haslam¹,

Wright²,

O’Reilly³

et al. 2011

Drug Metab Dispos

View full text Add to dashboard Cite

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“…This medium was selected since it has been well established that the oral bioavailability of Cip is related to the proportion of drug molecules that reach upper small intestine in solution state, as it is absorbed by passive paracellular transport (10,20,21). Figure 5 shows the uptake of simulated gastric fluid along time for the series of matrices.…”

Section: Preformulationmentioning

confidence: 99%

A Ciprofloxacin Extended Release Tablet Based on Swellable Drug Polyelectrolyte Matrices

et al. 2008

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Abstract. The aim of this work was the development of extended release tablets of 500 mg of ciprofloxacin based on swellable drug polyelectrolyte matrices (SDPM). A set of complexes of carbomer, ciprofloxacin and sodium, (CB-Cip) 50 Na x , having a molar ratio Cip/CB acid groups of 0.5 and variable proportions of Na + was used to prepare SDPM. Characterization of complexes by FT-IR, powder X-ray diffraction and thermal analysis revealed that Cip, in its protonated form, is ionically bonded to the functional groups of CB. Rates of fluid uptake of (CB-Cip) 50 Na x matrices as well as Cip release in simulated gastric fluid were modulated by changes in the proportion of Na + incorporated in the complexes. A direct correlation between fluid uptake and delivery rate was observed along the series of matrices. Release rates were modulated from 1.4 mg/min to 25 mg/min in going from (CB-Cip) 50 Na 10 to (CB-Cip) 50 Na 14 . The analysis of kinetic data suggest that rates of swelling, ionic pair dissociation and drug diffusion play a role in the kinetic control of delivery. Complexes were satisfactorily prepared and processed together with small amounts of antiadherent and lubricant excipients to obtain a series of extended release SDPM tablets through the current tableting technology processes. Cip release from matrices was widely modulated by the composition of the complexes yielding a flexible system that allows selecting a composition that releases in 120 min 90% of the dose in simulated gastric fluid.

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“…For oral drug delivery and nutrient absorption, it is known that villi and microvilli on the intestine wall have significant effects on solute permeation and absorption. Many studies have been focused on in vitro and in vivo measurements of solute permeation of small intestines [41][42][43][44]. Attempts have been also made to predict drug absorption [45].…”

Section: Discussionmentioning

confidence: 99%

A multi-scale model for solute transport in a wavy-walled channel

et al. 2008

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This paper concerns steady flow and solute uptake in a wavy-walled channel, where the wavelength and amplitude of the wall are comparable to each other but are much shorter than the width of the channel. The problem has two primary asymptotic regions: a core region where the walls appear flat at leading order and a wall region where there is full interaction between advection, diffusion and uptake at the wavy wall. For weak wall uptake, the effective uptake from the core is shown to increase with wall waviness in proportion to surface area, whereas for stronger wall uptake, it is found that the uptake from the core can be reduced as the wall amplitude increases. Conditions are identified under which this approximation is uniformly valid in a full channel flow, accounting for inlet conditions, and a comprehensive survey of the asymptotic distributions of solute both along and across the channel is provided. It is also shown how this multiscale approach can readily be extended to account for channel walls with multiple lengthscales of spatial variation.

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Ciprofloxacin permeability and its active secretion through rat small intestine in vitro

Cited by 47 publications

References 28 publications

Intestinal Ciprofloxacin Efflux: The Role of Breast Cancer Resistance Protein (ABCG2)

Intestinal Ciprofloxacin Efflux: The Role of Breast Cancer Resistance Protein (ABCG2)

A Ciprofloxacin Extended Release Tablet Based on Swellable Drug Polyelectrolyte Matrices

A multi-scale model for solute transport in a wavy-walled channel

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