The effects of mucus glycoproteins on the bioavailability of tetracycline. II. Binding

Kearney, P.; Marriott, Christopher

doi:10.1016/0378-5173(87)90132-3

Cited by 21 publications

(5 citation statements)

References 16 publications

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“…Braybrooks et al [19] observed a 50% decrease in the apparent permeability coefficients (P app ) for tetracycline in the presence of mucus. Kearney and Marriott [20] found an increase in lag-time as well as a decrease in the tetracycline transport rates using reverted gut experiments in the presence of mucus. Matthes et al [21] found that the disappearance rate of compounds of various polarities through a diffusion chamber was reduced when the buffer solutions in a drug-buffer mixture were replaced with mucus solution.…”

Section: Introductionmentioning

confidence: 97%

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Effect of pH, mucin and bovine serum on rifampicin permeability through Caco‐2 cells

Gonçalves

Fernandes

Chiann

et al. 2012

Biopharm & Drug Disp

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Rifampicin, a poorly soluble drug, has great importance in therapeutics as it is the main drug used to treat tuberculosis. The characterization of its permeability and the factors that influence it represent an important tool for predicting its bioavailability. Caco-2 cell monolayers were used as models of the intestinal mucosa to assess the uptake and transport of rifampicin and the effects of various experimental conditions were investigated, in order to establish the influence of these variables on rifampicin permeability. Different pHs (5.8, 6.8 and 7.4) in the apical medium, the presence or absence of mucin (3.0% w/v) in the donor site and the presence or absence of bovine serum albumin (4.0% v/v) in the receptor chamber were the evaluated conditions. The quantification of rifampicin in the apical or basolateral chambers was performed by a validated HPLC-UV method. The change in the donor chamber pH showed that permeability values were greater at pH 6.8, although this increase does not result in an alteration of the qualitative classification of rifampicin, which has high permeability. Mucin and bovine serum showed no effects on the permeability of rifampicin at the concentration tested. Overall, the current study suggests that pH, artificial mucin and bovine serum proteins have no influence on rifampicin permeability.

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Section: Introductionmentioning

confidence: 97%

“… observed a 50% decrease in the apparent permeability coefficients ( P app ) for tetracycline in the presence of mucus. Kearney and Marriott found an increase in lag‐time as well as a decrease in the tetracycline transport rates using reverted gut experiments in the presence of mucus. Matthes et al .…”

Section: Introductionmentioning

confidence: 99%

Effect of pH, mucin and bovine serum on rifampicin permeability through Caco‐2 cells

Gonçalves

Fernandes

Chiann

et al. 2012

Biopharm & Drug Disp

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“…Some drugs have been shown to chemically interact with the glycoproteins from mucus, limiting the drug absorption rate and decreasing drug bioavailability. These mucus–drug interactions can occur by electrostatic interactions between positively charged drugs and negatively mucins, which are ionized at pH > 2.6 (due to the sialic acid component), by hydrophobic interactions with the protein core of mucins or through hydrogen bonding [19–22] …”

Section: Introductionmentioning

confidence: 99%

Mucus thickness in the gastrointestinal tract of laboratory animals

Varum

Veiga

Sousa

et al. 2012

Journal of Pharmacy and Pharmacology

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“…The mechanism underlying the increase in OTC concentration in response to concurrent treatment with BHC is not known. Tetracyclines are highly bound to plasma proteins and have also been shown to bind to mucus glycoproteins (Brown et a1 1983;Kearney & Marriott 1987). BHC may compete for the same binding sites on glycoprotein or other mucus components thereby displacing OTC and leading to higher free concentrations of antibiotic.…”

Section: Discussionmentioning

confidence: 99%

Bromhexine plus Oxytetracycline: the Effect of Combined Administration Upon the Rheological Properties of Mucus from the Mini-pig

Martin

Loveday

Marriott

1993

Journal of Pharmacy and Pharmacology

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Three adult mini-pigs were employed to assess the effects of a twice daily dosage (40 mg kg-1) of oxytetracycline hydrochloride (OTC) and a combination of OTC with (0.5 mg kg-1) bromhexine hydrochloride (BHC) on the rheological properties and wet weight of secreted tracheal mucus. Mucus was collected daily from open-ended tracheal pouches established surgically in the mini-pigs. After a five day control period, either OTC or OTC plus BHC was administered twice daily with the normal diet. Each study period was followed by a five day washout period when mucus was collected but no drug given. The viscoelastic properties of each mucus sample were determined using creep compliance analysis. OTC was shown to increase the residual shear viscosity IP < 0.01) and increase the instantaneous compliance (P < 0.01). An increase in the wet weight of the collected mucus occurred in one pig only (P < 0.01). When BHC was co-administered with OTC, all of these changes were abolished. Evidence was obtained to suggest that BHC increased the concentration of OTC within the secreted mucus. BHC appeared to reverse the mucospissic activity of OTC in-vivo.

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The effects of mucus glycoproteins on the bioavailability of tetracycline. II. Binding

Cited by 21 publications

References 16 publications

Effect of pH, mucin and bovine serum on rifampicin permeability through Caco‐2 cells

Effect of pH, mucin and bovine serum on rifampicin permeability through Caco‐2 cells

Mucus thickness in the gastrointestinal tract of laboratory animals

Bromhexine plus Oxytetracycline: the Effect of Combined Administration Upon the Rheological Properties of Mucus from the Mini-pig

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