Food effect: The combined effect of media pH and viscosity on the gastrointestinal absorption of ciprofloxacin tablet

Radwan, Asma; Zaid, Abdel Naser; Jaradat, Nidal; Odeh, Yousef

doi:10.1016/j.ejps.2017.01.030

Cited by 20 publications

(22 citation statements)

References 24 publications

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“…These findings indicate that the absorption of ENR was more quickly and the quantity of ENR was higher in peak time at 0.3% LA level. Gastrointestinal pH is an important factor that can markedly affect oral drug absorption and bioavailability (Abuhelwa, Williams, Upton, & Foster, ) and decreased pH is beneficial to the dissolution and absorption of fluoroquinolone in the gastrointestinal tract (Radwan, Zaid, Jaradat, & Odeh, ). Jaafar et al found that organic acid feed supplementation can reduce the pH of gastrointestinal tract (Jaafar et al, ; Lim, Luckstadt, & Klesius, ).…”

Section: Discussionmentioning

confidence: 99%

Effect of lactic acid on enrofloxacin pharmacokinetics inEriocheir sinensis(Chinese mitten crab)

Wei

Sun

et al. 2019

Aquac Res

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As a representative acidifier, lactic acid (LA) is widely used in the diets of aquatic animals. LA is the main supporter of energy metabolism and may be associated with drug metabolism. This study was designed to explore the pharmacokinetics of enrofloxacin (ENR) in Eriocheir sinensis (Chinese mitten crab) fed diets containing 0.1%, 0.2% and 0.3% LA (designated groups LA1, LA2 and LA3 respectively). The concentrations of ENR in the haemolymph, hepatopancreas and muscle were determined by HPLC after a single oral dose of 10 mg/kg. Our results showed that LA had a significant effect on the peak ENR concentrations in all the tissues (p < 0.05) by one‐way ANOVA analysis. There was a trend that Cmax (peak concentration) of ENR was elevated with LA levels increasing up to 0.3% in haemolymph, hepatopancreas, muscle and Tmax (time‐point of the peak concentration of the drug), t1/2β (elimination half‐life) and AUC(0‐∞) of ENR were shortened. Taken together, 0.3% LA might be effective in improving ENR pharmacokinetics in E. sinensis. Furthermore, it can be speculated that the enhanced biotransformation of ENR in the hepatopancreas mediated by LA is responsible for the differences in the pharmacokinetics of ENR in E. sinensis.

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Section: Discussionmentioning

confidence: 99%

Effect of lactic acid on enrofloxacin pharmacokinetics inEriocheir sinensis(Chinese mitten crab)

Wei

Sun

et al. 2019

Aquac Res

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“…[31,[42][43][44][45] Various authors have proposed dissolution media to simulate the increase in the viscosity of gastric content using soup or various gelling agents such as guar gum, potato granules, HPMC and hydroxyethylcellulose to adjust the meal viscosity. [8,11,39,40] The large range of viscosities implemented in these studies demonstrate that it is difficult to identify a specific viscosity value that can be recommended for biorelevant media. Although the HPMC media applied in the zolpidem studies certainly provide a good qualitative description of the food effect, further work needs to be done in this area to arrive at a more quantitatively predictive dissolution method.…”

Section: Influence Of Meal Intake On Gastric Physiologymentioning

confidence: 99%

“…Other studies have indicated that there can be an inverse relationship between the increase in viscosity after food intake and drug absorption. An increase in viscosity can result in a decrease in drug diffusivity, slowing release of the drug into the gastric contents und potentially decreasing the rate of drug absorption …”

Section: Introductionmentioning

confidence: 99%

“…An increase in viscosity can result in a decrease in drug diffusivity, slowing release of the drug into the gastric contents und potentially decreasing the rate of drug absorption. [8,11] The biopharmaceutical classification system (BCS) proposed by Amidon et al in 1995 has been used to predict the type of food effect that can be expected for the different classes of drugs. Generally, for drugs that belong to BCS class I, which exhibit high solubility and high permeability, food intake is not expected to elicit changes in the extent of absorption.…”

Section: Introductionmentioning

confidence: 99%

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In-vitro–in-silicoinvestigation of the negative food effect of zolpidem when administered as immediate-release tablets

Paraiso

Watanabe

Andreas

et al. 2019

Journal of Pharmacy and Pharmacology

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Objectives The main objective of the present work was to combine in‐vitro and in‐silico tools to better understand the in‐vivo behavior of the immediate release (IR) formulation of zolpidem in the fasted and fed states. Methods The dissolution of zolpidem was evaluated using biorelevant media simulating the gastric and intestinal environment in the fasted and fed states. Additionally, the influence of high viscosity and high fat content on the release of zolpidem under fed state conditions was investigated. The in‐vitro results were combined with a physiologically based pharmacokinetic (PBPK) model constructed with Simcyp® to simulate the zolpidem pharmacokinetic profile in both prandial states. Key findings In vitro biorelevant dissolution experiments representing the fasted and fed states, combinedwith PBPKmodelling, were able to simulate the plasma profiles from the clinical food effect studies well. Experiments reflecting the pH and fat content of themeal led to a good prediction of the zolpidem plasma profile in the fed state, whereas increasing the viscosity of the gastricmedia led to an under‐prediction. Conclusions This work demonstrates that the combination of biorelevant dissolution testing and PBPK modelling is very useful for understanding the in‐vivo behavior of zolpidem in the fasted and fed states. This approach could be implemented in the development of other drugs exhibiting negative food effects, saving resources and bringing new drug products to the market faster.

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“…Physiologically based pharmacokinetic modelling (PBPK) has been applied in predicting a food effect using in silico simulation software packages, such as: GastroPlus™, SimCyp, PKsim and Stella. Some published literatures have suggested the coupling of in silico modelling with in vitro predictive dissolution testing for better prediction of food effect on drug performance (Andreas et al, ; Heimbach, Xia, Lin, & He, ; Ilić, Kovačević, & Parojčić, ; Jones, Parrott, Ohlenbusch, & Lavé, ; Parrott, Lukacova, Fraczkiewicz, & Bolger, ; Radwan, Zaid, Jaradat, & Odeh, ; Shono et al, ). Despite the many successful examples of food‐effect predictions using in silico tools, health authorities are still critical of the utility of PBPK modelling in predicting the clinical food effect on the oral absorption of drugs.…”

Section: Introductionmentioning

confidence: 99%

Evaluation of food effect on the oral absorption of clarithromycin from immediate release tablet using physiological modelling

Radwan

Jayyousi

Shraim

et al. 2019

Biopharm & Drug Disp

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Food effect: The combined effect of media pH and viscosity on the gastrointestinal absorption of ciprofloxacin tablet

Cited by 20 publications

References 24 publications

Effect of lactic acid on enrofloxacin pharmacokinetics inEriocheir sinensis(Chinese mitten crab)

Effect of lactic acid on enrofloxacin pharmacokinetics inEriocheir sinensis(Chinese mitten crab)

In-vitro–in-silicoinvestigation of the negative food effect of zolpidem when administered as immediate-release tablets

Evaluation of food effect on the oral absorption of clarithromycin from immediate release tablet using physiological modelling

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