Food, gastrointestinal pH, and models of oral drug absorption

Abuhelwa, Ahmad Y.; Williams, Dean C.; Upton, Richard N.; Foster, David J. R.

doi:10.1016/j.ejpb.2016.11.034

Cited by 223 publications

(171 citation statements)

References 155 publications

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“…The rate and extent of oral drug absorption is determined by a complicated process, which is not only dependent on the drug physicochemical properties but also the interaction between the gastrointestinal tract and the administrated formulation 26 . The FDM based 3D printed tablets usually have a rigid structure like hard plastic with different features from conventional tablets 25 .…”

Section: Resultsmentioning

confidence: 99%

Fused Deposition Modeling (FDM) 3D Printed Tablets for Intragastric Floating Delivery of Domperidone

Chai

Wang

et al. 2017

Sci Rep

246

119

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The aim of this study was to explore the feasibility of fused deposition modeling (FDM) 3D printing to prepare intragastric floating sustained release (FSR) tablets. Domperidone (DOM), an insoluble weak base, was chosen as a model drug to investigate the potential of FSR in increasing its oral bioavailability and reducing its administration frequency. DOM was successfully loaded into hydroxypropyl cellulose (HPC) filaments using hot melt extrusion (HME). The filaments were then printed into hollow structured tablets through changing the shell numbers and the infill percentages. Physical characterization results indicated that the majority of DOM gradually turned into the amorphous form during the fabrication process. The optimized formulation (contain 10% DOM, with 2 shells and 0% infill) exhibited the sustained release characteristic and was able to float for about 10 h in vitro. Radiographic images showed that the BaSO4-labeled tablets were retained in the stomach of rabbits for more than 8 h. Furthermore, pharmacokinetic studies showed the relative bioavailability of the FSR tablets compared with reference commercial tablets was 222.49 ± 62.85%. All the results showed that FDM based 3D printing might be a promising way to fabricate hollow tablets for the purpose of intragastric floating drug delivery.

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Section: Resultsmentioning

confidence: 99%

Fused Deposition Modeling (FDM) 3D Printed Tablets for Intragastric Floating Delivery of Domperidone

Chai

Wang

et al. 2017

Sci Rep

246

119

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“…In most early drug development trials, participants are required to be in a fasting state before administration of the investigational compound, since food intake is known to introduce physiological changes that show substantial intersubject variability and, among other effects, may influence the pharmacokinetics of the investigational drug (Abuhelwa, Williams, Upton, & Foster, 2017). During these trials, electrocardiograms (ECGs) are performed frequently to screen for adverse cardiac effects, and it is known that food intake can influence ECG parameters, such as changes in duration of the QTc interval (Taubel, Wong, Naseem, Ferber, & Camm, 2012) and/or QRS and T-wave morphology.…”

Section: Introductionmentioning

confidence: 99%

Effect of short‐term fasting on electrocardiographic parameters

Stuijt

Gal

Kemme

et al. 2019

Noninvasive Electrocardiol

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IntroductionDuring early drug development trials, electrocardiograms (ECGs) in healthy volunteers who are in a fasting state are evaluated to screen for possible adverse cardiac effects. However, the effect of the duration of fasting on electrocardiographic parameters is largely unknown. We compared the effects of fasting on standard 12‐lead electrocardiographic recordings.MethodsElectrocardiograms were available for 432 healthy subjects (mean age 28.5 ± 12.5; 88.9% male) who participated in early drug development studies after 4‐ and 10‐hr fasting. All ECGs were automatically analyzed for conduction intervals and wave amplitudes with the Marquette 12SL algorithm and compared among fasting duration. Mixed model analyses were used to identify confounding variables.ResultsAfter 10 hr of fasting, compared to after 4 hr of fasting, mean P‐wave duration and amplitude were reduced by 1.95 ± 1.48 ms and 2.18 ± 2.75 μV, mean R wave and S wave amplitude were decreased by 25.83 ± 31.16 μV and 55.39 ± 78.72 μV, mean QRS duration was decreased by 1.84 ± 6.61 ms, and mean T‐wave duration and amplitude were decreased by 2.06 ± 0.72 ms and 9.36 ± 17.21 μV (lead II). The mean PR interval was prolonged by 4.26 ± 17.67 ms, the ventricular rate was reduced by 3.64 ± 8.61 min, and QTcF was reduced by 3.87 ± 14.50 ms. These observations persisted after correction for demographics, electrolytes, blood pressure, heart rate variability, and diurnal variation.ConclusionThe present analysis showed that 10‐hr fasting compared to 4‐hr fasting resulted in changes to the surface ECG, consisting of a reduced wave amplitude and duration and increased isoelectric interval duration.

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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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Food, gastrointestinal pH, and models of oral drug absorption

Cited by 223 publications

References 155 publications

Fused Deposition Modeling (FDM) 3D Printed Tablets for Intragastric Floating Delivery of Domperidone

Fused Deposition Modeling (FDM) 3D Printed Tablets for Intragastric Floating Delivery of Domperidone

Effect of short‐term fasting on electrocardiographic parameters

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

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