Investigation of some factors contributing to negative food effects

Marasanapalle, Venugopal P.; Crison, John R.; Ma, Jingwen; Li, Xiaoling; Jasti, Bhaskara

doi:10.1002/bdd.647

Cited by 37 publications

(21 citation statements)

References 38 publications

(38 reference statements)

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“…[6][7][8] In the literature, no significant food effect has been reported when amlodipine and HCTZ tablets/capsules monotherapies were administered with…”

mentioning

confidence: 99%

Effect of food on the oral bioavailability of amlodipine/valsartan and amlodipine/valsartan/hydrochlorothiazide fixed dose combination tablets in healthy subjects

Sunkara

Jiang

Reynolds

et al. 2014

Clinical Pharm in Drug Dev

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A double fixed dose combination of amlodipine/valsartan and triple fixed dose combination of amlodipine/valsartan/HCTZ tablets have been developed to treat patients with moderate-to-severe hypertension. Here, we present the effect of food on the oral bioavailability of these two fixed dose combination tablets from two separate clinical studies in healthy subjects. Single oral doses of amlodipine/valsartan (10/160 mg) and amlodipine/valsartan/HCTZ (10/320/25 mg were administered under fasted or fed conditions. Blood samples were collected in both studies to determine the pharmacokinetic parameters of amlodipine, valsartan, and/or HCTZ using non-compartmental analysis. Following amlodipine/valsartan administration, the geometric mean ratios (GMRs, 90% CI) of AUC0-∞ and Cmax were 1.09 (1.05-1.13) and 1.03 (0.97-1.09) for amlodipine, and 0.94 (0.81-1.10) and 0.86 (0.73-1.02) for valsartan, respectively. Following amlodipine/valsartan/HCTZ administration, the GMRs (90%CI) of AUC0-∞ and Cmax were 1.09 (1.04-1.15) and 1.11 (1.05-1.08) for amlodipine, 1.14 (0.99-1.31) and 1.12 (0.98-1.29) for valsartan, and 1.09 (1.02-1.16) and 0.86 (0.79-0.93) for HCTZ, respectively. Considering the sample size and pharmacokinetic variability associated with analytes, these study results indicate that food effect is minimal or none when fixed dose combination tablets are administered with food. In conclusion, both fixed dose combination tablets can be administered without regards to meals.

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“…[6][7][8] In the literature, no significant food effect has been reported when amlodipine and HCTZ tablets/capsules monotherapies were administered with…”

mentioning

confidence: 99%

Effect of food on the oral bioavailability of amlodipine/valsartan and amlodipine/valsartan/hydrochlorothiazide fixed dose combination tablets in healthy subjects

Sunkara

Jiang

Reynolds

et al. 2014

Clinical Pharm in Drug Dev

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“…Fats, high concentrations of bile components and pH changes [101,102] are typical triggers for increased drug-release rates. These same factors can cause negative food effects for reasons such as adsorption of food contents, a decrease in luminal diffusivity due to an increase in viscosity in the upper GI tract and changes in the absorption rate due to food-induced changes in GI motility and passage time along the GI tract [103,104].…”

Section: Effect Of Food On Drug Relelasementioning

confidence: 99%

Drug release from matrix tablets: physiological parameters and the effect of food

Nokhodchi

Asare-Addo

2014

Expert Opinion on Drug Delivery

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Introduction: As dissolution plays an important and vital role in the drug-delivery process of oral solid dosage forms, it is, therefore, essential to critically evaluate the parameters that can affect this process. Areas covered:The consumption of food as well as the physiological environment and properties of the gastrointestinal tract, such as its volume and composition of fluid, the fluid hydrodynamics, properties of the intestinal membrane, drug dose and solubility, pK a , diffusion coefficient, permeability and particle size, all affect drug dissolution and absorption rate. There are several dissolution approaches that have been developed to address the conditions as experienced in the in vivo environment, as the traditional dissolution being a quality control method is not biorelevant and as such do not always produce meaningful data. This review also describes the development of a systematic way that differentiates between robust and non-robust formulations by varying the effects of agitation and ionic strength through the use of the automated United States Pharmacopeia type III Bio-Dis apparatus. Expert opinion:With the improved understanding of the physiological parameters that can affect the oral bioperformance of dosage forms, strides have, therefore, been made in making dissolution testing methods more bio-logically based with the view of obtaining more in vitro--in vivo correlations.Keywords: agitation rate, biodissolution, drug release, effect of food, hydrophilic matrices, ionic strength Highlights -Understanding all the physiological parameters can serve as a basis for designing dissolution testing methods and systems that can more fully represent the gastrointestinal (GI) tract in humans and allow more in vitro-in vivo (IVIVC) correlations to be obtained thereby improving the oral bioperformance of dosage forms.-Simulation of GI conditions is essential to adequately predict the in vivo behaviour of drug formulations.-The choice of appropriate media for in vitro tests is crucial to their ability to correctly forecast the food effect in pharmacokinetic studies.-Several methods of dissolution testing have been conducted and are still ongoing that seek to further understand and develop media and dissolution methods to better represent the in vivo conditions and to aid in the better prediction of in vivo drug release.-Systematic change of agitation method and ionic strength evaluation may be used as additional tools in allowing for the identification of potential fed and fasted effects on drug release from hydrophilic matrices in the drive for developing dissolution methodologies that are more relevant in helping to achieve more IVIVC.

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“…18 Indeed, SD was associated with signs of sympathetic nervous system activation, including a significant increase in HR and shortening of the PR interval at baseline. 19 Other mechanisms may include changes in the pH of the upper intestinal tract, resulting in changes in the ionization of atenolol, 20 or dietary salt-induced changes in transmucosal water flux. 21 Candesartan cilexetil is an inactive racemic ester prodrug that is rapidly and completely converted to its active metabolite, candesartan, by presystemic ester hydrolysis of the ester side chain in the gastrointestinal tract.…”

Section: Pharmacokinetic Consequences Of Differences In Dietary Sodiumentioning

confidence: 99%

Effect of Contrasted Sodium Diets on the Pharmacokinetics and Pharmacodynamic Effects of Renin–Angiotensin System Blockers

Azizi

Blanchard²,

Wuerzner³

et al. 2013

Hypertension

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There is considerable between-subject variability in the hemodynamic, cardiac, and renal responses to reninangiotensin system (RAS) blockers, and the contribution of the RAS to blood pressure (BP) control and other vascular, cardiac, and renal functions varies greatly between diseases and individuals.1 Age, genetic factors, ethnicity, and dietary sodium intake, in particular, are the principal factors influencing basal RAS status, which, in turn, is one of the major determinants of the pharmacodynamic effects of RAS blockers.1 Indeed, the hemodynamic, cardiac, and nephroprotective effects of RAS blockers are enhanced by the combination of these drugs with a low-sodium diet or diuretics because of RAS activation. [1][2][3][4] A pharmacokinetic interaction with the sodium content of the diet has been reported for drugs that do not interfere with the RAS. [5][6][7] We therefore compared the effect of contrasted sodium diets on the pharmacokinetics of single oral doses of various RAS blockers administered to normotensive healthy male subjects: an angiotensin-converting enzyme inhibitor (ramipril) and 2 different angiotensin II receptor blockers (candesartan cilexetil and valsartan). We selected 2 different angiotensin II receptor blockers to investigate whether in a same class, drugs with different physicochemical properties and pharmacokinetic profiles could be affected differently by the sodium content of the diet. To further understand the effects of sodium balance on the pharmacokinetics of these cardiovascular drugs, we also evaluated the effects of dietary sodium on atenolol, a selective β1-adrenergic blocker, that is absorbed passively through the intestinal wall 8 and is excreted unchanged by the kidney after glomerular filtration.9 Thus, any change in urinary excretion of atenolol with the sodium content of the diet should directly reflect a change in the net intestinal absorption of the drug in healthy subjects with Abstract-Dietary sodium, the main determinant of the pharmacodynamic response to renin-angiotensin system blockade, influences the pharmacokinetics of various cardiovascular drugs. We compared the effect of contrasted sodium diets on the pharmacokinetics of single oral doses of 8 mg candesartan cilexetil, 160 mg valsartan, 10 mg ramipril, and 50 mg atenolol administered to 64 (16 per group) normotensive male subjects randomly assigned to sodium depletion (SD) or sodium repletion (SR) in a crossover study. Pharmacodynamic response was assessed as the increase in plasma renin concentration for renin-angiotensin system blockers and electrocardiographic changes in PR interval duration for atenolol. The area under the curve (AUC) for plasma candesartan and atenolol concentrations was significantly lower for SR than for SD (respective ratios of AUC This trial is registered at ClinicalTrials.gov with trial identifier NCT00310778

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Investigation of some factors contributing to negative food effects

Cited by 37 publications

References 38 publications

Effect of food on the oral bioavailability of amlodipine/valsartan and amlodipine/valsartan/hydrochlorothiazide fixed dose combination tablets in healthy subjects

Effect of food on the oral bioavailability of amlodipine/valsartan and amlodipine/valsartan/hydrochlorothiazide fixed dose combination tablets in healthy subjects

Drug release from matrix tablets: physiological parameters and the effect of food

Effect of Contrasted Sodium Diets on the Pharmacokinetics and Pharmacodynamic Effects of Renin–Angiotensin System Blockers

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