Proceedings: Designing formulated foods for the cardiac-concerned.
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Coronary Disease↗
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The sports drink as a functional food: formulations for successful performance.
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Beverages↗
[Food allergy: effect of proteins-lipids and proteins-polysaccharides interactions].
The most widely used ingredients in food formulation are proteins, lipids and polysaccharides. Proteins-lipids and proteins-polysaccharides interactions play a key role in the structure, stability, sensorial and nutritional properties of formulated foods. The objective of the present study is to highlight the importance of proteins-lipids and proteins-polysaccharides interactions, on the immuno-reactivity of allergenic proteins. Two models have been studied, on the one hand refined and not refined oils (soya and sunflower) and soya lecithin, on the other hand mixtures based on peanut proteins and polysaccharides (arabic gum, pectin, xylan). STUDY OF OILS: We have extracted proteins, using a PBS buffer, from refined and not refined oils from soya, sunflower and from soya lecithin, determined protein concentrations and identified allergenic proteins using SDS-PAGE electrophoresis and immuno-blotting. Phospholipids are determined by atomic absorption spectrometry. The protein determination and SDS-PAGE show the presence of a higher amount of proteins in not refined oils and lecithin as compared to refined oils. An important amount of proteins associated to phospholipids are eliminated by degumming on the form of lecithin. On the other hand, residual proteins from refined oils are accompanied by phospholipids. Immuno-blots reveal the presence of a 56 kDa allergen in oils issued from soya seeds and soya lecithin, and the presence of a 67 kDa allergen in oils issued from sunflower seeds. We conclude that the presence or elimination of proteins, especially allergens from oils is linked to amphiphilic association to phospholipids. STUDY OF PEANUT PROTEINS-POLYSACCHARIDES MIXTURES: We have digested in vitro proteins in a dialysis bag using a multi-enzymatic method and characterized proteins and peptides using SDS-PAGE electrophoresis and immuno-blotting. Our results confirm that peanut proteins alone are digested by proteases and that a number of large peptides still have epitopes recognized by anti-peanut proteins antibodies. Our results also show that the presence of polysaccharides changes the peptidic profile after digestion and that, depending on the polysaccharide type, smaller or larger peptides can be obtained in the dialysis bag. Smaller peptides are obtained using pectin whereas larger peptides are obtained using arabic gum and xylan. In the latter case, an increasing amount of peptides reacts to antibodies. Our first observations clearly show the need to better understand modifications of proteins allergenicity induced by the presence of other ingredients such as polysaccharides and lipids, in relation to technological treatments.
Allergens↗
[Authorization request for the use of L-carnitine, calcium chloride and magnesium sulfate as nutritional additives in the formulation of food designed for specialized diets].
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Calcium Chloride↗
The utilization of local foods in the formulation of weaning foods.
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Amino Acids↗
Nutritional quality, functional properties and anti-nutrient compositions of the larva of Cirina forda (Westwood) (Lepidoptera: Saturniidae).
Determination of the proximate, nutritionally valuable minerals and anti-nutrient compositions in larvae of Cirina forda (W) showed that they contained high levels of protein, (55.50%+/-1.20%) with ash, moisture, fat, and carbohydrate levels being (10.26%+/-0.01%), (10.85%+/-0.38%), (4.68%+/-0.01%) and (18.70%+/-0.84%) respectively. Fibre was not detected. Protein solubility was higher in alkaline media than in acidic media while the isoelectric points were pH 4, 6 and 9 indicating that C. forda may be useful in food formulations involving foods like meat products. Phosphorus had the highest value of (215.54+/-0.21) mg/100 g while manganese had the lowest value of (1.14+/-0.10) mg/100 g. Copper, Co, Pb, Cr and Ni were not available. Water absorption capacity was (300%+/-0.15%), oil absorption capacity was (358.44%+/-0.21%) and foaming stability was (3%+/-0.00%). The results of anti-nutritional analysis revealed that oxalate and phytic acid contents were (4.11+/-0.05) mg/100 g and (1.02+/-0.00) mg/100 g respectively and that these values fell within nutritionally accepted values. Tannin was not detected in C. forda. C. forda, a rich source of animal nutrients, usable in human diets and animal feeds formulations.
Animals↗
Lysinoalanine content of formulas for enteral nutrition.
Casein and caseinates are the main ingredients of formulas for enteral nutrition. Their manufacturing procedure and the thermal treatments necessary to assure microbiological stabilization and satisfactory shelf-life of the end-products are particularly favorable for the formation of lysinoalanine (LAL), a cross-linked amino acid that is considered a useful marker of the thermal damage and reduced digestibility of proteins. The lysinoalanine content of 18 different kinds of formulas for enteral nutrition was determined by HPLC after derivatization. The liquid formulas have an average value of 528 microg/g protein LAL, ranging from 160 to 800 microg/g protein (average content of formulas for pediatric use 747 microg/g protein). These values are rather high considering that the average value detected in UHT-treated drinkable milk is 117 microg/g protein. In principle, the preparation of caseinates and the thermal stabilization of the end products are the two steps more favorable for the formation of LAL. The fact that the five samples stabilized by an UHT-treatment have an average value of 512 microg/g protein suggests that the LAL content depends more on the quality of the starting ingredients than on the sterilization process. A better selection of the starting ingredients should improve the quality of formulas for enteral nutrition, which is very desirable when formulating foods for consumers with very high nutritional demands.
Caseins↗
A predictive model for exemestane pharmacokinetics/pharmacodynamics incorporating the effect of food and formulation.
AIMS: Exemestane (Aromasin) is an irreversible aromatase inactivator used for the treatment of postmenopausal women with advanced breast cancer. The objective of this study was to evaluate the effect of formulation comparing a sugar-coated tablet (SCT) with a suspension and food on the pharmacokinetics (PK) and pharmacodynamics (PD) with respect to plasma estrone sulphate (E1S) concentrations of exemestane, using a PK/PD approach. METHODS: This was an open, three-period, randomized, crossover study. Twelve healthy postmenopausal women received single oral doses of 25 mg exemestane as a SCT after fasting or food and as a suspension after fasting. Exemestane and E1S concentrations were determined before and up to 14 days after drug administration. Population analysis was performed in two steps: (i) a compartmental PK model was selected incorporating the effect of food and formulation; (ii) conditional on the PK model, a PD model was developed employing indirect response models. Model selection was performed using standard statistical tests. Validation and assessment of the predictive capability of the selected model was performed using real test data sets obtained from the literature. RESULTS: A three-compartment model with first-order elimination rate best described exemestane disposition (k12 0.454, k21 0.158, k13 0.174, k31 0.016 and k 0.738 h(-1)). Absorption was described by a mono-exponential function [ka 2.3 (SCT after fasting), 1.1 (SCT after food) and 7.6 h(-1) (suspension); lag time 0.2 h]. The PD model assumed that E1S plasma concentrations are determined by a zero-order synthesis rate (6.5 pg ml(-1) h(-1)) and a first-order elimination constant (0.032 h(-1)). Exemestane inhibited E1S synthesis with a C50 value of 22.1 pg ml(-1). The mean population estimates were used to simulate the administration of different doses of the drug (0.5, 1, 2.5, 5 and 25 mg day(-1)). The model predictions were in agreement with historical data. CONCLUSIONS: Exemestane absorption is influenced by the formulation of the drug and by food, but its disposition is independent of both. PK differences do no translate into clinically important differences in the PD. The PK/PD model developed was able to predict successfully the response to different doses and administration schedules with respect to oestrogen suppression.
Administration, Oral↗
How far shall we go in the enrichment, fortification, and formulation of new foods?
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American Medical Association↗
Effects of food and formulation on the relative bioavailability of bismuth biskalcitrate, metronidazole, and tetracycline given for Helicobacter pylori eradication.
AIMS: To evaluate the effects of food and formulation on the pharmacokinetics of bismuth biskalcitrate, metronidazole and tetracycline when combined in a new 3-in-1 single capsule (BMT) for eradication of Helicobacter pylori. METHODS: In a randomized, 3 x 3 cross-over design, 23 healthy males received one dose of BMT in the fed and fasting states and equivalent doses of the three drugs given together but as separate capsules while fasting. Bioequivalence was evaluated according to 90% confidence intervals (CIs) of ratios of geometric least square means for C(max), AUC(t), and AUC(infinity). RESULTS: With respect to food, none of the three drugs met bioequivalence guidelines. Bismuth had lower limit CIs ranging from 12% for C(max) to 25% for AUC(infinity). The corresponding values for tetracycline were 59% and 51%. Metronidazole had a lower limit CI of 74% for C(max). With respect to formulation, bismuth had lower limits of CIs ranging from 39% for C(max) to 50% for AUC(t) and higher limits of 146% for AUC(t), metronidazole met bioequivalence guidelines, and tetracycline had lower limits of CIs between 72% for AUC(t) and 74% for AUC(infinity). CONCLUSIONS: Food significantly decreased the relative bioavailability of each drug but formulation was without effect. This decrease may be beneficial when a local gastric action is needed, as confirmed by a near 90% eradication rate when this combined capsule is administered with food to treat gastro-duodenal local infection by H. pylori.
Administration, Oral↗
Formulation-dependent food effects demonstrated for nifedipine modified-release preparations marketed in the European Union.
The objective of this study was a comparative investigation of the influence of concomitant food intake on the bioavailability of two nifedipine-containing controlled-release formulations. Adalat OROS and CORAL were compared in a randomised, non-blind, four-way crossover design in 24 healthy, male subjects after single dose administration following a high fat American breakfast or an overnight fast of 12 h, respectively. Plasma samples were withdrawn until 48 h post-dose. In the fasted state, the bioavailability (AUC and C(max) values) was lower for CORAL than for Adalat OROS. Under fed conditions, differences in bioavailability between both products were markedly increased. With respect to the therapeutic use of both products, the most important finding was the significant dose-dumping effect observed after fed administration of CORAL, resulting in nifedipine plasma concentrations of nearly three- to four-fold in 11 of 24 volunteers. The mean ratio of C(max) was 235% comparing CORAL with Adalat OROS under these conditions. The formulation-dependent food interaction observed in this study may be therapeutically relevant, especially in the case of changing administration conditions or switching from one product to the other.
Adult↗
Determination of L-carnitine in food supplement formulations using ion-pair chromatography with indirect conductimetric detection.
A novel method for the determination of L-carnitine in food supplement formulations was developed and validated, using ion-pair chromatography with indirect conductimetric detection. The chromatographic method was based on a non-polar (C18) column and an aqueous octanesulfonate (0.64 mM) eluent, acidified with trifluoroacetic acid (5.2 mM). The retention time was 5.4 min and the asymmetry factor 0.65. A linear calibration curve from 10 to 1000 microg/ml (r= 0.99998), with a detection limit of 2.7 microg/ml (25 microl injection volume), a repeatability %RSD of 0.8 (40 microg/ml, n = 5) and reproducibility %RSD of 2.6 were achieved. The proposed method was applied for the determination of carnitine in oral solutions and capsules. No interference from excipients was found and the only pretreatment step required was the appropriate dilution with the mobile phase. Recovery from spiked samples was ranged from 97.7 to 99.7% with a precision (%RSD, n = 3) of 0.01-2.1%.
Carnitine↗
Phytosterols and human lipid metabolism: efficacy, safety, and novel foods.
Plant sterols have been known for several decades to cause reductions in plasma cholesterol concentrations. These plant materials have been granted a conditional health claim in the United States regarding their effects in the prevention of cardiovascular disease and are being sold in functional foods in several countries in Europe as well as in the United States and Australia. It is generally suggested that daily consumption of approximately 2 g of plant sterols can lower cholesterol concentrations as part of a dietary prevention strategy. However, phytosterols have been added and tested for their cholesterol-lowering effects mainly in spreads. Consumption of these high-fat foods seemingly flies in the face of current recommendations for the promotion of heart health, which suggest lowering total fat and energy intake to maintain weight. Hence, new food formulations are being evaluated using phytosterols incorporated into low-fat and reduced-fat food items. The purpose of this review is to examine the cholesterol-lowering efficacy of plant sterols, focusing on novel food applications, their mechanism of action, and safety. These novel food formulations include new solubilization processes that lead to improved uses for plant sterols, as well as new foods into which phytosterols have been incorporated, such as breads, cereals, and beef. Such new foods and formulations should pave the way for greater use of phytosterols in heart health promotion, increasing the longer-term potential for the creation of innovative functional foods containing plant sterols and their derivatives.
Animals↗
A food-based formulation provides lycopene with the same bioavailability to humans as that from tomato paste.
Lycopene from fresh and unprocessed tomatoes is poorly absorbed by humans. Absorption of lycopene is higher from processed foods such as tomato paste and tomato juice heated in oil. The aim of the present study was to develop a food-grade lycopene formulation that is bioavailable in humans. A formulation of lycopene named "lactolycopene" has been designed in which lycopene is entrapped with whey proteins. Healthy subjects (n = 33; 13 men and 20 women) participated and were allocated randomly to one of the three treatment groups. After a 3-wk deprivation of dietary lycopene, subjects ingested 25 mg lycopene/d for 8 wk from lactolycopene, tomato paste (positive control) or a placebo of whey proteins while consuming their self-selected diets. Plasma lycopene concentrations reached a maximum after 2 wk of supplementation in both lycopene-treated groups and then a plateau was maintained until the end of the treatment. Increases in plasma lycopene at wk 8 were not different between supplemented groups (mean +/- SEM): 0.58 +/- 0.13 micromol/L with lactolycopene and 0.47 plus minus 0.07 micromol/L with tomato paste, although they were different from the control (P < 0.001). Similar time-concentration curves of lycopene incorporation were observed in buccal mucosa cells. Although lycopene was present mainly as all-trans isomers (>90%) in both lycopene supplements, plasma lycopene enrichment consisted of 40% as all-trans and 60% as cis isomers. The precursor of lycopene, phytofluene, was better absorbed than lycopene itself. The lactolycopene formulation and tomato paste exhibited similar lycopene bioavailability in plasma and buccal mucosa cells in humans.
Adult↗
Effects of formulation and food on the absorption of hydrochlorothiazide and triamterene or amiloride from combination diuretic products.
The absorption of three combination formulations of hydrochlorothiazide and either triamterene or amiloride was studied over a 5-year period in seven separate investigations under varying conditions of food and fasting. The most widely prescribed combination, containing 25 mg of hydrochlorothiazide and 50 mg of triamterene, demonstrated impaired absorption in the fasting state that was partially corrected by the addition of a breakfast high in fat. The increase in the fat content of the food appeared to correlate directly with the amount of both drugs absorbed from this formulation. The second formulation studied, a new combination formulation of 50 mg of hydrochlorothiazide and 75 mg of triamterene, demonstrated acceptable absorption in the fasting state that was not altered by the concurrent administration of a high-fat breakfast. The absorption of the third formulation, a combination of 50 mg hydrochlorothiazide and 5 mg amiloride, was acceptable in the fasting state and demonstrated a slight reduction in the absorption of the amiloride component when administered concurrently with a high-fat meal. The clinical and biopharmaceutic implications of these observations are discussed.
Amiloride↗
Analysis of formulation and food effect on the absorption of metoclopramide.
OBJECTIVES: Assessment of the relative and absolute bioavailability of immediate release and sustained release formulations of metoclopramide. Assessment of the effect of a high-fat meal on the pharmacokinetics of sustained release metoclopramide. MATERIAL AND METHODS: In a balanced 4-way crossover study in 16 healthy male volunteers, a sustained release (SR) formulation of metoclopramide was compared with a solution for injection (A) and an immediate release tablet (B). The SR formulation was administered after a fasting period (C) as well as after a high-fat meal (D). A single dose of 30 mg metoclopramide was investigated in each treatment. Metoclopramide concentrations were determined by HPLC. RESULTS: The absolute bioavailability of the sustained release formulation (fasting state) was 58% and thus about 17% lower than the bioavailability of the immediate release formulation. Comparing the treatments C (sustained release, fasting state) and D (sustained release, high-fat meal) no significant influence of food on the absorption of sustained release metoclopramide could be detected.
Absorption↗
Optimizing the diet with whole grains.
Dietary recommendations may be perceived by the general population as causing a shift to less food and perhaps to less aesthetically pleasing foods often resulting in noncompliance. Technology can play a key role in this scenario by creating new formulated foods as well as by utilizing technology to modify whole foods or foods containing whole foods and enhancing both their health benefits and acceptability. At present we have evidence for a positive role in health of nutrients and many nonnutrients in foods, such as whole grains. However, all the linkages between dietary components and disease are not clear. Therefore, it is critical to design not only appealing formulated foods, but to also ensure adequate consumption of whole foods in order to obtain those compounds we know to be linked to good health, as well as those yet-unknown compounds or interactions in food that are also linked to good health. In all cases, the technical and functional properties of food, as well as the nutritional, must be considered in order to optimize acceptability and assist in achieving compliance in meeting dietary recommendations.
Aged↗
Formulation and food deprivation affects 2,4-D neurobehavioral toxicity in rats.
The herbicide 2,4-Dichlorophenoxyacetic acid (2,4-D) is a commonly used herbicide and one component of Agent Orange. The herbicide is commonly formulated as the butyl ester. The effects of a 50:50 mixture of n-butyl and iso-butyl esters of 2,4-D (2,4-D mixed butyl esters, 150-175 mg/kg/day SC) on photocell locomotor activity and landing foot splay were assessed in rats. Similarly the effects of 2,4-D mixed butyl esters and pure 2,4-D-n-butyl ester (150 mg/kg/day SC) on photocell locomotor activity were assessed in both food deprived and free feeding rats. In general, food deprivation tended to decrease the sensitivity of rats to the effects of either formulation. The spectrum of neurobehavioral effects varied with the ester isomers. Both 2,4-D-n-butyl ester and 2,4-D mixed butyl esters depressed photocell locomotor activity. 2,4-D mixed butyl esters failed to increase landing foot splay as reported for 2,4-D-n-butyl ester. The extent of ester hydrolysis was similar when comparable concentrations of 2,4-D acid were measured in blood and brain four hours following either formulation. 2,4-D-n-butyl ester caused significantly more activity depression than 2,4-D mixed butyl esters. Additionally, tolerance developed more rapidly for animals receiving 2,4-D mixed butyl esters than for animals receiving 2,4-D-n-butyl ester. These studies exemplify the importance of herbicide formulation and subject nutritional status in the expression of neurobehavioral toxicity.
2,4-Dichlorophenoxyacetic Acid↗