类胡萝卜素的生物利用率

本文论述了作为维生素A前体的类胡萝卜素在体内的吸收代谢过程、类胡萝卜素生物利用率的定义、影响生物利用率的因素以及测定新方法。     

Total and acid-soluble fluoride content of infant cereals, beverages and biscuits from Brazil

Total fluoride (TF) and HCl 0.01 M ('gastric juice')-soluble fluoride (SF) were analysed in infant foods, beverages and calcium-rich biscuits. Samples were divided into seven categories: children cereals (A), chocolate-flavoured milk (B), soy beverages (C), filled biscuits (D), non-filled biscuits (E), wafer biscuits (F) and corn starch biscuits (G). Mean TF concentrations ± SD (amplitude, unit µg F ml^-1 or µg F g^-1) were: (A) 4.25 ± 3.04 (0.20 - 7.84, n = 6); (B) 0.34 ± 0.47 (0.05-1.27, n = 6); (C) 0.15 ± 0.07 (0.09-0.29, n = 8); (D) 8.44 ± 1.76 (7.65-10.47, n = 4); (E) 12.41 ± 1.15 (10.69-13.68, n = 4); (F) 0.35 ± 0 (0.34-0.36, n = 4) and (G) 7.77 ± 1.12 (6.86-8.68, n = 2). Five samples of cereals, one sample of chocolate-flavoured milk and 10 samples of biscuits were analysed for SF. In cereals analysed for SF, all fluoride was soluble, while for the chocolate-flavoured milk, approximately 50% of TF was soluble. Regarding the biscuits analysed for SF approximately 20% of TF was soluble. It was observed that some of the cereals and beverages, and most of the biscuits analysed, might be important contributors to total daily fluoride intake. When consumed just once per day, cereals and beverages might supply up to 25% of the maximum recommended daily fluoride intake (0.07 mg F kg^-1 body weight) for a 2-year-old child (12 kg). For the filled, non-filled and corn starch biscuits, when 3, 32 or 20 units of them, respectively, are consumed just once per day, they may supply up to 16% of the maximum recommended daily fluoride intake. However, only approximately 25% of fluoride absorption occurs from the stomach and 75% from the small intestine. Therefore, a higher fluoride bioavailability is possible.     

Bioavailability Assessment of Oral Coenzyme Q10 Formulations in Dogs

ABSTRACT

The purpose of this investigation was to compare the bioavailability of three coenzyme Q10 (CoQ10) formulations in dogs using an open, randomized, multiple-dose crossover design. The formulations included a powder-filled capsule (A, control) and two soft gelatin formulations (Q-Gel ® as the water-miscible form of CoQ10, B and Q-Nol?as the water-miscible form of ubiquinol, the reduced form of CoQ10, C). Formulations were evaluated in pairs, allowing a washout period of 14 days prior to crossing over. Blood samples were collected from each animal prior to dosing to determine the endogenous plasma CoQ10 concentrations. Serial blood samples were collected for 72 hr and plasma CoQ10 concentrations were determined by high-performance liquid chromatography. Plasma concentration–time profiles were corrected for endogenous CoQ10 concentrations. Results showed that the relative bioavailabilities of formulations B and C were approximately 3.6 and 6.2-fold higher than that of control formulation A. The AUC(µg. hr/mL)±SD, C_max(µg/mL)±SD, and T_max(hr)± SD for formulations A, B, and C were 1.695±0.06, 6.097±0.08, and 10.510±0.10; 0.096±0.035, 0.169±0.038, and 0.402±0.102; and 4.2±1.48, 4.1±1.57, and 4.5±0.58, respectively. While no significant differences were observed between T_max values of the three formulations, the AUC and C_max values for formulations B and C were significantly higher than those of the control (p<0.05). The present investigation demonstrates that soft gelatin capsules containing water-miscible CoQ10 formulations B (Q-Gel®) and C (Q-Nol?) are superior to powder-filled formulations with regard to their biopharmaceutical characteristics.     

The biological activities,chemical stability,metabolism and delivery systems of quercetin: A review

BackgroundQuercetin, one of the most well-known flavonoids, has been included in human diet for a long history. The use of quercetin has been widely associated with a great number of health benefits, including antioxidant, anti-inflammatory, antiviral and anticancer as well as the function to ease some cardiovascular diseases (i.e., heart disease, hypertension, and high blood cholesterol). However, poor water solubility, chemical instability and low bioavailability of quercetin greatly limit its applications. Utilization of delivery systems can improve its stability, efficacy and bioavailability.Scope and approachIn this review, biological activities, chemical stability, metabolism and toxicity of quercetin and different delivery systems for quercetin were discussed.Key findings and conclusionsQuercetin digested in human body (e.g., mouth, small intestine, liver, kidneys) undergoes glucuronidation, sulfation or methylation. During the food processing and storage, many factors such as heat, pH, metal ions, could affect the chemical stability (including oxidation and degradation) of quercetin. Utilization of delivery systems including lipid-based carriers, nanoparticles, inclusion complexes, micelles and conjugates-based encapsulation has the potential to improve both the stability and bioavailability and thus health benefits of quercetin. Each delivery system has its unique advantages and shortcomings, and the specific selection should be based on the application domains. Moreover, the exploration of natural food-grade ingredients as main compositions of delivery systems for quercetin might be required in the future.     

Effect of phytase treatment on iron bioavailability in faba bean (Vicia faba L.) flour

The effect of dephytinisation, using an exogenous phytase under optimal conditions (pH 5.5, 37 °C), and subsequent removal of the soaking solution after processing, on the bioavailability of iron from faba bean (Vicia faba L.) flour was studied. Soaking of the faba bean flour led to a considerable reduction in the content of iron (39%), whereas a lower reduction in iron content (10%), was obtained after additional treatment with phytase, than in the soaked faba bean flour. The digestive utilisation of iron from the raw and soaked faba bean flours by growing rats was negligible, but increased significantly as a result of phytase treatment. The low iron absorption obtained for the former two treatments, during an experimental period of 10 days, was not reflected in any of the haematological indices (red blood count, haemoglobin, haematocrit) or tissues (femur, heart, kidney) studied, with the exception of the sternum. The latter appears to be a useful indicator of iron bioavailability.     

Glycolipids improve lutein bioavailability and accumulation in eyes in mice

Intestinal carotenoid absorption is greatly affected by dietary factors. In this study, it was hypothesized that lipids with varying functional groups may influence differentially lutein bioavailability. Hence, the influence of glyco‐, phospho‐, neutral, crude (mixture of lipids) lipids, or mixed micelles (control) on the percent lutein micellarization in vitro and its postprandial plasma, liver, and eye response in mice were investigated. Results show that the percent micellarization of lutein with crude lipids and glycolipids were higher (91.4 and 45.7%) than control, while no significant difference was found between phospho‐ and neutral lipids. The mean plasma response of lutein was higher for crude‐ (6 times), glyco‐ (3 times), phospho‐ (2.7 times), and neutral (2 times) lipid than control (12.4 ± 1.18 nmol/mL 8 h^?1) group. Lutein levels (pmol/g) in liver were higher in crude (7.4 ± 1) and phospho‐ (3.6 ± 0.8) lipid groups while in eyes it was higher in glyco‐ (54.0) and neutral (21.2) lipid groups than control. The influential effect of glyco‐ and phospholipids may be due to smaller micellar size (glyco‐upto 3.43 µm, phospho‐ upto 5.78 µm) than the neutral lipids (upto 66 µm). Ingestion of lutein with glycolipid or phospholipids may improve lutein bioavailability. Practical applications: The findings of the present study will be useful in nutritional and biomedical applications for feeding lutein with specific lipid combinations to achieve enhanced lutein absorption. Specifically, feeding diet/emulsion with lutein and glyco‐ and phospholipid combination may reduce the risk of macular degeneration, owing to the influential effect of these lipids on intestinal absorption of lutein.     

Preparation and Characterization of Taxifolin Form II by Antisolvent Recrystallization

To improve the aqueous solubility and dissolution rate of taxifolin, taxifolin form II was successfully prepared through antisolvent recrystallization, in which 1‐butyl‐3‐methylimidazolium tetrafluoroborate and dichloromethane were used as solvent and antisolvent, respectively. The properties of taxifolin form II were characterized by scanning electron microscopy, Fourier transform infrared spectroscopy, X‐ray diffraction, differential scanning calorimetry, solid‐state NMR spectroscopy, the dissolving capability test, and the bioavailability test. The chemical structure of taxifolin form II was not changed, but its morphology and crystalline structure changed during the recrystallization process. Moreover, taxifolin form II showed higher solubility, faster dissolution rate, and better bioavailability than taxifolin form I.     

Novel aspects of wet milling for the production of microsuspensions and nanosuspensions of poorly water-soluble drugs

Micronization and nanoparticle production of poorly water-soluble drugs was investigated using single wet milling equipment operating in the attritor and stirred media modes. The drug particles in the median size range of 0.2–2?µm were prepared by changing the milling mode and operating conditions of a Micros mill with a purpose of elucidating the dynamics of the wet milling process. It was determined that particle breakage due to mechanical stresses and aggregation due to insufficient stabilization are two competing mechanisms which together control the wet milling dynamics of the poorly water-soluble drugs. The study in the attritor mode using four different classes of stabilizers with six drugs indicated that steric stabilization worked better than electrostatic stabilization for the drugs studied. In addition, the existence of different minimum polymer concentrations for the stabilization of microsuspensions and nanosuspensions was indicated. The major role of a non-ionic polymer during the production of fine particles is its stabilization action through steric effects, and no experimental evidence was found to support the so-called Rehbinder effect. Periodic addition of the polymer as opposed to the addition of the polymer at the start of milling process was introduced as a novel processing method. This novel method of polymer addition provided effective stabilization and breakage of drug particles leading to a narrower and finer particle size distribution. Alternatively, it may allow shorter processing time and lower overall power consumption of the milling process for a desired particle size.     

Nanoemulsion-based delivery systems for poorly water-soluble bioactive compounds: Influence of formulation parameters on Polymethoxyflavone crystallization

Polymethoxyflavones (PMFs) extracted from citrus peel exhibit potent anti-cancer activity, but are highly hydrophobic molecules with poor solubility in both water and oil at ambient and body temperature, which limits their bioavailability. The possibility of encapsulating PMFs within nanoemulsion-based delivery systems to facilitate their application in nutraceutical and pharmaceutical products was investigated. The influence of oil type (corn oil, MCT, orange oil), emulsifier type (β-lactoglobulin, lyso-lecithin, Tween, and DTAB), and neutral cosolvents (glycerol and ethanol) on the formation and stability of PMF-loaded nanoemulsions was examined. Nanoemulsions (r < 100 nm) could be formed using high pressure homogenization for all emulsifier types, except DTAB. Lipid droplet charge could be altered from highly cationic (DTAB), to near neutral (Tween), to highly anionic (β-lactoglobulin, lyso-lecithin) by varying emulsifier type. PMF crystals formed in all nanoemulsions after preparation, which had a tendency to sediment during storage. The size, morphology, and aggregation of PMF crystals depended on preparation method, emulsifier type, oil type, and cosolvent addition. These results have important implications for the development of delivery systems for bioactive components that have poor oil and water solubility at application temperatures.     

A novel application of electrospinning technique in sublingual membrane: characterization,permeation and in vivo study

Isosorbide dinitrate–polyvinylpyrrolidone (ISDN–PVP) electrospinning fibers were formulated and explored as potentially sublingual membrane. The addition of polyethylene glycol (PEG) to the formulation improved flexibility and reduced fluffiness of the fiber mat. The scanning electron microscopy (SEM) demonstrated that the fibers tended to be cross-linking, and the crosslinking degree increased with the increase of PEG amount. The differential scanning calorimetry (DSC) indicated that ISDN existed in non-crystalline state in the fibers (except at the highest drug content). The infrared spectroscopy suggested that ISDN had better compatibility with the ingredients owing to the hydrogen bonding (or hydrophobic interactions). The fibers were highly favorable for the fabrication of sublingual membrane due to neutral pH, large folding endurance and rapid drug release (complete dissolution within 120 s). The permeation study of ISDN through both dialysis membrane (DM) and porcine sublingual mucosa (SM) were carried out. A significant relationship of drug permeation rate through DM and SM was built up, which indicated that DM could be used to partly simulate SM and assess formulation. The pharmacokinetic study in rats demonstrated that the electrospinning fiber membrane had a higher C_max and lower T_max compared to the reference preparation, and the relative bioavailability of the fiber membrane was 151.6%.