Relative absorption of silicon from different formulations of dietary supplements: a pilot randomized, double-blind, crossover post-prandial study.

The purpose of the present study was to compare the relative absorption of a new powder presentation of silicon (Si) as orthosilicic acid with maltodextrin (Orgono Powder) compared to usual Si liquid presentations as orthosilicic acid with Equisetum arvense and Rosmarinus officinalis (G5 Siliplant) and orthosilicic acid with aloe vera (G7 Aloe). All dietary supplements were administered at the same Si oral dose (21.6 mg) in a randomized, double-blind, crossover post-prandial study conducted in 5 healthy men. Urine was collected at baseline and over the 6-h post-dose period in 2 separate 3-h collections for the analysis of Si concentration, which was conducted by inductively coupled plasma optical emission spectrometry as the gold standard method. No significant differences in total urinary Si excretion were found after the intake of these 3 dietary supplements; 34.6%, 32.4% and 27.2% of the ingested Si from G7 Aloe, G5 Siliplant and Orgono Powder, respectively, was excreted in urine over the 6-h follow-up period. The 3 different oral Si formulations tested, in powder and liquid presentations, provide highly bioavailable Si and present an equivalent relative absorption in healthy humans.

In vitro evaluation of different organic matrices used to modulate silicon bioavailability.

Silicon (Si) has numerous health properties. It is an element of the extracellular matrix; it is involved in collagen synthesis, bone mineralization, and immune system modulation; and it reduces metal accumulation in Alzheimer's disease and the risk of atherosclerosis. Given its poor intestinal absorption, Si is ingested in the form of orthosilicic acid (OSA) to promote its bioavailability. The aim of this work was to compare different commercial dietary supplements containing stabilized OSA to ascertain their bioaccessibility, bioavailability, and safety in a model of human intestinal epithelium. Biocompatibility with the glycocalyx was also investigated. Supplements containing collagen, maltodextrins, and choline as OSA stabilizers were analyzed. Bioaccessibility was explored by means of an in vitro digestive process. Bioavailability was investigated using a Caco2 cell line alone, or co-culturing with a HT29-MTX cell line. The safety of the compounds tested (in terms of intestinal epithelium integrity) was judged on the grounds of MTS assay, transepithelial electrical resistance, and apparent permeability. The three formulations were also tested in a Caco2 cell model of intestinal glycocalyx Si retention. The choline-formulated OSA formulation outperformed the maltodextrin-stabilized supplement, with a Si bioavailability about 14 times higher (P < .05). The choline-formulated OSA formulation increased cell permeability, with consequent intestinal epithelium disruption. The supplements' absorption and bioavailability (and harmfulness) differed considerably, depending on the OSA stabilizer involved. Of the three formulations tested, the collagen-formulated OSA represents the best Si dietary supplement.

In vitro investigation of intestinal transport mechanism of silicon, supplied as orthosilicic acid-vanillin complex.

SCOPE: Silicon (Si) is one of the most abundant trace elements in the body. Although pharmacokinetics data described its absorption from the diet and its body excretion, the mechanisms involved in the uptake and transport of Si across the gut wall have not been established. METHODS AND RESULTS: Caco-2 cells were used as a well-accepted in vitro model of the human intestinal epithelium to investigate the transport, across the intestinal barrier in both the absorption and excretion directions, of Si supplied as orthosilicic acid stabilized by vanillin complex (OSA-VC). The transport of this species was found proportional to the initial concentration and to the duration of incubation, with absorption and excretion mean rates similar to those of Lucifer yellow, a marker of paracellular diffusion, and increasing in the presence of EGTA, a chelator of divalents cations including calcium. A cellular accumulation of Si, polarized from the apical side of cells, was furthermore detected. CONCLUSION: These results provide evidence that Si, ingested as a food supplement containing OSA-VC, crosses the intestinal mucosa by passive diffusion via the paracellular pathway through the intercellular tight junctions and accumulates intracellularly, probably by an uptake mechanism of facilitated diffusion. This study can help to further understand the kinetic of absorption of Si.

Use of silicon for skin and hair care: an approach of chemical forms available and efficacy.

Silicon is the second most abundant element on Earth, and the third most abundant trace element in human body. It is present in water, plant and animal sources. On the skin, it is suggested that silicon is important for optimal collagen synthesis and activation of hydroxylating enzymes, improving skin strength and elasticity. Regarding hair benefits, it was suggested that a higher silicon content in the hair results in a lower rate of hair loss and increased brightness. For these beneficial effects, there is growing interest in scientific studies evaluating the efficacy and safety of using dietary supplements containing silicon. Its use aims at increasing blood levels of this element and improving the skin and its annexes appearance. There are different forms of silicon supplements available and the most important consideration to be made in order to select the best option is related to safety and bioavailability. Silicon supplements are widely used, though there is wide variation in silicon bioavailability, ranging from values below 1% up to values close to 50%, depending on the chemical form. Therefore, the aim of this study was to evaluate the scientific literature related to the different chemical forms of silicon supplements available and the limitations and recent progress in this field. According to reported studies, among the different chemical forms available, the orthosilicic acid (OSA) presents the higher bioavailability, whereas the others forms have absorption inversely proportional to the degree of polymerization. However, clinical studies evaluating safety and efficacy are still lacking.

Use of silicon for skin and hair care: an approach of chemical forms available and efficacy

Abstract Silicon is the second most abundant element on Earth, and the third most abundant trace element in human body. It is present in water, plant and animal sources. On the skin, it is suggested that silicon is important for optimal collagen synthesis and activation of hydroxylating enzymes, improving skin strength and elasticity. Regarding hair benefits, it was suggested that a higher silicon content in the hair results in a lower rate of hair loss and increased brightness. For these beneficial effects, there is growing interest in scientific studies evaluating the efficacy and safety of using dietary supplements containing silicon. Its use aims at increasing blood levels of this element and improving the skin and its annexes appearance. There are different forms of silicon supplements available and the most important consideration to be made in order to select the best option is related to safety and bioavailability. Silicon supplements are widely used, though there is wide variation in silicon bioavailability, ranging from values below 1% up to values close to 50%, depending on the chemical form. Therefore, the aim of this study was to evaluate the scientific literature related to the different chemical forms of silicon supplements available and the limitations and recent progress in this field. According to reported studies, among the different chemical forms available, the orthosilicic acid (OSA) presents the higher bioavailability, whereas the others forms have absorption inversely proportional to the degree of polymerization. However, clinical studies evaluating safety and efficacy are still lacking.

The fractional urinary fluoride excretion of adults consuming naturally and artificially fluoridated water and the influence of water hardness: a randomized trial.

AIMS: To assess whether there was any significant difference in the average fractional urinary fluoride excretion (FUFE) values among adults consuming (NaF) fluoridated Ca-free water (reference water), naturally fluoridated hard water and an artificially (H2SiF6) fluoridated soft water. DESIGN: Sixty adult females (N=20 for each treatment) participated in this randomized, double-blind trial. The experimental design of this study provided an indirect estimation of the fluoride absorption in different types of water through the assessment of the fractional urinary fluoride excretion of volunteers. RESULTS: Average daily FUFE values (daily amount of fluoride excreted in urine/daily total fluoride intake) were not significantly different between the three treatments (Kruskal-Wallis; p = 0.62). The average 24-hour FUFE value (n=60) was 0.69; 95% C.I. 0.65-0.73. CONCLUSIONS: The results of this study suggest that the absorption of fluoride is not affected by water hardness.

Pharmacokinetics of ingested fluoride: lack of effect of chemical compound.

UNLABELLED: Fluoride in drinking water may be present from natural sources or added as sodium fluoride (NaF), sodium silicofluoride (Na(2)SiF(6)) or fluorosilicic acid (H(2)SiF(6)). Results from an early study with rats suggested that, when ingested as Na(2)SiF(6), the absorption and excretion of fluoride were greater than when ingested as NaF. OBJECTIVE: The present single-blind, crossover study with 10 adults was done to determine three key pharmacokinetic parameters: the maximum plasma fluoride concentrations (C(max)), the elapsed time to reach the maximum concentrations (T(max)) and the 6-h areas under the time-plasma concentration curves (AUCs) after ingestion of 500 mL of water containing 0.67 or 5.45 mg F/L present naturally or added as NaF or H(2)SiF(6). DESIGN: Blood was collected prior to and at nine time points during 6h after ingestion of the test solutions. Plasma was analysed by electrode after HMDS-facilitated diffusion and the data were analysed for statistically significant differences using repeated measures ANOVA. RESULTS: The C(max), T(max) and AUC values after ingestion of the solutions containing natural fluoride, NaF or H(2)SiF(6) did not differ significantly at either dose level. Further, the T(max) values associated with the 0.67 and 5.45 mg/L solutions did not differ significantly indicating that the absorption, distribution and elimination rates were not affected by the dose size. CONCLUSIONS: Considered together with published reports, the present findings support the conclusion that the major features of fluoride metabolism are not affected differently by the chemical compounds commonly used to fluoridate water nor are they affected by whether the fluoride is present naturally or added artificially.

Effect of oral intake of choline-stabilized orthosilicic acid on hair tensile strength and morphology in women with fine hair.

The appearance of hair plays an important role in people's overall physical appearance and self-perception. Silicon (Si) has been suggested to have a role in the formation of connective tissue and is present at 1-10 ppm in hair. Choline-stabilized orthosilicic acid ("ch-OSA") is a bioavailable form of silicon which was found to improve skin microrelief and skin mechanical properties in women with photoaged skin. The effect of ch-OSA on hair was investigated in a randomized, double blind, placebo-controlled study. Forty-eight women with fine hair were given 10 mg Si/day in the form of ch-OSA beadlets (n = 24) or a placebo (n = 24), orally for 9 months. Hair morphology and tensile properties were evaluated before and after treatment. Urinary silicon concentration increased significantly in the ch-OSA supplemented group but not in the placebo group. The elastic gradient decreased in both groups but the change was significantly smaller in the ch-OSA group (-4.52%) compared to placebo group (-11.9%). Break load changed significantly in the placebo group (-10.8%) but not in the ch-OSA supplemented group (-2.20%). Break stress and elastic modulus decreased in both groups but the change was smaller in the ch-OSA group. The cross sectional area increased significantly after 9 months compared to baseline in ch-OSA supplemented subjects but not in the placebo group. The change in urinary silicon excretion was significantly correlated with the change in cross sectional area. Oral intake of ch-OSA had a positive effect on tensile strength including elasticity and break load and resulted in thicker hair.

[Enamel fluoride uptake following fluoride application and fluoride precipitation]. / Schmelz-fluoridaufnahme nach Fluoridierung und Fluoridfällung.

This study is on fluoride uptake into enamel following fluoride precipitation with calcium hydroxide. Five specimens each from 12 bovine incisors were polished, covered with a salivary pellicle, and distributed into five groups (n=12). A fluoride solution (43,500 ppm F from magnesiumfluorosilicate, copper-(II)-fluorosilicate and sodium-fluoride, pH 2; Tiefenfluorid Touchierlösung, Humanchemie) and Ca(OH)2-solution (Tiefenfluorid Nachtouchierlösung) were applied subsequently in group TN. "Touchierlosung" only was used in group T, sodium-fluoride (43,500 ppm F, pH 2) in group NaF, and aminefluoride (Elmex fluid, 10,000 ppm F, pH 4) in group EF. No fluoride was used in group NK (negative control). Following rinsing and 24 h storage in artificial saliva surface KOH-soluble fluoride content (KOHF), and structurally bound fluoride content (SBF) from three layers (0-33, 33-66 and 66-99 pm) was determined by fluoride electrode procedures. KOHF (median in microg/cm2) of NK was below the lower limit of quantification of the fluoride electrode. The other group values were significantly higher (Mann-Whitney test, p < or = 0.05). TN (1.6), T (1.4) and NaF (1.1) did not differ significantly. EF (0.6) was significantly smaller than TN and T but not smaller than NaF. SBF (0-33, 33-66, 66-99 pm; median in microg/cm3) of TN (445, 341, 275), T (644, 481, 360), NaF (804, 480, 307) and EF (449, 346, 280) did not differ significantly but, with the exception of TN, were significantly higher as compared to NK. A precipitation reaction with Ca(OH)2 following fluoridation did not increase enamel fluoride uptake.

Identification of the silicon form in xylem sap of rice (Oryza sativa L.).

Rice (Oryza sativa L.) is a typical silicon (Si)-accumulating plant, but the mechanism responsible for the translocation from the root to the shoot is poorly understood. In this study, the form of Si in xylem sap was identified by (29)Si-nuclear magnetic resonance (NMR) spectroscopy. In rice (cv. Oochikara) cultured in a monosilicic acid solution containing 0.5 mM Si, the Si concentration in the xylem reached 6 mM within 30 min. In the (29)Si-NMR spectra of the xylem sap, only one signal was observed at a chemical shift of -72.6 ppm, which is consistent with that of monosilicic acid. A (1)H-NMR study of xylem sap did not show any significant difference between the wild-type rice and mutant rice defective in Si uptake, and the components of the xylem sap were not affected by the Si supply. The Si concentration in the xylem sap in vitro decreased from an initial 18 mM to 2.6 mM with time. Addition of xylem sap to a solution containing 8 mM Si did not prevent the polymerization of silicic acid. All these results indicate that Si is translocated in the form of monosilicic acid through the xylem and that the concentration of monosilicic acid is high in the xylem only transiently.

The silicon content of beer and its bioavailability in healthy volunteers.

Dietary Si, as soluble orthosilicic acid (OSA), may be important for the growth and development of bone and connective tissue. Beer appears to be a major contributor to Si intake, although the Si content of beer and its bioavailability in human subjects have not been well established. Here we investigated the Si content of different beers and then estimated Si absorption from beer in healthy volunteers. The Si content of seventy-six different beers was estimated using inductively coupled plasma optical emission spectrometry and one of the beers, used in the ingestion study, was ultrafiltered to determine OSA content. Next, following the ingestion of 0.6 litres beer (22.5 mg Si; 4.6 % (v/v) ethanol), serum and urinary Si levels were measured in nine healthy volunteers over a 6 h period. A solution of OSA was similarly investigated as a positive control and water and 4.6 % ethanol as negative controls. The mean Si level of beer was 19.2 (sd 6.6) mg/l; the median Si level was 18.0 mg/l. There was no significant difference in the Si levels of the different beers by geographical origin or type of beer. Serum and urinary Si levels increased considerably following the ingestion of beer or a solution of OSA but not with the ingestion of either 4.6 % ethanol or water. The ultrafilterability of Si from beer (about 80 %) and its absorption in volunteers (about 55 %) was comparable with that of a solution of OSA suggesting that Si in beer is present chiefly in a monomeric form and is readily bioavailable.

Silicic acid: its gastrointestinal uptake and urinary excretion in man and effects on aluminium excretion.

Silicon (Si), as silicic acid, is suggested to be the natural antidote to aluminium (Al) toxicity, and was recently shown to promote the urinary excretion of Al from body stores. The metabolism of Si in man, however, remains poorly investigated. Here we report on the pharmacokinetics and metabolism of Si in healthy volunteers following ingestion of orthosilicic acid (27-55 mg/l Si) in water. We also investigated whether orthosilicic acid promotes the urinary excretion of endogenous Al. Minimum, median uptake of Si from the ingested dose was 50.3% (range: 21.9-74.7%, n = 8) based on urinary analysis following dosing. Significant correlations were observed between creatinine clearance and Si levels in serum or urine (r = 0.95 and 0.99, respectively). Renal clearance of Si was 82-96 ml/min suggesting high renal filterability. These results suggest that orthosilicic acid is readily absorbed from the gastrointestinal tract of man and then readily excreted in urine. There was no significant increase in Al excretion, over 32 h, following ingestion of the orthosilicic acid dose (P = 0.5; n = 5).

Kinetics of uptake and elimination of silicic acid by a human subject: a novel application of 32Si and accelerator mass spectrometry.

Silicon is possibly important in human physiology in protecting against the toxic effects of aluminium, but the kinetics of uptake and excretion of silicic acid, the bioavailable form, are not well characterised. We have used 32Si as a tracer in a human uptake experiment to determine a gastrointestinal uptake factor for silicic acid, and to elucidate the kinetics of renal elimination. Urine collections were made for extending intervals from 2 to 12 h over 2 days following ingestion by a single human subject of a neutral silicic acid solution containing tracer levels of 32Si (t1/2 approximately 150 y). Silicon was isolated as SiO2 and the 32Si content determined by accelerator mass spectrometry (AMS), using a gas-filled magnet technique to eliminate a prolific isobaric interference from 32S. Silicon uptake appears to have been essentially complete within 2 h of ingestion. Elimination occurred by two simultaneous first-order processes with half-lives of 2.7 and 11.3 h, representing around 90% and 10%, respectively, of the total output. The rapidly eliminated 32Si was probably retained in the extracellular fluid volume, whilst the slower component may represent intracellular uptake and release. Elimination of absorbed 32Si was essentially complete after 48 h and was equivalent to 36% of the ingested dose. This establishes only a lower limit for gastrointestinal absorption as, although there was no evidence for longer term retention of additional 32Si, the possibility could not be excluded by these results.

Silicosis in mice: effects of dose, time, and genetic strain.

Experimental silicosis allows study of the mechanisms of lung injury, inflammation, and fibrosis. Inbred mice are an attractive species in which to study these mechanisms because of recent progress in murine immunology, molecular biology, and genetics. We exposed mice to an aerosol of silica and examined the effects of exposure dose, the evolution of disease features over time, and the variation in responses among four inbred strains. In C3H/HeN mice incremental cumulative exposure doses of cristobalite silica caused increased initial lung dust burden 12 to 16 weeks post-exposure, progressively intense pathological responses, and increased total lung collagen (hydroxyproline). The histopathological changes and total lung collagen increased progressively over time after exposure. We compared the features of silicosis in four strains of inbred mice selected for common use or immunologic reactivity 16 weeks after aerosol inhalation exposure to crystalline cristobalite silica (70 mg/m3, 5 hours/day, 12 days). C3H/HeN mice demonstrated histopathological silicotic lesions and enlarged intrapulmonary lymphoid tissue, and increased lung wet weight, bronchoalveolar lavage (BAL) recovery of macrophages, lymphocytes, and neutrophils, and total lung collagen (hydroxyproline). BALB/c mice developed slight pulmonary lesions; MRL/MpJ mice demonstrated prominent pulmonary infiltrates with lymphocytes; New Zealand Black mice developed extensive alveolar proteinaceous deposits, inflammation, and fibrosis. Our findings demonstrate orderly dose-time-response relationships, and a substantial variation of responses among inbred strains of mice. This model should prove valuable for future experimental interventions into the mechanisms of silicosis.

Effect of a two-solution fluoride mouth rinse on deposition of loosely bound fluoride on sound root tissue and remineralization of root lesions in vitro.

A constant-composition fluoride (F) titration method was used to measure the amount of leachable F deposited on root surfaces in vitro by a 1-min rinse with a 12 mmol/l sodium fluoride (228 micrograms/g F) solution or a two-solution rinse that contained 2 mmol/l sodium fluorosilicate (228 micrograms/g total F ) and 10 mmol/l calcium chloride. The mean +/- standard deviations (n = 3) F uptake from the two rinse treatments were 0.70 +/- 0.24 micrograms/cm2 and 3.25 +/- 0.74 micrograms/cm2, respectively. In a separate experiment, the effects of sodium fluoride and the two-solution rinses on remineralization of root lesions were evaluated in an in vitro pH cycling model. The results showed that the average decrease in mineral loss (delta Z) in the two-solution rinse group (60%) was significantly greater than that obtained in the NaF rinse (41%) or the control (9%) group.

An investigation into the effect of cimetidine pre-treatment on raft formation of an anti-reflux agent.

It is now becoming common practice to co-administer H2-receptor antagonists and anti-reflux agents in the treatment of reflux oesophagitis. The mechanism by which anti-reflux agents achieve flotation requires a small amount of gastric acid to be present in the stomach. This study investigated whether an anti-reflux agent would remain effective after the decrease in acid secretion produced by a typical clinical dosage regimen of cimetidine (400 mg q.d.s., 7 days). Gastric distribution and residence of a meal and an anti-reflux agent were assessed in 12 normal subjects using gamma scintigraphy. The area under the gastric and fundal emptying curves demonstrated that Liquid Gaviscon (sodium alginate compound) had a significantly greater gastric residence than the meal, both during the control period and after cimetidine pretreatment, and that the majority of the Gaviscon was located in the fundus. The distribution of Gaviscon into the fundus was not affected by cimetidine pretreatment. Cimetidine pre-treatment slightly, but not significantly, increased the time for half the meal and the Gaviscon to empty from the stomach. The results suggest that the mechanism of action of Liquid Gaviscon is not compromised by concurrent H2-antagonist therapy.

Effect of time of dosing relative to a meal on the raft formation of an anti-reflux agent.

Gamma scintigraphy was used in twelve healthy volunteers to establish whether the time of dosing of Liquid Gaviscon relative to a meal influenced its therapeutic action. Indium-113m labelled Liquid Gaviscon was administered to fasted subjects, 30 min after a technetium-99m labelled meal or immediately before ingestion of the meal. The time for 50% of the Gaviscon to empty from the stomach was 0.36 +/- 0.13 h, 3.10 +/- 0.31 h and 0.68 +/- 0.04 h (s.e.m.), respectively. The preparation was found to empty rapidly from the fasted stomach and could not be floated on a meal consumed subsequently. For raft formation to occur, Liquid Gaviscon should be taken 30 min after a meal.

[Chemico-physical property and bile acid binding capacity of several antacids]. / Proprietà chimico-fisiche e capacità legante gli acidi biliari di alcuni antiacidi.

Liquid alginate (Gaviscon) binds small amount of bile acids. At pH 7 its viscosity (at low shear rate) is higher than that of other antiacids. High viscosity reduces the diffusion rate of bile salts and glucose and this property can play a role in the treatment of gastro-esophageal and duodeno-gastric refluxes.

Absorption studies of the H2-blocker nizatidine.

The absolute and relative bioavailability of nizatidine, an H2-blocker, was studied in healthy male volunteers. The absolute oral bioavailability, relative to that after intravenous administration, was 98% +/- 14%. The bioavailability of single and multiple oral doses of 150 mg nizatidine was unaffected by concurrent food ingestion; nizatidine may be administered either with or without food. The relative bioavailability of nizatidine was compared when given simultaneously with placebo or Gelusil, 30 minutes after propantheline, or 60 minutes before activated charcoal. Gelusil reduced the amount of nizatidine absorbed by about 10%, charcoal reduced it by about 30%, and propantheline did not affect it.