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A Bär

Publications and source records attributed to A Bär.

At least 19 recordsLinked to original sources

Embryotoxicity and teratogenicity study with alpha-cyclodextrin in rabbits.

In a standard embryotoxicity/teratogenicity study, alpha-cyclodextrin (alpha-CD) was administered to groups of sixteen, artificially inseminated New Zealand White rabbits at dietary concentrations of 0, 5, 10, or 20%. An additional group received a diet containing 20% lactose. Treatment started on day 0 of gestation and ended on day 29 when the animals were killed. Except for the occurrence of transient diarrhoea in one rabbit of the 20% alpha-CD group for a few days, the treatment was well tolerated. A reduced food intake in the 20% alpha-CD group during the first week of treatment resulted in a reduced weight gain from day 0 to 12 of the study. However, the difference to the controls was not significant and at termination of the study body weights were similar in all groups. Even at the highest dose level, which corresponds to an intake of 5.9-7.5 g/kg bw/day, no signs of maternal toxicity were observed. Maternal reproductive performance was not affected by the treatment. Uterine weight, placental weight, fetal weight, number of fetuses, sex ratio, number of implanation sites, resorptions, and corpora lutea did not differ among the groups. Visceral and skeletal examinations of the fetuses did not reveal any malformations, anomalies or variations that could be attributed to treatment. It was concluded that dietary alpha-CD is generally well tolerated by pregnant rabbits, has no adverse effect on maternal reproductive performance and is not embryotoxic, fetotoxic, or teratogenic at dietary concentrations of up to 20%, the highest dose level tested.

Abnormalities, Drug-Induced↗

Embryotoxicity and teratogenicity study with alpha-cyclodextrin in rats.

The embryotoxicity/teratogenicity of alpha-cyclodextrin (alpha-CD) was examined in Wistar Crl:(WI)WU BR rats. alpha-CD was fed at dietary concentrations of 0, 1.5, 5, 10, or 20% to groups of 25 pregnant female rats from day 0 to 21 of gestation. An additional group received a diet with 20% lactose. The additions to the diet of alpha-CD and lactose were made at the expense of pregelatinized potato starch. Body weight as well as food and water intake were recorded during the treatment period. The rats were killed on day 21 and examined for standard parameters of maternal reproductive performance. The fetuses were examined for external abnormalities, body weight and crown rump length. Fetuses were examined for skeletal and visceral abnormalities. Generally, alpha-CD was well tolerated and no deaths occurred in any group. Weight gain and food consumption were similar in all groups during gestation, except for a slightly yet significantly increased food intake in the 20% alpha-CD group from day 6 to 21. Water intake was similar in all alpha-CD groups; in the lactose group, it was significantly higher than in the controls. Maternal reproductive performance was not affected by the alpha-CD treatment. Examination of the fetuses for external, visceral and skeletal changes did not reveal any fetotoxic, embryotoxic, or teratogenic effects of alpha-CD. In conclusion, no adverse effects were observed at alpha-CD intakes of up to 20% of the diet, the highest dose level tested at which the rats consumed about 13 g/kg bw/day.

Abnormalities, Drug-Induced↗

Subchronic (13-week) oral toxicity study of alpha-cyclodextrin in dogs.

The oral toxicity of alpha-cyclodextrin (alpha-CD) was examined in a 13-week feeding study in which groups of Beagle dogs received alpha-CD in the diet at concentrations of 0 (control), 5, 10, or 20% (4 dogs/sex/group). No treatment-related changes were noted in behavior or appearance of the dogs and no mortalities occurred. Diarrhea occurred in all alpha-CD groups. The incidence and severity of diarrhea increased with increasing dietary levels of alpha-CD and was more pronounced in males than females. Nonetheless, all dogs remained in good health and gained weight. Food intake was slightly increased and food efficiency was slightly decreased in the 20% alpha-CD group. However, these changes did not reach statistical significance. No treatment-related differences were observed with respect to ophthalmoscopic examinations, hematological parameters, clinicochemical analyses of the plasma, and semiquantitative urine analyses. Only the urinary pH was slightly below control levels in males (p > 0.05) and females (p < 0.05) of the 20% alpha-CD group. No abnormalities were seen at necropsy that could be attributed to the treatment. The organ weight data revealed cecal enlargement in the 10 and 20% alpha-CD groups (significant only in males). The relative weight of the colon was also slightly increased in the 10 and 20% alpha-CD groups (significant only in females of the 10% alpha-CD group). On microscopic examination, no treatment-related alterations were observed in any of the various organs and tissues. In conclusion, transient diarrhoea, enlargement of the cecum and colon and a slightly increased acidity of the urine were the only treatment-related effects. These changes are well-known physiological responses to the presence of high amounts of not digested, fermentable carbohydrates in the lower gut. They are known to be reversible on cessation of the treatment and are not associated with histological alterations of the intestinal tissues. It is concluded, therefore, that the high dose level, at which the male and female dogs consumed about 9.8 and 10.4 g alpha-CD/kg bw/d, respectively, is the NOAEL of this 13-week toxicity study.

Administration, Oral↗

Subchronic oral toxicity studies with alpha-cyclodextrin in rats.

The toxicity of alpha-cyclodextrin (alpha-CD), a cyclic polymer of six alpha-1,4-linked glucopyranosyl units with potential applications as a food ingredient, more specifically a water-soluble dietary fiber, was examined in a 4-week range finding study and a 13-week oral toxicity study in rats. In the 4-week study, the test substance was administered to groups of Bor:WISW(SPF;Cpb) rats at dietary levels of 0, 1, 5, and 15% (5 rats/sex/group). An additional group received a diet with 5% beta-CD. In the 13-week study, groups of Crl:(WI)WU Br rats received diets with 0, 1.5, 5, or 20% alpha-CD. An additional group received a diet with 20% lactose (20 rats/sex/group). Satellite groups of 10 rats/sex were attached to the control, 20% alpha-CD and 20% lactose group. Following the 13-week treatment period, these satellite groups were kept on a standard, cereal-based rodent diet for a 4-week recovery period. Parameters measured during the two studies included clinical signs, body weights, food and water intake, hematological and clinicochemical parameters, and organ weights as well as gross and histopathological observations at necropsy. In the 13-week study, ophthalmoscopic examinations as well as urine and feces analyses were also conducted. There were no treatment-related mortalities in either study. In the 4-week study, persistent diarrhea was the most prominent, treatment-related effect observed in the animals of the 15% alpha-CD group especially in the male animals. In association with this effect, food consumption and food conversion efficiency were decreased. In line with observations from studies with other low-digestible, yet fermentable carbohydrates, the weight of the full and empty cecum was increased significantly in the 5% alpha-CD, 5% beta-CD, and 15% alpha-CD group. The reduced relative liver weights (in males and females) and the significantly increased relative testes weight which were observed in the 15% alpha-CD group, were attributed to the impaired nutritional condition (due to diarrhea) and the reduced body weight of the animals of this group, respectively. Microscopic examination of the main organs did not reveal pathological alterations that could be attributed to the alpha-CD treatment. In the 13-week study, soft stool and infrequent mild diarrhea were observed only during the first 2-3 weeks in the 20% alpha-CD and 20% lactose group (mainly male animals). Accordingly, body weights were reduced in males of the 20% lactose group throughout the study and in the 20% alpha-CD group during the last week of the study. Food intakes were slightly increased in the 20% alpha-CD group and the food conversion efficiency, was significantly reduced in males, but not females, of the 20% alpha-CD and 20% lactose group. There were no treatment-related changes of hematological parameters. In line with similar observations from studies on other low-digestible carbohydrates, the urinary pH was decreased and urinary calcium levels increased in the 20% alpha-CD and 20% lactose group. Similarly, the fecal dry weight and nitrogen output was increased in these groups. At termination of the treatment, significantly in creased cecum weights (full and empty) were observed in the 5 and 20% alpha-CD groups and the 20% lactose group. The relative (not absolute) weight of the spleen was significantly increased in males of the 20% alpha-CD group. In the 20% lactose group, the relative weights of the spleen and liver (females) and the testes, brain, and adrenals (males) were significantly increased. The histopathological examination of these and all other organs and tissues did not reveal any abnormalities that could be attributed to the alpha-CD or lactose treatment. In conclusion, the ingestion of alpha-CD for 13-weeks at dietary levels of up to 20% (corresponding to intakes of 12.6 and 13.9 g/kg bodyweight/d in male and female rats, respectively) did not produce any signs of toxicity or adverse effects.

Administration, Oral↗

Embryotoxicity and teratogenicity study with neohesperidin dihydrochalcone in rats.

The embryotoxicity/teratogenicity of neohesperidin dihydrochalcone (NHDC) was examined in Wistar Crl:(WI)WU BR rats. NHDC was fed at dietary concentrations of 0, 1.25, 2.5 or 5 to groups of 28 mated female rats from day 0 to 21 of gestation. At Cesarean section 25, 22, 23, and 23 rats were found to be pregnant in the control, low-, mid-, and high-dose group, respectively. The NHDC treatment was well tolerated and all animals survived till the end of the study. Body weights (bw) and body weight gains did not differ between controls and NHDC treatment groups. The intake of NHDC was 0.8-0.9, 1.6-1.7, and 3.1-3.4 g/kg bw/day for the low-, mid-, and high-dose group, respectively. Except for cecal enlargement, there were no changes observed at necropsy which could be related to the NHDC treatment. All dams had viable fetuses. The fecundity and gestation index, the number of corpora lutea, implantation sites, live and dead fetuses, early and late resorptions, pre- and post-implantation losses, and sex-ratio were not affected by the treatment. There were no differences for the mean weight of the gravid and empty uterus, ovaries, and placenta between the NHDC treatment groups and the controls. Examination of the fetuses for external, visceral, and skeletal changes did not reveal any fetotoxic, embryotoxic or teratogenic effects of NHDC. In conclusion, no adverse effects were observed at NHDC levels of up to 5% of the diet, the highest dose level tested, at which the rats consumed about 3.3g/kg body weight/day. The observed cecal enlargement is a well-known physiological, adaptive response to the ingestion of high doses of a low-digestible substance and is generally accepted to lack toxicological relevance.

Animals↗

Safety assessment of gamma-cyclodextrin.

Gamma-cyclodextrin (gamma-CD) is a cyclic alpha-(1,4)-linked oligosaccharide consisting of eight glucose molecules. Like other cyclodextrins, gamma-CD can form inclusion complexes with a variety of organic molecules because the inner side of the torus-like molecule is less polar than the outer side. In foods, gamma-CD may be used as a carrier for flavors, vitamins, polyunsaturated fatty acids, and other ingredients. It also has useful properties as a stabilizer in different food systems. The daily intake from all its intended uses in food at highest feasible concentrations has been estimated at 4.1g/person/day for consumers of gamma-CD containing foods. The present review summarizes the safety data of gamma-CD. The toxicity studies consist of standard genotoxicity tests, subchronic rat studies with oral and intravenous administration of gamma-CD for up to 3 months, a subchronic (3-month) toxicity study in dogs, a (1-year) oral toxicity study in rats, and embryotoxicity/teratogenicity studies in rats and rabbits. In the studies with oral administration, gamma-CD was given at dietary concentrations of up to 20%. All these studies demonstrated that gamma-CD is well tolerated and elicits no toxicological effects. Metabolic studies in rats showed that gamma-CD is rapidly and essentially completely digested by salivary and pancreatic amylase. Therefore, the metabolism of gamma-CD closely resembles that of starch and linear dextrins. A human study with ingestion of single doses of 8 g gamma-CD or 8 g maltodextrin did not reveal a difference in gastrointestinal tolerance of these two products. An interaction of ingested gamma-CD with the absorption of fat-soluble vitamins or other lipophilic nutrients is not to be expected because the formation of inclusion complexes is a reversible process, gamma-CD is readily digested in the small intestine, and studies with beta-CD, a non-digestible cyclodextrin, have shown that the bioavailability of vitamins (A, D, and E) is not impaired. On basis of these studies it is concluded that gamma-CD is generally recognized as safe (GRAS) for its intended uses in food.

Animals↗

Safety evaluation of an alpha-cyclodextrin glycosyltranferase preparation.

Alpha-cyclodextrin glucosyltransferase (alpha-CGTase, EC 2.4.1.19) is an amylolytic enzyme used for the production of alpha-cyclodextrin (alpha-CD), a novel, soluble dietary fiber, from food-grade starch. The safety of an alpha-CGTase preparation obtained by batch fermentation from a recombinant strain of Escherichia coli K12 harboring the alpha-CGTase gene from Klebsiella oxytoca strain M5a1 was examined. In a 13-week subchronic toxicity study in rats, the administration by gavage of the alpha-CGTase preparation at levels of up to 20 ml/kg bw/day, corresponding to a total organic solids dosage of 260 mg/kg bw/day, did not cause any systemic toxic effect. Some signs of irritation were observed in the respiratory tract which occurred, however, in one sex only and/or were not dose-related. Accordingly, these changes were considered to be an unspecific consequence of the reflux and aspiration of the dosing solution. There was no evidence of a genotoxic activity in Ames tests and a chromosome aberration test in cultured human lymphocytes. It is concluded that the examined alpha-CGTase preparation is safe when used for the production of alpha-CD.

Animals↗

Disposition of 14C-alpha-cyclodextrin in germ-free and conventional rats.

The absorption, disposition, metabolism, and excretion of uniformly (14)C-labeled alpha-cyclodextrin ((14)C-alpha-CD) was examined in four separate experiments with Wistar rats. In Experiment 1, (14)C-alpha-CD (25 microCi, 50 mg/kg bw) was administered intravenously to four male and four female conventional rats. In Experiment 2, (14)C-alpha-CD (25 microCi, 200 mg/kg bw) was given by gavage to four male and four female germ-free rats. In Experiments 3 and 4, (14)C-alpha-CD was given to groups of four male and four female conventional rats by gavage at different dose levels (100 microCi, 200 mg/kg bw; 25 microCi, 200 and 100 mg/kg bw). In all experiments, (14)C was measured in respiratory CO(2), urine, and feces over periods of 24-48 h, and in the contents of the gastrointestinal tract, blood, main organs, and residual carcass at termination of the experiments. The chemical identity of the (14)C-labeled compounds was examined by HPLC in blood (Experiment 1), urine (Experiments 1-4), feces (Experiments 2-4), and samples of intestinal contents (Experiments 2 and 4). Recovered (14)C was expressed as percentage of the administered dose. Experiment 1 showed that intravenously administered alpha-CD is excreted rapidly with urine. During the first 2h after dosing, plasma (14)C levels decreased rapidly (t(1/2), 26 and 21 min in male and female rats, respectively). About 13% of the administered (14)C dose (range 4.6-30.6) was detected in the feces, respiratory CO(2), organs, and carcass at the end of the experiment, i.e., 24 h after dosing. The presence of about 1.9% in the intestinal contents and feces suggests that a certain fraction of systemic alpha-CD is eliminated with the bile or saliva. Conclusive evidence, either positive or negative, for a hydrolysis and further metabolism of a small fraction of the administered alpha-CD by the enzymes of the mammalian body could not be gained from this experiment. Upon oral administration of (14)C-alpha-CD to germ-free rats (Experiment 2), about 1.3% of the label expired as CO(2) within 24 h. In the urine collected from 0 to 8 h after dosing, (14)C-alpha-CD was the only radiolabeled compound detected. The amounts of alpha-CD detected in the urine suggest that on average about 1% of an oral dose is absorbed in rats during small-intestinal passage. In conventional rats (Experiments 3 and 4), a delayed appearance of respiratory (14)CO(2) was observed which is attributed to the non-digestibility of alpha-CD and its subsequent microbial fermentation in the cecum and colon. In the urine collected at 4 h after dosing, a small amount of unchanged (14)C-alpha-CD was detected which confirms that about 1% of the ingested alpha-CD is absorbed intact and is excreted via the kidneys. No (14)C-alpha-CD was found in the feces. It is concluded from the data that ingested (14)C-alpha-CD is not digested in the small intestine of rats but is fermented completely by the intestinal microbiota to absorbable short-chain fatty acids. Therefore, the metabolism of alpha-CD resembles closely that of resistant starch or other fermentable dietary fibers.

Administration, Oral↗

[Subtotal bilateral adrenalectomy preserving adrenocortical function].

This study analyzed the frequency of recurrence and postoperative adrenocortical function in 16 patients who had been operated on by bilateral subtotal adrenalectomy since 1995. Bilateral pheochromocytoma was found in 13 patients, bilateral adrenal metastases in 2 patients, and bilateral micronodular adrenocortical hyperplasia with primary aldosteronism in 1 patient. An endoscopic approach was performed in four patients. The remaining 12 patients were operated on by an open approach. In ten patients, unilateral subtotal adrenalectomy with contralateral total adrenalectomy (synchronous or metachronous) was performed. Six patients underwent bilateral subtotal adrenalectomy. In all patients, a total of residual adrenal tissue of at least 1/3 of a normal adrenal gland was left in situ. 15 patients were successfully weaned from exogenous steroid substitution. During a mean follow-up period of 24 months, no recurrences were observed. Three patients died without local recurrence. The present study provided evidence for the safety and benefit of subtotal bilateral adrenalectomy, which could guarantee sufficient adrenocortical function in adrenal remnant volume of more than one-third of one adrenal gland even after dividing the main adrenal vein. At our institution, particularly in patients with inherited pheochromocytoma, subtotal adrenalectomy has become a common surgical strategy.

Adrenal Cortex Function Tests↗

Effect of oral D-tagatose on liver volume and hepatic glycogen accumulation in healthy male volunteers.

Standard toxicity tests with high levels of D-tagatose showed a reversible enlargement of the liver in Sprague-Dawley rats without increase of liver enzymes. The present study tests the hypotheses that partial substitution of dietary sucrose by D-tagatose for 28 days increases the volume of human liver and the concentration of liver glycogen. Twelve healthy, male volunteers were studied in a double-blind crossover study with ingestion of D-tagatose (3x15 g daily) and placebo (sucrose, 3x15 g daily) for periods of 28 days each. Liver volume and glycogen concentration have been determined by magnetic resonance (MR) imaging and spectroscopy, which were accompanied by routine medical examinations. MR examinations before and after the treatments revealed no effects (P>0.05) of treatment, period, or subject for changes in liver volume or glycogen concentration. A steady increase of liver volumes, independent of the D-tagatose or placebo intake, has been observed over the study in parallel with a slight increase in body weight. The treatment with D-tagatose was not associated with clinically relevant changes of the examined clinico-chemical and hematological parameters, including liver enzymes and uric acid.

Administration, Oral↗

L-Sorbose but not D-tagatose induces hemolysis of dog erythrocytes in vitro.

Previous investigations have demonstrated that L-sorbose induces hemolysis of dog erythrocytes. This effect is probably the consequence of an ATP depletion of the red blood cells subsequent to inhibition of hexokinase, and thus the glycolytic pathway, by sorbose 1-phosphate. In the present study, the susceptibility of dog erythrocytes to D-tagatose, a stereoisomer of L-sorbose, was examined. Washed dog erythrocytes were suspended in Hanks' balanced salt solution (HBSS, containing 5.6 mM glucose) with or without the addition of 0.6, 6, and 60 mM L-sorbose or D-tagatose, or in HBSS with total glucose concentrations of 5.6, 6 and 60 mM D-glucose. After incubation for 24 h at 34 degrees C, the suspensions were centrifuged, and the percentage of hemolysis was determined by measuring the hemoglobin in the sediment and the supernatant. The amount of hemoglobin released in the medium did not differ significantly between the control (HBSS) and the test incubations with glucose or D-tagatose supplementation. In contrast, the addition of 6 and 60 mM L-sorbose resulted in significant hemolysis. At the low dose (0.6 mM), L-sorbose did not have an adverse effect. It is concluded that D-tagatose, unlike L-sorbose, does not have a hemolytic effect on canine erythrocytes.

Animals↗

Effect of D-tagatose on liver weight and glycogen content of rats.

D-tagatose is an incompletely absorbed ketohexose (stereoisomer of D-fructose) which has potential as an energy-reduced alternative sweetener. In an earlier 90-day toxicity study, rats fed diets with 10, 15 and 20% D-tagatose exhibited increased liver weights, but no histopathological alterations. To determine whether there might be any toxicological relevance to this effect, three studies were conducted in male, adult Sprague-Dawley rats. In the first study, four groups received Purina diet (group A), Purina diet with 20% D-tagatose (group B), SDS diet (group C), or SDS diet with 20% D-tagatose (group D). For groups A and B, the 28-day treatment period was followed by a 14-day recovery period (Purina diet). Food remained available to all animals until the time of sacrifice. Groups of 10 rats were killed on days 14 (groups A and B), 28 (groups A-D), and 42 (groups A and B). Body weights, as well as weights of wet and lyophilized livers, were determined. The lyophilized livers collected on day 28 from groups A and B were analyzed for protein, total lipid, glycogen, DNA, and residual moisture. By day 14, relative wet liver weights had increased by 23% in group B. On day 28, the increase was 38% in group B and 44% in group D. At the end of the recovery period, the increase had diminished to 14% in group B. On day 28, liver glycogen content (in %) was significantly increased, and liver protein, lipid, and DNA contents were significantly decreased in group B compared to group A. Total amounts per liver of protein, total lipid, glycogen, and DNA were significantly increased. In the second study, four groups of 20 rats each received SDS diet with 0, 5, 10, and 20% D-tagatose for 29-31 days. The food was available until the time of sacrifice. At termination, plasma was obtained from 10 rats/group for clinicochemical analyses. Five rats/group were subjected to whole-body perfusion, followed by processing of livers for qualitative and quantitative electron microscopic examination. Livers of 6 rats/group were analyzed for acyl-CoA oxidase and laurate 12-hydroxylase (cytochrome P450 4A1) activity, DNA synthesis (Ki-67 index), and number of nuclei per unit area of tissue. Liver weights were significantly increased in linear relation to the D-tagatose intake. Plasma transaminases (but not glutamyl transferase and alkaline phosphatase) were increased in the high-dose group. Except for glycogen accumulation, no ultrastructural changes were seen on electron microscopic examination of livers of the control and high-dose groups. Morphometric analysis confirmed the increase of glycogen and the absence of alterations of endoplasmatic reticulum, mitochondria, and Golgi apparatus. The Ki-67 index did not differ between the groups. A dose-related decrease of the number of nuclei per unit area signified some hepatocellular hypertrophy. Acyl-CoA oxidase and CYP4A1 activity were significantly increased in the mid- and high-dose groups, but these increases were small and not accompanied by electron-microscopic evidence of peroxisome proliferation. In the third study, four groups received SDS diet (groups A and C) or SDS diet with 5% D-tagatose (groups B and D). All animals were killed on day 28. Groups A and B were fasted for 24 h before sacrifice; groups C and D had food available until sacrifice. Liver weights and liver composition were measured as in Study 1. Relative wet and dry liver weights were increased in response to the treatment in rats killed under the fed condition, but not in rats killed under the fasted condition. The livers of the treated rats (group D) had an increased glycogen content in comparison to the controls (group C). Taken together, these results demonstrate that D-tagatose at dietary levels of 5-20% increases liver glycogen deposition and relative liver weights in nonfasting rats. In fasted rats the 5% dose level is the no-effect level. (ABSTRACT TRUNCATED)

Animals↗

Characteristics and significance of D-tagatose-induced liver enlargement in rats: An interpretative review.

This review addresses the issue of asymptomatic liver enlargement in rats. It was necessitated by the observation of significantly increased liver weights in rats fed diets with 10 to 20% D-tagatose, a potential new bulk sweetener, for between 28 and 90 days. Increases of liver size without accompanying histopathological changes or impairment of organ function have been observed in rats in response to the ingestion of various xenobiotic compounds (including some food additives), changes of dietary composition (e.g. , high doses of fructose and sucrose), metabolic aberrations (e.g., diabetes), as well as normal pregnancy and lactation. The underlying mechanism(s) are not yet understood in detail but peroxisome proliferation, microsomal enzyme induction, increased storage of glycogen or lipids, and hyperfunction due to an excessive workload are well-established causes of hepatomegaly in rats. In D-tagatose- and fructose-fed rats, a treatment-related increase of hepatic glycogen storage was identified as a likely cause of the liver enlargement. Dietary levels of 5% and about 15-20% were determined as no-effect levels (NOEL) for D-tagatose- and fructose-induced liver enlargement, respectively. At doses above the NOEL, D-tagatose is about four times more efficient than fructose in inducing liver enlargement. On the other hand, the estimated intake of D-tagatose from its intended uses in food is about four times lower than the actual fructose intake. Consequently, a similar safety margin would apply for both sugars. Considering the similarity of the liver effects in rats of fructose, a safe food ingredient, and D-tagatose, the absence of histopathological changes in rats fed a diet with 20% D-tagatose for 90 days, and the absence of adverse long-term consequences of glycogen-induced liver enlargement in rats, it is concluded that the observed liver enlargement in D-tagatose-fed rats has no relevance for the assessment of human safety of this substance.

Animals↗

Gastrointestinal tolerance of gamma-cyclodextrin in humans.

The gastrointestinal tolerance of gamma-cyclodextrin (gamma-CD) was examined in 24 healthy human volunteers. In a double-blind, placebo-controlled, randomized cross-over study, single acute doses of 8 g maltodextrin (placebo) or 8 g gamma-CD (test) were consumed as a mid-morning snack after addition to 100 g yogurt. Gastrointestinal symptoms as well as frequency and consistency of stools were recorded before and after lunch at between 3-4 and 7-8 h after intake respectively. The perception of the symptoms was rated on a subjective scale ranging from 1 ('more than normal') to 3 ('exceptionally more than normal'). Following consumption of maltodextrin, five subjects reported a total of 12 symptoms of which seven, two and three were rated as having grade 1, 2 and 3, respectively. Following consumption of gamma-CD, five subjects reported six symptoms all of which were graded as 1. Two subjects reported flatulence, which is a frequent consequence of the consumption of malabsorbed carbohydrates, after placebo and test treatment. The incidence of individual and combined side-effects as well as the number and consistency of faeces passed was not significantly different between placebo and test treatment. It is concluded that single doses of 8 g gamma-CD and maltodextrin are tolerated equally well. This is in keeping with a good digestibility of gamma-CD by salivary and pancreatic amylase.

Adolescent↗

Disposition of [14C]gamma-cyclodextrin in germ-free and conventional rats.

The absorption, disposition, metabolism, and excretion of 14C-labeled gamma-cyclodextrin ([14C]gamma-CD) was examined in four separate experiments with Wistar rats. In experiment 1, [14C]gamma-CD (25 microCi, 600 mg/kg body wt) was administered intravenously to four male and four female conventional rats. In experiment 2, [14C]gamma-CD (25 microCi, 1000 mg/kg body wt) was given by gavage to four male and four female germ-free rats. In experiments 3 and 4, [14C]gamma-CD (25 and 100 microCi, respectively, 1000 mg/kg body wt) was given to four male and four female conventional rats by gavage. In all experiments, 14C was measured in respiratory CO2, urine, feces, contents of the gastrointestinal tract, blood, main organs, and residual carcass. The chemical identity of the 14C-labeled compounds was examined by HPLC in urine (experiments 1-4), blood (experiments 1 and 4), and samples of intestinal contents (experiments 3 and 4). Recovered 14C was expressed as a percentage of the administered dose. Total recovery of 14C varied between about 90% (experiments 3 and 4) and 100% (experiments 1 and 2). Experiment 1 showed that about 90% of intravenously administered gamma-CD is excreted in urine within 24 h. During the first 2 h after dosing, plasma 14C levels decreased rapidly (t1/2, 15-20 min). The remaining 10% of the dose was probably excreted into the gastrointestinal tract with bile and saliva. In addition, some [14C]gamma-CD may have been degraded by plasma and tissue amylases. Since glucose is the common product of systemic hydrolysis and intestinal digestion, it is not possible to quantitate the relative flux of [14C]gamma-CD through these two pathways. Upon oral administration of [14C]gamma-CD to germ-free rats (experiment 2), about 66% of the label was expired as CO2 within 24 h. The rate of 14C exhalation reached a maximum at 90 min after dosing and then declined steadily. In the urine, and in the contents of the cecum and colon collected at 24 h, [14C]gamma-CD was not found (except for a trace in the cecum of females). In conventional rats (experiments 3 and 4), a similar, fast appearance of respiratory 14CO2 was observed. There was no delayed formation of 14CO2 due to incomplete digestion and subsequent microbial fermentation in the cecum and colon. In pooled urine collected at 4 h after dosing, a small amount of unchanged [14C]gamma-CD was detected (experiment 4). From this result, it was estimated that less than 0.02% of ingested intact gamma-CD was absorbed and excreted with the urine. It is concluded from the data that ingested [14C]gamma-CD is rapidly and essentially completely digested in the small intestine to absorbable [14C]glucose. The absorption of intact [14C]gamma-CD by passive diffusion is very low (<0.02%). Therefore, the metabolism of gamma-CD resembles closely that of starch or linear dextrins.

Administration, Oral↗

Subchronic (13-week) oral toxicity study of gamma-cyclodextrin in dogs.

The oral toxicity of gamma-cyclodextrin (gamma-CD) was examined in a 13-week feeding study in which four groups of four male and four female Beagle dogs received gamma-CD in the diet at concentrations of 0 (control), 5, 10, or 20%. No treatment-related changes were noted in behavior or appearance of the dogs and no mortalities occurred. Transient diarrhea occurred in some dogs of the 5 and 10% dose groups and in all dogs of the 20% dose group. However, all dogs remained in good health and gained weight. During the last 6 weeks of the study, the males of the 20% dose group gained less weight, but body weights were not significantly reduced in comparison to controls. Food intakes and food efficiencies were comparable among all groups. No treatment-related differences were observed with respect to ophthalmoscopic examinations, hematological parameters, clinicochemical analyses of the plasma, and semiquantitative urine analyses. Only the urinary pH was slightly below control levels in males of the 20% dose group. No abnormalities were seen at necropsy that could be attributed to treatment. The organ weight data revealed some cecal enlargement in the 10 and 20% dose groups. Relative ovary weights were significantly increased in the 10 and 20% groups but this was probably a result of an unusually low ovary weight in the controls. An increase of relative liver weights in males of the 10 and 20% dose groups also was considered to lack toxicological relevance because it was not associated with changes in plasma liver enzyme levels or histopathological changes. On microscopic examination, no treatment-related effects were observed in any of the various organs and tissues. In conclusion, transient diarrhea, cecal enlargement, and a slightly increased acidity of the urine were the only treatment-related effects reported. These changes are well-known physiological responses to the presence of increased amounts of undigested, fermentable carbohydrates in the lower gut. At the high applied intakes an incomplete digestion of gamma-CD and/or a partial inhibition of pancreatic amylase by gamma-CD could account for these effects. It is concluded that daily gamma-CD consumption of up to 20% in the diet (approximately 7.7 g/kg body wt in male and 8.3 g/kg body wt in female dogs) was tolerated without any toxic effects.

Administration, Oral↗

Embryotoxicity and teratogenicity study with gamma-cyclodextrin in rats.

The embryotoxicity/teratogenicity of gamma-cyclodextrin (gamma-CD) was examined in Wistar Crl:(WI)WU BR rats. gamma-CD was fed at dietary concentrations of 0, 1.5, 5, 10, and 20% to groups of 25 pregnant female rats from day 0 to 21 of gestation. A comparison group received a diet with 20% lactose. The additions to the diet of gamma-CD and lactose were made at the expense of pregelatinized potato starch. Body weight and food and water intake were recorded during the treatment period. The rats were killed on day 21 and examined for standard parameters of reproductive performance. The fetuses were examined for signs of toxic and teratogenic effects. Generally, gamma-CD was well tolerated and no deaths occurred in any group. Weight gain and food consumption were similar in all groups during gestation, except for a slightly reduced food intake in the 20% gamma-CD group from day 0 to 16. Water intake was similar in all gamma-CD groups; in the lactose group, it was significantly higher than in the control group. Reproductive performance was not affected by the gamma-CD treatment. Examination of the fetuses for external, visceral, and skeletal alterations did not reveal any fetotoxic, embryotoxic, or teratogenic effects of gamma-CD. In conclusion, no adverse effects were observed at gamma-CD intakes of up to about 20% of the diet (approximately 11 g/kg body wt/day).

Animal Feed↗

Embryotoxicity and teratogenicity study with gamma-cyclodextrin in rabbits.

In a standard embryotoxicity/teratogenicity study, gamma-cyclodextrin (gamma-CD) was administered to groups of 16, artificially inseminated New Zealand White rabbits at dietary concentrations of 0, 5, 10, or 20%. A comparison group received a diet containing 20% lactose. Treatment started on day 0 of gestation and ended on day 29 when the animals were killed. Except for the occurrence of transient diarrhea in 2 and 3 rabbits of the 10 and 20% gamma-CD groups, respectively, in the first few days, the treatment was well tolerated. A reduced food intake in the 20% gamma-CD group during the first week of treatment resulted in a reduced weight gain during this period. However, after week 1 there were no differences in weight gains between the groups, and at termination of the study body weights were similar in all groups. Even at the highest dose level, which corresponds to an intake of 5-7 g/kg body wt/day, no signs of maternal toxicity were observed. Reproductive performance was not affected by the treatment. Uterine weight, placental weight, fetal weight, number of fetuses, sex ratio, number of implantation sites, resorptions, and corpora lutea did not differ among the groups. Visceral and skeletal examinations of the fetuses did not reveal any malformations, anomalies, or variations that could be attributed to treatment. It was concluded that dietary gamma-CD is well tolerated by pregnant rabbits, has no adverse effect on reproductive performance, and is not embryotoxic, fetotoxic, or teratogenic at dietary concentrations of up to 20%.

Animal Feed↗