Absorption and Conversion of a Single Oral Dose of beta-Carotene in Corn Oil to Vitamin A in Sprague-Dawley Rats with Low Reserve of Vitamin A

2003 ◽  
Vol 73 (4) ◽  
pp. 267-273 ◽  
Author(s):  
Barua

This study was carried out to determine how much of a single oral dose of beta-carotene in oil is absorbed and how much of the absorbed dose is converted to retinoids in rats having a vitamin A reserve at the lowest end of adequate status. Weanling rats raised on a vitamin A-deficient diet for four weeks were given a single oral dose of either corn oil or beta-carotene dissolved in corn oil (1.86 mumol). Serum, liver, and the entire digestive tract of the rats were analyzed for carotenoids and retinoids. Results showed that 4 hours after dosing, 1.64 mumol (88%) of the dose of beta-carotene was found intact, with 17.6% found in the stomach, 21% in the small intestine, and 49.3% in the large intestine. A total of 0.28 mumol of newly formed retinoids (expressed as retinyl palmitate) was present in serum, liver, and mucosa of small intestine. The results suggest that a single oral dose of beta-carotene might not be an effective way of raising vitamin A status in rats.

2020 ◽  
Vol 150 (7) ◽  
pp. 1977-1981 ◽  
Author(s):  
Michael H Green ◽  
Joanne Balmer Green

ABSTRACT Background Better methods are needed for determining vitamin A absorption efficiency. Objective Our objective was to measure vitamin A absorption in rats by adapting a plasma isotope ratio method previously used to determine cholesterol absorption. Methods Male Sprague-Dawley rats [n = 14; 340 ± 16 g (mean ± SD)] received an oral tracer dose of [3H]retinyl acetate in oil plus an intravenous dose of [14C]vitamin A–labeled lymph prepared in a donor rat that had received [14C]retinyl acetate intraduodenally. Blood samples were collected on days 1, 2, 3, 6, 9, and 12, and plasma was analyzed for 3H and 14C; vitamin A absorption was calculated for each sample as (fraction of oral dose/fraction of intravenous dose) × 100. Radioactivity was also measured in feces and urine collected as pools on days 3, 6, 9, and 12 and in liver and remaining carcass on day 12. Results Vitamin A absorption calculated as the plasma isotope ratio was >100% on day 1, 78% ± 5% on day 6, 76% ± 5% on day 9, and 74% ± 5% on day 12; fitting the data to an exponential function plus a constant predicted an absorption of 75% by day 14. Recovery of the oral dose in feces (day 0 to day 6) was low (6.2% ± 0.84%, n = 10) and the mean isotope ratio in day 9–12 urine pool was lower than that in plasma. Conclusions The plasma isotope ratio holds promise for estimating vitamin A absorption, but additional work is needed to determine how long studies need to be and if the doses should be administered simultaneously. For application of this method in humans, artificial chylomicrons labeled with a stable isotope of retinyl acetate could be used for the intravenous dose, with a different isotope required for the oral dose.


2000 ◽  
Vol 44 (4) ◽  
pp. 910-915 ◽  
Author(s):  
Jehangir K. Khan ◽  
Hashem Montaseri ◽  
Marzena Poglod ◽  
Hai-Zhi Bu ◽  
Zhong Zuo ◽  
...  

ABSTRACT The pharmacokinetics and distribution in tissue of several novel triazole antifungal agents were studied in different animal species in order to select an appropriate lead compound. The purpose of the study was also to determine species differences in pharmacokinetics for SYN azoles to select the most appropriate species for secondary efficacy and toxicological evaluation of the selected compound. SYN-2836, SYN-2869, SYN-2903, and SYN-2921 were rapidly absorbed into the systemic circulation and reached maximum concentrations (C maxs) of 7.31 ± 2.53, 6.29 ± 0.85, 6.16 ± 0.39, and 3.41 ± 0.34 μg/ml, respectively, in BALB/c mice after administration of an oral dose of 50 mg/kg of body weight, with bioavailability being greater than 45% in all mice. The areas under the concentration-time curve from time zero to infinity (AUC0–∞s) after administration of a single intravenous dose of 20 mg/kg to mice varied between 25.0 and 63.6 μg · h/ml. The half-life was in the range of 4.5 to 6 h. In Sprague-Dawley rats there was no significant difference in AUC0–∞ after administration of a single intravenous dose of 20 mg/kg, but on oral administration, the bioavailability of SYN-2836 was extremely low, while that of SYN-2869 was only 14.7%. In New Zealand White rabbits the C max and the time to reach C max for SYN-2836 and SYN-2869 after administration of a single oral dose of 50 mg/kg were similar. There were significant differences in AUC0–∞ and half-life between SYN-2836 and SYN-2869. On the other hand, in beagle dogs theC max and AUC0–∞ of SYN-2836 after administration of a single oral dose of 30 mg/kg were 4.82 ± 1.54 μg/ml and 41.8 ± 15.7 μg · h/ml, respectively, which were threefold higher than those of SYN-2869. The concentrations of the SYN compounds in tissue indicated that the AUC0–∞s of SYN-2836, SYN-2869, SYN-2903, and SYN-2921 in mouse lungs were significantly different from each other. The ratios of the concentrations of the SYN azoles in lungs to those in plasma were also significantly different from those for itraconazole. Among the SYN azoles the highest concentration in the lungs was found for SYN-2869. The higher level of distribution of SYN-2869 into lung tissue was considered to contribute to the potent efficacy in respiratory tract infection models compared with the potency of itraconazole. Significant differences in the pharmacokinetics of these compounds were observed in different animal species, and selection of an animal model for further evaluation was based on results obtained from these studies.


Author(s):  
A. S. Alekseeva ◽  
T. B. Shemeryankina ◽  
M. N. Lyakina ◽  
M. S. Smirnova ◽  
E. P. Fedorova ◽  
...  

Vitamin A is present in multivitamin products mainly in the form of retinol esters: retinyl acetate, retinyl palmitate, and beta carotene—retinol precursor (dimer) found in plants, which is capable of converting into retinol in liver cells. Retinol is determined in medicinal products primarily by high performance liquid chromatography (HPLC), with preliminary purification and vitamin isolation by liquid-liquid extraction. However, scientific literature also describes other methods of sample preparation and analysis of such compounds. An important issue is differentiation of vitamin A from other fat-soluble vitamins often included as components in multivitamin products. The aim of the study was to analyse and summarise data on current methods used for determination of vitamin A and its derivatives in medicinal products. The authors analysed the range of vitamin A products authorised in the Russian Federation, and the test methods described in their product specification files. The study demonstrated that the test method most often used for determination of retinol esters was HPLC with isocratic elution mode using octadecylsilyl packing in the reverse-phase mode, and, less frequently, aminopropylsilyl packing in the normal phase mode. Determination of beta carotene in medicinal products is most often performed using spectrophotometry. 


1975 ◽  
Vol 53 (2) ◽  
pp. 256-263
Author(s):  
Bill Woodward ◽  
B. E. March

The variable effect of excessive vitamin A intake on alimentary cholesterolemia was investigated in cockerels of strains of White Leghorns and New Hampshires. With the New Hampshire cockerels, the feeding of 0.5% of dietary cholesterol resulted in greater cholesterolemia when the diet contained 1 700 I.U. of vitamin A per kilogram than when it contained 22 000 I.U. of vitamin A per kilogram. With the White Leghorn cockerels, on the other hand, cholesterolemia was enhanced with the higher level of dietary vitamin A. Absorption of a single oral dose of cholesterol was increased in birds of both breeds when vitamin A had been given previously by injection. In the White Leghorn cockerels the percentage of newly absorbed cholesterol in the hepatic pool was reduced by vitamin A administration, whereas in the New Hampshire cockerels the percentage was increased. It was concluded that excess vitamin A may have divergent effects on alimentary cholesterolemia in chickens of different genetic backgrounds as a result of opposite effects on the liver–blood ratio of a large load of cholesterol.


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