• Asian-Australasian Journal of Animal Sciences
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• v.23 no.1
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• pp.90-97
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• 2010

An experiment was conducted to evaluate the effects of low concentrations of organic and inorganic dietary trace minerals on broiler performance and trace mineral digestibility along the small intestine of 35-day-old broiler chickens reared under floor-pen conditions. Eight hundred male, day-old Cobb broiler chickens were randomly allocated to 4 dietary treatments (25 birds per pen with 8 replicates per treatment). Broilers fed diets supplemented with 4, 20, 40 and 30 mg/kg, respectively, of Cu, Fe, Mn and Zn from organic chelates and inorganic salts achieved the same body weight gain as those supplemented at the NRC levels (8 mg Cu, 40 mg Fe, 60 mg Mn and 40 mg Zn/kg, respectively) from inorganic salts. However, birds fed a control diet without any supplementation at dietary levels of 7.4-8.8, 60.1-69.2, 14.6-15.4 and 19.1-20.6 mg/kg of Cu, Fe, Mn and Zn, respectively, had decreased feed intake and growth rate. There was no significant difference in the digestibility of Cu in all regions of the small intestine. Throughout the small intestine the apparent absorption of Mn from both organic and inorganic sources was small, whereas the digestibility of Zn seemed to be more complex, exhibiting differences in the apparent absorption due to both mineral source and intestinal site. Therefore, the digestibility of organic Zn was improved (p<0.01) in the ileum compared to inorganic Zn. The digestibility of Zn in the duodenum was smaller (p<0.05) than that in the ileum.

• The Korean Journal of Food And Nutrition
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• v.30 no.6
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• pp.1222-1228
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• 2017

In the current study, we investigated the inhibitory activity of water soluble ${\beta}-glucan$ from oat (Avena sativa) against various digestive enzymes such as ${\alpha}-glucosidase$, sucrase, maltase and glucoamylase. Inhibition of these enzymes involved in the absorption of disaccharide can significantly decrease the post-prandial increase of blood glucose level after a mixed carbohydrate diet. The ${\beta}-glucan$ had the highest documented rate of small intestinal sucrase inhibitory activity (2.83 mg/mL, $IC_{50}$) relevant for potentially managing post-prandial hyperglycemia. Furthermore, we evaluated the effects of ${\beta}-glucan$ on the level of post-prandial blood glucose in animal model. The post-prandial blood glucose levels were tested two hours after sucrose/starch administration, with and without ${\beta}-glucan$ (100, and 500 mg/kg-body weight). The maximum blood glucose levels (Cmax) of ${\beta}-glucan$ administration group were decreased by about 23% (from $219.06{\pm}27.82$ to $190.44{\pm}13.18$, p<0.05) and 10% (from $182.44{\pm}13.77$ to $165.64{\pm}10.59$, p<0.01) in starch and sucrose loading test, respectively, when compared to control in pharmacodynamics study. The ${\beta}-Glucan$ administration significantly lowered the mean, maximum, and minimum level of post-prandial blood glucose at 30 min after meal. In view of the foregoing, it is felt that our findings suggest that ${\beta}-glucan$ from oat serves to reduce post-prandial blood glucose rise secondary to slower absorption of glucose in the small intestine, via carbohydrate hydrolyzing enzymes inhibition.

• Korean Journal of Food Science and Technology
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• v.26 no.6
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• pp.745-749
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• 1994

Animal experiments were conducted to confirm the suppressive effect of green tea on the intestinal absorption and tissue accumulation of toxic heavy metals in rats. When drinking water contaminated with 500 and 5000 times level of water quality standard for lead or cadmium was administrated to rats for 3 weeks, feed intake and body weight gain were not significantly differrent among all groups except for high cadmium group. In the relative weights of target organs, kidney and femur showed a significant difference by heavy metal administration and green tea did not influence on the weights. Green tea showed a suppressing effect on the accumulation of heavy metals in target organs, in which the reducing effect in femur was $25{\sim}45%$ for lead, and 42% for cadmium. As calcium content of femur decreased by heavy metal administration was increased in green tea group, it was concluded that heavy metal accumulation in femur was interrupted by tea beverage.

• Biomolecules & Therapeutics
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• v.19 no.3
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• pp.364-370
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• 2011

The purpose of this study was to investigate the effects of curcumin on the pharmacokinetics of loratadine in rats. The effect of curcumin on P-glycoprotein (P-gp) and cytochrome P450 (CYP) 3A4 activity was evaluated. Pharmacokinetic parameters of loratadine were also determined after oral and intravenous administration in the presence or absence of curcumin. Curcumin inhibited CYP3A4 activity with an IC50 value of 2.71 ${\mu}M$ and the relative cellular uptake of rhodamine-123 was comparable. Compared to the oral control group, curcumin significantly increased the area under the plasma concentration-time curve and the peak plasma concentration by 39.4-66.7% and 34.2-61.5%. Curcumin also significantly increased the absolute bioavailability of loratadine by 40.0-66.1% compared to the oral control group. Consequently, the relative bioavailability of loratadine was increased by 1.39- to 1.67-fold. In contrast, curcumin had no effect on any pharmacokinetic parameters of loratadine given intravenously, implying that the enhanced oral bioavailability may be mainly due to increased intestinal absorption caused via P-gp and CYP3A4 inhibition by curcumin rather than to reduced renal and hepatic elimination of loratadine. Curcumin enhanced the oral bioavailability of loratadine in this study. The enhanced bioavailability of loratadine might be mainly attributed to enhanced absorption in the gastrointestinal tract via the inhibition of P-gp and reduced fi rst-pass metabolism of loratadine via the inhibition of the CYP3A subfamily in the small intestine and/or in the liver by curcumin.

• Journal of Pharmaceutical Investigation
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• v.40 no.5
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• pp.291-296
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• 2010

This study was to investigate the effect of baicalein, an antioxidant, on the bioavailability of nicardipine after orally or intravenously administered nicardipine in rats. Nicardipine was administered orally (12 mg/kg) or intravenously (4 mg/kg) with or without orally administered baicalein (0.4, 2 or 10 mg/kg) to rats. In the inhibitory effect of baicalein on CYP3A4 activity, baicalein inhibited CYP3A4 activity with $IC_{50}$ values of 9.2 ${\mu}M$. The cell-based P-gp activity test using rhodamine-123 also showed that baicalein (30-10 ${\mu}M$, p<0.01) significantly inhibited P-gp activity. Compared with the control group (given nicardipine alone), the area under the plasma concentration-time curve (AUC) was significantly (2 mg/kg, P<0.05; 10 mg/kg, P<0.01) increased by 25.9-60.0%, and the peak concentration ($C_{max}$) was significantly (10 mg/kg, P<0.01) increased by 40.0% in the presence of baicalein after orally administration of nicardipine. Consequently, the relative bioavailability (R.B.) of nicardipine was increased by 1.26- to 1.60-fold and the absolute bioavailability (A.B.) was significantly (2 mg/kg, P<0.05; 10 mg/kg, P<0.01) increased by 26.0-59.9%. Compared to the i.v. control, baicalein did not significantly change pharmacokinetic parameters of nicardipine in i.v. administration. Accordingly, the enhanced oral bioavailability of nicardipine might be mainly due to increased intestinal absorption caused by P-gp inhibition rather than to reduced elimination of nicardipine by baicalein. The increase in the oral bioavailability might be mainly attributed to enhanced absorption in the small intestine via the inhibition of P-gp and reduced first-pass metabolism of nicardipine via the inhibition of the CYP3A subfamily in the small intestine and/or in the liver by baicalein. Based on these results, nicardipine dosage should be adjusted when given concomitantly with baicalein.

• YAKHAK HOEJI
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• v.51 no.6
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• pp.440-446
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• 2007

Arcabose is a competitive inhibitor of the intestinal ${\alpha}$-glucosidases and reduces the postprandial digestion and absorption of carbohydrate and disaccharides. Due to its negligible oral absorption, measuring drug concentration in the plasma is impractical. Thus, the common pharmacokinetic study is not available to determine the bioequivalence of the generic acarbose preparations. The aim of this study is the establishment of pharmacodynamic assessment method for the bioequivalence test of the generic acarbose preparations. Placebo-controlled cross-over ($3{\times}3$) clinical study was conducted in 23 healthy volunteers. Volunteers received a single oral dose of placebo, reference drug ($Glucoby^{(R)}$ 100 mg, Lot # D043) or test drug ($Glucoby^{(R)}$ 100 mg, Lot # E005) just before breakfast, then blood samples for evaluation of serum glucose and insulin levels were taken during for 4 hours. $C_{max},\;AUC_{0-2},\;AUC_{0-4},\;{\Delta}C_{max},\;{\Delta}AUC_{0-2}\;and\;{\Delta}AUC_{0-4}$ of the postprandial plasma glucose level significantly decreased when a single dose of acarbose 100 mg preparations was administered. However, any significant difference was not detected between the groups taken the reference drug and the test drug. These results proposed that the pharmacodynamic protocols of this study is suitable to use for bioequivalence test of acarbose preparations. On the basis of the results of this study and the data of literature on this subject, the standard protocols of bioequivalence study of acarbose preparation are proposed.

• Archives of Pharmacal Research
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• v.28 no.8
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• pp.970-976
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• 2005

The purpose of this study was to investigate the effect of morin, a flavonoid, on the pharmacokinetics of diltiazem and one of its metabolites, desacetyldiltiazem in rats. Pharmacokinetic parameters of diltiazem and desacetyldiltiazem were determined after oral administration of diltiazem (15 mg/kg) in rats pretreated with morin (1.5, 7.5, and 15 mg/kg). Compared with the control group (given diltiazem alone), pretreatment of morin significantly increased the absorption rate constant $(K_a)$ and peak concentration $(C_{max})$ of diltiazem (p<0.05, p<0.01). Area under the plasma concentration-time curve (AUC) of diltiazem in rats pretreated with morin were significantly higher than that in the control group (p<0.05, p<0.01), hence the absolute bioavailability $(AB\%)$ of diltiazem was significantly higher than that of the control group (p<0.05, p<0.01). Relative bioavailability $(RB\%)$ of diltiazem in rats pretreated with morin was increased by 1.36- to 2.03-fold. The terminal half-life $(t_{1/2})$ and time to reach the peak concentration $(T_{max})$ of diltiazem were not altered significantly with morin pretreatment. AUC of desacetyldiltiazem was increased significantly (p<0.05) in rats pretreated with morin at doses of 7.5 and 15 mg/kg, but metabolite-parent ratio (MR) of desacetyldiltiazem was decreased significantly (p<0.05), implying that pretreatment of morin could be effective to inhibit the CYP 3A4-mediated metabolism of diltiazem. There were no apparent changes of $T_{max}$ and $t_{1/2}$ of desacetyldiltiazem with morin pretreatment. Collectively, the pretreatment of morin significantly altered pharmacokinetics of diltiazem, which can be attributed to increased intestinal absorption as well as reduced first-pass metabolism. Based on these results, dose modification should be taken into consideration when diltiazem is used concomitantly with morin or morin-containing dietary supplements in clinical setting.

• Polymer(Korea)
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• v.37 no.4
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• pp.533-538
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• 2013

Sodium chloride is present in our body fluids, and the blood contains approximately 0.9 wt% salt, which plays an important role in maintaining the osmotic pressure. However, the amount of salt intake has consistently increased, and an excessive intake can be the cause of high blood pressure, etc. In this study, it was investigated in vivo and in vitro whether biocompatible ionic polymers with K or Ca ions can be replaced by Na ions through an ion exchange process to be excreted. Among the polymers, Ca-polystyrene sulfonate, K-polystyrene sulfonate, Ca-carrageenan, and Ca-tamarind had an excellent Na exchange ability in the body temperature, simulated gastric fluid and also simulated intestinal fluid. The mechanism of Na removal by absorption and excretion without changing food taste in the mouth through the insolubility properties of these polymers is expected to be a solution for the current problems related with excess sodium intake.

• Journal of Nutrition and Health
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• v.55 no.4
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• pp.441-449
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• 2022

This review is focused on analyzing the limits and shortage of zinc (Zn) for the 2020 Dietary Reference Intakes for Koreans (KDRIs), and provides suggestions for the future establishment of the 2025 KDRIs for Zn. The 2020 KDRIs for Zn have been established to estimate the adequate requirement (EAR), recommended nutrient intakes (RNI), adequate intake (for only 0-5 mon) and tolerable upper intake level (UL). EAR was estimated in 2-stages: the first stage was to construct of the frame of analysis for Zn requirement and the second stage involved a factorial approach by considering the various factors which affect Zn requirement, such as intestinal and urine Zn loss, Zn requirement for growth and development, and Zn absorption rate. For a more precise and accurate establishment of the Zn requirement, we suggest for the following to be considered: 1) considering that Zn is present in minuscule amounts as a trace element in our body, the present values for Zn EAR (as 6-9 mg/d) should be expressed as a decimal point for more accurate DRIs; 2) the frame of analysis for Zn requirement has to be more specifically and should includes the factors which affect Zn requirement; 3) both, the factorial approach and extrapolation method need to be well reviewed and thoroughly understood for establishing precise Zn requirement; 4) currently, human clinical study and balance study (Zn intake, excretion and absorption rate) are limited and more human Zn subject studies are required. All these suggestions are provided to better establish the Zn requirement in the 2025 KDRIs.

• Journal of Pharmaceutical Investigation
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• v.38 no.4
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• pp.255-259
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• 2008

The present study aimed to investigate the in-vitro characteristics of N4-amino acid derivatives of cytarabine for the oral delivery of cytarabine. After the synthesis of L-Ile-cytarabine, L-Leu-cytarabine and L-Arg-cytarabine, the gastrointestinal stability of each prodrug was examined using artificial gastric juice and intestinal fluids. The cellular uptake characteristics of prodrugs were also examined in Caco-2 cells. While L-Ile-cytarabine and L-Leu-cytarabine appeared to be stable in all the tested biological media during 4-hr incubation, L-Arg-cytarabine was rapidly disappeared within 5 min. Accordingly, the cellular uptake of L-Ile-cytarabine and L-Leu-cytarabine was significantly higher than that of its parent drug, cytarabine in Caco-2 cells but the cellular uptake of L-Arg-cytarabine was similar to that from its parent drug. The cellular uptake of L-Ile-cytarabine and L-Leu-cytarabine appeared to be saturable as drug concentration increased from 0.4 to 4 mM. Collectively, L-Ile-cytarabine and L-Leu-cytarabine could be promising candidates to improve the oral absorption of cytarabine via a saturable transport pathway.