• Title/Summary/Keyword: bioavailability of Ca

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Pharmacokinetics of a new anti-HIV agent VP-0501 and development of its amino acid prodrug for improving oral bioavailability (Anti-HIV agent VP-0501의 생체이용성 향상을 위한 아미노산 프로드럭 개발 및 약물동태연구)

  • Cho, Hee-Jeong;Choi, Kyung-Ae;Sung, Ji-Min;Jeong, Sang-Min;Han, Jin-Soo;Kim, Jin-Suk;Shin, Ho-Chul
    • Korean Journal of Veterinary Research
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    • v.46 no.1
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    • pp.7-12
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    • 2006
  • We have studied pharmacokinetics of a new anti-human immunodeficiency virus (HIV) agent VP-0501 and its amino acid prodrug VP-0501AL which is designed to improve oral bioavailability. After oral administration at 100 mg/kg dose in rats (n = 4), VP-0501 was not detectable in plasma (<50 ng/ml), while after the administration of VP-0501AL, VP-0501 was quantitatively detected, at least for 8 hrs, with Cmax of ca. $2.5{\mu}g/ml$ and AUC of $8hr^{\ast}{\mu}g/ml$. When VP-0501 was intravenously administered at 50mg/kg, this compound appeared at a marginal level in plasma with AUC of $2hr^{\ast}{\mu}g/ml$, $t_{1/2}$ of 2 hr, $C_0$ of $0.7{\mu}g/ml$, and MRT of 3 hr. On the other hand, with intravenous VP-0501AL at the same dose, both the prodrug VP-0501AL and its metabolite VP-0501 appeared comparatively at higher level in the plasma: pharmacokinetic parameters of VP-0501AL including $Vd_{\beta}$, AUC, $t_{1/2,{\beta}}$, $C_0$, $CL_{tot}$, and MRT were ca. 2 L/kg, $70hr^{\ast}{\mu}g/ml$, 2 hr, $180{\mu}g/ml$, 0.7 L/hr/kg, and 1 hr, respectively. These results demonstrate that attachment of amino acid alanine to VP-0501 is an effective approach for improvement of its oral bioavailability. Therefore, VP-0501AL is expected to become a new highly bioavailable and potent anti-AIDS drug candidate/lead compound.

Biological Effectiveness of Methionine Hydroxy-analogue Calcium Salt in Relation to DL-Methionine in Broiler Chickens

  • Elwert, C.;de Fernandes, E. Abreu;Lemme, A.
    • Asian-Australasian Journal of Animal Sciences
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    • v.21 no.10
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    • pp.1506-1515
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    • 2008
  • Two feeding trials were conducted to assess the relative bioavailability (RBV) of methionine hydroxy analogue calcium salt (MHA-Ca) in comparison to DL-methionine (DL-Met). Male Ross 308 (1-38 days) and Cobb 500 chickens (1-42 days) were used in studies 1 and 2, respectively. Experimental diets based on wheat and soybean meal or sorghum and soybean meal were fed during three phases. In both experiments graded levels of DL-Met and MHA-Ca were supplemented to Met+Cys deficient basal diets. Additionally, in experiment 1, increasing levels of a DL-Met preparation diluted with corn starch to 65% purity (DL-Met65) were supplemented. Birds were kept in floor pens and feed and water were available ad libitum. Body weights and feed consumption were recorded at the beginning and end of the experimental periods and weight gain and feed efficacy were computed subsequently. At the end of the experiments, a number of birds were slaughtered for carcass evaluation (dressing percentage, breast meat yield). Dose response data were analysed by both ANOVA and nonlinear common plateau asymptotic regression. In both experiments birds responded significantly to increasing levels of either methionine source. However, RBV of MHA-Ca compared to DL-Met was markedly (in many cases significantly) below 84%, the value which would have been expected from MHA-Ca's chemical characteristics. Excluding some extremely low RBV figures of trial 2, RBV of MHA-Ca averaged to about 63% in relation to DL-Met. In addition, supplementation of DL-Met65 allowed confirmation of nonlinear common plateau asymptotic regression to be suitable to determine RBV.

Minerals, Oxalate and Phytate Contents of Recommended Soybean Cultivars in Korea (국산 콩 장려품종의 Minerals, Oxalate 및 Phytate 함량)

  • Kim, Ki-Chan;Hwang, In-Guk;Yoon, Gun-Mook;Song, Hang-Lin;Kim, Hong-Sig;Jang, Keum-Il;Jeong, Heon-Sang
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.38 no.7
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    • pp.870-878
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    • 2009
  • This study was conducted to select the soybean cultivar to minimize the formation of calcium oxalate, and investigate the ingredients for total oxalate (Ox), phytate ($InsP_6$) and minerals such as calcium (Ca), magnesium (Mg), sodium (Na), zinc (Zn), and potassium (K) in 113 recommended soybean cultivars in Korea. Ca content ranged from 0.586 mg/g in Saealkong to 3.177 mg/g in Daolkong, and Mg content ranged from 0.559 mg/g in Taekwankong to 3.085 mg/g of dry seed in Seonheukkong. The total oxalate content ranged from 1.24 mg/g in Seonheukkong to 3.81 mg/g in Ilmikong, and InsP6 content ranged from 0.43 mg/g in Mailikong to 4.72 mg/g of dry seed in Dagikong. In the cross-correlation analysis for the contents of Ca, Mg, Ox and $InsP_6$, Seonheukkong and Danmi2 were selected to minimize the formation of calcium oxalate because the contents of Ca and $InsP_6$ were much higher than the content of Ox. These cultivars could be useful for producing soy foods beneficial to populations at risk for calcium oxalate kidney stones and for improved mineral bioavailability.

Effect of Calcium Compounds from Oyster Shell Bouind Fish Skin Gelatin Peptide in Calcium Deficient Rats (어피 젤라틴 펩티드와 결합한 굴껍질 유래 칼슘 화합물이 칼슘 결핍 흰쥐에 미치는 영향)

  • KIM Gyu-Hyung;JEON You-Jin;BYUN Hee-Guk;LEE Yeon-Sook;LEE Eung-Ho;KIM Se-Kwon
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.31 no.2
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    • pp.149-159
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    • 1998
  • To utilize the oyster shell containing a lot of calcium, we investigated the bioavailability of calcium compounds from oyster shell. First, calcium oxide was prepared by burning of oyster shell at $1200^{\circ}C$. Its purity was approximately $98.5\%$. Calcium compounds, $CaCl_2$, and $CaHPO_4$, from the calcium oxide were prepared by chemical reaction. Effect on calcium absorption by the calcium compounds from oyster shell was improved using fish skin gelatin peptides.(FSGP), which was prepared by enzymatic hydrolysis of fish skin gelatin for 4hr with tuna pyloric caeca crude enzyme (TPCCE). in vitro experiment, calcium absorption by addition of FSGP in a mixture solution of calcium and phosphate was higher approximately $70\%$ than that by control. in vivo using calcium deficient rats, a group taken the diets with $3\%$ FSGP and $CaHPO_4$ was significantly improved amount of calcium and ash in femur and strength of femur. These results suggest that calcium compounds from oyster shell and FSGP could be used as an effective dietary calcium source.

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Changes in Availability of Toxic Trace Elements (TTEs) and Its Effects on Soil Enzyme Activities with Amendment Addition

  • Lee, Sang-Hwan;Park, Misun;Kim, Min-Suk
    • Ecology and Resilient Infrastructure
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    • v.7 no.2
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    • pp.134-144
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    • 2020
  • In-situ stabilization is a remediation method using amendments to reduce contaminant availability in contaminated soil. We tested the effects of two amendments (furnace slag and red mud) on the availability of toxic trace elements (TTEs) and soil enzyme activities (dehydrogenase, phosphatase, and urease). The application of amendments significantly decreased the availability of TTEs in soil (p < 0.05). The decreased availability of TTE content in soils was accompanied by increased soil enzyme activities. We found significant negative relationships between the TTE content assessed using Ca(NO3)2-, TCLP, and PBET extraction methods and soil enzyme activities (p < 0.01). Soil enzyme activities responded sensitively to changes in the soil environment (pH, EC, and availability of TTEs). It could be concluded that soil enzyme activities could be used as bioindicators or ecological indicators for soil quality and health in environmental soil monitoring owing to their high sensitivity to changes in soil.

Bioavailability of Microspheres Containing Felodipine (필로디핀이 함유된 미립구의 생체이용률)

  • 양재헌;나성범;김영일;김남순
    • YAKHAK HOEJI
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    • v.44 no.5
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    • pp.440-447
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    • 2000
  • Microspheres of felodipine, which is one of the calcium channel blocker using a mixture of Eudragi $t^{R}$ RL, L, E, and cellulose on the base of Eudragi $t^{R}$ RS were investigated. Cremopho $r^{R}$ was added to each preparation of polymers in order to increase the release of felodipine from microspheres. Felodipine-loaded microspheres were prepared by a solvent evaporation method, which is based on dispersion of methylene chloride containing felodipine and polymers in 0.5 w/v % polyvinyl alcohol solution. The average diameter based on the size distribution of the felodipine-loaded microspheres was observed to be ca. 40-55 ${\mu}{\textrm}{m}$. A good and smooth surface were showed in all types of the microspheres. The amount of felodipine loaded was over 90 w/w % in all types of microspheres. The dissolution profiles of felodipine from microspheres were similar with each type of polymer, and about a 60 w/w % of the total amount of felodipine loaded to microsphere was released within 7 hours. Dissolution rate of felodipine from the microsphere was increased by addition of Cremophor. After oral administration of the felodipine-loaded microspheres in PVA solution and felodipine alone in PEG solution to rats, respectively, the pharmacokinetic study revealed that the Tmax values of the microspheres were observed in the range of 0.67~l.0 hr while that of the felodipine solution was obtained 0.33 hr. In addition, the AUC of the microspheres at 0 to 7 hr was remarkably increased in comparison to that of felodipine solution. These results revealed that the microspheres based on Eudragit RS could be a good candidate for the controlled release drug delivery system for felodipine.e.e.e.

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Stabilization of As and Heavy Metals in Farmland Soil using Iron Nanoparticles Impregnated Biochar (비소 및 중금속의 식물체 전이감소를 위한 철 나노 입자가 담지된 바이오차의 농경지 토양 안정화제 적용성 평가)

  • Koh, Il-Ha;Kim, Jung-Eun;Park, So-Young;Choi, Yu-Lim;Kim, Dong-Su;Moon, Deok Hyun;Chang, Yoon-Young
    • Journal of Soil and Groundwater Environment
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    • v.27 no.6
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    • pp.1-10
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    • 2022
  • This study assessed the feasibility of iron oxide nanoparticles impregnated with biochar (INPBC), derived from woody biomass, as a stabilizing agent for the stabilization of farmland soil in the vicinity of an abandoned mine through pot experiments with 28 days of lettuce growth. The lettuce grown in the INPBC amended soils increased by more than 100% and the concentrations of inorganic elements (Cu, Ni, Zn) decreased by more than 40%. As, Cd and Pb were not transferred properly from the soils to the lettuce biomass. The bioavailability of arsenic and heavy metals in the INPBC amended soils were decreased by 26%~50%. It seems that the major mechanisms of stabilization were arsenic adsorption on iron oxides, heavy metal precipitation by soil pH increasing and heavy metal adsorption on organic matter. These results revealed that the lower bioavailability of the inorganic pollutants in the soils stabilized using INPBC induced lower transfer to the lettuce. Thus, INPBC could be used as an amendment material for the stabilization of farmland soils contaminated by arsenic and heavy metals. However, a pre-review of the chemical properties of the amended soil must be performed prior to applying INPBC in farmland soil because the concentration of the nutrients in the soil such as available phosphates and exchangeable cations (Ca, Mg, K) could be decreased due to adsorption on the surface of the iron oxides and organic matter.

Characteristics of Agricultural Paddy Soil Contaminated by Lead after Bench-scale In-situ Washing with FeCl3 (납 오염 논토양의 원위치 세척을 위한 FeCl3의 Bench-scale 적용성 평가: 세척전후 토양 특성변화)

  • Koh, Il-Ha;Kim, Gi Suk;Chang, Yoon-Young;Yang, Jae-Kyu;Moon, Deok Hyun;Choi, Yulim;Ko, Myoung-Soo;Ji, Won Hyun
    • Journal of Soil and Groundwater Environment
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    • v.22 no.1
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    • pp.18-26
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    • 2017
  • In a previous study, we assessed the feasibility of ferric chloride ($FeCl_3$) as a washing agent in bench-scale in-situ soil washing to remove Pb from agricultural paddy soil. Herein is a subsequent study to evaluate variations in soil properties after $FeCl_3$ soil washing in terms of fractionation and bioavailability of Pb and chemical properties of the soil. After soil washing, the soil pH decreased from 4.8 to 2.6 and the exchangeable fractions of Pb in the soil increased from 12 mg/kg to 15 mg/kg. Variations in the Pb fractionation of the soil increased Pb bioavailability by almost three-fold; however,the base saturation decreased by 75%. The concentrations of total nitrogen and available phosphate were similar before and after soil washing. The available silicate concentration significantly increased after soil washing but was two times lower than that of soil washed with HCl, which is widely used as a washing agent. This indicates that $FeCl_3$ can be an acceptable washing agent that protects the soil clay structure. The results suggest that soil amendment, such as liming, is needed to recover soil pH, reduce mobility of Pb, and provide exchangeable bases of Ca, Mg, and K as essential elements for the healthy growth of rice plants in reused soil that has been washed.

Effects of Feeding Oxalate Containing Grass on Intake and the Concentrations of Some Minerals and Parathyroid Hormone in Blood of Sheep

  • Rahman, M.M.;Nakagawa, T.;Niimi, M.;Fukuyama, K.;Kawamura, O.
    • Asian-Australasian Journal of Animal Sciences
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    • v.24 no.7
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    • pp.940-945
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    • 2011
  • In order to determine whether oxalate from grasses affects feed intake, blood calcium (Ca) and other blood parameters of adult sheep, two feeding trials were conducted. In Trial 1, one group of sheep received guineagrass (0.47% soluble oxalate) and another group received setaria (1.34% soluble oxalate) for 28 d. In Trial 2, one group of sheep received guineagrass while another group received the same grass treated with an oxalic acid solution (at a rate of 30 g oxalic acid/kg dry matter of hay) for 72 d. All sheep received concentrate mixtures (0.5% of body weight) throughout the experiment. In both trials, it was observed that plasma Ca concentration (11.0-11.7 mg/dl) was significantly (p<0.05) lower in sheep fed high oxalate-containing grasses than in sheep fed low oxalate-containing grasses (12.4-13.7 mg/dl). No differences (p>0.05) were observed in concentrations of magnesium, phosphorus and parathyroid hormone in plasma between the feeding of low and high oxalate-containing grasses. In addition, no differences (p>0.05) were observed in roughage dry mater (DM) intake, total DM intake or body weight of sheep. This study suggests that sheep may consume oxalate-rich forage, but Ca bioavailability may decrease with increasing oxalate levels in the ration.

Stabilization of Arsenic in Paddy Soils Using Stabilizers (논토양 내 비소 불용화에 대한 안정화물질의 처리 효과)

  • Kang, Min Woo;Oh, Sejin;Kim, Sung-Chul;Lee, Sang Soo
    • Korean Journal of Environmental Agriculture
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    • v.38 no.1
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    • pp.17-22
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    • 2019
  • BACKGROUND: Soil contamination of As is a very sensitive environmental issue due to its adverse impact on human health and different characteristics with other heavy metals. With public awareness of As poisoning, there has been growing interest in developing guideline and remediation technologies for As-contaminated soil. The objective of this research was to evaluate the effectiveness of stabilizing amendments and soil dressing methods on the mobility of As in the contaminated rice paddy soils nearby mining area. METHODS AND RESULTS: Different amendments were mixed with surface and subsurface contaminated soils at a ratio of 3% (w/w) and monitored for five months. Three different extractants including 0.01M $CaCl_2$, TCLP, and PBET were used to examine As bioavailability in the soil and the concentration of As in rice grain was also measured with an inductively coupled plasma (ICP) spectroscopy. The results showed that all amendment treatments decreased As concentration compared to the control. Especially, coal mine drainage sludge (CMDS) treatment showed the highest efficiency of decreasing As concentration in the soil and rice grain. The values of Pearson correlation (r) between As concentrations in the soil and rice grain were 0.782, 0.753, and 0.678 for $CaCl_2$, TCLP, and PBET methods, respectively. Especially, $CaCl_2$ method was highly correlated between As concentrations of the soil and soil solution (r=0.719), followed by TCLP (r=0.706), PBET (r=0.561) methods. CONCLUSION: Stabilizing amendments can effectively reduce available As concentration in the soils as well as soil solution, and thereby potentially mitigating risks of crop contamination by As.