• 제목/요약/키워드: bioavailability of Ca

검색결과 79건 처리시간 0.027초

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

  • 조희정;채경애;성지민;정상민;한진수;김진석;신호철
    • 대한수의학회지
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    • 제46권1호
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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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    • 제21권10호
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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.

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

  • 김기찬;황인국;윤건묵;송항림;김홍식;장금일;정헌상
    • 한국식품영양과학회지
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    • 제38권7호
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    • pp.870-878
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    • 2009
  • 본 연구는 국산 113종 콩 장려품종의 total oxalate(Ox), phytate($InsP_6$)와 calcium(Ca), magnesium(Mg), sodium (Na), zinc(Zn), potassium(K)을 분석하여 옥살산칼슘 결정생성을 최소화할 수 있는 품종의 선발 및 안전한 콩 가공식품 제조를 위한 자료를 제시하고자 하였다. 113종의 콩 장려품종에서 Ca과 Mg 함량 분포는 각각 $0.586{\sim}3.177$$0.559{\sim}3.085\;mg/g$이었으며, Ca는 다올콩은 3.177 mg/g으로 가장 높았고, Mg는 선흑콩은 3.085 mg/g으로 가장 높은 함량을 보였다. Ca과 Mg 사이에서 품종간 유의적인 차이가 나타나지 않았다. Ox와 InsP6 함량 분포는 각각 1.24(선흑콩)$\sim$3.81(다원콩)과 0.43(만리콩)$\sim$4.72(다기콩) mg/g 범위이었고, 옥살산칼슘 결정의 저해물질인 $InsP_6$의 함량이 Ox의 함량보다 상대적으로 높은 함량 분포로 존재하였다. 또한 Ca, Mg, Ox 및 $InsP_6$ 함량 사이의 교차상관관계분석을 통해 Ca과 $InsP_6$ 함량이 Ox 함량보다 높은 선흑콩과 단미2가 옥살산칼슘 생성의 잠재적 위험성을 최소화할 수 있는 품종으로 판단되었다.

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

  • 김규형;전유진;변희국;이연숙;이응호;김세권
    • 한국수산과학회지
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    • 제31권2호
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    • pp.149-159
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    • 1998
  • 매년 막대한 양이 폐기되어져 환경오염 문제를 유발시키는 굴껍질에 다량 함유되어 있는 칼슘 성분을 체내 칼슘 공급원으로 이용하기 위하여 굴껍질을 $1200^{\circ}C$로 소성 가공시켜 $98.6\%$의 수율로 산화칼슘을 만들었고, 이로부터 $CaCl_2$$CaHPO_4$ 등과 같은 칼슘화합물을 제조하였다. 여러 가지 효소로 가수분해시켜 얻은 어피 젤라틴 유래 펩티드를 굴껍질 유래 칼슘화합물들에 대한 칼슘 흡수 촉진제로 사용하였는데, in vitro 실험 결과 참치 유문 수 유래 조효소인 TPCCE를 사용하여 4시간 동안 가수분해시켜 얻은 어피 젤라틴 펩티드가 가장 뛰어난 $CaHPO_4$ 침전 저지 효과를 나타내었으며, 무첨가와 비교했을 때 $70\%$의 상승 효과를 나타내었다. 이상의 결과들을 바탕으로 칼슘을 결핍시킨 수컷 흰쥐(SD-Dawley male rats)를 이용하여 in vivo에서 칼슘 흡수 촉진 실험을 실시한 결과, 칼슘 흡수 촉진제로 어피 젤라틴 펩티드가 첨가된 굴껍질 유래 칼슘화합물을 섭취시킨 군들은 대조군에 비해 유의적으로 높은 칼슘 및 회분량을 나타내었으며, $1\%$보다는 $3\%$의 펩티드를 섭취시킨 군들이 좋은 것으로 나타났다. 또한 $CaCl_2$ 섭취군 보다는 $CaHPO_4$ 섭취군들에게서 더 뛰어난 촉진 효과를 볼 수 있었다. 또한 분으로의 칼슘 배출은 대조군의 약 $50\%$이하로 나타나는 것으로 보아 소장내 불용화 칼슘의 형성에 매우 뛰어난 효과를 갖는 것으로 나타났다.

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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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    • 제7권2호
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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.

필로디핀이 함유된 미립구의 생체이용률 (Bioavailability of Microspheres Containing Felodipine)

  • 양재헌;나성범;김영일;김남순
    • 약학회지
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    • 제44권5호
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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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비소 및 중금속의 식물체 전이감소를 위한 철 나노 입자가 담지된 바이오차의 농경지 토양 안정화제 적용성 평가 (Stabilization of As and Heavy Metals in Farmland Soil using Iron Nanoparticles Impregnated Biochar)

  • 고일하;김정은;박소영;최유림;김동수;문덕현;장윤영
    • 한국지하수토양환경학회지:지하수토양환경
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    • 제27권6호
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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.

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

  • 고일하;김지숙;장윤영;양재규;문덕현;최유림;고명수;지원현
    • 한국지하수토양환경학회지:지하수토양환경
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    • 제22권1호
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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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    • 제24권7호
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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.

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

  • 강민우;오세진;김성철;이상수
    • 한국환경농학회지
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    • 제38권1호
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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.