• Title/Summary/Keyword: 경구흡수율

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Application of Oral Absorption in Establishment of AOEL for Pesticides and Occupational Risk Assessment for farm worker (경구흡수율을 반영한 농약의 AOEL 설정 및 농작업자 위해성 평가)

  • You, Are-Sun;Hong, Soonsung;Lee, Je Bong;Lee, Seungdon;Ihm, Yangbin
    • The Korean Journal of Pesticide Science
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    • v.18 no.4
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    • pp.342-349
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    • 2014
  • Methods of establishment of AOEL (Acceptable Operator Exposure Level), application of oral absorption by country, and calculation of exposure dose for operator risk assessment in USA, EU and Korea were investigated. Oral absorption of 141 active substances for pesticides was also investigated, then operator risk assessment was conducted with AOEL including oral absorption and Korean AOEL. Internal dose converted to external dose with oral or dermal absorption in USA and EU, but external dose to which oral absorption was not applied was used for establishment of AOEL in Korea. Oral absorption of 50 active substances among 141 were below 80%. In case of application of oral absorption as a correction factor in below 80%, AOELs of about 36% active substances were considered to be lower than the current Korean AOELs. Operator risk assessment of 28 active substances among 50 active substances with oral absorption below 80% was conducted with EU AOELs. TER (Toxicity Exposure Ratio) of 12 plant protection products including chlorothalonil WG (Water-dispersible Granule) was less than 1 and the risk was high. Operator risk assessment of 24 active substances among 50 active substances with oral absorption below 80% was conducted with Korean AOELs. TER of 6 plant protection products including chlorothalonil WG were less than 1 and the risk was high. Operator risk assessment of 4 plant protection products not having Korean AOEL was conducted with converted EU AOEL into AOEL not including oral absorption. The results indicated TER of 4 products including daminozide WP (Wettable Powder) was over 1 and risk was low. 22 products except 6 products such as oxadiagyl SC (Suspension Concentration) were shown the same results of risk assessment between EU AOELs and Korean AOELs. As a result, it was considered that AOELs including oral absorption was possible to be used for operator risk assessment. It was considered operator risk assessment with AOEL including oral absorption was more like real assessment method, and improvement of assessment was needed for application to evaluate pesticides in registration.

Experiment to Improve Bioavailability and Oral Absorption of Solubilized Curcumin Using Beta-cyclodextrin and Lysine (Beta-cyclodextrin과 Lysine을 이용한 가용화 커큐민 생체 이용률 및 경구 흡수율 개선 확인 실험)

  • Ye Jin Hwang;Hyeon Woo Kim;Seo Kyung Lee;Ji Hoon Park;Sang Yoon Lee;Jae Seon Kang
    • Journal of Life Science
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    • v.34 no.8
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    • pp.548-557
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    • 2024
  • Curcumin, the primary active compound in Curcumae Radix of the ginger family, exhibits a range of therapeutic effects, including blood sugar regulation, immunoregulation, antioxidant, antibacterial, and antitumor activities. However, its poor water solubility and chemical instability result in suboptimal pharmacokinetics with low oral absorption (0.18%) and bioavailability, thus limiting its efficacy. To overcome these limitations, this study aimed to enhance the oral absorption and bioavailability of curcumin by incorporating lysine and β-cyclodextrin. Following oral administration of solubilized cur- cumin, blood samples were collected to assess the oral absorption rate. Solubilized curcumin showed an approximately 1.55-fold increase in absorption at 120 min compared to its non-solubilized form. Furthermore, intravenous administration followed by blood analysis showed a 25-fold increase in bio- availability at 61 min for the solubilized curcumin compared to the non-solubilized variant. In conclusion, employing lysine for dispersion and stabilization, combined with β-cyclodextrin to enhance solubility, significantly improves curcumin's oral absorption and bioavailability. The results of this experiment are expected to lead to the development of herbal medicines and pharmaceuticals that amplify curcumin's anti-inflammatory, anti-tumor, and blood-sugar-regulation effects.

Pharmacokinetics and the Intestinal Permeability of Amaranth in Rats (적색식용색소인 아마란스의 약동학 특성 및 위장관 투과도 연구)

  • Han, Youjin;Goo, Soo Hyeon;Nam, So Jeong;Kang, Yun Ju;Kwon, Mihwa;Song, Im-Sook
    • Journal of Life Science
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    • v.27 no.7
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    • pp.812-816
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    • 2017
  • Although amaranth, a red-colored tar dye, is usually used in foods, cosmetics, and pharmaceutics, its bioavailability and intestinal absorption have not previously been investigated. Therefore, the purpose of this study was to investigate the pharmacokinetics properties and intestinal permeability of amaranth in rats following the intravenous and oral administration of this dye. Amaranth rapidly disappeared from the plasma following the intravenous injection, with a half-life of 38.8 minutes. However, the plasma concentration of amaranth was increased to 400 minutes following the oral administration of amaranth, and the absorption time and bioavailability of amaranth were calculated to be 356 minutes and 55.6%, respectively. This suggests that once amaranth exists in the gut, this dye may be efficiently and effectively absorbed. Consistent with this result, the intestinal permeability of amaranth was comparable to atenolol, a marker compound of moderate permeability, and to one-third of caffeine's intestinal permeability (a highly permeable compound). In conclusion, a significantly long absorption time and substantial intestinal absorption of amaranth was observed following the oral administration of amaranth at a dose of 300 mg/kg in rats, despite the rapid elimination of this dye from the plasma. These results may suggest the necessity of a careful and limited use of amaranth dye when it is added to food, lip-care cosmetics, and orally administered pharmaceutics.

LC15-0133, a DPP IV Inhibitor: Efficacy in Various Animal Models (LC15-0133, DPP IV 저해제: 여러 동물 모델에서의 효능)

  • Yim, Hyeon-Joo
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2008.04a
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    • pp.5-20
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    • 2008
  • GLP-1-based drugs (GLP-1 analogues and DPP IV inhibitors) and incretin mimetics are currently one of the most exciting classes of agents for type II diabetes. GLP-1, a gut peptide, is an incretin that potentiates glucose-dependent insulin release from the pancreas, slows GI-transit and stimulates the proliferation of beta-cells. DPP IV inhibitors act like incretins by inhibiting DPP IV which inactivates GLP-1. LC15-0133 is a competitive, reversible DPP IV inhibitor ($IC_{50}$ = 24 nM, Ki=0.247 nM) with excellent selectivity over other critical human proteases such as DPP II, DPP 8, elastase, trypsin. and urokinase. LC15-0133 showed long half-life and good bioavailability in rats and dogs. Inhibition of plasma DPP IV activity by LC15-0133 was kept more than 50% 24 hours after oral dosing in rats and dogs at 0.1 mg/kg and 0.02 mg/kg, respectively. The Minimum effective doses of LC15-0133 were 0.01 mg/kg for lowering blood glucose excursion during oral glucose tolerance test and 0.1 mg/kg for increasing glucose-induced GLP-1 response in C57BL/6 mice. Repeat oral administration of LC15-0133 for 1 month delayed the progression to diabetes and reduced HbA1c levels in a dose-dependent manner in Zucker Diabetic Fatty rats. In conclusion, LC15-0133 is a novel, potent, selective and orally active DPP IV inhibitor and showed an excellent blood glucose lowering effects in various animal models.

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Laser Micro Machining in MEMS (레이저를 이용한 미세가공)

  • 윤경구;이성국;김재구;최두선;신보성;황경현
    • Proceedings of the Optical Society of Korea Conference
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    • 2000.08a
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    • pp.48-49
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    • 2000
  • 최근 몇 년 동안 레이저는 품질과 신뢰성의 계속적인 향상으로 인하여 여러 산업 응용분야에서 폭넓게 사용되어 지고 있다. 재료가공에 있어서 레이저의 적용분야는 금속의 절단, 용접 및 드릴링, 세라믹의 스크라이빙, 플라스틱과 복합재료의 절단 및 여러 가지 재료의 마킹, 등을 포함한다. 이러한 가공 메카니즘은 레이저의 조사에 의하여 재료를 용융, 증발시키는 열적 메카니즘이다. 특히 요즘에는 자외선 영역의 조사와 높은 빔의 세기에 의해 다른 종류의 에너지 전달 메카니즘이 가능한 UV 영역의 엑사이머 레이저의 사용이 증가하고 있다.$^{(1)}$ 이러한 엑사이머 레이저가 기존의 다른 레이저에 비해서 갖는 이점은 다음과 같다. 첫째, 모든 금속이 엑사이머 레이저에 대해서는 높은 흡수율을 가지므로 레이저 에너지가 가공 에너지로 효율적으로 변환되기 때문에 얇은 표면층에서 완전히 흡수하게 된다. (중략)

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Two Cases of Gitelman's Syndrome Diagnosed by Renal Clearance Study (신장청소검사를 이용하여 진단한 Gitelman 증후군 2례)

  • Kim, Tae Hwa;Kim, Seung Jun;Seo, Yu Kyung;Shim, Jung-Yeon;Jung, Hye Lim;Park, Moon Soo;Kum, Dong Hyuk
    • Clinical and Experimental Pediatrics
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    • v.45 no.3
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    • pp.413-417
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    • 2002
  • Gitelman's syndrome is an autosomal recessive disorder characterized by hypokalemic metabolic alkalosis, hypomagnesemia, and hypocalciuria that has recently been reported to be linked to thiazide- sensitive Na-Cl cotransporter gene mutation. In this study, we performed renal clearance studies to differentiate Gitelman's from Bartter's syndrome and to confirm the diagnosis in two patients clinically diagnosed with Gitelman's syndrome. Each patient was hydrated by 20 mL/kg body weight of oral water within 30 minutes, which was followed by intravenous half saline. When urinary flow reached 10 mL/min, samples of urine and serum were obtained to calculate the osmolar clearance, free water clearance, chloride clearance, and distal fractional chloride reabsorption. Subsequently, furosemide or hydrochlorothiazide was administered. Samples were collected and the same parameters were calculated. In our patients, chloride clearance was increased more than 10 times after furosemide administration(2.1 : 25.7 and 2.2 : 27.4 mL/min/100 mL GFR), but not increased after hydrochlorothiazide treatment(2.1 : 1.6 and 2.2 : 2.6 mL/min/100 mL GFR). And the distal fractional chloride reabsorption was significantly decreased by furosemide injection (73% : 15% and 75% : 4.6%), whereas hydrochlorothiazide had no effect on it(73% : 63% and 75% : 78%). These findings indicate that our patients have a defect in thiazide-sensitive Na-Cl cotransporter in the distal tubule, which is compatible with the pathophysiology of Gitelman's syndrome.

The Effects of Levan on Blood Lipids and the Absorption of Calcium in Rats Fed a Low Calcium Diet (레반의 혈장지질 감소와 칼슘흡수율 증가 효과)

  • No, Jung-Ran;Park, Sun-Young;Kim, Mi-Kyoung;Jo, Han-Young;Lee, In-Young;Ly, Sun-Yung
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.36 no.1
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    • pp.51-57
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    • 2007
  • Levan, the fructose polymer is an indigestible carbohydrate regularly consumed by humans. Its physiological functions, in terms of hypocholesterolemic effect and calcium metabolism, have not been well documented. The objective of this study was to investigate the effects of levan on blood lipids and the calcium absorption ratio in rats fed a 0.1% low calcium diet. Thirty rats were divided into three groups and fed a 0.1% low calcium diet (control) or low calcium diets containing either 2.5% levan or 5% levan for eight weeks. The blood lipid and biomarkers relevant to Ca metabolism (urinary Ca and hydroxyproline), the femoral weight and the Ca contents were determined. The body weight gains were lower in the 5% levan group than the control group. Plasma concentrations of triacylglycerol and LDL-cholesterol decreased in the 5% levan group, compared to the control group, but the atherogenic indice were not affected. Blood alkaline phosphatase activity, Ca and urinary hydroxyproline excretion levels were not different in the three groups. The net calcium absorption in rats fed a 5% levan diet was greater than rats fed the control diet, while the femoral weights and Ca contents were not significantly different in the three groups. We concluded that a 5% levan diet could both enhance the calcium absorption and improve the lipid profiles in rats fed a low calcium diet.

Development of a Method for Producing Liposome Ascorbic acid with Increased Bio-absorption (생체 흡수율이 증가된 liposomal ascorbic acid 제조법 개발)

  • Cha, Ji Hyun;Woo, Young Min;Jo, Eun Sol;Cha, Jae Young;Lee, Sang Hyeon;Lee, Keun Woo;Kim, Andre
    • Journal of Life Science
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    • v.32 no.3
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    • pp.232-240
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    • 2022
  • Various methods are known for preparing liposomes, the simplest being the Bangham method which has been widely used. Although it is possible to produce liposomes effectively on a small experimental level with this approach, large-scale production cannot be easily performed due to difficulties in removing the organic solvent and the size of the reactor required to form the lipid film. On the other hand, emulsion can mass produce tons of liposomes with uniform particles but has the disadvantage of a significantly low capture rate. This study therefore developed an optimal liposome processing method using heat with improved capture rate and stability, and bio-absorption experiments were performed by oral administration to SD rat alongside capture rate, particle size, and zeta potential. Through the heating method, a small and uniform liposome of about 214 nm was formed and the capture rate was 38.67%, confirming that the liposome prepared by heating has a higher capture rate than the 26.46% achieved through emulsion. Comparing blood concentrations, it showed a 1.5 to 2 fold increase in all groups, gradually decreasing until 4-12 hr. The highest blood concentration of ascorbic acid powder was about 12.017 ㎍/ml, the emulsion liposome 13.871 ㎍/ml, and the heating liposome 16.322 ㎍/ml, thereby showing an improved absorption rate.

The Effect of Exercise on the Conversion Rate of Ingested Glueose to Glycogen in the Hindlimb Skeletal Muscles in Rats (흰위에서 운동부하후 경구투여한 Glucose가 특성이 다른 골격근에서 Glycogen으로 합성되는 속도)

  • Jung, Kyung-Hwa;Kim, Jong-Yeon;Kim, Yong-Woon;Lee, Suck-Kang
    • Journal of Yeungnam Medical Science
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    • v.5 no.2
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    • pp.79-86
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    • 1988
  • In the present study the effect of exercise on the conversion rate of ingested glucose to glycogen in the different types of hindlimb skeletal muscles in Sprague-Dawley male rats was studied. The amounts of synthetized glycogen from ingested glucose of fast-twitch white(WV), fast-twitch red(RV), mixed type of fast-twitch white and red(EDL), and slow-twitch(SOL) muscles were determined at 30 and 90 min. after ingestion of 25% glucose solution which contained $^{14}C$-glucose($2m{\ell}(1uCi)$/100gm B. W.)in control and exercise loaded rats. The result was summarized as follows : The about 55% at 30 min. and 70% at 90 min. after glucose ingestion were absorbed from gastrointestinal tract. This result shows no effects of exercise on absorption rate from gastrointestinal tract. The amount of synthetized glycogen of SOL from ingested glucose at 30 and 90 min. after glucose ingestion were highest, whether WV were lowest in hindlimb skeletal muscles in control and exercise loaded rats. In the exercise loaded rats, the amounts of synthetized glycogen of SOL, RV, and EDL at 90 min. after glucose ingestion was much higher than control rats, but not different in WV between exercise-loaded and control rats. At 30 min. after glucose ingestion, only SOL of exercise loaded rats was higher than control rats. In the control rat, the synthesis of glycogen was almost completed during initial 30 minutes. On the other hand, in the exercise loaded rat, except WV was opposite result of control rats, i. e., amounts of synthetized glycogen were major during late period. The amount of synthetized glycogen of liver at 30 and 90 min. after glucose ingestion in exercise loaded rats was higher than control rats. The rate of glycogen synthesis in control and exercise loaded rats were higher between 30-90 minute than initial 30 minute.

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