• Title/Summary/Keyword: Oral absorption

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Pharmacokinetics of Oral Administration of Oxytetracycline in Eel, Anguilla japonica (Oxytetracycline의 경구 투여에 따른 뱀장어 체내 약물동태학적 특성)

  • Kim, Jin-Do;Seo, Jung-Soo;Kim, Ju-Wan;Lee, Joo-Seok;Jung, Sung-Hee;Ji, Bo-Young;Kim, Jin-Woo;Kim, Eung-Oh
    • Journal of fish pathology
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    • v.21 no.2
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    • pp.119-127
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    • 2008
  • Oxytetracycline (OTC) has been widely used in eel culture as a therapeutic and prophylactic agent because of its broad-spectrum activity against gram-positive and -negative bacteria. The oral treatment dosage of OTC approved for the treatment of edwardsiellosis, furunculosis and vibriosis in eel is 50 mg/kg/day for 3-7 days in Korea. To determine new optimum dose of OTC in eel, the pharmacokinetics of OTC after single oral administration (100 mg/kg B.W., 200 mg/kg B.W.) in cultured eel, Anguilla japonica was examined. In oral dosage of 100 and 200 mg/kg body weight, the highest plasma concentrations of OTC were 1.19±0.42 ㎍/㎖ and 2.69±0.57 ㎍/㎖, respectively. Plasma concentrations of OTC were not detected after 720 h post-dose in all experiments. The kinetic profile of absorption, distribution and elimination of OTC in plasma wwas calculated fitting to a 1- and 2-compartment model by WinNonlin program. The following parameters were obtained for a single dosage of 100 and 200 mg/kg respectively: 1-compartment model, AUC= 82.48 and 432.68 ㎍*h/㎖, Tmax= 3.93 and 14.24 hr, Cmax= 0.94 and 2.34 ㎕/㎖; 2-compartment model, AUC= 448.73 and 530.65 ㎍*h/㎖, Tmax= 6.37 and 8.96 hr, Cmax= 0.90 and 3.21 ㎕/㎖.

Pharmacokinetics of oxytetracycline in olive flounder (Paralichthys olivaceus) by dipping and oral administration (Oxytetracycline의 약욕 및 경구투여에 따른 넙치(Paralichthys olivaceus) 체내 약물동태학적 특성)

  • Jung, Sung-Hee;Choi, Dong-Lim;Kim, Jin-Woo;Jo, Mi-Ra;Seo, Jung-Soo;Jee, Bo-Young
    • Journal of fish pathology
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    • v.21 no.2
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    • pp.107-117
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    • 2008
  • The pharmacokinetic properties of oxytetracycline (OTC) were studied after dipping and oral administration to cultured olive flounder, Paralichthys olivaceus (600 g). Plasma concentrations of OTC were determined after oral dosage (50, 100 and 200 mg/kg body weight) and dipping (50, 100 and 200 ppm, 1 h) in olive flounder (average 600 g, 23±1℃). Plasma samples were taken at 3, 5, 10, 15, 24, 32, 48, 72, 120, 168 and 240 h post-dose. In oral dosage of 50, 100 and 200 mg/kg, the peak plasma concentrations of OTC, which attained at 3 h post-dose, were 0.34, 0.44 and 1.18 ㎍/㎖, respectively. In dipping of 50, 100 and 200 ppm, those of OTC which also observed at 5 h post-dose, were 0.43, 0.38 and 0.64 ㎍/㎖, respectively. Plasma concentrations of OTC were not measurable at 240 h post-dose in all experiments. The kinetic profile of absorption, distribution and elimination of OTC in plasma were analyzed fitting to a one-compartment model by WinNonlin program. The following parameters were calculated for a single dosage of 50, 100 and 200 mg/kg body weight, respectively: AUC (the area under the concentration-time curve)=31.40, 28.07 and 32.97 ㎍∙h/㎖; T1/2 (half-life)􀆫0.89, 1.12 and 0.43 h; Tmax (time for maximum concentration)= 5.25, 3.70 and 7.30 h, Cmax (maximum concentration)=0.25, 0.38 and 0.61 ㎕/㎖. Following dipping at 50, 100 and 200 ppm, these parameters were AUC􀆫15.51, 14.63 and 19.72 ㎍∙h/㎖; T1/2= 0.75, 0.41 and 0.74 h; Tmax=4.90, 7.08 and 4.68 h, Cmax=0.40, 0.32 and 0.46 ㎕/㎖.

Effect of 2.5 hr-interval single oral combination treatment of Gamisoyo-san with Tamoxifen on the pharmacokinetics profiles of Tamoxifen in rats

  • Kim, Joo-Ik;Ku, Sae-Kwang;Lee, Young-Joon
    • The Journal of Korean Medicine
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    • v.41 no.4
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    • pp.1-11
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    • 2020
  • Objectives: Objectives: The object of this study was to elucidate the possible effects on the pharmacokinetics of tamoxifen after single oral co-administration of Gamisoyo-san (GMSYS) with 2.5 hr-intervals combination therapy of tamoxifen with GMSYS. Methods: After 2.5 hr of 50 mg/kg of tamoxifen treatment, GMSYS 100 mg/kg was administered. The plasma was collected at 30 min before administration, 30 min, 1, 2, 3, 4, 6, 8 and 24 hrs after end of GMSYS treatment, and plasma concentrations of tamoxifen were analyzed using LC-MS/MS methods. PK parameters of tamoxifen were analysis as compared with tamoxifen single administered rats. Results: Although single co-administration with GMSYS with 2.5 hr-interval induced increased trends of plasma tamoxifen concentrations, there are no significant changes on the plasma concentrations of tamoxifen were demonstrated in tamoxifen and GMSYS 100 mg/kg co-administrated rats with 2.5 hr-intervals as compared to those of tamoxifen single 50 mg/kg treated rats, and also GMSYS co-administrated rats did not showed any significant changes on the all pharmacokinetic parameters as compared to those of tamoxifen single formula treated rats. Conclusions: According to the this study, single co-administration of GMSYS with 2.5 hr-intervals did not critically influenced on the oral bioavailability of tamoxifen, suggesting GMSYS did not critically influenced on the absorption and excretion of tamoxifen, the oral bioavailability, when they were co-administered with 2.5 hr-intervals, at the dose levels of tamoxifen 50 mg/kg and GMSYS 100 mg/kg.

CYTOTOXICITY OF DENIAL CAST BASE METAL ALLOYS ON HUMAN ORAL KERATINOCYTES (구강점막 상피세포에 대한 치과 주조용 비귀금속 합금의 세포독성)

  • Choi, Young-Jin;Yook, Jong-In;Chung, Moon-Kyu
    • The Journal of Korean Academy of Prosthodontics
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    • v.37 no.6
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    • pp.717-729
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    • 1999
  • Although many studies on the cytotoxicity of the dental cast base metal alloys and their components have been carried out, the results are rather conflicting because of the different type of cells used and the various experimental procedures taken. Recently a number of scientists have claimed that it would be preferable to focus on the use of cells from relevant specific location of the human bodies. Consequently, the primary cultured oral keratinocyte derived from oral mucous along with nickel chloride and several of widely used dental cast base metal alloys(two Ni-Cr alloys and one Co-Cr alloy)in domestic were selected for this study, from which 1) The amounts of released metal ions were determined using atomic absorption spectrometry, 2) The cytotoxicity of nickel chloride and dental cast base metal alloys was evaluated via MTT assay, and finally, 3) The amounts of released metal ions and the cytotoxicity of nickel chloride were correlated with the cytotoxicity of dental cast base metal alloys And, the results were summarized as follows; 1. Nickel ion from Ni-Cr alloys and Cobalt ion from Co-Cr alloys resulted in maximum releasing rate during first 2h hours, followed by a decrease in releasing rate with time. Chromium ion were found to be minimal in all alloys. 2. In cytotoxic test. with $40{\mu}M,\;80{\mu}M$ of nickel chloride, there were observed an increase in the relative cell number compared to control samples after 24 hours. With $160{\mu}M$, there was found to be no difference in the relative cell number with control, except that 48 hour showed a increase in relative cell number. With $320{\mu}M$, the relative cell number remained constant and decreased after 48 hours, and with $640{\mu}M$, a continuing decrease in relative cell number was observed throughout test period. 3 The sensitivity of primary cultured oral epithelium to nickel was lower compared to the cells used in other studies. 4. CB-80 Soft and Regalloy showed no cytotoxicity to primary cultured oral epithelium and New crown resulted in a slight cytotoxicity. In conclusion, it was shown that the primary cultured oral keratinocytes could be applied successfully as testing cells in cytotoxicity test. Futhermore, the dental cast base metal alloys used in this study were found to be biocompatible.

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Effect of Type I Collagen on Hydroxyapatite and Tricalcium Phosphate Mixtures in Rat Calvarial Bony Defects

  • Kim, Jung-Hwan;Kim, Soung-Min;Kim, Ji-Hyuck;Kwon, Kwang-Jun;Park, Young-Wook
    • Journal of the Korean Association of Oral and Maxillofacial Surgeons
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    • v.34 no.1
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    • pp.36-48
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    • 2008
  • To repair bone defects in the oral and maxillofacial field, bone grafts including autografts, allografts, and artificial bone are used in clinical dentistry despite several disadvantages. The purpose of this study was to evaluate new bone formation and healing in rat calvarial bone defects using hydroxyapatite (HA, $Ca_{10}[PO_4]_6[OH]_2,\;Bongros^{(R)}$, Bio@ Co., KOREA) and tricalcium phosphate (${\beta}-TCP,\;Ca_3[PO_4]_2$, Sigma-Aldrich Co., USA) mixed at various ratios. Additionally, this study evaluated the effects of type I collagen (Rat tail, BD Biosciences Co., Sweden) as a basement membrane organic matrix. A total of twenty, 8-week-old, male Sprague-Dawley rats, weighing 250-300g, were divided equally into a control group (n=2) and nine experimental groups (n=2, each). Bilateral, standardized transosseous circular calvarial defects, 5.0 mm in diameter, were created. In each experimental group, the defect was filled with HA and TCP at a ratio of 100:0, 80:20, 70:30, 60:40, 50:50, 40:60, 30:70, 20:80, and 0:100 with or without type I collagen. Rats were sacrificed 4 and 8 weeks post-operation for radiographic (standardized plain film, Kodak Co., USA), histomorphologic (H&E [Hematoxylin and Eosin], MT [Masson Trichrome]), immunohistochemical staining (for BMP-2, -4, VEGF, and vWF), and elementary analysis (Atomic absorption spectrophotometer, Perkin Elmer AAnalyst $100^{(R)}$). As the HA proportion increased, denser radiopacity was seen in most groups at 4 and 8 weeks. In general radiopacity in type I collagen groups was greater than the non-collagen groups, especially in the 100% HA group at 8 weeks. No new bone formation was seen in calvarial defects in any group at 4 weeks. Bridging bone formation from the defect margin was marked at 8 weeks in most type I collagen groups. Although immunohistochemical findings with BMP-2, -4, and VEGF were not significantly different, marked vWF immunoreactivity was present. vWF staining was especially strong in endothelial cells in newly formed bone margins in the 100:0, 80:20, and 70:30 ratio type I collagen groups at 8 weeks. The calcium compositions from the elementary analysis were not statistically significant. Many types of artificial bone have been used as bone graft materials, but most of them can only be applied as an inorganic material. This study confirmed improved bony regeneration by adding organic type I collagen to inorganic HA and TCP mixtures. Therefore, these new artificial bone graft materials, which are under strict storage and distribution systems, will be suggested to be available to clinical dentistry demands.

Subacute Oral Toxicity of Chitosan Oligosaccharides on Sprague Dawley Rats

  • Kim, Se-Kwon;Jeon, You-Jin;Park, Pyo-Jam
    • Proceedings of the Korean Society of Fisheries Technology Conference
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    • 2000.05a
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    • pp.88-89
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    • 2000
  • Chitosan is derived from chitin by deacetylation in the presence of alkali, which is a copolymer consisting of $\beta$-(1longrightarrow4)-2-acetamido-D-glucose and $\beta$-(1longrightarrow4)-2-amino-D-glucose units with the latter usually exceeding 80% (Arvanitoyannis et al., 1998). Chitosan has been developed as new physiological material since it possesses antibacterial activity, hypocholesterolemic activity and antihypertensive action. However, even though chitosan has very strong functional properties in many areas, its high molecular weight and high viscosity may restrict the use in vivo. In addition, there is little doubt that such properties will influence absorption in the human intestine. Recently, studies on chitosan have attracted interest for converted chitosan to oligosaccharide, because the oligosaccharide possesses not only water-soluble property but also versatile functional properties such as antitumor activity, immune-enhancing effects, enhancement of protective effects against infection with some pathogens in mice, antifungal activity, calcium absorption accelerating effect (Jeon et al., 1999) and antimicrobial activity. There is, however, little information on the toxicity of chitosan oligosaccharide. (omitted)

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Deposition of Inhaled Smoke Particles Produced by Fire (화재에 의한 흡입연기의 호흡기 내 침착에 관한 연구)

  • Goo, Jae-Hark
    • Fire Science and Engineering
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    • v.21 no.2 s.66
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    • pp.64-73
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    • 2007
  • The absorption characteristics of hazardous materials onto human body and defense mechanism differ from each other region within the respiratory tracts, thus adverse health effects of inhaled smokes are associated with not only the concentration but also the location of the particles deposited. In this work, the deposition fraction per surface area and the deposition sites of the smoke particles in human respiratory tracts for each rest and light exercise conditions together with oral and nasal breathing were calculated by using segmental volume tracking method. The results would be used for deriving the amount of absorption of hazardous materials onto human body, thus contribute to the health risk assessments of inhaled fire smokes.

Bioavailability of Commercially Available Aspirin Tablets in Human (시판 아스피린 정제의 생체내 이용율)

  • Lee, Jin-Hwan;Choi, Jun-Shik;Baik, Chai-Sun;Burm, Jin-Pil
    • Journal of Pharmaceutical Investigation
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    • v.19 no.3
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    • pp.131-136
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    • 1989
  • This study was attempted to investigate the dissolution rate and the bioavailability after oral administration of commercially available aspirin tablets in normal volunteers. The dissolution test was conducted in artificial gastric juice using basket method with three aspirin preparations (A, B and C) which were chemically equivalent. The results were as follows; The dissolution rate was higher in the order of three different brand B>A >C. Area under the blood concentration and peak blood concentration were larger in the order of brand A>B>C. Absorption rate constant and peak time were larger in the order of brand B>A>C, and there was a little difference in elimination rate constant and biological half-life. The correlation of the dissolution rate and absorption rate constant, as well as correlation of the dissolution rate and peak time showed significant linear relationship respectively. From the results of this experiment, it can be concluded that the bioavailability of aspirin tablets showed much difference according to commercial preparations, and that the bioavailability of aspirin tablets in human may be predicted from the results of dissolution rate studies.

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Preparation and Evaluation of Solid lipid Microspheres Containing Cyclosporine A (사이클로스포린을 함유한 고형 지질미립구의 제조와 평가)

  • 양수근;박준상;최영욱
    • YAKHAK HOEJI
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    • v.39 no.5
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    • pp.487-494
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    • 1995
  • Solid lipid microspheres (SLMs) were prepared using various lipids and solidifying agents, in order to enhance the gastrointestinal absorption of Cyclosporine A (Cs A) which is a practically water-insoluble drug with low systemic bioavailability. Egg lecithin and HCO-60 (polyoxyethylated 60 mol, hydrogenated castor oil) were used as lipids. Stearic acid and stearyl alcohol were used as solidifying agents. Emulsion concentrates containing Cs A were prepared by mixing the melted lipid and solidifying agent with water, employing bile salts as a cosurfactant. SLMs were obtained by dispersing the warm emulsion concentrate in cold distilled water under mechanical stirring, followed by freeze drying. Physical characteristics of each SLM were investigated by particle size analysis, optical microscopy and scanning electron microscopy. Mean particle size of SLMs was in the range of 30 to 40.mu.m. The SLMs were in good appearance with spherical shape before freeze drying, but were deformed partially after freeze drying. Drug loading efficiencies of SLMs were observed as high as 80 to 90% in average. The systemic bioavailability of Cs A from different SLM formula was investigated in rats following oral administration. Cs A in whole blood was extracted and assayed by HPLC. SLMs revealed the higher bioavailabilities than the standard formula based on the marketed product. SLMs might have several advantages over standard formula for enhanced gastrointestinal absorption, controlled release properties, high loading capacity of the water-insoluble drug, and feasibility of solid dosage forms with better stability in storage.

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Anti-Oxidant Effects of Highly Bioavailable Curcumin Powder in High-Fat Diet Fed- and Streptozotocin-Induced Type 2 Diabetic Rats

  • Paik, Jean Kyung;Yeo, Hee Kyung;Yun, Jee Hye;Park, Hyun-Ji;Jang, Se-Eun
    • The Korean Journal of Food And Nutrition
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    • v.32 no.2
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    • pp.133-137
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    • 2019
  • Curcumin is a hydrophobic polyphenol extracted from turmeric that exhibits a variety of biological functions has albeit with limited efficacy as a functional food material owing to its low absorption when administered orally. The newly developed curcumin powder formulation exhibits improved absorption rate in vivo. This study evaluates the anti-oxidant effects of $Theracurmin^{(R)}$ (TC), which is highly bio-available in curcumin powder. The antioxidant activity of TC was investigated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging activity, ferrous reducing antioxidant power (FRAP) assays, NO radical, superoxide radical, $H_2O_2$ scavenging activity, and total antioxidant capacity (TAC). Additionally, we evaluated the antioxidant activity of TC in high-fat diet (HFD)-fed streptozotocin (STZ)-induced Type 2 diabetic rats. As a result of oral administration of TC for 13 weeks in type 2 diabetic rats, the group administration of 2,000 mg/kg significantly increased FRAP, superoxide dismutase (SOD), and reduced the level of glutathione (GSH) in liver tissue 1.9, 1.2, and 1.2-times, respectively. Furthermore, serum TAC levels increased by 1.3-fold after the rats were administered with a dose of 500 mg/kg. These results were consistent with the in vitro assay results. In conclusion, TC exhibited its potential as a functional food material through its antioxidant properties.