• Title/Summary/Keyword: HPLC blood concentration

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The Studies on the Physiological Active Substances of Mugwort Components for the Utilization to the Foods of Animal Husbandry (축산식품에 이용하기 위한 쑥 성분중의 생리활성에 관한 연구)

  • Lee, Chi-Ho
    • Proceedings of the Korean Society for Food Science of Animal Resources Conference
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    • 1998.05a
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    • pp.37-54
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    • 1998
  • This study was conducted to investigate the effects of mugwort extracts on the blood ethanol concentration, liver function and low level of cadmuim(Cd) in rats. The effects of mugwort extracts on the blood ethanol concentration was studied in Sprague-Dawley rats (10 weeks old) administered p.o. with 25% ethanol (5g/1kg body weight) and then injected with mugwort extracts (at the 2% levels of daily feed consumption compared with the concentration of catechins level in mugwort extracts) in caudal vein. SD rats were divided into five groups : control group (CON-E, only ethanol and 0.85% saline sol'n treated instead of each extracts), water extracts of mugwort treated to the control (MDW-E), ethanol extracts of mugwort treated to the control (POH-E). And then rat plasma of each time (0hr, 1hr, 2hr, 3hr) was investigated ethanol concentration by gas chromatography. Another rats were measured at the time of 0 and 5hr for the test of GOD(Glutamic Oxaloacetic Transaminase) and GPT(Glutamic Pyruvic Transaminase). Components of each extracts were analyzed by using high performance liquid chromatography. The effects of mugwort extracts on the liver function were studied in culture of rat hepatocyte composed of three groups : Control group and two groups treated with each extracts (1% & 2% MDW, 1% & 2% MOH). Condition of rat hepatocytes cultured for 36hr at $37^{\circ}C$(5% $CO_2$ incubator), number of cells, GOT and GPT activity were investigated. The results obtained were summarized as follows ; 1. Catechins level of mugwort extracts was $8{\sim}10mg/100g(MDW)$, $3{\sim}4mg/100g(MOH)$ 2. The contents of (-)-Epigallocatechin was high in MDW 3. The effects of mugwort extracts on the blood ethanol concentration were as follows; 1) The order in ethanol degradation efficiency was MDW-E > MOH-E > CON-E. 2) Ethanol concentration significantly decreased (p<0.05) in MDW-E and MOH-E. 4. The effects of mugwort extracts on the liver function were as follows; (rat hepatocytes cultured for 36hr at $37^{\circ}C$) 1) Cells condition of MDW-L was better than other groups. 2) The order in number of cells (rat hepatocytes) was 2% MDW-L >1% MDW-L >1% MOH-L > Con-L > 2% MOH-L 5. Cd treatment increased concentrations of hepatic GSH level, and decreased GOT activity in plasma. Therefore, this results suggest that the effects of mugwort extracts may an important rols in degradation ethanol and recovery liver function in body. Also, Mugwort extracts may modify the toxicities of Cd in Cd-treated rats and play an important roles in preventing the liver from various toxicants including Cd in Cd treated rats.

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Anti-obesity effects of cultivated ginseng, -wild simulated ginseng and -red ginseng extracts (인삼, 산양산삼 및 홍삼 추출물의 항비만 효과)

  • Kim, Ha-Rim;Lee, Chang-Hyun;Jung, Mun Yhung;Kim, Jong-Seok;Kim, Hong-Jun;Jeon, Hye-Sook;Lee, Seung-Hyun;Kim, Ji-Hyun;Shin, Min-Ji;Ma, Sang-Yong;Kwon, Jin;Oh, Chan-Ho
    • Herbal Formula Science
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    • v.27 no.4
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    • pp.269-284
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    • 2019
  • This study was to investigate whether cultivated ginseng (CG), cultivated wild simulated ginseng (CWG) and cultivated red ginseng (CRG) extracts influences on the obesity. The saponin contents of 3 kinds of ginsengs were analysed by HPLC-ESI-TOF-MS. Total saponin contents were determined in CG on the most contents and since red ginseng has the highest PD (protopanaxadiol type) / PT (protopanaxatriol type) ratio, there may be differences between ginseng, wild ginseng, and red ginseng with respect to their pharmacological effects. Male C57BL/6J mice were fed a normal diet(N), HFD (60% Kcal fat, C), HFD with CG, CWG and CRG extracts (800 mg/kg) for 5 weeks. We observed change of total body weight, degree of hepatic lipid accumulation and immunohistochemical change of GLP-1 and insulin-secreting cells. Also this study attempts to use the physiological analysis method to analyze the changes of blood lipids, insulin and leptin concentration. The change of body weight and size of accumulated lipid droplets in liver lobules decreased in all of the experimental groups than the control(C) group. In the pancreas, the immunohistochemical density of insulin-secreting cells were significantly stronger in the CWG and CRG than C group. The levels of serum insulin and leptin significantly decreased 55.6%, 54.3% respectively in CWG and CRG. The changes of triglyceride, total cholesterol in serum decreased in CRG than the C group. Obesity related CG, CWG and CRG extracts might have contribute to improvement of obesity by regulating the levels of blood lipids and biochemical indicator of fat accumulation.

Pharmacokinetics of 11-Hydroxyaclacinomycin X (ID-6105), a Novel Anthracycline, after i.v. Bolus Multiple Administration in Rats

  • Yoo Bo-Im;Ahan Kwang Bok;Kang Min Hee;Kwon Oh-Seung;Hong Young-Soo;Lee Jung Joon;Lee Hong Sub;Ryu Jung Su;Kim Tae Yong;Moon Dong-Cheul;Song Sukgil;Chung Youn Bok
    • Archives of Pharmacal Research
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    • v.28 no.4
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    • pp.476-482
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    • 2005
  • We investigated the pharmacokinetics of 11-hydroxyaclacinomycin X (ID-6105), a novel anthracycline, after intravenous (i.v.) bolus administration at a multiple dose every 24 h for 5 days in rats. To analyze ID-6105 levels in biological samples, we used an HPLC-based method which was validated in a pharmacokinetic study by suitable criteria. The concentrations of ID-6105 after the multiple administration for 5 days were not significantly different from the results after the single administration. The $t_{1/2\alpha}, t_{l/2\beta}, V_{dss}, and CL_{t}$ after the multiple administration were not significantly different from the values after the single administration. Moreover, the concentrations of ID-6105 1 min at day 1-5 after i.v. bolus multiple administration did not show the significant difference. Of the various tissues, ID-6105 mainly distributed to the kidney, lung, spleen, adrenal gland, and liver after i.v. bolus multiple administration. ID-6105 concentrations in the kidney or lung 2 h after i.v. bolus administration were comparable to the plasma concentration shortly after i.v. bolus administration. However, the ID-6105 concentrations in various tissues 48 h after i.v. bolus administration decreased to low levels. ID-6105 was excreted largely in the bile after i.v. bolus multiple administration at the dose of 3 mg/kg. The amounts of ID-6105 found in the bile by 12 h or in the urine by 48 h after the administration were calculated to be $14.1\% or 4.55\%$ of the initial dose, respectively, indicating that ID-6105 is mostly excreted in the bile. In conclusion, ID-6105 was rapidly cleared from the blood and transferred to tissues, suggesting that ID-6105 might not be accumulated in the blood following i.v. bolus multiple dosages of 3 mg/kg every 24 h for 5 days. By 48 h after i.v. bolus administration, ID-6105 concentrations in various tissues had decreased to very low levels. The majority of ID-6105 appears to be excreted in the bile.

Comparative Study on Phenolic Compounds of Cheorwon Onion by Phosphite Treatment (아인산염 처리에 따른 철원양파의 페놀화합물 비교 연구)

  • Kim, Y.B.;Lee, H.J.;Park, C.H.;Kim, D.H.;Koo, H.J.;Chang, K.J.
    • Journal of Practical Agriculture & Fisheries Research
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    • v.20 no.2
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    • pp.105-114
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    • 2018
  • The aim of this study was to evaluate the change of phenolic compounds after phosphite treatment on Cheorwon onion. Onion is a perennial plant belonging to the lily family. It is native to Persia of Southwest Asia. It is widely cultivated in the temperate regions of the world. Onion is a good name for the 'Okchong' to drop blood cholesterol and cardiovascular blood flow to increase the prevention of adult diseases. Cheorwon area is inland, but it has high continental climate due to its high altitude. Therefore it is said that the onion cultivated in this region has higher sugar content and higher taste than onion grown in the southern region. Phosphorus components are particularly important ingredients for promoting muscle development. However, if the phosphoric acid content of the soil part is maintained to a large extent until the harvest, the competition of the nutrients tends to cause decay of the root part. Therefore, it is important to improve the quality and shelf life of onion by inducing nutrient balance by applying foliar fertilization method on the reducing phosphorus at harvest time. In this study, acidity was controlled by diluting phosphorous acid(H3PO3) and potassium hydroxide(KOH), followed by leaf surface treatment with phosphite on onion. In this study, the concentration of phosphite was diluted to 500, 1,000, 1,500ppm and sprayed three times over the onion leaves in May 2018 using an atomizer and harvested at the end of June, and the phenolic compounds were analyzed by HPLC. As a result, the content of quercetin, one of the important substances in onion, was phosphite 500ppm(179.70㎍/g), 1,000(150.27), 1,500(105.95). The contents of caffeic acid, p-coumaric acid, ferulic acid, rutin, kaempferol, and sugar content were higher in the treatments than in the control. Therefore, the phosphite does not have a great influence on the growth, but it may play a role as a method of achieving balance with nitrogen in the rainy season by supplying the role of the material catalyst and the water soluble phosphoric acid and the potassium in the influence of the material change.

Development and Characterization of an Anti-Acne Gel Containing Siamese Crocodile (Crocodylus siamensis) Leukocyte Extract

  • Phupiewkham, Weeraya;Lu, Qiumin;Payoungkiattikun, Wisarut;Temsiripong, Threeranan;Jangpromma, Nisachon;Lai, Ren;Klaynongsruang, Sompong
    • Journal of Microbiology and Biotechnology
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    • v.28 no.5
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    • pp.707-717
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    • 2018
  • Leukocytes are reportedly the first line of the innate immune defense and essential for the control of common bacterial infections. Therefore, in this work, the antibacterial activity of crocodile leukocyte extract against Propionibacterium acnes was evaluated, and we also characterized the related activity of skin infection. The leukocyte extract showed the minimum inhibitory concentration to be $100{\mu}g/ml$ to P. acnes. SEM imaging demonstrated that the leukocyte extract adversely affected P. acnes cell permeability in a concentration-dependent manner. Furthermore, the crocodile leukocyte extract could significantly reduce proinflammatory markers and decrease inflammatory signs in infected mouse ears. The crude leukocyte extract was further purified using FPLC and RP-HPLC. The resulting fraction F5 was indicated as the anti-acne peptide-containing fraction. The molecular mass of the peptide contained in F5 was calculated to be 4,790.5 Da. N-Terminal sequencing revealed the amino acid sequence as GPEPVPAIYQ, which displays similarities to immunoglobulin A and leucine-rich repeat neuronal protein. This is the first reported amino acid sequence of a crocodile leukocyte extract that possesses anti-acne activity. To attempt to use it in a prototype cosmetic, an anti-acne gel containing crude crocodile leukocyte extract was formulated, resulting in seven gel formulations (G1, G2, G3, G4, G5, G6, and G7). The formulations G5, G6, and G7 exhibited 2-fold higher anti-acne activity than G1-G4. Investigation of accelerating stability studies of anti-acne gel formulations G5, G6, and G7 demonstrated that a low storage temperature ($4^{\circ}C$) is suitable for maintaining the physical properties and biological activity of the anti-acne gel products.

Comparison of pharmacokinetic characteristics of sildenafil citrate chewable tablets and film-coated tablets in healthy male subjects

  • Yoo, Hyounggyoon;Cho, Sang Min;Choi, Youn Woong;Lee, Hye Jung;Kwon, Ji-Hye;Kim, Soo-Whan;Kim, Jae Woo;Lee, SeungHwan;Hong, Jang-Hee
    • Translational and Clinical Pharmacology
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    • v.25 no.3
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    • pp.153-156
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    • 2017
  • UI14SDF100CW is a chewable tablet of sildenafil citrate, which was developed to improve compliance through convenience of administration. The purpose of this study was to compare the pharmacokinetic (PK) properties of sildenafil citrate chewable tablets (UI14SDF100CW) and conventional sildenafil citrate film-coated tablets ($Viagra^{(R)}$, Pfizer). A randomized, open-label, single dose, two-treatment, two-period, two-way crossover study was conducted in 60 healthy male volunteers. In each period, the subjects received a single oral dose of UI14SDF100CW or $Viagra^{(R)}$ (both tablets contain 140.45 mg of sildenafil citrate, which is equivalent to 100 mg of sildenafil). Serial blood samples were collected up to 24 h post-dose for PK analysis. The plasma concentration of sildenafil was determined using a validated HPLC-MS/MS assay. PK parameters of sildenafil were calculated using non-compartmental methods. The plasma concentration-time profiles of sildenafil in both formulations were similar. For UI14SDF100CW, the $C_{max}$ and $AUC_{last}$ of sildenafil were $1068.69{\pm}458.25$ (mean${\pm}$standard deviation) mg/L and $3580.59{\pm}1680.29h{\cdot}mg/L$, and the corresponding values for $Viagra^{(R)}$ were $1146.84{\pm}501.70mg/L$ and $3406.35{\pm}1452.31h{\cdot}mg/L$, respectively. The geometric mean ratios (90% confidence intervals) of UI14SDF100CW to $Viagra^{(R)}$ for $C_{max}$ and $AUC_{last}$ were 0.933 (0.853-1.021) and 1.034 (0.969-1.108), respectively, which met the bioequivalence criteria of Korean regulatory agency. In conclusion, UI14SDF100CW and $Viagra^{(R)}$ showed similar PK properties. Therefore, UI14SDF100CW can be an alternative to sildenafil for the treatment of erectile dysfunction, providing better compliance.

Pharmacokinetic Profiles of Isoniazid and Rifampicin in Korean Tuberculosis Patients (한국인 결핵환자에서 Isoniazid와 Rifampicin의 약동학)

  • Ahn, Seok-Jin;Park, Sang-Joon;Kang, Kyeong-Woo;Suh, Gee-Young;Chung, Man-Pyo;Kim, Ho-Joong;Kwon, O-Jung;Rhee, Chong-H.;Cha, Hee-Soo;Kim, Myoung-Min;Choi, Kyung-Eob
    • Tuberculosis and Respiratory Diseases
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    • v.47 no.4
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    • pp.442-450
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    • 1999
  • Background : Isoniazid(INH) and rifampicin(RFP) are the most effective anti-tuberculosis drugs which make the short-course chemotherapy possible. Although prescribed dosages of INH and RFP in Korea are different from those recommended by American Thoracic Society, there has been few study about pharmacokinetic profiles of INH and RFP in Korean patients who receive INH, RFP, ethambutol(EMB) and pyrazinamide(PZA) simultaneously. Methods : Among the patients with active tuberculosis from Dec. 1997 to July 1998, we selected 17 patients. After an overnight fast, patients were given INH 300mg, RFP 450mg, EMB 800mg and PZA 1500mg daily. Blood samples for the measurement of plasma INH(n=15) and RFP(n=17) level were drawn each at 0, 0.5, 1, 1.5, 2, 4, 6, 8 and 12hrs, and urine was also collected. INH and RFP level in the plasma and the urine were measured by high-performance liquid chromatography(HPLC). Pharmacokinetic parameters such as peak serum concentration(Cmax), time to reach to peak serum concentration(Tmax), half-life, elimination rate constant(Ke), total body clearance(CLtot), nonrenal clearance(CLnr), and renal clearance(CLr) were calculated. Results : 1) Pharmacokinetic parameters of INH were as follows: Cmax; $7.63{\pm}3.20{\mu}g/ml$, Tmax; $0.73{\pm}0.22hr$, half-life; $2.12{\pm}0.84hrs$, Ke; $0.83{\pm}0.15hrs^{-1}$, CLtot; $17.54{\pm}8.89L/hr$, CLnr; $14.74{\pm}8.35L/hr$, CLr; $2.79{\pm}1.31L/hr$. 2) Pharmacokinetic parameters of RFP were as follows: Cmax; $8.93{\pm}3.98{\mu}g/ml$, Tmax; $1.76{\pm}1.13hrs$, half-life; $2.27{\pm}0.54hrs$, Ke; $0.32{\pm}0.08hrs^{-1}$, CLtot; $14.63{\pm}6.60L/hr$, CLr; $1.04{\pm}0.55L/hr$, CLnr; $13.59{\pm}6.21L/hr$. 3) While the correlation between body weight and Cmax of INH was not statistically significant (r=-0.514, p value>0.05), Cmax of RFP was significantly affected by body weight of the patients(r=-0.662, p value<0.01). Conclusion : In Korean patients with tuberculosis, 300mg of INH will be sufficient to reach the ideal peak blood level even in the patients over 50kg of body weight However, 450mg of RFP will not be the adequate dose in the patients who weigh over 50~60kg.

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Tissue Distribution after dipping administration of Oxytetracycline and Tetracycline in Olive flounder (Paralichthys olivaceus), Rockfish (Sebastes schlegeli), and Red sea bream (Pagrus major) (Oxytetracycline과 Tetracycline의 약욕에 따른 양식어류 (넙치, 조피볼락, 참돔)의 조직내 잔류량의 변화)

  • Lee, Hu-Jang;Kim, Suk;Ha, Ji-Young;Kang, Seok-Jung;Jung, Won-Cheol;Chung, Hee-Sik;Heo, Sung-Hyek;Shin, Yong-Woon;Kim, Kyoung-Won;Kim, Dae-Geun
    • Journal of fish pathology
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    • v.19 no.2
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    • pp.155-164
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    • 2006
  • Tissue distribution and residue depletion of oxytetracycline (OTC) and tetracycline (TC) following dipping administration were evaluated in olive flounder (Paralichthys olivaceus), rockfish (Sebastes schlegeli), and red sea bream (Pagrus major) under field conditions. Fishes were held in floating cages placed in sea water and fed a commercial diet for 15 days to acclimate to a new surrounding. Fishes were dipped in OTC 50 g/ton water for 30min and TC 18 g/ton water for 5 hours. Blood and muscle were sampled from fishes on 0th, 1th, 2th, 3th, and 5th day after administration. After solid-phase extraction, OTC and TC analyses were carried out by HPLC. The recovery rate of OTC in serum and muscle samples was 71-77% and 78-84%, respectively. Also, the recovery rate of TC in serum and muscle samples was 70-79% and 73-78%, respectively. The results of recovery rate were similar to previous studies reported. At the termination of dipping administration of OTC and TC, residue concentration in muscle samples of rockfish was significantly higher than those of olive flounder and red sea bream. At day 5, residue concentrations of all samples were believed to decrease to lower than 0.05 mg/kg, the detection limit. The present study showed that residue concentrations of OTC and TC decreased to below 0.05 mg/kg after treatment 5th day, faster than the established withdrawal period. The tissue reside depletion time of dipping administration of OTC and TC seems to be shorter than those of oral or parenteral administration.

Endotoxin-induced inflammation disturbs melatonin secretion in ewe

  • Herman, Andrzej Przemyslaw;Wojtulewicz, Karolina;Bochenek, Joanna;Krawczynska, Agata;Antushevich, Hanna;Pawlina, Bartosz;Zielinska-Gorska, Marlena;Herman, Anna;Romanowicz, Katarzyna;Tomaszewska-Zaremba, Dorota
    • Asian-Australasian Journal of Animal Sciences
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    • v.30 no.12
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    • pp.1784-1795
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    • 2017
  • Objective: The study examined the effect of intravenous administration of bacterial endotoxin-lipopolysaccharide (LPS) -on the nocturnal secretion of melatonin and on the expression of enzymes of the melatonin biosynthetic pathway in the pineal gland of ewes, taking into account two different photoperiodic conditions: short-night (SN; n = 12) and long-night (LN; n = 12). Methods: In both experiments, animals (n = 12) were randomly divided into two groups: control (n = 6) and LPS-treated (n = 6) one. Two hours after sunset, animals received an injection of LPS or saline. Blood samples were collected starting one hour after sunset and continuing for 3 hours after the treatment. The ewes were euthanized 3 hours after LPS/saline treatment. The concentration of hormones in plasma was assayed by radioimmunoassay. In the pineal gland, the content of serotonin and its metabolite was determined by HPLC; whereas the expression of examined genes and protein was assayed using real-time polymerase chain reaction and Western Blot, respectively. Results: Endotoxin administration lowered (p<0.05) levels of circulating melatonin in animals from LN photoperiod only during the first hour after treatment, while in ewes from SN photoperiod only in the third hour after the injection. Inflammation more substantially suppressed biosynthesis of melatonin in ewes from SN photoperiod, which were also characterised by lower (p<0.05) cortisol concentrations after LPS treatment compared with animals from LN photoperiod. In the pineal gland of ewes subjected to SN photoperiod, LPS reduced (p<0.05) serotonin content and the expression of melatonin biosynthetic pathway enzymes, such as tryptophan hydroxylase and arylalkylamine-N-acetyltransferase. Pineal activity may be disturbed by circulating LPS and proinflammatory cytokines because the expression of mRNAs encoding their corresponding receptors was determined in this gland. Conclusion: The present study showed that peripheral inflammation reduces the secretion of melatonin, but this effect may be influenced by the photoperiod.

Bioequivalency and Pharmacokinetics of Two Clarithromycin Tablets (Clarithromycin 정제의 생물학적 동등성 및 약물동태)

  • Kang, Won Ku;Park, Sun Young;Park, Yong Soon;Woo, Jong Su;Choi, Kyung Eob;Kwon, Kwang Il
    • Korean Journal of Clinical Pharmacy
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    • v.9 no.1
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    • pp.49-54
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    • 1999
  • This study was carried out to compare the bioavailability of Hanmi clarithromycin (250 mg/tablet) with that of $Klaricid^{(R)}$ The bioavailability was examined on 20 volunteers who received a single dose (500 mg) of each drug in the fasting state in a randomized balanced 2-way crossover design. After dosing, blood samples were collected for a period of 12 hours. Plasma samples were analyzed for clarithromycin and roxithromycin(internal standard) by HPLC/Coulometric BCD. The pharmaco-kinetic parameters ($AUC_{0-l2hr}$, Cmax, Tmax, $AUC_{inf}$, Ka, Kel, $t_{1/2}$, Vd/F and Cl/F) were calculated from the plasma clarithromycin concentration-time data of each volunteer. The computer program 'WinNonlin' was used for compartmental analysis. One compartment model with first-order input, from order output with lag time, weighting factor $l/y^2$ was chosen as the appropriate pharmacokinetic model. The major pharmacokinetic parameters ($AUC_{0-l2hr},\;AUC_{inf}$, Cmax and Tmax) of Hanmi clarithromycin were $10.7\pm0.5\;{\mu}g{\cdot}hr{\cdot}ml^{-1},\;12.7\pm0.7\;{\mu}g{\cdot}hr{\cdot}ml^{-1},\;1.7\pm0.1\;{\mu}g/ml\;and\;2.0\pm0.2\;hr$, respectively, and those of $Klaricid^{(R)}\;were\;9.8\pm0.5\;{\mu}g{\cdot}hr{\cdot}ml^{-1},\;11.7\pm0.6\;{\mu}g{\cdot}hr{\cdot}ml^{-1},\;1.6\pm0.1\;{\mu}g/ml\;and\;2.1\pm0.1\;hr$, respectively. The differences in mean values of $AUC_{0-l2hr},\;AUC_{inf}$ and Cmax between two products were $9.88\%,\;8.94%\;and\;6.59\%$, respectively. The least significant differences at $\alpha=0.05$ for $AUC_{0-l2hr},\;AUC_{inf}$ and Cmax were $16.08\%,\;17.81\%\;and\;18.94\%$, respectively. Though the plasma clarithromycin concentrations of Hanmi clarithromycin were higher than those of $Klaricid^{(R)}$ at all observed times, the bioavailability of Hanmi clarithromycin appeared to be bioequivalent with that of $Klaricid^{(R)}$. The Ka, Kel, $t_{1/2}$, Vd/F and Cl/F of the Hanmi clarithromycin were $2.69\pm0.53\;hr^{-1},\;0.18\pm0.01 hr^{-1},\;3.9\;hr,\;248.8\pm11.4\;L\;and\;43.7\pm2.6\;L/hr$, respectively, and those of $Klaricid^{(R)} were 2.19\pm0.51\;hr^{-1},\;0.18\pm0.02\;hr^{-1},\;3.7\;hr,\;266.7\pm22.4\;L\;and\;45.3\pm2.8L/hr$, respectively. There were no statistically significant differences between two drugs in all pharmacokinetic parameters.

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