• Title/Summary/Keyword: Tmax

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Scintigraphic Assessment of Hepatobiliary Functions in Healthy Miniature Pigs (건강한 미니돼지에서 간담도 기능의 핵의학적 평가)

  • Kim, Se-Eun;Shim, Kyung-Mi;Yoo, Kyeong-Hoon;Lee, Won-Guk;Choi, Seok-Hwa;Park, Soo-Hyun;Han, Ho-Jae;Kang, Seong-Soo
    • Journal of Veterinary Clinics
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    • v.24 no.4
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    • pp.593-596
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    • 2007
  • The purpose of this study is to investigate normal hepatobiliary functions in healthy miniature pigs. $^{99m}Tc-DISIDA$ hepatobiliary scintigraphy(HBS) was used for it. Five mCi dose of $^{99m}Tc-DISIDA$ was injected intravenously into 3 healthy adult miniature pigs, and dynamic images were obtained during 1 hour. $^{99m}Tc-DISIDA$ HBS in a miniature pig was evaluated for 6 variables. A cardiac washout occurred within 1 min in all miniature pigs and radioactivities in the gallbladder were not detected in two miniature pigs. Thus, the initial radioactivity and Tmax of the gallbladder were non-available to identify. Mean Tmax of liver was $8.67{\pm}2.08$ min and initial small intestinal radioactivity was seen at $9.67{\pm}2.52$ min after $^{99m}Tc-DISIDA$ injection. Mean hepatic washout time was not detected in 60 min dynamic images. Therefore, $^{99m}Tc-DISIDA$ HBS is the effective diagnostic method to evaluate the function of hepatocyte and bile flow rate. However, it was not a proper method to evaluate the function of gallbladder, which indicates that an additional study is needed to further specify the reasons for the absence of radioactivities in gallbladder of two miniature pigs.

Effects of Various Formulations on Bioavailability of Acetaminophen Soft Gelatin Capsules in Rabbits (토끼에서 아세트아미노펜 연집캅셀제의 생체이용율에 미치는 제제처방들의 영향)

  • Park, Gee-Bae;Lee, Yong-Suk;Choi, Myung-Ho;Lee, Do-Ik;Lee, Kwang-Pyo
    • YAKHAK HOEJI
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    • v.36 no.6
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    • pp.598-603
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    • 1992
  • The purpose of this study was to assess the effect of three formulations; product A (polyethylene glycol was used as a main dispersing agent), product B (wax mixture was used as a main dispersing agent) and product C(silicon dioxide was used as a main dispersing agent) on bioavailability of acetaminophen soft gelatin capsules(softgels) and to develop an effective acetaminophen softgel which exhibits an excellent bioavailability. Acetaminophen softgels of various formulations were prepared as 4 minim round type by rotary die method. Four softgels of the three formulation (A, B, C), each of which contained 50 mg acetaminophen, were administered orally to 12 normal healthy rabbits using a three-way cross over design. Plasma acetaminophen concentrations were measured by HPLC. The results obtained in this study were as follows: 1. The Tmax rank order of acetaminophen softgel was C$(63.75{\pm}10.62\;min)$>A$(36.25{\pm}5.37\;min)$>B$(35{\pm}6.74\;min)$. 2. The decreasing Cmax order of softgel product was A$(93.51{\pm}0.55\;{\mu}g/ml)$>B$(3.16{\pm}0.37\;{\mu}g/ml)$>C$(2.6{\pm}0.55\;{\mu}g/ml)$. 3. The $[AUC]^{\infty}_0$ rank order for three acetaminophen softgel formulations was A $(14.89{\pm}1.56\;{\mu}g/ml{\cdot}min)$ >B$(14.39{\pm}1.43\;{\mu}g/ml{\cdot}min)$>C$(11.45{\pm}1.49\;{\mu}g/ml{\cdot}min)$. 4. Pharmacokinetic parameters such as Tmax, Cmax and $[AUC]^{\infty}_0$ of product A and B did not differ significantly(p>0.05). On the other hand, those of product C were significantly different(p>0.05).

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Studies on Pharmacokinetics of a new NSAID SJ-151(I)

  • Kim, Dong-Sup;Chung, Hye-Joo;Na, Han-Kwang;Park, Yoon-Ju;In Sook, Park;Ahn, Mi-Lyung;Chang, Young-Sup
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1996.04a
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    • pp.220-220
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    • 1996
  • The objectives of this study were to evaluate the pharmacokinetics of SJ-151 which is a new NSAID in male Beagle dogs following a single oral dosing. Seven beagle dogs (10-l2kg) were all administered a single oral gavage(10mg/kg) of SJ-151 tablet and serial blood samples of approximately 5$m\ell$ were then drawn from the cephalic vein of each animal at 0(predose), 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24hours postdosc. SJ-151 (Cinmetacinㆍbutendiol)and cimetacin were quantified in the plasma fraction by HPLC assay. The pharmacokinetic parameters calculated from the plasma concentrations of SJ-151 in dayl are Cmax(ng/$m\ell$)509$\pm$248, Tmax(hr) 1.50$\pm$0.45, AUC(ng.hr/$m\ell$) 1,750$\pm$762, tl/2$\alpha$ 0.98$\pm$0.30, t1/2$\beta$ 12.0$\pm$6.75. The pharmacokinetic parameters calculated from the plasma concentrations of Cinmetacin in day 1 are Cmax(ng/$m\ell$)258$\pm$74.1, Tmax(hr)2.42$\pm$ 0.92, AUC(ng.hr/$m\ell$) 1,820$\pm$318, t1/2$\alpha$ 1.74$\pm$0.49, t1/2$\beta$ 25.4$\pm$13.4.

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Effects of mixed formulation of tamoxifen and blue honeysuckle on the pharmacokinetics profiles of tamoxifen after single oral administration

  • Hu, Jin-Ryul;Jang, Tae-Woo;Kang, Su-Jin;Ku, Sae-Kwang;Choi, Seong-Hun;Lee, Young-Joon
    • The Journal of Korean Medicine
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    • v.40 no.4
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    • pp.1-15
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    • 2019
  • Objectives: Here, we investigated the effects of concentrated and lyophilized powders Blue honeysuckle (BH) on the PK of tamoxifen, to establish the pharmacokinetics (PK) profiles as one of essential process in new drug development. Methods: After single oral treatment of 0.4 mg/ml of tamoxifen or tamoxifen 0.4 with BH 40, 20 and 10 mg/ml, the plasma were collected at 0.5 hr before administration, 0.5, 1, 2, 3, 4, 6, 8 and 24 hr after end of single or mixed formula treatment. Plasma concentrations of tamoxifen were analyzed using LC-MS/MS methods. Tmax, Cmax, AUC, t1/2 and MRTinf were analyzed using noncompartmental PK data analyzer programs. Results: Tamoxifen and BH 40 mg/ml did not induce any significant change on the plasma tamoxifen concentrations, while significant decreases were observed in tamoxifen and BH 10 mg/ml from 2 to 8 hr as compared with tamoxifen only, respectively. Furthermore, significant increases of Tmax in tamoxifen and BH 40 mg/ml, significant decreases of Cmax in tamoxifen and BH 20 mg/ml, significant decreases of AUC0-t, AUC0-inf and MRTinf in tamoxifen and BH 10 mg/ml were demonstrated as compared with tamoxifen only. Conclusion: Taken together, tamoxifen and BH 10 mg/ml induced significant decrease of the oral bioavailability of tamoxifen, while tamoxifen and BH 40 or 20 mg/ml did not critically influenced, suggesting formulated BH concentration-independencies. It, therefore, seems to be needed that pharmacokinetic study after repeated administration should be tested to conclude the effects of BH on the pharmacokinetics of tamoxifen.

Characteristics of Kenaf Fibers Treated by Alkali (알칼리 처리에 따른 케나프 섬유의 특성 변화 연구)

  • Yoo, Hye-Ja;Lee, Hye-Ja
    • Journal of the Korean Society of Clothing and Textiles
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    • v.35 no.8
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    • pp.982-990
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    • 2011
  • Kenaf fiber can be obtained by decortications of the kenaf plant stem. The properties of the kenaf fiber treated by alkali (NaOH) were investigated by spectrocolorimeter, SEM, X-ray diffractometer, FT-IR and TGA. The kenaf fibers treated by alkali became darker and their Munsell color values changed from Y (yellow) to YR (yellowred) according to an increased NaOH concentration. SEM observation of the kenaf fibers showed that their crimps were developed and their surfaces were cleaned by the removal of protruding ends and impurities after alkali treatments. In the x-ray diffraction analysis, the structures of the fibers were found in the form of cellulose I when treated with a 0-16% alkali concentration and cellulose II when treated with over 20%. It was also confirmed that the crystallinity was lowered according to an increased NaOH concentration. The change of fiber compositions was investigated in FT-IR analysis. Strong band of $1,738cm^{-1}$ and asymmetrical stretching strong bands of $1,630-1,600cm^{-1}$ in spectrum (which represent pectin) were not found in the samples because the pectin was removed by the alkali treatment. Weak bands of $1,728-1,730cm^{-1}$ and peaks of $1,245-1,259cm^{-1}$ (which represent hemicellulose) and peaks of $1,592cm^{-1}$, $1,504cm^{-1}$, $1,462cm^{-1}$ and $1,429cm^{-1}$ (which are related to lignin) were not found or reduced in the samples treated with a concentration over 20%. TGA indicated that the kenaf fiber had the better hydrophilic properties by alkali treatment. The higher Tmax in TGA and the higher thermal stability when treated by alkali with the higher concentration. The fibers treated with an alkali concentration over 30% did not show any changes in Tmax.

Bioequivalence of Dybis Tablet (Metformin Hydrochloride 500 mg) (다이비스 정 (염산메트폴민 500 mg)의 생물학적 동등성)

  • 최준식;박영진;박상묵;범진필
    • YAKHAK HOEJI
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    • v.47 no.4
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    • pp.239-243
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    • 2003
  • Metformin is an oral antihyperglycemic agent used in the therapy of noninsulin-dependent diabetes mellitus and does not cause hypoglycemia at the therapeutic dose. The purpose of the present study was to evaluate the bioequivalence of two metformin hydrochloride tablets, Glucophage tablet (DaeWoong Pharmaceutical Co., reference drug) and Dybis tablet (Shinpoong Pharmaceutical Co., test drug), according to the guidelines of Korea Food and Drug Administration(KFDA). Twenty-four normal volunteers, 26.6$\pm$4.01 years in age and 60.6$\pm$9.80 kg in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After one tablet containing 500 mg of metformin hydrochloride was orally administered, blood was taken at predetermined time intervals and the concentrations of metformin hydrochloride in serum were determined using HPLC with UV detector. The pharmacokinetic parameters such as AUCt, Cmax and Tmax were calculated and ANOVA test was utilized for the statistical analysis of the parameters. The results showed that the differences in AUCt, Cmax and Tmax between two products were -1.05%, -6.76% and -4.51%, respectively, when calculated against the reference drug. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log0.8$\leq$$\delta$$\leq$log1.25 (e.g., log0.9082$\leq$$\delta$$\leq$log1.0906 and log0.8188$\leq$$\delta$$\leq$log1.0392 for $AUC_{t}$ and $C_{max}$, respectively). The 90% confidence intervals using untransformed data was within $\pm$20% (e.g., -17.66%$\leq$$\delta$$\leq$8.63% for $T_{max}$). All parameters met the criteria of KFDA for bioequivalence, indicating that Dybis tablets (Shinpoong Pharmaceutical Co.) is bioequivalent to Glucophage tablets (DaeWoong Pharmaceutical Co.).

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 ㎕/㎖.

Effects of the mixed formulation of sorafenib and blue honeysuckle on the pharmacokinetics profiles of sorafenib

  • Kang, Hyun-Gu;Kang, Su-Jin;Ku, Sae-Kwang;Choi, Seong-Hun;Lee, Young-Joon
    • Journal of Society of Preventive Korean Medicine
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    • v.23 no.1
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    • pp.83-94
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    • 2019
  • Objective : This study investigated the effects of concentrated and lyophilized blue honeysuckle powders (BH) on the pharmacokinetics (PK) of sorafenib were observed. Method : The blood was collected at 0.5 hr before single oral treatment of sorafenib (40 mg/kg) or sorafenib with BH (400, 200 and 100 mg/kg) mixed formulas administration, and 0.5, 1, 2, 3, 4, 6, 8 and 24 hrs after the end of single or mixed formula administration. Plasma concentrations of sorafenib were analyzed using LC-MS/MS methods. Tmax, Cmax, AUC, $t_{1/2}$ and $MRT_{inf}$ of sorafenib were analysis as compared with sorafenib single treatment. Results : Single oral administration of mixed formulas induced significant increases of plasma sorafenib concentrations from 0.5 hr after end of administration throughout all blood collected time points, as compared with sorafenib single formula treated rats, and significant decreases of sorafenib Tmax with increases of Cmax, $AUC_{0-t}$ and $AUC_{0-inf}$ were detected in sorafenib and BH 400 mg/kg mixed formulation treated rats as compared with sorafenib single formula treated rats, respectively. Inaddition, sorafenib and BH 200 or 100 mg/kg mixed formula treated rats also showed significant increases of sorafenib Cmax, $AUC_{0-t}$ and $AUC_{0-inf}$, respectively. Conclusions : According to these results, mixed formulation of BH with sorafenib increased the bioavailability of sorafenib through the increment of the absorptions.