• Title/Summary/Keyword: Pharmacokinetic studies

Search Result 177, Processing Time 0.042 seconds

Determination of Glimepiride in Human Plasma by LC-MS/MS

  • Kim, Ho-Hyun;Roh, Hyeong-Jin;Lee, Hee-Joo;Han, Sang-Beom
    • Proceedings of the PSK Conference
    • /
    • 2003.04a
    • /
    • pp.282.1-282.1
    • /
    • 2003
  • This study established a sensitive novel Quantification method for detecting glimepiride in human plasma using LC-MS/MS for pharmacokinetic studies. The mobile phase used after degassing was composed of 10 mM ammonium acetate and acetonitrile (20:80, pH 3.0), with flow rate of 200uL/min. One mL plasma were pipetted into glass tubes and spiked with 0.1 mL of internal standard solution. (omitted)

  • PDF

Pharmacokinetic studies on ADME of G009

  • Deuk, Han-Man;Hoon Jeong;Lee, June-Woo;Kim, Su-Ung;Lee, Seung-Yong;Song, Jae-Jin;Chung, Sung-Kyun;Kim, Kee-Nam;Back, Seong-Jin
    • Proceedings of the Korean Society of Applied Pharmacology
    • /
    • 1995.04a
    • /
    • pp.108-108
    • /
    • 1995
  • Pharmacokinetic studies on time-course of blood levels, tissue distribution, and excretion of G009, a potential hepatoprotective agent, were performed in male rats after a single oral dose(20mg/kg) of $\^$14/C-labelled G009. The radioactivity concentrations in plasma during 0~3 hours are low, but subsequently increase to a maximum at 12 hours after dosing. $\^$14/C-G009 was well distributed to all tissue. Tissue concentration profiles of radioactivity vary among tissues on time-course after administration. G009(single oral dosage) was distributed and/or absorbed at gastric intestines and excretional organs for initial time of 0-7 hours, and distributed to most tissue at 12-24 hours. In special, the concentration of radioactivity in tiller at 48 hours were 1% of total radioactivity of $\^$14/C-G009 administered. The expired air, urinary and fecal excretion of radioactivity within 24hours after administration were 61.5%, 1.9% and 21.2% of total radioactivity of $\^$14/C-G009 administered. The biliary excretion of radioactivity in rat increased slightly for 0-6 hours after administration. The biliary excretion of radioactivity within 48hours were 1.97%.

  • PDF

A Multi-chambered Single Autoinjector and KMARK-1 Containing Atropine and 2-PAM: Comparative Bioavailability Studies Using Single Intramuscular Injection with Beagle Dogs (아트로핀 및 팜 함유 다중챔버 단일주사기 및 KMARK-1: 비글개를 이용한 단회 근육투여 비교 생체이용률 연구)

  • Lee, Keunwoo;An, Seoyeon;Kwon, Taekeun;Jung, Inhong;Kim, Dongyeon
    • Journal of the Korea Institute of Military Science and Technology
    • /
    • v.20 no.4
    • /
    • pp.587-596
    • /
    • 2017
  • In this study, multi-chambered single autoinjector(2in1) and KMARK-1 containing atropine and 2-PAM(pyridine-2-aldoxime methylchloride) were administered to the beagle's muscle, and blood samples were taken for a certain period of time to compare and evaluate the pharmacokinetic profiles of the two drugs. Male beagles were used and classified into two test groups(G1, G2), and crossover pharmacokinetic studies were performed in two test groups. Blood samples were collected from the jugular vein for analysis after administration. The 90 % confidence interval(CI) for log transformed data indicated that the Cmax for both atropine(log 0.9683 ~ log 1.113) and 2-PAM(log 0.9453 ~ log 1.214) was within the limits of bioequivalence criteria, but the AUC for atropine(log 1.1786 ~ log 1.3238) failed to meet this criteria. This is expected as the amount of atropine dose is 25 % higher for the test as compared to the reference formulation. In summary, in view of the ATNAA(antidote for nerve agent of US) authorization, the Cmax equivalence was more important than AUC equivalence, so in this study, we also focused on verifying the equality of Cmax between the two autoinjectors.

Pharmacokinetics of amoxicillin after intramuscular injection at different temperatures to cultured olive flounder, Paralichthys olivaceus (Amoxicillin의 근육투여에 따른 수온별 넙치 체내 약동학적 특성)

  • Kim, Ji-Soo;Lee, Ji-Hoon;Lee, Soo-Jin;Park, Kwan-Ha
    • Journal of fish pathology
    • /
    • v.28 no.1
    • /
    • pp.43-51
    • /
    • 2015
  • The pharmacokinetic properties and residue levels of amoxicillin (AMOX) were studied after intramuscular injection to cultured olive flounders ($100{\pm}50g$), Paralichthys olivaceus. For pharmacokinetic studies, AMOX of 20 to 80 mg/kg body weight was administered at $17{\pm}2^{\circ}C$ or $22{\pm}2^{\circ}C$ and AMOX concentrations were determined in plasma, the liver, and the kidney by HPLC-UVD. Plasma samples were assessed at 0.25, 0.5, 1, 3, 6, 12, 24, 48, 72, 96, 168 hours post-dose, whereas liver and kidney concentrations were measured at 0.25 to 48 hours post-dose. The kinetic profiles of AMOX were analyzed by fitting to a 2-compartmental model with PKSolver program. The following parameters were obtained for a single dosage of 20, 40 and 80 mg/kg of body weight at $22^{\circ}C$ and 20 and 40 mg/kg of body weight at $17^{\circ}C$ in plasma, liver and kidney, respectively: $C_{max}$ (the peak concentration)= $27.23-257.36{\mu}g/m{\ell}$, $5.49-41.65{\mu}g/g$, $16.75-129.31{\mu}g/g$; $t_{max}$ (the time for peak concentration)= 0.05-0.91, 1.36-3.28, 1.95-4.49 h. For residue studies, AMOX of 40 and 400mg/kg was administered, and muscle samples were taken at 2, 5, 7, 14 and 21 days post-dose. The residueof AMOX in the muscle were found under the MRLs (maximum residue levels) within 7 days for the two doses.

Drug-herb interactions: Mechanisms involved and clinical implications of five commonly and traditionally used herbs

  • Ong, Chin Eng;Pan, Yan
    • CELLMED
    • /
    • v.4 no.3
    • /
    • pp.17.1-17.8
    • /
    • 2014
  • Herbal remedies are commonly used by patients worldwide. Because these herbal preparations share the same metabolic and transport proteins with prescribed medicines, the potential for a drug-herb interaction is substantial and is an issue of significant concern. This review paper summarizes drug-herb interactions involving inhibition or induction of cytochrome P450 enzymes, drug transporters as well as modulation of drug pharmacodynamics. An increasing number of in vitro and animal studies, case reports and clinical trials evaluating such interactions have been reported, and implications of these studies are discussed in this review. The most commonly implicated drugs in the interaction include anticoagulants, antiplatelets, immunosuppressants, anti-neoplastics, protease inhibitors, and some antidepressants. Pharmacokinetic and/or pharmacodynamic interactions of five commonly used herbal remedies (danshen, garlic, Ginkgo biloba, ginseng, and St John's wort) with these drugs are presented, with focus of discussion being the potentials for interaction, their mechanisms and clinical implications. There is a necessity for adequate pharmacovigilance to be carried out in minimizing unanticipated but often preventable drug-herb interactions.

Pharmaceutical Studies on Ferroglycine Fumarate (II) -Studies on Optimization of Controlled Release Ferroglycine Fumarate Tablets- (푸마르산철글리신 복합체의 약제학적 연구 (제2보) -지속성 푸마르산철글리신 정제의 최적화에 관한 연구-)

  • Shin, Hyun-Jong;Lee, Wan-Ha
    • Journal of Pharmaceutical Investigation
    • /
    • v.17 no.3
    • /
    • pp.101-110
    • /
    • 1987
  • In order to reduce gastric irritation in the stomach of iron preparations, ferroglycine fumarate (FGF) granules coated with hydroxyethylcellulose was made by matrix granulator, and the constrained optimization method, employing the Lagrange equation, was successfully applied to the manufacturing process design of controlled release tablets. The effects of stearic acid and dried corn starch on tablet hardness, friability, dissolution rate $t_{50%}$ and tablet volume were found to be very significant. In rabbit test, pharmacokinetic parameters $(K_a,\;C_{max}\;and\;AUC^{0-12})$ and urinary excretion rate $(K_e)$ of the controlled release FGF tablets were higher than those of controlled release ferroglycine sulfate tablets which were manufactured in the same optimal conditions. Controlled release FGF tablets were more stable than controlled release ferroglycine sulfate tablets in accelerated storage conditions.

  • PDF

New Analytical Method of Methyltestosterone in Human Serum by Gas Chromatography/Maa Spectrometry for Pharmacokinetics and Bioequivalence Studies in Human Volunteers

  • Kim, Hye-Jung;Bae, Sung-Seok;Myung, Seung-Woon;Ryu, Jae-Chun;Chung, Youn-Bok;Kwon, Oh-Seung
    • Proceedings of the PSK Conference
    • /
    • 2003.10b
    • /
    • pp.241.3-242
    • /
    • 2003
  • A simple, specific and sensitive method for the determination of methyltestosterone (MT) in human serum has been developed by gas chromatography/mass spectrometry with the purpose of conducting pharmacokinetic and bioequivalence studies of MT. This method involves the use of liquid-liquid extraction with diethyl ether and derivatization with MSTFA, using 1 ml of serum obtained from volunteers orally taken 50 mg MT. MT showed good resolutions in this conditions and no significant interfering peaks were observed. (omitted)

  • PDF

Corticosteroid Resistant Asthma

  • Lane, Stephen J.;Lee, Tak-H.
    • Tuberculosis and Respiratory Diseases
    • /
    • v.42 no.6
    • /
    • pp.801-812
    • /
    • 1995
  • CR asthma is associated with disease chronicity, a positive family history of asthma and in vitro and in vivo defects in mononuclear cell function. The HPA axis in CR asthmatics is suppressed normally by dexamethasone and the pharmacokinetic profile of an oral dose of prednisolone is similar to that found in CS subjects. In addition, competitive binding studies have shown that the ligand binding and nuclear translocation functions of the GR are similar in the two groups. Studies using gel retardation assay have indicated a defect in DNA binding in CR subjects. Chemical mutational analysis of the GR has shown that is not due to a defect in its structure at the cDNA level. Scatchard analysis of the GR/DNA and GR/ligand interactions suggests that there may be transcriptional interference of the GR with other transcriptionally active molecules leading to defective gene transcription.

  • PDF

Hepatobiliary Excretion of Tributylmethylamonium in Rats with Lipopolysaccharide-Induced Acute Inflammation

  • Lee, In-Kyung;Lee, Young-Mi;Song, Im-Sook;Chung, Suk-Jae;Kim, Sang-Geon;Lee, Myung-Gull;Shim, Chang-Koo
    • Archives of Pharmacal Research
    • /
    • v.25 no.6
    • /
    • pp.969-972
    • /
    • 2002
  • The alteration in the pharmacokinetic behaviors of organic cations (OCs) in rats during acute inflammation (AI) was investigated. AI was induced by an intraperitoneal injection of lipopolysaccharide (LPS, 5 mg/kg) 24 hr prior to the start of pharmacokinetic studies. Tributylmethylammonium (TBuMA) was selected as a model OC since it is largely excreted into bile, and is neither metabolized nor binds to proteins in the body. When TBuMA was administered intravenously to AI rats at a dose of 6.6 $\mu$mole/kg, the AUC was increased, while biliary excretion (i.e., cumulative amount and apparent clearance) was decreased compared to normal rats. When TBuMA was administered intravenously to AI rats at a constant rate (i.e., a bolus injection at a dose of 1.5 $\mu$mole/kg followed by a constant infusion at a rate of 1.5 $\mu$mole/kg/hr for 165 min), steady-state concentrations of plasma and liver concentrations of TBuMA were increased significantly, while in vivo hepatic uptake (amount) and canalicular excretion (clearance) were decreased. These results are consistent with a hypothesis in which both the sinusoidal uptake of TBuMA into hepatocytes via the OCT1 and the canalicular excretion of the compound from hepatocytes via the P-gp are decreased by LPS-induced AI.

Metabolic Pharmacokinetics in Rats: Differences between Pure Amygdalin and Amygdalin in a Decoction of Peach Seeds

  • Chen, Jianbo;Yan, Xitao;Kim, Tae-Jin;Kim, Sang-Hyuck;Kim, Kyung-Tae;Lee, Young-Keun;Cho, Cheong-Weon;Baek, Jong-Suep;Park, Yong-Ki;Kim, Young-Ho;Lee, Won-Jae;Kang, Jong-Seong
    • Bulletin of the Korean Chemical Society
    • /
    • v.33 no.5
    • /
    • pp.1470-1474
    • /
    • 2012
  • The pharmacokinetics of prunasin after oral administration of amygdalin or a decoction of peach seeds was determined and compared in rats. A $C_{18}$ column was used for separation at a column temperature of $25^{\circ}C$. The mobile phase consisted of 20% aqueous acetonitrile, and the flow rate was 0.5 mL/min. After oral administration of a decoction of peach seeds, prunasin was absorbed rapidly, reaching a maximum plasma concentration ($C_{max}$) of 62.1 mg/L within 45 min. After oral administration of amygdalin, the absorption of prunasin was delayed. The $C_{max}$ of prunasin was 42.9 mg/L and was reached at 60 min. Values for the pharmacokinetic parameters of prunasin, including $T_{max}$, $C_{max}$, AUC, $T_{1/2}$, CL/F, and V1/F, were significantly different for the oral administration of amygdalin compared with that of a decoction of peach seeds.