• Title/Summary/Keyword: Drug Distribution

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Development of Polymeric Nanopaclitaxel and Comparison with Free Paclitaxel for Effects on Cell Proliferation of MCF-7 and B16F0 Carcinoma Cells

  • Yadav, Deepak;Anwar, Mohammad Faiyaz;Garg, Veena;Kardam, Hemant;Beg, Mohd Nadeem;Suri, Suruchi;Gaur, Sikha;Asif, Mohd
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.5
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    • pp.2335-2340
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    • 2014
  • Paclitaxel is hydrophobic in nature and is recognized as a highly toxic anticancer drug, showing adverse effects in normal body sites. In this study, we developed a polymeric nano drug carrier for safe delivery of the paclitaxel to the cancer that releases the drug in a sustained manner and reduces side effects. N-isopropylacrylamide/vinyl pyrrolidone (NIPAAm/VP) nanoparticles were synthesized by radical polymerization. Physicochemical characterization of the polymeric nanoparticles was conducted using dynamic light scattering, transmission electron microscopy, scanning electron microscopy and nuclear magnetic resonance, which confirmedpolymerization of formulated nanoparticles. Drug release was assessed using a spectrophotometer and cell viability assays were carried out on the MCF-7 breast cancer and B16F0 skin cancer cell lines. NIPAAm/VP nanoparticles demonstrated a size distribution in the 65-108 nm range and surface charge measured -15.4 mV. SEM showed the nanoparticles to be spherical in shape with a slow drug release of ~70% in PBS at $38^{\circ}C$ over 96 h. Drug loaded nanoparticles were associated with increased viability of MCF-7 and B16F0 cells in comparison to free paclitaxel. Nano loaded paclitaxel shows high therapeutic efficiency by sustained release action for the longer period of time, i increasing its efficacy and biocompatibility for human cancer therapy. Therefore, paclitaxel loaded (NIPAAm/VP) nanoparticles may provide opportunities to expand delivery of the drug for clinical selection.

Drug Utilization Review of Antiulcerative Agents in Korean Elderly Inpatients (노인 입원환자에 대한 항궤양약물 처방양상 분석)

  • Lee, Won-Sik;Lee, Seung-Mi;Koo, Hye-Won;Park, Byung-Joo
    • Journal of Preventive Medicine and Public Health
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    • v.35 no.1
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    • pp.41-48
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    • 2002
  • Objectives : To review the drug prescription pattern of antiulcerative agents for elderly inpatients, Methods : The study population comprised inpatients of community hospitals who were members of the Korean Elderly Pharmacoepidemiologic Cohort (KEPEC), aged 65 years or over, beneficiaries of the Korea Medical Insurance Corporation (KMIC) and residing in Busan city in 1993. The drug prescription information was collected from the claims data of hospitals where the cohort members received medical care between January 1993 and December 1594. The information included personal identification, age, gender, diagnosis, drug dosage, date of hospital admission and name of medical institutions where the study subjects received drug prescriptions. The data analysis produced outcomes in terms of distribution of antiulcerative agents by class and by medical institution and trend of relative prescription, Analysis was also performed in terms of combined prescriptions of antiulceratives and drugs that could induce risk from drug interaction with antiulceratives. Results : The number of patients prescribed antiulcerative agents was 1,059 (64,9%) male and 1,724 (65.5%) female among the total inpatients. An antacid and composite agent was the most frequently prescribed antiulcerative agent (70.8%), followed by $H_2$ antagonist (16.0%), Among the potential drugs that could induce risk from drug interaction with the antiulcerative agents, diazepam was the most frequently prescribed. The proportion of diazepam co-prescription was 22.5% of the total cimetidine prescriptions and 14.5% of the fetal omeprazole prescriptions. Conclusions : Antiulcerative drugs were frequently prescribed in the elderly inpatients. The adverse drug reaction could possibly be due to drug interaction. The study results could be used as fundamental data for further drug utilization review of antiulceratiye agents.

Pharmacokinetics and Tissue distribution of DWP20373, a Novel Fluoroquinolone, in Rats and Beagle Dogs (신규 플르오로퀴놀롤계 항생물질인 DWP20373의 흰쥐 및 개에서의 체내동태와 조직분포)

  • 조재열;한승희;김병오;남권호;김지연;유영호;이재욱;박명환;김재환
    • Biomolecules & Therapeutics
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    • v.5 no.2
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    • pp.179-186
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    • 1997
  • The pharmacokinetics and tissue distribution of DWP20373, a novel fluoroquinolone, were examined in rats and beagle dogs after a single intravenous and oral administration. Analysis of DWP20373 in plasma, tissue, and urine was performed by both HPLC and microbiological assay. The plasma drug concentration declined biexponentially both rats and beagle dogs. In the rats, the terminal drug elimination half-life (t$_{1}$2$\beta$/) was 64 min (IV) and 57 min (PO) by bioassay, and 76 min (IV) and 77 min (PO) by HPLC. Whereas in beagle dogs, t$_{1}$2$\beta$/ was 196 min (IV) and 350 min (PO). The volume of distribution at steady-state (Vd$_{ss}$ ) was 811 ml/kg (bioassay) and 2061 ml/kg (HPLC) in rats, and 2738 ml/kg (bioassay) in beagle dogs. The total body clearance (Cl$_{t}$) of DWP20373 was 10 ml/min/kg (bioassay) and 7 ml/min/kg (HPLC) in rats, and 11 m1/min/kg (bioassay) in beagle dogs. The extent of bioavailability after oral administration was 49% (bioassay) and 67% (HPLC) in rats, and 84% (bioassay) in beagle dogs. The 24-h urinary recovery, measured by bioassay, was 2.7% after oral dosing and 5.5% after intravenous dosing in rats. Serum protein binding ratio determined at 27g/ml was 78%. This drug was also distributed in tissues in the decreasing order of liver, kidney, spleen, lung, heart, and muscle determined at 30 min after oral administration.on.

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Prediction of successful caudal epidural injection using color Doppler ultrasonography in the paramedian sagittal oblique view of the lumbosacral spine

  • Yoo, Seon Woo;Ki, Min-Jong;Doo, A Ram;Woo, Cheol Jong;Kim, Ye Sull;Son, Ji-Seon
    • The Korean Journal of Pain
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    • v.34 no.3
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    • pp.339-345
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    • 2021
  • Background: Ultrasound-guided caudal epidural injection (CEI) is limited in that it cannot confirm drug distribution at the target site without fluoroscopy. We hypothesized that visualization of solution flow through the inter-laminar space of the lumbosacral spine using color Doppler ultrasound alone would allow for confirmation of drug distribution. Therefore, we aimed to prospectively evaluate the usefulness of this method by comparing the color Doppler image in the paramedian sagittal oblique view of the lumbosacral spine (LS-PSOV) with the distribution of the contrast medium observed during fluoroscopy. Methods: Sixty-five patients received a 10-mL CEI of solution containing contrast medium under ultrasound guidance. During injection, flow was observed in the LSPSOV using color Doppler ultrasonography, following which it was confirmed using fluoroscopy. The presence of contrast image at L5-S1 on fluoroscopy was defined as "successful CEI." We then calculated prediction accuracy for successful CEI using color Doppler ultrasonography in the LS-PSOV. We also investigated the correlation between the distribution levels measured via color Doppler and fluoroscopy. Results: Prediction accuracy with color Doppler ultrasonography was 96.9%. The sensitivity, specificity, positive predictive value, and negative predictive value were 96.7%, 100%, 100%, and 60.0%, respectively. In 52 of 65 patients (80%), the highest level at which contrast image was observed was the same for both color Doppler ultrasonography and fluoroscopy. Conclusions: Our findings demonstrate that color Doppler ultrasonography in the LS-PSOV is a new method for determining whether a drug solution reaches the lumbosacral region (i.e., the main target level) without the need for fluoroscopy.

Comparison of Positron Emission Tomography(PET) imaging-based initial in vivo pharmacokinetics by administration routes of [18F]FDG

  • Yiseul Choi;Jang Woo Park;Eun Sang Lee;Ok-Sun Kim;Hye Kyung Chung
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.7 no.2
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    • pp.99-103
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    • 2021
  • In this study, the initial in vivo pharmacokinetic changes according to the routes of drug administration were investigated using bioimaging techniques. The purpose of this study was to quantify the degree of distribution of each major organ in normal mice over time by acquiring Positron Emission Tomography/Computed Tomography images while administering routes F-18 fluorodeoxyglucose such as intravenous, intraperitoneal and per oral, a representative diagnostic radiopharmaceutical. Dynamic Positron Emission Tomography images were acquired for 90 minutes after drug administration. Radioactivity uptake was calculated for major organs using the PMOD program. In the case of intravenous administration, it was confirmed that it spread quickly and evenly to major organs. Compared to intravenous administration, intraperitoneal administration was about three times more absorbed and distributed in the liver and intestine, and it was showed that the amount excreted through the bladder was more than twice. In the case of oral administration, most stayed in the stomach, and it was showed that it spread slowly throughout the body. In comparison with intravenous administration, it was presented that the distribution of kidneys was more than 9 times and the distribution of bladder was 66% lower. Since there is a difference in the initial in vivo distribution and excretion of each administration method, we confirmed that the determination of the administration route is important for in vivo imaging evaluation of new drug candidates.

Review of Gender Differences in Medicine and Primary Factors Resulting in Gender Differences (의약품에서의 성별차이 및 유발요인)

  • Kim, Hyun-Ju;Choi, Jong-Min;Kim, You-Jin;Chae, Song-Wha;Park, Jung-Hyun;Oh, Ji-Hyun;Kim, Kyung-Hee;Heo, Jung-Sun;Gwak, Hye-Sun;Lee, Hwa-Jeong
    • Korean Journal of Clinical Pharmacy
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    • v.20 no.2
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    • pp.128-137
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    • 2010
  • This review summarizes gender differences in pharmacokinetics, pharmacodynamics, and adverse drug reactions. Gender differences in pharmacokinetics are categorized by four major factors: absorption/bioavailability, distribution, metabolism, and elimination. There are sex-based differences in gastric emptying time, gastric alcohol dehydrogenase activity, apparent volume of distribution, ${\alpha}1$-acid glycoprotein level, phase I (CYP) and phase II metabolizing enzymes, glomerular filtration rate, and drug transporters. This review also reports gender differences in pharmacokinetics and pharmacodynamics of cardiovascular agents, central nervous system acting agents and antiviral agents. In addition, it has been reported that females experience more adverse reactions such as coughing, tachycardia, nausea, vomiting, rash, hypersensitivity, hepatotoxicity, and metabolic disorder after taking cardiovascular, central nervous system acting and antiviral agents. Therefore, in order to provide optimal drug dosage regimens both in male and female, gender differences in pharmacokinetics, pharmacodynamics, and adverse drug reactions must be considered.

Genetic properties of R plasmids in Salmonella isolates of swine and bovine origin in Korea I. Distribution and drug resistance of Salmonella isolated from dairy cow (우(牛), 돈(豚)에서 분리(分離)한 Salmonella유래(由來) R plasmid의 유전학적(遺傳學的) 및 분자생물학적(分子生物學的) 성상(性狀)에 관한 연구(硏究) I. 유우(乳牛)에서 Salmonella속균(屬菌)의 분포상황(分布狀況) 및 약제내성(藥劑耐性))

  • Choi, Won-pil;Lee, Hi-suk;Yeo, San-geon;Lee, Hun-jun;Chae, Tae-chul
    • Korean Journal of Veterinary Research
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    • v.28 no.2
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    • pp.331-337
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    • 1988
  • This paper dealt with the distribution of Salmonella (S) infection on 4 herds in Kyungju and Taegu during the period from May to October 1986. Isolated Salmonella were examined for serotypes, antimicrobial drug resistance and detection of R plasmid. The results obtained were summarised as followings: 1. Of total 4.622 samples from 4 herds, 67 Salmonella were isolated from 51 samples(1.1%), and their serovar strains were S typhimurium 6, S derby 5, S infantis 4, S bareilly 4, S dublin 3, S anatum 2, S montevideo 2 and untypable 41. 2. The isolation rate of Salmonella was higher in summer and autumn. 3. Of the 67 strains examined, 45 (67.2%) were resistant to one or more antibiotics, such as ampicillin (Am), cephalothin (Ce), chloramphenicol (Cm), rifampicin (Rf), sulfadimethoxine (Su), and tetracycline (Tc), and higher resistant to Sm (40.2%), Ce (31.3%), Am (23.9%). 4. Of the 45 resistant Salmonella strains, 44 (97.8%) harbored conjugative R plasmids and the transfer frequency of Sm (100%), Ce (95.2%), Tc (91.0%) and Su (80.0%) resistance was much higher than that of the other drug resistance. 5. The most common resistant patterns were Sm, Ce, AmCeCmSmSuTc, and AmCe. 6. In 4 herds, the incidience of drug resistance was 57.7%~100% and transfer frequency of conjugative R plasmid was 96.1%~100%.

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Chronopharmacology in Clinical Medicine (임상에서 시간약물학)

  • Lee, Heon-Jeong;Kim, Leen
    • Sleep Medicine and Psychophysiology
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    • v.11 no.2
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    • pp.67-72
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    • 2004
  • Circadian rhythm is a global phenomenon, the control mechanisms of which are manifested at every level of biological organization, from genes and intracellular mechanisms to networks of cell populations, and to all central neuronal systems at the organismic level. In pharmacotherapy, the pharmacokinetic parameters such as drug absorption and distribution, drug metabolism, and renal elimination show diurnal variations. The symptoms and signs in diseases like asthma, myocardiac infarction, angina pectoris, hypertension and stroke also show diurnal fluctuations. These observations require drug treatment considering the circadian rhythm of body function and disease. Circadian time has to be taken into account as an important variable influencing a drug's pharmacokinetics and/or its effects or side effects in clinical practice.

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