• Title/Summary/Keyword: Pharmaceutical Industry

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Identification of ML106 Phase 1 Metabolites in Human Liver Microsomes Using High-Resolution Quadrupole-Orbitrap Mass Spectrometry

  • Jo, Jun Hyeon;Nam, WoongShik;Kim, Sunjoo;Lee, Doohyun;Min, Kyung Hoon;Lee, Taeho;Lee, Sangkyu
    • Mass Spectrometry Letters
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    • v.7 no.3
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    • pp.69-73
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    • 2016
  • High-resolution quadrupole-Orbitrap mass spectrometry (HRMS), with high-resolution (> 10,000 at full-width at half-maximum) and accurate mass (< 5 ppm deviation) capabilities, plays an important role in the structural elucidation of drug metabolites in the pharmaceutical industry. ML106, a derivative of imidazobenzimidazole, decreased melanin content and tyrosinase activity in a dose-dependent manner. Here, we investigated the phase 1 metabolic pathway of ML106 using HRMS in human liver microsomes (HLMs) and recombinant cDNA-expressed cytochrome P450 (CYP). After the incubation of ML106 with pooled HLMs and recombinant cDNA-expressed CYP in the presence of NADPH, five phase 1 metabolites, including three mono-hydroxylated metabolites (M1-3) and two di-hydroxylated metabolites (M4 and M5), were investigated. The metabolite structures were postulated by the elucidation of protonated mass spectra using HRMS. The CYP isoforms related to the hydroxylation of ML106 were studied after incubation with recombinant cDNA-expressed CYP. Here, we identified the phase 1 metabolic pathway of ML106 induced by CYP in HLMs.

Management Efficiency Analysis of Innovative Pharmaceutical Companies' Technological Innovation Activities (혁신형제약기업의 기술혁신활동에 대한 경영효율성 분석)

  • Lim, Hye Ryon;Min, Hyun-Ku
    • The Journal of the Korea Contents Association
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    • v.21 no.11
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    • pp.361-374
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    • 2021
  • The purpose of this study is to analyze the efficiency and productivity of technological innovation activities of companies certified as innovative pharmaceutical companies by the government to diagnose their competitiveness and derive measures to strengthen them. This study collected pharmaceutical input (R&D expenditures and number of employees) and output (sale, operating profit and patent) data between 2017 and 2019 for 38 innovative pharmaceutical companies. This study analyzed them using the data envelopment analysis (DEA) method, Tobit model and the Malmquist Productivity Index (MPI). First, the DEA result of the innovative pharmaceutical companies show that between the value of the CCR model of the scale efficiency and the value of the BCC model to diagnose the internal operation efficiency is differences. Second, efficiency does not differ between corporate characteristics. Third, Tobit model shows that number of patents held have positive effects on efficiency. Forth, overall MPI is 0.89. This can be interpreted as the rate of TECI decreased 3%p and TCI has increased 4%p. The results of this study can be used as decision-making data for response strategies to improve efficiency by identifying the cause of inefficiency and presenting target values.

Drug Polymorphism and its Importance on Drug Development Process

  • Jeong, Seong-Hoon;Youn, Yu-Seok;Shin, Beom-Soo;Park, Eun-Seok
    • Journal of Pharmaceutical Investigation
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    • v.40 no.spc
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    • pp.9-17
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    • 2010
  • Polymorphism has been recognized to be a critical issue throughout the drug product development process. Most of solid phase drugs have polymorphism, which has generated a great deal of interest and the field has been evolving rapidly. Preferably, thermodynamically most stable form of a drug substance is selected to obtain consistent bioavailability over its shelf life and various storage conditions. Moreover, it has the lowest potential for conversion from one polymorphic form to another. However, metastable or amorphous forms may be used intentionally to induce faster dissolution rate for rapid drug absorption and higher efficacy. For pharmaceutical industry, polymorphism is one of the key activities in form selection process together with salt selection. This article introduces the main features in the investigation of solid form selection especially polymorphic behavior with thermodynamic backgrounds, physicochemical properties with solubility, dissolution, and mechanical properties, and characterization techniques for proper analysis. The final form can be recommended based on the physicochemical and biopharmaceutical properties and by the processability, scalability and safety considerations. Pharmaceutical scientists especially in charge of formulation need to be well aware of the above issues to assure product quality.

Isolation of Phytochemicals from Salvia plebeia Using Countercurrent Chromatography Coupled with Reversed-phase HPLC

  • Kil, Hyun Woo;Rho, Taewoong;Seo, Young Ju;Yu, Aram;Yoon, Kee Dong
    • Natural Product Sciences
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    • v.26 no.3
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    • pp.236-243
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    • 2020
  • Salvia plebeia R. Br. is a plant which has been used as an edible crop and traditional medicine in Asian countries. In this study, HPLC-PDA analysis and countercurrent chromatography (CCC) coupled with reversed-phase (RP) HPLC method were applied to isolate ten isolates from 3.3 g of n-butanol soluble extract from hot-water extract of S. plebeia. The use of CCC enabled us to efficiently fractionate the starting material with less sample loss and facilitate the isolation of compounds from S. plebeia extract using RP-HPLC. The isolates were determined to be caffeic acid (1), 6-hydroxyluteolin 7-O-β-D-glucoside (2), eudebeiolide B (3), (R)-rosmarinic acid (4), homoplantaginin (5), eudebeiolide D (6), plebeiolide C (7), salpleflavone (8), eupafolin (9) and hispidulin (10) based on the spectroscopic evidence.

Secondary structure analysis of MRA1997 from Mycobacterium tuberculosis and characterization of DNA binding property

  • Kim, Hyo Jung;Lee, Ki-Young;Kim, Yena;Kwon, Ae-Ran;Lee, Bong-Jin
    • Journal of the Korean Magnetic Resonance Society
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    • v.20 no.2
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    • pp.36-40
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    • 2016
  • MRA1997 is a highly conserved protein from mycobacterial strains. However, no structural and functional information is associated with it. Thus, to obtain details about structure and function of this protein, we have utilized NMR spectroscopy. The recombinant MRA1997 was highly purified and its DNA binding mode was characterized. The tertiary structure of MRA1997 was modeled on the basis of our NMR chemical shift data combined with the webserver CS23D. The binding of MRA1997 with DNA was first monitored by electrophoresis mobility shift assays. The residues involved in DNA binding are identified using NMR chemical shift perturbation experiments. Based on our study, we suggest that MRA1997 interacts with DNA and may play an important role in Mycobacterium tuberculosis physiology.

Antibacterial Activity of Zabofloxacin, a Novel Fluoroquinolone, against Gram-Positive Bacteria (그람양성세균에 대한 새로운 퀴놀론계 항균제 Zabofloxacin의 항균력)

  • Park, Hee-Soo;Jung, Sung-Ji;Jeong, Ji-Woong;Choi, Dong-Rack;Kim, Hyo-Hyun;Choi, Eung-Chil;Kwak, Jin-Hwan
    • YAKHAK HOEJI
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    • v.55 no.1
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    • pp.11-15
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    • 2011
  • Zabofloxacin is a novel broad spectrum fluoroquinolone with excellent anti-pneumococcal activity. We investigated the in vitro activity of zabofloxacin against clinical isolates of gram-positive bacteria and the in vivo activity against systemic infection in mice. Zabofloxacin was very active against gram-positive bacteria except QRSA (Quinolone-resistant S. aureus) and VRE(Vancomycin-resistant Enterococci). Especially, zabofloxacin was extremely potent against clinical isolates of Streptococci. Zabofloxacin was as active as gemifloxacin against systemic infection in mice. In view of its improved antibacterial activities against gram-positive bacteria and good pharmacokinetic profiles in animals, the clinical usefulness of zabofloxacin should be established by further studies.

Backbone 1H, 15N and 13C Resonance Assignment and Secondary Structure Prediction of HP0062 (O24902_HELPY) from Helicobacter pylori

  • Jang, Sun-Bok;Ma, Chao;Park, Sung-Jean;Kwon, Ae-Ran;Lee, Bong-Jin
    • Journal of the Korean Magnetic Resonance Society
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    • v.13 no.2
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    • pp.117-125
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    • 2009
  • HP0062 is an 86 residue hypothetical protein from Helicobacter pylori strain 26695. HP0062 was identified ESAT-6/WXG100 superfamily protein based on structure and sequence alignment and also contains leucine zipper domain sequence. Here, we report the sequence-specific backbone resonance assignment of HP0062. About 97.7% of all $^1H_N,\;^{15}N,\;^{13}C_{\alpha},\;^{13}C_{\beta}\;and\;^{13}C=O$ resonances were assigned unambiguously. We could predict the secondary structure of HP0062 by analyzing the deviation of the $^{13}C_{alpha}\;and\;^{13}C_{\beta}$ chemical shifts from their respective random coil values. Secondary structure prediction shows that HP0062 consist of two ${\alpha}$-helices. This study is a prerequisite for determining the solution structure of HP0062 and can be used for the study on interaction between HP0062 and DNA and other Helicobacter pylori proteins.

The Impact of Prices and Distribution on Customer Satisfaction in the Pharmaceutical Industry of Kazakhstan

  • Аida OMIR;Assel BEKBOSSINOVA;Orazaly SABDEN;Anel A. KIREYEVA
    • Journal of Distribution Science
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    • v.22 no.7
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    • pp.83-94
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    • 2024
  • Purpose: This article aims to investigate the influence of pricing and distribution on the level of satisfaction and purchase decisions among consumers of pharmaceutical products in Kazakhstan. Research design, data, and methodology: A mixed-methods research design was utilized, incorporating primary and secondary data. Primary data were collected through a survey administered to customers across various pharmacy types, with 100 valid responses analyzed. Secondary data involved an extensive review of existing literature and analysis of national statistics concerning the pharmaceutical market trends from 2008 to 2022. Results: The results reveal a complex relationship between price perceptions and customer satisfaction. A significant segment of the population views current drug prices as high, which affects their satisfaction levels and purchase decisions. The study also highlights the importance of service quality in enhancing customer satisfaction, suggesting that service improvements could mitigate some of the negative perceptions of pricing. Conclusions: This research contributes to the limited but growing body of knowledge on the impact of pricing strategies on consumer satisfaction in the pharmaceutical sectors of developing countries like Kazakhstan. Focusing on economic and behavioral aspects, this study provides a more holistic understanding of the factors driving consumer satisfaction and purchase behaviors in this critical sector.

Antioxidant and Hyaluronidase Inhibition Activities of Prunus persica Batsch var. davidiana Maximowicz

  • Cha, Bae-Cheon;Lee, Eun-Hee
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.200.3-200.3
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    • 2003
  • Reactive oxygen species(ROS) are produced at a high rate continuously as a by-product of aerobic metabolism. Several lines of evidence provided that ROS appears to cause to develop aging and various diseases. High level of hyaluronic acid with decreased molecular weight has been detected in patients with inflammatory diseases including rheumatoid arthritis. Hyaluronidase is an endohexosaminidase that initiates the degradation of hyaluronic acid with high molecular weight. Prunus persica Batsch var. davidiana Maximowicz has been known as a korean folk medicine for treatment of neuritis and rheumatism. (omitted)

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A Study on the Factors Influencing the Satisfaction of Certification and Support Policy of Innovative Pharmaceutical Companies : Focusing on the policy formation process variables (혁신형 제약기업 인증·지원 정책만족도에 대한 영향요인 연구 : 정책형성과정 변인을 중심으로)

  • Kim, Daejin;Oh, Kihwan;Ha, Dongmun
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.19 no.8
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    • pp.360-369
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    • 2018
  • Innovative pharmaceutical company certification support policies have been implemented since 2012. This study was conducted to identify the perceptions of stakeholders and related experts on the formation process and policy satisfaction of this policy, and to identify factors that explain policy satisfaction. The survey was conducted by e-mail and facsimile of the pharmaceutical companies, universities, and government - affiliated research institutes. The effective response rate was 38.4% (61/159). As a result of the cross-sectional survey, the perception of policy necessity was the most positive among the policy formation process, and all the other stages and perception of policy satisfaction were at the medium level. As a result of examining the influential factors related to the variables of the respondents' personal variables and the policy formation process, it is confirmed that the factors that have the greatest influence on the policy satisfaction are the perception of the performance of the certified company. Also, perceptions of appropriateness and follow - up ability were similar in magnitude of impact on policy satisfaction. This study can be used as a basic data to systematically and effectively improve the certification and support policies of innovative pharmaceutical companies based on the consumer's perception. However, due to limitations such as being carried out at the beginning of policy implementation, verification and supplementation are necessary through further research.