• 제목/요약/키워드: KPS

검색결과 773건 처리시간 0.024초

Disintegrating Behavior of A Rapidly Disintegrating Famotidine Tablet Formulation

  • Park, Jeong-Sook;Shin, Kwang-Hyun;Park, Jong-Bum;Lee, Si-Beum;Hwang, Sung-Joo
    • Journal of Pharmaceutical Investigation
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    • 제37권5호
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    • pp.275-280
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    • 2007
  • A rapidly disintegration famotidine tablet formulation in the oral cavity was developed using microcrystalline cellulose (MCC) and low-substituted hydroxypropyl cellulose (L-HPC), or additionally cropovidone as an internal disintegrant. Effects of disintegrants on the disintegration time in vitro and hardness were evaluated. Average wetting time of the tablets prepared in scale-up manufacturing process was less than 15 sec. Among the formulations tested, the tablet prepared with crospovidone as an internal disintegrant and Emcocel $90M^{(R)}$ as an external disintegrant showed fastest disintegration. These results may suggest that crospovidone and Emcocel $90M^{(R)}$ possessed excellent wetting nature, which result in the rapid disintegration of tablet.

Effect of Hypoxia on the Doxorubicin Sensitivity of Human MCF-7 Breast Cancer Cells

  • Lim, Soo-Jeong;Kang, He-Kyung
    • Journal of Pharmaceutical Investigation
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    • 제37권5호
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    • pp.287-290
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    • 2007
  • Intrinsic or acquired resistance to chemotherapeutic drugs is one of the major obstacles to effective cancer treatment. Hypoxia is widespread in solid tumors as a consequence of decreased blood flow in the tumor-derived neovasculature. The recent finding of a link between hypoxia and chemoresistance prompted us to investigate whether hypoxia induces doxorubicin resistance in human MCF-7 breast cancer cells. Low oxygen concentration decreased the doxorubicin sensitivity in MCF-7 cells. The expression of p-glycoprotein, a major MDR-related transporter, and those of apoptosis-related proteins (anti-apoptotic Bcl-2, Bcl-XL and pro-apoptotic Bax) were not altered by hypoxia in MCF-7 cells. Intracellular uptake of doxorubicin was significantly decreased under hypoxic conditions. Decreased cellular uptake of doxorubicin under hypoxia may contribute to causing doxorubicin resistance in these cells. The use of agents that can modulate the doxorubicin uptake for adjuvant therapy may contribute to improving the therapeutic efficacy of doxorubicin in breast cancer patients.

Effects of Surface Charges on the Retention of Placenta-loaded Liposome Formulations Administered by Intramuscular Route

  • Noh, Sang-Myoung;Park, Da-Eui;Kim, Young-Bong;Oh, Yu-Kyoung
    • Journal of Pharmaceutical Investigation
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    • 제39권5호
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    • pp.333-337
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    • 2009
  • We aimed to optimize the formulation of porcine placental extract (PPE)-loaded liposomes for intramuscular administration and to investigate the effect of surface charges on the muscular retention in mice. PPE-loaded liposomes were formulated to have neutral, anionic, or cationic surface charges. The in vitro release profiles were studied by spectrofluorometry. In vivo distribution patterns at mice were studied using molecular imaging technology. Among the three types of liposomes, 1,2-dioleoyl-3-trimethylammonium-propane and 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine-based cationic liposomes showed the most prolonged in vitro release profile. Consistent with the in vitro results, the in vivo distribution study revealed that the cationic liposomes were retained at the site of administration for the longest period. Our results suggest the potential of cationic PPE-loaded liposomes for sustained release of the components after intramuscular administration.

Pharmacokinetic-Pharmacodynamic Modeling of a Direct Thrombin Inhibitor, Argatroban, in Rats

  • Park, Eun-Hye;Shin, Beom-Soo;Yun, Chi-Ho;Lee, Mann-Hyung;Yoo, Sun-Dong
    • Journal of Pharmaceutical Investigation
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    • 제39권5호
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    • pp.373-379
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    • 2009
  • This study was conducted to develop a pharmacokinetic-pharmacodynamic (PK/PD) model of a direct thrombin inhibitor, argatroban to predict the concentration-effect profiles in rats. Argatroban was i.v. injected to rats at 0. 2, 0.8 and 3.2 mg/kg doses (n = 4-5 per dose), and plasma drug levels were determined by a validated LC/MS/MS assay. The pharmacokinetics of argatroban was linear over the i.v. dose range studied. The thrombin time (TT) and the activated partial thromboplastin time (aPTT) were measured in rat plasma and they were found to linearly increase with increasing the dose. A 2-compartment pharmacokinetic model linked with an indirect response pharmacodynamic model was successfully utilized to evaluate the drug concentration-response relationship.

Stability of Octreotide Acetate in Aqueous Solutions and PLGA Films

  • Ryu, Ki-Won;Na, Dong-Hee
    • Journal of Pharmaceutical Investigation
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    • 제39권5호
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    • pp.353-357
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    • 2009
  • As a synthetic analog of the naturally occurring hormone somatostatin, octreotide has been commercially formulated in poly(lactide-co-glycolide) (PLGA) microspheres for the treatment of acromegaly. The purpose of this study was to evaluate stability of octreotide acetate in aqueous solutions at various pH values and PLGA films. Stability-indicating reversed-phase high-performance liquid chromatographic method was developed with good precision and accuracy, and it was applied to the stability studies. In aqueous solutions at pH 2.5-9.0, the degradation of octreotide followed approximately first order kinetics and the most favorable stability was found at pH 4. In PLGA films, the formation of acylated octreotides reached approximately 55% of the released octreotides. Various acylated octreotides was structurally identified by liquid chromatography-mass spectrometric analysis.

소성변형에 의한 배관 용접부의 잔류응력 개선 방법 (A Method of Residual Stress Improvement by Plastic Deformation in the Pipe Welding Zone)

  • 최상훈;왕지남
    • 설비공학논문집
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    • 제25권10호
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    • pp.568-572
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    • 2013
  • The main components, such as a reactor vessel, in commercial nuclear power plants have been welded to pipes with dissimilar metal in which Primary Water Corrosion Cracking (PWSCC) has been occurred. PWSCC has become a worldwide issue recently. This paper addresses the results of experimental and numerical analysis to prevent PWSCC by changing the stress profile that is tensile stress to compressive stress at interesting regions with plastic deformation generated by mechanical pressure. Based on the results of experimental and numerical analysis with a 6 inch pipe and dissimilar metal welded pipes, compressive stress 68~206 Mpa is generated at all locations of inner surface in the heat affected zone.

Determining Two-Sided Surface Profiles of Micro-Optical Elements Using a Dual-Wavelength Digital Holographic Microscope With Liquids

  • Lee, Hong Seok;Shin, Sanghoon;Lee, Heonjoo;Yu, Younghun
    • Journal of the Optical Society of Korea
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    • 제18권5호
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    • pp.495-499
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    • 2014
  • In this paper, a method is proposed for simultaneously measuring the front and back surface profiles of transparent micro-optical components. The proposed method combines a dual-wavelength digital holographic microscope with liquids to record holograms at different wavelengths, and then numerically reconstructs the three-dimensional phase information to image the front and back sides of the sample. A theoretical model is proposed to determine the surface information, and imaging of an achromatic lens is demonstrated experimentally. Unlike conventional interferometry, our proposed method supports nondestructive measurement and direct observation of both front and back profiles of micro-optical elements.

Effect of Scutellariae Radix Extract on Human CYP450 Mediated-Drug Metabolism

  • Yoo, Hye-Hyun;Lim, Sun-Young;Kim, Dong-Hyun
    • Journal of Pharmaceutical Investigation
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    • 제41권3호
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    • pp.143-146
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    • 2011
  • Scutellariae Radix is widely used in the traditional herbal medicine for the treatment of fever, cough, dysentery, hepatitis and hypertension in Korea, China and Japan. In this study, we investigated the effects of 70% ethanolic extract of Scutellariae Radix (SRE) on CYP450-mediated drug metabolism in the in vitro systems using human liver microsomes and hepatocytes. The microsomal incubation assay showed that SRE inhibited the drug metabolism reactions catalyzed by CYP1A2, CYP2C8 and CYP2C9 in a dose-dependent manner. In particular, SRE was shown to strongly inhibit the metabolic activity of CYP1A2 with an $IC_{50}$ value of 4.6 ${\mu}g/mL$. When SRE was evaluated for its effect on the induction of CYP450 enzyme activities in cryopreserved human hepatocytes, SRE did not exhibit any effect.

Preparation and Evaluation of Novel Fenofibrate-loaded Self-Microemulsifying Drug Delivery System (SMEDDS)

  • Cho, Young-Dae;Park, Young-Joon
    • Journal of Pharmaceutical Investigation
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    • 제40권6호
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    • pp.339-345
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    • 2010
  • Fenofibrate has been used for many years to lower cholesterol levels and its pharmacokinetic profile is well understood. However, due to its low solubility in water, it has low bioavailability after oral administration. In order to improve the dissolution rate, fenofibrate was formulated into a self-microemulsifying drug delivery systems (SMEDDS). We used pseudo-ternary phase diagrams to evaluate the area of microemulsification, and an in vitro dissolution test was used to investigate the dissolution rate of fenofibrate. The optimized formulation for in vitro dissolution assessment consisted of Lauroglycol FCC (60%), Solutol HS 15 (27%), and Transcutol-P (13%). The mean droplet size of the oil phase in the microemulsion formed from the SMEDDS was about 130 nm. The dissolution rate of fenofibrate from SMEDDS was significantly higher than that of the reference tablet. Our studies suggested that the fenofibrate containing SMEDDS composition can effectively increase the solubility and oral bioavailability of poorly water-soluble drugs.

새로운 약물전달체계 회사 데이터베이스의 구축 (Newly Established Drug Delivery Systems Company Database)

  • 한인구;정혜선
    • Journal of Pharmaceutical Investigation
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    • 제38권6호
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    • pp.429-432
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    • 2008
  • Drug delivery systems (DDS) have entered mainstream in the pharmaceutical industry in the recent years. Major pharmaceutical companies as well as small or medium-sized biotechnology companies are developing various DDS-based products. We have established Drug Delivery System Company Database, which is an online searchable database of companies that develop DDS-based products and technologies or supply formulations and/or materials. Company summary, products and key technologies are listed in the database. DDS technology fields also include administration routes and indications of drugs. DDS terminologies, Statistical analysis, Useful Links, Glossary and Comments pages are also provided.