• Title/Summary/Keyword: Polymeric drug

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Crosslinking reaction system of polymers (고분자 가교반응 시스템)

  • Ko, Jong-Sung
    • Journal of the Korean Applied Science and Technology
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    • v.29 no.1
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    • pp.19-32
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    • 2012
  • Pharmaceutical use accounts for a great part of articles and papers on crosslinking of polymers. Crosslinking of polymers used for tissue engineering and drug delivery respects non-cytotoxicity and in situ gelling. The crosslinking of polymers is aimed not only at the improvement of modulus, chemical resistance, and thermal resistance, but also at endowing them with such functions as metal adsorption, antifouling, and ion exchange via crosslinked segments. Smart polymers responding to environmental change, and cosslinking mediated by light, enzyme, natural compound and in aqueous medium in consideration of environment are being studied. Developing new polymeric materials is essential along with the pharmaceutics aiming at the longevity of 120 years old. Functionalization and property adjustment of polymers through crosslinking will be done more delicately. Hydrogels will be focused on injectable and in situ gel forming. In the coating industry crosslinking system with low non-toxicity and low energy consumption will be developed in consideration of workers and environment.

Formulation and Pharmacokinetic Evaluation of Sustained Release Preparation Containing Clebopride Malate (말산클레보프리드 서방성 제제의 제조 및 약물동태학적 평가)

  • Ryou, Hae-Won;Lee, Joo-Han;Chi, Yong-Ha;Hahn, Yang-Hee;Tan, Hyun-Kwang;Lee, Kyu-Heung;Kim, Sang-Lin;Jeon, Seung-Yoon;Choi, Young-Wook
    • Journal of Pharmaceutical Investigation
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    • v.30 no.3
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    • pp.179-189
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    • 2000
  • Clebopride malate(Cm) is a new benzamide drug which has a potent central antidopaminergic activity possessing antiemetic and anxiolytic properties. A purpose of this study was to assess the feasibility of formulating sustained release preparation by dispersing a drug in hydrophilic polymeric matrices and double layered tablets(DLT), using HPMC, carbopol, PEO, PVP/VA and other polymers as a rate controlling barrier. The matrix and DLT showed optimum dissolution pattern up to 8 hours and the contents of polymer were optimized at 30% level in this preparation. After an oral administration in beagle dog, Cm concentration was determined by use of GC-ECD and pharmacokinetic parameters were calculated by Vallner's method. The AUC of DLT showed similar results and the duration of action was increased 55% compared to that of regular release dosage form. The calculated absorption rate effectiveness(ARE) and controlled release effectiveness(CRE) for DLT increased 50% compared to that of matrix, the overall effectiveness(E) of this product appears to be about 70%. in vivo effectiveness test, DLT showed significant differences from control on antiemetic action of Cm. In consequence, it was possible to conclude that double layered tablet might be a good candidate for the sustained release dosage forms.

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Preparation and Characterization of Solid Dispersions of Eprosartan with Hydrophilic Polymers (친수성 고분자를 이용한 에프로살탄 고체분산체의 제조 및 특성 분석)

  • Hwang, Jun-Seok;Ko, Ji-Eun;Kim, So-Hee;Huh, Kang-Moo
    • Polymer(Korea)
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    • v.36 no.4
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    • pp.500-506
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    • 2012
  • In this study, we developed and optimized hydrophilic polymer based solid dispersion formulations (SDs) for enhancing the aqueous solubility of eprosartan, one of poorly soluble drugs, that has been broadly used for the treatment of high blood pressure. Poly(ethylene glycol) (PEG) and poly(vinyl pyrrolidone) (PVP) based SDs were prepared by hot melting and solvent evaporation methods and the drug/polymer composition varied in the range of 1:1~1:5 with or without poloxamer 407 (P407) as a polymeric surfactant. The SDs prepared by solvent evaporation showed more reduced crystallinity than ones by hot melting, and PVP based SDs showed more enhanced solubility and lower crystallinity than PEG based SDs. Furthermore, it was observed from DSC and PXRD analysis that the SDs with P407 (drug:polymer: P407 = 1:5:1) demonstrated no crystallinity and the most enhanced solubility (more than 3~4 times).

Photocatalytic Membrane for Contaminants Degradation: A Review (오염물질 분해를 위한 광촉매 분리막: 총설)

  • Kahkahni, Rabea;Patel, Rajkumar;Kim, Jong Hak
    • Membrane Journal
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    • v.32 no.1
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    • pp.33-42
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    • 2022
  • Growing industrialization leads to severe water pollution. Organic effluents from pharmaceuticals and textile industries released in wastewater adversely affect the environment and human health. Presence of antibiotics used for antibacterial treatment in wastewater leads to the growth of drug resistance bacteria, which is very harmful for human being. Various small organic molecules are used for the preparation of organic dye molecules in the textile industries. These molecules hardly degrade, which is present in the wastewater effluents from printing and dyeing industries. In order to address these problems, photoactive catalyst is embedded in the membrane and wastewater are passed through it. Through this process, organic molecules are photodegraded and at the same time, the degraded compounds are separated by the membrane. Titanium dioxide (TiO2) is a semiconductor which behave as excellent photocatalyst. Photocatalytic ability is enhanced by the making its composite with other transition metal oxide and incorporated into polymeric membrane. In this review, the degradation of dye and drug molecules by photocatalytic membrane are discussed.

Improvement of Dissolution rate of Felodipine Using Solid Dispersion and its Sustained Release Oral Dosage Form (고체분산체에 의한 펠로디핀의 용출율 개선과 서방성 경구제제)

  • Gil, Young-Sig;Hong, Seok-Cheon;Yu, Chang-Hun;Shin, Hyun-Jong;Kim, Jong-Sung
    • Journal of Pharmaceutical Investigation
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    • v.32 no.3
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    • pp.185-190
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    • 2002
  • To improve the solubility of poorly water-soluble drug and to develop a sustained release tablets, the need for the technique, the formation of solid dispersion with polymeric materials that can potentially enhance the dissolution rate and extent of drug absorption was considered in this study. The 1:1, 1:4, and 1:5 solid dispersions were prepared by spray drying method using PVP K30, ethanol and methylene chloride. The dissolution test was carried out at in phosphate buffer solution at $37^{\circ}C$ in 100 rpm. Solid dispersed drugs were examined using differential scanning calorimetry and scanning electron microscopy, wherein it was found that felodipine is amorphous in the PVP K30 solid dispersion. Felodifine SR tablets were prepared by direct compressing the powder mixture composed of solid dispersed felodipine, lactose, Eudragit and magnesium stearate using a single punch press. In order to develop a sustained-release preparation containing solid dispersed felodipine, a comparative dissolution study was done using commercially existing product as control. The dissolution rate of intact felodipine, solid dispersed felodipine and its physical mixture, respectively, were compared by the dissolution rates for 30 minutes. The dissolution rates of felodipine for 30 minutes from 1:1, 1:4, 1:5 PVP K30 solid dispersion were 70%, 78% and 90%. However, dissolution rate offelodipine from the physical mixture was 5% of drug for 30 minutes. Our developed product Felodipine SR Tablet showed dissolution of 17%, 50% and 89% for 1, 4, and 7 hours. This designed oral delivery system is easy to manufacture, and drug releases behavior is highly reproducible and offers advantages over the existing commercial product. The dissolution rate of felodipine was significantly enhanced, following the formation of solid dispersion. The solid dispersion technique with water-soluble polymer could be used to develop a solid dispersed felodipine SR tablet.

Preparation and Characterization of Alginate-Chitosan Microsphere for Controlled Delivery of Silver Sulfadiazine (설파디아진은의 방출제어를 위한 알지네이트-키토산 미립구의 제조 및 특성)

  • Cho, Ae-Ri
    • Journal of Pharmaceutical Investigation
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    • v.31 no.2
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    • pp.101-106
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    • 2001
  • Alginate-chitosan (anion-cationic polymeric complex) was prepared to control the release rate of silver sulfadiazine (AgSD). Na-alginate (2%) solution containing AgSD was gelled in $CaCl_2$ solution. The gel beads formed were immediately encapsulated with chitosan (CS). The gel matrix and membrane were then reinforced with chondroitin-6-sulfate (Ch6S). Release rate of AgSD from the gel matrix was investigated by placing alginate beads in the sac of cellulose membrane simmered in HEPES-buffer solution. The concentration of AgSD released was analyzed by UV at 264 nm. Incorporation capacity of AgSD in Ca-alginate gel was more than 90%. Alginate-Ch6S-CS could control the release rate of AgSD. The amount of AgSD release was dependent on the AgSD loading dose. Incorporation of tripolyphosphate (polyanionic crosslinker) onto the alginate-Ch6S-CS bead increased the release rate of AgSD. Collagen-coating had no influence on the AgSD release rate. Alginate-Ch6S-CS beads with a sufficiently high AgSD encapsulation were capable of controlling the release of the drug over 10 days. In summary, alginate-Ch6S-CS beads could be used as a sustained delivery for AgSD and provide local targeting with low silver toxicity and patient discomfort.

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Nanoparticle Induced Oxidative Stress in Cancer Cells: Adding New Pieces to an Incomplete Jigsaw Puzzle

  • Nogueira, Daniele Rubert;Rolim, Clarice M. Bueno;Farooqi, Ammad Ahmad
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.12
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    • pp.4739-4743
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    • 2014
  • Nanotechnology is an emerging field with many promising applications in drug delivery systems. Because of outstanding developments in this field, rapidly increasing research is directed to the development of nanocarriers that may enhance the availability of drugs to the target sites. Substantial fraction of information has been added into the existing scientific literature focusing on the fact that nanoparticles usually generate reactive oxygen species to a greater extent than micro-sized particles. It is worth mentioning that oxidative stress regulates an array of cell signaling cascades that resulted in cancer cell damage. Accumulating experimental evidence over the years has shown that wide-ranging biological mechanisms are triggered by these NPs in cultured cells due to the unique properties of engineered nanoparticles. In this review, we have attempted to provide an overview of the signaling cascades that are activated by oxidative stress in cancer cells in response to different kinds of nanomaterials, including quantum dots, metallic and polymeric nanoparticles.

Synthesis of KIT-1 Mesoporous Silicates Showing Two Different Macrosporous Strucrtues; Inverse-opal or Hollow Structures (거대기공 구조-역오팔 또는 중공 구조를 갖는 KIT-1 메조포러스 실리케이트의 제조)

  • Baek, Youn-Kyoung;Lee, Jung-Goo;Kim, Young Kuk
    • Journal of Powder Materials
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    • v.23 no.3
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    • pp.189-194
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    • 2016
  • We report a facile method for preparing KIT-1 mesoporous silicates with two different macroporous structures by dual templating. As a template for macropores, polystyrene (PS) beads are assembled into uniform three dimensional arrays by ice templating, i.e., by growing ice crystals during the freezing process of the particle suspension. Then, the polymeric templates are directly introduced into the precursor-gel solution with cationic surfactants for templating the mesopores, which is followed by hydrothermal crystallization and calcination. Later, by burning out the PS beads and the surfactants, KIT-1 mesoporous silicates with macropores are produced in a powder form. The macroporous structures of the silicates can be controlled by changing the amount of EDTANa4 salt under the same templating conditions using the PS beads and inverse-opal or hollow structures can be obtained. This strategy to prepare mesoporous powders with controllable macrostructures is potentially useful for various applications especially those dealing with bulky molecules such as, catalysis, separation, drug carriers and environmental adsorbents.

Controlled Release and Stabilization of Cefaclor from Alginate-based Matrices for Oral Delivery Design

  • Bak, So-Im;Lee, Jue-Yeon;Song, Hye-Won;Hwang, Jeong-Hyo;Lee, Seung-Jin
    • Journal of Pharmaceutical Investigation
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    • v.32 no.4
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    • pp.327-330
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    • 2002
  • Alginate based polymeric matrices were designed for controlled release and stabilization of cefaclor in gastrointestinal fluid. Cefaclor is known to be acid stable and subjected to be degraded at neutral and alkaline pHs. In order to achieve an effective release profile of cefaclor in gastrointestinal tract, a particular strategy in dosage form design should be required from the view point of maintaining its activity. The amphiphilic nature of cefaclor allowed its controlled release using ionic polymers based on ionic interaction between the drug and polymers. The thrust of this study was to develop a technique that delivers cefaclor keeping effective release rate in the intestinal tract. Considering the fast degradation of cefaclor in the intestinal fluid, the matrices were designed to release surplus amount of cefaclor. The alginate based matrices demonstrated increase in release rate in the simulated intestinal fluid, which was favorable to compensate the degraded portion of cefaclor. In addition, stabilization of cefaclor in the intestinal fluid was obtained by employing citric acid that provides an local acidic environment. The matrices might be valuably used for the development of an oral cefaclor dosage form.

Morphology Development in a Range of Nanometer to Micrometer in Sulfonated Poly(ethylene terephthalate) Ionomer

  • Lee, Chang-Hyung;Inoue, Takashi;Nah, Jae-Woon
    • Bulletin of the Korean Chemical Society
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    • v.23 no.4
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    • pp.580-586
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    • 2002
  • We investigated the effect of ionic component on crystalline morphology development during isothermal annealing in a sodium neutralized sulfonated poly(ethylene terephthalate) ionomer (Ion-PET) by time-resolved small-angle x-ray scattering (TR-SAX S) using synchrotron radiation. At early stage in Ion-PET, SAXS intensity at a low annealing temperature (Ta = 120 $^{\circ}C)$ decreased monotonously with scattering angle for a while. Then SAXS profile showed a peak and the peak position progressively moved to wider angles with isothermal annealing time. Finally, the peak intensity decreased, shifting the peak angle to wider angle. It is revealed that ionic aggregates (multiplets structure) of several nm, calculated by Debye-Bueche plot, are formed at early stage. They seem to accelerate the crystallization rate and make fine crystallites without spherulite formation (supported by optical microscopy observation). From decrease of peak intensity in SAXS,it is suggested that new lamellae are inserted between the preformed lamellae so that the concentration of ionic multiplets in amorphous region decreases to lower the electron density difference between lamellar crystal and amorphous region. In addition, analysis on the annealing at a high temperature (Ta = 210 $^{\circ}C)$ by optical microscopy, light scattering and transmission electron microscopy shows a formation of spherulite, no ionic aggregates, the retarded crystallization rate and a high level of lamellar orientation.