• Title/Summary/Keyword: Controlled-release

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Development of Controlled Release Oral Drug Delivery System by Membrane-Coating Method-III- Preparation of Theophylline Tablets and Pharmacokinetic Evaluation in Man- (피막법에 의한 경구투여용 제어방출제제의 개발-III-테오필린함유 제어방출제제의 제조 및 사람의 타액중 농도로부터의 평가-)

  • Shim, Chang-Koo;Kim, Chong-Kook;Lee, Min-Hwa;Kim, Shin-Keun
    • Journal of Pharmaceutical Investigation
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    • v.22 no.3
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    • pp.205-210
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    • 1992
  • In order to develop a controlled-release oral drug delivery system (DDS) of theophylline (TP), microporous membrane-coated tablets were prepared and evaluated in vitro and in vivo. Rapidly water-soluble core tablets of TP (300 mg) were prepared by wet granulation and compression technique, Then the core tablets were spray-coated with polyvinylchloride (PVC) in which micronized sucrose particles were dispersed. Effect of formula compositions of coating suspensions on the pharmaceutical characteristics such as membrane strength and dissolution was investigated in vitro. The membranes remained unbroken in pH 1.2 buffer at $37^{\circ}C$ at least for 2 hours after the disintergration test. TP was released from the coated-released tablets at a zero-order rate over 8 hours. The release at pH 1.2 and 4.0 was similar in rate but a little more rapid than that at pH 6.8. The coated tablets were administered to three healthy male volunteers and their saliva profiles of TP were compared with those from the commercial sustained release TP tablets such as Slobid and Asconthin. Saliva TP concentrations from the coated tablets were successfully sustained over 48 hours after the dosing and were comparable to those of the commercial sustained-release tablets. The membrane-coating technique is very simple and does not need any sophisticated equipments. In this respect, the membrane-coated tablets may be superior to the commercial sustained-release tablets and this technique is worth adopting by the pharmaceutical industries.

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Controlled Release of Tamsulosin from Enteric Coated Sustained-Release Matrices with Aqueous Microchannels (수성미세채널을 형성하는 서방성 매트릭스 장용정을 이용한 탐스로신의 방출제어)

  • Lee, Ki-Bong;Choi, Sung-Up;Jeon, Hong-Ryeol;Lee, Bong-Sang;Kim, Hyun-Il;Lee, Jae-Hwi;Choi, Young-Wook
    • Journal of Pharmaceutical Investigation
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    • v.34 no.6
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    • pp.471-475
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    • 2004
  • Tamsulosin has been frequently used for the treatment of benign prostatic hyperplasia. To avoid dose-dependent side effects of tamsulosin upon oral administration, the development of sustained-release delivery system is required, that can maintain therapeutic drug levels for a longer period of time. The aim of this study was therefore to formulate sustained-release tamsulosin matrix tablets and assess their formulation variables. We designed enteric coated sustained-release tamsulosin matrices to fulfill above statement. Aqueous microchannels in the enteric film need to be formed in order to obtain tamsulosin release even in an acidic environment such as gastric region. In the sustained-release tamsulosin matrix, low viscosity hydroxypropylmethylcellulose was used as a rate controller. Povidone K30 was also added to the matrices to facilitate water uptake so that a decrease in the release rate of tamsulosin as time elapses was prevented, possibly leading to pseudo zero-order release of the drug. The matrices were enteric-coated with hydroxypropylmethylcellulose phthalate (HPMCP), along with povidone K30 as an aqueous microchannel former. With the aqueous microchannels formed within the enteric film, tamsulosin could be released in an acidic condition. The release of tamsulosin decreased with increasing thickness of HPMCP membrane while the release rates of tamsulosin from those having different HPMCP thickness in pH 7.2 aqueous media were not considerably different, indicating that the enteric film was promptly dissolved at pH 7.2. These results clearly suggest that the sustained-release oral delivery system for tamsulosin could be designed with satisfying drug release profile approved by the KFDA.

Encapsulation of Flavors by Molecular Inclusion Using $\beta$-Cyclodextrin: Comparison with Spray-drying Process Using Carbohydrate-based Wall Materials

  • Cho, Young-Hee;Park, Ji-Yong
    • Food Science and Biotechnology
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    • v.18 no.1
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    • pp.185-189
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    • 2009
  • Microencapsulation of flavor was carried out by molecular inclusion process using $\beta$-cyclodextrin (${\beta}CD$). ${\beta}CD$-flavor complex was prepared at various flavor-to-${\beta}CD$ ratios (1:6-1:12) to determine the effect of ${\beta}CD$ concentration on the inclusion efficiency. Maximum total oil retention and minimal surface oil content were obtained at flavors to ${\beta}CD$ ratio of 1:10. The physical properties and controlled release pattern of flavors from ${\beta}CD$-flavor complex were measured and compared with spray-dried microcapsules prepared using carbohydrate wall system. ${\beta}CD$-flavor complex showed higher total oil retention and surface oil contents, smaller mean particle size, lower moisture uptake, and higher oxidation stability than spray-dried microcapsule. Oxidative stability of flavor was correlated with hygroscopicity of wall materials. The controlled release mechanism was highly affected by temperature and characteristics of wall materials.

Controlled Release Behavior of pH-Responsive Composite Hydrogel Containing Activated Carbon

  • Yun, Ju-Mi;Im, Ji-Sun;Oh, Ae-Ri;Lee, Young-Seak;Kim, Hyung-Il
    • Carbon letters
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    • v.10 no.1
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    • pp.33-37
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    • 2009
  • Activated carbon (AC) is one of the most effective adsorbents for organic compounds because of their extended surface area, high adsorption capacity, microporous structure and special surface reactivity. The composites of pH-sensitive hydrogel and activated carbon were prepared in order to improve the loading capacity of drug. The pH-sensitive hydrogel matrix swelled well in the basic condition to release the drug loaded in AC. The release of drug was controlled depending on both the pH due to the ionization of the carboxylic acid group and the AC due to the surface properties.

In Vitro Controlled Release of Piracetam with Coated Ion-Exchange Resin (이온교환수지를 이용한 피라세탐의 in vitro 방출조절)

  • Hwang, Young-Sook;Lee, Kyung-Tae;Seo, Seong-Hoon
    • Journal of Pharmaceutical Investigation
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    • v.29 no.2
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    • pp.105-109
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    • 1999
  • The sustained release of piracetam by complexation with ion exchange resin was prepared. The complex was coated with Eudragit RS100 and their releases in vitro were conducted with various different kinds of medium solution. Dissolution rate increased as ionic strength, acidity and drug concentrations increased and reached its maximal plateau concentration within 5 min. Based on these data, The controlled release of piracetam using ion-exchange piracetam complex coated with Eudragit RS100 could be available.

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Controlled Release Behavior of Temperature Responsive Composite Hydrogel Containing Activated Carbon

  • Yun, Ju-Mi;Im, Ji-Sun;Jin, Dong-Hwee;Lee, Young-Seak;Kim, Hyung-Il
    • Carbon letters
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    • v.9 no.4
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    • pp.283-288
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    • 2008
  • The composites of temperature-sensitive hydrogel and activated carbons were prepared in order to improve both the mechanical strength of hydrogel matrix and the loading capacity of drug in a hydrogel drug delivery system. The swelling of composite hydrogel was varied depending on the temperature. Both the swelling and the release behavior of the composite hydrogel were varied depending on the kind of activated carbon. The release behavior showed the high efficiency which is important for practical applications.

Swelling Controlled Delivery of Antibiotic from a Hydrophilic Macromolecular Matrix with Hydrophobic Moieties

  • Shukla, Sandeep;Bajpai, Anil Kumar;Bajpai, Jaya
    • Macromolecular Research
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    • v.11 no.4
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    • pp.273-282
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    • 2003
  • A hydrophilic macromolecular network containing hydrophobic moieties has been prepared by free radical copolymerization of acrylamide and styrene in the presence of poly(vinyl alcohol) (PVA) and its potential as controlled drug delivery carrier was evaluated with tetracycline as a model antibiotic drug. The amount of drug was assayed spectrophotometrically. The network was characterized by optical microscopy, infra-red spectroscopy and structural parameters such as average molecular weight between cross1inks ($M_c$), cross1ink density (q) and number of elastically effective chains ($V_e$) were evaluated. It was found that with increasing concentration of PVA, ST and MBA in the hydrogel, the release rate initially increases but after definite concentrations of the above components the release rate falls. In the case of AM, release rate constantly decreases with increasing AM concentration in the hydrogel.

Effects of Solvent Selection and Fabrication Method on the Characteristics of Biodegradable Poly(lactide-co-glycolide) Microspheres Containing Ovalbumin

  • Cho, Seong-Wan;Song, Seh-Hyon;Shoi, Young-Wook
    • Archives of Pharmacal Research
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    • v.23 no.4
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    • pp.385-390
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    • 2000
  • To demonstrate the effect of formulation conditions on the controlled release of protein from poly(lactide-co-glycolide) (PLGA) microspheres for use as a parenteral drug carrier, ovalbumin (OVA) microspheres were prepared using the W/O/W multiple emulsion solvent evaporation and extraction method. Methylene chloride or ethyl acetate was applied as an organic phase and poly(vinyl alcohol) as a secondary emulsion stabilizer. Low loading efficiencies of less than 20% were observed and the in vitro release of OVA showed a burst effect in all batches of different microspheres, followed by a gradual release over the next 6 weeks. Formulation processes affected the size and morphology, drug content, and the controlled release of OVA from PLGA microspheres.

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Analysis of cell survival genes in human gingival fibroblasts after sequential release of trichloroacetic acid and epidermal growth factor using the nano-controlled release system (나노방출제어시스템을 이용하여 trichloroacetic acid와 epidermal growth factor의 순차적 방출을 적용한 인간치은섬유아세포의 세포생존 관련 유전자 연구분석)

  • Cho, Joon Youn;Lee, Richard sungbok;Lee, Suk Won
    • Journal of Dental Rehabilitation and Applied Science
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    • v.36 no.3
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    • pp.145-157
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    • 2020
  • Purpose: This study was to determine the possible effects of trichloroacetic acid (TCA) and epidermal growth factor (EGF) through cell survival genes of the PI3K-AKT signaling pathway when applying an hydrophobically modified glycol chitosan (HGC)-based nanocontrolled release system to human gingival fibroblasts in oral soft tissue regeneration. Materials and Methods: An HGC-based nano-controlled release system was produced, followed by the loading of TCA and EGF. The group was divided into control (CON), TCA-loaded nano-controlled release system (EXP1), and the TCA- and EGF- individually loaded nano-controlled release system (EXP2). A total for 29 genes related to the PI3K-AKT signaling pathway were analyzed after 48h of culture in human gingival fibroblasts. Real-time PCR, 1- way ANOVA and multiple regression analysis were performed. Results: Cell survival genes were significantly upregulated in EXP1 and EXP2. From multiple regression analysis, ITGB1 was determined to be the most influential factor for AKT1 expression. Conclusion: The application of TCA and EGF through the HGC-based nano-controlled release system can up-regulate the cell survival pathway.

Fabrication and Characterization of Flurbiprofen loaded Chitosan Beads for Periodontal Regeneration (치주조직 재생용 플루르비프로펜 함유 키토산 비드의 제조 및 용출특성)

  • Rhee, Su-Jin;Park, Yoon-Jeong;Lee, Seung-Jin;Chung, Chong-Pyoung
    • Journal of Pharmaceutical Investigation
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    • v.27 no.1
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    • pp.71-77
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    • 1997
  • With the aim of improving periodontal regeneration efficacy, as a biodegradable local drug delivery device, drug releasing chitosan beads were prepared. Chitosan beads were prepared through the formation of intermolecular or intramolecular ionic interaction bewteen chitosan and sodium tripolyphosphate and were loaded with flurbiprofen. The mean diameter of the beads was $250\;{\mu}m$. Drug loading efficiency was improved by regulating the pH of tripolyphosphate solution. The drug release kinetics mainly depended upon the hydrophobic properties of the flurbiprofen, that is, the release of flurbiprofen showed initial burst with rapid release for the first day followed by a levelling off of the release rate. However, the release rate could be controlled by the formulation factor including the pH, concentration of the tripolyphosphate solution, gelation time, drug contents. From these results, flurbiprofen loaded chitosan beads were anticipated as biodegradable local drug delivery devices for periodontal regeneneration.

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