• Title/Summary/Keyword: drug release rate

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Preparation and Drug Release Properties of Naproxen Imprinted Biodegradable Polymers Based Multi-Layer Biomaterials (나프록센이 각인된 생분해성 고분자 기반 다층 바이오소재의 제조 및 약물 방출 특성)

  • Eun-Bi Cho;Han-Seong Kim;Min‑Jin Hwang;Soon-Do Yoon
    • Applied Chemistry for Engineering
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    • v.34 no.2
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    • pp.161-169
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    • 2023
  • In this study, we prepared naproxen (NP) imprinted biodegradable polymer based multi-layer biomaterials using allbanggae starch (ABS), polyvinyl alcohol (PVA), and alginic acid (SA), and investigated their physicochemical properties and the controlled drug release effects. In addition, the prepared multi-layer biomaterials were characterized by FE-SEM and FT-IR. In order to confirm the controlled drug release effect for the transdermal drug delivery system (TDDS), the NP release properties of NP imprinted multi-layer biomaterials were investigated using various pH buffer solutions and artificial skin at 36.5 ℃. The results of NP release in various pH buffer solutions indicated that the NP release at high pH was about 1.3 times faster than that at low pH. In addition, NP release in multi-layer biomaterials was about 4.0 times slower than that in single-layer biomaterials. It was confirmed that the NP release rate in triple-layer biomaterials was 4.0 times slower than that in single-layer biomaterials while using artificial skin. Also, it could be found that NP in double-layer biomaterials and triple-layer biomaterials was released sustainably for 12 h. The NP release mechanism in pH buffer solutions followed the Fickian diffusion mechanism, but followed the non-Fickian diffusion mechanism with artificial skin.

Development of Automated Diffusion Cell for Determining In Vitro Drug Release from Transdermal Device (경피흡수제형의 in vitro 약물방출실험을 위한 연속확산 장치의 개발)

  • Byun, Young-Rho;Choi, Young-Kweon;Jeong, Seo-Young;Kim, Young-Ha
    • YAKHAK HOEJI
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    • v.34 no.3
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    • pp.161-165
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    • 1990
  • An automated, simple, and reliable method was developed for determining in vitro drug release rate from transdermal delivery dosage forms. The patch is held in position in the heating block by sandwiching it between the middle plate and the bottom plate of diffusion cell. The dissolution profile of the commercially available transdermal scopolamine patch was determined over a 72-h period, and the results were compared with those obtained with other methods; paddle-over-disk method, reciprocating method, and diffusion cell method. It was demonstrated that the flow-through method is equivalent in terms of release rate profile and accumulated released drug amount over the lifetime of the dosage form tested. Also this method is simple, reliable and reproducible. Therefore, this technique can be used in a quality control for assuring product uniformity.

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The Preparation of Controlled-Release Microcapsules for Captopril and Their Dissolution Characteristics (제어 방출협 캅토프릴 마이크로캅셀의 제조 및 용출 특성)

  • Choi, Hyun-Soon;Ge, Jiang;Lee, Gye-Won;Jee, Ung-Kil
    • Journal of Pharmaceutical Investigation
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    • v.28 no.1
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    • pp.7-13
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    • 1998
  • The captopril microcapsules were prepared and were investigated by measuring their size distribution using Scanning Electron Microscopy(SEM) and dissolution of captopril. Cetyl alcohol microcapsules prepared by emulsion melted-cooled method with various ratios of drug to cetyl alcohol were spherical and uniform. The release rate of cetyl alcohol microcapsules was decreased proportionally as the content of cetyl alcohol increased but, the particle size of microcapsules was increased. The surface of cetyl alcohol microcapsules was comparatively rough as drug content increased. Pellet type microcapsules were prepared using fluidized-bed coating system by spraying captopril solution on nonpareil-seeds followed by applying $Eudragit^{\circledR}$ RS solution containing propylene glycol as a plasticizer. The release rate of drug from pellet type microcapsules decreased as the content of $Eudragit^{\circledR}$ RS increased.

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Preparation and Characterization of pH-Sensitive Poly(ethylene oxide) Grafted Methacrylic Acid and Acrylic Acid Hydrogels by ${\gamma}-ray $ Irradiation

  • Lim, Youn-Mook;Lee, Young-Moo;Nho, Young-Chang
    • Macromolecular Research
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    • v.13 no.4
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    • pp.327-333
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    • 2005
  • pH-sensitive hydrogels were studied as a drug carrier for the protection of insulin from the acidic environment of the stomach before releasing it in the small intestine. In this study, hydrogels based on poly(ethylene oxide) (PEO) networks grafted with methacrylic acid (MAA) or acrylic acid (AAc) were prepared via a two-step process. PEO hydrogels were prepared by ${\gamma}-ray $ irradiation (radiation dose: 50 kGy, dose rate: 7.66 kGy/h), grafted by either MAA or AAc monomers onto the PEO hydrogels and finally underwent irradiation (radiation dose: 520 kGy, dose rate: 2.15 kGy/h). These grafted hydrogels showed a pH-sensitive swelling behavior. The grafted hydrogels were used as a carrier for the drug delivery systems for the controlled release of insulin. Drug-loaded hydrogels were placed in simulated gastric fluid (SGF, pH 1.2) for 2 hr and then in simulated intestinal fluid (SIF, pH 6.8). The in vitro drug release behaviors of these hydrogels were examined by quantification analysis with a UV-Vis spectrophotometer.

Sustained Release Injectable of Recombinant Bovine Somatotropin in Biodegradable Poly(D,L-lactide-co-glyceride) Microspheres (생분해성 폴리락티드/글리콜리드 미립구를 이용한 재조합 소 성장호르몬(rBST)의 지속성주사제 설계)

  • Jeon, Hong-Ryeol;Lee, Bong-Sang;Kown, Do-W;Yoon, Mi-Kyoung;Jeon, Hyun-Joo;Shin, Taek-Hwan;Choi, Young-Wook
    • Journal of Pharmaceutical Investigation
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    • v.32 no.3
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    • pp.199-207
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    • 2002
  • In order to develop a sustained release formulation of bovine somatotropin (BST), which has been used to increase the body weight of oxen or the milk production of dairy cows, poly(D,L-lactide-co-glyceride)(PLGA) microspheres were made by W/O/W multiple emulsification method and solvent extraction method. Physical properties including particle size, drug entrapment, drug release, protein denaturation, and in vivo body weight increase in rats were characterized. The size of the microspheres was increased as the molecular weight of PLGA increased. When Span 65 and stearic acid during preparation were added, the size was decreased but the amount of surface protein was increased, resulting in a high loading efficiency, with fast release of BST from the microspheres. Aggregation or fragmentation of BST by SDS-PAGE during microsphere preparation and drug release study was not observed. Body weight of Sprague-Dawley's male rats was significantly increased after subcutaneous administrations of BST-loaded PLGA microspheres. There was a good correlation between in vivo weight gain and in vitro release rate of microspheres. PLGA microspheres with a high surface protein ratio could be a good candidate for the sustained delivery of BST.

Release Characteristics to Vitamin $B_{2}$ of Chitosan Ointments In vitro (In vitro에서 키토산 연고의 비타민 $B_{2}$ 방출 특성)

  • Oh, Se-Young;Hwang, Sung-Kwy;Hwang, Yong-Hyun
    • Journal of the Korean Applied Science and Technology
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    • v.17 no.1
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    • pp.43-48
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    • 2000
  • Drug delivery system(DDS) applied to various fields, such as medicine, cosmetics, agriculture and necessities of life. Among these application fields, DDS is often used as the method of drug dosage into the epidermic skin. We investigated characters of transdermal therapeutic system(TTS) and the skin permeability of that with applying DDS. Chitosan was selected as material of TTS. We investigated the permeation of chitosan ointment containing drug in rat skin using horizontal membrane cell model. Permeation properties of materials were investigated for water-soluble drug such as riboflavin in vitro. We used glycerin, PEG 600 and oleic acid as enhancers. Since dermis has more content water(hydration) than the stratum corneum, skin permeation rate at steady state was highly influenced when glycerin was used in water-soluble drug. The permeation rate of content enhancer and drug was found to be faster than that of content water-soluble drug only. These results showed that skin permeation rate of drug across the composite was manly dependent on the property of ointment base and drug. Proper selection of the polymeric materials which resemble and enhance properties of the delivering drug was found to be important in controlling the skin permeation rate.

Synthesis of Lactide/Hyaluronic Acid Polymer Membrane for the Application of Drug Delivery System (약물방출시스템 적용을 위한 락타이드/히아루론산 고분자 막의 제조)

  • Kim, Min-Su;Kwon, Ji-Young;Cheong, Seong-Ihl
    • Membrane Journal
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    • v.15 no.4
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    • pp.281-288
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    • 2005
  • The hyaluronic acid (HA) with excellent biocompatibility can be combined with lactide, the ester dimer of polylactide, with good biodegradability to produce biocompatible materials applicable to drug delivery system. By freeze drying method, HA and lactide were crosslinked with crosslinking agent, 1-ethyl-3-(3-dimethyl aminopropyl) carbodiimide. Degree of lactide and EDC reaction was determined by the analysis of nuclear magnetic resonance (NMR) spectroscopy. The degree of lactide and EDC reaction increased and swelling ratio decreased as the mole ratio of lactide to HA or crosslinking agent concentration increased or reaction temperature decreased. The drug release experiment result from membranes having different degree of lactide reaction showed that drug release rate reduced in proportion to the degree of lactide reaction. The drug release experiment result from drugs having different hyrodphobicity showed that the more hydrophobic drug was released more slowly.

Preparation of Biodegradable PHBV Devices Containing Gentamicin Sulfate (PHBV를 이용한 황산겐타마이신 서방성 제형의 제조와 방출거동)

  • 최학수;김상욱;윤덕일;강길선;이종문;김용식;이해방
    • Polymer(Korea)
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    • v.25 no.3
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    • pp.334-342
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    • 2001
  • Gentamicin sulfate (GS)-loaded poly(3-hydroxybutyrate-co-3-hydroxyvalerate)(PHBV) devices were prepared for controlled-release of antibiotics. In this study, the effects of thickness, hydroxyvalerate (HV) content, initial drug-loading ratio, and additive content on the release profile have been investigated. The morphology of devices was examined with scanning electron microscope (SEM) before and after in vitro release; their highly porous surface and cross-sectional were observed. It could be suggested that device would be affected by the packing of the HV and additive content, which would depend on their structure. A high performance liquid chromatography (HPLC) was used to detect and quantify the release of GS from the device. The drug release from all the devices showed biphasic release patterns, and some matrices released the incorporated antibiotic throughout 30 days with a near zero-order release rate. The release patterns were shown to be changed by altering the thickness, copolymer ratio, and additive content.

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Injectable Sustained Release Gel as a Local Drug Delivery for Periodontal Diseases (치주질환치료를 위한 국소적용 서방출성 리오겔)

  • Kim, Ki-jun;Shin, Young-hee
    • YAKHAK HOEJI
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    • v.60 no.1
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    • pp.46-50
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    • 2016
  • The purpose of this study was the development of sustained-release lyogel of chlorhexidine in the treatment of periodontal diseases. A sustained-release chlorhexidine lyogel (CHX-G) was formulated, based on Eudragit$^{(R)}$ (1~3%), polyvinyl pyrrolidone (PVP) (0~10%), triacetin (20~40%), hydroxy ethyl cellulose (HEC) (1%) and glycerin. In vitro studies were performed to determine the release rate of chlorhexidine from CHX-Gs using dialysis tube. Our results suggest that the release rate of chlorhexidine from lyogel could be controlled by changing the lyogel compositions.

Formulation and Preparation of Sustained Release Pellet for Alfuzosin HCI Using Fluid-bed coater (유동층 코팅기를 이용한 염산알푸조신의 서방형 과립 설계 및 제조)

  • Na, Jin-Sang;Yoon, Yang-No;Seo, Hui;Jeong, Sang-Young;Park, Eun-Seok;Hwan, Sung-Joo;Shin, Byung-Cheol;Kim, Sung-Hoon;Cho, Sun-Hang
    • Journal of Pharmaceutical Investigation
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    • v.38 no.6
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    • pp.387-392
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    • 2008
  • Alfuzosin, an Alphal-adrenoceptor antagonist is used for the treatment of patients with voiding and in a lesser extent storage lower urinary tract symptoms (LUTS) associated to benign prostatic hyperplasia (BPH). The objective of this study was to formulate sustained release alfuzosin HCl granules and assess their formulation variables. The $Eudragit^{(R)}$ as a polymer, sustained release membrane, and dibutyl sebacate (DBS) as a plasticizer were used. Multi-coated alfuzosin HCl delivery systems composed of sugar sphere, various excipients, $Eudragit^{(R)}$ and HPMC (hydroxy propyl methyl cellulose), Cellulose Acetate were prepared by fluid-bed coater. Membrane layer were used $Eudragit^{(R)}$ RS PO and NE 30D. And the alfuzosin HCl coated beads were coated immediate release drug layer for initial burst. Its dissolution test was carried out compared to conventional products ($XATRAL^{(R)}$ XL). The release rate of drug from coated beads was higher than that from $XATRAL^{(R)}$ XL in pH 6.8.