• Title/Summary/Keyword: slow-release preparation

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The Formulation and Bioavailability of Oral Sustained Release Sulindac Delivery System (설린닥의 경구용 지속성 제제설계 및 생체이용율)

  • Rhee, Gye-Ju;Park, Sun-Hee;Whang, Sung-Joo
    • YAKHAK HOEJI
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    • v.41 no.1
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    • pp.60-73
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    • 1997
  • In order to design a 24 hr sustained release preparation of sulindac for oral administration, fast release pellet (FR), slow release pellet (SR) and two combined formulation (1 : 1 and 1 : 2) were prepared. The pharmacokinetic effect of such preparations has been evaluated using rabbits as a suitable in vivo model, and tested in man. Dose determination was carried out using curve fitting according to RSTPJP II program. In bioavailability test using rabbit, AUCs of sulindac in a few designed formulations were similar to each other. $C_{max}$- of RF and SR were 1.8 times and 1.2 times higher, respectively, compared to that of combined formulation (FR:SR=1:1). While plasma concentration of FR and SR decreased rapidly, that of combined formulation (FR:SR 1:1) lasted at the level close to $C_{max}$ for 24 hrs. Plasma concentration of sulfide form from the combined pellet(FR:SR=1:1) lasted for 24 hrs, and its AUC value was 1.4-fold, 2.7-fold. and 1.2-fold greater than FR pellet, SR pellet and combined pellet (FR:SR 1 : 2). Thus, the combined pellet of 1:1 ratio was found to be the most effective for oral sustained release formulation. Bioavailability test in human showed that AUC of sulfide from TSRP (1 : 1) was approximately 1.5 times greater than total AUC of Immbaron$^{\circledR}$ administered twice in a day. While $T_{max}$ of sulfide from lmmbaron$^{\circledR}$ was 4.33 +/- 1.37 hr (lst administration) and 3.33 ${pm}$ 0.82 hr (2nd administration), respectively, that of sulfide from TSRP increased to 7.17 ${pm}$ 2.86 hr. Plasma concentration of sulfide from TSRP was sustained at more, than 1.0 ${\mu}g{\cdot}$hr/ml until 24 hrs after one dose administration. In addition, TSRP may decrease local adverse reaction in the stomach, since plasma concentration of sulfide from the combined pellet was low within 2hrs in the stomach. In conclusion, it is suggested that TSRP formulation may be effective for oral 24 hr sustained release formulation of sulindac dosing 300 ~ 350mg once a day.

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Respiratory Depression during Oral MS-Contin Administration for Pain Management of Gall Bladder Cancer (말기 담낭암 환자의 통증조절을 위해 MS Contin 투여중 발생한 호흡억제 -증례 보고-)

  • Lee, Chul-Woo;Lee, Byung-Ho;Lee, Yong-Hee
    • The Korean Journal of Pain
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    • v.9 no.1
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    • pp.239-243
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    • 1996
  • MS-Contin is an oral controlled-release preparation of morphine sulfate that has been used widely in the management of advanced cancer pain. It prolongs plasma concentration of morphine with no observable accumulation properties following repeated dosing, thereby promoting uninterrupted sleep and hopefully improving patient's quality of life. The common side effects of MS Contin are nausea, vomiting, drowsiness and constipation. But these symptoms are usually mild and respiratory depression is a rare problem. We experienced respiratory depression during oral administration of MS contin for the pain management of advanced gall bladder cancer of 76 years old male patient with metastasis at liver, intestine and cervical lymph node. After we increased the dosage of MS Contin from 160mg to 220mg per day, due to abdominal pain, we observed morphine reaction of MS Contin overdose such as pinpoint pupil, deeply slow respiration below 8/minute, and drowsiness. After intravenous bolus injection of 0.4 mg naloxone followed by continuous administration of 0.2 mg/hr for 4 hours, the patient regained consciousness. The administered route of morphine was changed to intravenous PCA (patient controlled analgesia). There was no aspiration sign as confirmed by chest x-ray. The patient was comfortable and delayed no signs of respiratory depression until now.

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Liposome-Microencapsulation of Lysozyme and Its Stimulated Release (Lysozyme의 Liposome 미세캡슬화와 유출 촉진)

  • Kim, Tae-Jong;Kim, Young-Sook;Pyun, Yu-Ryang
    • Korean Journal of Food Science and Technology
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    • v.28 no.3
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    • pp.399-404
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    • 1996
  • Encapsulation of lysozyme using lecithin vesicles and its stimilated release properties were studied. Lecithin vesicles were prepared by the dehydration-rehydration (DR)method. The highest encapsulation efficiency (EE) value of 80.1% was obtained by sonicating the multilamellar vesicles (MLVs) at 100 KHz for 120 min in bath sonicator. The value of entrapment progressively increased with the concentration of lysozyme, while the EE value decreased with the increase of enzyme concentration up to 50mg per 100mg per 100mg of lecithin, and then became nearly constant. At the pH of 5.9, only a small amount of lysozyme was released from DR vesicles during incubation at $37^{\circ}C$ As the pH decreased to 3.0, lysozyme was released more rapidly. Lysozyme release was accelerated for 24h and reached a plateau after 72h incubation with 1% Tween 80, $Ca^{2+}$ gave a pulse-like-release in the first hour, which was followed by a slow release.

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Quality Changes of Strawberry by Slow-released ClO2 Gas Gel-pack during Storage (서방형 이산화염소 가스 젤팩을 이용한 딸기의 저장 중 품질 변화)

  • Lee, Kyung-Haeng;Bong, So-Jung;Yoon, Ye-Ji;Lee, Bom;Kwak, Il-Hwan;Min, Kyung-Hoon;Kim, Hong-Gil
    • The Korean Journal of Food And Nutrition
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    • v.30 no.3
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    • pp.591-598
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    • 2017
  • To prolong the shelf-life of strawberry, samples were treated with gel packs containing slow-released chlorine dioxide($ClO_2$) gas at 3~7 ppm for 6 days at room temperature. The weight loss and decay ratio as well as changes in pH, color and texture properties of the treated samples were investigated. The weight of the control and $ClO_2$ gas treated samples decreased slightly, but the weight of the control changed faster than those of the $ClO_2$ gas treated samples during the storage period. The decay ratio of control was higher than those of the $ClO_2$ gas treatments since 4 days of storage. The pH and acidity in the control and in the $ClO_2$ gas treated samples were no differences during storage period. The lightness of strawberry decreased during storage, but there was no difference in lightness among the treatments even when storage time was extended. The redness and yellowness of the control showed higher change than those of the $ClO_2$ gas treatments during 6 days. The firmness of the control changed more rapidly than those of the $ClO_2$ gas treatments during 6 days. Especially, the samples treated 3 and 5 ppm $ClO_2$ gas were the least changed. And the scores for appearance, firmness and overall acceptance control and 7 ppm $ClO_2$ gas treatment decreased more rapidly than those of 3 and 5 ppm treatment.

Quality Changes of Chicken Breast Meat by Slow-Released ClO2 Gas Gel-Pack during Storage (서방형 이산화염소 가스 젤팩을 이용한 닭가슴육 저장 중 품질 변화)

  • Lee, Kyung-Haeng;Yoon, Ye-Ji;Kwon, Hye-Won;Lee, Bom;Kim, Hong-Gil
    • The Korean Journal of Food And Nutrition
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    • v.31 no.1
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    • pp.127-134
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    • 2018
  • To prolong the shelf-life of chicken breast meat, samples were treated with gel packs containing slow-released chlorine dioxide ($ClO_2$) gas at 7~15 ppm for eight days at $4^{\circ}C$. The microbial, physicochemical properties and sensory evaluation of the treated samples were investigated. The total number of bacteria in the control increased during storage and showed 6.78 log CFU/g on the 8th day of storage, but $ClO_2$ gas treatments showed 6.24~6.58 log CFU/g at the same time. The initial pH of chicken breast meat was 6.00 and gradually increased during storage. And $ClO_2$ gas treatments did not show any significant difference from the control during storage period, but maintained a generally lower pH than that of the control. The lightness, redness, and yellowness during storage were not significantly different between the control and the 7~10 ppm $ClO_2$ gas treatments. However, as the storage period was increased, the redness of 15 ppm $ClO_2$ gas treatment was reduced. The cooking loss and shear force were not different between the control and $ClO_2$ gas treatments during the storage period. Volatile basic nitrogen (VBN) increased in the control from the 6th day of storage and 23.80 mg% in the 8th day of storage. However, VBN of $ClO_2$ treatments showed lower than that of the control. In the change of sensory evaluation during storage, 10 ppm $ClO_2$ treatment showed the highest preference in odor, appearance and overall acceptance during storage period.

Preparation and Characterization of Deoxycholic Acid-Conjugated Low Molecular Weight Water-Soluble Chitosan Nanoparticles for Hydrophobic Antifungal Agent Carrier (소수성 항진균제 전달체로 응용하기 위한 데옥시콜릭산이 결합된 저분자량 수용성 키토산 나노입자의 제조와 특성)

  • Choi, Chang-Yong;Jung, Hyun;Nam, Joung-Pyo;Park, Yoon-Kyung;Jang, Mi-Kyeong;Nah, Jae-Woon
    • Polymer(Korea)
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    • v.33 no.4
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    • pp.389-395
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    • 2009
  • To develop the carrier of hydrophobic antifungal agents based on low molecular weight water-soluble chitosan (LMWSC), LMWSC was chemically modified with deoxycholic acid (DA) which is one of the bile acid as a hydrophobic group. The nanoparticles (WSCDA) using DA conjugated LMWSC were characterized using dynamic light scattering (DLS) and transmittance electron microscope (TEM). The particle size of WSCDA ranged from 250 to 350 nm and increased with the number of DA substitution. The loaded itraconazole as an antifungal agent WSCDA nanoparticles (WSCDA-ITCN) were prepared by solvent evaporation method. The drug content and the loading efficiency were investigated approximately $9{\sim}10%$ and $61{\sim}68%$ by UV spectrophotometer, respectively. The release of drug from nanoparticles was slow and showed sustained release characteristics. Based on the results of release study that the higher DA contents in WSCDA, the slower the releasing rate, the WSCDA-ITCN could be used as an excellent antifungal agent.

Effect of Cosurfactants on the Release Behavior of Zaltoprofen-loaded PLGA Microspheres in In Vitro : Preparation and Characterization (보조계면활성제 첨가에 따른 잘토프로펜을 함유한 PLGA 미립구의 생체외 방출 거동: 제조 및 특성)

  • Eom, Shin;Yoo, Seok-Cheol;Kim, Yong-Ki;Lee, Young-Hyun;Lee, Eun-Yong;Yu, Hyeon;Lee, Dong-Won;Khang, Gil-Son
    • Polymer(Korea)
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    • v.34 no.4
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    • pp.333-340
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    • 2010
  • Zaltoprofen, a propionic acid derivative non-steroidal anti-inflammatory drug (NSAID), is known to have powerful inhibitory effects on acute, subacute and chronic inflammation. We developed poly(lactide-co-glycolide)(PLGA) microspheres loaded with zaltoprofen for sustained controlled delivery using an oil-water solvent evaporation methods by varying PLGA molecular weight and cosurfactant contents. Physicochemical properties and morphology of zaltoprofen-loaded PLGA microspheres were investigated by scanning electron microscope, X-ray diffraction and differential scanning calorimeter. The size of microspheres increased with the molecular weight of PLGA and the content of cosurfactants. The increase of PLGA molecular weight and cosurfactant content decreased the porosity of microspheres, subsequently resulting in the slow drug release. The results demonstrated that the adjustment of PLGA molecular weight and the cosurfactant content allowed us to control the drug release profiles of drug-loaded microspheres.

Quality Changes of Lentinula edodes GNA01 Mushroom by Choline Dioxide Gas Treatment during Storage (서방형 이산화염소 가스를 이용한 이슬송이버섯의 저장 중 품질 변화)

  • Yoon, Young-Tae;Bong, So-Jung;Kang, Han-Sol;Yoon, Ye-Ji;Kim, Hong-Gil;Min, Kyung-Hun;Lee, Kyung-Haeng
    • The Korean Journal of Food And Nutrition
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    • v.29 no.4
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    • pp.499-505
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    • 2016
  • To improve the shelf-life of mushrooms, Lentinula edodes GNA01 mushrooms were treated with gel packs containing slow-released chlorine dioxide ($ClO_2$) gas at 5~10 ppm for 5 days at $20^{\circ}C$ and the weight loss rate as well as the changes in pH, color and texture properties of the treated samples were investigated. The weight of the control and $ClO_2$ gas treated samples were decreased slightly, and there were no differences during the storage period. However, the weight of the control changed faster than those of the $ClO_2$ gas treated samples during storage period. The pH in the control and in the $ClO_2$ gas treated samples were decreased during storage period, but the samples treated with 5 and 7 ppm $ClO_2$ gas were the least changed. On the other hand, the samples treated with 10 ppm $ClO_2$ gas showed no difference from the other treatments during 4 days, but the pH was lower than that of the control on the fifth day. The lightness of inside and outside in mushroom were decreased whereas redness and yellowness were increased during storage period. However, color changes in the $ClO_2$ gas treated samples were lower than those of the control. Especially, the samples treated with 5 and 7 ppm $ClO_2$ gas were the least changed. The texture of the mushroom were decreased consistently during storage period. The texture of the control changed faster than those of the $ClO_2$ gas treatments during 5 days. Especially, the samples treated 5 ppm $ClO_2$ gas were the least changed.

Preparation and Characterizatino of Nano-sized Liposome Containing Proteins Derived from Coptidis rhizoma (황련유래 단백질이 함유된 나노리포좀의 제조 및 특성)

  • Oh, Seng Ryong;Lee, Sang Bong;Cho, Kye Min;Choi, Moon Jae;Jin, Byung Suk;Han, Yong Moon;Lee, Young Moo;Shim, Jin Kie
    • Applied Chemistry for Engineering
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    • v.17 no.1
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    • pp.52-57
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    • 2006
  • Coptidis Rhizoma, an antimicrobial agent from natural source, is known to have the antiviral effect on the Candida albicans that causes the infectious dermatitis. The valuable protein was extracted from the Coptidis Rhizoma, To prevent denaturalization from external stimulus and improve adsorption onto the skin, the nano-sized liposomes were prepared as a carrier. The CPR-containing liposomes showed an average diameter of 187 nm, surface charge of 3.337 mV and 33% encapsulation efficiency. The release behavior of CRP from the liposome was investigated with various temperature and releasing time. The PVA solution was coated on the surface of liposome to improve the stability. The coated liposome showed slow release behavior in comparison with the non-coated liposome. The CRP in the liposome maintained the effect on the Candida albicans after treating it at 50 and with ultraviolet for 24 h.