• Title/Summary/Keyword: Drug loading

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Preparation and Characterization of Pioglitazone Loaded PLGA Nanospheres for the Treatment of Type 2 Diabetes (제2형 당뇨병 치료제인 Pioglitazone을 봉입하기 위한 PLGA 나노입자 제조 및 분석)

  • Woo, Hyun-Ju;Kim, Jin-Soo;Kim, Jun-Gi;Nurunnabi, Md.;Huh, Kang-Moo;Cho, Kwang-Jae;Lee, Yong-Kyu
    • Polymer(Korea)
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    • v.34 no.6
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    • pp.527-533
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    • 2010
  • The pioglitazone loaded poly(lactide-co-glycolide)(PLGA) nanospheres were prepared by emulsion-evaporation method and optimized for particle size and entrapment efficiency. The optimized particles were 125~170 nm in size with narrow size distribution and showed above 85% entrapment efficiency at 30% of pioglitazone loading when prepared with 3% w/v of poly(vinyl alcohol) (PVA) as a surfactant. These particulate carriers exhibited a controlled in vitro release of pioglitazone for 40 days at a nearly constant rate. The pioglitazone loaded PLGA nanospheres were not only effective to reduce the blood sugar level of diabetic rats but also non-toxic for the animal body, in particular for sensitive organs like kidney, liver, heart, lung and spleen. These results indicate that PLGA nanospheres have a great potential for oral delivery of pioglitazone.

Patient Controlled Analgesia for Pain Management after Upper Abdominal Surgery (Baxter $Infusor^{(R)}$를 이용한 상복부 술후 통증 자가 조절)

  • Lee, Jung-Koo;Kim, Jin-Mo;Chung, Jung-Kil;Cheun, Jae-Kyu
    • The Korean Journal of Pain
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    • v.5 no.2
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    • pp.229-233
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    • 1992
  • Recently a non-electronic, disposable and portable infusor, Baxter $Infusor^{(R)}$, has developed for delivering not only a continuous drug infusion but also extradoses of medication on a demand basis. The present study examined the impact of two methods of pain management on recovery in 20 patients undergoing upper abdominal surgery for stomach cancer. One group, 10 patients, received IV meperidine in the recovery room and IM meperidine on the ward on a PRN basis(PRN group). In the other group, 10 patients, a loading dose of nalbuphine 0.1mg/kg was given when the patient first complained of pain in the recovery room and patient controlled analgesia with IV nalbuphine, 0.5mg/kg day for continuous infusion, was initiated and continued for 72 hours(PCA group). The devices for PCA group was Baxter Infusor with patient control module which had flow rate 0.5ml/hr and lockout time was 15 min. As results of this study, the patients of PCA group get less pain than PRN group on operation day, the first and second days after surgery. VAPS values are $6.47{\pm}1.64$ vs $4.44{\pm}1.38$, $5.02{\pm}1.22$ vs $2.62{\pm}0.93$ and $3.22{\pm}1.47$ vs $2.02{\pm}0.71$ respectively pertaining to PRN and PCA groups(p<0.05). In conclusion, PCA group with IV nalbuphine provided more effective postoperative analgesia than PRN group with conventional meperidine IM.

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Intravenous levetiracetam versus phenobarbital in children with status epilepticus or acute repetitive seizures

  • Lee, Yun-Jeong;Yum, Mi-Sun;Kim, Eun-Hee;Ko, Tae-Sung
    • Clinical and Experimental Pediatrics
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    • v.59 no.1
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    • pp.35-39
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    • 2016
  • Purpose: This study compared the efficacy and tolerability of intravenous (i.v.) phenobarbital (PHB) and i.v. levetiracetam (LEV) in children with status epilepticus (SE) or acute repetitive seizure (ARS). Methods: The medical records of children (age range, 1 month to 15 years) treated with i.v. PHB or LEV for SE or ARS at our single tertiary center were retrospectively reviewed. Seizure termination was defined as seizure cessation within 30 minutes of infusion completion and no recurrence within 24 hours. Information on the demographic variables, electroencephalography and magnetic resonance imaging findings, previous antiepileptic medications, and adverse events after drug infusion was obtained. Results: The records of 88 patients with SE or ARS (median age, 18 months; 50 treated with PHB and 38 with LEV) were reviewed. The median initial dose of i.v. PHB was 20 mg/kg (range, 10-20 mg/kg) and that of i.v. LEV was 30 mg/kg (range, 20-30 mg/kg). Seizure termination occurred in 57.9% of patients treated with i.v. LEV (22 of 38) and 74.0% treated with i.v. PHB (37 of 50) (P=0.111). The factor associated with seizure termination was the type of event (SE vs. ARS) in each group. Adverse effects were reported in 13.2% of patients treated with i.v. LEV (5 of 38; n=4, aggressive behavior and n=1, vomiting), and 28.0% of patients treated with i.v. PHB (14 of 50). Conclusion: Intravenous LEV was efficacious and safe in children with ARS or SE. Further evaluation is needed to determine the most effective and best-tolerated loading dose of i.v. LEV.

Fabrication of Compound K-loaded Polymeric Micelle System and its Characterization in vitro and Oral Absorption Enhancement in vivo

  • Hong, Sun-Mi;Jeon, Sang-Ok;Seo, Jo-Eun;Chun, Kyeung-Hwa;Oh, Dong-Ho;Choi, Young Wook;Lee, Do Ik;Jeong, Seong Hoon;Kang, Jae Seon;Lee, Sangkil
    • Bulletin of the Korean Chemical Society
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    • v.35 no.11
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    • pp.3188-3194
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    • 2014
  • Compound K (CK) was formulated as polymeric micelles (PM) using Pluronic$^{(R)}$ F-127 to enhance the oral absorption of CK, an intestinal bacterial metabolite of ginseng protopanaxadiol saponin. The physicochemical properties of Ck-loaded PM were characterized and an in vitro transport study using the Caco-2 cell system as well as an in vivo pharmacokinetic study using SD rats was carried out. The hydrodynamic mean particle size of CK-loaded PM (CK-PM) was $254{\pm}23.45nm$ after rehydration and the drug loading efficiency was ca. 99.9%. The FT-IR spectroscopy, X-ray diffraction, differential scanning calorimetry and scanning electron microscopy data supported the presence of a new solid phase in the PM. The $P_{app}$ value of in vitro Caco-2 cell permeation of CK-PM and the oral absorption of CK was enhanced about 1.2-fold and 2.6-fold compared to CK suspension, respectively, showing that the present PM formulation enabled an enhancement of oral CK absorption.

A Case of Interstitial Pneumonitis in a Patient with Rheumatoid Arthritis Treated with Leflunomide (Leflunomide로 치료중인 류마티스 관절염 환자에서 발생한 간질성 폐렴 1예)

  • Shin, Ah-Young;Kim, Seung Soo;Kim, Kyung Hee;Ju, Il-Nam;Ko, Hyeok Jae
    • Tuberculosis and Respiratory Diseases
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    • v.66 no.6
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    • pp.477-481
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    • 2009
  • Leflunomide, a disease-modifying antirheumatic drug (DMARD) for the treatment of rheumatoid arthritis has been available in Korea since 2003. Leflunomide-associated interstitial pneumonitis has been appearing recently. A 25-year-old woman with a 12-month history of seronegative rheumatoid arthritis (RA) presented with acute respiratory insufficiency. She developed fever, dyspnea, and non-productive cough. Her medication history included methotrexate (15 mg/week. commencing 1 year prior) and leflunomide (20 mg/day, no loading dose, commencing 4 months prior). She was diagnosed with leflunomide-associated interstitial pneumonitis based on history, physical examination, laboratory and radiologic findings. She recovered quickly after leflunomide was withdrawn and steroids and cholestyramine were initiated quickly. We report a case of leflunomide-associated interstitial pneumonitis treated successfully with intravenous high-dose steroid and cholestyramine.

Experience and pharmacokinetics of Levetiracetam in Korean neonates with neonatal seizures

  • Shin, Jae Won;Jung, Yun Seob;Park, Kyungsoo;Lee, Soon Min;Eun, Ho Seon;Park, Min Soo;Park, Kook In;Namgung, Ran
    • Clinical and Experimental Pediatrics
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    • v.60 no.2
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    • pp.50-54
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    • 2017
  • Purpose: The aims of this study were to evaluate the safety and pharmacokinetics of levetiracetam (LEV) in neonates with seizures and to establish a population pharmacokinetics (PPK) model by using the software NONMEM. Methods: A retrospective analysis of 18 neonatal patients with seizures, who were treated with LEV, including 151 serum samples, was performed. The mean loading dose was 20 mg/kg, followed by a mean maintenance dose of 29 mg/kg/day. Results: Seventeen neonates (94%) had seizure cessation within 1 week and 16 (84%) remained seizure-free at 30 days under the LEV therapy. The mean serum concentration of LEV was $8.7{\mu}g/mL$. Eight samples (5%) were found above the therapeutic range. No serious adverse effects were detected. In the PPK analysis for Korean neonates, the half-life was 9.6 hours; clearance, 0.357 L/hr; and volume of distribution, 4.947 L, showing differences from those in adults. Conclusion: LEV is a safe and effective option for the treatment of neonatal seizures with careful therapeutic drug monitoring.

Sustainability Evaluation for Shellfish Production in Gamak Bay Based on the Systems Ecology 1. EMERGY Evaluation for Shellfish Production in Gamak Bay (시스템 생태학적 접근법에 의한 가막만 패류생산의 지속성 평가 1. 가막만 패류양식의 에머지 평가)

  • Oh, Hyun-Taik;Lee, Suk-Mo;Lee, Won-Chan;Jung, Rae-Hong;Hong, Suk-Jin;Kim, Nam-Kook;Tilburg, Charles
    • Journal of Environmental Science International
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    • v.17 no.8
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    • pp.841-856
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    • 2008
  • This research outlines a new method for evaluation of shellfish production in Gamak Bay based on the concept of EMERGY. Better understanding of those environmental factors influencing oyster production and the management of oyster stocks requires the ability to assess the real value of environmental sources such as solar energy, river, tide, wave, wind, and other physical mechanisms. In this research, EMERGY flows from environment sources were 76% for shellfish aquaculture in Gamak Bay. EMERGY yield ratio, Environmental Loading Ratio, and Sustainability Index were 4.26, 0.31 and 13.89, respectively. Using the Emergy evaluation data, the predicted maximum shellfish aquaculture production in Gamak Bay and the FDA (Food and Drug Administration, U.S.) designated area in Gamak Bay were 10,845 ton/y and 7,548 ton/yr, respectively. Since the predicted shellfish production was approximately 1.3 times more than produced shellfish production in 2005, the carrying capacity of Gamak Bay is estimated to be 1.3 times more than the present oyster production.

Biological Effects Of Flurbiprofen Loaded Chitosan To Gingival Fibroblast (Flurbiprofen 함유 키토산 제제가 치은 섬유아세포에 미치는 영향)

  • Chung, Chong-Pyoung;Park, Yoon-Jeong;Lee, Seung-Jin;Rhyu, In-Cheol;Choi, Sang-Mook
    • Journal of Periodontal and Implant Science
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    • v.26 no.1
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    • pp.317-333
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    • 1996
  • The main goal of periodontal regeneration is to be achieved by epithelial exclusion, periodontal ligament cell activation or alveolar bone regeneration. The purpose of this study was to investigate on the physico- chemical and biological characteristics of biodegradable chitosan beads. Chitosan beads were fabricated by ionic gelation with sodium tripolyphosphate and they had the size in 300um diameter. As therapeutic agent, flurbiprofen was incorporated into the beads by 10, 20% loading contents. The release of drugs from the chitosan beads was measured in vitro. Also, biological activity tests of flurbiprofen loaded chitosan beads including cytotoxicity test, ihhibition of $IL-1{\beta}$ production, suppression to $PGE_2$ production, collagenase inhibition test, the ability of total protein synthesis, and tissue response were evaluated. The amount of flurbiprofen released from chitosan was 33-50% during 7 days. Minimal cytotoxicity was observed in chitosan beads. Flurbiprofen released from chitosan beads significantly suppressed the $IL-1{\beta}$ production of monocyte, $PGE_2$ production and markedly inhibited collagenase activity. Meanwhile, flurbiprofen released from this system showed increased ability for protein synthesis. Throughout 4 -week implantation period, no significant inflammatory cell infiltrated around chitosan bead and also fibroblast like cell types at the beads - tissue interface were revealed with gradual degradation of implanted chitosan beads. From these results, it was suggested that flurbiprofen loaded chitosan beads can be effectively useful for biocompatible local delivery system in periodontal regeneration.

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Remifentanil-Propofol Sedation as an Ambulatory Anesthesia for Carpal Tunnel Release

  • Lee, Jae-Jun;Hwang, Sung-Mi;Jang, Ji-Su;Lim, So-Young;Heo, Dong-Hwa;Cho, Yong-Jun
    • Journal of Korean Neurosurgical Society
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    • v.48 no.5
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    • pp.429-433
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    • 2010
  • Objective : This prospective study evaluated the use of continuous sedation using propofol and remifentanil when carpal tunnel release (CTR) was performed under local anesthesia. Methods : We sedated 60 patients undergoing CTR using local anesthesia with remifentanil at loading and continuous doses of $0.5\;{\mu}g\;kg^{-1}$ and $0.05\;{\mu}g\;kg^{-1}min^{-1}$, respectively, and propofol, using a target controlled infusion (TCI) pump set to a target of $2\;{\mu}g\;mL^{-1}$ (group A), or with the same drug doses except that the continuous remifentanil dose was $0.07\;{\mu}g\;kg^{-1}min^{-1}$ (group B) or $0.1\;{\mu}g\;kg^{-1}min^{-1}$ (group C). Results : In group B, the levels of pain when local anesthetics were administered (p = 0.001), intraoperative pain (p < 0.001) and anxiety (p = 0.001) were significantly lower than those of group A. Furthermore, the incidence of adverse events, including desaturation (p < 0.001) and vomiting (p = 0.043), was significantly lower in group B than in group C. Conclusion : Continuous sedation using an appropriate dose of remifentanil and propofol can be used as safe, efficacious ambulatory anesthesia in cases of CTR under local anesthesia, performed using only 2 mL of local anesthetic, with a high degree of patient satisfaction.

Preparation of Biodegradable PLGA Microspheres for Sustained Local Anesthesia and Their in vitro Release Behavior (지속적인 국소마취를 위한 생분해성 PLGA 미립구의 제조와 생체외 방출 거동)

  • 조진철;강길선;최학수;이종문;이해방
    • Polymer(Korea)
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    • v.24 no.5
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    • pp.728-735
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    • 2000
  • Fentanyl-loaded biodegradable poly(L-lactide-co-glycolide) (75 : 25 by mole ratio of lactide to glycolide, PLGA) microspheres (MSs) were prepared to study the possibility for long-acting local anesthesia. We developed the fentanyl base (FB, slightly water-soluble)-loaded PLGA MSs by means of conventional O/W solvent evaporation method. The size of MSs was in the range of 10~150 ${\mu}{\textrm}{m}$. The morphology of MSs was characterized by SEM, and the in vitro release amounts of FB were analyzed by HPLC. The lowest porous cross-sectional morphology and the highest encapsulation efficiency were obtained by using gelatin as an emulsifier. The influences of several preparation parameters, such as emulsifier types, molecular weights and concentrations of PLGA, and initial drug loading amount, etc., have been observed in the release patterns of FB. The release of FB in vitro was more prolonged over 25 days, with close to zero-order pattern by controlling the preparation parameters. We also investigated the physicochemical properties of FB-loaded PLGA MSs by X-ray diffraction and differential scanning calorimeter.

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