• 제목/요약/키워드: Drug loading

검색결과 215건 처리시간 0.022초

Enhanced Local Anesthetic Efficacy of Bioadhesive Ropivacaine Gels

  • Cho, Cheong-Weon;Choi, Jun-Shik;Shin, Sang-Chul
    • Biomolecules & Therapeutics
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    • 제19권3호
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    • pp.357-363
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    • 2011
  • In relieving local pains, ropivacaine has been widely used. In case of their application such as ointments and creams, it is difficult to expect their effects for a significant period of time, because they are easily removed by wetting, movement and contacting. Therefore, the new formulations that have suitable bioadhesion were needed to enhance local anesthetic effects. The effect of drug concentration and temperature on drug release was studied from the prepared 1.5% Carboxymethyl cellulose (CMC) (150MC) gels using synthetic cellulose membrane at $37{\pm}0.5^{\circ}C$. As the drug concentration and temperature increased, the drug release increased. A linear relationship was observed between the logarithm of the permeability coefficient and the reciprocal temperature. The activation energy of drug permeation was 3.16 kcal/mol for a 1.5% loading dose. To increase the skin permeation of ropivacaine from CMC gel, enhancers such as saturated and unsaturated fatty acids, pyrrolidones, propylene glycol derivatives, glycerides, and non-ionic surfactants were incorporated into the ropivacaine-CMC gels. Among the enhancers used, polyoxyethylene 2-oleyl ether showed the highest enhancing effects. For the efficacy study, the anesthetic action of the formulated ropivacaine gel containing an enhancer and vasoconstrictor was evaluated with the tail-flick analgesimeter. According to the rat tail-flick test, 1.5% drug gels containing polyoxyethylene 2-oleyl ether and tetrahydrozoline showed the best prolonged local analgesic effects. In conclusion, the enhanced local anesthetic gels containing penetration enhancer and vasoconstrictor could be developed using the bioadhesive polymer.

BI기술을 적용한 약물부작용감시시스템 개발 (Development of Adverse Drug Event Surveillance System using BI Technology)

  • 이영호;강운구;박래웅
    • 한국콘텐츠학회논문지
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    • 제9권2호
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    • pp.106-114
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    • 2009
  • 본 연구에서는 국내 약물부작용감시시스템 연구의 활성화 및 상용화를 목표로 약물부작용 시스템 사례를 분석하고 비즈니스인텔리전스(BI) 기술을 적용하여 약물부작용감시시스템의 기술구조를 제시한다. 최근에는 전자적과정(electronic review)과 수동적 리뷰과정(manual review process)을 병행하는 방법으로 약물부작용을 탐지하는 추세이며, 본 연구에서는 BI 기술중 ETL(Extract, Transform, Loading)을 적용하여 CDW(Clinical DataWarehouse)구축하였다. 부작용 판별 결과 처방의사 701명, 대상 환자는 남자 1,528명, 여자 1,531명으로 기간 내 환자는 총 3059명 이었으며 이중에서 약물부작용으로 의심되는 사례는 전체 318,222건 중에서 약 0.6%에 해당하는 2,085건으로 확인되었다. 이를 신호별로 분류하면 단순유형의 T.Bilirubin> 3mg/dL(부작용 유형-LabR0005)가 전체 2085건에서 548건으로 가장 높았다.

Polystyrene-b-poly(oligo(ethylene oxide) Monomethyl Ether Methacrylate)-b-polystyrene Triblock Copolymers as Potential Carriers for Hydrophobic Drugs

  • You, Qianqian;Chang, Haibo;Guo, Qipeng;Zhang, Yudong;Zhang, Puyu
    • Bulletin of the Korean Chemical Society
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    • 제34권2호
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    • pp.558-564
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    • 2013
  • A simple and effective method is introduced to synthesize a series of polystyrene-b-poly(oligo(ethylene oxide) monomethyl ether methacrylate)-b-polystyrene (PSt-b-POEOMA-b-PSt) triblock copolymers. The structures of PSt-b-POEOMA-b-PSt copolymers were characterized by Fourier-transform infrared spectroscopy (FTIR) and nuclear magnetic resonance ($^1H$ NMR) spectroscopy. The molecular weight and molecular weight distribution of the copolymer were measured by gel permeation chromatography (GPC). Furthermore, the self-assembling and drug-loaded behaviours of three different ratios of PSt-b-POEOMA-b-PSt were studied. These copolymers could readily self-assemble into micelles in aqueous solution. The vitamin E-loaded copolymer micelles were produced by the dialysis method. The micelle size and core-shell structure of the block copolymer micelles and the drug-loaded micelles were confirmed by dynamic light scattering (DLS) and transmission electron microscopy (TEM). The thermal properties of the copolymer micelles before and after drug-loaded were investigated by different scanning calorimetry (DSC). The results show that the micelle size is slightly increased with increasing the content of hydrophobic segments and the micelles are still core-shell spherical structures after drug-loaded. Moreover, the glass transition temperature (Tg) of polystyrene is reduced after the drug loaded. The drug loading content (DLC) of the copolymer micelles is 70%-80% by ultraviolet (UV) photolithography analysis. These properties indicate the micelles self-assembled from PSt-b-POEOMA-b-PSt copolymers would have potential as carriers for the encapsulation of hydrophobic drugs.

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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    • 제23권4호
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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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Drug Release from Bioerodible Hydrogels Composed of $Poly-{\varepsilon}-Caprolactone/poly(Ethylene{\;}glycol)$ Macromer Semiinterpenhetrating Polymer Networks

  • Kim, Sung-Ho;Ha, Jeong-Hun;Jung, Yong-Jae;Cho, Chong-Su
    • Archives of Pharmacal Research
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    • 제18권1호
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    • pp.18-21
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    • 1995
  • Poly(ethylene glycol)(PEG) macrocers teminated with acrylate groups and semi-interpenetrating polymer networks (IPNs) composed of poly-.epsilon.-capolactone(PCL) and PEG macromer were syntheswized with the aim of obtaining a bioerodible hydrogel that could be used to release drugs for implantable delivery system. Polymerization of PEG macromer resulted in the formation of cross-linked gels due to the multifunctionality of macromer. Non-crosslinked PCL chains were interpenetrated into the cross-linked three-dimensions networks of PEG. The IPNs, largw drug loading lower concentration of PEG macromer in the IPNs concentration and the higher molecular weight of PEG macromer. Also, 5-FU was more fast released than hydrocortisone to the increased water solubility.

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Active components delivery rate from acrylic resin maxillary surgical obturator: Part I

  • Al-Kaabi, Arshad;Hamid, Mohammed A.
    • Advances in materials Research
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    • 제9권2호
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    • pp.109-114
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    • 2020
  • The purpose of this study was to observe the trend of compounds release from acrylic resin oral prosthesis when used for drug delivery as well as a restoration. In this study, 10 specimens of heat-cured polymethylmethacrylate material were prepared and loaded with methylene blue biological stain. The specimens were then submerged in vials with 5 ml distilled water for 24 hours. The extraction procedure continued for 4 days, each day the specimens were immersed in another 5 ml distilled water vial. All extracted solutions were analyzed by visible light spectroscopy for absorbance comparison. The statistical results showed that the absorbance values were significantly different in the first day of extraction than the following days. However, there was no statistical difference among the 2nd, 3rd and 4th days of extraction. Biological stain loading to acrylic resin at the mixing stage, and then after extraction in distilled water, showed a burst release during the first day followed by a constant release during the following few days.

Challenge of 2-dimensional Inorganic Nanoparticles in Nuclear Medicine

  • Sairan Eom;Jin-Ho Choy;Kyo Chul Lee;Yong Jin Lee
    • 대한방사성의약품학회지
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    • 제8권2호
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    • pp.119-128
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    • 2022
  • 2-Dimensional inorganic nanoparticles with high surface area and ion-exchangeable properties have been continuously growing based on nanotechnology in the field of nanomedicine. Among one of the 2-D nanoparticles, layered double hydroxide (LDH) has been intensively explored as drug delivery due to its low toxicity, enhanced cellular permeability, and high drug loading capacity. Moreover, controllable chemical composition makes possible varying isomorphic layered materials for therapy and imaging of diseases. In this review, specific structural characteristics of LDH were introduced, and its potential for application as a biocompatible therapeutic agent and diagnostic one was addressed in nuclear medicine, one of promising fields in nanomedicine.

뇌졸중 환자군의 Warfarin Nomogram 설정을 위한 실제 처방전 평가 (Evaluation of Prescription Data for Development of Warfarin Nomogram in Korean Patients with Cerebral Infarction)

  • 장주영;고경미;윤지연;한옥연;임성실
    • 약학회지
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    • 제53권2호
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    • pp.83-88
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    • 2009
  • Warfarin is the most widely used oral anticoagulant in the world but maintenance of proper therapeutic range and prevention of adverse drug events always need to be careful. Especially, in Korea, warfarin dosing for patients with cerebral infarction is currently based on the nomogram which is done by foreign clinical trials not for the Korean. Therefore we evaluate warfarin dose of patients in the neurology and eventually get the base data of warfarin nomogram for Korean with stroke. We performed this study retrospectively on reviewing the medical charts to evaluate the prescribed loading dose (LD) and maintenance dose (MD) of warfarin and each responding International Normalized Ratio (INR) with any bleeding adverse drug reaction including of patient's characteristics for total 75 patients with stroke in the department of neurology of Kangnam ST. Mary's Hospital from January 2005 to June 2008. All evaluated patients should not be treated with warfarin in the past at all and should be initiated warfarin therapy first.ly at this time. All evaluated patients were divided as two classes by wafarin LD which is; 1) HDG - a high loading dosing group prescribed over 5mg, and 2) LDG - a low loading dosing group prescribed 5mg or below. As a result, average LD was $9.34{\pm}0.22$ mg (p=0.000) in HDG and $4.25{\pm}0.39$ mg (p=0.000) in LDG. Average baseline INR was $0.91{\pm}0.05$ (p=0.161) in HDG and $1.26{\pm}0.14$ (p=0.002) in LDG. On the first and second week, daily MD was $4.21{\pm}0.14$ mg (p=0.000) and $2.96{\pm}0.19$ mg (p=0.696) in HDG and also in LDG, $2.95{\pm}0.29$ mg (p=0.000) and $3.14{\pm}0.36$ mg (p=0.696). Also average reacting daily INR was respectively $2.53{\pm}0.12$ (p=0.141) and $2.51{\pm}0.16$ (p=0.678) in HDG, and in LDG, $2.11{\pm}0.17$ (p=0.141) and $2.42{\pm}0.14$ (p=0.678). After the second week, INR was not measured in regularly. Also most of underlying diseases were hypertension (n=38), diabetes mellitus (n=14), dyslipidemia (n=8) in order. Four ADRs with simple hemorrhage were occurred and those were due to drug interaction by comedication. In the conclusion, proper starting LD for Korean with stroke is 10 mg if baseline INR is around 1.0 or 5 mg if over 1.3. Proper MD need to be more evaluated in the future for setting up warfarin nomogram to make prospective study.

척추경나사못을 이용한 유합술과 동반 시술된 극돌기간 삽입기구의 생체역학적 연구 (Biomechanical Analysis of a Combined Interspinous Spacer with a Posterior Lumbar Fusion with Pedicle Screws)

  • 김영현;박은영;이성재
    • 대한의용생체공학회:의공학회지
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    • 제36권6호
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    • pp.276-282
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    • 2015
  • Recently, during the multi-level fusion with pedicle screws, interspinous spacer are sometimes substituted for the most superior level of the fusion in an attempt to reduce the number of fusion level and likelihood of degeneration process at the adjacent level. In this study, a finite element (FE) study was performed to assess biomechanical efficacies of the interspinous spacer combined with posterior lumbar fusion with a previously-validated 3-dimensional FE model of the intact lumbar spine (L1-S1). The post-operative models were made by modifying the intact model to simulate the implantation of interspinous spacer and pedicle screws at the L3-4 and L4-5. Four different configurations of the post-op model were considered: (1) a normal spinal model; (2) Type 1, one-level fusion using posterior pedicle screws at the L4-5; (3) Type 2, two-level (L3-5) fusion; (4) Type 3, Type 1 plus Coflex$^{TM}$ at the L3-4. hybrid protocol (intact: 10 Nm) with a compressive follower load of 400N were used to flex, extend, axially rotate and laterally bend the FE model. As compared to the intact model, Type 2 showed the greatest increase in Range of motion (ROM) at the adjacent level (L2-3), followed Type 3, and Type 1 depending on the loading type. At L3-4, ROM of Type 2 was reduced by 34~56% regardless of loading mode, as compared to decrease of 55% in Type 3 only in extension. In case of normal bone strength model (Type 3_Normal), PVMS at the process and the pedicle remained less than 20% of their yield strengths regardless of loading, except in extension (about 35%). However, for the osteoporotic model (Type 3_Osteoporotic), it reached up to 56% in extension indicating increased susceptibility to fracture. This study suggested that substitution of the superior level fusion with the interspinous spacer in multi-level fusion may be able to offer similar biomechanical outcome and stability while reducing likelihood of adjacent level degeneration.

이트라코나졸 마이크로스폰지의 약물 전달 시스템: 제조, 특성 및 방출 연구 (The Microsponge Delivery System of Itraconazole: Preparation, Characterization and Release Studies)

  • 조영호;이종화;김학형;이계원
    • KSBB Journal
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    • 제26권3호
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    • pp.217-222
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    • 2011
  • Itraconazole is a triazole antifungal agent to inhibit most fungal pathogens. To improve the oral absorption and dissolution of poorly water-soluble itraconazole, microsponge system composed of $Eudragit^{(R)}$ E100 and polyvinyl alcohol(PVA) formulated by quasi-emulsion solvent diffusion method, and its physicochemical properties and pharmacokinetic parameters of itraconazole were studied. The microsponge of itraconazole were discrete free flowing micro sized particles with perforated orange peel like morphology as visualized by scanning electron microscope (SEM). Results showed that the drug loading efficiency, production yield, and particle size of itraconazole microsponge were affected by drug to polymer ratio, the volume of internal phase containing methylene chloride, stirring rate and the concentration of PVA used. Also, the results showed that the dissolution rate of itraconazole from the microsponges was affected by drug to polymer ratio. In other words, the release rate of itraconazole from microsponges was increased from at least 27.43% to 64.72% after 2 h. The kinetics of dissolution mechanism showed that the dissolution data followed Korsmeyer-Peppas model. Therefore, these results suggest that microsponge system can be useful for the oral delivery of itraconazole by manipulating the release profile.