• Title/Summary/Keyword: 약물용출

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In vivo evaluation of infrared LASER mediated drug release of PLA-tetracycline complexes coated gold nanoparticle-titania nanotubes with mouse (마우스를 이용한 PLA - tetracycline 복합체 코팅 금 나노입자 - 티타니아 나노튜브의 적외선 레이저 유도 약물용출 생체 내 평가)

  • Moon, Kyung-Suk;Jeoung, Chan-Gwoun;Bae, Ji-Myung;Oh, Seunghan
    • Korean Journal of Dental Materials
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    • v.44 no.1
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    • pp.33-41
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    • 2017
  • In this study, we prepared PLA-tetracycline complexes coated gold nanoparticle-titania nanotubes and estimated their infrared LASER mediated drug release in the abdominal region of ICR mouse. The results of UV-Vis spectrophotometer showed the highest absorbance at the wavelength of 530 nm and 809 nm indicating the existence of gold nanoparticles. EDX analysis showed that the amounts of gold nanoparticle coated on titania nanotubes were approximately 3.62-36.5 wt%. In vivo test resulted that the tetracycline release value of experimental groups (6.5 ng/mL) was higher than that of control group (5.8 ng/mL) on the condition of 30 minutes of LASER irradiation. Therefore, it is expected that PLA-tetracycline complexes coated gold nanoparticle-titania nanotubes have the feasibility in the field of infrared remote controlled drug device and overcome the limitation of location and time of drug release in dental implant.

Preparation and Dissolution Characteristics of the Compression-Coated Controlled Release Tablet Exhibiting Three-step Release (압축코팅법에 의한 3단계 약물방출형 지속성제제의 제조 및 용출특성)

  • Kim, Cheol-Soo;Kwon, Hyeok-Lo;Cha, Bong-Jin;Kwon, Jong-Won;Yang, Joong-Ik;Min, Shin-Hong
    • Journal of Pharmaceutical Investigation
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    • v.22 no.2
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    • pp.133-137
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    • 1992
  • A novel oral controlled release tablet which may offer more uniform drug level in the body than simple zero-order was developed. The tablet is composed of three layers; outer film layer, middle part compression-coated hydroxypropylmethylcellulose (HPMC) matrix layer, and inner core layer. Each layer contains nicardipine HCl as a model drug. In vitro dissolution test showed that the tablet released the drug in clear three steps; a rapid initial release, followed by a constant rate of release, and then a second phase of fast release of drug. The dissolution characteristics could be modified easily by changing the grade of HPMC, thickness of matrix layer, content of methylcellulose in matrix layer, content of active ingredient in each layer. The pH of dissolution medium did not affect the release profile. This three-step release system is expected to raise the blood concentration rapidly to effective level and to maintain effective blood level longer than simple slow-release systems.

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Improvement of Dissolution Rate of Poorly Water Soluble Drug Using Self-microemulsifying Drug Delivery System (SMEDDS를 이용한 난용성 약물의 용출율 향상)

  • Kim, Kye-Hyun;Rhee, Yun-Seok;Bae, Joon-Ho;Chi, Sang-Cheol;Park, Eun-Seok
    • Journal of Pharmaceutical Investigation
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    • v.29 no.1
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    • pp.37-45
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    • 1999
  • ABSTRACT-A self-microemulsifying drug delivery system (SMEDDS) was developed to enhance the solubility and dissolution rate of poorly water soluble drug, biphenyl dimethyl dicarboxylate, DDB. The system was optimized by evaluating the solubility of DDB and the microemulsion existence range after the preparation of microemulsions with varying compositions of triacetin and surfactant-cosurfactant mixtures (Labrasol as surfactant (S) and the combination of Transcutol, Cremophor RH 40 and Plurol oleique as cosurfactant (CoS)). SMEDDS in this study markedly improved the solubility of DDB in water up to 10 mg/ml and the size of the o/w microemulsion droplets measured by dynamic light scattering showed a narrow monodisperse size distribution with an average diameter less than 50 nm. The microemulsion existing range is increased proportional to the ratio of S/CoS, however, it decreased remarkably as the oil content was more than 20%. In vitro dissolution study of SMEDDS showed a significantly increased dissolution rate of DDB in water (> 12 fold over DDB powder), and SMEDDS also had significantly greater permeability of DDB in Caco-2 cell compared to powders.

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Effect of Poloxamer Content on Dissolution of Diltiazem Hydrochloride from Core Pellets (딜티아젬 함유 코아 펠렛으로부터 약물의 용출에 미치는 폴록사머 함량의 영향)

  • Lee, Seung-Woo;Kam, Sung-Hoon;Hong, Ji-Woong;Choi, Ki-Song;Park, Eun-Seok;Chi, Sang-Cheol
    • Journal of Pharmaceutical Investigation
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    • v.32 no.4
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    • pp.305-311
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    • 2002
  • In order to evaluate the effect of poloxamer 407 content on the dissolution profiles of pellets, diltiazem HCl (DTL) core pellets were prepared with poloxamer 407 (50-90% w/w, with lactose as filler) using an extruder and a spheronizer. Any possible interaction between the drug and excipients was evaluated using DSC, IR and TLC. Dissolution tests were performed using USP basket method. In addition, scanning electron micrograph was performed to examine the surface roughness and cross sections. The release of DTL from the core pellets was decreased with increasing poloxamer 407 content. Cracks appeared on the surface of the core pellets with increasing the poloxamer 407 content, which may play a role on the retardation of the release of DTL from core pellets. There was no any significant interaction between the drug and excipients employed to prepare the core pellets.

Particle Size Distribution, Drug Loading Capacity and Release Profiles of Solid Lipid Nanoparticles of Phenylpropionic Acids (페닐프로피온산계 해열진통제 고형지질나노입자의 입도분포와 약물봉입 및 용출특성)

  • Kim, Yoon-Sun;Kim, Kil-Soo
    • Journal of Pharmaceutical Investigation
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    • v.28 no.4
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    • pp.249-255
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    • 1998
  • Solid Lipid Nanoparticle(SLN), one of the colloidal carrier systems, has many advantages such as good biocompatibility, low toxicity and stability. In this paper, the effects of drug lipophilicity and surfactant on the drug loading capacity, particle size and drug release profile were examined. SLNs were prepared by homogenization of melted lipid dispersed in an aqueous surfactant solution. Ketoprofen, ibuprofen and pranoprofen were used as model drugs and tweens and poloxamers were tested for the effect of surfactant. Mean particle size of prepared SLNs was ranged from 100 to 150nm. The drug loading capacity was improved with the most lipophilic drug and low concentration of surfactant. Particle size and polydispersity of SLNs were changed according to the used lipid and surfactant. The rates of drug release were controlled by the loading drug and surfactant concentration. SLN system with effective drug loading efficiency and proper particle size for the intravenous or oral formulation can be prepared by selecting optimum drug and surfactant.

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Enhancement of Dissolution Properties through Formulations of Insoluble Drug Biphenyl Dimethyl Dicarboxylate (난용성약물 Biphenyl Dimethyl Dicarboxylate의 제제화를 통한 용출증대)

  • Lee, Soon-Ah;Song, Kyung;Park, Eun-Jin;Sohn, Dong-Hwan;Go, Geon-Il;Kim, Jae-Baek
    • Journal of Pharmaceutical Investigation
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    • v.26 no.1
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    • pp.23-28
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    • 1996
  • The dissolution characteristics of DDB were markedly enhanced by preparing solid dispersions of drug with polyethylene glycol 6000. Solid dispersions of various weight fraction were formed by a melting method. And various tablets$(A{\sim}E)$ were prepared from these solid dispersions with excipients (lactose, com starch, Avicel and PVP) by wet granulation method. There were no significant differences in dissolution rates between physical mixture and DDB alone. But dissolution rates of solid dispersions were $1.4{\sim}2.0$ times greater than that of DDB alone and $1.2{\sim}1.8$ times greater than those of a commercial tablet.

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A Model for Diffusion and Dissolution Controlled Drug Release from Dispersed Polymeric Matrix (고분자 분산 매트릭스로부터의 약물방출에 관한 확산 및 용출 제어 모델)

  • Byun, Young-Rho;Choi, Young-Kweon;Jeong, Seo-Young;Kim, Young-Ha
    • Journal of Pharmaceutical Investigation
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    • v.20 no.2
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    • pp.79-88
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    • 1990
  • A numerical model for diffusion and dissolution controlled transport from dispersed matrix is presented. The rate controlling process for transport is considered to be diffusion of drug through a concentration gradient coupled with time-dependent surface change and/or disappearance of the dispersed drug in response to the dissolution. The transport behavior of drug was explained in terms of ${\nu}$ parameter: ${\nu}$ value means a ratio of diffusion time constant and dissolution time constant. This general model has wide range of application from where release is controlled by the diffusion rate to where release is governed by the dissolution rate. Based on this model, theoretical drug concentration, particle size distributions in the polymer matrix system and the resulting release rate were also investigated.

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Effect of the Viscosity of (Hydroxypropyl)methyl Cellulose on Dissolution Rate of Alfuzosin-HCl Granule Tablet (HPMC의 점도에 따른 염산 알푸조신 과립정제의 용출률 조절)

  • Kim, Won;Song, Byung-Joo;Kim, Dae-Sung;Kim, Su-Jin;Lee, Seon-Kyoung;Kim, Hye-Lin;Lee, Dong-Won;Khang, Gil-Son
    • Polymer(Korea)
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    • v.34 no.3
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    • pp.269-273
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    • 2010
  • The primary objective of this work is to find the optimal condition for the granule tablet formulation of alfuzosin-HCl that aims to achieve a sustained drug release. (Hydroxypropyl)methyl cellulose (HPMC) is one of the most widely used polymer as a drug formulation and therefore has been utilized in this study as an excipient. Alfuzosin-HCl granule tablet was developed using the various viscosities of HPMC and the effects of viscosity on drug release was investigated. Fourier transform-infrared (FTIR) and X-ray diffraction (XRD) were employed to investigate the chemical structure and crystallization of alfuzosin-HCl in the formulation. We prepared the granule tablet by a direct compression method and studied the release profile in the stimulated intestinal fluid (pH 6.8). As the viscosity of HPMC increased the release of alfuzosin-HCl decreased, demonstrating that controlled release of alfuzosin-HCl can be achieved by varying the viscosity of HPMC.

Development of Pharmaceutical Dosage Forms with Biphasic Drug Release using Double-Melt Extrusion Technology (이중 고온용융 압출 성형된 이중 방출능을 가지는 제형의 개발)

  • Kim, Dong-Wook;Kang, Chin-Yang;Kang, Changmin;Park, Jun-Bom
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.17 no.9
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    • pp.228-234
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    • 2016
  • The aim of this study was to develop pharmaceutical dosage forms with a bi-phasic drug using a double extrusion approach. Hot melt extrusion was performed using a co-rotating twin-screw extruder. The. 1st melt extrusion was performed using polymer with a relatively higher Tg, such as HPMC and the 2nd melt extrudate was obtained using the 1st extrudate and polymers with a lower Tg, such as HPMC-AS and PEO. In addition, the formulation with all the content in the same proportion as the double extudate was produced using single extrusion for comparison. Physical characterization was performed on the formulations employing differential scanning calorimetry (DSC). In vitro release tests were studied using a USP Type-I apparatus at $37{\pm}0.5^{\circ}C$ and 100 rpm. The similarity factor (f2) was also used to check the difference statistically. The DSC results indicated that the crystallinity of ibuprofen was changed to an amorphous state after extrusion in both double and single melt extrusion. Double melt extrudate with ibuprofen showed the desired release in acidic media (pH 1.2) in the first two hours and basic (pH 6.8) during six hours. Double melt extrudate with glimepiride showed faster release in 60 min of over 80%, whereas the single extrudate with glimepiride showed retarded release due to the interaction with HPMC. The similarity factor(f2) value was 28.5, which demonstrates that there were different drug release behavior between the double and single extrusion. Consequently, the double melt extrudated formulation was robust and gave the desired drug release pattern.

Determination of new anti-HIV agents, the KR-V series, in rat plasma using microbore high-performance liquid chromatography (HPLC를 이용한 랫드혈장내 새로운 항HIV제 KR-V series의 분석법)

  • Lee, Young-mi;Park, Myung-jin;Kim, Jin-suk;Shin, Ho-chul
    • Korean Journal of Veterinary Research
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    • v.40 no.4
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    • pp.741-746
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    • 2000
  • We have developed a rapid, simple and precise high-performance liquid chromatographic (HPLC) method using an UV detection system for the determination of new anti-HIV candidates, nineteen KR-V compounds, in rat plasma. We used a analytical columnn of $C_{18}$ ($5{\mu}m$, $250{\times}2.0mm$ I.D.) and a mobile phase of water and ACN mixture (40/60, v/v). Under these conditions, all the KR-V compounds were readily separated from plasma with retention times of 4-12 min. The limits of quantitation for the 19 KR-V compounds were 15-30 ng/ml. The recoveries from the plasma were higher than 85% (C.V.<10%) with exception of KR-V 2, 7 and 15. The compounds KR-V 2, 7 and 15, containing ester moieties, were found to be unstable in plasma. This result suggests that esters, like KR -V 2, 7 and 15, should be excluded from future structure design studies of anti-HIV KR-V agents. In conclusion, the current HPLC method is a valuable analytical tool for investigating the pharmacokinetics of the KR-V series in rats.

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