• 한국산학기술학회논문지
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• 제21권3호
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• pp.215-222
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• 2020

메트포르민은 제2형 당뇨병의 1차 치료제로 사용되는 약물로 다른 당뇨병 치료제에 비해 투여 용량이 크고 용해도는 높으나 위장관 투과도가 낮은 특성을 갖고 있으며 주로 위장관 상부에서만 흡수되는 이유로 생체이용률이 40~60%로 낮은 편이다. 따라서 본 연구를 통해 위체류 약물전달시스템을 적용하여 제제가 위에 머무르는 시간을 증가시키고 제제로부터 방출된 약물을 서서히 소장으로 이동시킨다면 생체이용률을 증가시킬 수 있을 것으로 기대된다. 팽윤성 시스템은 다른 위체류 약물전달시스템에 비해 안정성이 높아 개발목표기술로 선정하였고, 팽윤성 기제로는 기존의 연구와 다르게 카라기난과 히프로멜로오스를 병용하여 차별성을 확보하였다. 카라기난과 히프로멜로오스 병용 시스템은 각각의 함량이 15/110 질량분율일 때 가장 높은 팽윤성과 적절한 서방성 용출패턴을 나타내었다. 또한 각각의 함량이 15 %와 14 %가 되도록 제조한 메트포르민 정제를 시판 정제와 비교 시 더 우수한 팽윤성이 나타남을 확인하였다. 결론적으로 본 연구 결과에 의해 메트포르민의 서방출을 위한 새로운 팽윤성 위체류 약물전달시스템이 개발되었으며 다양한 주성분에 대한 추가적인 연구가 수행되면 의약품, 화장품, 건강기능식품 등의 분야에서 효과적인 약물전달시스템으로 응용될 수 있을 것으로 기대된다.

• 정보처리학회논문지D
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• 제13D권7호
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• pp.977-984
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• 2006

본 연구는 RFID를 이용하여 특수의약품의 생산, 유통, 병원으로 이어지는 약품의 흐름을 추적 관리하는데 목적이 있다. 이는 유통과정에서 약품의 위변조를 막고, 유통흐름의 투명성을 제고하기 위해 의약품의 생산시점에 RFID Tag를 부착하여, 유통과정 각 단계에서 의약품의 흐름을 추적 관리하여 최종 사용자가 안심하고 사용할 수 있도록 한다. 또한 부가적으로 유통흐름상의 각 단계의 주체들에게 재고관리 정보를 제공하여 의약품 수급 및 관리에 대해 편의성을 제공하고 입출고 작업을 원활하게 수행할 수 있도록 한다. 본 연구는 의약품 분야에 FRID 적용가능성을 검토하는 연구로서 약품코드에 대한 RFID코드 표준안의 적용과 국산 미들웨어의 적용을 시도하였고 향후 의약품 분야의 이력관리를 할 수 있는 E-pedigree의 기초를 마련하고자 한다 또한 기술적으로 유통분야에 많이 쓰이는 90Mhz 대역의 리더 적용 및 약품에 적합한 RFID Tag의 설계 및 선정 결과를 제시한다.

• Journal of Pharmaceutical Investigation
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• 제35권6호
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• pp.445-451
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• 2005

As a selective ${\alpha}_{1A}-adrenoreceptor$ antagonist, tamsulosin has been used clinically for urinary obstructed patients with benign prostatic hyperplasia. The single and multi-layered pellets containing tamsulosin hydrochloride were prepared in an effort to control the drug release, avoiding dose-dependent side effects of tamsulosin hydrochloride upon oral administration. The drug release from multi-layered pellets was substantially controlled, compared with single layered pellets. The drug release from coated pellets with single or multi layer was affected by the nature of coating agent, the percentage of coating level and the presence of hydrophilic material in coating layer. In conclusion, the controlled release oral delivery system using multi-layered pellet is very useful for tamsulosin hydrochloride, resulting in improvement of patient compliance and therapeutic drug levels for a longer period of time.

• Archives of Pharmacal Research
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• 제28권5호
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• pp.612-618
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• 2005

A mucoadhesive microsphere was prepared by an interpolymer complexation and solvent evaporation method, using chitosan and poly(acrylic acid) (PAA), to prolong the gastric resid ence time of the delivery system. The Fourier transform infrared results showed that microspheres were formed by an electrostatic interaction between the carboxyl groups of the PAA and the amine groups of the chitosan. X-ray diffraction and differential scanning calorimetry analysis showed that the enrofloxacin in the chitosan-PAA microsphere was molecularly dispersed in an amorphous state. Scanning electron microscopy of the surface and the quantity of mucin attached to the microspheres indicated that chitosan-PAA microspheres had a higher affinity for mucin than those of chitosan alone. The swelling and dissolution of the chitosan-PAA microspheres were found to be dependent on the pH of the medium. The rate of enrofloxacin released from the chitosan-PAA microspheres was slower at higher pH; therefore, based on their mucoadhesive properties and morphology, the chitosan-PAA microspheres can be used as a mucoadhesive oral drug delivery system.

• 약학회지
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• 제49권3호
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• pp.217-224
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• 2005

Human Immunodeficiency Virus type 1 (HIV-l) based lentivirus vector has demonstrated great potential as gene therapy vectors mediating efficient gene delivery and long-term transgene expression in both dividing and nondividing cells. However, for clinical studies it must be confirmed that vector preparations are safe and not contaminated by replication competent lentivirus (RCL) related to the parental pathogenic virus, HIV-l. In this study, we would like to establish the method for titration and RCL detection of lentivirus vector. The titration was determined by vector expression containing the green fluorescent protein, GFP in transduced cells. The titer was $1{\times}10^7$ Transducing Unit/ml in the GFP expression assay and $8.9{\times}10^7$ molecules/ml in the real-time PCR. Also, for the detection of RCL, we have used a combination method of PCR and p24 antigen detection. First, PBS/psi and VSV-G region in the genomic DNA of transduced cells was detected by PCR assay. Second, transfer and expression of the HIV-1 gag gene was detected by p24 ELISA. In an attempt to amplify any RCL, the transduced cells were cultured for 3 weeks (amplification phase) and the supernatant of amplified transduced cell was used for the second transduction to determine whether a true RCL was present (indicator phase). Analysis of cells and supernatant at day 6 in indicator phase were negative for PBS/psi, VSV-G, and p24 antigen. These results suggest that they are not mobilized and therefore there are no RCL in amplification phase. Thus, real-time PCR is a reliable and sensitive method for titration and RCL detection of lentivirus vector.

• Journal of Pharmaceutical Investigation
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• 제38권3호
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• pp.163-169
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• 2008

Liposomes are spherical vesicles composed of lipid bilayer membranes. However, the conventional liposomes have been found to be plagued by rapid opsonization and taken up by the reticuloendothelial system (RES), resulting in shortened circulation time and limited intracellular uptake to target cell. In this study, polyethyleneglycol-cationic liposomes (PCL) containing cationic lipid and DSPE-mPEG were prepared by thin film cast-hydration method. The PEG liposomes had approximately $97.0{\pm}1.3\;nm$ of mean particle diameter and $-21.7{\pm}1.2\;mV$ of zeta potential value. PCL had $96.4{\pm}1.8\;nm$ of mean particle diameter and $-8.7{\pm}1.1\;mV$ of zeta potential value with a decrease of about 10 mV compared to the PEG liposomes. Loading of model drug, doxorubicin (DOX), in liposomes were carried out by using remote loading method and the loading efficiency of DOX in liposomes was about $95.0{\pm}1.9%$. Intracellular uptake and cytotoxicity of PCL were higher than that of PEG liposomes to murine B16F10 melanoma cells. In addition, anti-tumor activity of PCL was similar to that of PEG liposomes on growth of A549 human lung carcinoma in BALB/c mice. Consequently, PCL modified with cationic lipid may be applicable as anticancer drug carriers that can increase intracellular uptake and therapeutic efficacy.

• Journal of Pharmaceutical Investigation
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• 제30권4호
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• pp.247-252
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• 2000

The advantages of transdermal administration are avoiding hepatic first pass effect, minimizing inter- and intra-patient variation, maintaining steady-state plasma level to provide long-term therapy from a single dose, and allowing a rapid termination of drug input. Clenbuterol, a selective ${\beta}_2-adrenergic$ receptor stimulant, has been introduced as a potent bronchodilator for patients with bronchial asthma, chronic obstructive bronchial disease. For the development of transdermal systems containing clenbuterol, two limiting factors - long lag time and low flux - must be overcome. In this study, we attempted to select optimal formulation for preparation of clenbuterol patch using hairless mouse skin and flow-through diffusion cell. The flux of clenbuterol increased as the percent of clenbuterol dose dependently in the concentration range of 5-15%. Based on this result, we fixed the concentration of clenbuterol as 15%. The effect of various penetration enhancers on percutaneous absorption of clenbuterol through hairless mouse skin was investigated. Labrafil was the most effective enhancer, which increased the permeability of clenbuterol approximately 4-fold compared with the control without penetration enhancer. Optimal enhancer concentration was 3%. The effect of various adhesives on penetration of clenbuterol was also investigated. Among the adhesives studied, MA-31 was the most effective adhesive. Furthermore, the clenbuterol patch composed of 15% clenbuterol, 3% Labrafil and 82% MA-31, which gave most excellent penetration of drug in in vitro penetration study, maintained therapeutic plasma levels in in vivo study using S.D. rats. These studies demonstrated a good feasibility of clenbuterol administration through the intact skin using a transdermal patch, and show a possibility of the development of clenbuterol patches.

• 대한의용생체공학회:의공학회지
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• 제23권3호
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• pp.189-196
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• 2002

피부를 통한 약물 전달 방법은 국소 병변 부에 직접적으로 약물을 전달할 수 있는 장점을 가졌으나 피부의 가장 바깥 층인 각질층의 장벽기능으로 인해 약물 전달 능력에 제한이 있다. 본 연구에서는 산소 압력 방법과 초음파 방법을 결합하는 방법을 시도하여 약물 전달 능력의 향상 정도를 검증해 본다. 흡수 물질로는 수분을 사용하였고 수분의 흡수도를 측정하기 위해 피부 임피던스 방법을 선택하였다. 실험은 총 42명을 대상으로 각각 대조군(13명) 초음파군(13명), 산소 압력군(6명). 초음파와 산소압력 결합군(10명)으로 나누어서 시행하였다. 각 군마다 다른 약물 전달방법을 손등 부위에 적용하여 20분간 피부 임피던스 변화를 측정 한 값을 PC에 저장하였다. 수분을 적용한 대조군의 경우 피부 임피던스의 변화가 거의 일어나지 않고. 초음파를 적용한 군과 산소를 적용한 군은 수분을 적용한 군보다 25-30배정도 높은 수분 홉수를 보였으며. 초음파와 산소 압력을 결합한 방법은 수분을 적용한 군보다 70배정도 높은 수분 흡수를 보였다. 이러한 평균의 타이를 반복 측정된 분산방법(Repeated Measures Analysis of Variance)의 다변량 검증과 다중비교를 통해 변화량간의 차이를 검증하여 유의성을 확인하였다

• Journal of Ginseng Research
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• 제41권1호
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• pp.78-84
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• 2017

Background: In the present study, metabolite profiles of ginsenosides Rk1 and Rg5 from red ginseng or red notoginseng in zebrafish were qualitatively analyzed with ultraperformance liquid chromatography/quadrupole-time-of-flight MS, and the possible metabolic were pathways proposed. Methods: After exposing to zebrafish for 24 h, we determined the metabolites of ginsenosides Rk1 and Rg5. The chromatography was accomplished on UPLC BEH C18 column using a binary gradient elution of 0.1% formic acetonitrile-0.1% formic acid water. The quasimolecular ions of compounds were analyzed in the negative mode. With reference to quasimolecular ions and MS2 spectra, by comparing with reference standards and matching the empirical molecular formula with that of known published compounds, and then the potential structures of metabolites of ginsenosides Rk1 and Rg5 were acquired. Results: Four and seven metabolites of ginsenoside Rk1 and ginsenoside Rg5, respectively, were identified in zebrafish. The mechanisms involved were further deduced to be desugarization, glucuronidation, sulfation, and dehydroxymethylation pathways. Dehydroxylation and loss of C-17 residue were also metabolic pathways of ginsenoside Rg5 in zebrafish. Conclusion: Loss of glucose at position C-3 and glucuronidation at position C-12 in zebrafish were regarded as the primary physiological processes of ginsenosides Rk1 and Rg5.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1996년도 춘계학술대회
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• pp.278-278
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• 1996

Judging from hydrocortisone concentration in dosing area, the extent of absorption was reduced in the liposome-gel formulation. However, higher and sustained skin concentrations of hydrocortisone were achieved for the liposome-gel as compared to the ointment. Drug concentration in both viable and deep skin reached its maximum within 0.5 h after application of both formulations to both skin types. Drug concentrations in both skins from the ointment declined with time, while those from the liposome-gel were greatly sustained. The sustainment by the liposome-gel was more remarkable in the viable skin than in the deep skin. Drug concentration in the viable skin could be maintained at a nearly constant level for over 8 h by applying the liposome-gel. As a result, a 5-fold higher viable skin drug concentration was obtained from the liposome-gel than from the ointment at 8 h after the application to the SC-removed skin. However, the plasma concentration of hydrocortisone at 4 h from the liposome-gel was only one-fourth (p<0.01) the value from the ointment when the drug was applied to the SC-removed skin, consistent with. the lower urinary (one-third, p<0.05) and fecal (one-half, p＜0.05) excretion. Conclusions : Retarded diffusion of the drug from the skin to the systemic blood stream appears to be a potential factor in the sustained skin concentration of hydrocortisone from the liposome-gel, Interaction of hydrocortisone in the skin with phosphatidylcholine, a component of the liposomes and skin, may well be a factor in retarding the diffusion of the drug in the skin.