• Polymer(Korea)
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• v.28 no.4
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• pp.291-297
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• 2004

Water-soluble chitosan micro spheres were prepared by emulsification of chitosan solution in mineral oil followed by cross linking reaction with different amount of the cross linking agent (glutraraldehyde), different chitosan concentration. Then, the physicochemical properties such as morphological change by degradation, drug loading efficiency, and drug release profiles were investigated with the drug loaded water-soluble chitosan microspheres. Norfloxacin loaded water-soluble chitosan micro spheres showed excellent drug entrapping capacities without burst release caused by surface bound drug. The absence of the surface bound drug also confirmed by X-ray diffraction study. Degradation and drug release studies showed that the amount of the crosslinking agent played a crucial role for drug loading, release and degradation. The water-soluble chitosan micro spheres showed more sustained drug release profiles with slower degradation and larger particle size by increasing crosslinking agent.

• Journal of Periodontal and Implant Science
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• v.27 no.4
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• pp.751-765
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• 1997

Periodontal disease is a bacterially causal by disease, To remove plaque and bacteria, it has been necessary to prescribe chemical drug to patient to subjugate therapeutic unvalue by mechanical scaling. As a patient on a high dosage of the antibiotics to maintain the effective concentration may produce unfavorable side effects, this decase demands the Slow-release local drug delivery system. The object of the experiment is to study on the slow-release local drug delivery effects of calcium sulfate compounded with tetracycline that mainly used in periodontal disease. Experimental groups were divided into four classes as follow: Group 1 10% tetracycline compounded modified calcium sulfate paste. Group 2 : compounded and hardened 10% tetracycline and calcium sulfate. Group 3 : compounded 10% tetracycline and calcium sulfate, used Just before hardened. Group 4 : tetracycline-ethylene vinyl acetate fiber. In the four groups, release concentration, it's durability and the period of absorption by times are observed and concluded as follow: 1. An effective concentration($4{\mu}g/ml$) remained until 5 weeks in group 1, 9 days in group 2, 7 days in group 3, 15 days in group 4. 2. It was fully fused at 11.8 days average in group 2 and 14.8 days average in group 3. . There were no statistically significant results in tetracycline concentration until a week in group 2 and 3(p<0.05) These results suggest that tetracycline loaded calcium sulfate release sufficient tetracycline and fused in $11{\sim}14$ days, so calcium sulfate is useful carrier as slow release local drug delivery system.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1994.04a
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• pp.203-203
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• 1994

3) 결과 및 고찰 : 급성독성시험 : 대조군 및 G009투여군(최저 312.5mg/kg, 최고 5000mg/kg) 5용량에서 모두 사망예가 관찰되지 않았다 체중변화에 있어서도 대조군과 투여군 사이에 유의성 있는 차이는 없었다. 육안적 소견은 생존동물 모두에 약물에 기인한 내부장기의 이상이 관찰되지 않았다. 유전독성시험 : 마우스 골수세포를 이용한 소핵시험에서 약물 투여에 의한 어떠한 독성의 징후도 관찰되지 않았다. 포유류 배양세포를 이용한 염색체이상 시험에서 모든 농도에서 염색체 이상을 가진 세포의 출현빈도가 3% 이하로서 G009는 CHL세포에 대하여 염색체 이상유발성이 없었다. 살모넬라균을 이용한 복귀돌연변이 시험에서 투여군은 음성대조와 같은 정도 또는 그 이하의 복귀변이 집락수를 나타내었다.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1994.04a
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• pp.296-296
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• 1994

수술시 근육 이완제로 사용되고 있는 metocurine iodide는 항생물질 투여환자, 중증 근무력중, 전해질 평형실조, 중증 신질환이 있는 환자 등에서는 작용이 증가되어서 상용량에서도 약화사고의 우려가 있어 규제가 필요한 약물이다. Metocurine iodide를 생체 시료중에서 분석하기 위해 rosebengal과 착제를 형성시켜 유기용매로 이온쌍 추출을 한 후, HPLC를 이용하여 rose bengal율 분석함으로써 metocurine iodide를 간접 정량하는 방법을 확립하였다. 이 방법은 뇨와 혈액증에 함유된 metocurine iodide를 0.09 - 9.10$\mu\textrm{g}$/m1농도에서 분석할 수 있었으며, 상관계수는 0.994 - 0.999로 양호한 직선성을 나타내었고, 동시 처방 약물의 영향은 거의 없었다. 뇨 및 혈액중 metocurine iodide의 검출 한계는 각각 0.8ng. 1.2ng (S =3)이었다.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1993.04a
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• pp.79-79
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• 1993

BALB/C mice 에게 FVA를 감염시킨 후, zidobudine을 1 mg/ml 의 농도로 식수에 용해하여 18일 동안 자유롭게 섭취 시켰을때 (150-200 mg/kg/day) 비장비대가 90% 억제되었고, 혈액 중 reverse transcriptase 활성은 85%로 억제효과를 나타내었으며, 빈혈지수는 회복되는 경향을 나타내었다. 한편, ddI 는 AZT와 동일 용량에서 비장비대는 17%, 혈액 중 reverse transcriptase 억제효과는 34% 억제효과를 나타내었다. 반면에 ddC는 단독투여시 비장비대를 38% 억제하였으며, interferon $\alpha$와 병용투여시 83%의 억제효과를 나타내었다. 이상은 FVA 감염에 의한 mice의 비장비대를 지표로 하여 reverse transcriptase의 억제효과를 지닌 항 AIDS약물의 약효검색법으로 활용할 수 있음을 제시해준다.

• Progress in Medical Physics
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• v.20 no.3
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• pp.125-131
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• 2009

In this study, the paclitaxel eluting stent (PES) was prepared by coating a biliary stent with paclitaxel using various biopolymer such as poly (vinyl acetate) (PVAc), poly (lactic-co-glycolic acid) (PLGA), Silicone rubber for restenosis prevention in gastrointestinal disease by a dip-coating method. Drug contents of PES were increased as surface area of stent, concentration and molecular weight of coating polymer increase. In $^1H-NMR$ specta, we know that drug did not change by confirming specific peaks of paclitaxel in PES. As shown in SEM image, PES prepared using various biopolymer is coated clearly and regularly except Silicone rubber coating polymer. In in vitro cell cytotoxicity test, bare stent showed low cytotoxic effect against CT-26 colon carcinoma cell line on 3 day. However, PES coated with PLGA 502H showed the highest cytotoxicity because PLGA 502H is biodegradable polymer and has less molecular weight than other coating polymer. These results suggest that PES coated various biopolymer can be prevented restenosis in gastrointestinal disease.

• Korean Chemical Engineering Research
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• v.58 no.4
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• pp.541-549
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• 2020

The Drug Delivery System (DDS) is defined as a technology for designing existing or new drug formulations and optimizing drug treatment. DDS is designed to efficiently deliver drugs for the care of diseases, minimize the side effects of drug, and maximize drug efficacy. In this study, the optimization of tripolyphosphate (TPP) concentration on the size of Chitosan nanoparticles (CNPs) produced by crosslinking with chitosan was measured. In addition, the characteristics of Fe₃O₄-CNPs according to the amount of iron oxide (Fe₃O₄) were measured, and it was confirmed that the higher the amount of Fe₃O₄, the better the characteristics as a magnetic drug carrier were displayed. Through the ninhydrin reaction, a calibration curve was obtained according to the concentration of γ-aminobutyric acid (GABA) of Y = 0.00373exp(179.729X)-0.0114 (R² = 0.989) in the low concentration (0.004 to 0.02 wt%) and Y = 21.680X-0.290 (R² = 0.999) in the high concentration (0.02 to 0.1 wt%). Absorption was constant at about 62.5% above 0.04 g of initial GABA. In addition, the amount of GABA released from GABA-Fe₃O₄-CNPs over time was measured to confirm that drug release was terminated after about 24 hr. Finally, GABA-Fe₃O₄-CNPs performed under the optimal conditions were spherical particles of about 150 nm, and it was confirmed that the properties of the particles appear well, indicating that GABA-Fe₃O₄-CNPs were suitable as drug carriers.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1996.04a
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• pp.249-249
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• 1996

Gentamicin은 임상에서 많이 사용되는 aminoglycoside계 항생물질로서 세균의 세포막 단백질 합성을 억제하여 살균작용을 나타낸다. 최근 Gentamicin이 동물사료에 포함되거나 동물약품으로 많이 사용되어, 이를 복용한 식용가축에서의 잔류 량에 대한 인체유해성이 WHO/FAO 식품첨가물 전문가 협의회에서 논의되고 있다. Gentamicin의 육가공류의 잔류허용량 기준설정을 위한 독성 재평가의 일환으로 in vivo. in vitro 염색체이상시험을 실시하여 다음과 같은 결론을 얻었다. 1. 체외 염색체이상시험에서는 포유동물 배양세포인 chinese hamster lung cell을 배양하여 gentamicin sulfate 및 gentamicin을 최고 처리농도 5mg/$m\ell$부터 세포독성시험을 실시한 결과, 세포독성을 나타내지 않았다. 본 시험에서는 5mg/$m\ell$를 최고농도로 2.5, 1.25mg/$m\ell$의 3농도를 직접법 및 대사활성화법으로 각 농도당 2매의 플레이트씩 슬라이드를 제작, 결과를 판독한 결과, 직접법 및 대사활성화법 모두에서 전 농도 군에서 음성대조군과 같은 정도의 염색체이상을 유발하여 유전독성이 없음을 나타내었다. 2. 체내 염색체 이상시험에서는 ddY마우스를 이용하여 gentamicin sulfate의 LD$_{50}$의 1/2에 해당하는 200mg/kg을 최고농도로 gentamicin 과 gentamicin sulfate를 암수 각각 3마리씩 공비 2의 3농도로 투여한 후, 24시간째 골수세포의 염색체 표본을 제작하여 관찰한 결과, 세포독성 및 염색체 이상을 유발하지 않았다. 또한 동물약품으로 사용되는 치료용량 및 투약방법에 근거하여 10mg/kg 및 5, 2.5mg/kg을 1일 1회씩 4회 투여한 군에서도 암수에 상관없이 전 농도 군에서 염색체이상을 나타내지 않아 유전독성을 나타내지 않음을 관찰하였다.

• Journal of the Korea Academia-Industrial cooperation Society
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• v.13 no.5
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• pp.2125-2132
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• 2012

Fluoxetine and tianeptine are commonly used as antidepressants (AD), and haloperidol and risperidone are widely used as antipsychotic drugs (APD), and it modulates various ion channels. TREK2 channel subfamily is very similar to physiological properties of TREK1 channel which can play important roles in the pathophysiology of mental disorders such as depression and schizophrenia, therefore, the pharmacological effect of psychiatric and depression drug on TREK2 channel may be similar to those of TREK1. Using the excised inside-out patch-clamp technique, we have examined the effects of APD and AD on cloned TREK2 channel expressed CHO cells. Fluoxetine (selective serotonin release inhibitor, SSRI) inhibited the TREK2 channel in a concentration-dependent manner ($IC_{50}$ $13{\mu}M$), whereas selective serotonin reuptake enhancer (SSRE) tianeptine increased without reducing the TREK2 channel activity. Haloperidol also inhibited the TREK2 channel in a concentration-dependent manner ($IC_{50}$ $44{\mu}M$), whereas even higher concentration ($100{\mu}M$) of risperidone did not completely inhibit on the activity. This study showed that TREK2 channel was preferentially blocked by fluoxetine rather than tianeptine, and inhibited by haloperidol rather than risperidone, suggesting differential effect of TREK2 channels by APD and AD may contribute to some mechanism of adverse side effects.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1996.04a
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• pp.239-239
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• 1996

DA-1131은 Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Enterobacter cloacae, Proteus mirabilis, Proteus vulgaris 및 Pseudomonas aeruginosa 의 시험균주에 대하여 1-4의 MBC/MIC 비를 나타내었으며, 약물첨가에 의한 세균증식억제 과도 매우 우수하였으므로 광범위의 강력한 살균력을 나타내는 것으로 확인되었다. DA-1131의 PAE는 S. aureus Smith에 대하여는 1.28시간, K. pneumoniae 1에 대하여는 0.65시간, P. aeruginosa 93에 대하여는 1.90시간으로 나타나, MIC 이하의 낮은 농도에서도 세균에 대한 생육저해 효과가 관찰되었으며, 이러한 현상은 E. coli K-12에 DA-1131을 1/4 MIC(0.0125 $\mu\textrm{g}$/$m\ell$) 농도로 작용시켰을 때 균의 팽화와 신장 및 구형화가 동시에 일어나는 등 균형태변화를 초래하는 효과와 큰 상관성을 나타내었다. 또한, DA-1131은 감염방어효 에 매우 큰 영향을 끼치는 mouse macrophage와 매우 우수한 협력적살균작용을 나타내어 E. coli K-12 생세포는 1/16 MIC 이상의 DA-1131 공존하에서 쉽게 식균소화(phagocytosis) 되었다.