• 폴리머
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• 제36권4호
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• pp.500-506
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• 2012

본 연구에서는 고혈압 치료제로 사용되고 있는 난용성 약물인 에프로살탄의 용해도 개선을 위한 고체분산체제제를 개발하기 위한 제조방법 및 조성비를 최적화하였다. 친수성 고분자 기제로 poly(ethylene glycol)(PEG)와 poly(vinyl pyrrolidone)(PVP)를 이용하여, 약물과 고분자의 조성비가 1:1에서 1:5 사이의 고체분산체를 용매증발법과 열용융법에 의해 제조한 후 비교 평가하였다. 용매증발법이 균일한 고체분산체 제조에 효과적이었고, 고분자의 조성비 증가와 함께 약물 결정성이 감소되었다. PEG 보다는 PVP가 약물과의 우수한 상용성을 바탕으로 결정화도 감소와 용해도 개선 효과가 우수하였다. 또한 고체분산체 제조 시 고분자 계면활성제인 poloxamer 407를 첨가한 경우, 약물의 결정성이 대부분 사라져 고체분산체 내 대부분의 약물 분자들이 무정형으로 분산되어 있음을 알 수 있었고,약물의 용해도 또한 3~4배 이상 향상되었다.

• 폴리머
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• 제34권5호
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• pp.459-463
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• 2010

전신 진균감염 치료에 널리 사용되는 광범위 항진균제이며 대표적인 소수성 약물인 amphotericin B(AmB)의 효과적인 점막부착형 약물전달체로서 가용화제인 L-arginine, 점착성 고분자인 카보폴(carbopol), 온도감응성 고분자인 Poloxamer 407(P 407)로 구성된 하이드로젤 제형을 제조하였다. L-Arginine의 첨가로 AmB의 용해도가 2.6 mg/mL까지 향상되었으며, P 407 수용액은 20% w/v 이상의 농도에서 온도 변화에 따른 졸-젤-졸 상전이(phase transition)를 보였다. 이러한 상전이 온도는 약물 및 L-arginine의 존재에 의해 영향을 받았고, 점착성 고분자인 카보폴의 혼합에 의해 상전이 영역이 확장되었다. L-Arginine의 가용화 효과로 AmB의 약물방출특성이 향상되었고, 점착성 고분자인 카보폴의 첨가는 농도에 의존하여 약물방출을 지연시키는 효과가 있었다.

• 한국임상수의학회:학술대회논문집
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• 한국임상수의학회 2008년도 추계학술대회
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• pp.178-178
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• 2008

• Journal of Pharmaceutical Investigation
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• 제35권3호
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• pp.165-171
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• 2005

Itraconazole is a triazole antifungal agent to inhibit most fungal pathogens. However, it is difficult for itraconazloe to be delivered by topical system due to its poor aqueous solubility. First, niosomes containing drug were prepared with span 60, cholesterol. tocopherol and poloxamer 407 as vesicle forming agents in an effort to increase solubility of itraconazole. And then prepared niosomes were dispersed in O/W creams (containing xanthan gum, glycerin, vaseline, glyceryl monostearate and $Cerix^{\circledR}-5$) or gels (containing xanthan gum and poloxamer 407). Both creams and gels were evaluated with respect to their rheological properties, in vitro permeation through excised skin of hairless mouse. Creams or gels containing niosome showed pseudoplastic flow and hysteresis loop. For both creams and gels, viscosity was increased with increasing the content of glycerine or vaseline and the content of gel forming polymer, respectively. In creams, the permeability of drug to skin was decreased with increasing the viscosity of cream. The permeability of drug was affected by pH as well as viscosity of gel. In vitro permeation test results demonstrated that cream formulations showed better permeability than gels. In conclusion, these results suggest that creams formulation containing niosome can be useful for the topical delivery of intraconazole.

• KSBB Journal
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• 제31권4호
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• pp.219-227
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• 2016

Valsartan, a drug for the treatment of cardiovascular disease, exhibited low bioavailability which was caused by, at least in part, limited solubility at low pH. Present investigation deals with the preparation and characterization of gastro-retentive drug delivery system (GRDDS) using valsartan solid dispersion. We prepared solid dispersion using surfactants (Poloxamer 407) and alkalizer ($Na_2CO_3$) which may to be useful for improving solubility of valsartan at low pH and evaluated by saturated solubility of valsartan in distilled water. Valsartan gastro-retentive (GR) tablets containing solid dispersion prepared and evaluated by weight variation, floating time and dissolution rate. Compression at lower pressures resulted in the tablets floating over simulated gastric fluid (pH 1.2) for more than 17 h. In vitro release of valsartan from GR tablet was dependent on the amount of poloxamer 407 and hydroxypropyl methylcellulose. On the basis of evaluation parameter, formulation E-3 was selected as a final formulation. Therefore, it can be concluded that the GR tablets containing solid dispersion may be exploited successfully for the delivery of poorly drug such as valsartan.

• 한국자원식물학회지
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• 제30권6호
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• pp.601-611
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• 2017

Hyperlipidemia is an increase in one or more of the plasma lipids, including triglycerides, cholesterol. Ginseng has been used as a valuable tonic and for the treatment of various diseases. The objective of this study was to evaluate the effects of Jinan red ginseng (JRG) water extract on the blood and serum in rabbits with hyperlipidemia induced by poloxamer 407 when supplied in drinking water. JRG treatment was performed for 20 weeks. We evaluated the effects of the JRG treatment on diabetes through hematological and biochemical analysis before and after JRG treatment were performed. Our results indicate that LDL, total cholesterol, and triglycerides were significantly decreased compared prior JRG supply. CRE, BUN, CK and UA levels indicating renal functions are significantly reduced when compared to those prior to the JRG supply. In addition, AST, ALT, ALP, and LDH were significantly reduced indicating hepatoprotective effect. Blood electrolytes deteriorated in HL rabbits were improved when JRG supplied. In conclusion, Biochemical and hematological analysis demonstrate that the JRG is effective to alleviate the hyperlipidemia signs.

• 약학회지
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• 제40권6호
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• pp.646-652
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• 1996

Epidermal Growth Factor (EGF), discovered by Stanley Cohen in 1960, has a potential healing effect for wounds and bums. Considering wound care, in order to avoid physical stress at the wound surface and efficiently apply EGF, the need for viscous spraying solutions was essential. Viscous spraying solutions containing EGF were prepared by utilizing viscosity-building polymer, poloxamer 407, and by introducing liposome systems. On the other hand, EGF is purified on reverse HPLC gradient program with the mobile solvent of acetonitrile. It is necessary to observe liposomal EGF changes as the acetonitrile contents varied in order to introduce liposome systems at the step of EGF solution (at the time of EGF purifying). By evaluating the size distribution and entrapment efficiency of EGF liposome, it was possible to detemine the limit contents of acetonitrile and establish the optimal conditions for solution formulations. It has been revealed that, as the acetonitrile content increases, mean diameter of EGF liposomes increased and the width of size distribution tends to decrease. The limit contents of acetonitrile were 10%, since there was little difference to the acetonitrile free liposomes.

• Archives of Pharmacal Research
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• 제29권10호
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• pp.928-933
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• 2006

Percutaneous delivery of NSAIDs has advantages of avoiding hepatic first pass effect and delivering the drug for extended period of time at a sustained, concentrated level at the inflammation site that mainly acts at the joint and the related regions. To develop the new topical formulations of pranoprofen that have suitable bioadhesion, the gel was formulated using hydroxypropyl methylcellulose (HPMC) and poloxamer 407. The effects of temperature on drug release was performed at $32^{\circ}C$, $37^{\circ}C$ and $42^{\circ}C$ according to drug concentration of 0.04%, 0.08%, 0.12%, 0.16%, and 0.2% (w/w) using synthetic cellulose membrane at $37{\pm}0.5^{\circ}C$. The increase of temperature showed the increased drug release. The activation energy (Ea), which were calculated from the slope of lop P versus 1000/T plots was 11.22 kcal/ mol for 0.04%, 10.79 kcal/mol for 0.08%, 10.41 kcal/mol for 0.12% and 8.88 kcal/mol for 0.16% loading dose from the pranoprofen gel. To increase the drug permeation, some kinds of penetration enhancers such as the ethylene glycols, the propylene glycols, the glycerides, the non-ionic surfactants and the fatty acids were incorporated in the gel formulation. Among the various enhancers used, propylene glycol mono laurate showed the highest enhancing effects with the enhancement factor of 2.74. The results of this study suggest that development of topical gel formulation of pranoprofen containing an enhancer is feasible.

• 한국임상수의학회지
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• 제26권6호
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• pp.547-555
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• 2009

이 실험은 복강 유착 방지효과를 나타내는 Poloxamer/Sodium Alginate (PX/SA) 혼합물의 최소용량과 주요기 관의 독성 여부에 대해 알아보기 위해 실시하였다. 건강한 잡종성견 25마리를 음성대조군 (무처치), 양성대조군 (2% carboxymethyl chitosan 용액 처치), 실험군 1 (PX/SA 혼합물 0.25 ml 처치), 실험군 2 (PX/SA 혼합물 0.5 ml 처치), 실험군 3 (PX/SA 혼합물 1.0 ml 처치) 으로 나누고 각 군당 5마리씩 배치하였다. 혈액학 검사 (백혈구,섬유소원)와 혈액화학 검사(AST, ALT, ALP, BUN, Creatinine)를 위해 정맥에서 혈액을 채취하였다. 유착방지효과를 알아보기 위해 돌창자에 찰과상을 일으켜 carboxymethyl chitosan 용액, PX/SA 혼합물을 처치하는 장막 찰과 모델을 이용하였다. 유착부위의 유착강도는 장력측정기를 이용하여 측정하였다. 조직검사를 위해 각 군의 모든 개로부터 간과 신장 조직을 채취하였다. PX/SA혼합물을 처치한 실험군이 음성 대조군보다 유착발생 빈도와 유착강도 모두 낮게 측정되었다. 실험군 간의 비교에서 실험군 2에서 유착강도가 유의적으로 감소하였다. AST, ALT, ALP, BUN, Creatinine 은 대조군과 실험군 사이 유의적 차이가 발견되지 않았으며, 모든 군에서 얻어진 조직 표본에서도 군간 유의적 차이를 보이지 않았다. 본 실험의 결과, PX/SA 혼합물 0.5 ml는 복강 유착 형성을 효과적으로 감소시켰으며, 물질이며, 혈액 및 주요 장기에 대한 독성도 없는 것으로 사료된다

• 대한한의학방제학회지
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• 제21권1호
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• pp.99-110
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• 2013

Objectives : This study was designed to investigate the effect of a herbal preparation HJ01 consisting of Salicornia herbacea, Citri Reticulatae Pericarpium, Crataegi Fructus and Glycyrrhizae Radix on adipocyte differentiation in OP9 cells and on poloxamer 407(P-407)-induced hyperlipidemia in mice. Methods : 1. MTT assay was used to evaluate the potential cytotoxicity of Salicornia herbacea, Citri Reticulatae Pericarpium, Crataegi Fructus, Glycyrrhizae Radix and HJ01, respectively. 2. Bone-marrow derived OP9 cells were treated with HJ01, and the alterations in fat storage in the cells were determined by the Oil red O assay. 3. The protein level of CAAAT/enhancer binding protein alpha($C/EBP{\alpha}$), as a adipocyte differentiation marker, was examined using western blot analysis in differentiated OP6 cells. 4. Adult male C57BL6 mice received intraperitoneal injections of P407 to induce hyperlipidemia, simultaneously, were treated with HJ01 for 4 weeks. Then the cholesterol (TC), triglyceride (TG) and high-density lipoprotein-cholesterol (HDL-c) levels in sera and liver tissues were measured. Results : 1. The MTT assay exhibited that Salicornia herbacea, Citri Reticulatae Pericarpium, Crataegi Fructus, Glycyrrhizae Radix and HJ01 showed no significant cytotoxicity in tested dosages. 2. Ten days' treatment with HJ01 markedly inhibited the increases in fat storage in differentiated OP6 cells. 3. Four weeks' treatment with HJ01 down-regulated the protein level of CAAAT/enhancer binding protein alpha($C/EBP{\alpha}$) but up-regulated the levels of adiponectin in differentiated OP9 cells. 5. HJ01 inhibited the accumulation of TC and TG in liver tissues and increased serum levels of TC in hyperlipidemic mice. Conclusions : These results suggest that HJ01 can in vitro inhibit adipocyte differentiation and fat storage in OP6 cells, in vivo improve the hyperlipidemia induced by P-407 in mice, which may be mediated by promoting glucose uptake and improving a lipid metabolite profile.