• 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.

• The Korean Journal of Physiology and Pharmacology
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• 제8권6호
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• pp.329-333
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• 2004

In this study, we investigated whether TNF-alpha, IL-1beta, CTMA (carboxymethyl trimethylammonium) and LPD (Lup-20[29]-ene-3beta,28-diol) affect mucin release from airway goblet cells and compared the activities of these agents with the inhibitory action of PLL and the stimulatory action of ATP on mucin release. Confluent primary hamster tracheal surface epithelial (HTSE) cells were metabolically radiolabeled with $^3H-glucosamine$ for 24 h and chased for 30 min in the presence of varying concentrations of each agent to assess the effects on $^3H-mucin$ release. The results were as follows: TNF-alpha, CTMA and LPD increased mucin release at the highest concentration, but IL-1beta did not. We conclude that CTMA and LPD can stimulate mucin release by directly acting on airway mucin-secreting cells, and suggest that these agents should be further investigated for the possible use as mild expectorants during the treatment of chronic airway diseases.

• 약학회지
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• 제32권1호
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• pp.26-39
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• 1988

Eudragit $RS^{\circledR}$ polymer was used as a wall material for the microencapsulation of aspirin by a phase separation method from chloroform-cyclohexane system with 5% polyisobutylene (PIB) in cyclohexane, and microcapsules obtained were evaluated by particle size analysis, scanning electron microscopy (SEM), drug release and drug stability test. With PIB as a coacervation inducing agent, smooth and tight microcapsules with less aggregation were obtained. Below 1 : 0.3 core-wall ratio, it was possible to coat individual particle. Variation of production conditions showed that increasing the proportion of wall material, particle size and wall thickness of microcapsules and the concentration of paraffin wax in cyclohexane as a sealant sustained drug release rates effectively. SEM confirmed that larger microcapsules after drug release did not rupture into smaller particles but contained a few small pores on the surface. Aspirin release from Eudragit $RS^{\circledR}$ coated microcapsules was independent of the pH of medium, and the mechanism of drug release from non-sealed and sealed microcapsules appeared to fit Higuchi matrix model kinetics. Aspirin in the mixture of aspirin microcapsules and sodium bicarbonate was by far more stable than that in the mixture of pure aspirin and sodium bicarbonate.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.294.2-295
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• 2003

Gentisic acid, a skin-whitening agent, is known to possess tyrosinase inhibition activity. In order to develop an effective skin-whitening agent, hydroquinone derivatives in which the carboxylic acid moiety of gentisic acid was replaced with various functional groups, were selected and evaluated for their ability to inhibit tyrosinase activity as well as to inhibit melanin release. (omitted)

• 구강회복응용과학지
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• 제35권2호
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• pp.81-89
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• 2019

목적: 이 연구의 목적은 RMGIC에 레진 표면 코팅제를 적용하였을 때 용해도와 불소 유리량 간의 상관관계를 알아보는 것이다. 연구 재료 및 방법: 불소 유리량과 용해도 측정을 위해 표면 코팅제를 도포하지 않은 Fuji II $LC^{(R)}$, $Filtek^{TM}$ Z350XT와 G coat $plus^{TM}$를 도포한 Fuji II $LC^{(R)}$, $Permaseal^{(R)}$를 도포한 Fuji II $LC^{(R)}$를 준비하고 불소 유리량과 용해도를 측정하였다. 결과: 일간 불소 유리량은 표면 코팅제 간의 차이는 유의하지 않았다. 불소 누적 유리량은 56일에 RMGIC를 사용한 군에서 유의한 차이를 보였다(P < 0.05). 용해도 측정에서 표면 코팅제를 도포하지 않은 RMGIC가 다른 세 군에 비하여 7일 째에서만 유의한 차이를 보였다(P < 0.05). 결론: 표면 코팅제는 RMCIG에서 초기 용매에 의한 물성 저하를 막아 수복재 내부에 불소를 보존하며 추후 수복재의 불소의 방출과 저장에 대한 영향 또한 감소한다.

• Journal of Pharmaceutical Investigation
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• 제28권2호
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• pp.87-92
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• 1998

Kojic acid (KA) is an antimelanogenic agent which has been widely used in cosmetics to whiten the skin color. However, it has the drawbacks of the skin irritancy and the instability against the pH, temperature, and light. In order to overcome these problems, various topical gels and multiple emulsion creams which can control the release of active ingredient, KA, were formulated employing cream bases of mineral oil with caprylic capric triglyceride and hydrophilic polymers such as chitosan, carbopol. and pluronics. Using Franz diffusion cells mounted with a synthetic cellulose membrane (MWCO 12,000), drug release characteristics of the formulations were evaluated by the HPLC assay of KA concentration in the receptor compartment of pH 7.4 phosphate buffered saline solution. Drug release from chitosan-based gels (ChitoGel) obeyed to the first order kinetics with a rapid release especially in the initial period. However, pluronic-based gels (PluGel) and carbopol-based gels (CarboGel) revealed controlled release of drug to some extent, followed by the square root-time kinetics. Moreover, the release of KA was further controlled with the W/O/W multiple emulsion creams (MultiCream), showing the apparent zero order release kinetics by virtue of dynamic ratecontrolling membrane of the oil layer. The flux $(J,\;{\mu}g/cm^2/hr)$ of ChitoGel. CarboGel. PluGel. and MultiCream in the initial period of 6hr were 73.30, 28.67. 24.04 and 7.72, respectively. On the other hand, the skin irritancy score of ChitoGel and MultiCream were observed as 2.5 and 2.3 respectively, in the rabbit skin irritation test. Although there were insignificant differences at p<0.05 between those formulations, it was possible to conclude that the W/O/W multiple emulsion creams containing KA might be a good candidate for an antimelanogenic drug delivery system due to the controlled release of acidic drug molecules.

• 폴리머
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• 제26권5호
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• pp.691-700
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• 2002

항암제가 함유된 생분해성 고분자 디바이스를 이용한 국소전달요법은 종양 부위에 고농도로 약물을 전달시킬 수 있는 이유로 약물의 효율성을 증가시킬 수 있다. 1,3-bis(2-chloroethyl)-1-nitro-sourea (BCNU, carmustine)는 뇌종양 치료를 위하여 가장 일반적으로 사용되는 화학요법적 약물이다. 표적 부위까지 항암제를 효과적으로 전달하기 위한 이식제의 설계는 중요한 인자이다. 본 연구에서 약물의 방출경향을 조절하기 위해서 생분해성 웨이퍼의 첨가제와 다양한 제형 변화로부터 BCNU의 방출패턴을 조사하였다. 각각 3.85, 10, 20 및 30%의 BCNU를 함유한 PLGA 웨이퍼를 다양한 형태(직경 3, 5 및 10 mm, 두께 0.5, 1 및 2 mm)로 직접 압축성형법에 의해 제조하였다. 생체외 방출실험에서 BCNU 함유 PLGA 웨이퍼로부터 약물 방출거동은 웨이퍼의 포기 약물 함유량, 무게, 직경, 두께, 부피, 표면적 및 PLGA 분자량뿐만 아니라 첨가제의 종류와 같은 다양한 변수로 조절했다. 웨이퍼로부터 약물의 방출은 BCNU 함유량 및 염화나트륨 (NaCl)과 폴리엔비닐피롤리돈 (PVP)이 증가할수록 촉진되었다. 또한, BCNU가 함유된 PLGA 웨이퍼의 무게와 형태변화에 대한 조사를 통하여 다양한 기하학적 인자들과 첨가제의 효과를 고찰하였다.

• 접착 및 계면
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• 제9권2호
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• pp.8-15
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• 2008

마이크로캡슐은 다양한 기능성 물질의 약물 전달 시스템으로서 화장품과 제약 분야에서 널리 적용되고 있다. 키토산은 천연에 풍부하게 존재하는 생체고분자로 생체적합성이 우수하며 무독성이다. 본 연구에서는 키토산 마이크로캡슐을 글루타르알데히드를 가교제로 사용하여 W/O 형태의 유화법으로 제조하였다. 유화제로는 span80을 사용하였으며 가교가 시행되는 bath상의 물질은 mineral oil을 사용하였다. 제조된 키토산 마이크로캡슐은 완벽한 구의 형태로 평균 $2{\sim}10{\mu}m$ 크기를 보였으며, 교반속도와 유화제의 농도에 따른 캡슐의 직경 및 형태 변화를 관찰하였다. 마이크로캡슐의 방출실험을 하기 위하여 가교제, 키토산, 그리고 유화제의 양을 변화시키면서 방출 속도를 측정하였다. Riboflavin의 방출속도는 키토산의 가교 정도와 사용한 유화제의 양에 따라 크게 변하였다.

• 멤브레인
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• 제15권4호
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• pp.281-288
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• 2005

생체 적합성이 우수한 히아루론산과 생분해성이 우수한 폴리 락타이드의 이량체를 결합하여 약물 방출 시스템에 적용할 수 있는 생체 재료를 제조하고자 하였다. 냉동 건조법을 이용하여 히아루론산과 락타이드를 가교제 1-ethyl-3-(3-dimethyl aminopropyl) carbodiimide (EDC)로 가교시켰다. 생성된 막을 핵자기 공명 분광법으로 분석하여 락타이드 반응도와 EDC 반응도를 결정하였다. 히아루론산에 대한 락타이드 몰비, 가교제 농도가 증가할수록 혹은 가교 온도가 감소할수록, 락타이드 반응도가 증가하였으며 팽윤도는 감소하였다. 서로 다른 락타이드 반응도를 가진 막으로 약물 방출 실험을 수행한 결과 락타이드 반응도가 증가하면 약물 방출 속도가 감소하는 경향을 보였다. 또 친수성이 다른 여러 가지 약물로 약물 방출 실험을 수행한 결과 친수성이 우수한 약물일수록 서서히 방출되었다.

• Biomolecules & Therapeutics
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• 제13권4호
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• pp.251-255
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• 2005

In the present study, we tried to investigate whether protein kinase C (PKC) activator, phorbol 12-Myristate 13-Acetate (PMA), and PKC inhibitors, $G\"{o}-6976$, Ro-31-8220 and rottlerin significantly affect basal mucin relesed from cultured airway goblet cells. Confluent primary hamster tracheal surface epithelial (HTSE) cells were metabolically radiolabeled with $^3H$-glucosamine for 24 hr and chased for 30 min in the presence of each agent to assess the effects on $^3H$-mucin release. The results were as follows: (1) PMA increased mucin release from cultured HTSE cells, during 30 min of treatment period; (2) However, $G\"{o}-6976$, Ro-31-8220 and rottlerin did not significantly affect mucin release, during 30 min of treatment period. This finding suggests, at least in part, that PKC might playa minor role in the signaling pathways involved in basal - physiological or constitutive - mucin release from airway goblet cells, although further studies are needed.