• Journal of Pharmaceutical Investigation
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• 제27권1호
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• pp.11-14
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• 1997

This laboratory has recently reported the solubility and in vivo absorption enhancement of diclofenac sodium by ${\beta}-cyclodextrin$ complexation. The acute gastroduodenal mucosa injury provoked by administration of 34 mg/kg and 68 mg/kg of a diclofenac sodium (DS) and equivalent dose of new formulation [diclofenac sodium-beta-cyclodextrin complexation$(DS-{\beta}-CD)$] was evaluated and compared. Microscopic examinations, performed after 18-hrs treatment, demonstrated that $DS-{\beta}-CD$ was less gastrolesive than DS. The drop in gastrophy after a single dose of the assigned drug was considerably greater for DS than for $DS-{\beta}-CD$, which registered similar values to control. Since gastrophy is an expression of the anatomy-functional integrity of the gastric barrier, the results indicate that $DS-{\beta}-CD$ exerts less direct acute damage on the gastric mucosa. Therefore, when administered short-term, $DS-{\beta}-CD$ appears to be less gastrolesive than the standard DS formulation.

• 대한임상독성학회지
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• 제9권2호
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• pp.101-104
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• 2011

Nicolau syndrome is a rare adverse reaction at the site of an intramuscular injection, and is characterized by severe pain immediately after the injection and rapid development of distinct skin lesions. As this syndrome is rare, it may be overlooked at the early clinical phase and subsequently, clinical outcomes may be worse due to delay in treatment. We report on a female who developed Nicolau syndrome following intramuscular diclofenac injection, which required surgical reconstruction. Understanding the characteristics of Nicolau syndrome and careful surveillance for relevant clinical features may help physicians to more quickly diagnose and treat this condition.

• Journal of Pharmaceutical Investigation
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• 제31권2호
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• pp.95-100
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• 2001

Various alkyl ester prodrugs of diclofenac were synthesized in order to investigate the relationship between their skin permeation characteristics and physicochemical properties. Solubility in various vehicles was measured at room temperature. 1-Octanol/water partition coefficients (Log P) and capacity factors (k') were measured to determine the lipophilicity of the prodrugs. Stability of prodrugs in the skin extract and homogenate was also investigated before conducting the skin permeation studies. Increases in the Log P and capacity factor values were observed when alkyl esters of diclofenac were prepared. Since the aqueous solubility of the prodrugs was not high enough, they were saturated in propylene glycol (PG) for skin permeation studies. Prodrugs were rapidly metabolized to diclofenac, both in skin homogenate and in dermal extract of skin. The skin permeation rate of alkyl ester prodrugs was significantly higher than diclofenac with shorter lag time. Moreover, a parabolic relationship was observed between the permeation rate and the log P values of prodrugs, and the maximum flux was achieved at a log P value of around 4.0.

• Journal of Pharmaceutical Investigation
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• 제34권2호
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• pp.91-94
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• 2004

To develop a poloxamer-based solid suppository with poloxamer mixtures, the melting points of various formulations composed of P 124 and P 188 were investigated. To investigate the effect of poloxamer to the dissolution ad dissolution mechanism of diclofenac sodium from the suppository the dissolution of diclofenac sodium delivered by the poloxamer-based suppository was performed. Furthermore, to investigate the mucoadhesive property of the poloxamer-based sold suppository, the identification test in the rectum was carried out after its rectal administration in rats. The poloxamer mixtures composed of P 124 and P 188 were homogeneous. Ver small amounts of P 188 affected the melting points of poloxamer mixtures. In particular, the poloxamer mixture [P 124/P 188 (97/3%)] with the melting point of about $32^{\circ}C$ was a sold for at room temperature and instantly melted at physiological temperature. Furthermore, very small amounts of P 188 in the poloxamer-based suppository hardly affected the dissolution rates of diclofenac sodium from the suppository. Dissolution mechanism analysis showed the dissolution of diclofenac sodium was proportional to the time. At 4 h after administration, the blue colo of poloxamer-based suppository [diclofenac sodium/poloxamer mixture (2.5/97.5%)] with the P 124/ P 188 ratio of (97/3%) and blue lake in the rectum was faded. However, the position of suppository in the rectum did not significantly change with time. Thus, it retained in thε rectum for at least 4 h. Our results indicated that the poloxamer-based sold suppository with P 124 and P 188 would be a candidate of rectal dosage form for diclofenac sodium.

• 한국임상수의학회지
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• 제27권4호
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• pp.315-324
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• 2010

본 실험은 Aureobasidium pullulans SM-2001 유래 베타글루칸의 콜라겐 유발 류마티스 관절염에서의 효과를 알아보고자 하였다. 6 주령 DBA/1J 수컷 마우스를 1주일간 적응기간을 거친 후 콜라겐 200 ug를 프로인트 완전면역 보강제와 함께 꼬리부위 피내에 접종하였으며, 21일 후에 콜라겐을 프로인트 불완전면역보강제와 함께 추가접종을 하였다. 베타글루칸 (체중당 21.25, 42.5, 85 mg/kg), 디클로페낙 (체중당 2 mg/kg)을 첫 접종일부터 추가접종 후 1주일간 투여하였다. 관절염 유발군에서는 과증식된 비장(증가된 백색속질)과 연골손상의 증가가 관찰되었다. 이러한 증상은 폴리칸 21.25 mg/kg 투여군의 일부 항목(경골, 연골)을 제외한 모든 폴리칸 투여군에서 용량의존적으로 유의한 효과를 나타내었다. 아우레오바시디움 플루란스 유래 베타글루칸이 콜라겐으로 유발된 류마티스관절염과 과면역을 효과적으로 억제하는 것을 알 수 있었다.

• 대한환경공학회지
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• 제31권10호
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• pp.831-838
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• 2009

본 연구에서는 염소, 오존 및 오존/과산화수소 산화공정에서의 의약물질 3종의 제거특성을 살펴본 결과 diclofenac과 naproxen은 쉽게 산화공정에서 제거가 가능한 것으로 나타난 반면 ibuprofen의 경우는 산화공정에서 제거가 어려운 것으로 나타났다. 오존 단독공정 보다는 오존/과산화수소 산화공정에서의 의약물질의 제거효율이 높았으며, $H_2O_2/O_3$ 비가 1 이상에서는 제거율의 상승이 둔화되었다. 염소, 오존 및 오존/과산화수소 투입농도별 의약물질 3종에 대한 산화분해 속도 상수와 반감기를 살펴본 결과 염소, 오존 단독 투입에 비하여 오존/과산화수소 공정에서의 산화분해 속도상수가 높게 나타났고, 반감기는 단축되었다.

• 분석과학
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• 제21권3호
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• pp.191-200
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• 2008

의약물질(PPCPs)은 수질 환경 시료에서 새로운 오염물질로 대두되고 있다. 본 연구에서는 LC/ESI-MS/MS를 이용하여 환경 수질 시료로부터 7 종(2-퀴노사린카르복시산, 아세틸살리실산, 디클로페낙-소듐, 나프록센, 이부프로펜, 메페남산, 탈니플루메이트)의 산성의약물질을 동시 분석하는 방법을 비교하여 개선하였으며 폐수처리장의 유입수 및 방류수 그리고 연장선상의 하천수의 오염도를 측정하였다. LC/ESI-MS/MS 분석을 위해서 MCX (Mixed Cation eXchange) 카트리지와 HLB (Hydrophilic-Lipophilic Balance) 카트리지를 연결하는 텐뎀 고체상 추출법과 MCX 카트리지만을 사용하는 고체상 추출법을 이용하여 효과적인 시료 정제 및 추출을 수행하였다. 검출한계(LODs)와 방법검출한계(MDLs)는 각각 0.05~1.50 pg/mL, 0.17~4.90 pg/mL 범위를나타내었다. 시료중 1.0 ng/mL 농도(n=3)에서절대회수율은 81.9%~116.3%를 나타내었다. 수질 환경 시료에서 수 pg/mL~ng/mL의 농도로 산성의약물질이 측정되었다.