• Biomolecules & Therapeutics
• /
• 제7권2호
• /
• pp.198-203
• /
• 1999

Loxoprofen-Na (sodium 2-〔4-(2-oxocyclopentylmethyl)pheny)propionate dihydrate) is a potent analgesic drug. We developed loxoprofen-Na plasters to extend duration time of analgesic activity and to reduce side effect on gastrointestinal tract. Analgesic effect of Loxoprofen-Na plasters was investigated. Loxoprofen-Na plaster had good analgesic effect in rat paw pressure test, Tail-flick latency test and acetic acid-induced writhing test. Also, it had anti-inflammatory effect on carrageenan-induced rat hind paw edema. In pharmacokinetic study of Loxoprofen-Na, plasters dosage form showed that plasma drug concentration was prolonged up to 14 hours. So, we can conclude that loxoprofen-Na plasters, when applied on skin, will be a new type of drug for controlling the various local pain or inflammation.

• Biomolecules & Therapeutics
• /
• 제6권4호
• /
• pp.417-422
• /
• 1998

Loxoprofen sodium (sodium 2-[4-(2-oxocyclopentylmethyl)phenyl] propionate dehydrate) is a nonsteroidal antiinflammatory drug of $\alpha$-phenyl propionic acid derivative. To test the bioequivalence of loxoprofen, the pharmacokinetic parameters of new preparation of loxoprofen, LENOX was compared with LOXONIN as a reference drug. Fourteen healthy volunteers were entered to the stydy (Yonsei University College of Medicine, Severance Hospital IRB approval No. 9608). They were administered 60 mg of loxoprofen in 2$\times$2 cross-over design. There was one week of drug-free interval between doses. The blood sample was taken on schedule up to 8 hours, and the plasma concentration loxoprofen was measured by reverse phase high-performance liquid chromatography (HPLC) with UV-detector. There were no significant difference between two preparations when AUC, Cmax, and Tmax were compared by ANOVA. The mean differences of AUC, Cmax, and Tmax were within 20% of the reference drug: the values were 2.22,5.61, and 12.50%, respectively. The confidence limits of AUC and Cmax but not Tmax satisfied the bioequivalence criteria. These results suggest that the tested LENOX is bioequivalent to the reference drug.

• KSBB Journal
• /
• 제21권5호
• /
• pp.371-375
• /
• 2006

본 실험의 목적은 frontal analysis(FA)와 pluse input method(PIM) 방법으로 흡착분리공정에 있어서 중요한 전 단계의 하나인 등온흡착식을 결정하는데 있다. FA를 수행하기에 앞서 대상물질이었던 loxoprofen의 용해도를 측정하여 hexane/ethanol=95/5일 때 시료의 농도를 $0.2{\sim}3mg/ml$로 결정하고, pH조정을 위한 acetic acid는 0.5%로 결정하였다. 이동상의 주성분인 hexane의 조성이 증가함에 따라 용해도는 감소하였지만 분리도는 증가하는 경향을 확인하였다. 이런 용해도와 분리도 사이의 trade-off 또한 흡착분리과정에서의 조작변수가 될 수 있음을 의미한다. FA로 구한 이성분계 등온흡착식은 $$C_{S,re}=\frac{5.282C_{M,re}}{1+0.1412C_{M,re}+0.2139C_{M,ex}}$$, $$C_{S,ex}=\frac{6.413C_{M,ex}}{1+0.2139C_{M,ex}+0.1412C_{M,re}}$$로 결정하였고, PIM으로 구한 이성분계 등온흡착식은 $$C_{S,re}=\frac{5.245C_{M,re}}{1+0.1667C_{M,re}+0.2054C_{M,ex}}$$, $$C_{S,ex}=\frac{6.061C_{M,ex}}{1+0.2054C_{M,ex}+0.1667C_{M,re}}$$로 결정 하였다.

• Journal of Pharmaceutical Investigation
• /
• 제31권4호
• /
• pp.217-224
• /
• 2001

To develop a novel transdermal delivery system of loxoprofen (LP), a potent antiinflammatory and analgesic agent, the effects of various vehicles and penetration enhancers on the skin permeation of LP from solution formulations were investigated. The permeation rate of LP through excised guinea pig skin was measured using a side-by-side permeation system at $32^{\circ}C$. The solubilities of LP in various vehicles were determined by the equilibrium solubility method, and partition coefficients $(P_c)$ were determined. The solubility of LP increased in the rank order of water & isopropyl myristate (IPM) & glyceryl dicaprylate/dicaprate & propylene glycol dicaprylate/caprate & propylene glycol laurate (PGL) & polyethylene glycol 400 & diethylene glycol monoethyl ether (DGME) & ethanol. n-Octanol-water $P_c$ value was 15.5. Among pure vehicles tested, IPM and PGL showed highest fluxes of $89.9{\pm}5.0$ and $45.4{\pm}0.3\;{\mu}g/cm^2/hr$ from saturated solutions, respectively. However, it was not possible to demonstrate any correlation between the solubility of LP and its permeation rate, indicating the change in the barrier property of the skin and/or carrier mechanisms by vehicles tested. The addition of DGME to IPM or PGL markedly increased the solubility of LP, but the permeation rate did not decrease when the concentration of DGME in the cosolvent was increased upto 40%. The addition of linoleic acid (3%) in the cosolvent slightly increased the permeation rate, but others such as lauroyl sarcosine, fatty alcohols and fatty acids tested did not show enhancing effect. In conclusion, the DGME-IPM or DGME-PGL cosolvent system proved to be a good vehicle to enhance the skin permeation of LP.

• Korean Chemical Engineering Research
• /
• 제55권5호
• /
• pp.600-608
• /
• 2017

산업현장에서 취급되거나 가공되는 원료의약품 분진의 폭발 위험성은 항상 존재하며, 이로 인한 폭발사고가 자주 발생되고 있다. 본 연구에서는 원료의약품 시료 3종의 분진폭발특성을 측정하였다. 주요 폭발특성 측정값은 록소프로펜산은 평균 입경이 $5.31{\mu}m$이며, $P_{max}$는 8.4 bar, 최소점화에너지는 1 mJ < MIE < 3 mJ이며 최소점화온도는 $550^{\circ}C$이다. 클로피도그렐 캄포르술폰산염은 평균 입경이 $95.63{\mu}m$이며, $P_{max}$는 7.9 bar, 최소점화에너지는 30 mJ < MIE < 100 mJ이며 최소점화온도는 $510^{\circ}C$이었다. 리팜피신은 평균 입경이 $26.48{\mu}m$이며 $P_{max}$는 7.9 bar, 최소점화에너지는 1 mJ < MIE < 3 mJ이며 최소점화온도는 $470^{\circ}C$로 나타났다. 이들 값을 적용하여 폭연지수($K_{st}$)와 폭발지수(EI)의 폭발위험등급을 구하고, 원료의약품 분진의 폭발 위험성을 비교 검토하였다. 그 결과 폭발 위험성은 록소프로펜산과 리팜피신의 폭발등급은 St 2이고 폭발위험등급은 severe이며, 클로피도그렐 캄포르술폰산염의 폭발등급은 St 1이고 폭발위험등급은 strong으로 나타났다.