• Biomolecules & Therapeutics
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• v.7 no.2
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• pp.198-203
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• 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
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• v.6 no.4
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• pp.417-422
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• 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
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• v.21 no.5
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• pp.371-375
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• 2006

Frontal analysis(FA) and Pulsed input method(PIM) have been frequently utilized to measure isotherm of single solute, as well as non-competitive isotherms of two solutes in chromatography(1). FA and PIM were used in this study as complementary methods to measure adsorption isotherms of loxoprofen racemate in HPLC. Prior to FA and PIM experiments, measurements of loxoprofen solubility were made at hexane/ethanol=50/50, 80/20, 95/5(v/v) with acetic acid(0.5%) for adjusting pH. The last composition(95/5) of hexane/ethanol allows us to separate loxoprofen racemate into two forms(retentate, extract). PIM and FA were used to determine the isotherms of re-and ex-loxoprofen.

• Journal of Pharmaceutical Investigation
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• v.31 no.4
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• pp.217-224
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• 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
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• v.55 no.5
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• pp.600-608
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• 2017

Hazard risk of explosion on pharmaceutical raw materials dust in pharmaceutical industry often exists when it is handled or processed in the industrial sites, and explosion accident is caused by this. In this study, the dust explosion characteristics of the three pharmaceutical raw materials samples were measured. The main explosion characteristics are as follows: $P_{max}$, MIE and MIT of loxoprofen acid having $5.31^{\circ}C$ of median diameter are obtained 8.4 bar, 1 mJ < MIE < 3 mJ and $550^{\circ}C$. $P_{max}$, MIE and MIT of camphorsulfonate having $95.63^{\circ}C$ of median diameter are obtained 7.9 bar, 30 mJ < MIE < 100 mJ and $510^{\circ}C$. $P_{max}$, MIE and MIT of rifampicine having $26.48^{\circ}C$ of median diameter are obtained 7.9 bar and 1 mJ < MIE < 3 mJ and $470^{\circ}C$. The deflagration index ($K_{st}$) and the explosion index (EI) were obtained by using these data. The explosion hazard assessment of pharmaceutical raw materials dust was compared and examined. As a result, the explosion hazard assessment according to deflagration index and explosion index were the explosion class with St 2 and the explosion hazard rating of severe for loxoprofen acid & rifampicine and St 1 and strong for clopidogrel camphorsulfonate, respectively.