Phase I study of new non-steroidal antiinflammatory drug, CS-670.

Matsuki, Shigeki; Sugimoto, Masanao; Kobayashi, Minae; Shibata, Hisao; Kawabata, Kiyoshi; Hoshiyama, Kazuko; Sasahara, Kunihiko

doi:10.2492/jsir1981.13.195

Cited by 3 publications

(2 citation statements)

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“…As one or two asymmetric centers are generated by this reduction, it has many stereoisomers. In particular, unsaturated-(M-B) and trans-alcohol (M-D) were found to be active metabolites in vitro studies of prostaglandin synthesis [8,9], which means that the active metabolites of pelubiprofen should be determined to estimate pharmacological effects. Several analytical methods have been reported for the determination of pelubiprofen and its metabolites.…”

Section: Introductionmentioning

confidence: 99%

Development and validation of an LC-MS/MS method for the determination of pelubiprofen and its active metabolite, trans-alcohol, in human plasma and its application to pharmacokinetic study

Ryu

Park

et al. 2015

Journal of Chromatography B

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Section: Introductionmentioning

confidence: 99%

Development and validation of an LC-MS/MS method for the determination of pelubiprofen and its active metabolite, trans-alcohol, in human plasma and its application to pharmacokinetic study

Ryu

Park

et al. 2015

Journal of Chromatography B

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“…In addition, PEL is metabolized rapidly to unsaturated-, cis-, and trans-alcohols after the intestinal absorption (Asami et al, 1996;Ryu et al, 2017). The plasma half-lives of PEL and its active metabolite (PEL-transOH) are 0.36 h and 1.5 h, respectively (Matsuki et al, 1993). Therefore, the frequent dosing of PEL is required to maintain the adequate plasma levels.…”

Section: Introductionmentioning

confidence: 99%

Sustained-release solid dispersion of pelubiprofen using the blended mixture of aminoclay and pH independent polymers: preparation and in vitro/in vivo characterization

et al. 2017

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The present study aimed to develop the sustained-release oral dosage form of pelubiprofen (PEL) by using the blended mixture of 3-aminopropyl functionalized-magnesium phyllosilicate (aminoclay) and pH-independent polymers. The sustained-release solid dispersion (SRSD) was prepared by the solvent evaporation method and the optimal composition of SRSD was determined as the weight ratio of drug: EudragitV R RL PO: EudragitV R RS PO of 1:1:2 in the presence of 1% of aminoclay (SRSD(F6)). The dissolution profiles of SRSD(F6) were examined at different pHs and in the simulated intestinal fluids. The drug release from SRSD(F6) was limited at pH 1.2 and gradually increased at pH 6.8, resulting in the best fit to Higuchi equation. The sustained drug release from SRSD(F6) was also maintained in simulated intestinal fluid at fasted-state (FaSSIF) and fed-state (FeSSIF). The structural characteristics of SRSD(F6) were examined by using powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FT-IR), indicating the change of drug crystallinity to an amorphous form. After oral administration in rats, SRSD(F6) exhibited the prolonged drug exposure in plasma. For both PEL and PEL-transOH (active metabolite), once a day dosing of SRSD(F6) achieved oral exposure (AUC) comparable to those from the multiple dosing (3 times a day) of untreated drug. In addition, the in vivo absorption of SRSD(F6) was well-correlated with the in vitro dissolution data, establishing a good level A in vitro/in vivo correlation. These results suggest that SRSD(F6) should be promising for the sustained-release of PEL, thereby reducing the dosing frequency.ARTICLE HISTORY

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