(R)-Naproxen acyl-b-D-glucuronide - CAS 112828-15-6
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(R)-Naproxen acyl-b-D-glucuronide
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CAS 112828-15-6 (R)-Naproxen acyl-b-D-glucuronide

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Reference Reading

1.Novel organogels for topical delivery of naproxen: design, physicochemical characteristics and in vitro drug permeation.
Osmałek T1, Milanowski B1, Froelich A1, Górska S1, Białas W2, Szybowicz M3, Kapela M1. Pharm Dev Technol. 2016 Jan 20:1-16. [Epub ahead of print]
Taking into account possible irritation of the skin upon contact with naproxen (NPX) crystals and lower bioavailability after administration of the suspended or ionized drug, the aim of the work was to design and characterize novel and easy-to-formulate gels with the entirely dissolved drug in the acidic form. The formulations contained ethanol, SynperonicTMPE/L 62 and Arlasolve® DMI or Transcutol®. Carbopol®940 was used as the thickener. The properties of organogels were compared with six market products. The rheological measurements included steady flow experiments and oscillatory analysis. The texture profile analysis was conducted to calculate the mechanistic parameters. The in vitro permeation studies were performed on SOTAX CE 7 smart apparatus with the application of Strat-M artificial membranes. The obtained organogels fulfilled the requirements for topical products in terms of consistency, uniformity, stability, drug dissolution and permeation.
2.Pharmacokinetic Parameters Determination and In Vitro-In Vivo Correlation of Ileocolonic-Targeted pH-Responsive Coated Mini-Tablets of Naproxen.
Hadi MA1, Raghavendra Rao NG2, Srinivasa Rao A3. Sci Pharm. 2015 Jun 2;83(4):645-58. doi: 10.3797/scipharm.1503-16. eCollection 2015.
This research work aims to determine the pharmacokinetic parameters and in vitro-in vivo correlation of the selected ileocolonic-targeted coated mini-tablet filled capsule formulation of naproxen. The pure suspension and coated mini-tablet filled capsule formulation of naproxen were administered to adult albino rabbits through the oral route. The samples were analyzed for naproxen by an HPLC method. For the pure drug suspension, the peak plasma concentration was found as 8.499±0.029 μg/ml at 1.139±0.010 hours and the half-life was found to be 9.459±0.387 hours, whereas for the formulation the peak plasma concentration was found as 6.814±0.037 μg/ml at 8.042±0.069 hours and the half-life was found to be 19.657±0.359 hours. This decreased the peak plasma concentration at a delayed time and increased the half-life of the capsule formulation in comparison with the pure drug suspension which showed that naproxen was only targeted to the ileocolonic region.
3.Fixed Drug Eruption Due to Selective Hypersensitivity to Naproxen with Tolerance to other Propionic Acid NSAIDs.
Noguerado-Mellado B1, Rodriguez Gamboa A, Rojas Perez-Ezquerra P, Morales Cabeza C, Pelta Fernandez R, De Barrio Fernandez M. Recent Pat Inflamm Allergy Drug Discov. 2016 Apr 4. [Epub ahead of print]
BACKGROUND: Naproxen is a non-steroidal anti-inflammatory drug (NSAID), belonging to propionic acid group, and its chemical structure is a 6-metoxi-metil-2-naftalenoacetic acid. Fixed drug eruptions (FDE) have been rarely reported.
4.Impact of chirality on the photoinduced charge transfer in linked systems containing naproxen enantiomers.
Khramtsova EA1, Sosnovsky DV1, Ageeva AA1, Nuin E2, Marin ML2, Purtov PA1, Borisevich SS3, Khursan SL3, Roth HD4, Miranda MA2, Plyusnin VF1, Leshina TV5. Phys Chem Chem Phys. 2016 Apr 21. [Epub ahead of print]
The model reaction of photoinduced donor-acceptor interaction in linked systems (dyads) has been used to study the comparative reactivity of a well-known anti-inflammatory drug, (S)-naproxen (NPX) and its (R)-isomer. (R)- or (S)-NPX in these dyads is linked to (S)-N-methylpyrrolidine (Pyr) using a linear or cyclic amino acid bridge (AA or CyAA), to give (R)-/(S)-NPX-AA-(S)-Pyr flexible and (R)-/(S)-NPX-CyAA-(S)-Pyr rigid dyads. The donor-acceptor interaction is reminiscent of the binding (partial charge transfer, CT) and electron transfer (ET) processes involved in the extensively studied inhibition of the cyclooxygenase enzymes (COXs) by the NPX enantiomers. Besides that, both optical isomers undergo oxidative metabolism by enzymes from the P450 family, which also includes ET. The scheme proposed for the excitation quenching of the (R)- and (S)-NPX excited state in these dyads is based on the joint analysis of the chemically induced dynamic nuclear polarization (CIDNP) and fluorescence data.