Delving into the Latest Updates on Lobuprofen with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

ICJ 2280A, ICJ-2280A

Target

COXs

Action

inhibitors

Mechanism

COX inhibitors(Cyclooxygenases inhibitors)

Therapeutic Areas

Nervous System DiseasesOther Diseases

Active Indication-

Inactive Indication

Pain

Originator Organization

Juste SA Quimico Farmaceutica

Active Organization-

Inactive Organization

Juste SA Quimico Farmaceutica

License Organization-

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC25H33ClN2O2

InChIKeyJFGXBHHLHQAGRR-UHFFFAOYSA-N

CAS Registry98207-12-6

The pharmacokinetics of lobuprofen (I) following a single administration of i.v. or oral dose of 13 mg/kg of dual labeled (³H/¹⁴C)-lobuprofen in rats were studied.Lobuprofen, like other ester-type analgesics, is hydrolyzed in vivo yielding the acid (ibuprofen) and alc. (II) metabolites.The time level course of both hydrolysis products was simultaneously studied.Plasma level data were fitted to a 2-compartment open model, and the main pharmacokinetic parameters were calculatedUrinary and fecal excretion were monitored over a period of 168 h.[³H]ibuprofen was mainly excreted in the urine, feces being the the main excretion route for II.

Revista de Farmacologia Clinica y Experimental

Pharmacokinetics of ibuprofen following oral administration of single-dose lobuprofen in healthy volunteers

Author: Montes-Jovellar, B. ; Fos, D. ; Honorato Perez, J. ; Martin Martin, F. ; Suarez, J. ; Alamo, C.

The pharmacokinetics of ibuprofen was studied in healthy humans given single doses of 2, 4, or 8 mg/kg of the parent ester drug lobuprofen (I).Blood plasma levels of ibuprofen were determined by HPLC.At the 2 higher doses the pharmacokinetic parameters indicated a second compartment in some subjects, which would explain the lack of AUC linearity and increased mean residence time and elimination half-life.I had no adverse side-effects on clin. status and blood or urine indexes.

100 Deals associated with Lobuprofen

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