Lobenzarit disodium - CAS 64808-48-6
Catalog number: B0084-074412
Category: Inhibitor
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Lobenzarit disodium is an immunomodulator commonly used for the treatment of arthritis.
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Catalog Number Size Price Stock Quantity
B0084-074412 100 mg $299 In stock
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Related CAS:
63329-53-3 (free acid)
Lobenzarit sodium; Lobenzarit disodium salt; Disodium 4-chloro-2,2'-iminobenzoate; disodium 2-(2-carboxylatoanilino)-4-chlorobenzoate
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1.Application of a new mathematical method for the estimation of the mean surface area to calculate the percolation threshold of lobenzarit disodium [correction of dissodium] salt in controlled release matrices.
Boza A1, Blanquero R, Millan M, Caraballo I. Chem Pharm Bull (Tokyo). 2004 Jul;52(7):797-801.
One of the practical handicaps for the application of the percolation theory to estimate the percolation threshold of drugs in controlled release systems is the fact that the dissolution studies must be carried out so that only one surface of the tablet is exposed to the dissolution medium. The aim of this work is to estimate the percolation threshold of the antiarthritic drug lobenzarit dissodium (LBD) in inert matrices prepared with the excipients Ethocel((R)) 100 and Eudragit((R)) RS-PO (10-75% w/w). Release assays were performed using the paddle method. The whole surface of the tablets was exposed to the dissolution medium. For the first time, a new mathematical method is developed to transform the amount of drug released in amount released per surface area in order to calculate the percolation thershold of LBD. The mathematical method proposed allows to calculate, using a new equation, the evolution of the mean surface area (O((t))).
2.Identifying mechanism-of-action targets for drugs and probes.
Gregori-Puigjané E1, Setola V, Hert J, Crews BA, Irwin JJ, Lounkine E, Marnett L, Roth BL, Shoichet BK. Proc Natl Acad Sci U S A. 2012 Jul 10;109(28):11178-83. doi: 10.1073/pnas.1204524109. Epub 2012 Jun 18.
Notwithstanding their key roles in therapy and as biological probes, 7% of approved drugs are purported to have no known primary target, and up to 18% lack a well-defined mechanism of action. Using a chemoinformatics approach, we sought to "de-orphanize" drugs that lack primary targets. Surprisingly, targets could be easily predicted for many: Whereas these targets were not known to us nor to the common databases, most could be confirmed by literature search, leaving only 13 Food and Drug Administration-approved drugs with unknown targets; the number of drugs without molecular targets likely is far fewer than reported. The number of worldwide drugs without reasonable molecular targets similarly dropped, from 352 (25%) to 44 (4%). Nevertheless, there remained at least seven drugs for which reasonable mechanism-of-action targets were unknown but could be predicted, including the antitussives clemastine, cloperastine, and nepinalone; the antiemetic benzquinamide; the muscle relaxant cyclobenzaprine; the analgesic nefopam; and the immunomodulator lobenzarit.
3.Investigation of the influence of particle size on the excipient percolation thresholds of HPMC hydrophilic matrix tablets.
Miranda A1, Millán M, Caraballo I. J Pharm Sci. 2007 Oct;96(10):2746-56.
In previous papers of our research group, a linear relationship between the drug percolation threshold and the relative drug particle size (drug/excipient) has been found, in the case of the inert matrices. The objective of the present paper is to investigate the influence of the particle size on the excipient percolation threshold in the case of hydrophilic matrices. This influence can have important consequences on the release behaviour of these controlled release devices. Matrix tablets have been prepared using KCl/Lobenzarit Disodium as drugs and HPMC K4M as matrix forming material, employing six different excipient/drug particle size ratios (ranging from 0.42 to 4.16). The formulations studied contain a drug loading in the range of 20-90% (w/w). In order to estimate the percolation threshold, the behaviour of the kinetic parameters with respect to the volumetric fraction of each component at time zero, was studied. The obtained results support the existence of a linear relationship between a component percolation threshold (drug or excipient) and its relative particle size (drug/excipient in the case of the drug percolation threshold or excipient/drug in the case of the excipient percolation threshold).
4.Estimation of the percolation thresholds in ternary lobenzarit disodium-dextran-HPMC hydrophilic matrices tablets: effects of initial porosity.
Castellanos Gil E1, Iraizoz Colarte A, Bataille B, Brouillet F, Caraballo I. Eur J Pharm Sci. 2009 Nov 5;38(4):312-9. doi: 10.1016/j.ejps.2009.07.013. Epub 2009 Aug 8.
The aim of this work is to estimate the excipient percolation threshold for a new combined matrix native dextran (DT), series B110-1-2 (Mw 2 x 10(6)): HPMC K4M CR: lobenzarit disodium (LBD) system and demonstrate the advantages of this ternary system with respect to previously reported binary dextran:LBD and HPMC:LBD tablets. The formulations studied were prepared with different amounts of excipient (DT:HPMC, 4:1 (wt/wt) for all tablets and relative polymer/drug particle size of 4.17) in the range of 10-70% (wt/wt). Dissolution studies were carried out using the paddle method (100 rpm) and one face water uptake measurements were performed using a modified Enslin apparatus. The Higuchi's models as well as the non-linear regression were employed as empiric methods to study the released data. Values of diffusion exponent 0.588<n<0.784 (Korsmeyer equation) for dissolution profile and water uptake mechanism 0.715<n<0.960 (Davidson and Peppas equation) suggests anomalous or complex mechanisms in all cases.
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CAS 64808-48-6 Lobenzarit disodium

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