Felbinac Trometamol

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 527501

CAS#: 935886-64-9

Description: Felbinac Trometamol is an intravenous formulation for the treatment of severe post-operative pain. The maximum plasma concentration (C(0)) and area under the plasma concentration-time curve (AUC) of felbinac administered at doses of 3.36, 8.40 and 21.0 mg/kg felbinac trometamol increased linearly with dose. Felbinac was highly protein bound (~95%) at plasma concentrations up to 75 μg/ml and extensively metabolized with only small amounts being excreted unchanged in urine (0.318%), feces (0.530%) and bile (0.465%).


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Felbinac Trometamol is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 527501
Name: Felbinac Trometamol
CAS#: 935886-64-9
Chemical Formula: C18H23NO5
Exact Mass:
Molecular Weight: 333.384
Elemental Analysis: C, 64.85; H, 6.95; N, 4.20; O, 23.99


Related CAS #: 935886-64-9 (trometamol); 5728-52-9 (free base)  

Synonym: Felbinac Trometamol; Felbinac; L 141; L141; L-141

IUPAC/Chemical Name: 2-amino-2-(hydroxymethyl)propane-1,3-diol 2-([1,1'-biphenyl]-4-yl)acetate

InChi Key: SWKYVGAYFCGGRP-UHFFFAOYSA-N

InChi Code: InChI=1S/C14H12O2.C4H11NO3/c15-14(16)10-11-6-8-13(9-7-11)12-4-2-1-3-5-12;5-4(1-6,2-7)3-8/h1-9H,10H2,(H,15,16);6-8H,1-3,5H2

SMILES Code: O=C(O)CC1=CC=C(C2=CC=CC=C2)C=C1.OCC(CO)(N)CO


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


References

1: Zheng Y, Hu X, Liu J, Wu G, Zhai Y, Wu L, Shentu J. Qualitative and quantitative analysis of felbinac and its major metabolites in human plasma and urine by liquid chromatography tandem mass spectrometry and its application after intravenous administration of felbinac trometamol injection. J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Apr 1;986-987:60-8. doi: 10.1016/j.jchromb.2015.01.042. PubMed PMID: 25706568.

2: Ferrone V, Carlucci M, Palumbo P, Carlucci G. Bioanalytical method development for quantification of ulifloxacin, fenbufen and felbinac in rat plasma by solid-phase extraction (SPE) and HPLC with PDA detection. J Pharm Biomed Anal. 2016 May 10;123:205-12. doi: 10.1016/j.jpba.2016.01.062. PubMed PMID: 26898973.

3: Zhang C, Cui X, Yang Y, Gao F, Sun Y, Gu J, Fawcett JP, Yang W, Wang W. Pharmacokinetics of felbinac after intravenous administration of felbinac trometamol in rats. Xenobiotica. 2011 Apr;41(4):340-8. doi: 10.3109/00498254.2010.544422. PubMed PMID: 21182394.

4: Liu N, Song W, Song T, Fang L. Design and Evaluation of a Novel Felbinac Transdermal Patch: Combining Ion-Pair and Chemical Enhancer Strategy. AAPS PharmSciTech. 2016 Apr;17(2):262-71. doi: 10.1208/s12249-015-0342-9. PubMed PMID: 26070544; PubMed Central PMCID: PMC4984900.

5: Shinkai N, Korenaga K, Takizawa H, Mizu H, Yamauchi H. Percutaneous penetration of felbinac after application of transdermal patches: relationship with pharmacological effects in rats. J Pharm Pharmacol. 2008 Jan;60(1):71-6. PubMed PMID: 18088507.

6: Zhang C, Wang L, Yang W, Wang X, Fawcett JP, Sun Y, Gu J. Validated LC-MS/MS assay for the determination of felbinac: Application to a preclinical pharmacokinetics study of felbinac trometamol injection in rat. J Pharm Biomed Anal. 2009 Aug 15;50(1):41-5. doi: 10.1016/j.jpba.2009.03.019. PubMed PMID: 19376665.

7: Kasuya F, Miwa Y, Kazumi M, Inoue H, Ohta H. Effect of enoxacin, felbinac, and sparfloxacin on fatty acid metabolism and glucose concentrations in rat tissues. Int J Toxicol. 2011 May;30(3):367-76. doi: 10.1177/1091581810397619. PubMed PMID: 21633127.

8: Takayama K, Hirose A, Suda I, Miyazaki A, Oguchi M, Onotogi M, Fotopoulos G. Comparison of the anti-inflammatory and analgesic effects in rats of diclofenac-sodium, felbinac and indomethacin patches. Int J Biomed Sci. 2011 Sep;7(3):222-9. PubMed PMID: 23675240; PubMed Central PMCID: PMC3614831.

9: Sakaguchi Y, Yoshida H, Hayama T, Yoshitake M, Itoyama M, Todoroki K, Yamaguchi M, Nohta H. Fluorous derivatization and fluorous-phase separation for fluorometric determination of naproxen and felbinac in human plasma. J Pharm Biomed Anal. 2011 Apr 28;55(1):176-80. doi: 10.1016/j.jpba.2011.01.011. PubMed PMID: 21310574.

10: Wada Y, Takaoka Y, Nozawa M, Goto M, Shimokawa KI, Ishii F. Generic selection criteria for safety and patient benefit [VI]: Comparing the physicochemical and pharmaceutical properties of brand-name, generic, and OTC felbinac tapes. Drug Discov Ther. 2017 Jan 15;10(6):300-306. doi: 10.5582/ddt.2016.01053. PubMed PMID: 27725574.

11: Van Eerdenbrugh B, Fanwick PE, Taylor LS. 2-(Biphenyl-4-yl)acetic acid (felbinac). Acta Crystallogr Sect E Struct Rep Online. 2010 Sep 25;66(Pt 10):o2609. doi: 10.1107/S1600536810035828. PubMed PMID: 21587585; PubMed Central PMCID: PMC2983253.

12: Ventura CA, Paolino D, Pedotti S, Pistarà V, Corsaro A, Puglisi G. Synthesis, characterization and in vitro evaluation of dimethyl-beta-cyclodextrin-4-biphenylylacetic acid conjugate. J Drug Target. 2003 May;11(4):233-40. PubMed PMID: 14578110.

13: Carlucci G, Mazzeo P, Palumbo G. Simultaneous determination of rufloxacin, fenbufen and felbinac in human plasma using high-performance liquid chromatography. J Chromatogr B Biomed Appl. 1996 Jul 12;682(2):315-9. PubMed PMID: 8844425.

14: Ohtani H, Noma S, Kawakami J, Sawada Y, Iga T. Lack of potentiation with felbinac patch on the convulsive toxicity of enoxacin in rats. Biol Pharm Bull. 1996 Jul;19(7):995-7. PubMed PMID: 8839976.

15: Kawakami J, Yamamoto K, Asanuma A, Yanagisawa K, Sawada Y, Iga T. Inhibitory effect of new quinolones on GABA(A) receptor-mediated response and its potentiation with felbinac in Xenopus oocytes injected with mouse-brain mRNA: correlation with convulsive potency in vivo. Toxicol Appl Pharmacol. 1997 Aug;145(2):246-54. PubMed PMID: 9266796.

16: Leeb B. [Topical felbinac in therapy of athletic injuries]. Fortschr Med. 1994 Feb 28;112(6):77-80. German. PubMed PMID: 8163257.

17: Minami K, Hirayama F, Uekama K. Colon-specific drug delivery based on a cyclodextrin prodrug: release behavior of biphenylylacetic acid from its cyclodextrin conjugates in rat intestinal tracts after oral administration. J Pharm Sci. 1998 Jun;87(6):715-20. PubMed PMID: 9607948.

18: Barkin RL. Topical Nonsteroidal Anti-Inflammatory Drugs: The Importance of Drug, Delivery, and Therapeutic Outcome. Am J Ther. 2015 Sep-Oct;22(5):388-407. doi: 10.1097/MJT.0b013e3182459abd. PubMed PMID: 22367354.

19: Hosie G, Bird H. The topical NSAID felbinac versus oral NSAIDS: a critical review. Eur J Rheumatol Inflamm. 1994;14(4):21-8. Review. PubMed PMID: 7601178.

20: Zang L, Morikane D, Shimada Y, Tanaka T, Nishimura N. A novel protocol for the oral administration of test chemicals to adult zebrafish. Zebrafish. 2011 Dec;8(4):203-10. doi: 10.1089/zeb.2011.0726. PubMed PMID: 22181663.