CAS Number: 145202-66-0

Maxalt / Rizatriptan benzoate | 145202-66-0

Rizatriptan benzoate is a selective serotonin 5-HT1B/1D receptor agonist used for the acute treatment of migraine headaches, but its oral tablet form (Maxalt) has limitations including slow absorption (Tmax of 1–1.5 hours), low oral bioavailability (approximately 45% due to first-pass metabolism), and delayed onset of action of at least 30 minutes, which is problematic for patients experiencing severe pain, nausea, or gastrointestinal disturbances. To overcome these issues, researchers have developed alternative delivery systems: inhalable microparticles prepared by spray freeze-drying using sugars (mannitol or trehalose) and amino acids (leucine, phenylalanine, or serine) have shown excellent aerosolization performance with fine particle fractions up to 61.1%, particularly using trehalose and phenylalanine; intranasal spray formulations using co-solvent systems (ethanol, water, propylene glycol, polyethylene glycol) achieved rapid absorption in beagle dogs with Cmax reaching 312 ng/mL within 5 minutes; and solid lipid nanoparticles for nasal administration demonstrated superior pharmacokinetics in rats (Cmax 473.56 ng/mL, Tmax 1 hour) compared to oral and intravenous routes. Additionally, analytical methods such as electrochemical sensors using Fe3O4/multiwall carbon nanotube-modified glassy carbon electrodes have been developed for sensitive determination of rizatriptan benzoate in pharmaceutical and serum samples, while kinetic studies have explored the catalytic oxidation of rizatriptan to rizatriptan-N-oxide.

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References

  • An electrochemical sensor for rizatriptan benzoate determination using Fe3O4 nanoparticle/multiwall carbon nanotube-modified glassy carbon electrode in real samples
    In this paper, a sensitive electrochemical sensor based on Fe3O4 nanoparticle/multiwall carbon nanotube modified glassy carbon electrode was constructed and successfully applied in the detection of RZB. The modified GCE displayed substantially higher electrocatalytic activity to RZB oxidation than MWCNTs/GCE, Fe3O4/GCE and bare GCE. The modified electrode showed a low detection limit, wide linear concentration range, high stability, good reproducibility and fast response in detecting RZB concentrations. Moreover, the obtained results from the application of the proposed method for determination of RZB in real samples confirm the good reliability and accuracy of our proposed method.
    DOI: 10.1016/j.msec.2016.03.041
  • Sensitive and selective methods for the determination of rizatriptan benzoate in pharmaceuticals using N-bromosuccinimide and two dyes
    One titrimetric and two spectrophotometric methods were developed and validated for the determination of rizatriptan benzoate using NBS as brominating agent. The new approach of utilizing NBS and calmagite as reagents in spectrophotometry is the first of such reports. Method B is the most sensitive among the proposed methods. The proposed spectrophotometric methods have two additional advantages of simplicity of operations and low-cost instrument. All the methods make use of very easily available and cheaper reagents which demonstrates their cost-effectiveness and the procedures do not involve any tedious sample preparation. The assay methods involve less stringent control of experimental parameters such as the stability of the colored species, time of analysis and temperature independence. These advantages encourage the application of the proposed methods in routine quality control analysis of rizatriptan benzoate in pharmaceutical formulations.
    DOI: 10.1016/j.jscs.2012.02.003
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