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Rizatriptan Benzoate

Potent 5-HT1B/1D agonist CAS# 145202-66-0

Rizatriptan Benzoate

2D Structure

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Rizatriptan Benzoate

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Chemical Properties of Rizatriptan Benzoate

Cas No. 145202-66-0 SDF Download SDF
PubChem ID 77997 Appearance Powder
Formula C22H25N5O2 M.Wt 391.47
Type of Compound N/A Storage Desiccate at -20°C
Synonyms MK 462
Solubility Soluble to 100 mM in water and to 50 mM in DMSO
Chemical Name benzoic acid;N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethanamine
SMILES CN(C)CCC1=CNC2=C1C=C(C=C2)CN3C=NC=N3.C1=CC=C(C=C1)C(=O)O
Standard InChIKey JPRXYLQNJJVCMZ-UHFFFAOYSA-N
Standard InChI InChI=1S/C15H19N5.C7H6O2/c1-19(2)6-5-13-8-17-15-4-3-12(7-14(13)15)9-20-11-16-10-18-20;8-7(9)6-4-2-1-3-5-6/h3-4,7-8,10-11,17H,5-6,9H2,1-2H3;1-5H,(H,8,9)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Rizatriptan Benzoate

Description5-HT1B/1D agonist. Antimigraine agent; attenuates effects of CGRP on light aversion in mice. Orally bioavailable.

Rizatriptan Benzoate Dilution Calculator

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Preparing Stock Solutions of Rizatriptan Benzoate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.5545 mL 12.7724 mL 25.5447 mL 51.0895 mL 63.8619 mL
5 mM 0.5109 mL 2.5545 mL 5.1089 mL 10.2179 mL 12.7724 mL
10 mM 0.2554 mL 1.2772 mL 2.5545 mL 5.1089 mL 6.3862 mL
50 mM 0.0511 mL 0.2554 mL 0.5109 mL 1.0218 mL 1.2772 mL
100 mM 0.0255 mL 0.1277 mL 0.2554 mL 0.5109 mL 0.6386 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Rizatriptan Benzoate

Rizatriptan Benzoate is a selective serotonin 5-HTID receptor agonist which is structurally derived from tryptamine.

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References on Rizatriptan Benzoate

Development and validation of UV spectrophotometric method to study stress degradation behaviour of rizatriptan benzoate.[Pubmed:25993836]

Guang Pu Xue Yu Guang Pu Fen Xi. 2015 Jan;35(1):137-40.

Rizatriptan Benzoate is a 5 HT 1B/1D receptor agonist which is prescribed for the treatment of migraine. In the present study new, simple, specific ultraviolet spectrophotometric method for Rizatriptan Benzoate was developed and validated. Forced degradation studies were carried out in acidic, alkaline and neutral pH conditions. The absorbance maxima peak was found to be 224 nm and linearity was observed in the concentration range of 0. 5-2. 5 microg . mL-1 with regression coefficient value of 0. 998 8. The method was validated and found to be precise. The percent recovery for Rizatriptan Benzoate was found to be 98. 576+/-0. 202. The bulk drug was found to be stable in neutral and acidic pH conditions but got degraded in 1 N NaOH solution.

Formulation of rizatriptan benzoate fast dissolving buccal films by emulsion evaporation technique.[Pubmed:25838995]

Int J Pharm Investig. 2015 Apr-Jun;5(2):101-6.

AIM: The present study deals with the formulation of fast dissolving films of Rizatriptan Benzoate that is used for the treatment of Migraine. The concept of fast-dissolving drug delivery emerged from the desire to provide patient with more conventional means of taking their medication. MATERIALS AND METHODS: In the present research work, various trials were carried out using film forming agents such as maltodextrin, gum karaya and xanthan gum to prepare an ideal film. Emulsion evaporation method was used for the preparation of films. The prepared films were evaluated for weight uniformity, drug content, film thickness, folding endurance, dispersion test and curling. The in vitro dissolution studies were carried out using simulated salivary fluid (pH 6.8 phosphate buffer). RESULTS: About 97% of the drug was found to be released from the film within 10 min that is a desirable character for fast absorption. The drug excipient interaction studies carried out by differential scanning calorimetry analysis and Fourier transform infrared studies revealed that there were no major interactions between the drugs and excipients used for the preparation of films. CONCLUSION: Fast dissolving films of Rizatriptan Benzoate prepared by emulsion evaporation technique were found to be suitable for eliciting better therapeutic effect in the treatment of migraine.

An electrochemical sensor for rizatriptan benzoate determination using Fe3O4 nanoparticle/multiwall carbon nanotube-modified glassy carbon electrode in real samples.[Pubmed:27040259]

Mater Sci Eng C Mater Biol Appl. 2016 Jun;63:637-43.

In this paper a sensitive and selective electrochemical sensor for determination of Rizatriptan Benzoate (RZB) was proposed. A glassy carbon electrode was modified with nanocomposite of multiwalled carbon nanotubes (MWCNTs) and Fe3O4 nanoparticles (Fe3O4/MWCNTs/GCE). The results obtained clearly show that the combination of MWCNTs and Fe3O4 nanoparticles definitely improves the sensitivity of modified electrode to RZB determination. The morphology and electroanalytical performance of the fabricated sensor were characterized by scanning electron microscopy (SEM), transmission electron microscopy (TEM), X-ray diffraction (XRD), energy dispersive X-ray spectroscopy (EDS), square wave voltammetry (SWV) and cyclic voltammetry (CV). Also, the effect of experimental and instrumental parameters on the sensor response was evaluated. The square wave voltammetric response of the electrode to RZB was linear in the range 0.5-100.0 mumol L(-1) with a detection limit of 0.09 mumol L(-1) under the optimum conditions. The investigated method showed good stability, reproducibility and repeatability. The proposed sensor was successfully applied for real life samples of blood serum and RZB determination in pharmaceutical.

Multivariate Optimization of Rizatriptan Benzoate-Loaded Solid Lipid Nanoparticles for Brain Targeting and Migraine Management.[Pubmed:27126007]

AAPS PharmSciTech. 2017 Feb;18(2):517-528.

The present investigation aimed at development of brain-targeted Rizatriptan Benzoate-loaded solid lipid nanoparticles (RB-SLNs) by design of experiment, for improvement of its anti-migraine potential. Several formulation variables affecting the fabrication of RB-SLNs were screened using the Plackett-Burman design (PBD). The PBD results demonstrated lipid (Precirol(R) ATO 5) concentration, co-surfactant (Phospholipon(R) 90 H) concentration and temperature of lipid melt to be the critical variables, having a significant effect on the achievement of minimum particle size, maximum entrapment efficiency coupled with sustained drug release. The interactions between these formulation parameters and the variability between the batches were further explored employing the Box-Behnken design (BBD). The BBD results were validated by fabricating the suggested optimized solution, which yielded 220.4 +/- 2.3 nm particle size with a sufficiently high entrapment efficiency of 71.8 +/- 1.9% and 45.9 +/- 2.7% cumulative drug release in 8 h. The optimized formulation was, thereafter, characterized by FTIR spectroscopy, wide angle XRD, thermal analysis and TEM imaging technique. The in vivo studies revealed the brain uptake potential of optimized RB-SLNs to be 18.43-folds higher with respect to the pure drug in its free form, post 2 h of oral drug administration. The significant anti-migraine efficacy of RB-SLNs was corroborated through the pharmacodynamic studies on adult male Swiss albino mice. The results hence explicate that RB-SLNs have distinctly improved brain target ability and offer an apt approach for the efficient therapeutic management of migraine.

Description

Rizatriptan Benzoate(Maxalt) is a 5-HT1 agonist triptan drug for the treatment of migraine headaches.

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