Pizotifen malate - CAS 5189-11-7
Catalog number: B0046-093556
Category: APIs
Molecular Formula:
C19H21NS·C4H6O5
Molecular Weight:
429.53
COA:
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Description:
Pizotifen is a benzocycloheptene-based drug used for the treatment of recurrent migraine headaches. It acts as an antagonist of 5-HT2A and 5HT2C receptors.
Ordering Information
Catalog Number Size Price Stock Quantity
B0046-093556 2.5 g $198 In stock
B0046-093556 5 g $368 In stock
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Purity:
>98%
Related CAS:
15574-96-6
Synonyms:
BC-105; BC 105; BC105
MSDS:
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InChIKey:
IWAWCPZVTXCFKD-UHFFFAOYSA-N
InChI:
InChI=1S/C19H21NS.C4H6O5/c1-20-11-8-15(9-12-20)19-16-5-3-2-4-14(16)6-7-18-17(19)10-13-21-18;5-2(4(8)9)1-3(6)7/h2-5,10,13H,6-9,11-12H2,1H3;2,5H,1H2,(H,6,7)(H,8,9)
Canonical SMILES:
CN1CCC(=C2C3=C(CCC4=CC=CC=C42)SC=C3)CC1.C(C(C(=O)O)O)C(=O)O
1.HPLC-UV analytical method for determination of pizotifen after in vitro transdermal diffusion studies.
Serna-Jiménez CE1, del Rio Sancho S, Calatayud-Pascual MA, Balaguer-Fernández C, Femenía-Font A, López-Castellano A, Merino V. Biomed Chromatogr. 2012 Jun;26(6):769-74. doi: 10.1002/bmc.1727. Epub 2011 Oct 17.
Pizotifen malate is an antihistamine and serotonin inhibitor used in the preventive treatment of migraine and eating disorders. A simple, rapid, accurate and precise high-performance liquid chromatography (HPLC) method involving ultraviolet detection was validated for the quantitative analysis of pizotifen malate in samples from in vitro transdermal diffusion studies. The method was validated for specificity, linearity, accuracy, precision, limit of detection, limit of quantification and robustness. Drug stability in the solution was also determined under different conditions. Separation was carried out using a 250 × 4.0 mm Kromasil(®) C(18) column at room temperature. The detector response, fitted at 254 nm, was found to be linear in a concentration range between 0.24 and 24.0 µg/mL. The limit of detection was 0.02 µg/mL and the limit of quantification was 0.07 µg/mL. Finally, in vitro transdermal diffusion of pizotifen malate was characterized using the validated HPLC method.
2.Solubility of solid dispersions of pizotifen malate and povidone.
Margarit MV1, Marín MT, Contreras MD. Drug Dev Ind Pharm. 2001 Jul;27(6):517-22.
We analyzed the physicochemical characteristics of solid dispersions of pizotifen malate and povidone (Kollidon 12) at different proportions; we used X-ray diffraction, infrared spectrometry and differential scanning calorimetry (DSC) and tested the solubility of the solid dispersions in equilibrium. The results were compared with findings for physical mixtures with the same proportions. A solid dispersion with a drug proportion of 16%-17% formed a eutectic mixture. Solubility of pizotifen malate increased with the proportion of drug in the solid dispersion up to a drug:polymer ratio of 40:60. The hydrotropic effect of the polymer also favored solubility: In physical mixtures, this effect was greatest at a drug:polymer ratio of 10:90; solubility at this proportion was equal to that of the solid dispersion at the same proportion.
3.Development of antimigraine transdermal delivery systems of pizotifen malate.
Serna-Jiménez CE1, del Rio-Sancho S2, Calatayud-Pascual MA2, Balaguer-Fernández C2, Femenía-Font A2, López-Castellano A2, Merino V3. Int J Pharm. 2015 Aug 15;492(1-2):223-32. doi: 10.1016/j.ijpharm.2015.07.033. Epub 2015 Jul 18.
The aim of this study was to develop and evaluate a transdermal delivery system of pizotifen malate. Pizotifen is frequently used in the preventive treatment of migraine, but is also indicated in eating disorders. In the course of the project, the effects of chemical enhancers such as ethanol, 1,8-cineole, limonene, azone and different fatty acids (decanoic, decenoic, dodecanoic, linoleic and oleic acids) were determined, first using a pizotifen solution. Steady state flux, diffusion and partition parameters were estimated by fitting the Scheuplein equation to the data obtained. Among the chemical enhancers studied, decenoic acid showed the highest enhancement activity, which seemed to be due to the length of its alkyl chain and unsaturation at the 9th carbon. The influence of iontophoresis and the involvement of electrotransport in said process was determined. The absorption profile obtained with iontophoresis was similar to that obtained with fatty acids and terpenes, though skin deposition of the drug was lower with the former.
4.Validation and application of reversed phase high-performance liquid chromatographic method for quantification of pizotifen malate in pharmaceutical solid dosage formulations.
Rahman SM1, Lutfulkabir A, Jahan MD, Momen AZ, Rouf AS. Pak J Pharm Sci. 2010 Oct;23(4):435-41.
The aim of this study was to develop and validate an isocratic reversed phase high-performance liquid chromatographic method for quantification of pizotifen malate in pharmaceutical solid dosage formulations. Good chromatographic separation of pizotifen malate was achieved by using an analytical column, C(18) ODS column. The system was operated at 40°C oven temperature using a mobile phase consisting of acetonitrile and acetate buffer pH 7.0 (60:40) at a flow rate of 2 ml/min. The method showed high sensitivity with good linearity (r(2)= 0.99997) over the tested concentration range of 0.0020-0.0300 mg/ml for pizotifen malate. Detection was carried out at 231 nm and retention time was 2.838 min. Placebo and blank studies were performed and no peak was observed at the retention time of pizotifen malate. The intermediate precision and accuracy results (mean ± RSD, n=3) were (99.11±0.21) % and (99.19±0.55) % respectively with tailing factor (1.
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CAS 5189-11-7 Pizotifen malate

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