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Pizotifen Malate

CAS# 5189-11-7

Pizotifen Malate

Catalog No. BCC4825----Order now to get a substantial discount!

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Chemical structure

Pizotifen Malate

3D structure

Chemical Properties of Pizotifen Malate

Cas No. 5189-11-7 SDF Download SDF
PubChem ID 168993 Appearance Powder
Formula C23H27NO5S M.Wt 429.53
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble in DMSO > 10 mM
Chemical Name 4-(4,5-dihydrobenzo[1,2]cyclohepta[3,4-b]thiophen-10-ylidene)-1-methylpiperidine;2-hydroxybutanedioic acid
SMILES CN1CCC(=C2C3=C(CCC4=CC=CC=C42)SC=C3)CC1.C(C(C(=O)O)O)C(=O)O
Standard InChIKey IWAWCPZVTXCFKD-UHFFFAOYSA-N
Standard 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)
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.

Pizotifen Malate Dilution Calculator

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Pizotifen Malate Molarity Calculator

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Preparing Stock Solutions of Pizotifen Malate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.3281 mL 11.6406 mL 23.2813 mL 46.5625 mL 58.2032 mL
5 mM 0.4656 mL 2.3281 mL 4.6563 mL 9.3125 mL 11.6406 mL
10 mM 0.2328 mL 1.1641 mL 2.3281 mL 4.6563 mL 5.8203 mL
50 mM 0.0466 mL 0.2328 mL 0.4656 mL 0.9313 mL 1.1641 mL
100 mM 0.0233 mL 0.1164 mL 0.2328 mL 0.4656 mL 0.582 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 Pizotifen Malate

Pizotifen malate is a highly selective 5-HT receptor blocking agent, which is a benzocycloheptane based drug.

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References on Pizotifen Malate

Development of antimigraine transdermal delivery systems of pizotifen malate.[Pubmed:26196273]

Int J Pharm. 2015 Aug 15;492(1-2):223-32.

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. Transdermal delivery systems (TDS) of pizotifen were manufactured by including chemical enhancers, decenoic acid or oleic acid, and were subsequently characterized. When the results obtained with solutions were compared with those obtained with the TDS, a positive enhancement effect was observed with the latter with respect to the partitioning and diffusion of the drug across the skin. Our findings endorse the suitability of our TDS for delivering therapeutic amounts of Pizotifen Malate.

Solubility of solid dispersions of pizotifen malate and povidone.[Pubmed:11548858]

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.

Validation and application of reversed phase high-performance liquid chromatographic method for quantification of pizotifen malate in pharmaceutical solid dosage formulations.[Pubmed:20884459]

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 degrees 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 (1.26+/-0.19). The proposed method was validated in terms of selectivity, linearity, accuracy, precision, range, detection and quantitation limit, system suitability and solution stability.This method can be successfully employed for simultaneous quantitative analysis of Pizotifen Malate in pharmaceutical solid dosage formulations.

Description

Pizotifen malate (BC-105 malate) is a potent 5-HT2 receptor antagonist, with a high affinity for 5-HT1C binding site.

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