Ketotifen FumarateCAS# 34580-14-8 |
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Quality Control & MSDS
3D structure
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| Cas No. | 34580-14-8 | SDF | Download SDF |
| PubChem ID | 5282408 | Appearance | Powder |
| Formula | C23H23NO5S | M.Wt | 425.5 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 100 mg/mL (235.02 mM) H2O : 16.67 mg/mL (39.18 mM; Need ultrasonic) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | (E)-but-2-enedioic acid;10-(1-methylpiperidin-4-ylidene)-5H-benzo[1,2]cyclohepta[3,4-b]thiophen-4-one | ||
| SMILES | CN1CCC(CC1)=C2c3ccccc3CC(=O)c4sccc24.OC(=O)C=CC(O)=O | ||
| Standard InChIKey | YNQQEYBLVYAWNX-WLHGVMLRSA-N | ||
| Standard InChI | InChI=1S/C19H19NOS.C4H4O4/c1-20-9-6-13(7-10-20)18-15-5-3-2-4-14(15)12-17(21)19-16(18)8-11-22-19;5-3(6)1-2-4(7)8/h2-5,8,11H,6-7,9-10,12H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1+ | ||
| 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. |
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| 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. |
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| 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. | ||
| Description | An H1 receptor antagonist. |
Ketotifen Fumarate Dilution Calculator
Ketotifen Fumarate Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.3502 mL | 11.7509 mL | 23.5018 mL | 47.0035 mL | 58.7544 mL |
| 5 mM | 0.47 mL | 2.3502 mL | 4.7004 mL | 9.4007 mL | 11.7509 mL |
| 10 mM | 0.235 mL | 1.1751 mL | 2.3502 mL | 4.7004 mL | 5.8754 mL |
| 50 mM | 0.047 mL | 0.235 mL | 0.47 mL | 0.9401 mL | 1.1751 mL |
| 100 mM | 0.0235 mL | 0.1175 mL | 0.235 mL | 0.47 mL | 0.5875 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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Ketotifen (fumarate) is a second-generation noncompetitive H1-antihistamine and mast cell stabilizer, which is used to prevent asthma attacks.
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Generic selection criteria for safety and patient benefit [V]: Comparing the pharmaceutical properties and patient usability of original and generic nasal spray containing ketotifen fumarate.[Pubmed:27210891]
Drug Discov Ther. 2016;10(2):88-92.
The pH, osmotic pressure (cryoscopy), viscosity, squeeze force, spray angle, and spraying frequency of nasal spray containing Ketotifen Fumarate (1 brand-name product and 8 generic products) were measured. Based on the results of pH measurement, all products were weakly acidic (4.0 to 5.1). For all products, the osmotic pressure ratio to physiological saline was approximately 1. The viscosity of various products ranged from approximately 1.0 to 1.5 mPa.s. The spray angle of drug solution differed among the products: minimum, 46 degrees (Sawai and Fusachol); and maximum, 68.7 degrees (Sekiton). In particular, TOA, Sawai, Fusachol, and TYK showed significantly smaller angles compared to Zaditen (brand-name product). Container properties varied among the products: minimum squeeze force, 19.0 N (Sekiton); and maximum squeeze force, 43.1 N (Sawai). Based on these results, although all the above products are identical in dosage form and active ingredient, the differences in pharmaceutical properties, such as container operations and drug-solution spraying/attachment, may markedly influence patients' subjective opinions.
Comparison of Different Nanosuspensions as Potential Ophthalmic Delivery Systems for Ketotifen Fumarate.[Pubmed:27766218]
Adv Pharm Bull. 2016 Sep;6(3):345-352.
Purpose: The objective of this study was to develop, characterize, and comparatively investigate the Ketotifen Fumarate (KF) nanosuspensions (NSS) to enhance the permeability of KF. Methods: In the present work, the NSP and NSE were prepared by double-emulsion solvent evaporation/nanoprecipitation methods with poly (D,Llactide-co-glycolide) and Eudragit RL100 polymers, respectively. The loading efficiency, particle size, and polydispersity index of prepared different NSs were evaluated with scanning electron microscopy (SEM), X-ray diffraction, differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), and in vitro release and transcorneal permeation . NSs were also compared on the basis of particle size and polydispersity index. Results: Particle size, polydispersity index, and loading efficiency of NSP1 and NSE3 showed the best value (158 nm, 117 nm, 0.21, 0.43 and 43%, 95.23%, respectively). SEM showed spherical globules and DSC results showed the reduction in crystallinity. The NSE3 formulations demonstrated significantly (p<0.05) higher drug release rates than the NSP1 due to increases in the surface area. Comparative studies showed that NSE release and permeability are higher than NSP. Conclusion: It is concluded that both NSP and NSE provide a useful dosage form for the ocular drug delivery which can enhance the permeability of KF.
Design of eudragit RL nanoparticles by nanoemulsion method as carriers for ophthalmic drug delivery of ketotifen fumarate.[Pubmed:27403262]
Iran J Basic Med Sci. 2016 May;19(5):550-60.
OBJECTIVES: Ketotifen Fumarate (KF) is a selective and noncompetitive histamine antagonist (H1-receptor) that is used topically in the treatment of allergic conditions of rhinitis and conjunctivitis. The aim of this study was to formulate and improve an ophthalmic delivery system of KF. Ocular nanoparticles were prepared with the objective of reducing the frequency of administration and obtaining controlled release to improve the anti-inflammatory drug delivery. MATERIALS AND METHODS: In the present study, ocular KF loaded Eudragit RL 100 nanoparticles were prepared using O/W solvent diffusion method. The nanoparticles were evaluated for particle size, entrapment efficiency, surface morphology, X-ray diffraction (XRD), Fourier transform spectroscopy (FTIR), and differential scanning calorimetry (DSC). In vitro release and permeation studies were also carried out on nanoparticles. RESULTS: An average size range of 182 to 314.30 nm in diameter was obtained and encapsulation efficiency up to 95.0% was observed for all the formulations. Drug release for all formulations after 24 hr was between 65.51% and 88.82% indicating effective controlled release property of KF. The mechanism of drug release for best formulation was found to be fickian diffusion mechanism. KF nanoparticles containing high polymer concentration (1:15) presented a faster drug release and a higher drug penetration; on the contrary, nanoparticles containing low polymer concentration (1:7.5) were able to give a more sustained release of the drug and thus a slower KF permeation through the cornea. CONCLUSION: The study revealed that KF NPs were capable of releasing the drug for a prolonged period of time and increasing the ocular bioavailability.
