Tocofersolan

Tocofersolan
  • CAS No.:9002-96-4
Other grades of this product :
Tocofersolan Basic information
Product Name:Tocofersolan
Synonyms:DL-A-TOCOPHEROL POLYETHYLENE GLYCOL SUCCINATE;DL-ALPHA-TOCOPHEROL POLYETHYLENE GLYCOL SUCCINATE;d-alpha-tocopheryl polyethylene glycol succinate;alpha-(4-((3,4-dihydro-2,5,7,8-tetramethyl-2-(4,8,12-trimethyltridecyl)-2h-1-benzopyran-6-yl)oxy)-1,4-dioxobutanol poly(ethylene glycol) succinate;tocofersolan;tocopherosolan;2-ethanediyl),.alpha.-[4-[[3,4-dihydro-2,5,7,8-tetramethyl-2-(4,8,12-trimethyltridecyl)-2H-1-benzoPoly(oxy-1;poly(oxy-1,2-ethanediyl),alpha-(4-((3,4-dihydro-2,5,7,8-tetramethyl-2-(4,8,12
CAS:9002-96-4
MF:(C2H4O)nC33H54O5
MW:0
EINECS:
Product Categories:Other APIs;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals
Mol File:9002-96-4.mol
Tocofersolan Chemical Properties
Melting point 34-38°C
storage temp. 2-8°C
solubility H2O: soluble1g/10 mL, clear to faintly turbid, colorless to faintly yellow
form Solid
color White to Pale Yellow Waxy
Safety Information
WGK Germany 2
RTECS TR1581200
MSDS Information
Tocofersolan Usage And Synthesis
Chemical PropertiesVitamin E polyethylene glycol succinate is a synthetic product. It is available as a white to light-brown, waxy solid and is practically tasteless. Chemically, it is a mixture composed principally of monoesterified polyethylene glycol 1000, the diesterified polyethylene glycol 1000, free polyethylene glycol 1000, and free tocopherol.
UsesTocofersolan is a polyethylene glycol derivative of α-Tocopherol (T526125). Tocofersolan is a synthetic water-soluble vitamin E unlike its natural counterpart which are fat soluble. Tocofersolan is used in pediatrics in the treatment vitamin E-deficient cholestatic children. Tocofersolan has potential application as a absorption enhancer in drug delivery systems.
Usestocophersolan is an anti-oxidant, this is a water-soluble form of vitamin e.
UsesTocofersolan is a polyethylene glycol derivative of α-Tocopherol (T526125). Tocofersolan is a synthetic water-soluble vitamin E unlike its natural counterpart which are fat soluble. Tocofersolan is used in pediatrics in the treatment vitamin E-deficient cholestatic children. Tocofersolan has potential application as a absorption enhancer in drug delivery systems. Typical batch, n = 21
Production MethodsVitamin E polyethylene glycol succinate is prepared by esterification of the acid group of crystalline D-a-tocopheryl acid succinate by polyethylene glycol 1000.
Pharmaceutical ApplicationsVitamin E polyethylene glycol succinate is an esterified vitamin E (tocopherol) derivative primarily used as a solubilizer or emulsifying agent because of its surfactant properties. Structurally, it is amphipathic and hydrophilic, unlike the tocopherols, and therefore it is a water-soluble derivative that can be used in pharmaceutical formulations such as capsules, tablets, hot-melt extrusion, microemulsions, topical products, and parenterals. One of the most important applications is its use as a vehicle for lipid-based drug delivery formulations. It can also be used as a source of vitamin E. Vitamin E polyethylene glycol succinate has been characterized with respect to its mechanism of action and studied as a Pglycoprotein inhibitor.
Biochem/physiol ActionsD-α-Tocopherol polyethylene glycol 1000 succinate (TPGS) also known as vitamin E TPGS, is a therapeutic agent for vitamin E deficiency in children, administered during chronic childhood cholestasis. TPGS exerts anti-tumor activity in MCF-7 and breast cancer cells by downregulating anti-apoptotic proteins. TPGS finds its application as an emulsifier in the preparation of poly(lactic-co-glycolic acid) (PLGA) particles for DNA labelling, produces particles of uniform size, high encapsulation efficiency, increases hydrophilicity and prevents aggregation of particles.
SafetyVitamin E polyethylene glycol succinate has been used at levels of 280 mg/capsule in the product Agenerase (amprenavir), which was dosed at 8 capsules (2240mg vitamin E TPGS) per day. An additional assessment of the safety of vitamin E polyethylene glycol succinate has been published, which includes a report showing no-observed-adverse-effect-level (NOAEL) in rats of 1000 mg/kg/day.
storageVitamin E polyethylene glycol succinate is stable at ambient room temperature for up to 4 years. It reacts with alkalis and acids. Aqueous solutions of vitamin E polyethylene glycol succinate are stable over a pH range of 4.5–7.5 and can be further stabilized with propylene glycol.
IncompatibilitiesVitamin E polyethylene glycol succinate is incompatible with strong acids and strong alkalis.
Regulatory StatusGRAS listed. Included in the FDA Inactive Ingredients Database (ophthalmic solution or drops; oral capsules, solution, tablet; topical solution or drops). Included in the Canadian List of Acceptable Non-medicinal Ingredients.
Tocofersolan Preparation Products And Raw materials

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