Vitamin E polyethylene glycol succinate

• BPTocofersolan
• Ph. Eur.Tocofersolan
• USP–NFVitamin E Polyethylene Glycol Succinate

Tocofersolan; TPGS; vitamin E TPGS; d-α-tocopheryl polyethylene glycol 1000 succinate; Kolliphor TPGS

RRR-α-Tocopheryl polyethylene glycol 1000 succinate · [9002-96-4]

C33O5H54(CH2CH2O)n, n ≈ 22 · ≈ 1513

Solubilising agent, Surfactant, emulsifier

Typical concentrations: — · Dosage forms: Liquid

A non-ionic surfactant used as a solubiliser, emulsifier and absorption enhancer for poorly soluble drugs in oral liquids, lipid-based capsule fills, solid dispersions and self-emulsifying systems. It also inhibits P-glycoprotein efflux, which can improve the oral bioavailability of some drugs, and is used as a water-miscible source of vitamin E for patients with fat malabsorption.

A white to light brown, waxy solid that is practically odourless and tasteless. It is made of a lipophilic d-α-tocopherol head linked through succinic acid to a hydrophilic polyethylene glycol 1000 chain, and contains small amounts of free tocopherol, tocopheryl succinate and the diester.

HLB

about 13

Critical micelle concentration

about 0.02% w/w (in water at 37 °C)

Melting point

about 37–41 °C

Solubility

soluble in water (forms micellar solutions at up to about 20% w/w; liquid-crystalline phases form at higher concentrations); soluble in ethanol and many lipids

Physical form

white to light brown, waxy solid

Stable in air but the ester bonds hydrolyse in alkaline conditions, so solutions are best kept below about pH 7. Store in a tightly closed container, protected from light and heat.

Incompatible with strong oxidising agents and strong alkalis.

Prepared by esterifying d-α-tocopheryl acid succinate with polyethylene glycol 1000.

Generally well tolerated orally; it is hydrolysed in the gut to release tocopherol. Very large doses may cause diarrhoea. The combination of high TPGS and propylene glycol content in some paediatric oral solutions has raised concern in young children.

Observe normal precautions for the quantity handled. Eye protection and gloves are recommended. The waxy solid is usually melted (above about 40 °C) for processing.

Included in the FDA Inactive Ingredient Database (oral capsules and solutions) and in medicines licensed in the USA and Europe, including a vitamin E preparation for children with chronic cholestasis.

Alpha tocopherol; polyethylene glycol; polysorbate 80; macrogolglycerol ricinoleate.

Because it melts near body temperature, it can be filled as a melt into hard or soft capsules. Its P-glycoprotein inhibition may alter the absorption of co-administered substrates, which should be considered when it is used at high levels.