Витамин Е сукцинат полиэтиленгликоля (TPGS)

Химические свойства

Vitamin 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.

Методы производства

Vitamin E polyethylene glycol succinate is prepared by esterification of the acid group of crystalline D-a-tocopheryl acid succinate by polyethylene glycol 1000.

Фармацевтические приложения

Vitamin 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.

Безопасность

Vitamin 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.

хранилище

Vitamin 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.

Несовместимости

Vitamin E polyethylene glycol succinate is incompatible with strong acids and strong alkalis.

Регуляторный статус

GRAS 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.