Functional Category
Color adjuvant; flavor enhancer; freeze-drying agent; humectant; stabilizing agent; sweetening agent; tablet diluent; thickening agent
Applications in Pharmaceutical Formulation
Trehalose is used for the lyoprotection of therapeutic proteins, particularly for parenteral administration. Other pharmaceutically relevant applications include use as an excipient for diagnostic assay tablets;(1) for stabilization during the freeze–thaw and lyophilization of liposomes;(2,3) and for stabilization of blood cells,(4) cosmetics,(5) and monoclonal antibodies.(6) Trehalose may also be used in formulations for topical application.(7)
Description
Trehalose occurs as virtually odorless, white or almost white crystals with a sweet taste (approximately 45% of the sweetness of sucrose).(8)
Stability and Storage Conditions
Trehalose is a relatively stable material. At 608C for 5 hours it loses not more than 1.5% w/w of water (the dihydrate water of T 746 Trehalose crystallization is retained). Open stored powder may liquefy at high relative humidity (590%). Trehalose should be stored in a cool, dry place in a well-sealed container
Incompatibilities
Trehalose is incompatible with strong oxidizing agents, especially in the presence of heat.
Safety
Trehalose is used in cosmetics, foods, and parenteral and nonparenteral pharmaceutical formulations. It is generally regarded as a relatively nontoxic and nonirritant material when used as an excipient. In the gut, trehalose is rapidly metabolized to glucose by the specific enzyme trehalase. A small minority of the population exhibits a primary (hereditary) or secondary (acquired) trehalase deficiency and thus may experience intestinal discomfort after ingestion of excessive amounts of trehalose owing to the osmotic activity of undigested trehalose in the gut. However, smaller amounts of trehalose are tolerated by such individuals without any symptoms.(8) Trehalose is used as a sweetener and is reported to have substantially less cariogenic potential than sucrose. LD50 (dog, IV): >1 g/kg LD50 (dog, oral): >5 g/kg LD50 (mouse, IV): >1 g/kg LD50 (mouse, oral): >5 g/kg LD50 (rat, IV): >1 g/kg LD50 (rat, oral): >5 g/kg