Trehalose

Category

Color adjuvant; Flavor enhancer; freeze-drying Agents; Humectant; Stabilizing Agents; Sweetening Agents; Diluent; Thickening Agents

Grade

Pharmceutical Excipients

Description

Trehalose occurs as virtually odorless, white or almost white crystals with a sweet taste (approximately 45% of the sweetness of sucrose).

UNII

NA

Chemical Name

(2R, 3R, 4S, 5R, 6R)-2-(Hydroxymethyl)-6-[(2R, 3R, 4S, 5R, 6R)- 3, 4, 5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-oxane-3, 4, 5- triol anhydrous [99-20-7] (2R, 3R, 4S, 5R, 6R)-2-(Hydroxymethyl)-6-[(2R, 3R, 4S, 5R, 6R)- 3, 4, 5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-oxane-3, 4, 5- triol dihydrate [6138-23-4]

Synonyms

Ascend; α-D-glucopyranosyl-α-D-glucopyranoside; (α-D-glucosido)-α-D-glucoside; mycose; natural trehalose; α, α-trehalose; Treha; trehalose dihydrate

Administration route

Injection

Dosage Form

Injections

Stability and Storage Conditions

Trehalose is a relatively stable material. At 60℃ for 5 hours it loses not more than 1.5% w/w of water (the dihydrate water of crystallization is retained). Open stored powder may liquefy at high relative humidity (≥90%). Trehalose should be stored in a cool, dry place in a well-sealed container.

Source and Preparation

Trehalose is prepared from liquefied starch by a multistep enzymatic process.The commercial product is the dihydrate.

Applications

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; for stabilization during the freeze-thaw and lyophilization of liposomes; and for stabilization of blood cells, cosmetics, and monoclonal antibodies.Trehalose may also be used in formulations for topical application.

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. 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

Incompatibilities

Trehalose is incompatible with strong oxidizing agents, especially in the presence of heat.