Lactitol

Basic Information

Name: Lactitol

CAS No: 4-O-(b-D-Galactopyranosyl)-D-glucitol [585-86-4], 4-O-(b-D-Galactopyranosyl)-D-glucitol monohydrate [81025-04-9] 4-O-(b-D-Galactopyranosyl)-D-glucitol dihydrate [81025-03-8]

Functional Categories

Sweetening agent Tablet and capsule diluent Therapeutic agent

1. Nonproprietary Names

BP: Lactitol Monohydrate PhEur: Lactitol Monohydrate USP-NF: Lactitol

2. Synonyms

E966; b-galactosido-sorbitol; Finlac DC; lactil; lactite; lactitolum monohydricum; lactobiosit; lactosit; Lacty

3. Chemical Name & CAS Registry

4-O-(b-D-Galactopyranosyl)-D-glucitol [585-86-4], 4-O-(b-D-Galactopyranosyl)-D-glucitol monohydrate [81025-04-9] 4-O-(b-D-Galactopyranosyl)-D-glucitol dihydrate [81025-03-8]

4. Empirical Formula & Molecular Weight

C12H24O11 344.32 (anhydrous) C12H24O11H2O 362.34 (monohydrate) C12H24O112H2O 380.35 (dihydrate)

5. Structural Formula

6. Applications

Lactitol is used as a noncariogenic replacement for sucrose. It is also used as a diluent in solid dosage forms.(1) A direct-compression form is available,(2,3) as is a direct-compression blend of lactose and lactitol. Lactitol is also used therapeutically in the treatment of hepatic encephalopathy and as a laxative

7. Description

Lactitol occurs as white orthorhombic crystals. It is odorless with a sweet taste that imparts a cooling sensation. It is available in powdered form and in a range of crystal sizes. The directly compressible form is a water-granulated product of microcrystalline aggregates.

8. Pharmacopeial Specifications

See Table I

9. Typical Properties

Acidity–alkalinity pH = 4.5–7.0 (10% w/v solution) Density 1.54 g/cm3 Heat of solution 54 J/g Loss of water of crystallization 145–1858C Moisture content 4.5–5.5% for the monohydrate; 40.5% for the anhydrous. NIR spectra see Figure 1. Osmolarity A 7% w/v aqueous solution is isoosmotic with serum. Refractive index nD 20 = 1.3485 (10% solution); nD 20 = 1.3650 (20% solution); nD 20 = 1.3827 (30% solution); nD 20 = 1.4018 (40% solution); nD 20 = 1.4228 (50% solution); nD 20 = 1.4466 (60% solution). Solubility Slightly soluble in ethanol (95%) and ether. Soluble 1 in 1.75 of water at 208C; 1 in 1.61 at 308C; 1 in 1.49 at 408C; 1 in 1.39 at 508C. Specific rotation [a]D 20 = þ14.58 to þ158 Viscosity (dynamic) 1.3 mPa s (1.3 cP) for 10% solution at 208C; 1.9 mPa s (1.9 cP) for 20% solution at 208C; 3.4 mPa s (3.4 cP) for 30% solution at 208C; 6.9 mPa s (6.9 cP) for 40% solution at 208C; 18.9 mPa s (18.9 cP) for 50% solution at 208C; 80.0 mPa s (80.0 cP) for 60% solution at 208C.

10. Stability & Storage

Lactitol as the monohydrate is nonhygroscopic and is stable under humid conditions. It is stable to heat and does not take part in the Maillard reaction. In acidic solution, lactitol slowly hydrolyzes to sorbitol and galactose. Lactitol is very resistant to microbiological breakdown and fermentation. Store in a well-closed container. When the compound is stored in an unopened container at 258C and 60% relative humidity, a shelf-life in excess of 3 years is appropriate.

12. Method of Manufacture

Lactitol is produced by the catalytic hydrogenation of lactose.

13. Safety

Lactitol is regarded as a nontoxic and nonirritant substance. It is not fermented significantly in the mouth, and is not cariogenic.(4) It is not absorbed in the small intestine, but is broken down by microflora in the large intestine,(5) and is metabolized independently of insulin. In large doses it has a laxative effect; therapeutically, 10–20 g daily in a single oral dose is administered for this purpose. LD50 (mouse, oral): >23 g/kg(6) LD50 (rat, oral): 30 g/kg

14. Handling Precautions

Observe normal precautions appropriate to the circumstances and quantity of material handled. Eye protection is recommended.

15. Regulatory Status

GRAS listed. Accepted for use as a food additive in Europe. Included in the Canadian List of Acceptable Non-medicinal Ingredients.

17. Comments

Finlac DC is a commercially available water-granulated directly compressible lactitol.(2) Lactitol has a sweetening power about one-third that of sucrose. It does not promote dental caries and has a caloric value of 9.9 J/g (2.4 cal/g). The EINECS number for lactitol is 209-566-5.