Lactose, Monohydrate

Synonyms: CapsuLac; GranuLac; Lactochem; lactosum monohydricum; Monohydrate; Pharmatose; PrismaLac; SacheLac; SorboLac; SpheroLac; SuperTab 30GR; Tablettose

Description: In the solid state, lactose appears as various isomeric forms, depending on the crystallization and drying conditions, i.e. alactose monohydrate, b-lactose anhydrous, and a-lactose anhydrous. The stable crystalline forms of lactose are a-lactose monohydrate, b-lactose anhydrous, and stable a-lactose anhydrous. Lactose occurs as white to off-white crystalline particles or powder. Lactose is odorless and slightly sweet-tasting; a-lactose is approximately 20% as sweet as sucrose, while b-lactose is 40% as sweet.

Chemical Name: O-b-D-Galactopyranosyl-(1!4)-a-D-glucopyranose monohydrate

Dry powder inhaler carrier; lyophilization aid; tablet binder; tablet and capsule diluent; tablet and capsule filler.

• Lactose is widely used as a filler and diluent in tablets and capsules, and to a more limited extent in lyophilized products and infant formulas.

• Lactose is also used as a diluent in dry-powder inhalation; seeLactose, Inhalation.

• Various lactose grades are commercially available that have different physical properties such as particle size distribution and flow characteristics.

• This permits the selection of the most suitable material for a particular application; for example, the particle size range selected for capsules is often dependent on the type of encapsulating machine used.

   

• Usually, fine grades of lactose are used in the preparation of tablets by the wet-granulation method or when milling during processing is carried out, since the fine size allows better mixing with other formulation ingredients and utilizes the binder more efficiently.

• Other applications of lactose include use in lyophilized products, where lactose is added to freeze-dried solutions to increase plug size and aid cohesion.

• Lactose is also used in combination with sucrose (approximately 1 : 3) to prepare sugar-coating solutions.

• It may also be used in intravenous injections.

• Lactose is also used in the manufacture of dry powder formulations for use as aqueous film-coating solutions or suspensions

A Maillard-type condensation reaction is likely to occur between lactose and compounds with a primary amine group to form brown, or yellow-brown-colored products. The Maillard interaction has also been shown to occur between lactose and secondary amine. However, the reaction sequence stops with the formation of the imine, and no yellow-brown coloration develops. Lactose is also incompatible with amino acids, amfetamines, and lisinopril

Lactose is widely used in pharmaceutical formulations as a filler and filler-binder in oral capsule and tablet formulations. It may also be used in intravenous injections. Adverse reactions to lactose are largely attributed to lactose intolerance, which occurs in individuals with a deficiency of the intestinal enzyme lactase. This results in lactose being undigested and may lead to cramps, diarrhea, distension, and flatulence. In lactose-tolerant individuals, lactase hydrolyzes lactose in the small intestine to glucose and galactose, which are then absorbed. Lactase levels are normally high at birth, and levels decline rapidly in early childhood. Malabsorption of lactose (hypolactasia) may occur at an early age (4–8 years) and varies among different ethnic groups. Lactose is excreted unchanged when administered intravenously.

Observe normal precautions appropriate to the circumstances and quantity of material handled. Excessive generation of dust, or inhalation of dust, should be avoided.

Lactose, anhydrous; lactose, inhalation; lactose, monohydrate and corn starch; lactose, monohydrate and microcrystalline cellulose; lactose, monohydrate and povidone; lactose, monohydrate and powdered cellulose; lactose, spray-dried.