Лактоза 1-водн

Химические свойства

White or almost white, crystalline powder.

Использование

Excipient.

Методы производства

Lactose is a natural disaccharide consisting of galactose and glucose, and is present in the milk of most mammals. Commercially, lactose is produced from the whey of cows’ milk; whey being the residual liquid of the milk following cheese and casein production. Cows’ milk contains 4.4–5.2% lactose; lactose constitutes 38% of the total solid content of milk.
a-Lactose monohydrate is prepared by crystallization from supersaturated solutions below 93.5°C. Various crystalline shapes are prism, pyramidal, and tomahawk; these are dependent on the method of precipitation and crystallization. Direct compression grades of a-lactose monohydrate are prepared by granulation/ agglomeration and spray-drying.

Фармацевтические приложения

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. Direct-compression grades of lactose monohydrate are available as granulated/agglomerated a-lactose monohydrate, containing small amounts of anhydrous lactose.
Direct-compression grades are often used to carry lower quantities of drug and this permits tablets to be made without granulation.
Other directly compressible lactoses are spray-dried lactose and anhydrous lactose; see Lactose, Spray-Dried and Lactose, Anhydrous.

хранилище

Mold growth may occur under humid conditions (80% relative humidity and above). Lactose may develop a brown coloration on storage, the reaction being accelerated by warm, damp conditions. The purities of different lactoses can vary and color evaluation may be important, particularly if white tablets are being formulated. The color stabilities of various lactoses also differ. Solutions show mutarotation.
Lactose should be stored in a well-closed container in a cool, dry place.

Несовместимости

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.

Регуляторный статус

GRAS listed. Included in the FDA Inactive Ingredients Database (IM, IV, and SC: powder for injections; oral: capsules and tablets; inhalation preparations; vaginal preparations). Included in nonparenteral and parenteral medicines licensed in the UK. Included in the Canadian List of Acceptable Non-medicinal Ingredients.