ラクトース一水和物 化学特性,用途語,生産方法
化学的特性
White or almost white, crystalline powder.
使用
Excipient.
調製方法
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.
応用例（製薬）
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.
貯蔵
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.
不和合性
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.
規制状況(Regulatory Status)
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.
ラクトース一水和物 上流と下流の製品情報
原材料
準備製品