Lactose monohydrate is known as Dry powder inhaler carrier, lyophilization aid, tablet binder, tablet and capsule diluent, tablet and capsule filler. This product is available in Arvin Kala’s diverse product portfolio.
In its solid state, lactose can exist in various isomeric forms depending on the crystallization and drying conditions, such as α-lactose monohydrate, β-lactose anhydrous, and α-lactose anhydrous. The stable crystalline forms of lactose include α-lactose monohydrate, β-lactose anhydrous, and stable α-lactose anhydrous.
Applications in Pharmaceutical Formulation or Technology
Lactose is extensively used as a filler and diluent in tablets and capsules, and to a lesser extent in lyophilized products and infant formulas. It is also employed as a diluent in dry-powder inhalation formulations. Various grades of lactose are commercially available, each with different physical properties such as particle size distribution and flow characteristics, allowing for the selection of the most suitable material for specific applications. For instance, the particle size range chosen for capsules often depends on the type of encapsulating machine used. Typically, fine grades of lactose are used in tablet preparation by the wet-granulation method or when milling during processing, as the fine size allows for better mixing with other formulation ingredients and more efficient use of the binder.
Lactose is also used in lyophilized products, where it is added to freeze-dried solutions to increase plug size and improve cohesion. Additionally, lactose is combined with sucrose (approximately 1:3 ratio) to prepare sugar-coating solutions. It can also be used in intravenous injections.
Lactose is also utilized in the production of dry powder formulations for use in aqueous film-coating solutions or suspensions.
Direct-compression grades of lactose monohydrate are available as granulated or agglomerated α-lactose monohydrate, which contain small amounts of anhydrous lactose.
Direct-compression grades are frequently utilized to accommodate smaller amounts of medication, allowing tablets to be produced without the need for granulation.
Other types of directly compressible lactoses include spray-dried lactose and anhydrous lactose; refer to Lactose, Spray-Dried and Lactose, Anhydrous for more details.
Stability and Storage Conditions
Mold can grow in humid conditions (80% relative humidity or higher). Lactose may turn brown during storage, especially in warm, damp environments. The purity of different lactose types can vary, making color evaluation crucial, particularly for formulating white tablets. Additionally, the color stability of various lactoses differs, and their solutions exhibit mutarotation.
Lactose should be kept in a tightly sealed container in a cool, dry environment.
Method of Manufacture
Mold can grow in humid conditions (80% relative humidity or higher). Lactose may turn brown during storage, especially in warm, damp environments. The purity of different lactose types can vary, making color evaluation crucial, particularly for formulating white tablets. Additionally, the color stability of various lactoses differs, and their solutions exhibit mutarotation.
Store lactose in a tightly sealed container in a cool, dry location.
Safety
Lactose is commonly used in pharmaceutical formulations as a filler and filler-binder in oral capsules and tablets, and it can also be used in intravenous injections. Adverse reactions to lactose are mainly due to lactose intolerance, which occurs in individuals lacking the enzyme lactase. This deficiency prevents lactose digestion, leading to symptoms such as cramps, diarrhea, bloating, and flatulence. In lactose-tolerant individuals, lactase breaks down lactose in the small intestine into glucose and galactose, which are then absorbed. Lactase levels are typically high at birth but decrease rapidly in early childhood. Lactose malabsorption (hypolactasia) can begin as early as ages 4 to 8 and varies among different ethnic groups. When administered intravenously, lactose is excreted unchanged.
The symptoms of lactose intolerance arise from the osmotic effect of unabsorbed lactose, which increases water and sodium levels in the intestinal lumen. When unabsorbed lactose reaches the colon, it can be fermented by colonic bacteria, producing gas and causing abdominal distension and discomfort. A lactose tolerance test, which measures blood glucose and breath hydrogen levels, has been developed. However, its effectiveness is debated since the test uses a 50 g dose of lactose.
Lower doses of lactose cause fewer adverse effects, and it is better tolerated when consumed with other foods. Consequently, many people with lactose malabsorption can still consume normal amounts of lactose, such as that found in milk, without experiencing adverse side effects.
Most adults can consume about 25 grams of lactose per day (equivalent to 500 mL of milk) without experiencing symptoms. When symptoms do occur, they are typically mild and related to the dose. The amount of lactose in most pharmaceuticals rarely exceeds 2 grams per day. Therefore, it is unlikely that severe gastrointestinal symptoms are caused by the lactose in standard oral solid-dosage forms, especially in adults who have not been previously diagnosed with severe lactose intolerance. However, there have been anecdotal reports of drug-induced diarrhea due to lactose intolerance following the use of pharmaceutical products containing lactose.
It has been suggested that lactose intolerance might play a role in irritable bowel syndrome, but this connection remains unclear.
In the past, there were concerns about transmissible spongiform encephalopathies (TSE) contamination in animal-derived products. However, based on current scientific knowledge, milk and milk derivatives are considered unlikely to pose any risk of TSE contamination, regardless of their geographical origin. The risk of TSE is negligible if calf rennet is produced according to regulations.
LD50 (rat, IP): >10 g/kg
LD50 (rat, oral): >10 g/kg
LD50 (rat, SC): >5 g/kg
Handling Precautions
Take standard precautions based on the situation and the amount of material being handled. Avoid creating or inhaling excessive dust.
Chemical-physical values
| TESTS | Unit | Specification |
|---|---|---|
|
Acidity or alkalinity |
ml |
Max 0.4 |
|
speck optical rotation (anhydrous
substance)
|
|
Min 54.4 &
Max 55.8
|
|
Absorbance at400 nm |
|
Max 0.04 |
|
Absorbance from 210 to 220 nm
|
|
max 0.25 |
|
Absorbancefrom 270 to 300 nm
|
|
max 0.07 |
|
Heavy metals |
µg/g |
max5 |
|
Water |
% |
Min 4.5 &
Max 5.5
|
|
Loss on dryin |
% |
max 0.5 |
| TESTS | Unit | Specification |
|---|---|---|
|
Sulfated ash |
% |
Max 0.1 |
|
Partazle see distribution < 53 µm |
% |
Min 20 &
Max 42
|
|
Particle size distribution < 212 µm |
% |
min 95 |
|
Appearance of solution |
NTU |
max 3 |
|
Total aerobic microbial count (TAMC) |
cfu/g |
max 100 |
|
Total combined yeasts/moulds count (TYMC) |
cfu/g |
max 10 |
|
.Salmonella spp |
In 100g/ |
absence |
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