INHALATION LACTOSE

Inhalation Lactose is produced under strict Good Manufacturing Practice (GMP) conditions in specialized facilities to ensure maximum safety and consistent performance during pulmonary drug delivery.
Inhalation lactose undergoes extensive purification to remove impurities, microbial contamination, and unwanted particle fractions. 
Inhalation Lactose is thoroughly characterized for properties such as anomeric purity, amorphous content, particle size distribution, morphology, moisture level, and trace element content. 

CAS Number: 5989-81-1
Molecular Formula: C12H24O12
Molecular Weight: 360.31
EINECS Number: 611-913-4

Synonyms: Lactose monohydrate, 5989-81-1, alpha-Lactose monohydrate, alpha-D-Lactose monohydrate, D-Lactose monohydrate, 64044-51-5, a-Lactose monohydrate, Respitose, a-D-Glucopyranose, 4-O-b-D-galactopyranosyl-, monohydrate, alpha-lactose hydrate, Lactose monohydrate [NF], (2R,3R,4S,5R,6S)-2-(hydroxymethyl)-6-[(2R,3S,4R,5R,6S)-4,5,6-trihydroxy-2-(hydroxymethyl)oxan-3-yl]oxyoxane-3,4,5-triol;hydrate, EWQ57Q8I5X, 4-O-beta-D-Galactopyranosyl-alpha-D-glucose, Lactose monohydrate (NF), MFCD00150747, lactose hydrate, |A-lactose monohydrate, Inhalac 120 (contains b anomer), Microtose, Pharmaose, Lactopress, Lactose, hydrous, (2R,3R,4S,5R,6S)-2-(hydroxymethyl)-6-{[(2R,3S,4R,5R,6S)-4,5,6-trihydroxy-2-(hydroxymethyl)oxan-3-yl]oxy}oxane-3,4,5-triol hydrate, (2S,3R,4R,5S,6R)-6-(Hydroxymethyl)-5-(((2S,3R,4S,5R,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)tetrahydro-2H-pyran-2,3,4-triol hydrate, 66857-12-3, Spherolac 100, Lactose(Monohydrate), alpha-D-Glucopyranose, 4-O-beta-D-galactopyranosyl-, monohydrate, Lactose (TN), NSC-760401, UNII-EWQ57Q8I5X, Pharmatose, Lactochem, Lactohale, Wyndale, Wynhale, Lactose hydrous, .alpha.-D-Glucopyranose, 4-O-.beta.-D-galactopyranosyl-, monohydrate, Pharmatose dcl ii, Supertab 11sd, Supertab 14sd, Supertab 30gr, Supertab 50 odt, lactose spray-dried, Supertab 11sd nz, Pharmatose dcl 11, Lactopress spray dried, Lactose (JP17), Lactose fastflo 316, |A-Lactose (hydrate), alpha-Lactose (hydrate), LACTOSE,MONOHYDRATE, |A-D-Lactose monohydrate, alpha -lactose monohydrate, SCHEMBL16787, LACTOSE HYDRATE [JAN], LACTOSE, HYDROUS [II], D-Glucose, 4-O-beta-D-galactopyranosyl-, monohydrate, orb2278570, alpha-D(+)-Lactose monohydrate, PHARMATOSE DCL II [II], D-Glucose, 4-O-.beta.-D-galactopyranosyl-, monohydrate, DTXSID1052828, LACTOSE MONOHYDRATE [II], MSK3219, CHEBI:189432, alpha-Lactose, analytical standard, 4-O-A-D-Galactopyranosyl-D-glucose, LACTOSE MONOHYDRATE [USP-RS], LACTOSE MONOHYDRATE [WHO-IP], AKOS015896871, FS-3862, HY-W087904, NSC 760401, OL02402, OL05009, LACTOSE MONOHYDRATE [EP MONOGRAPH], OL176363, CS-0128727, LACTOSUM, MONOHYDRATE [WHO-IP LATIN], NS00099491, D03226, E80712, EN300-1608278, /b-D-galactopyranosyl-(1,4)-D-glucose monhydrate, alpha-4-O-(beta-D-galactopyranosido)-D-glucopyranose, Q27277391, 4-O-b-D-Galactopyranosyl-a-D-glucopyranose monohydrate, alpha-Lactose monohydrate, >=99% total lactose basis (GC), -D-Glucopyranose, 4-O-BATE-D-galactopyranosyl-, hydrate(1:1), Alpha-D(+)-Lactose Monohydrate(Discontinued,See C4X-214913), alpha-D-Glucopyranose, 4-O-beta-D-galactopyranosyl-, hydrate, |A-D-Glucopyranose, 4-O-|A-D-galactopyranosyl-, hydrate(1:1), alpha-Lactose monohydrate, BioXtra, >=99% total lactose basis (GC), alpha-Lactose monohydrate, suitable for cell culture, BioReagent, .alpha.-D-Glucopyranose, 4-O-.beta.-D-galactopyranosyl-, hydrate (1:1), 4-O-b-D-Galactopyranosyl-D-glucopyranose monohydrate;b-D-Gal-(1,4)-D-Glc, (2R,3R,4S,5R,6S)-2-(hydroxymethyl)-6-[(2R,3S,4R,5R,6S)-4,5,6-trihydroxy-2-(hydroxymethyl)tetrahydropyran-3-yl]oxy-tetrahydropyran-3,4,5-triol;hydrate, MILK SUGAR;MILK SUGAR MONOHYDRATE;ALPHA-LACTOSE MONOHY;alpha-D-Lactose Monohydrate, 99.5+%, 2-4% beta-isoMer;alpha-D-Lactose Monohydrate, USP/NF, Ph.Eur., JP 250GR;4-O-beta-D-Galactopyranosyl-alpha-D-glucopyranose monohydrate;LACTOSE MONOHYDRATE, a-(RG);Pharmatose 150M

Inhalation Lactose occurs as white to off-white crystalline particles or powder. 
Inhalation Lactose is odorless and slightly sweet-tasting. 
Spray-dried directcompression grades of lactose are generally composed of 80–90% specially prepared pure a-lactose monohydrate along with 10–20% of amorphous lactose.

Inhalation Lactose a sugar that occurs in many plants. 
Inhalation Lactose is extracted commercially from sugar cane and sugar beet. Sucrose is a disaccharide formed from a glucose unit and a fructose unit. 
Inhalation Lactose is hydrolyzed to a mixture of fructose and glucose by the enzyme invertase. 

Since this mixture has a different optical rotation (levorotatory) than the original sucrose, the mixture is called invert sugar.
Inhalation Lactose is a highly purified form of α‑lactose monohydrate that is specifically processed for use as a carrier excipient in dry powder inhalers (DPIs) and nasal drug delivery systems. 

These parameters are closely monitored to meet regulatory requirements for inhalation‑grade excipients.
To suit different formulations, inhalation lactose is available in multiple particle size grades. 

Coarse sieved lactose provides excellent flowability and carrier properties, milled lactose is used to fine‑tune cohesion and dispersion, while micronized lactose enhances the fine particle fraction for deeper lung deposition. 
Each grade is precisely controlled for particle size (d10, d50, d90), density, and flow characteristics to meet formulation needs.

Inhalation Lactose functions as the primary carrier in most dry powder inhalation products, facilitating the uniform blending and dispersion of active pharmaceutical ingredients with aerodynamic diameters small enough to reach the lower respiratory tract. 
Its controlled physical properties ensure consistent dosing, efficient lung delivery, and good manufacturability.
Due to its long history of safe use, reliable performance, and compatibility with a wide range of formulations, inhalation lactose has become the industry standard carrier excipient for pulmonary drug delivery.

Fine milled DPI lactose further enhances aerodynamic performance, promoting efficient dispersion and reducing agglomeration in inhalation devices. 
Micronized DPI lactose, with an even smaller particle size, is particularly effective for modifying powder cohesion and achieving precise drug-carrier interactions, ensuring optimal deep lung deposition.

Using a dry powder inhaler (DPI) for drug delivery can provide many advantages over traditional oral delivery of pharmaceuticals. 
Inhalation Lactose’s also offer advantages over older respiratory delivery methods such as those using nebulizers or pressurized CFC containing aerosols. 
This is due to the fact that dry powder inhalers allow for the potential to deliver a wider range of drugs than these older methods. 

Typically, with Inhalation Lactose’s, the active ingredient and a carrier are blended and used to fill the inhaler; or with some inhalers, a capsule or blister that includes one singular dose. 
During use, the dose delivery is performed by the patient simply inhaling, or is assisted by a burst of air, depending on the type of inhaler used.

Pharmaceutical Lactose has often been used as a carrier in these applications due to its inertness, low cost, availability, particle size, and patient tolerability. 
However, two of the most important characteristics of the formula are: dose uniformity, and the efficiency of delivering the drug (i.e. the amount of drug that reaches the patients lungs relative to the amount in the starting dose). 
The selection of the grade of lactose used as a carrier will most certainly have an effect on both of these characteristics.

Inhalation lactose is a unique pharmaceutical excipient because it is specifically optimized for the demanding conditions of pulmonary drug delivery, where precise particle behavior determines the therapeutic success of the formulation. 
Unlike conventional lactose used in oral or injectable formulations, inhalation lactose must meet far more stringent requirements for purity, particle engineering, and performance consistency.

Melting point: 219 °C
Boiling point: 412.35 °C (rough estimate)
Optical rotation (α): [α]D20 +52.2～+52.8°
Density: 1.53 g/cm³
Refractive index: 1.6480 (estimate)
RTECS: OD9625000
Storage temp.: Inert atmosphere, Room temperature
Solubility: H₂O: soluble, 1 M, clear, colorless
Form: Solid
Color: White to off-white
pH: 4.0–6.0 (50 g/L, 25 °C)
Biological source: Bovine milk
Water Solubility: Soluble in water
Stability: Hygroscopic
InChIKey: WSVLPVUVIUVCRA-KPKNDVKVSA-N

Inhalation lactose is a highly specialized excipient that combines purity, physical stability, and controlled particle engineering to ensure consistent, safe, and effective drug delivery to the lungs. 
Inhalation lactose continues to be the benchmark material in the field of inhalation therapies due to its well‑documented safety record, excellent performance characteristics, and adaptability to modern drug delivery technologies.

Inhalation lactose is the primary sugar present in milk and the main energy source to a newborn mammalian through its mother′s milk. 
Inhalation lactose is digested by the intestinal lactase (EC 3.2.1.108), an enzyme expressed in newborns. 
The enzyme′s activity declines following weaning which can lead to lactose intolerance in adult mammals.

A suspension of a-lactose monohydrate crystals in a lactose solution is atomized and dried in a spray drier. 
Approximately 10–20% of the total amount of lactose is in solution and the remaining 80–90% is present in the crystalline form. 
The spray-drying process predominantly produces spherical particles. 

The compactibility of the material and its flow characteristics are a function of the primary particle size of the lactose monohydrate and the amount of amorphous lactose.
Inhalation lactose is a reducing sugar. 
The amorphous lactose, which is the most reactive form of lactose present in spray-dried lactose, will interact more readily than conventional crystalline grades. 

Typical reactions include the Maillard reaction with either primary or secondary amines.
Inhalation lactose should be stored in a well-closed container in a cool, dry place.
Inhalation lactose are specifically developed for dry powder inhalation (DPI) applications. 

Kerry’s unique processing also maintains the crystallinity of the lactose, which can be a critical factor when formulating DPI’s.
Kerry has a long, and well established history of supplying world class lactose, mainly for oral solid dose & capsule filling applications. 
There is however, a growing demand for lactose that is suitable for developing dry powder inhalers.

The processing techniques used in the production of inhalation lactose, such as sieving, milling, and micronization, allow manufacturers to tailor its properties to specific inhaler devices and drug formulations. 
Each grade, whether coarse or fine, is designed to meet different aerodynamic and dispersion requirements.

Beyond its functional performance, inhalation lactose is chemically inert, non‑toxic, and compatible with a wide variety of active pharmaceutical ingredients, which further supports its widespread use. 
It does not undergo significant chemical changes during processing or storage, which is essential for maintaining the integrity of sensitive drug compounds.

One of the most important characteristics of inhalation lactose is its controlled surface energy. 
The surface energy influences how drug particles adhere to or detach from the carrier during aerosolization. 
A surface that is too smooth or has too low energy might not retain drug particles well during handling, leading to segregation and inconsistent dosing. 

Conversely, a surface with excessively high energy could retain the drug too strongly, preventing efficient detachment in the inhaler device. 
Manufacturers carefully control this property to achieve the right balance, often by selecting specific crystallization methods and drying techniques.

Another crucial aspect is the absence of contaminants. 
Even trace levels of impurities, endotoxins, or microbial residues can pose a risk in inhalation products, which directly reach sensitive lung tissues. 
Therefore, inhalation lactose undergoes additional purification and testing beyond what is required for lactose used in other dosage forms. 

This includes strict monitoring of heavy metals, microbial load, and residual solvents.
From a mechanical perspective, the flowability and compressibility of inhalation lactose are critical for the manufacturing process. 
In dry powder Inhalation lactose formulations, good flow ensures uniform mixing with the active drug and consistent filling of inhaler capsules or reservoirs. 

Poorly flowing powders could lead to dose variability or clogging in automated filling machines. 
Coarse lactose grades typically improve flow, while fine lactose fractions enhance drug detachment during inhalation. 
Many formulations use a mixture of these grades to optimize both manufacturing and performance.

Inhalation lactose also undergoes rigorous stability testing under various temperature and humidity conditions. 
Since Inhalation lactoses are often stored for extended periods, it is essential that the excipient does not undergo polymorphic changes, amorphization, or moisture-induced degradation that could alter its performance. 

The monohydrate form of lactose is particularly valued because its crystalline water contributes to structural stability, preventing unwanted phase transitions under normal storage conditions.
Furthermore, the interaction between inhalation lactose and different active pharmaceutical ingredients (APIs) is a key consideration. 

Inhalation lactose with varying surface properties, charges, and hydrophobicity respond differently to the carrier.
Formulators often choose specific lactose grades to maximize drug‑carrier compatibility and ensure reproducible aerosolization profiles.

Finally, inhalation lactose has a long track record of clinical safety. 
Its widespread use in commercially available inhalers over decades provides strong evidence of its biocompatibility. 
Because it is a naturally occurring sugar, it is metabolized and cleared efficiently by the body, minimizing the risk of accumulation or adverse reactions.

Uses Of Inhalation lactose:
Inhalation lactose is used as a carrier and stabiliser of aromas, pharmaceutical products, Food industry.
Inhalation lactose is widely used as a binder, filler-binder, and flow aid in direct compression tableting.

Inhalation lactose is primarily used as a carrier excipient in dry powder inhaler (DPI) formulations, where it plays a crucial role in improving the delivery of finely micronized drug particles to the lungs. 
The active pharmaceutical ingredients (APIs) used in DPIs are typically extremely small, often with aerodynamic diameters less than 5 micrometers, which makes them prone to aggregation due to high surface energy. 

Inhalation lactose provides a larger, inert surface for these particles to adhere to, ensuring uniform dispersion during manufacturing, storage, and handling.
When the patient inhales through the device, the airflow and turbulence cause the drug particles to detach from the lactose carrier and travel deep into the respiratory tract, achieving efficient deposition in the lower lungs where therapeutic action is required.

Beyond its role as a carrier, inhalation lactose is also used to enhance the flow properties of dry powder formulations.
Many micronized drugs have poor flowability, which can cause difficulties in accurate dosing, capsule filling, or reservoir loading during the manufacturing process. 
By blending with carefully engineered lactose particles, the overall powder blend gains better flow characteristics, reducing dose variability and ensuring reproducible delivery of the medication.

Another important use of inhalation lactose is its function as a spacer and stabilizer in DPI blends. 
Inhalation lactose separates individual drug particles, preventing them from sticking together or forming large aggregates that could compromise aerosolization. 
This physical separation is especially critical during storage because it minimizes changes in the formulation’s properties over time, preserving both the stability of the drug and the consistency of its delivery performance.

Inhalation lactose is also utilized to optimize the aerodynamic behavior of the inhaler system. 
The size and density of the lactose particles are selected to ensure that they mostly deposit in the upper respiratory tract and are not carried deep into the lungs. This design allows the carrier to serve its purpose of transporting and releasing the drug without itself contributing to lung deposition, thereby reducing unnecessary exposure to excipient particles.

Furthermore, it is used in various therapeutic areas where pulmonary delivery is required, including the treatment of asthma, chronic obstructive pulmonary disease (COPD), cystic fibrosis, and other respiratory disorders. 
Inhalation lactose is also applied in delivering certain antibiotics, antifungals, and even systemic therapies through the pulmonary route, as this pathway provides rapid absorption and avoids first‑pass metabolism.

In addition to these functions, inhalation lactose has technological uses during product development and device optimization. 
Formulation scientists use different lactose grades—ranging from coarse carriers to fine and micronized fractions—to fine‑tune drug release, dispersion behavior, and device compatibility. 
Some formulations incorporate engineered lactose particles with tailored surface properties to achieve a more controlled and predictable drug detachment process.

Inhalation lactose extend far beyond simply acting as an inert filler; it is an essential functional component that enables the reliable, efficient, and safe delivery of medications to the lungs, while supporting the complex requirements of modern inhalation therapy devices.
Inhalation lactose also serves several specialized roles in the broader context of pulmonary drug delivery, making it indispensable in the formulation of inhalation products. 

One of its extended uses is in the enhancement of drug bioavailability for medications delivered via the lungs. 
By facilitating the proper dispersion of active ingredients, it ensures that a greater proportion of the drug reaches its intended site of action, improving therapeutic outcomes while reducing the required drug dose. 
This results in fewer side effects and more efficient treatment regimens, which is particularly valuable in chronic respiratory conditions where patients rely on daily inhalation therapies.

Another notable use of inhalation lactose lies in its ability to modify the aerodynamic performance of dry powder inhalers. 
The physical characteristics of the lactose particles, such as their shape, roughness, and porosity, can be tailored to control how easily drug particles detach during inhalation. 
For example, rougher or slightly irregular lactose particles may enhance drug adherence during storage but release the drug more efficiently under the shear forces generated during inhalation. 

This tunability allows manufacturers to design inhalation products that perform consistently across a wide range of patient inhalation efforts and device designs.
Inhalation lactose is also commonly employed as a platform excipient in research and development of new inhalation therapies. 

Its extensive history of regulatory approval, safety data, and predictable behavior in inhalation devices makes it the preferred starting point for developing novel drug formulations. 
Researchers often use lactose carriers to test new active ingredients, new inhalation devices, and new particle engineering techniques because it provides a well‑characterized and stable baseline for comparisons.

Additionally, it plays a significant role in extending the shelf life of inhalation formulations. 
The crystalline structure of lactose monohydrate contributes to the stability of the entire powder blend by reducing the risk of moisture uptake and preventing amorphous transitions that could lead to clumping or changes in particle size distribution. 
This stability ensures that the inhaler device continues to deliver the correct dose even after long periods of storage, which is crucial for products distributed globally and stored in varying environmental conditions.

Inhalation lactose is also utilized in combination therapies, where multiple drugs with different particle sizes or physicochemical properties are incorporated into a single inhalation product. 
In such cases, different lactose grades can be combined or modified to ensure that each active ingredient is appropriately dispersed and delivered to its target region within the lungs. 
This is particularly useful in the treatment of diseases like asthma or COPD, where patients often require both bronchodilators and anti-inflammatory agents within the same inhaler.

Safety Profile Of Inhalation lactose:
Inhalation lactose is widely used in pharmaceutical formulations as a diluent in oral capsule and tablet formulations. 
Inhalation lactose may also be used in intravenous injections.
Adverse reactions to lactose are largely due to lactose intolerance, which occurs in individuals with a deficiency of the enzyme lactase.

The hazards of inhalation lactose are generally considered low because it is a naturally occurring sugar (α‑lactose monohydrate) that is widely regarded as safe for pharmaceutical use. 
However, as with many inhaled substances, there are certain risks and considerations associated with its handling, manufacturing, and use in inhalation products.

One potential hazard is related to inhalation of large quantities of lactose dust during production or processing. 
In occupational settings, workers exposed to airborne lactose powder may experience irritation of the respiratory tract, throat, and nasal passages. 
Prolonged exposure to high concentrations of dust can lead to symptoms such as coughing, sneezing, and shortness of breath, particularly in individuals with pre-existing respiratory conditions such as asthma. 

Therefore, manufacturing environments require the use of dust control measures, local exhaust ventilation, and personal protective equipment like masks or respirators to minimize inhalation risks.
Another hazard is the possibility of allergic reactions. 

Although rare, some individuals may have lactose hypersensitivity, which can manifest as respiratory irritation, skin reactions, or other allergic responses when exposed to lactose particles. 
Unlike lactose intolerance, which involves digestive symptoms due to the inability to metabolize lactose, allergic reactions involve the immune system and may occur even with minimal exposure in sensitive individuals.