MEGGLE pharmaceutical grade lactose as filler-binder

High functionality pharmaceutical excipients play an increasingly prominent role in modern dosage formulations. Choice of precisely targeted excipients allows manufacturers to overcome API deficiencies such as poor solubility, bioavailability or functional performance.

MEGGLE uses crystallization, spray drying, agglomeration, sieving, milling and micronization to process a very wide range of lactose monohydrate powder grades for the pharmaceutical industry to support the whole spectrum of pharmaceutical applications, including wet and dry granulation, direct compression tableting, capsule or sachet filling and dry powder inhalation.

Application & processing of pharmaceutical lactose

Lactose disaccharide, also called ‘milk sugar; occurs naturally as a simple carbohydrate in mammalian milk. Chemically, lactose is composed of molecules of D-galactose and D-glucose. It can exist in either alpha lactose and beta isomeric forms (a-lactose or b-lactose).

In the pharmaceutical industry, lactose is one of the oldest and still widely used filler and diluent in tablets and capsules, due to its inherent advantages like low hygroscopicity, water solubility, and compatibility with active ingredients, coupled with excellent physical and chemical stability.

The chemical and physical stability of crystalline lactose monohydrate powdered lactose makes it highly suitable for oral pharmaceutical applications, with versatile properties for binding or filling, compressibility and global availability.

Functions of lactose

Principal lactose uses are as excipients (filler or filler-binder) in production of pharmaceutical tablets and capsules. They are also useful as diluents in dry-powder inhalation (DPI) formulations and in baby feed formulas or freeze-dried products.

Pharmaceutical lactose plays an important role as binder, carrier and filler and can be used in a wide field of industrial applications like traditional wet and dry granulation (roller compaction), direct compression (DC), spheronization, manufacturing of parenterals or dry powder inhalation (DPI).

Lactose occurs in different forms, with crystalline, thermodynamically most stable alpha-lactose monohydrate (“tomahawk-shaped” crystals) and lactose anhydrous (“kite-like” crystals) as the most frequently used polymorphs.

Additionally, amorphous lactose, a mixture of α-, and ß-anomer, has been revealed as advantageous in introducing plasticity into spray-dried lactose and other pharma grade lactose products. While theoretically equivalent in basic chemistry, various lactose pharma grades show distinct differences in their physical performance.

Pharma grade lactose types

Meggle’s lactose range comprises of different product groups with more than 20 specialty grades, covering all areas from solid dosage forms, dry powder inhalations and parenteral dosage forms. These grades are sub-divided into seven types:

• Sieved Lactose: Alpha lactose monohydrate is derived from re-crystallization of lactose solution. This results in formation of tomahawk shaped crystals. Narrow fractionation of these randomly sized lactose crystals results in coarse sieved grades. Meggle’s sieved alpha-lactose monohydrates, including PrismaLac 40, CapsuLac 60, SacheLac 80, and SpheroLac 100, are inherently free flowing in nature with low Carr’s and flowability indices, making them suitable for capsule, sachet filling and powder triturates.
• Milled Lactose: The tomahawk shaped crystals of lactose when milled, results in the formation of finer sharper-edged particles that have poor flow but show good binding and compaction properties due to their small particle size and high specific surface area. These grades, such as GranuLac 70, GranuLac 140, GranuLac 200, GranuLac 230, and SorboLac 400, are therefore especially useful in wet and dry granulation.
• Spray Dried Lactose: With spray-dried lactose, rapid water evaporation causes the formation of 10-15% amorphous lactose depending on the solids content and process conditions. Unlike alpha-lactose monohydrate which is known to exhibit brittle fracture during compaction, amorphous lactose deforms plastically. Due to the synergistic plastic and brittle nature of spray-dried lactose, it exhibits superior compactibility. The spherical nature of Meggle’s FlowLac 90 and FlowLac 100 is attributed to spray-drying of fine milled alpha-lactose monohydrate suspension. This morphology along with the particle size distribution makes FlowLac the best flowable lactose amongst all the grades.
• Agglomerated Lactose: Agglomerated lactose is developed by combining the good flow of coarse lactose and good compactibility of fine powder grade. This grade is manufactured by wet granulation process by spraying water on fluidized fine particles of lactose monohydrate. This creates liquid bridges which bring the particles together. Upon drying, the excess water is evaporated and the bridges are maintained resulting in a very stable, non-hygroscopic alpha lactose monohydrate with no amorphous lactose. Meggle’s agglomerated lactose grades are marketed as Tablettose 70, Tablettose 80, and Tablettose 100.
• Anhydrous Lactose: Roller / Drum drying of concentrated lactose solution above 93.5°C results in the formation of anhydrous lactose in the ratio of 80% beta and 20% alpha form. Anhydrous beta lactose is more brittle as compared to alpha lactose monohydrate and hence is well suited for direct compression and roller compaction. On compaction, DuraLac H fragments and exposes clean surfaces with numerous binding sites, for more robust tablets in DC process. DuraLac H is also recommended for dry granulation, retaining its compactibility after the initial slugging step.
• Lactose Monohydrate Low Endotoxin: Lactose is widely used in lyophilized processes as bulking agent in parenterals or for isotonic laboratory reagents. During lyophilization it prevents protein denaturation and aggregation to improve API stability. Furthermore Lactose Monohydrate Low Endotoxin is stable in virtually all common sterilization techniques and resistant to low and high pH values. Meggle offers Lactose Monohydrate, Low Endotoxin grade with an endotoxin limit of NMT 5 EU/g.
• Lactose Monohydrate for Inhalation: Dry powder inhalers (DPI) are widely used in pulmonary drug delivery due to their ease of handling, portability, small size and no requirement of breath-actuation co-ordination. The carrier used in DPI formulations not only acts as a filler but also plays an important role in deposition of drug into the lungs. Lactose is the most used carrier in DPIs owing to the fact that it is inert, has a well-established safety profile and is accepted by regulatory and medical authorities. MEGGLE manufactures InhaLac® inhalation grade lactose by a two-step crystallization process to give preliminary lactose monohydrate with stringent microbial limits and endotoxin limit of less than 5 EU/g. The lactose is then either sieved (InhaLac® 70, InhaLac®  120, InhaLac®  160, InhaLac®  230, InhaLac®  251), milled (InhaLac®  400, InhaLac® 140, InhaLac® 150, InhaLac® 300,) or micronized (InhaLac®  500) to give different InhaLac®  grades to cater to specific customer needs.

Resources

Click on MEGGLE lactose product configurator for detailed product information and applications.
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