MEGGLE Lactose Monohydrate Low Endotoxin (LE) for Inhalation and Parenteral applications

The latest product from pharmaceutical excipients specialist MEGGLE is Lactose LE, a Lactose Monohydrate Low Endotoxin sieved product.

This is a formulation of exceptional microbiological purity that takes advantage of lactose’s well-known protective properties in freeze-dried (lyophilized) or spray-dried parenteral products to make it highly suitable for inhalation, and parenteral applications. Lactose LE is therefore also useful as a protective and bulking agent in formulations for temperature-sensitive products.

Lactose as protective and bulking agent

Lactose as a Dissacharide can be used as a protectant during drying processes where protection of biological materials during spray-drying and freeze-drying is critical in preserving their integrity, functionality, and stability.

Cryo- and lyoprotectants or stabilizers provide molecular protection for sensitive ingredients that would otherwise be damaged by freezing or drying processes. Disaccharides like lactose, sucrose and trehalose are effective in this role through a ‘vitrification effect’ in which they form a glassy or amorphous matrix surrounding the biomolecules to stabilize them by reducing mobility and preventing crystallization and aggregation.

Moreover, lactose can replace water molecules through hydrogen bonds to the biological material, which reduces stress during drying and minimizes structural damage and denaturation of proteins and nucleic acids.

The glass transition temperature of amorphous lactose is lower than the one for trehalose, but higher than the one for sucrose. The high solubility of lactose, as well as its lower costs, provide additional advantages over trehalose. A further benefit of lactose is its well-established suitability for inhalation products.

Additives like leucine can also be used to further improve performance and stability.

Emphasizing microbiological purity

Unlike most MEGGLE products, Lactose LE is not produced to a target particle size distribution (PSD) but is supplied as ‘raw material’ for manufacturers who perform milling or fractionation to their own desired particle size.

Rather, MEGGLE has prioritized microbiological quality and minimized the endotoxin content to make Lactose LE ideal for use in inhalation and parenteral products. The product’s cryo- and lyoprotective properties have also proven advantageous in other applications, such as freeze- or spray-drying of sensitive APIs.

Very few excipients, suitable to stabilize products during lyophilization, are also approved by regulatory agencies for parenteral formulations, which must be proven safe, non-toxic, sterile, pyrogen-free, and particle-free. Notable, lactose is listed in the FDA Inactive Ingredient Database (IID) for parenteral and ophthalmic applications, with monitored β-Lactoglobulin (BLG) levels below LOQ (0.010 ppm).

Careful design of production processes and sourcing of raw materials gives Lactose LE a very low bioburden, making it well suited for the manufacturing of parenteral final dosage forms because market authorization holder is obliged to ensure sterility in its final dosage form.

It is entirely free of Salmonella, gramnegative bacteria, Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Burkholderia cepacia, with very low (NMT 10 cfu/g) total aerobic microbial count and combined yeasts and molds, and even lower in bacterial endotoxins (< 5 EU/g).

Resources

Click on Lactose Monohydrate Low Endotoxin (LE) from MEGGLE Excipients for further information