Why DILACTOSE® is recommended filler for direct compression? Excipients 2021.08.31

Direct compression is a simple process of blending API with excipients and compressing the finished tablets without granulation process.
Therefore, it is economical in cost and is often selected while handling heat and moisture sensitive API.
Direct compression not only has above mentioned merits, but also has demerits.
Demerits can be covered during formulation design; however, selecting appropriate at filler at this stage is important.

Direct Compression has its own merits and demerits, like any other compression method.

1. Economical process (Cost reduction, less manufacturing space, time etc.) is possible by eliminating process (Granulation, drying, sieving).
2. Suitable for heat or moisture sensitive API as drying and granulation process is eliminated.

1. Difficult to ensure Content Uniformity
Finely powdered APIs generally have poor flowability and particles tend to stick to each other. In other words, miscibility of multiple ingredients is difficult.

It is easy to improve miscibility of ingredients in wet granulation method. When the ingredients are mixed well, it is possible to ensure content uniformity of API.

However, as direct compression method only consists of mixing ingredients and compressing, it is difficult to obtain content uniformity if appropriate excipients are not selected.

If the content uniformity cannot be ensured, the amount of the API and the disintegration time may differ for each tablet manufactured.

2. Poor Compactibility
Compactibility of ingredients impacts the finished tablets. If the compactibility is poor when the tablet is compressed, it is difficult to form tablet, and even if tablets are formed, it will crumble easily.
Tablets which crumble easily can be crushed during transportation. Having said that, even if compactibility is improved and tablets with hardness are obtained, it should disintegrate easily when taken.

Demerits of direct compression can be covered during formulation design. In most tablets, fillers make up a major portion by volume. In other words, fillers greatly influence quality of a tablet (content uniformity or compactibility). Therefore, choosing the right filler is important.

Compactibility and disintegration of granulated lactose differ depending upon granulation method.
・When manufactured using High Shear Granulation: Generally has poor compactibility.
・When manufactured using Spray Dry method: Excels in compactibility, however disintegration tends to become slower.
・When manufactured using Fluid bed granulation: Excels in both compactibility and disintegration.

An ideal excipient for direct compression improves miscibility of all raw materials and　maintains balance of conflicting properties (Compactibility and Disintegration).
Filler should have reasonable hardness while also easy to disintegrate.

We provide excipients that meet various needs. Among them is DILACTOSE®, which is lactose granulated using Fluid bed granulation and is suitable for direct compression.
There are 3 grades of DILACTOSE with different particle size and has following features that are useful for formulation design. Let us introduce it in brief.

・Well balanced between Compactibility and Disintegration

・Excellent Miscibility and Flowability
Even though the particle size for DILACTOSE® S and F is very fine, these products have excellent flowability. Our unique granulating method succeeded in granulating fine crystals of lactose which makes it possible to have excellent flowability.

・Excellent Stability
As the hygroscopicity of DILACTOSE is not as high as spray-dried lactose, the possibility of caking over time is low.

In other words, tablets with high hardness and fast disintegration can be obtained when DILACTOSE® is used as filler.