Application of D-trehalose|CAS:6138-23-4| in the field of pharmaceutical preparations

D-trehalose（CAS:6138-23-4） is an organic compound with a molecular formula of C₁₂H₂₂O₁₁·2H₂O and a molecular weight of 378.3. Trehalose has stable biofilm and protein structure, and is mainly used in the protection of biological products, such as genetically engineered enzymes and other enzymes, cell membranes, antibodies, antigens, organelles, etc. A kind of metformin hydrochloride sustained-release tablet composition is introduced in CN112972411B patent, and the technical scheme is as follows:

In this patent, the metformin hydrochloride multi-unit sustained-release tablet composition contains three parts: a plain pill core, a coating layer and a filler:

Plain pill core: 50.0 parts of metformin hydrochloride, 13.2 parts of D-trehalose, 0.8 part of hypromellose;

Coating layer: 19.8-20.5 parts of D-trehalose, 4.8-5.5 parts of ethyl cellulose Surelease® 174 (Surelease® 174 for short), 0.8 part of magnesium stearate;

Filler: 10.0 parts of microcrystalline cellulose;

(The parts mentioned above are mass percentages)

In the process of preparing the core of the plain pill, D-trehalose is used as the filler of the plain pill. When the pellet coating is dried, D-trehalose tightly wraps the adjacent main drug, forming a carbohydrate glass body similar in structure to glass-like ice, so that the main drug maintains a certain spatial structure. In addition, the above scheme improves the porosity of the plain pill, increases the yield pressure, and avoids the rupture of the coating film caused by the poor deformation of the pill core during the tableting process.

The invention provides a metformin hydrochloride multi-unit sustained-release tablet that meets clinical needs, and overcomes the problem of easy rupture of the ethyl cellulose film coating.

References

CN112972411B A kind of metformin hydrochloride sustained-release tablet composition.