Discussion On The Role Of Lactose In Solid Preparations

Lactose has been used as a pharmaceutical excipient in the 1960s for more than 60 years. Now lactose has become a common basic excipient in solid preparations, and it occupies the forefront in the proportion of prescriptions. Lactose can occupy such an important position in preparation excipients. It is naturally formed by human beings through long-term practice and selection. So what role does lactose play in the preparation?

01 Excipients, Diluents

Lactose is added to solid preparations to increase weight and volume, and auxiliary drugs are provided to patients in a certain shape and fixed dose. If lactose is only recognized as an excipient in the preparation, it is undoubtedly far from enough.

02 Mixing Uniformity

Content uniformity is achieved through uniform mixing. Lactose is generally a relatively high proportion of ingredients in the prescription, which has a greater impact on mixing uniformity. Generally speaking, the better the fluidity, the easier it is to mix evenly. The shape of spray lactose and granule lactose particles is smaller Close to spherical shape can provide excellent fluidity; the smoother the surface of the particles, the better the fluidity. The smoother the surface of sieved lactose, it also has good fluidity. The fluidity of pulverized lactose is not as good as the above lactose. The closer the particle size and bulk density of lactose are to the bulk drug, the easier it is to mix evenly.

03 Loading Difference

In the production of tablets, capsules, granules, etc., the weight is generally determined indirectly through the filling volume. Powder particle size distribution, powder fluidity and powder compressibility are important factors affecting the difference in filling volume.

In terms of particle size distribution, lactose can achieve a narrow particle size distribution through certain processes, such as sieving lactose and spraying lactose, etc. In terms of fluidity, spraying lactose and granulated lactose can provide excellent fluidity and can adjust the particle size of lactose Diameter, shape, etc. to achieve good compressibility; lactose itself has poor hygroscopicity, which is also a favorable factor for achieving no significant difference in loading capacity.

04 Hardness

Lactose is a brittle material with good compactability and high hardness. Generally speaking, anhydrous lactose has the best compressibility, followed by sprayed lactose and crushed lactose; The smaller the particle size in the range, the better the compressibility.

05 Dissolution

Since lactose is a water-soluble substance, it naturally has a certain influence on the dissolution of the drug. The faster the lactose dissolves, the more favorable it is for the tablet to disintegrate, erode, or form water channels, so that the drug can be completely infiltrated in the water environment and accelerate the dissolution of the drug. Dissolution: Generally speaking, anhydrous lactose dissolves the fastest, followed by spray lactose, and then granular lactose. Under the same model, the smaller the particle size of lactose, the faster the dissolution rate.

06 Other

(1) Lactose has a certain sweetness of about 70% of sucrose, which can increase the compliance of patients, especially children; tablets compressed with lactose have a very good finish, giving people a beautiful visual experience and increasing the aesthetic feeling of patients when taking it.

• With the development of pharmaceutical technology, the application of lactose in preparations is not limited to solid oral preparations. It also acts as a freeze-drying protectant and diluent in mid-to-high-end preparations such as freeze-dried preparations and powder inhalation preparations.

Lactose is currently used as a basic pharmaceutical excipient and is widely used in preparations. Generally speaking, the role of lactose in solid preparations is to ensure the stable industrial production of preparations, which is an industrial function or a physical function. Its influence on dissolution and disintegration and its effect on freeze-dried preparations are a kind of pharmaceutical function. With the development of the times and the advancement of science and technology, more functions of lactose will be developed by people. It is believed that lactose can make more contributions to preparations in the future, let us wait and see.