Application Of Microcrystalline Cellulose in Pharmaceutical
Microcrystalline cellulose (MCC), the main component is a linear polysaccharide bound by β-1,4-glucosidic bonds, is a free-flowing natural cellulose hydrolyzed to the limit degree of polymerization (LODP) by dilute acid. Very fine short rod-like or powder-like porous particles, composed of white, odorless, tasteless crystalline powder.
In general plant fibers, microcrystalline cellulose accounts for about 70%, and the other 30% is amorphous. In view of the unique structure and properties of microcrystalline cellulose, it is widely used as a disintegrant, a stable emulsifier, etc. in the national economic sectors such as medicine and health, food and beverage, and light chemical industry.
Because cellulose widely exists in nature, hundreds of billions of tons of cellulose-rich biomass residues can be produced every year in the world. If these residues are well transformed and utilized, they will be a rich resource. In China, the expansion of the production scale of tanning, daily chemicals, medicine, food, and chlor-alkali industries and the improvement of product grades have increased the demand for microcrystalline cellulose year by year, so microcrystalline cellulose has broad market prospects. Internationally, microcrystalline cellulose has been included in the US FDA Evaluation of Food Additive Safety Index (GRAS), approved as a food additive in Europe, and included in the FDA's "Inactive Ingredients Guide", and approved in the United Kingdom for non-injectable preparations.
Microcrystalline cellulose is commonly used as adsorbent, suspending agent, diluent, disintegrant. Microcrystalline cellulose is widely used in pharmaceutical preparations, mainly used as diluent and binder in oral tablets and capsules, not only for wet granulation but also for dry direct compression. There is also some lubrication and disintegration, which is very useful in tablet preparation.
Due to the existence of hydrogen bonds between the molecules of microcrystalline cellulose, the hydrogen bonds are associated when pressed, so it has a high degree of compressibility and is often used as a binder; after the compressed tablet encounters a liquid, the moisture quickly enters the microcrystalline cellulose containing microcrystalline cellulose. In the tablet of crystalline cellulose, the hydrogen bond is broken immediately, so it can be used as a disintegrant. Therefore, it is a widely used excipient in tablet production, which can improve the hardness of the tablet. For example, in the preparation of rifampicin tablets, microcrystalline cellulose and starch (mass ratio of 6.25:1) and various raw materials can be mixed uniformly and directly compressed, and the product disintegrates into a mist within 1 minute. Moreover, the content remains unchanged within the validity period, and the drug stability can be well improved. Another example, due to the addition of microcrystalline cellulose, the dissolution rate of prednisone acetate and berberine acetate (berberine hydrochloride) tablets increased to more than 80%. There is no need to go through the traditional granulation process when using microcrystalline cellulose as an auxiliary material for tableting. For example, in the preparation of Kebiqing tablets, the microcrystalline cellulose is added, which solves the serious stickiness caused by the easy moisture absorption of Kebiqing wet granulation tablets. rush phenomenon, and disintegrate rapidly.
Microcrystalline cellulose can also be used as a sustained release agent for pharmaceuticals. The sustained release process is the entry of the active substance into the porous structure of the carrier. The active material is contained by intermolecular hydrogen bonds, and the active material is fixed after drying. When the active substance is released, due to the swelling caused by the diffusion of water in the capillary system of the polymer carrier, the bond between the carrier via the base and the fixed active substance is destroyed, and the active substance is slowly released.
Microcrystalline cellulose powder can form a stable dispersion system in water, and it can be mixed with medicine to make creamy or suspended medicine liquid, and can also be used as capsule. Microcrystalline cellulose is gelatinized by vigorous stirring in water, and can also be used to manufacture paste and suspension type pharmaceutical preparations.
