Selection of excipients during tableting

Starch

The most commonly used is corn starch, which is of a nature and stability and does not work with most drugs, with a water content of 6% to 8%. In actual production, it is often mixed with powdered sugar and dextrin which are more compressible, because the compressibility of starch is poor, and when used alone, the pressed tablet is too loose.

Incompatibility: Some drugs with strong acidity are not suitable for use as a filler, because wet particles can partially hydrolyze starch during the drying process, affecting the quality of the tablets.

Sugar powder (Sucrose) refers to the white powder of crystalline sucrose after low-temperature drying and pulverization. It has strong adhesion and can be used to increase the hardness of the tablet, making the surface of the tablet smooth and beautiful, but due to the powdered sugar. The hygroscopicity is relatively strong, and long-term storage may make the hardness of the tablet too large, and it is difficult to disintegrate or dissolve.

Note: In addition to buccal tablets or soluble tablets, it is generally not used alone, often in combination with dextrin and starch.

Dextrin

Dextrin is a general term for starch hydrolyzed intermediates, and has strong cohesiveness. Improper use may cause pitting on the surface, watermarking, or disintegration or dissolution of the tablet; if insufficient in content determination The pulverization extraction will affect the accuracy and reproducibility of the measured results, so it is rarely used in large quantities, often in combination with powdered sugar and starch.

Incompatibility: Dextrin is weaker than sugar powder and is not suitable for fibrous powder.

Lactose

It is an excellent filler. It is usually used to contain lactose with a crystal water. It has no hygroscopicity, good compressibility and fluidity. The pressed tablet has a smooth and beautiful surface and a good drug dissolution rate. The tablet is exposed to the air and is not easy to absorb moisture and loose, which is convenient for packaging. The disintegration time of the tablets is not delayed during storage.

Incompatibility: Lactose as a tablet excipient, such as a tablet that is compressed with an amine drug, will appear brownish yellow for a long time. If the prescription contains tartrate, citrate or acetate at the same time, or under the influence of an alkaline lubricant, it can accelerate the color change reaction, and should be paid attention to when using it.

Compressible starch

It can also be called pre-gelatinized starch, which is obtained by partial hydrolysis of starch. One part is intact starch granules, and the other part is spheroids which are hydrolyzed and denatured. It is a multi-functional excipient with good fluidity, compressibility, self-lubricity and dry adhesion, and has good disintegration.

Note: If it is used for direct compression of powder, the amount of magnesium stearate should not exceed 0.5% to avoid softening effect.

Microcrystalline cellulose (MCC)

Microcrystalline cellulose is a crystalline cellulose which is partially hydrolyzed to obtain a small degree of polymerization, and has good compressibility, and has the functions of adhesion, flow aid, disintegration and the like. Microcrystalline cellulose is plastically deformed during the pressurization process, and combined with capillary action, it is easy to introduce water into the interior to destroy the bonding force between the particles, and promote the disintegration of the film. Tablets generally contain 20% microcrystalline cellulose and disintegrate better.

Note: For alkaline stearate lubricants, if the dosage is higher (above 0.75%) and the mixing time is longer, the tablet may soften and may affect disintegration or dissolution.

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