The diluent can affect the formability and formulation properties of the formulation (such as powder flowability, wet granule or dry granule formability, content uniformity, disintegration, dissolution, tablet appearance, tablet hardness and friability, Physical and chemical stability, etc.). Some diluents (such as microcrystalline cellulose) are often used as dry binders because they give the tablet high strength during the final compression.
The main purpose is to increase the weight and volume of the tablet. For the convenience of application and production, the diameter of the tablet is generally not less than 6mm, and the total weight of the tablet is generally not less than 100 mg. Therefore, when the dose of the drug is less than 100 mg, it is often necessary to add a diluent. The addition of diluent not only guarantees a certain volume, but also reduces the deviation of the dosage of the main components, and improves the compression molding of the medicine. When the medicine of the tablet contains oily components, an absorbent should be added to absorb the oily substance to keep it in a "dry" state so as to facilitate the manufacture of tablets.
Corn starch is more commonly used, its properties are very stable, it does not work with most drugs, the price is relatively cheap, the hygroscopicity is small, the appearance is good, and in actual production, it is often used with powdered sugar, The mixed use of dextrin is because the compressibility of starch is poor. If used alone, the pressed tablets will be too loose.
Powdered sugar refers to the white powder formed by low-temperature drying and crushing of crystalline sucrose. Storage will make the tablets too hard and difficult to disintegrate or dissolve. Except for the buccal tablets or soluble tablets, they are generally not used alone. They are often used in combination with dextrin and starch.
It is the general name of starch hydrolysis intermediate products. Its water-soluble matter is about 80%. It dissolves slowly in cold water, and is more soluble in hot water and insoluble in ethanol. It is also known as high paste (high viscosity dextrin), that is, it has strong adhesiveness. Improper use will cause pitting, watermark on one side or cause the tablet to disintegrate or dissolve slowly; for the same reason, in the content determination If it is not sufficiently crushed and extracted, it will affect the accuracy and reproducibility of the measurement results. Therefore, dextrin is rarely used as a bulking agent alone, and it is often used in combination with powdered sugar and starch.
Commonly used crystalline lactose containing one molecule of water (i.e. n-hydrous lactose), non-hygroscopic, good compressibility, stable properties, does not chemically react with most drugs, and the pressed tablets are smooth and beautiful; made by spray drying method Lactose is non-crystalline lactose, which has good fluidity and compressibility and can be used for direct compression of powder.
Compressible starch is a partially pregelatinized product (fully pregelatinized starch is also called d-starch). This product is a multi-functional auxiliary material, can be used as a filler, has good fluidity, compressibility, self-lubricity and dry adhesion, and has a good disintegration effect. 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 with a small degree of polymerization obtained by partial hydrolysis of cellulose. It has good compressibility and strong binding force. The compressed tablet has a large hardness and can be used as a powder. The "dry adhesive" for direct compression is used.
Mainly some inorganic calcium salts, such as calcium sulfate, calcium hydrogen phosphate and medicinal calcium carbonate (prepared by the sedimentation method, also known as sedimented calcium carbonate) and so on. Among them, calcium sulphate is more commonly used. Its properties are stable, odorless and tasteless, slightly soluble in water, and compatible with a variety of drugs. The tablets made are smooth in appearance, good in hardness and disintegration, and have no adsorption effect on drugs. Calcium sulfate dihydrate is often used in tablet excipients. However, it should be noted that calcium sulfate interferes with the absorption of certain main drugs (tetracycline drugs) and should not be used at this time.
It is in the form of granules or powder, which absorbs heat when it dissolves in the mouth, so it has a cool feeling and has a certain sweetness at the same time.
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