Posted: February 1st, 2023

Ideal excipient properties and their roles

Excipients can range from inert and simple compounds to active and complicated substances that can be difficult to classify. Excipients, such as corn, wheat, sugar, and minerals, were traditionally structurally simple, biologically inert, and natural. Excipients’ inert and harmless nature is no longer a given feature in medication formulations. At therapeutic levels, excipients should be safe in humans. Excipients serve various purposes, including assisting in the processing of the drug delivery system throughout production, protect, support, improve patient tolerance, bioavailability, and stability. It assists in the identification of products and improves any aspect of overall safety. It assists in the drug’s efficacy and distribution. It assists in keeping the medication product’s integrity during storage. The ideal properties include easy availability, thermostability, pharmaceutical acceptability, non-toxicity, inert physically, chemically, and therapeutically.

Excipients are classified into several functional types based on the role they are supposed to play in the final formulation. They are mainly classified as tablet excipient and liquid/suspension excipient.

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Tablet excipients types
Excipients used in tablet dosage forms are as follows:

Diluents: Diluents are fillers that are used to give the tablet its bulk form. The diluent is chosen based on various factors, including the manufacturers’ experience with different tablet preparations, cost, and compatibility with other formulation ingredients. A calcium salt, for example, should not be used as a diluent in the production of tetracycline antibiotic tablets or capsules because calcium interferes with antibiotic absorption from the gastrointestinal (GI) tract. Diluents are classified further based on their chemical nature as organic and inorganic diluents and solubility as water-soluble and water-insoluble diluents. Lactose-anhydrous and spray-dried lactose, microcrystalline cellulose, hydrolyzed starch, sucrose, sorbitol, and mannitol are examples of diluents.

Binders: These are the dry powders or liquids that are used to improve cohesion during wet granulation. It gives the tablet mechanical strength. Cellulose, methylcellulose is, e.g., for powder binders and gelatine, polyethylene glycol (PEG), sucrose, starch are examples for solution binders.

Disintegrants: These are included in the formulation. They break down the dosage form into smaller fragments when it comes into contact with the liquid; these tiny fragments have a larger surface area, increasing the drug’s solubility. Various mechanisms are proposed for disintegrations, like repulsion where the tablet comes into contact with the liquid. The liquid enters into the tablet’s pores and breaks it into fragments. In deformation, the pill comes into contact with water and expands and ruptures into small fragments. Starch, cellulose, and starch derivatives are some examples.

Lubricant and glidants: Lubricants are used to prevent tablet materials from adhering to the surfaces. These decrease inter-particle friction and enhance the tablet granulation flow. Stearic acid, stearic acid salt, talc, magnesium stearate, surfactants, and polyethylene glycols are examples of lubricants. Glidants are designed to reduce friction between granules or powder materials, allowing them to freely flow. 5-10% concentrated corn starch, silica derivatives, colloidal silicas, aerosol, and syloid are examples of glidants.

Posted: February 1st, 2023

Ideal excipient properties and their roles

Excipients can range from inert and simple compounds to active and complicated substances that can be difficult to classify. Excipients, such as corn, wheat, sugar, and minerals, were traditionally structurally simple, biologically inert, and natural. Excipients’ inert and harmless nature is no longer a given feature in medication formulations. At therapeutic levels, excipients should be safe in humans. Excipients serve various purposes, including assisting in the processing of the drug delivery system throughout production, protect, support, improve patient tolerance, bioavailability, and stability. It assists in the identification of products and improves any aspect of overall safety. It assists in the drug’s efficacy and distribution. It assists in keeping the medication product’s integrity during storage. The ideal properties include easy availability, thermostability, pharmaceutical acceptability, non-toxicity, inert physically, chemically, and therapeutically.

Excipients are classified into several functional types based on the role they are supposed to play in the final formulation. They are mainly classified as tablet excipient and liquid/suspension excipient.

Don't use plagiarized sources. Get Your Custom Essay on
Ideal excipient properties and their roles
Just from $13/Page
Order Essay

Tablet excipients types
Excipients used in tablet dosage forms are as follows:

Diluents: Diluents are fillers that are used to give the tablet its bulk form. The diluent is chosen based on various factors, including the manufacturers’ experience with different tablet preparations, cost, and compatibility with other formulation ingredients. A calcium salt, for example, should not be used as a diluent in the production of tetracycline antibiotic tablets or capsules because calcium interferes with antibiotic absorption from the gastrointestinal (GI) tract. Diluents are classified further based on their chemical nature as organic and inorganic diluents and solubility as water-soluble and water-insoluble diluents. Lactose-anhydrous and spray-dried lactose, microcrystalline cellulose, hydrolyzed starch, sucrose, sorbitol, and mannitol are examples of diluents.

Binders: These are the dry powders or liquids that are used to improve cohesion during wet granulation. It gives the tablet mechanical strength. Cellulose, methylcellulose is, e.g., for powder binders and gelatine, polyethylene glycol (PEG), sucrose, starch are examples for solution binders.

Disintegrants: These are included in the formulation. They break down the dosage form into smaller fragments when it comes into contact with the liquid; these tiny fragments have a larger surface area, increasing the drug’s solubility. Various mechanisms are proposed for disintegrations, like repulsion where the tablet comes into contact with the liquid. The liquid enters into the tablet’s pores and breaks it into fragments. In deformation, the pill comes into contact with water and expands and ruptures into small fragments. Starch, cellulose, and starch derivatives are some examples.

Lubricant and glidants: Lubricants are used to prevent tablet materials from adhering to the surfaces. These decrease inter-particle friction and enhance the tablet granulation flow. Stearic acid, stearic acid salt, talc, magnesium stearate, surfactants, and polyethylene glycols are examples of lubricants. Glidants are designed to reduce friction between granules or powder materials, allowing them to freely flow. 5-10% concentrated corn starch, silica derivatives, colloidal silicas, aerosol, and syloid are examples of glidants.

 

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