Lecture 4

Question 1

Excipients are…

Answer 1

• components of a finished drug product other than the active pharmaceutical ingredient (API) and are added during formulation for a specific purpose.
• listed as inactive ingredients by FDA, but have well-defined functions in a drug product.”

Question 2

Excipients Examples

Answer 2

• Diluents
• Binders
• Disintegrants
• Lubricants
• Glidants
• Solubilizing Agents
• Colorants
• Sweeteners
• Flavors

Question 3

Diluents

Answer 3

• Select the diluent to have a similar particle size distribution to the granulation
or
• Make the granulation to a similar size of the diluent selected
• Should have good flow and binding properties

Question 4

Binders

Answer 4

• Binders are typically not used as an excipient in direct compression tablet formulations
• Binders are used in the manufacture of granules that are blended with other components and compressed/encapsulated
• May be used in solution, dry or a combination

Question 5

Disintegrants

Answer 5

• swell causing tablets to break apart

- ultimate goal is to aid in dissolution of the active drug substance

Question 6

Lubricants

Answer 6

• Prevent sticking of the blend to the compression punches and dies/encapsulator fillers
• Aid in ejection of the tablet from the die
• Can slow dissolution
• Reduce compressibility

Question 7

Glidants

Answer 7

• Improve flow by reducing inter-particulate friction

* these materials have poor flow and compressibility by themselves

Question 8

Solubilizing Agents

Answer 8

• Used to improve solubility/bioavailability of an API

Question 9

Color Additives

Answer 9

• Used in low concentrations for product identification

Question 10

Flavors

Answer 10

• For taste-masking
• Flavor selected based on drug taste and target population
• Used in low concentrations
• Flavors composed of many chemical

Question 11

Additional Agents

Answer 11

• Thickening/Suspending Agents
• Preservatives (mainly liquid products)
• Antoixidants/Chelating Agent (mainly liquid products)

Question 12

Excipient Safety Regulations

Answer 12

• Current FDA Guidance for a New Excipient (Ref. 2)
– Pivotal toxicology studies (assess pharmacological activity)
– Vary based on duration of use
– Additional requirements for pulmonary, injectable and topical
– Photosafety
– Exceptions: life saving therapies, pediatric use

Question 13

Excipient Examples for Intravenous - Ready To Use Solution

Answer 13

Forming an Acceptable Solution

• Vehicle (sterile water for injection)
• Cosolvents: ethanol, glycerin
• Buffer (acetate, citrate, phosphate)
• Tonicity Adjustment

Stability Theme

• Antioxidant
• Chelating agents
• Preservatives