Lecture 1 Pharmaceutics terminology

Drug substance

active pharmaceutical ingredient (API) within a medication

• specific moiety (part) responsible for producing pharmacological activity and intended therapeutic effect

Drug substances are _______ administered alone

rarely

pharmaceutical excipient

inactive ingredients of a formulation

• generally considered to be all ingredients in a dosage form other than the active pjaramctuical ingredient (API)

Drug Product

This includes the

• drug substance

• inactive ingredients (excipients)

• packaging (and other elements that make the drug ready for patient use)

Binders

Help tablet contents stick together; provide stability and strenght→ help retain compaction

e.g: Starch paste (common binder)

Diluents and fillres

Increase bulk in liquids; aid in dissolution

• increase solubility in water

Disintegrants

Faciliatet tablet breakup after oral adminsitration to enable drug release 

• allow tablet to be broken down

  • e.g: helps breakdown whole tablet of acetaminophen throughout time in our GI tract

Flavors and Sweetners (Function)

Mask unpleasant taste/odor 

• make the drug more appealing

Sweetners

mask unpleasant taste/odor

e.g: Aspartme, Saccharin, Sucarlose, Glycerin, Dextrose, Sugar alcohols like Stevia

Colorant

• are appealing

• sometimes these are used to differentiate various doses of a drug

  • e.g: 2.5mg, 5mg dose, 10mg dose

  • another example: drugs colored in red, blue, or white→ not for fun but to help pt distinguish different doses

Preservatives

prevent microbial growth in formulation (and are also sometimes used in multi-dose and non-sterile preparations)

• ampoules→ single dosage form, vials→ multi-use dosage form

• Examples: Chlorohexidine (antiseptic), povidones, sodium benzoate, ****thimerosal

Thimerosal

contains mercury, used in some vaccines

• a BIG DEAL of debate because contains mercury!!!!

  • but manufacturers argue the amount of mercury in it is less than in a can of tuna

Coating Agents

**final step in the formulation process

• coat the surface of the tablet or formulation to protect drug against humidity, O2 from envt, or to simply mask bitter taste (of drug)

• also controls amount released into GI tract

• e.g: Cellulose acetate, gelatin, gluten

Humectants → Haribo

think “gummy bears”→ squishy nature, soft glossy surface

• helps retain moisture (preventing brittleness)

• e.g: Glycerin, glycol, Polyethylene glycol (PEG), hylauronic acid

Formulation

process of combining various chemical entities, including the active drug into final medicinal product

Key Components of Formulation

• select appropriate dosage form

• Combining active ingredient with excipients

• Ensuring stability, safety, efficacy

Dosage Form

• Drug + Excipients

• physical form in which a drug is produced and dispensed such as tablets, capsules, liquids, gels, or injectables 

• provides a safe, convenient, and accurate mechanism for delivering drug to patient 

• Delivers API → appropriate site in body 

• Enhanced patient compliance, drug stability, and therapeutic efficiency

The Need for Dosage Forms