Pharmaceutics Excipients Flashcards
What are excipients
Ingredients that are included in dosage forms not for therapeutic action
Can be to:
a. aid manufacturing process
b. protect, support, or enhance physical, chemical, and microbiological stability
c. Improve drug release, solubility, and bioavailability
d. Enhance patient acceptability
Sources of excipients
- Animals: Lactose, gelatin
- Plants: Starch, sugar, cellulose
- Minerals: Calcium phosphate, silica
- Synthesis: PEG, polysorbates
Safety of excipients
June 25, 1938 “Federal Food, Drug, and Cosmetic Act”
- All marketed drug products must be safe and pure
- Companies are required to submit a new drug application (NDA)
FDA GRAS
The FDA creates a list of excipients that they generally recognize as safe
Need to reapply for each new excipient or function
Ideal excipient properties
- Pharmacologically inactive
- Provide the desired functionality
- Non-toxic
- Compatible
- Stable and reproducible
- Cost effective
Possible adverse events while using GRAS excipients
- Used in unusually high quantities
- If administered in an inappropriate route
- If resulted in an unintended or excessive absorption
- If created sensitivity or toxicity in special populations
- Gluten
- Lactose intolerance
- Aspartame sweetener
Which excipients can be particularly problematic?
- Preservatives
- Antioxidants
- Sesame oil
- Coloring agents
- Lanolin
- Aspartame
- Methyl ester of phenylalanine
- Patients with phenylketonuria
Pharmacists’ responsibility regarding excipients
- Explain to patients and healthcare providers the purpose of the excipients
- What is the best product for the patient
- Is the adverse effect dur to excipients
- Is drug interaction or incompatibility due to excipients
Excipient vs Drug
Some excipients may have a drug role in some products
- PEG: Osmotic laxative
- Celluloses: Artificial tears, dry eyes
- Calcium carbonate: Antacid
- a-Tocopherol: Vitamin E
- Benzalkonium chloride: Local anti-infective
