Materials and Excipients II

Question 1

What else is included in addition to API in tablet formulations?

Answer 1

Coated in sugar - Palatability

Fillers - Inc size

Question 2

What else is included in addition to API in solution formulations?

Answer 2

Water, flavour, sweeteners - Palatability

Question 3

What else is included in addition to API in topical formulations?

Answer 3

Water, Viscose (enhancer) - To easily spread

Question 4

What else is included in addition to API in IV formulations?

Answer 4

Water, salts - Isotonic salt level balance compared to bloodstream

Question 5

What is used to provide bulk to formulations?

Answer 5

Fillers or diluents

Question 6

What should fillers be?

Answer 6

Inert (non-reactive), non-toxic, stable, cheap, good mechanical properties eg hard, tough

Question 7

Give an example of common diluents

Answer 7

Lactose and calcium salta

Question 8

Give examples of formulations containing fillers

Answer 8

Granules, tablets, powder-filled capsules

Question 9

Define disintegrants

Answer 9

Materials that aid breakdown of solid dosage forms

Question 10

How do disintegrants work?

Answer 10

Expand on contact with water, aid uptake of water

Question 11

Examples of formulations containing disintegrants

Answer 11

Tablets, effervescent tablets, powder-filled capsules

Question 12

Define lubricants

Answer 12

Added to tablets/capsule plugs to stop dosage form sticking to machinery

Question 13

Define glidants

Answer 13

Added to powder to aid flow

Question 14

Define binders

Answer 14

Polymer solutions in water aid adhesion of powders to form granules

Question 15

Define vehicle/base and give examples for IV, gels, suppositories

Answer 15

Liquid or semi-solid which a drug is contained eg:
IV - water/oil base (sc/im)
Gels - water, oils
Suppositories - fatty triglycerides

Question 16

Define thickener/viscosifiers

Answer 16

Enhance viscosity of liquid formulation (usually hydrophilic polymers) eg for topical gels

Question 17

Define solubility enhancers and give examples

Answer 17

Improve solubility of drug in solvent eg surfactants, co-solvents

Question 18

What are organoleptic properties?

Answer 18

Fragrance, colourants (act as warning), sweeteners, flavourings

Question 19

How is stability ensured in drugs?

Answer 19

Using antioxidants and preservatives

Question 20

Define antioxidants

Answer 20

Slow down oxidation process, stop reactions with O2

Question 21

Define preservatives

Answer 21

Stop growth of microbes, enhanced shelf life and kill bacteria

Question 22

What can excipients impact?

Answer 22

Quality, Efficacy, safety of medicines

Question 23

Define friability (Quality)

Answer 23

Testing the durability of the tablets during transport, placed in a spinning machine to see effect of transport to tablet coating

Question 24

How are excipients regulated?

Answer 24

Approval needed, depending on difference between new/existing products

Question 25

How can you check the quality standards of excipients?

Answer 25

Excipients already in use have pharmacopoeial monographs that set standards

Question 26

What are the regulatory requirements for general products?

Answer 26

Parenteral, ophthalmic, oral: Contain same excipients in same conc as reference

Question 27

What are the regulatory requirements for other ROA?

Answer 27

No requirements excipients in final form be same as ref but must show inactive excipients doesn't affect safety/efficacy of drug

Question 28

What are the regulatory requirements for new drug applications (NDA)?

Answer 28

Marketed pursuant to biologics license application (BLA) supported by data

Question 29

When would a NDA be approved?

Answer 29

If excipients better than historic ones or perform new functions (need to be vital to justify costs)

Question 30

Describe the example of B-cyclodextrin case study | What it's used for and how it functions

Answer 30

Drug used to enhance water sol of poorly soluble drugs | Put dex in solution, add poor sol drug it moves to centre forming hydrophobic interactions and solubilises in centre

Question 31

What is a disadvantage of cyclodexrins?

Answer 31

Limited solubility (18mg/ml) - Limits how much drug can be dissolved in centre before dissolving itself