Materials and Excipients II Flashcards
What else is included in addition to API in tablet formulations?
Coated in sugar - Palatability
Fillers - Inc size
What else is included in addition to API in solution formulations?
Water, flavour, sweeteners - Palatability
What else is included in addition to API in topical formulations?
Water, Viscose (enhancer) - To easily spread
What else is included in addition to API in IV formulations?
Water, salts - Isotonic salt level balance compared to bloodstream
What is used to provide bulk to formulations?
Fillers or diluents
What should fillers be?
Inert (non-reactive), non-toxic, stable, cheap, good mechanical properties eg hard, tough
Give an example of common diluents
Lactose and calcium salta
Give examples of formulations containing fillers
Granules, tablets, powder-filled capsules
Define disintegrants
Materials that aid breakdown of solid dosage forms
How do disintegrants work?
Expand on contact with water, aid uptake of water
Examples of formulations containing disintegrants
Tablets, effervescent tablets, powder-filled capsules
Define lubricants
Added to tablets/capsule plugs to stop dosage form sticking to machinery
Define glidants
Added to powder to aid flow
Define binders
Polymer solutions in water aid adhesion of powders to form granules
Define vehicle/base and give examples for IV, gels, suppositories
Liquid or semi-solid which a drug is contained eg:
IV - water/oil base (sc/im)
Gels - water, oils
Suppositories - fatty triglycerides
Define thickener/viscosifiers
Enhance viscosity of liquid formulation (usually hydrophilic polymers) eg for topical gels
Define solubility enhancers and give examples
Improve solubility of drug in solvent eg surfactants, co-solvents
What are organoleptic properties?
Fragrance, colourants (act as warning), sweeteners, flavourings
How is stability ensured in drugs?
Using antioxidants and preservatives
Define antioxidants
Slow down oxidation process, stop reactions with O2
Define preservatives
Stop growth of microbes, enhanced shelf life and kill bacteria
What can excipients impact?
Quality, Efficacy, safety of medicines
Define friability (Quality)
Testing the durability of the tablets during transport, placed in a spinning machine to see effect of transport to tablet coating
How are excipients regulated?
Approval needed, depending on difference between new/existing products
How can you check the quality standards of excipients?
Excipients already in use have pharmacopoeial monographs that set standards
What are the regulatory requirements for general products?
Parenteral, ophthalmic, oral: Contain same excipients in same conc as reference
What are the regulatory requirements for other ROA?
No requirements excipients in final form be same as ref but must show inactive excipients doesn’t affect safety/efficacy of drug
What are the regulatory requirements for new drug applications (NDA)?
Marketed pursuant to biologics license application (BLA) supported by data
When would a NDA be approved?
If excipients better than historic ones or perform new functions (need to be vital to justify costs)
Describe the example of B-cyclodextrin case study
What it’s used for and how it functions
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
What is a disadvantage of cyclodexrins?
Limited solubility (18mg/ml) - Limits how much drug can be dissolved in centre before dissolving itself
