Summary
Samenvatting Les 13 'Pharmaceutical development'
- Course
- Institution
This document includes the summary of Lesson 13 (info slides with notes) of the “Preclinical drug research” course.
[Show more]
Seller
Follow
evagoormans
Content preview
Lecture 13: 4/12Pharmaceu)cal development
Introduc)on
Formula(on of drug candidate
- Essen(al In development of new drug
- Complex, (me-consuming and expensive
- Chemist/researchers versus pharmacists
- Now: more sophis(cated drug delivery system
o Targe(ng to relevant cells/(ssues (nanoformula(ons, liposomes, ..)
o Intelligent systems adjust dosage according to clinical response
- Formula(on that have been tested preclinically
- For oligonucleo(des -> bind to certain groups, GalNAc
o Liver will take up everything
- Formula(on will also be dependent by the route of administra(on
o Oral: can be tablet (ideally), can be a capsule (if it has a biMer taste), it could be a
solu(on or even an emulsion in some cases
Solu)on
What?
- Homogeneous mixtures of 2 or more components
o One or more solutes
o One or more solvents
Solu(ons for oral dosage
- Administered volume: usually a mul(ple of 5 ml
- Advantages over solid dosage form:
o Easier to swallow (children, elderly pa(ents)
o Readily absorbed from the GI tract
- Disadvantages over solid dosage for
o Bulky and not convenient to carry around
o Less microbiologically and chemically stable
o “Unpleasant taste” difficult to formulate
- Dose volume will be limited depending on the animal species you use
- O[en easily absorped compared with the tablet
- Some forms o Syrups
- Oral drops (e.g. vitamins) o...
Solu(ons for other pharmaceu(cal uses
- Mouthwashes and gargles (e.g. hextril®)
o Contain an(sep(cs, analgesics or weak astringents
o External use!
- Nasal solu(ons
o Drops or sprays
o Isotonic and buffered at pH 5.5-6.5
o Use: decongestant, local steroids, ...
- Ear drops
o Vehicles: propylene glycol, glycerol and water
, o Use: so[ening earwax, trea(ng infec(ons and inflamma(on
o O[en oily -> more easily to stay in the ear
Suspension
What?
- Contain one or more insoluble medicaments in a vehicle
- Disperse system in which one substance is homogeneously distributed in par(culate
form throughout another
o Par(cle size > 1 μm
o Slowly separa(ng (!) on standing
Advantages and uses
- If drug has low solubility
- Drugs with unpleasant taste;
o chloramphenicol (soluble) → chloramphenicol palmitate (insoluble)
- Dissolu(on rate: solu(on > suspension > solid form
- Slower degrada(on of drug in water
- Drugs suscep(ble to water → suspend in non-aqueous phase
- Bulky, insoluble powders → easier to take as suspension
- IM and SC injec(ons → prolonged release of drug
Formula(on of suspen(on
- Control par(cle size (using a mortar and pestle)
- Thickening agent to increase viscosity of vehicle
o To avoid that the conpount will be precipitate and will not be longer in solu(on
o To slow down sedimenta(on
o Thixotropic → semisolid on standing & flow readily a[er shaking !!
o Semisynthe(c polysaccharides: methylcellulose, carboxymethylcellulose
- Use a wekng agent
o To prevent solids to float
o Reducing interfacial tension between solid & vehicle o Surfactants, such as
polysorbates
o Ethanol, glycerol, ...
Emulsion
What?
- Consists of two immiscible liquids, one of which is uniformly dispersed throughout the
other as fine droplets (diameter: 0.1-100 μm)
o Emulsifying agent is required !!
Pharmaceu(cal applica(ons
- Oral, rectal and topical administra(on of oils & oil-soluble drugs
- Formula(on of oil- and water-soluble drugs together
- To enhance palatability of oils
- Increasing absorp(on through intes(nal wall
The benefits of buying summaries with Stuvia:
Guaranteed quality through customer reviews
Stuvia customers have reviewed more than 700,000 summaries. This how you know that you are buying the best documents.
Quick and easy check-out
You can quickly pay through credit card or Stuvia-credit for the summaries. There is no membership needed.
Focus on what matters
Your fellow students write the study notes themselves, which is why the documents are always reliable and up-to-date. This ensures you quickly get to the core!
Frequently asked questions
What do I get when I buy this document?
You get a PDF, available immediately after your purchase. The purchased document is accessible anytime, anywhere and indefinitely through your profile.
Satisfaction guarantee: how does it work?
Our satisfaction guarantee ensures that you always find a study document that suits you well. You fill out a form, and our customer service team takes care of the rest.
Who am I buying these notes from?
Stuvia is a marketplace, so you are not buying this document from us, but from seller evagoormans. Stuvia facilitates payment to the seller.
Will I be stuck with a subscription?
No, you only buy these notes for $7.68. You're not tied to anything after your purchase.
Can Stuvia be trusted?
4.6 stars on Google & Trustpilot (+1000 reviews)
52510 documents were sold in the last 30 days
Founded in 2010, the go-to place to buy study notes for 14 years now