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MD16 and 17 Oral dosage forms
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1Disadvantages of conventional immediate-release:
1. [blank_start]Sawtooth[blank_end] profile
2. [blank_start]Repeat[blank_end] administrations needed
3. Patient [blank_start]compliance[blank_end]
4. Short [blank_start]half-life[blank_end] drugs
5. [blank_start]Side effects[blank_end]- ASawtooth
- BRepeat
- Ccompliance
- Dhalf-life
- ESide effects
2Reasons for wanting rapid dissolution:
• Increase the bioavailability of [blank_start]poorly water soluble[blank_end] drugs (90% of [blank_start]drug candidates[blank_end] are classified as poorly water-soluble)
• [blank_start]Reduce the time[blank_end] for onset of drug action (eg for analgesics)
• [blank_start]Dysphagia[blank_end] (dissolve in mouth so patient doesn't need to swallow)- Apoorly water soluble
- Bdrug candidates
- CReduce the time
- DDysphagia
3If using a co-solvent to increase solubility you must be cautious about precipitation occurring from dilution in the GIT.
- ATrue
- BFalse
4Choice of salt depends on pKa:
Acidic drugs: pKa of counterion should be 2 pH units [blank_start]above[blank_end] drug pKa.
Basic drugs: pKa of counterion should be 2 pH units [blank_start]below[blank_end] drug pKa.- Aabove
- Bbelow
5Salts are hygroscopic.
- ATrue
- BFalse
6Cyclodextrin complexes are [blank_start]cyclic[blank_end] sugars and [blank_start]chiral[blank_end] organic molecules. They have a hydrophobic cavity and can carry BSC [blank_start]Class II[blank_end] drugs. They improve drug solubility and [blank_start]stability[blank_end] and can be incorporated into [blank_start]tablets[blank_end].
- Acyclic
- Bchiral
- CClass II
- Dstability
- Etablets
7Choose the correct statement.
- AVolume of cyclodextrin cavity depends on number of units in the CD ring.
- BGamma-cyclodextrin is the most commonly used size.
8Physical methods to increase dissolution rate:
1. Nanosizing
Particle [blank_start]size reduction[blank_end] under one micrometre to increase [blank_start]surface area[blank_end] and therefore dissolution. Reduces [blank_start]food[blank_end] effects. Done by [blank_start]milling[blank_end]. Avoid aggregation by using [blank_start]surfactants or polymers[blank_end].
2. Polymorphs
Amorphous form [blank_start]more[blank_end] soluble, but [blank_start]less[blank_end] stable.
3. Solid dispersions
Solid solute dispersed in a solid solvent. E.g. [blank_start]Eutectics[blank_end]; increased surface area and sharp [blank_start]lower[blank_end] melting point.- Asize reduction
- Bsurface area
- Cfood
- Dmilling
- Esurfactants or polymers
- Fmore
- Gless
- HEutectics
- Ilower
9Pulsatile release is a form of delayed release.
- ATrue
- BFalse
10Delayed release may be useful when drug is [blank_start]acid labile[blank_end](must protect from release in stomach), to prevent [blank_start]gastric irritation[blank_end](eg by NSAIDs), to [blank_start]target delivery[blank_end] to small intestine, or to suit the [blank_start]circadian rhythm[blank_end] of disease state.
- Aacid labile
- Bgastric irritation
- Ctarget delivery
- Dcircadian rhythm
11Strategies to achieve delayed release:
1. Enteric coating
No initial release, [blank_start]pH change[blank_end] is trigger for polymer coat. May be tricky because of [blank_start]ileum pH rise[blank_end]. Must be cautious of gastric [blank_start]residence time[blank_end] to avoid [blank_start]dose dumping[blank_end].
2. Osmotically controlled systems
Core has a drug and an [blank_start]osmotic agent[blank_end]. There is a rate controlling [blank_start]membrane[blank_end] and a hard shell around them with a [blank_start]pore[blank_end] drilled through. After coating dissolves, water diffusion [blank_start]in[blank_end] through membrane forces drug out through pore via [blank_start]osmotic pressure[blank_end]. Release rate is [blank_start]zero[blank_end] order.
3. Time delay system
Film coat for immediate release, tablet core for later release. Coating [blank_start]erodes over time[blank_end] independent of pH to give tailored [blank_start]lag time[blank_end] before drug release. eg for rheumatoid arthritis treatment.- ApH change
- Bileum pH rise
- Cresidence time
- Ddose dumping
- Eosmotic agent
- Fmembrane
- Gpore
- Hin
- Iosmotic pressure
- Jzero
- Kerodes over time
- Llag time
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- PHCY211 (Medicines) Quiz on MD16 and 17 Oral dosage forms, created by Mer Scott on 20/05/2018.
- Author
- Mer Scott
- Language
- English
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