W11 Capsules and Suppositories Flashcards
Capsules
- Solid dosage forms
- With hard or soft shells of various shapes and capacities
- Usually containing a single dose of active substance
- Intended for oral administration
What are the advantages of capsules?
Patient compliance & Drug delivery…?
- Patient compliance
* Easier to swallow- Smooth & slippery
* Tasteless and odourless- Eliminate all contact between drug and mouth)
* Can be opened up- Contents sprinkled on food
* Clear, high-gloss coloured film- Can be printed on - Drug delivery
* Fast acting- Breakdown of capsule shell
occurs readily ≈ disintegration of
tablet
* Beads/pellets/granules in
addition to dry powder fills- A mixture of beads with different release rates
* Other dosage forms in a capsule- Mini tablets and liquids
Hard capsules
What are the 2 types?
Made of a cap and a body
- Gelatin- Bovine, porcine, fish
* Collagen of animal bones
and hides (subjected to maceration and purification with acids and alkalis)
* 13 – 16% moisture, contributing to shell
flexibility - Alternative polymers (vegetarian)
* HPMC, pullulan
* HPMC: 4 – 6% moisture,
suitable for moisture-sensitive/hygroscopic
formulation
* Pullulan (polysaccharide from corn syrup): 12% moisture
What is the process of Hard capsule manufacture and filling?
- Gel solution preparation
- Capsule dipping
- Capsule drying
What are some Hard capsule examples?
- Oruvail Prolonged-release Hard
Capsules= Prolonged-release pellets in capsule - Omeprazole Gastro-resistant Hard
Capsules= Enteric-coated pellets in capsule - Practical Applications for Single Pill Com
binations in the Cardiovascular Continuum
Dissolution from hard capsules
- Hard gelatin capsules containing only hydrophobic drug particles
- In GI fluids, hard gelatin capsule shell dissolves, thereby exposing contents of fluids
- Contents remain as capsule-shaped
plug. Hydrophobic nature of contents
impedes penetration of GI fluids - Dissolution of drug occurs only
from surface of plug-shaped mass.
Relatively low rate of dissolution
Faster action:
* 2. Hard gelatin capsules containing
hydrophobic drug particles () and
hydrophilic diluent particles** ()
* Particles of hydrophilic diluent dissolve in
GI fluids leaving a porous mass of drug
* GI fluids can penetrate porous mass Effective surface area of drug and hence dissolution rate is increased
* Effective surface area of drug and hence
dissolution rate is increased
What are the 2 types of Soft capsule shell?
- Hermetically sealed one piece
- Gelatin
- Vegetarian softgels
Modified starch, carrageenan (extract of red
seaweed), disodium phosphate, glycerol and/or
sorbitol, purified water
What are soft capsule examples?
- Ibuprofen e.g .Flarin
- Loperamide e.g. Imodium
- Peppermint oil e.g. BuscoMint
Dissolution from soft capsules (for info)
What occurs?
Swell to a certain size, break up. Small particles inside are released from soft gel into stomach acid or small intestine
What quality control tests are done for tablets and capsules?
Uniformity of dosage Units- T, C
Dissolution test T, C
Disintegration test- T
Resistance to Crushing- T
Friability- T
What are suppositories?
Solid dosage forms
* Rectally – suppository
* Vaginally – pessary
* Designed to melt, dissolve or disperse so that a local or systemic effect is exerted
* Come in a few shapes (cone, bullet or torpedo-shaped)
What are the different suppository applications? (2)
What can they be used to treat?
- Local effect (rectum/lower colon)
* Laxative effect
* Treat haemorrhoids (piles)
* Inflammation in lower third of the colon (ulcerative colitis) - Systemic effect
* Oral dosage not possible (vomiting)
* Bypass liver first-pass metabolism
* Prolonged effect (e.g. pain relief at night)
Suppository bases
What are the types? (2)
Examples?
- The drug is either incorporated in a base which melts or dissolves
- Fat-soluble
* Cocoa butter
* Soap as a lubricant
* Made with a suppository mould (reusable or disposable) - Water-soluble
* Polyethylene glycol
* Lubricant often not required
Suppository manufacture
What are the steps?
- Apply lubricant- with a brush not with a cotton wool
- Pouring molten base and drug- In excess to overfill mould
(heated base and drug, cool in fridge or freezer)
What are some suppository making problems? (3)
Aim: to have the same amount of drug in each pessary and that it is evenly dispersed
* Common problems:
1. Uneven amounts of drug, usually gather in tip
Causes:
* Did not stir continuously
* Poured at too high a temperature
* Drug particles too coarse
2.Bubbles
Causes: Uneven pouring
3. Broken in half
Causes:
* Not cooled properly
* Not enough lubricant
