Lec 20- MR systems- ODT Flashcards
1
Q
Terminology
A
- Fast-dissolving
- Orodispersible- hypo-Salivation can lead to poor dissolving
- Fast-melting
- Orally dissolving- Needs to disintegrate in under 3 minutes
- FDA has adopted the term
- Orally disintegrating tablets (ODT’s)
2
Q
Orally disintegrating tablets
A
- Advantages
- Administration to patients who cannot, should not or will not swallow
- Children, elderly, vets, stroke patient
- Convenience (no water needed)
- Taste masking is crucial-superior taste
- Rapid intervention
- Altered absorption profile
- In solution when reach stomach or buccal absorption
- Decreased onset time
- Enhanced bioavailability
- New business opportunity
- In solution when reach stomach or buccal absorption
- Administration to patients who cannot, should not or will not swallow
3
Q
Bioavailability
A
- Some tablets are designed to dissolve in saliva remarkably fast, within a few seconds and are true fast-dissolving tablets
- Others contain agents to enhance the rate of tablet disintegration in the oral cavity and are more appropriately termed fast-disintegrating tablets as they may take up to 1 minute to completely disintegrate
- Increased bioavailability using such formulations is possible if there is sufficient absorption via the oral cavity prior to swallowing
- If the amount of swallowed drug varies
- There is the potential for inconsistent bioavailability
4
Q
Challanges
A
- Taste- masking is crucial
- Flavouring agent- spray drying
- Dose
- Moisture sensitivity- we normally have to use hygroscopic materials
- Excessive water: microbial contamination, drug stability, disintegration of the tablet (or just weakness)
- Friability- low compression means tha
- High prosit, low density low hardnes
- Taste masking is crucial
5
Q
Technologies
A
- Zydis
- Orasolv/Durasolv
- Flashdose
- Flashtab
- Wowtab
6
Q
Zydis
A
- Freeze-drying methods
- Suspend excipients in liquid and freeze
- Sublimation then occurs (going from a solid to a gas without the liquid stage)- this will leave behind poors- encouraging disintegration- this is done by lowering the pressure
- Zydis
- E.g. lorazepam, piroxicam, loperamide, loratidine, enalapril, selegiline
- Ideal for poorly water-soluble drugs
- Water-insoluble
- Dose<400mg, size<100um, acceptable taste
- Water soluble
- Dose- <500mg, acceptable taste, high eutectic temperature- the higher this point the easier it is to freeze this dosage form
- Zydis
7
Q
Composition
The matrix consists of
A
- Water soluble polymer (gelatine, dextran or alginate)
- Give the shape and resilience of the tablets
- Saccharide (mannitol or sorbitol)- mouth feel
- Give crystallinity, hardness and elegance
- Lyoprotectant (Glycine)
- Protects against collapsing of tablets during freeze drying- because we have to increase the temperature after freezing which can breakdown due to heat, this stops this
- Other excipients (flavours, sweeteners and colouring agents)
8
Q
Zydis
preparation
A
- Preparation
- Solution of polymer and saccharide in water
- Drug suspended or dissolved in carrier solution
- Precise dosing into pre-formed blisters
- Frozen in liquid nitrogen
- Rapidly freeze-dried
- Heat-seal process for blisters to ensure stability and protect the fragile tablet during removal by the patient
- Complex nature of manufacture and scale up results in a relatively high manufacturing cost
9
Q
Zydis
A
- Porous matrix
- Network of water-soluble carriers
- Active ingredient
- Microencapsulation and complexation with ion-exchange resins can be used along with other flavours and sweeteners for taste-masking for bitter drugs
10
Q
Characterisation
A
- Successful tablet formulation must have adequate mechanical strength
- The tablet dosage forms are exposed to various mechanical stresses during the manufacturing steps (e.g. packaging process), shipping and handling by patients
- Conventional tablets are usually assessed in terms of hardness and friability
- Do you think the same can be used for freeze-dried tablets
11
Q
Flashdose
A
- Modified tabletting technology
- Granulation of a low moldable sugar with a high moldable sugar to produce a fast disintegrating formulation
- The inclusion of effervescing agents using microparticulate systems
- Expensive
- Formulations are friable and moisture sensitive, therefore requiring specialized packaging
12
Q
Tablet compression
A
- Durasolv (Cima Labs) and Ziplets (Eurand)
- Excipients play a major role in the successful formulation and uperdisintegrants, hydrophilic polymers and effervescent compounds are included
- Effective taste-masking is required for ALL formulation
13
Q
Tablet compression
A
- Blending and compression of excipients- e.g. direct compression
- Dry granulation e.g. roller compaction
- Wet granulation
14
Q
Therapeutic area’s
A
- PPI (e.g. Zoton Fastab®)
- Migraine (e.g.Maxalt Melt®, Zomig Rapimelt®)
- Reflux (e.g.Pepcid®, Propulsid®, Domperidone®)
- Antihistamine/antiemetic (e.g.Zofran®, Clarityn®)
- Analgesia/NSAID (e.g.Calpol®, Feldene®, Zamadol melt®)
- Antidiarrhoeal (e.g.Imodium®)
- Antipyschotic (e.g.Risperdal Quicklet)
15
Q
Maxalt melt
A
- Convenient (Fast) relief of migraine
- In addition to tablets, nasal spray and injection
- Rizatriptan (10mg) in wafer
- Without liquids
- To reduce risk of nausea
- Oral lyophilisates
- Contain gelatin mannitol, glycine, aspartame, peppermint
17
Q
Zomig Rapimelt
A
