Lecture 22: Quick oral relief formulations

What is the main goal of quick relief formulations?

To achieve drug action within minutes by ensuring rapid drug dissolution and absorption

Why must quick relief formulations require minimal effort in administration?

Because patients may have reduced dexterity or cognitive ability during pain episodes

What are some absorption routes used for quick pain relief formulations?

Oromucosal (sublingual and buccal), dispersible, and orodispersible routes

What are dispersible formulations, what are their benefits and disadvantages?

They are tablets dispersed in water before intake, offering rapid onset and ease for patients with swallowing issues

May have unpleasant taste, requires potable water

How do sublingual and buccal formulations provide rapid absorption and what are their disadvantages?

They absorb drugs directly into the bloodstream, bypassing first-pass metabolism

May have unpleasant taste, salivary washout, interferes with eating/drinking

What advantages do orodispersible tablets offer?

Rapid onset, no choking/swallowing difficulties, and no need for water

What are common methods used to produce orodispersible tablets?

Lyophilisation (freeze-drying), moulding, or direct compression

What are the three steps in the freeze-drying process for ODTs?

1. Rapid freezing to form ice

2. Primary drying—ice sublimes to vapour without melting

3. Secondary drying—desorption of residual moisture

Why are orodispersible tablets porous and have low hardness?

To allow rapid water uptake by capillary action for fast disintegration

What are common disintegration aids used to achieve rapid dissolution?

Superdisintegrants and effervescent disintegrants

Give examples of superdisintegrants

Crospovidone, sodium croscarmellose, and sodium starch glycolate

What packaging consideration is important for these formulations?

They must be protected from moisture to maintain stability

What substances are typically used as effervescent disintegrants?

Carbonate salts, bicarbonate salts, or citric acid

What is mucus composed of and what is its charge at a physiological pH?

A gelatinous layer made of water and mucin surrounding oral epithelial cells - has a negative charge

What are the main functions of mucus in the oral cavity?

Provides lubrication, forms a permeability barrier, offers antimicrobial protection, and supports intercellular adhesion