Pharmaceutical dosage forms that are solid in nature
When formulating any pharmaceutical dosage form, there is an equilibrium between the bioavailability of the product, its chemical and physical stability and the technical feasibility of producing it
Any changes made to a formulation in an attempt to optimize one property is likely to have an effect on the other two properties that must be considered
This is especially true of immediate-release solid dosage forms
Tablets and hard gelatin capsules form the vast majority of solid dosage forms on the market
Tablet
A pharmaceutical oral dosage form or solid unit dosage form comprising a mixture of active substances and excipients, usually in powder form, that are pressed or compacted into a solid dose
Tablets
Ensure a consistent dose of medicine that is easy to consume
Advantages of administering medication in pill form
Affordability
Stable dosage form
Accurate dosing
Ease of use
Light and compact
Convenience of combination products
Bitter medicines can be coated to make them more palatable
Disadvantages of tablets
Aftertaste
Slower acting
More likely to irritate the gastrointestinal tract causing nausea, vomiting, and diarrhea
Enteric coated tablets
Coated with special polymers that prevent them from dissolving in stomach acid and allow them to be absorbed in the small intestine
Enteric coated tablets
Certain antibiotics and proton pump inhibitors to treat gastroesophageal reflux disease
Sublingual tablets
Placed under the tongue, where they dissolve and are absorbed into the blood via the oral mucosa
Sublingual tablets
Sublingual nitroglycerine used to treat angina chest pain
Sublingual tablets
Useful when you want the drug to work quickly, suitable for people who cannot swallow tablets, useful for medications that are not well absorbed in the stomach or if their effectiveness is decreased by digestion
Disadvantages of sublingual tablets
Eating, drinking, and smoking can affect how well they work
They can irritate the mouth
Chewable tablets
Form of medicine that is chewed and then swallowed
Advantages of chewable tablets
Quick action
Come in various flavors
You don't need water to swallow them, so you can take them anytime
Disadvantages of chewable tablets
It may not taste pleasant to some people
It may need special storage and careful handling
Can interfere with dental appliances
Orally disintegrating tablets
Pills that dissolve on the tongue, become liquified, are swallowed subconsciously, and then the tiny pieces of the drug travel to the stomach and intestines, where the absorption occurs
Pros of orally disintegrating tablets
Ease of use
Quick onset of action
Cons of orally disintegrating tablets
May be more expensive
May not be as stable as other solid dosage forms
Effervescent tablets
Dissolved in water and then drunk
Pros of effervescent tablets
Ease of use
Better absorption
Reasonably quick action onset
Cons of effervescent tablets
Relatively more expensive
You should pay attention to what type of liquid this tablet can be dissolved in
Lozenges
Medicated tablets that dissolve slowly in the mouth and lubricate or soothe irritated tissues in patients with sore throats
Lozenges
Offer local pain relief and ease of use for children and adults who have difficulty swallowing pills
Tablet machines
Used to produce tablets, where powder is filled to a specified depth in a die and compressed between two punches
Tablet compression cycle
1. Die filling
2. Powder compression
3. Tablet ejection
Rotary tablet machines
Commercial tablet manufacturing machines with a rotating turret of punch and dies, allowing higher output
Rotary tablet machine operation
1. Powder filled into die cavities by suction and gravity
2. Powder compacted between upper and lower punches
3. Tablet ejected from die
Properties required for an optimal tablet formulation
Compatibility of drug substance with excipients
Flow ability
Compatibility
Lubricity
Appearance
Disintegration
Dissolution
Direct compression
Tablet manufacture that does not involve the pretreatment of the drug substance apart from blending with excipients
Advantages of direct compression
Simplicity and economy
Fewer operations
Lower energy consumption
Savings in labor costs
Simpler process validation
Improved stability and dissolution for certain drugs
Disadvantages of direct compression
Cannot be used for all drug substances
Challenges with low dose drugs and achieving homogeneous mix
Granulation
The process of particle enlargement where particles are agglomerated while retaining the integrity of the original particles, using either wet or dry methods
Purpose of granulation
Transforms powdered starting materials into a form suitable for tabletting, by improving flow properties, reducing elasticity, and densifying the material
Wet granulation
The most commonly used tablet manufacturing method, involving the addition of a liquid and a polymeric binder to the powdered starting materials, followed by drying
Non-aqueous granulation may be used when the active substance is particularly unstable in the presence of water, when water will not wet the powder, or if the drug substance forms a significant portion of the granulate and demonstrates extreme solubility in aqueous media
Granulation
Improves flow properties by increasing particle size
Involves addition of polymeric binder to stick particles together
Can reduce elasticity of starting materials, improving compatibility
Polymeric binders are usually hydrophilic, which can aid dissolution of hydrophobic drugs
Results in densification and volume reduction of starting material