By: Emelie Grace Cachero, RPh

The Need for Dosage Forms:

• To protect the drug substance from the destructive influences of
atmospheric oxygen or humidity (coated tablets, sealed ampoules)
• To protect the drug substance from the destructive influence of
gastric acid after oral administration (enteric-coated tablets)
• To conceal the bitter, salty, or offensive taste or odor of a drug
substance (capsules, coated tablets, flavored syrups)
• To provide liquid preparations of substances that are either insoluble
or unstable in the desired vehicle (suspensions)
• To provide clear liquid dosage forms of substances (syrups, solutions)
• To provide rate-controlled drug action (various controlled-release
tablets, capsules, and suspensions)
• To provide optimal drug action from topical administration sites
(ointments, creams, transdermal patches, and ophthalmic, ear, and
nasal preparations)
• To provide for insertion of a drug into one of the body’s orifices (rectal
or vaginal suppositories)
• To provide for placement of drugs directly in the bloodstream or body
tissues (injections)
• To provide for optimal drug action through inhalation therapy
(inhalants and inhalation aerosols)
Preformulation Considerations
1. Physical Description
2. Microscopic Examination
3. Heat of Vaporization
4. Melting Point Depression
5. The Phase Rule
6. Particle Size
7. Polymorphism
8. Solubility
9. Solubility & Particle Size
10. Solubility & pH
11. Dissolution
12. Membrane Permeability
13. Partition Coefficient
14. pKa/ Dissociation Constants
5 Types of Stability Concern for Pharmacist
• Chemical
• Physical
• Microbiologic
• Therapeutic
• Toxicologic
Factors of Patients considered in determining
a drug dose in clinical investigations
1. Age
2. Pharmacogenetics
3. Body Weight
4. Body Surface Area
5. Sex
6. Pathologic State
7. Tolerance (the ability to endure the influence of drug)
8. Concominant Drug Therapy
9. Time & Condition of Administration
10. Dosage Form & Route of Adminstration
SOLID DOSAGE FORMS
POWDERS
GRANULES
TABLETS
CAPSULES
 POWDERS
• small individualized drug particles
• intimate mixtures of finely divided drugs or chemicals intended to be
used internally or externally
• Advantages:
• flexibility in compounding
• relatively dry & devoid of moisture
• relatively stable

• Disadvantages:
• not easily wetted
• inaccuracy of the dose
• not suitable for dispensing
• some powders are hygroscopic & deliquescent
 PARTICLE SIZE ANALYSIS
• Purpose: to obtain quantitative data regarding the size, shape, &
distribution of drug particles & particles & other components to be
used in the formulation
PARTICLE SIZE ANALYSIS
 COMMINUTION
1. reduction in particle size
2. process of reducing larger solid unit masses to smaller sizes by
mechanical means/ milling
3. to aid processing
4. to improve solubility up to certain extent
5. to reduce bulk volume
 Small Scale
1. TRITURATION
• the use of mortar & pestle
• 1:10 dilution/ method

• Three Types of Mortar & Pestle:

• (1)Porcelain - soft aggregates/ crystals
• (2)Wedgewood - crystal
• (3)Glass - smooth surface/ non porous
- solution, suspension, & ointment
- used for staining substance
 LEVIGATION
• commonly used in small scale preparation of ointments &
suspensions to reduce particle size & grittiness of the added products
• https://www.youtube.com/watch?v=hPpD2vxVulk&t=4s
• formation of paste by addition of nonsolvent (levigating agent):
• mineral oil
• glycerin
• propylene glycol
 Pulverization by intervention
• Addition of volatile substances

• Ex. Camphor + alcohol

• https://www.youtube.com/watch?v=r9QAqXIBT1I
 BLENDING POWDERS
SPATULATION
• Spatulation is blending small
amounts of powders by
movement of a spatula through
them on a sheet of paper or an
ointment tile.
 BLENDING POWDERS

SIFTING
• This process is not acceptable for the incorporation
of potent drugs into a diluent powder.
• by passing them through sifters
• for non potent powders
• Sifting results in a light, fluffy product.
 BLENDING POWDERS
TUMBLING
• drug particles are enclosed in a
rotating chamber
• use motorized blades by shaking
or rotating
• thorough but time-consuming
 BLENDING POWDERS
GEOMETRIC DILUTION
- to ensure the uniform
distribution of potent drug,
which is placed w/ an
approximately equal volume of
the diluents in a mortar & is
mixed thoroughly by trituration
 TYPES OF POWDERS
• Hygroscopic and Deliquescent Powders
• Efflorescent Powders
• Aerosol Powders
• Powder Blowers or Insufflators
• Bulk Powders
• Divided Powders
HYGROSCOPIC AND DELIQUESCENT
POWDERS

• Hygroscopic powders will

absorb moisture from the air.

• Deliquescent powders will

absorb moisture from the air to
the extent that they will partially
or wholly liquefy.
HYGROSCOPIC AND DELIQUESCENT
POWDERS
 EFFLORESCENT POWDERS

• An efflorescent is a crystalline
powder that contains water of
hydration or crystallization.
 AEROSOL POWDERS
• Some medicated powders are
administered by inhalation with the aid
of dry powder inhalers (DPIs), which
deliver micronized particles of
medication in metered quantities.
• A DPI is a device used to administer an
inhalation powder in a finely divided
state suitable for oral inhalation by the
patient. An inhalation powder is one used
with a device that aerosolizes and
delivers an accurately metered amount.
• Micronization – a method of producing
finer drug particles under 10um size
 EXAMPLES OF ORAL INHALATION
POWDERS
• Advair Diskus 100/50, 250/50,
and 500/50
• It is a specially designed plastic
device containing a double-foil
blister strip of a powder
formulation of fluticasone
propionate and salmeterol
xinafoate intended for oral
inhalation only
 EXAMPLES OF ORAL INHALATION
POWDERS
• This combination product contains
two medications: budesonide and
formoterol. 

• This medication is used to treat

reversible obstructive airways
disease, often known as
asthma. When combined, these
medications help to control the
symptoms of asthma and prevent
asthma attacks by keeping the airways
open to make breathing easier.
 EXAMPLES OF ORAL INHALATION
POWDERS
• Zanamivir for inhalation (Relenza)
is used to treat influenza
• It is a neuraminidase inhibitor.
Relenza is packaged in Rotadisks
and is administered using a
Diskhaler
• For Relenza, the usual dose is two
inhalations (one blister per
inhalation) twice daily for 5 days;
therefore, four blisters will be used
each day
 POWDER BLOWERS OR
INSUFFLATORS

• Finely divided powders intended

to body cavity by a device known
as “Insufflator”
 BULK POWDERS
Among the bulk powders available
in prepackaged amounts are:

• Oral Powders
• antacids (sodium bicarbonate)
• laxatives (psyllium [Metamucil])
 BULK POWDERS
• DOUCHE POWDERS
• dissolved in warm water by the patient for vaginal
use
Components of Douche Powders:
• a. Boric Acid or Sodium Borate
• b. Astringents, for example, potassium, alum, ammonium alum,
zinc sulfate
• c. Antimicrobials, for example, oxyquinoline sulfae, povidone
iodine
• d. Quaternary Ammonium Compounds, for example,
Benxethonium Chloride
• e. Detergents, for example, Sodium Lauryl Sulfate
• f. Oxydizing Agents, for example, Sodium Perborate
• g. Salts, for example, Sodium Citrate, Sodium Chloride
• h. Aromatics, for example, Methol, Thymol, Eucalyptol, Methyl
Salicylate, Phenol
 DIVIDED POWDERS
• Each divided portion of powder
may be placed on a small piece
of paper (Latin chartula; abbrev.
chart.; powder paper) that is
folded to enclose the
medication.
 DIVIDED POWDERS
Types of Paper in Paper Tablets
(1)Simple Bond paper - has no moisture resistance
(2)Vegetable Parchment - a thin semiopaque w/ limited moisture
resistance
3)Glassine - a glazed, transparent paper, also w/ limited moisture
resistance
(4)Waxed paper - a transparent waterproof paper and they use for
hygroscopic or deliquescent powder
GRANULES
 GRANULES
 They are defined as a dosage form composed of dry aggregates of powder
particles that may contain one or more APIs, with or without other
ingredients.
 They are usually in the 4- to 12-mesh sieve size range
Advantages:
1. Flows well compared to powders facilitates the transport of the drug
material from the hopper to the tablet press
2. Less surface area more stable from atmosphere humidity  less tendency
to cake or harden
3. Easily wetted  suitable for material that needs reconstitution prior to use
 GRANULES
1) WET METHODS
a) To moisten the powder or powder mixture and then pass the
resulting paste through a screen of the mesh size to produce the
desired size of granules. The granules are placed on drying trays and are
dried by air or under heat. The granules are periodically moved about
on the drying trays to prevent adhesion into a large mass.
b) Fluid bed processing, in which particles are placed in a conical piece
of equipment and are vigorously dispersed and suspended while a
liquid excipient is sprayed on the particles and the product dried,
forming granules or pellets of defined particle size
 GRANULES
2) DRY METHODS
Two Processes:
a. Roll Compaction
- Uses thin sheets
- Powders are rolled into dense
sheets
- Sheets are granulated using a
mechanical granulator
- Sieve granules to obtain desired size
 GRANULES
2) DRY METHODS
b. Slugging
- tablet pressed
- slugging of powders (formation
of large tablets called a “slugs”)
- slugs are granulated using an
appropriate equipment
- sieve the granules to obtain
desired size
- poorly formed tablets
 TWO TYPES OF GRANULES
a. Good Granules  particles that
pass through sieve 20 & are retain
at sieve 40
Quality of a Good Granulation:
• as spherical as possible
• uniform in content
• normal or bell-shaped
distribution of particle sizes
b. Fines
- Particles that pass sieve 40
- Act as bridges by filling
interparticulate spaces
• Excess Fines  there is
interparticulate friction
• Excess Granules  there is void
spaces
 EFFERVESCENT GRANULATED
SALTS
• Are granules or coarse to very coarse powders containing a medicinal
agents: sodium bicarbonate, citric acid and tartaric acid.
• Tartaric acid alone – granules lose firmness and crumble
• Citric acid alone – sticky mixture difficult to granulate
• Dry method (Fusion)
• Wet Method - water
 WAYS TO IMPROVE FLOWABILITY
1. Alteration of particle size & size distribution
2. Alter particle shape & texture
3. Use of Flow Activators
4. Alter process condition
5. Alteration of surface Forces