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Powders

composed of a solid or mixture of solids reduced to a fine powder and intended for internal or external use

Granules

composed of agglomerates of powder particles that may contain one or more APIs, with or without other ingredients

Capsules

solid dosage forms in which medicinal agents and/or inert substances are enclosed in a small gelatin shell

Tablets

solid dosage forms usually prepared with the aid of suitable pharmaceutical binders

Ointments

semisolid preparations intended for external application to the skin or mucous membranes

Suppositories

solid dosage forms intended for insertion into body orifices where they melt, soften, or dissolve and exert local or systemic effects

Solutions

liquid preparations that contain one or more chemical substances dissolved in a suitable solvent or mixture of miscible solvents

Suspensions

preparations containing finely divided drug particles (the dispersed phase) distributed somewhat uniformly throughout a vehicle in which the drug exhibits a low degree of solubility

Emulsions

dispersion in which the dispersed phase is composed of small globules of a liquid distributed throughout a second liquid in which it is immiscible

Pharmaceutical aerosols

pressurized dosage forms that, upon actuation, emit a fine dispersion of liquid and/or solid materials containing one or more active ingredients in a gaseous medium

Delayed-release systems

• Use repetitive, intermittent dosing of a drug from one or more immediate-release units incorporated into a single dosage form

• Do not produce or maintain uniform drug blood levels within the therapeutic range

• Examples: Enteric-coated tablets, Repeat-action tablets

Sustained-release systems

Achieves slow release of drug over an extended period of time

Extended release

Maintains therapeutic blood levels of the drug for a prolonged period

Controlled Drug Delivery

Delivery of a drug at a predetermined rate and/or location according to the needs of the body

1. Site-specific targeting

2. Receptor targeting

Site-specific targeting

targeting the diseased organ or tissue (or the adjacent parts)

Receptor targeting

target: receptor within organ or tissue

Select the oral dosage form, which contains one or more active ingredients that are unstable in the water phase but stabilized in oil-in-water dispersions; either or both phases may contain dissolved solids.

A. Oral emulsion

B. Elixir

C. Syrup

D. Oral drops

Select the oral dosage form that contains one or more active ingredients that are dissolved in a suitable base.

A. Oral emulsion

B. Linctus

C. Oral solution

D. Elixir

Identify the pharmaceutical dispersed system that is a low-viscosity liquid preparation intended for application to the skin.

A. Suspension

B. Gel

C. Emulsion

D. Lotion

Analyze which drug delivery system achieves slow release of drug over an extended period of time.

A. Site-specific release

B. Sustained release

C. Delayed release

D. Receptor-targeting

The following are advantages of transdermal drug delivery systems, EXCEPT _______.

A. NOT suitable for all drugs

B. Avoid the risk and inconvenience of parenteral therapy

C. Avoid the first-pass effect

D. Provides the capacity for multiday therapy with a single application, thereby improving patient compliance

Select the statement that BEST describes pharmaceutical aerosols.

A. Enhances drug stability and therapeutic activity.

B. Protects the drug from thermal degradation.

C. All kinds of drug may be formulated as aerosols.

D. These are pressurized dosage forms that contain one or more active ingredients, which upon activation emit a fine dispersion of liquid and/or solid materials in a gaseous medium.

Select the delivery system, which does NOT produce or maintain uniform drug levels within the therapeutic range but is more effective for patient compliance than conventional dosage forms.

A. Sustained release

B. Delayed release

C. Site-specific release

D. Receptor release

Powders

• Finely divided particles

• Used internally or externally

• Fineness:

  • Vegetable/animal drug

  • Chemical

Powders: Sieve

	Vegetable/Animal Drug	Chemical
Very coarse	8
Coarse	20	20
Moderately coarse	—	40
Fine	—	80
Very fine	80	120

How is a powder composed of particles that all pass through a No. 80 sieve classified?

A. Coarse powder

B. Fine powder

C. Very fine powder

D. Very coarse powder

BULK POWDERS

• For non-potent drugs

• Non-individual dosing

• Packaging

  • Plastic containers

  • Glass jars

  • Sifter-top jars

Dentifrice

• Powder for cleaning teeth

• Abrasive, anti-cariogenic

Oral powder

• Intended to be ingested

Dentrifice

• Cleanse the oral cavity

• Powder dissolved in warm (tepid) water

• pH usually 3.5 to 5 when solution prepared

Insufflation

• Introduced into oral cavity

• Powder placed in insufflator → squeeze bulb to release particles through nozzle to intended region

• Passed through mesh #100

Dusting powder

• Dusted on the skin by means of sifter-top containers

• Provides low systemic toxicity

• Grit-free

DIVIDED POWDERS

• Aka Chartulae

• For potent drugs

• Powders divided into single doses

• Packaging: Individual papers or packets

• More accurate dosage form than bulk powder

Types of Paper (Divided Powders)

• Waxed paper

  • Transparent, waterproof

  • Low moisture resistance

  • Applicable for hygroscopic substances

• Glassine

  • Glazed, transparent

  • Moderate moisture resistance

• Vegetable parchment

  • Thin, semi-opaque paper

  • Moderate moisture resistance

• Bond paper

  • Opaque

  • High moisture resistance

  • Used if nonvolatile or not adversely affected by moisture

Waxed paper

• Transparent, waterproof

• High moisture resistance

• Applicable for hygroscopic substances

Glassine

• Glazed, transparent

• Moderate moisture resistance

Vegetable parchment

• Thin, semi-opaque paper

• Moderate moisture resistance

Bond paper

• Opaque

• No moisture resistance

• Used if nonvolatile or not adversely affected by moisture

COMMUNITION TECHNIQUES

• Levigation

• Trituration

• Pulverization by intervention

• Milling

Levigation

• Use of non-volatile liquid solvent known as levigating agent

• Examples:

  • Mineral oil (aka liquid paraffin)

  • Glycerin

  • Propylene glycol

Trituration

• Grinding using mortar & pestle

• Examples:

  • Porcelain mortar & pestle

  • Wedgewood mortar & pestle

• Intended both to comminute and blend powders

Pulverization by intervention

• Use of volatile solvent such as:

  • Alcohol

  • Ether

• Applicable for crystalline materials

Milling

• Principle: Cutting

• For comminuting:

  • Fibrous materials

  • Tough materials

Principle: Compression with application of pressure

• Principle: Impact

• Comminuting hard drugs, except thermolabile substances

• Principle: Impact and attrition

• Ball as impact media

• Pin as attrition media

Rolling mill

Principle: Attrition and compression

Which of the following statements about milling equipment is/are TRUE?

I. Fluid-energy mills are used for tough, fibrous materials and provide a successive cutting or shearing action.

II. The colloid mill is used to process dry materials as finely as possible.

III. The hammer mill is an impact mill using a high-speed rotor to which a number of swinging hammers are fixed.

IV. The ball mill uses a combination of impact and attrition.

A. I, II

B. III, IV

C. I, III

D. II, IV

BLENDING POWDERS

• Spatulation

• Trituration

• Tumbling

• Sifting

Spatulation

• Blending small amounts of powders by movement of spatula

• NOT for large scale and cohesive powders

• Application: potent mixtures

Trituration

• Intended both to comminute and blend powders

• Geometric dilution

  • Addition of equal amount of diluent to a potent drug to ensure uniform distribution

Geometric dilution

Addition of equal amount of diluent to a potent drug to ensure uniform distribution

Tumbling

• Powder is enclosed in a rotating container which rotates by a motorized process

• For large-scale mixing

Sifting

• Use of a sieve

• Result: light, fluffy powder

• Not for potent drugs

GRANULES

• Agglomerates of powders

• Size: 0.2–4 mm

GRANULES

Why granulate?

• Better flow and compaction

• Better compressibility in tablet manufacturing process

• Reduce dust during material processing

• Uniformly distributes essential ingredients within the granules

Wet Granulation

• Most widely employed method to produce compressed tablets

• Equipment: Fluid Bed Granulator

Wet Granulation

WEIGH AND MIX FORMULATION (EXCEPT LUBRICANT)

PREPARE DAMP

SCREEN THE DAN POWDER INTO FEL OR GRANULES

DRY THE WET GRANULES

SIZE GRANULES BY DRY SCREENING

LUBRICATE & COMPRESS

True

Care must be exercised not to over-wet or under-wet the powder

• Overwetting → granules that are too soft

• Underwetting → granules that are too dry and tend to powder

Dry Granulation

For drugs degraded by moisture or elevated temperature required for drying wetted material

Dry Granulation

WEIGH FORMULATION INGREDIENTS

MIX

COMPRESS into SLUGS

MILL AND SIEVE SLUGS

MIX WITH DISINTEGRANT AND LUBRICANT

COMPRESS

Determine the effect of overwetting to resulting granules.

A. Granules will be dry

B. Granules will be hard

C. Granules will be soft

D. Granules will be soggy

Identify the method of preparing powders that consists of enclosing the powder enclosed in a container, which rotates and mixes the powder ingredients.

A. Sifting

B. Tumbling

C. Mechanical mixing

D. Trituration

Analyze which method of preparing powders may be employed both to comminute and mix the ingredients; for comminution purposes, a porcelain or Wedgewood mortar with a rough inner surface is preferred; and for chemicals that may stain the porcelain or Wedgewood surface, a glass mortar is preferred.

A. Sifting

B. Mechanical mixing

C. Trituration

D. Tumbling

This method involves the addition of a granulating fluid together with other blended components to achieve a wet mass. This wet mass is passed through screens and the granules are then dried.

A. Wet granulation

B. Slugging

C. Dry granulation

D. None of the above

The following are the advantages of granules over powders, EXCEPT

A. Better flow property

B. Not easily wetted by liquids

C. More stable to humidity

D. Less tendency to cake or harden

TABLETS

API + Excipients

Diluents or Fillers

• Most common: Lactose

• Chewable: Mannitol

• Sugar-free chewable: Xylitol

• Microcrystalline cellulose (MCC)

• Kaolin

Disintegrants

• Most common: Starch

• Alginates

• Cellulose

• Clays

• Gums

• MCC

• Polacrilin potassium

Binders

• Starch paste

• Pregelatinized starch

• Methylcellulose

• For moisture-sensitive materials: Povidone

• For chewable: Acacia

Natural (Mineral pigments)

• Fe₂O₃

• TiO₂

Natural (Plant pigments)

• Green: Chlorophyll

• Orange-red: Annatto

• Red: Alizarin

• Blue: Indigo plant

• Golden yellow: Saffron

Synthetic colorants

• Coal tar

• Nitroso-dyes

• Nitro-dyes

• Azo-dyes

Glidants

• Colloidal silica

• Cornstarch

• Talc

Anti-adherents

Magnesium stearate

Lubricants

• Most common: magnesium stearate

• Sodium stearyl fumarate

• Stearic acid

• Mineral oil

• PEG

Sweeteners

• Sodium cyclamate

• Aspartame (CI: 50)

• Saccharin

• Acesulfame K

• Sucralose

• Stevia

Flavoring Methodology

Commonly done by mixing or blending

• Sour taste → fruit flavors, salty flavors

• Bitter → blended with salty, sweet, and sour tastes

• Chemicals used in blending: sucrose, MSG, benzaldehyde

Flavorants

• Salty (e.g., NH₄Cl): salty flavor

• Bitter (e.g., Quinine): bitter flavor

• Acrid or sour (e.g., HCl): sour flavor

• Oily taste (e.g., castor oil): aromatic rhubarb or sarsaparilla

Methods to Modify Taste

• Physical

• Chemical

• Physiological

• Overshadow

Physical

• Formation of inclusion compounds

• Coating

• Effervescence

• Viscosity increase

Chemical

Complexation

Physiological

• Anesthetize taste buds

• Menthol or mint

Overshadow

• (+) flavors whose intensity is stronger than the obvious taste

• Methyl salicylate & menthol

METHODS OF COATING TABLETS

Sealing → Subcoating → Smoothing → Finishing & Coloring → Imprinting → Polishing

Sealing

• Aka waterproofing coat

• For tablet components adversely affected by moisture

• Waterproofing substance: shellac

Subcoating

• Multiple subcoats of sugar-based syrups

• Bonds sugar coating to tablet and provides rounding

• Subcoating substances: gelatin, acacia, or PVP

Smoothing

• Additional coatings of a thick syrup to complete rounding

• Smoothing substances: sugar-based syrup

Finishing & Coloring

• Addition of several color coats to attain final appearance and appropriate color

• Step performed in a clean pan

Imprinting

By FDA regulation, all solid DFs for human consumption must be imprinted with product-specific identification codes (except drugs used in clinical trials, radiopharmaceuticals, and extemporaneously compounded drugs)

Polishing

Use of wax and/or

Select the INCORRECT statement about sugarcoating of tablets.

A. The sugarcoating process seals and protects the tablet dosage form and adds a distinctive look and taste to the tablet.

B. Many tablets are sugarcoated today as it is a more cost-efficient process than film-coating.

C. One or more coats of a waterproofing substance such as shellac are applied to the tablets before the subcoating application.

D. After the tablets are subcoated, additional coatings of a thick syrup are applied to round and smooth the coatings.

Determine the role of an alloying substance in a nonaqueous film coating solution.

A. Produces flexibility and elasticity to the coat

B. Provides water solubility or permeability

C. Enhances spreadability of the coat

D. Produces smooth thin film coat

FILM COATING

Skin-tight coating of a plastic-like material over the compressed tablet to produce coated tablets with essentially the same weight, shape, and size as the originally compressed tablets

FILM COATING

• Intended to pass through the stomach undissolved to disintegrate and release drug content for absorption along the intestinal tract

• Must resist dissolution in the highly acidic environment of the stomach

Enteric Coating Substances

• Cellulose acetate phthalate

• Polyvinyl acetate phthalate

• Diethyl phthalate

• HPMC

• Other cellulose derivatives

Film former

cellulose acetate phthalate, HPMC

Alloying substance

provides water solubility or permeability (e.g., polyethylene glycol)

Plasticizer

• provides flexibility and elasticity

Surfactant

• enhances spreadability