MODULE 5│PHARMACEUTICS 1
DOSAGE FORM & DRUG DELIVERY SYSTEM
DOSAGE FORM & DRUG DELIVERY SYSTEMS USP Classification of Powders
I. INTRODUCTION TO DOSAGE FORMS Sieve number
• no. of square openings per linear inch
A. DEFINITION
Descriptive Term Sieve Number
Dosage Forms very coarse no. 8
• Drug products/preparations containing: coarse no. 20
• Active Pharmaceutical Ingredient (API)/ Drug moderately coarse no. 40
• Excipients/ Additives/Adjuncts fine no. 60
very fine no. 80
Drug Delivery System
• Drug products that allow the uniform release and targeting of Compounding of Powders
drugs into body
1. Comminution
Drug
• an agent intended for use in diagnosis, cure, treatment, a. Trituration
mitigation or prophylaxis in man and other animals – affects • mortar and pestle
the structure or any function of the body
b. Levigation
Excipients (aka adjuncts or additives) • forming a paste by the addition of a levigating agent (ex.
• nontherapeutic ingredients which improve the physical mineral oil, glycerin)
characteristics and efficacy of a drug in a dosage form
• Role: drugs → more appealing and efficacious c. Pulverization by Intervention
• Use: solubilize, suspend, emulsify, dilute, stabilize, • addition of volatile substance to a gummy material (ex.
preservatives, color, flavor, etc. camphor + alcohol; I2crystals + ether)
Cosmetics 2. Mixing/ Blending
• any substance/preparation intended to be placed in contact
with external parts of human body or with teeth and mucous a. Trituration
membranes of oral cavity • mortar and pestle
• with a view exclusively or mainly to cleaning them, perfuming
them, correcting body odors, changing their appearance, Types of mortar and pestle
protecting them and/or keeping them in good condition • Glass – smooth non-porous surface; for simple admixture;
for chemicals that stain
Food Supplement • Porcelain – rough inner surface; for comminution
• processed food products that help supplement the diet • Wedgewood – rougher surface; for crystalline substances
• may contain dietary ingredients such as vitamins, minerals,
herbs, amino acids, and other dietary substances b. Spatulation
• make take various forms including those of liquids, capsules, • Blending of powders with a spatula on a tile or paper
powders, etc., except parenteral • Use: small quantities, non-potent drugs, eutectic mixtures
Compounding c. Sifting
• process of combining, mixing, or altering ingredients to • Powders are passed through sifters
create a medication tailored to the needs of an individual • Results in light, fluffy product
patient. • Not for potent substances
B. LOCAL & SYSTEMIC EFFECTS d. Geometric Dilution
• addition of an equal volume of diluent to a potent substance
Local effects placed in a mortar
• felt in general area of administration Step 1: 100mg of potent drug + 100mg of diluent = 200mg of mixture
• common route: topical Step 2: 200mg of mixture + 200mg of diluent = 400mg of mixture
Step 3: 400mg of mixture + 400mg of diluent = 800mg of mixture
Systemic effects Step 4: 800mg of mixture + remaining diluent = 1000mg of mixture
• occur in tissues distant from the site of contact between the
body and the drug e. Tumbling
• drug must enter the bloodstream • large containers rotated by a motorized process
• common route: oral and parenteral
Types of Powders
II. SOLID DOSAGE FORMS
1. Bulk Powders – dispensed in large quantities
A. POWDERS
a. Oral Powders
• mixtures of finely divided drugs and/ or chemicals in a dry • dissolved in water prior to use
form which may be intended for internal or external use
• Advantages: b. Dentifrices
• rapid dispersion of ingredients • used to clean and polish teeth
• flexibility in compounding • contain a soap, mild abrasive and anticariogenic agent
• good chemical stability
• Disadvantages: c. Dusting Powders
• inaccuracy of dose • locally applied non-toxic powders that have no systemic
• not suitable for unpleasant-tasting, deliquescent and action
hygroscopic drugs
d. Douche Powders
• dissolve in warm water prior to introduction into a body cavity
Module 5 – Dosage form & Drug Delivery System Page 1 of 9 RJAV 2022
, e. Insufflations a. Compressed Tablets
• blown into body cavities using an insufflator • formed by compression
• some are scored
f. Trituration
• dilutions of potent powdered drugs (10% API) b. Multiple Compressed Tablets
• Layered tablets – formed by compressing 2 or 3 layers of
2. Divided Powders/Chartulae – dispensed in individual doses formulation against each other (ex. Neozep tablet)
usually in folded papers; block-and-divide method • Compression coated tablets – formed by compressing an
outer shell around a tablet core
Types of Powder Paper
c. Coated Tablets
a. White Bond Paper • Sugar Coated Tablets – coated with sucrose-based solution
• opaque paper with no moisture resistance • Film Coated Tablets – coated with a thin layer of polymer
material
b. Vegetable Parchment • Enteric-Coated Tablets – remain intact in the stomach but
• thin, semi-opaque, moisture resistant paper disintegrate in the small intestine
c. Glassine Paper 2. Tablets Used in the Oral Cavity
• glazed transparent moisture-resistant paper
a. Chewable Tablets
d. Waxed Paper • chewed first before swallowing
• transparent waterproof paper; suitable for deliquescent and • diluent: mannitol and xylitol
hygroscopic drugs • (ex. Multivitamins, antacids)
B. GRANULES b. Rapidly/ Orally Disintegrating Tablets
• liquefy on the tongue and then the patients swallow the liquid
• dry aggregates of powder particles • (ex. Risperidone, Ondansetron)
• Normal sieve no. 4 to 12
• Tablet formulation: sieve no. 12 to 20 c. Buccal Tablets
• placed in the lining of the cheeks
Advantages of Granules over Powder • disintegrate slowly (4 hours)
• (ex. Progesterone)
• Flow well compared to powders
d. Sublingual Tablets
• Less tendency to cake or harden
• More stable to humidity • placed under the tongue for systemic absorption
• More easily wetted by liquids • disintegrate rapidly (2-3 minutes)
• (ex. Nitroglycerin, ISDN)
Compounding of Granules
e. Lozenges
• solid dosage forms in a hard candy or sugar base that
1. Wet Granulation dissolve slowly in mouth for local effect
• addition of granulating fluid or liquid binder • (ex. Strepsils® - dicholorobenzyl alcohol + amylmetacresol)
• most common; • Types:
• Troches – compressed lozenges
2. Dry Granulation • Pastilles – molded lozenges
• for moisture-sensitive and heat labile materials • Lollipops – lozenges on sticks
• use compaction/ compression forces
3. Tablets Used to Prepare Solutions
3. Effervescent Granules
• dissolved in water before use in which CO2 gas is released a. Effervescent Tablets
to mask the unpleasant taste of drug • Release CO2 upon dissolution in water
• Components: • ex. Berocca®, Alka-Seltzer® - antacid + pain reliever
• Sodium bicarbonate
• Citric acid →sticky b. Compounding/ Dispensing Tablets
• Tartaric acid →crumble • contain a large amount of API used by pharmacists in
• Preparation: compounding multiple dosage units
• Dry/Fusion Method – binder is 1 molecule of water in • no longer use
citric acid
• Wet Method – binder is water + alcohol c. Hypodermic Tablets
• used by physicians to prepare parenteral solutions
C. TABLETS • no longer use
• solid dosage forms which are prepared mainly by d. Molded Tablets/ Tablet Triturates
compression or molding • prepared by moistening powders and then putting on a
• Advantages: triturate mold (may be compressed)
• uniform content • results to cylindrical tablets which are very soluble in water
• less manufacturing cost
• easy to package and ship D. CAPSULES
• simple to identify
• most stable of all oral dosage form • solid dosage forms in which the drug is enclosed within in
• tamperproof either a hard or soft, soluble shell, usually made of gelatin
• Disadvantages: • Gelatin – partial hydrolysis of collagen from the skin/bones
• some drugs resist compression of animals
• some drugs that require encapsulation prior to • Types:
compression • Type A – mainly from pork skin; acid processing
• Type B – from bones and animal skins; alkaline
Types of Tablets processing
• Vegetable Capsules – alternative hydroxypropyl
1. Tablets for Oral Ingestion methylcellulose (HPMC) or hard starch
Module 5 – Dosage form & Drug Delivery System Page 2 of 9 RJAV 2022
DOSAGE FORM & DRUG DELIVERY SYSTEM
DOSAGE FORM & DRUG DELIVERY SYSTEMS USP Classification of Powders
I. INTRODUCTION TO DOSAGE FORMS Sieve number
• no. of square openings per linear inch
A. DEFINITION
Descriptive Term Sieve Number
Dosage Forms very coarse no. 8
• Drug products/preparations containing: coarse no. 20
• Active Pharmaceutical Ingredient (API)/ Drug moderately coarse no. 40
• Excipients/ Additives/Adjuncts fine no. 60
very fine no. 80
Drug Delivery System
• Drug products that allow the uniform release and targeting of Compounding of Powders
drugs into body
1. Comminution
Drug
• an agent intended for use in diagnosis, cure, treatment, a. Trituration
mitigation or prophylaxis in man and other animals – affects • mortar and pestle
the structure or any function of the body
b. Levigation
Excipients (aka adjuncts or additives) • forming a paste by the addition of a levigating agent (ex.
• nontherapeutic ingredients which improve the physical mineral oil, glycerin)
characteristics and efficacy of a drug in a dosage form
• Role: drugs → more appealing and efficacious c. Pulverization by Intervention
• Use: solubilize, suspend, emulsify, dilute, stabilize, • addition of volatile substance to a gummy material (ex.
preservatives, color, flavor, etc. camphor + alcohol; I2crystals + ether)
Cosmetics 2. Mixing/ Blending
• any substance/preparation intended to be placed in contact
with external parts of human body or with teeth and mucous a. Trituration
membranes of oral cavity • mortar and pestle
• with a view exclusively or mainly to cleaning them, perfuming
them, correcting body odors, changing their appearance, Types of mortar and pestle
protecting them and/or keeping them in good condition • Glass – smooth non-porous surface; for simple admixture;
for chemicals that stain
Food Supplement • Porcelain – rough inner surface; for comminution
• processed food products that help supplement the diet • Wedgewood – rougher surface; for crystalline substances
• may contain dietary ingredients such as vitamins, minerals,
herbs, amino acids, and other dietary substances b. Spatulation
• make take various forms including those of liquids, capsules, • Blending of powders with a spatula on a tile or paper
powders, etc., except parenteral • Use: small quantities, non-potent drugs, eutectic mixtures
Compounding c. Sifting
• process of combining, mixing, or altering ingredients to • Powders are passed through sifters
create a medication tailored to the needs of an individual • Results in light, fluffy product
patient. • Not for potent substances
B. LOCAL & SYSTEMIC EFFECTS d. Geometric Dilution
• addition of an equal volume of diluent to a potent substance
Local effects placed in a mortar
• felt in general area of administration Step 1: 100mg of potent drug + 100mg of diluent = 200mg of mixture
• common route: topical Step 2: 200mg of mixture + 200mg of diluent = 400mg of mixture
Step 3: 400mg of mixture + 400mg of diluent = 800mg of mixture
Systemic effects Step 4: 800mg of mixture + remaining diluent = 1000mg of mixture
• occur in tissues distant from the site of contact between the
body and the drug e. Tumbling
• drug must enter the bloodstream • large containers rotated by a motorized process
• common route: oral and parenteral
Types of Powders
II. SOLID DOSAGE FORMS
1. Bulk Powders – dispensed in large quantities
A. POWDERS
a. Oral Powders
• mixtures of finely divided drugs and/ or chemicals in a dry • dissolved in water prior to use
form which may be intended for internal or external use
• Advantages: b. Dentifrices
• rapid dispersion of ingredients • used to clean and polish teeth
• flexibility in compounding • contain a soap, mild abrasive and anticariogenic agent
• good chemical stability
• Disadvantages: c. Dusting Powders
• inaccuracy of dose • locally applied non-toxic powders that have no systemic
• not suitable for unpleasant-tasting, deliquescent and action
hygroscopic drugs
d. Douche Powders
• dissolve in warm water prior to introduction into a body cavity
Module 5 – Dosage form & Drug Delivery System Page 1 of 9 RJAV 2022
, e. Insufflations a. Compressed Tablets
• blown into body cavities using an insufflator • formed by compression
• some are scored
f. Trituration
• dilutions of potent powdered drugs (10% API) b. Multiple Compressed Tablets
• Layered tablets – formed by compressing 2 or 3 layers of
2. Divided Powders/Chartulae – dispensed in individual doses formulation against each other (ex. Neozep tablet)
usually in folded papers; block-and-divide method • Compression coated tablets – formed by compressing an
outer shell around a tablet core
Types of Powder Paper
c. Coated Tablets
a. White Bond Paper • Sugar Coated Tablets – coated with sucrose-based solution
• opaque paper with no moisture resistance • Film Coated Tablets – coated with a thin layer of polymer
material
b. Vegetable Parchment • Enteric-Coated Tablets – remain intact in the stomach but
• thin, semi-opaque, moisture resistant paper disintegrate in the small intestine
c. Glassine Paper 2. Tablets Used in the Oral Cavity
• glazed transparent moisture-resistant paper
a. Chewable Tablets
d. Waxed Paper • chewed first before swallowing
• transparent waterproof paper; suitable for deliquescent and • diluent: mannitol and xylitol
hygroscopic drugs • (ex. Multivitamins, antacids)
B. GRANULES b. Rapidly/ Orally Disintegrating Tablets
• liquefy on the tongue and then the patients swallow the liquid
• dry aggregates of powder particles • (ex. Risperidone, Ondansetron)
• Normal sieve no. 4 to 12
• Tablet formulation: sieve no. 12 to 20 c. Buccal Tablets
• placed in the lining of the cheeks
Advantages of Granules over Powder • disintegrate slowly (4 hours)
• (ex. Progesterone)
• Flow well compared to powders
d. Sublingual Tablets
• Less tendency to cake or harden
• More stable to humidity • placed under the tongue for systemic absorption
• More easily wetted by liquids • disintegrate rapidly (2-3 minutes)
• (ex. Nitroglycerin, ISDN)
Compounding of Granules
e. Lozenges
• solid dosage forms in a hard candy or sugar base that
1. Wet Granulation dissolve slowly in mouth for local effect
• addition of granulating fluid or liquid binder • (ex. Strepsils® - dicholorobenzyl alcohol + amylmetacresol)
• most common; • Types:
• Troches – compressed lozenges
2. Dry Granulation • Pastilles – molded lozenges
• for moisture-sensitive and heat labile materials • Lollipops – lozenges on sticks
• use compaction/ compression forces
3. Tablets Used to Prepare Solutions
3. Effervescent Granules
• dissolved in water before use in which CO2 gas is released a. Effervescent Tablets
to mask the unpleasant taste of drug • Release CO2 upon dissolution in water
• Components: • ex. Berocca®, Alka-Seltzer® - antacid + pain reliever
• Sodium bicarbonate
• Citric acid →sticky b. Compounding/ Dispensing Tablets
• Tartaric acid →crumble • contain a large amount of API used by pharmacists in
• Preparation: compounding multiple dosage units
• Dry/Fusion Method – binder is 1 molecule of water in • no longer use
citric acid
• Wet Method – binder is water + alcohol c. Hypodermic Tablets
• used by physicians to prepare parenteral solutions
C. TABLETS • no longer use
• solid dosage forms which are prepared mainly by d. Molded Tablets/ Tablet Triturates
compression or molding • prepared by moistening powders and then putting on a
• Advantages: triturate mold (may be compressed)
• uniform content • results to cylindrical tablets which are very soluble in water
• less manufacturing cost
• easy to package and ship D. CAPSULES
• simple to identify
• most stable of all oral dosage form • solid dosage forms in which the drug is enclosed within in
• tamperproof either a hard or soft, soluble shell, usually made of gelatin
• Disadvantages: • Gelatin – partial hydrolysis of collagen from the skin/bones
• some drugs resist compression of animals
• some drugs that require encapsulation prior to • Types:
compression • Type A – mainly from pork skin; acid processing
• Type B – from bones and animal skins; alkaline
Types of Tablets processing
• Vegetable Capsules – alternative hydroxypropyl
1. Tablets for Oral Ingestion methylcellulose (HPMC) or hard starch
Module 5 – Dosage form & Drug Delivery System Page 2 of 9 RJAV 2022
