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Module 5 – Dosage form & Drug Delivery System Page 1 of 10 RJAV 2022
 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 2 of 10 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 3 of 10 RJAV 2022
Types of Capsules:

1. Hard Gelatin Capsules

Plasma concentration

Plasma concentration
• dry-filled or two-piece capsules (cap and body) Immediate
• main components: gelatin, sugar and water Sustained
• additives: colorant, opacifying agent (TiO2) + SO2 [0.15%] (to
prevent decomposition of gel)
• moisture content: 12-16%
• stored at 21-25°C/30-35% RH Time Time
• capsule sizes: (increase capsule size = decrease capacity)
• Human – No. 5 (smallest) – No. 000 (largest) Controlled Release
• Veterinary – No 10. – No. 12 Sustained Release
• Other designs:
• Pulvule – tapered at one end 2. Delayed-Release
• Spansule – tapered at both ends • drug release is other than the time of prompt administration
• Ex: enteric-coated
2. Soft Gelatin Capsules
• one-piece capsules 3. Repeat Actions
• used to contains non-aqueous liquids (vitamin e, cod liver oil, • contains 2 single doses of a medication
digoxin), suspensions, pastes, and dry materials • (1st dose → immediate; 2nd dose → delayed)
• main components: gelatin, plasticizer (glycerin, sorbitol) and
preservatives against fungi 4. Targeted Release
• moisture content: 6-10% • drug release is isolated in a specific body region/ tissue →
• no specific sizes absorption and action

E. ORAL MODIFIED-RELEASE SOLID DOSAGE FORMS • Colonic Tablets – deliver the drug into the colon without
dilution in other regions of GIT
• drug release features are based on time, course and • Gastro Retentive Tablets – remain in the stomach for long
locations period (floating tablets)
• Advantages:
• Economic savings F. PHARMACEUTICAL INSERTS
• Avoid patient compliance problems
• Reduce fluctuation in drug level (to prolong therapeutic 1. Suppositories
effect → to reduce dosing frequency) • Solid or semisolid masses intended to be inserted into a
• Minimize or eliminate side effects body orifice for local or systemic effect; they will melt at body
temperature or dissolve into aqueous secretions of body
Mechanism of Immediate-Release Formulation cavity
• Used when oral route is inadvisable
• Disadvantages
• Inconvenient
Plasma concentration

MTC
• Erratic absorption

Types of suppositories

Rectal Vaginal (Pessaries) Urethral (Bougies)

bullet, torpedo, little globular, ovoid, cone pencil-like
MEC finger
2 g (adult) 5g 4 g (male)
Duration 1 g (children) 2 g (female)
32 mm (adult) varies 140 mm (male)
onset Time 16 mm (children) 70 mm (female)

a. Rectal
Plasma concentration

• Advantages
• Low cost and lack of technical difficulties compared to
cmax
parenteral therapy
• Partially avoid the first-pass-effect
• Ex. Bisacodyl
• Disadvantages
• Surface area for absorption is smaller
AUC • Defecation may interrupt absorption
• Fluid content is less
• More expensive compared to oral dosage forms
Time • Stigma of violating patient’s dignity
tmax
b. Vaginal
• Indicated for bacterial or fungal infections and HRT
Types of Modified-Release Dosage Forms
• May be in the form of tablet, suppository, and semisolids
• Buffered to pH of 4.5
1. Extended-Release
• provides a prompt desired effect followed by a gradual c. Urethral
release of remaining amount • Inserted into the urethra after urination
• Problem: dose dumping • Ex: Alprostadil micro suppository
• Types:
• Controlled Release – zero order Suppository Bases
• Sustained Release – first order • Criteria:
• Inert, non-irritating, and non-sensitizing
• Firm and does not melt at RT
• Dissolves rapidly in the cavity fluid

Module 5 – Dosage form & Drug Delivery System Page 4 of 10 RJAV 2022
a. Oleaginous Base • Example:
• Cocoa Butter – most common and good base for rectal • Polyethylene Glycol (PEG) Ointment
suppository; solid at 32°C, melts at 34-35°C; exhibits • MW < 600 → clear, colorless liquids
polymorphism (ȣ - least stable [18°C]; α; β’; β – most stable • MW 600-1000 → semisolids
[34.5°C] • MW > 1000 → white, wax-like solids
• Wecobee – from coconut oil
• Witepsol – lauric acid is the major component; saturated B. CREAMS
fatty acids (C12-C18)
• semi-solid preparations containing 1 or more APIs dissolved
b. Water-Soluble/Miscible Base or dispersed in either w/o or o/w emulsion
• Glycerinated Gelatin – most common base for vaginal • soft, spreadable consistency
suppositories • Examples:
• Polyethylene Glycol (PEG) • Vanishing Creams – o/w base; large % water (ex.
glycerin, propylene glycol – + stearic acid)
1. Vaginal Tablets/Inserts • Cold Creams/ Petrolatum Rose Water Ointment –
• Ovoid or bullet-shaped tablets inserted into the vagina using w/o base; mineral oil → less rancid; white wax;
a plastic inserter for local effects spermaceti (cetyl esters wax) + Na borate
• contains antimicrobial agents • Components
• Aqueous solution
2. Implants/Pellets • Oleaginous portion
• long-acting dosage forms that provide continuous release of • Emulsifying agent
the drug to the body • Humectant
• administered parenterally or subcutaneously • Preservatives
• Pellet implants – small, sterile, cylindrical masses
• Levonorgestrel (Norplant ®) – 5 years C. GELS
• Leuprolide acetate (Viadur®) – prostate cancer 1 year
• clear, transparent, and non-greasy semisolids, containing
III. SEMISOLID DOSAGE FORMS API(s) dissolved in aqueous liquid, rendered jelly-like by the
addition of gelling agent
A. OINTMENTS

• semisolid dosage forms intended for external use Phenomena in Gels

• Uses:
• emollient 1. Thixotropy – reversible gel-sol formation
• occlusive 2. Imbibition – taking up of liquid without an increase in size
• vehicle 3. Swelling – taking up of liquid with increase in size
4. Syneresis – liquid is squeezed out and the gel shrinks, forming a
Ointment Bases: Xerogel

1. Oleaginous/ Hydrocarbon Base D. PASTES

• have emollient, occlusive
• greasy, anhydrous, non-water washable • semisolid preparations containing a large proportion of solid
• Examples: material (≥25%) and therefore stiffer than ointments
• Petrolatum, USP (Yellow Petrolatum, Petroleum • Use: to prolong contact of drug
Jelly or Vaseline®) – purified mixture of semisolid • Zinc Oxide Paste (ZnO) – treatment of diaper rash
hydrocarbon from petroleum
• White Petrolatum, USP – bleached or decolorized E. PLASTERS
• Yellow Wax (Beeswax) – wax obtained from the
honeycomb of Apis mellifera • solid or semisolid adhesive masses spread on a backing
• White Wax – bleached or decolorized material (paper, fabric, moleskin or plastic)
• Yellow Ointment, USP (Simple Ointment) – yellow • Use:
petrolatum + yellow wax • Protection and mechanical support
• White Ointment, USP – white petrolatum + white wax • Provide prolonged and close contact with the skin
• Salicylic Acid Plaster – keratolytic (10-40% salicylic acid)
2. Absorption Base
• without emulsion F. POULTICES/ CATAPLASM
• greasy and non-water-washable
• less emollient and occlusive effects • soft, moist masses of meal, herbs, seeds, etc.; applied hot in
• can absorb small amounts of water a cloth that consists of gruel-like consistency
• Examples: • Use: to localize infectious materials and counterirritant
• Hydrophilic Petrolatum, (Aquaphor) – white • Kaolin Poultice – treatment for boils and anti-inflammatory
petrolatum + white wax + cholesterol + stearyl alcohol
• Lanolin, USP (Anhydrous lanolin) – wax-like G. PLEDGETS
substance from the wool of sheep Ovis aries containing
0.25% moisture • Small compress or tuft, usually of cotton or cotton wool, used
• Hydrous Lanolin – 25% moisture to apply disinfectant or medicament to the skin
• Modified Lanolin – without free lanolin alcohols
and excess detergents H. GLYCEROGELATIN

3. Water-Removable Base • plastic masses applied on skin with a fine brush

• o/w emulsions or creams • components:
• easily washed off with water • 40% glycerin
• may be diluted with large amounts of water • 35% water
• Example: • 15% gelatin
• Hydrophilic Ointment • 10% API
• Zinc Gelatin Boot – treatment of varicose ulcers
4. Water-Soluble Base
• lipid-free
• greaseless and water-washable
• used for incorporation of solid materials

Module 5 – Dosage form & Drug Delivery System Page 5 of 10 RJAV 2022
 IV. TRANSDERMAL DRUG DELIVERY SYSTEMS V. LIQUID DOSAGE FORMS

• controlled release DDS or patches that allow the passage of A. SINGLE PHASE SYSTEMS
drugs from the skin to the systemic circulation
• Advantages: SOLUTIONS
• Constant dosage can be maintained
• Avoids first pass effect • liquid preparations containing one or more substances
• Reduced need for active administration dissolved in a suitable solvent
• Noninvasive compared to parenteral therapy • Advantages
• Can be promptly interrupted by removal • homogenous dose
• Disadvantages: • immediate availability for absorption
• Skin structure poses a barrier on the MW of the drug • flexibility
• Usually reserved for extremely potent drugs • Disadvantages
• Drug should have adequate solubility in both lipophilic • bulky
and aqueous environments • difficult to mask unpleasant taste and odor
• Development of contact dermatitis • less stable than solid dosage forms → degrade more
rapidly
Types of TDDS • interact with another component
• leaching: container → solution
1. Monolithic Systems • sorption: solution → container
• Incorporate matrix layer (polymer with dispersed drug)
beneath the backing layer Solubility

2. Membrane-controlled Systems Descriptive Term Parts of Solvent Required for 1

• Contain a drug reservoir or pouch (liquid or gel) and a rate- Part of Solute
controlling membrane Very Soluble <1
Freely Soluble 1-10
Parts of TDDS Soluble 10-30
Sparingly Soluble 30-100
Slightly Soluble 100-1,000
1. Occlusive Backing Layer Very Slightly Soluble 1,000-10,000
• protects the patch from outer environment Insoluble >10,000
• prevents drug loss and water loss
Pharmaceutical Solvents/ Diluting Agents
2. Drug Reservoir/ Matrix System
• stores and releases the drug at the skin site
1. Water
• most common
3. Rate controlling membrane
Official Types of Water
• controls drug release from the reservoir in membrane-
controlled systems
a. Purified Water
4.. Adhesive Layer • obtained by distillation, ion exchange, reverse osmosis
• ensures contact of the patch to the skin • used for aqueous dosage forms except parenteral and other
sterile solutions
5.. Release Liner b. Water for Injection
• protects the drug during storage and is removed prior to use c. Sterile Water for Injection
d. Bacteriostatic Water for Injection
Examples e. Sterile Water for Inhalation
Drug Use Application f. Sterile Water for Irrigation
Scopolamine Motion sickness (1st Behind the ear every
(Transderm Scop®) TDDS developed) 3 days 2. Alcohol
Nitogylcerin (Deponit®) Prophylactic Upper part of body • aka ethyl alcohol/ ethanol/ C2H5OH
treatment of angina once daily • can dissolve water-insoluble substances
Clonidine 1st TDDS for HTN Upper part of body • used with co-solvents such as glycols and glycerin
(Catapres-TTS®) every 7 days
Nicotine Smoking cessation Upper part of body Alcohol Content Limit
(Nicoderm®) once daily
• proposed by FDA to manufacturers of OTC oral products
Fentanyl Breakthrough pain Upper part of body
Age Limit
(Duragesic®) every 3 days
Methylphenidate ADHD Hip area 2 hours <6 years old 0.5%
(Daytrana®) before an effect is 6 to 12 years old 5%
needed > 12 years old 10%
Estradiol HRT Lower abdomen or
(Climar®) upper buttocks twice Types of Alcohol:
daily
Testosterone HRT Androderm® - upper
a. Alcohol, USP
(Androderm®, part of body or thighs
Testoderm®) Testoderm® - scrotum • 94.9% to 96.0% v/v ethanol

Application b. Dehydrated alcohol

• NLT 99.5% v/v ethanol
• site of application should be rotated c. Rubbing alcohol
• cur or dry-shave first the hair before pacing the patch • 70% v/v ethanol, the remainder consisting of water and
• it may be left on when showering, bathing or swimming denaturant
• use of skin lotion should be avoided at the application site • Denaturant: 8 parts acetone, 1.5 parts methyl isobutyl
ketone, 100 parts ethyl alcohol

d. Isopropyl Rubbing Alcohol

• 70% v/v isopropyl alcohol, the remainder consisting of water

Module 5 – Dosage form & Drug Delivery System Page 6 of 10 RJAV 2022
3. Glycerin • Evacuation Enema – to evacuate the bowel (ex. Fleet
• clear, syrupy liquid with a sweet taste Enema) – sodium phosphates enema
• miscible with both water and alcohol • Retention Enema – retained in the intestine for systemic
• has humectant, emollient and preservative qualities absorption (ex. Sulfasalazine Enema) – ulcerative colitis

4. Propylene Glycol f. Mouthwashes

• viscous liquid • aqueous solutions used by swishing the liquid in the oral
• miscible with both water and alcohol cavity to cleanse the mouth
• can be used as substitute for glycerin • May contain alcohol
• Use: therapeutic, cosmetic
5. Fixed Oils
• usually of vegetable origin g. Gargles
• can also use mineral oil for stability • aqueous solutions used for treating pharynx and
• Examples: nasopharynx by forcing air from the lungs through the
• Corn oil solution held in the throat
• Cottonseed oil
• Peanut oil 2. Sweet and Other Viscid Aqueous Solutions
• Sesame oil • Viscous liquids or semisolids
• Contain sugars, polyols, and/ or polysaccharides
Classifications of Solution
a. Syrups
1. Aqueous Solution • Concentrated aqueous solutions of sugar or sugar substitute
• Solvent or vehicle is mainly water with or without flavoring agents and medicinal substances
• May contain alcohol as preservatives
a. Aromatic Water/Medicated Waters
• clear, saturated aqueous solutions of volatile oils or other Types of Syrups
aromatic substances
• Use: flavored /perfumed vehicles for water soluble drugs i. Simple Syrup/ Syrup NF
• Examples: • 85% w/v or 65% w/w
• Peppermint Water, USP • sp. gr. = 1.313
• Stronger Rose Water, USP • self-preserving at ≥65% sugar
• Preparations: • low solvent capacity for drugs
• Distillation – universal but not practical/ economical
• Used for Preparing Stronger Rose Water, Orange ii. Flavored Syrups
Flower Water • syrups containing flavoring agents but not medicinal
• Simple Solution – more economical and simpler substances
• Talc may be used as dispersant • Examples:
• Instability: Salting out – formation of insoluble layer at top • Orange and Cherry syrup – acidic medium
• Cocoa syrup – bitter
b. Diluted Acids • Raspberry syrup – sour and salty
• prepared by diluting concentrated acids with purified water • Glycyrrhiza – masks bitterness of the complex vitamins
• expressed on a %w/v basis • Acacia syrup – masking bitter taste for urea
• most have strength of 10% w/v with the exception of diluted • Eriodictyon syrup – masking bitter taste for alkaloids
acetic acid
• Example: iii. Medicated Syrups
• Diluted HCl – treatment for achlorhydria; taken with • Simple or flavored syrups with API(s)
straw • Examples:
• Dextromethorphan + Guaifenesin
c. Topical Solutions • Diphenhydramine
• Astringent – locally applied solutions that precipitate • Ipecac
proteins and cause constriction of the skin
• Aluminum Acetate (Burrow Solution) – 5% aqueous Preparations of Syrups
solution; wet dressing in contact dermatitis
• Calcium Hydroxide (Limewater or Liquor calcis) – Solution with Heat
0.14% aqueous solution; more soluble in cold water • fastest methods
• Coal Tar (LCD) – 20% alcoholic solution; for eczema • problem: overheating may cause sucrose inversion/
• Anti-infective agents caramelization
• Hydrogen peroxide (Agua oxinada) – 3% aqueous or
10 volumes solution; anti-infective Solution without Heat
• Povidone Iodine (Betadine) – 10% aqueous solution; • avoids sucrose inversion
anti-infective
• Chlorhexidine gluconate – 4% aqueous solution; Percolation
0.12% solution is used as antiplaque mouthwash • preferred
• Thimerosal (Merthiolate) – 0.1% solution • water is passed through a bed of sucrose in a column
• slow rate (1mL/min) → to prevent bubbles (oxidation)
d. Douches
• aqueous solutions directed against a part into a cavity of the Reconstitution
body • addition of sugar to a medicated liquid
• Use: cleansing or antiseptic agent • addition of medicated liquid to syrup
• Examples:
• Eye Douche – removes foreign particles and b. Linctuses
discharges • viscous oral liquid that contains one or more active
• Pharyngeal Douche – throat ingredients dissolved in a suitable base that generally
• Vaginal Douche – maintain the acidic pH of the vagina contains a higher concentration of sugar or other sugars
(ex. pH Care® - chlorhexidine gluconate) • indicated for cough and colds

e. Enemas c. Honeys
• aqueous solutions administered rectally for either local or • thick liquid preparations somewhat allied to syrups but using
systemic effect honey as a base
• Types:

Module 5 – Dosage form & Drug Delivery System Page 7 of 10 RJAV 2022
d. Mucilage a. Liniments (Embrocation)
• thick, viscid, adhesive liquids • alcoholic or oleaginous solutions of various APIs intended to
• Preparation: be rubbed on the skin
• Dispersion of gum in water • Types:
• Extraction of mucilaginous principles with water • Alcoholic – counterirritant, rubefacient and penetrating
• Examples: action
• Acacia Mucilage • Oleaginous – massage; less irritating
• Tragacanth Mucilage b. Collodions
• Liquid preparations composed of pyroxylin dissolved in a
e. Jellies solvent mixture usually composed of 3:1 mixture of ether and
• Class of gels in which the structural coherent matrix contains alcohol
a high portion of water
Pyroxylin
• Uses:
• cotton + HNO3 + H2SO4 (act as catalyst)
• Lubricant (ex: K-Y Jelly)
• aka nitrocellulose, collodion cotton, soluble guncotton
• Contraceptive (ex: Nonoxynol-9)
• harsh to touch and flammable
• Topical anesthetic (ex: Lidocaine)
• Uses:
3. Alcoholic or Hydroalcoholic Solutions • Occlusive protective coating to the skin
• Solvent may be either pure alcohol or alcohol mixed with • Applied using a hair brush
water • Water repellant
• Types:
a. Elixirs • Flexible Collodion
• Clear, sweetened or flavored, hydroalcoholic solutions • +3% castor oil – flexible
intended for oral use • +2% camphor – waterproof
• Alcohol content: 5-40% • Salicylic Acid Collodion
• may contain glycerin and syrup • 10% salicylic acid in flexible collodion
• self-preserving at >10% alcohol • Keratolytic
• Elixirs vs. Syrups
• Less sweet c. Oleo vitamins
• Less viscous • Fish liver oils diluted with edible vegetable oil or solutions of
• More stable and more easily prepared vitamins in fish liver oil
• Less effective in masking unpleasant taste
• Preparations: d. Extracts
• Simple Solution • medicinally active portions of vegetable drugs which have
• Admixture of 2 Medicated Liquids been isolated using a solvent or solvent mixture
• Types:
• Medicated Elixir – digoxin, phenobarbital, Methods of Extraction:
diphenhydramine, dexamethasone
• Non-Medicate Elixir – aromatic elixirs, iso-alcoholic • Maceration – soaking
elixir – better solvent; higher content • Digestion – maceration with gentle heat
• Infusion – maceration in hot or cold water
b. Tinctures • Decoction – boiling in water
• alcoholic or hydroalcoholic solutions prepared from • Percolation – passage of solvent through column of the
vegetable drugs or chemical substances drug
• Alcohol content varies Forms of Extracts:
• Strength: 10% w/v
• Preparations:
• Semi-Liquid Extract – syrupy consistency prepared without
• Process P – percolation (ex. Belladonna Tincture)
the intent of removal the menstruum
• Process M – maceration (ex. Sweet Orange Peel
• Pilular/ Solid Extract – plastic consistency prepared with
Tincture)
nearly all of the menstruum
• Simple Solution – Iodine Tincture (2% in 50% alcohol);
• Powdered Extract – prepared to be dry by the removal of all
• Examples:
menstruum
• Laudanum – Opium Tincture
• Paregoric – Camphorated Opium Tincture
B. DISPERSE SYSTEMS
• Green Soap Tincture – topical detergent
• Iodine Tincture – topical anti-infective
• contain undissolved or immiscible drug distributed
• Compound Benzoin Tincture – topical protectant
throughout a liquid vehicle
• Phases:
c. Spirits/ Essences
• Dispersed Phase
• hydroalcoholic solutions of volatile oils
• Dispersed Medium
• Alcohol content: 50-90%
• Types:
• Preparations:
• Colloidal Dispersion: 1 nm – 0.5 μm
• Simple Solution – (ex: aromatic ammonia spirit)
• Fine Dispersion: 0.5 – 10 μm
• Solution with Maceration – (ex: peppermint spirit)
• Coarse Dispersion: 10 – 50 μm
• Chemical Reaction – (ex: ethyl nitrite spirit)
• Distillation – (ex: brandy spiritus vinivitis; whisky
Disperse Systems
spiritus frumenti)
1. Suspensions
d. Fluidextracts
• liquid preparations containing insoluble, solid drug particles
• hydroalcoholic solutions from vegetable drugs (ONLY)
(suspensoid) dispersed throughout a liquid vehicle
prepared by percolation
(suspending medium)
• “100% Tinctures” - too potent and too bitter
• Reasons
• Preparation:
• Improved stability
• Percolation
• Enhanced palatability
• Example:
• For drugs insoluble in a specific liquid
• Cascara Sagrada Fluidextract – cathartic
• Desired Features:
• Fine, uniform-sized particles
4. Other Non-Aqueous Solutions
• Slow rate of sedimentation
• Solvent may be ethereal or oleaginous
• Ease of redispersion
• Pour readily and evenly from its container
Module 5 – Dosage form & Drug Delivery System Page 8 of 10 RJAV 2022
Types of Suspensions

a. Gels
• Examples:
• Betamethasone Gel – anti-inflammatory
• Tretinoin Gel – keratolytic
• Aluminum Hydroxide Gel – antacid
• Phenomena in Gels c. Interfacial Film Theory (Plastic Theory)
• Imbibition – no increase in size • the emulsifier forms an interface between the oil and water,
• Swelling – increase in size surrounding the droplets of the internal phase as a thin layer
• Syneresis – gel shrinks of film adsorbed on the surface of the drops
• Xerogel – formed when only framework remains
d. Viscosity Theory
b. Magmas/ Milks • the viscosity of the medium aids in the emulsification by the
• Aqueous suspensions of large, insoluble inorganic drugs mechanical hindrance to coalesce the globules
giving them a whitish color compared to gels
• Examples: Methods of Emulsion Preparation
• Bentonite Magma – suspending agent
• Milk of Magnesia [Mg(OH)2] – antacid Dry Gum (Continental) Method
• 4(oil): 2(water): 1(gum)
c. Lotions • oil + gum, then add water all at once
• liquid suspensions or dispersions intended for external • w/o
application to the body
• Examples: Wet Gum (English) Method
• Calamine Lotion – ZnO + ferric oxide; trituration; • 4(water): 2(oil): 1(gum)
antipruritic; • water + gum, then add oil gradually in small portions
• White Lotion – ZnSO4 + sulfurated potash; • o/w
astringent, protective and mild antibacterial action
Forbes Bottle Method
d. Mixtures • for volatile oils or fixed oils of low viscosities
• Contain API which are dissolved or suspended in a liquid • the gum and oil are shaken in a bottle; then water is added in
vehicle portions
• Examples: • 3:2:1 or 2:2:1
• Bordeaux Mixture (CuSO4 + CaO) – algaecide in pools
• Kaopectate (Kaolin + Pectin) – antidiarrheal Nascent Soap/ In Situ Soap Method
• formation of a soap by mixing equal volumes of oil and an
2. Emulsions aqueous alkali solution
• Prepared by combining 2 immiscible liquids, one of which is • soap formed acts as an emulsifier
dispersed throughout the other
• Components VI. STERILE DOSAGE FORMS
• Internal Phase – discontinuous/ dispersed phase
• External Phase – continuous phase/ dispersion • dosage forms that are required to have absence of living
medium microorganisms including its spores
• Emulsifying agent – reduces interfacial tension • Examples:
• Parenteral – injectable
• Ophthalmic – eyes
Types of Emulsions • Inhalations
• Irrigation solution
a. Oil-in-water (o/w) • Dialysis Solutions
• oil id the dispersed phase & water is the dispersion medium • Implants
b. Water-in-oil (w/o)
• water is the dispersed phase and oil is the dispersion A. PARENTERALS
medium
• Injected through the skin or directly into the body
c. Multiple Emulsions • Must conform to strict requirements for microbiological
• the dispersed phase contains smaller droplets that have the impurity, particulate matter, pyrogenicity and isotonicity
same composition as the external phase
• w/o/w or o/w/o Parenteral Routes

d. Microemulsions 1. Intravenous (IV)

• clear, stable, liquid mixtures of oil, water, and solubilizer • Directly into the systemic circulation (back of the hand or
• vs. Macro emulsions: dorsal forearm
• clear, transparent liquid • Can be injected at all one (IV bolus) or gradually over a
• 10-200 nm diameter sustained period of time (IV infusions)
• formed by simple mixing 2. Intramuscular (IM)
• thermodynamically stable • Deep into the skeletal muscles (gluteal or deltoid muscle)
• For greater volume (2 to 5 mL)
Theories of Emulsification • Ex: vaccines, antipsychotics
3. Subcutaneous (SC/ SQ)
a. Surface Tension Theory • Injected into loose connective and adipose tissue (lower
• the internal forces in liquid droplet promote association of the abdomen, upper arm, anterior thigh)
molecule of the substance resisting distortion of the droplet • Small volumes (1.3 mL or less)
into a less spherical form • Ex: Insulin
4. Intradermal (ID)
b. Oriented Wedge Theory • Into the corium of the skin
• the surfactant forms monomolecular layers around the • Minimal volume (0.1 mL)
droplets of the internal phase of the emulsion • Ex: tuberculin skin tests
5. Intracardiac
• Heart chamber

Module 5 – Dosage form & Drug Delivery System Page 9 of 10 RJAV 2022
6. Intra-arterial C. INHALATIONS
• Artery
7. Intraspinal • Administered directly into the lungs for local action on the
• Vertebral column bronchial tree or systemic action
8. Intrathecal • may be in form of dry powders or solutions
• Cerebrospinal fluid • Advantages:
9. Intra-articular • Large area for absorption
• Joint space • Good blood supply
10. Intrasynovial • Avoids first pass effect
• Joint fluid • Example: Budesonide (Budecort®)
11. Epidural
• Near the dura mater of the CNS D. IRRIGATION

Components of Parenteral • Used to wash, soak, or flush wounds, surgical openings, or

body tissues
1. Solvent/ Vehicle – carrying agent • Usually packaged in large volume containers
• Examples:
a. Aqueous • Sodium Chloride Irrigation
• Water for Injection (WFI) – pyrogen-free water obtained by • Acetic Acid Irrigation
distillation or reverse osmosis
• Sterile Water for Injection (SWFI) – WFI that has been VII. AEROSOLS
sterilized
• Bacteriostatic Water for Injection (BWFI) – SWFI with • pressurized dosage forms designed to deliver drugs
antimicrobial agent (benzyl alcohol) systematically or topically with aid of a liquefied or propelled
• Sodium Chloride Injection – 0.9% NaCl in WFI gas fire (liquid/ solid drug in a gaseous medium)
b. Non-Aqueous Advantages Disadvantages
• Alcohol • rapid onset of action • environmental concern
• Glycerin • prevents first pass effect • poor inhaler technique
• greater drug stability • risk of oropharyngeal
• Propylene Glycol • fewer systemic side effects deposition
• Polyethylene Glycol • painless and relatively • airway obstruction and
• Fixed vegetable oils (CoCoPeSe) convenient bronchospasms
• Ethyl oleate
• Isopropyl myristate Types of Aerosols

2. Solutes 1. Space Spray

• remain in the air for prolonged periods
a. Active Pharmaceutical Ingredient (API) 2. Surface Spray
• carry the API to a surface
b. Buffers – maintain the required pH of the solution (ex: citrate, 3. Foams
acetate, phosphate) • formed when expansion of propellant within an emulsion
result in production of small bubbles
c. Tonicity Adjusters – reduce the pain of injection (ex: NaCl, Formulation:
dextrose)

d. Preservatives – maintain sterility (ex: thimerosal, benzyl alcohol, 1. Product Concentrate

benzalkonium chloride) • API combined with required adjuncts:
• Surfactant
3. Inert Gas – prevent oxidation of components (ex: Nitrogen Gas) • Antioxidant
• Solvents
Type of Parenteral Injections 2. Propellant
• Gas which develops the pressure within an aerosol and
expels the product when the valve is opened
1. Small-volume Injection – 100 mL or less • Types:
• Packaged in ampoules, vials, prefilled syringes, or minibags • Liquefied Gas – propane, butane, isobutene,
hydrofluorocarbons, dimethyl ether
2. large-volume injection – more than 100 mL • Compressed Gases – CO2, N2, N2O
• Packaged in plastic infusion bags or glass bottes with or
without an air vent tube Parts of an Aerosol
a. Fluid and Electrolyte Replenisher
• Sodium Chloride Injection – 0.9% NaCl
• Ringer’s Injection – NaCl + KCl + CaCl2 1. Pressurizable Container
• Sodium Lactate Injection – systemic alkalinizer • Glass – prone to breakage
• Lactated Ringer’s Injection – NaCl + KCl + CaCl2 + Na • Tin-Plated Steel – most widely
lactate used
• Aluminum – seamless and
b. Fluid and Nutrient Replenisher more inert
• Dextrose Injection 5% (D5W) – most common
• Invert Sugar Injection – dextrose + fructose 2. Valve Assembly – regulates flow
• Amino Acid Injection – for protein synthesis • Actuator – button pressed to
• Mannitol Injection – diagnostic aid in renal function activate valve for emission of
the product
B. OPHTHALMIC • Stern – supports actuator and
delivers formulation in the proper form
• Designed to be instilled onto the external surface of the eye • Gasket – prevents leakage of formulation when the valve is
(topical) or administered inside the eye (intraocular) closed
• May be in the form of solutions, emulsions, suspensions, and • Spring – the mechanism by which the actuator retracts
ointments • Mounting Cup – holds the valve in place
• Problem: Low drug bioavailability • Housing – links the dip tube, stem, and actuator
• Remedy: increase viscosity • Dip Tube – brings the formulation from the container valve
• Example: Eye Mo

Module 5 – Dosage form & Drug Delivery System Page 10 of 10 RJAV 2022