Professional Documents
Culture Documents
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- Ease of administration
Drug Delivery System o Cosmetics
- Any substance/ preparation intended to be
place and contact with the external parts of
I. Introduction
the human body or with the teeth and mucous
o Drug- it is an agent intended for use in the diagnosis,
membrane of the oral cavity.
mitigation, treatment, cure, prevention of disease in
- Main used: Clean, Perfume, Changing the
humans/ animals.
appearance, Correcting Body Odor, To
o Dosage form- containing the following: API and
protect and for keep in good condition.
Excipient/ adjuncts/ additives.
o Compounding- preparation, mixing, packaging, or
Excipient/ Adjuncts/ Additives
labelling of a drug to prepare an individualized drug
- Inert (should have no reaction with the API,
treatment for a patient.
maintain the stability of drug)
II. Solid Dosage Forms and Solid Modified-Release Drug
o Drug Delivery System- is a system that is used as a
Delivery System
medium or carrier for administering a Pharmaceutical
Powders
product to a patient.
Granules
o Reasons for formulating dosage form:
Tablets
1. To protect the drug substance from
Capsules
destructive influences of atmospheric oxygen/
A. Powders
humidity
- Intimate mixtures of dry, finely divided drugs
2. To protect the drug substance from
and or chemicals that may be intended for
destructive influences of gastric acid after oral
“internal or external”
administration.
- Advantages:
3. To conceal the bitter, salty or offensive taste or
o Flexibility in Compounding
odor of a drug substance.
o Good Chemical Stability
4. To provide rate-controlled drug action.
o Rapid dispersion of ingredient
5. To provide liquid preparation of substance that
- Disadvantages:
are either insoluble/ unstable in the desired
o Inaccuracy of dose
vehicle.
o Not suitable for dispensing
To sum it up: unpleasant fasting, deliquescent or
hygroscopic drugs.
- Improve palatability Deliquescent- absorb moisture and
- Appearance liquefy (e.g. Naphthalene balls)
- Stability
- Solubility
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as cleaning agent and antiseptic. - Process: Powder → Tablet Molder → Slug (flat
e) Insufflation- Powders blown into a body cavity using an insufflator
(powder blower).
face and about 2.5 cm (1 in) in
f) Triturations- Dilution of potent powdered drugs. (1:10 dilution) (10% diameter)→Granulator→Granules
dilution)
II. Divided Powder
- a.k.a. “Chartulae”
- Example: Effervescent Granule
- Dispensed in individual doses usually in folded papers (Chartula) - Dissolve in water before use
- Block and Divide Method where CO2 gas (has something to
Types of Powder Papers
a) White Bond Paper
do with the taste buds) is released
- Opaque paper with no moisture resistance to mask the unpleasant taste of
b) Glassine the drug.
- Glazed, transparent
- Moisture resistant - Components: (Incorporate all to
c) Vegetable Parchment balance)
- Thin, Semi-opaque with moisture resistant paper a. Sodium Bicarbonate-
d) Waxed Paper
- Transparent undergo neutralization
- Waterproof paper suitable for deliquescent (absorb b. Citric Acid- sticky
moisture and liquefy) and hygroscopic powders (does c. Tartaric Acid- crumble easily
not absorb moisture and liquefy)
- ↓ Photodegradation C. Tablets
- A solid dosage form prepared by “Compression” or
B. Granules “Molding”
- Are prepared agglomerates of smaller particles of - Excipients:
powder. o Diluent/ fillers- add a necessary bulk
- #14-#12 Sieve Size Range o Binders/ adhesive- promote adhesion
- Advantage: o Disintegrant- promote break-up of the tab
o Flowability after oral administration
o More stable to humidity o Antiadherent, glidants (powder)- enhance
o Wettability flow of material (Machine and powder)
o Less tendency to cake/ hardens - Types of Tablets:
- Methods in preparation of Granules: 1) Tablets for Oral ingestion:
1) Wet Method/ Wet Granulation a) Compressed Tablet
- Most common method which produced - Formed by compression
tablet of best quality - Scored (line in the middle of the
- Process: Powder + Solvent= Wet Mass tablet)
→Sieve #4→Oven (60 ℃)→Granules b) Multiple Compressed Tablet
2) Dry Method/ Dry Granulation 1. Layer tablets
- For Moisture and heat sensitive materials
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A. TTDS c) TD Clonidine
- Is a controlled release delivery system/ patches - Catapress TTS (Transdermal Therapeutic System)
which facilitate the passage of therapeutic - First TDDS for hypertension
quantities of drug substance through the skin d) TD Fentanyl
(Stratum corneum) and into general circulation - Good analgesic (Chronic pain)
for systemic effects. e) TD Estradiol
- Nitropatch - (Estraderm)
- Hormone Replacement Therapy
f) TD Testosterone
- (Testoderm), (Androderm)
- Hormone Replacement Therapy
A. Suppositories
1. Occlusive backing - Solid dosage forms intended for insertion into
- Film- prevents loss of water from the body orifices where they melt, soften or dissolve
skin or prevents drug loss from the and exert local or systemic effects.
matrix. - Types:
2. Drug Reservoir/ Drug Matrix System o Rectal
- It is where the system drug is store o Vaginal/ Pessaries
and release. o Urethral/ Bougies
3. Adhesive layer
- Ensure TDDS are kept in place after Features Rectal Vaginal Urethral
a.k.a. Pessaries Bougies
application to the skin. Sex Both Female Both
4. Protective linear/ Release liner Age Adults/ Children Adults Adults
- Remove before application to the Shape Pencil-like Globular, Pencil-shaped
shaped Oviform,
skin. Cone shaped
- Examples of TDDS: Weight Adults: 2 g 3 grams Male: 4 g
a) Transdermal Drug (TD) Scopolamine Children: 1 g Female: 2 g
Size Adults: 32 mm Varies Male: 140 mm
- First TDDS to receive FDA approval Children: ½ Female: 70 mm
- Used for motion sickness Intended use Local and Local local
- a.k.a. “Transderm scop” systemic
Commonly used Cocoa butter Glycerenated
b) TD Nitroglycerin
based gelation
- Nitro-Dur, Transderm-Nitro B. Oleaginous Base
- For prophylactic treatment of angina - Example:
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3 Ether consistency
- No intention of
removing the solvent
2.Pilular/ Solid Extract
- Plastic consistency
(Cellulose tetranitrate) 1 Alcohol - An intention of
Nitric and Sulfuric removing nearly all
- Use of Collodion: intended for solvent
external use as an occlusive 3.Powder Extracts
protective to the skin. - Prepared to be dry by
- Types of Collodion: removing all solvent
1. Flexible Collodion
- Prepared by adding:
o 2% Camphor: B. Disperse System
makes the product 1) Suspension
“waterproof”
o 3% Castor oil:
- Is a preparation containing finely divided
renders the drug particles (suspensoid) distributed
product “flexible” uniformly throughout a vehicle
2. Salicylic Acid Collodion
- 10% Salicylic acid in
- Example of suspension:
flexible collodion o Gels
- Used for its keratolytic - semisolid system consisting of
effects.
dispersions made up of either
c) Extracts small inorganic particles or
- Concentrated preparations of large organic molecules.
vegetable or animal drugs.
- Method of extraction: - Characteristics of Gels:
o Maceration- soaking for 3 days a. Imbibition
with frequent agitation - Taking up of liquid
o Digestion- maceration with
gentle heat without an increase
o Percolation- meaning to strain, in size or volume.
a process in which a b. Swelling
comminuted drug is extracted
of its soluble constituents by - Taking up of liquid
the slow passage of suitable but with an increase
solvent through a column of
in size or volume.
the drug.
o Decoction- boiling in water for c. Synerersis
15 minutes - Liquid comes out of
o Infusion- maceration in hot/
cold water
the gel and the gel
- Three forms of Extracts: shrinks.
1. Semisolid Extracts d. Thixotropy
- Liquid/ syrup
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- Method of Preparation:
a) Dry gum or “continental method”
- a.k.a. “4:2:1 method”
- 4:2:1 (oil: water: gum)
- Oil + Gum → Trituration → Add
water (all at once)
b) Wet gum or English method
- Same proportion as in dry gum
method (4:2:1) Basic parts and components
Propellant/API - Supplies the necessary force to expel
- Water + Gum→ Trituration → Add oil product and some save as the solvent or
in portion diluent.
c) Forbes bottle method - Types of Propellant:
o Liquefied gases
- For volatile oils and less viscous oil - Saturated hydrocarbon
- Oil + Gum in bottle → Shake → Add (propane)
- Chlorofluorocarbon
water in proportion (2:2:1 (oil:
(CFC’s) - degrades zone
water: gum) layer
d) Lu situ soap method - Hydrofluorocarbon- more
accepted
- Oil + Aqueous Alkali’s solution o Compressed gases:
(calcium hydroxide) - CO2
- Emulsifying agent: salt of free fatty - Nitrogen
Container for a) Tin-plated steel
acid Aerosol - Most widely used for
e) Microemulsion metal container for
- Are thermodynamically stable, aerosols.
b) Actuator
optically transparent isotropic - Is the button the user
mixtures of a biphasic o/w system presses to activate the
stabilized with surfactants. emission of the product
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- Contains
multiple dose
- USP limit: not
larger than 30
mL
5. Bacteriostatic Sodium - Is a sterile water for injection
Chloride Injection containing one or more
antimicrobial agent.
6. Ringer’s injection - Contents in water for injection:
NaCl, KCl, CaCl