Midterms Flashcards
They serve as carriers for drugs that are topically delivered by way of the skin, cornea, rectal tissue, nasal mucosa, vagina, buccal tissue, urethral membrane, and external ear lining
SEMI-SOLID DOSAGE FORMS
advantageous in terms of its easy application, rapid
formulation, and ability to topically deliver a wide variety of drug molecules
SEMI-SOLID DOSAGE FORMS
usually are intended for localized drug delivery
SEMI-SOLID DOSAGE FORMS
PHYSICAL PROPERTIES OF SEMI-SOLID DOSAGE FORMS
▪ Smooth texture ▪ Elegant in appearance ▪ Non dehydrating ▪ Non gritty ▪ Non greasy and non-staining ▪ Non hygroscopic
PHYSIOLOGICAL PROPERTIES OF SEMI-SOLID DOSAGE FORMS
▪ Non irritating
▪ Do not alter membrane / skin functioning
▪ Miscible with skin secretion
▪ Have low sensitization index
APPLICATION PROPERTIES
▪ Easily applicable with efficient drug release.
▪ High aqueous wash ability
homogenous, translucent, viscous, semi solid preparation intended for external application to skin or mucous membranes
Ointments
Ointments also called
(Unguents)
should be of such composition that they soften but not
necessarily melt when applied to the body
Ointments
GENERAL USES OF OINTMENTS
- Acts as protective or protectant - serve as physical barrier to environment
- Acts as emollient - softens skin and makes it pliable
- Carrier of medicament – vehicle
TYPES OF OINTMENTS
Medicated
non-medicated
FACTORS OF SELECTING OINTMENT BASES Characteristics
- Physicochemical properties of the medicaments
- Patient’s conditions
- Intended site of application
- Characteristics of the various vehicles available
are water-free, and aqueous preparations may only be incorporated into them in small amounts and then with difficulty
HYDROCARBON BASES
HYDROCARBON BASES uses
- used mainly for their emollient effect and not intended for penetration into the skin.
- They are difficult to wash off.
- They do not “dry out” or change noticeably upon aging
Characteristics of HYDROCARBON BASES
a) Retained on the skin for prolong period of time
b) Do not permit the escape of moisture to the skin to the atmosphere
c) Difficult to wash as such they act as occlusive dressing
d) They do not change noticeably upon aging
e) Insoluble in water
f) Not water-washable
g) Anhydrous
h) Will not absorb water
i) Emollient
j) Occlusive
k) Greasy
l) Nonirritating
m) Inexpensive, non-reactive
Sources Of Hydrocarbon Bases
Vegetable Oil
Animal Fat
HC
Liquid hydrocarbon
mineral oil
Animal Fat
Oleic oil
HC from
Petrolatum
3 Forms of HC
Liquid hydrocarbon
Semi-solid HC petrolatum
Solid HC
Semi-solid HC petrolatum
Vaseline
Solid HC
Paraffin
Examples Of Hydrocarbon Bases
- Petrolatum, NF
- White Petrolatum, USP
- Yellow Ointment
- White Ointment, USP
- Mineral Oil, USP
- Paraffin, NF
- Olive Oil, USP
mixture of semisolid HC obtained from petroleum
Petrolatum, NF
Properties of Petrolatum, NF
An unctuous mass, color yellowish to light amber
Petrolatum, NF melts between
380C -600C
Petrolatum, NF synonyms
Yellow petrolatum, Petroleum jelly
Commercial product of Petrolatum, NF
Vaseline
is petrolatum that has been decolorized
White Petrolatum, USP
White Petrolatum, USP uses
diaper rash, dry skin
White Petrolatum, USP synonym
White Petroleum Jelly
White Petrolatum, USP commercial
White Vaseline
Yellow Ointment contains
Each 100 g contains 5 g yellow wax and 95 g of
petroleum
purified wax obtained from honeycomb of the bee (Apis mellifera)
Yellow wax
Yellow Ointment synonyms
Simple Ointment
White Ointment, USP contains
100 g contains 5% of white wax (bleached purified beeswax) and 95% white petrolatum
is a mixture of liquid HC obtained from petroleum
Mineral Oil, USP
Mineral Oil, USP is useful in
levigating of substances insoluble in it in the
preparation of ointment base
Mineral Oil, USP
Salicylic acid, Zinc oxide
Mineral Oil, USP synonyms
Liquid Petrolatum
a purified mixture of solid HC obtained from petroleum
Paraffin, NF
Characteristics of Paraffin, NF
colorless or white, more or less translucent mass that may be used to harden or stiffen oleaginous semisolid ointment bases
from crushed olives- also called ___________
Olive Oil, USP - sweet oil
Those that permit the incorporation of
aqueous solutions resulting in the formation of water-in-oil emulsion.
Anhydrous absorption bases
Anhydrous absorption bases characteristics
a) Insoluble in water
b) Not water washable
c) Anhydrous
d) Can absorb water
e) Emollient
f) Occlusive
g) Greasy
Greasy examples
Hydrophilic Petrolatum and Anhydrous Lanolin
Those that are already water-in-oil emulsion that permits the incorporation of small additional quantities of aqueous solution
Emulsion Base
Emulsion Base characteristics
a) Insoluble in water
b) Not water washable
c) Contains water (limited)
d) Emollient
e) Occlusive
f) Greasy
Are oil-in-water emulsion that are capable of being washed from skin or clothing with water
water removable base
water removable base frequently referred to as
“water washable” ointment base
By this method, all or some of the components of an ointment are combined by melting together and cooled with constant stirring until congeal.
Fusion method
In fusion method added last when temperature is low enough not to cause decomposition
heat labile substances and volatile constituents
Semisolid pharmaceuticals frequently either in
jars or in tubes
The jars may be made
glass, uncolored, colored green, amber or blue or
opaque and porcelain white
The tubes are made of tin or plastic. These are called
“collapsible tube”
TESTS REQUIREMENTS FOR OINTMENTS
Microbial Content
Minimum Fill Test
Packaging, Storage, and Labeling
Additional Standards
Microbial Content
▪ Meet acceptable standard for microbial
▪ Must contain antimicrobial preservatives
Microbial Content: Preservatives
methylparaben, propyl paraben, phenols, benzoic acid,
sorbic, quaternary ammonium salts
example of Microbial Content
Betamethasone Valerate Ointment
Betamethasone Valerate Ointment – must be absence of
Staphylococcus aureus and Pseudomonas aeruginosa
net weight and volume
Minimum Fill Test
Packaging, Storage, and Labeling
▪ metal, plastic tubes, jar
▪ Well close containers, light sensitive, light resistant
▪ Labeling- type of base used (water soluble or insoluble)
Additional Standards
▪ Examine the viscosity
▪ Vitro drug release to ensure within lot and lot-to-lot uniformity
A semisolid dosage form containing one or more drug substances dissolved or dispersed in either a water-in-oil emulsion or an oil-in-water or in another
type of water-washable base.
creams
These are viscous semisolid emulsions which are meant for external use
creams
Cream is divided in to two types namely as
1) Aqueous creams
2) Oily creams
the emulsions are o/w type & it is relatively non
greasy
Aqueous creams
The emulsifying waxes are (examples)
anionic, cationic & non –ionic
used as emulsifying agent in creams
polysorbate, triethanolamine soap
In case of oily creams w/o type & it is relatively
greasy
emulsifying agent in oily creams
wool fat, wool alcohols, beeswax & calcium soap
The cream should be store in
collapsible tube & supplied in well closed
container to prevent evaporation & contamination.
are semi-solid systems consisting of dispersions of small or large molecules in an aqueous liquid vehicle rendered jellylike by the addition of a gelling agent.
gels
gels are sometimes called
“Jellies”
gels may thicken on standing, forming a
“thixotropy”
True or false
must be shaken before use to liquefy gel and enable pouring
True
Examples of gelling agents: synthetic macromolecules
Carbomer 934
Examples of gelling agents: Cellulose derivatives
carboxymethylcellulose
Examples of gelling agents: natural gums
tragacanth
high-molecular-weight water-soluble polymer
cabomers
They are used as gelling agents
carbomers
carbomers concentrations
0.5% to 2.0% in water
Classes of Gel: 2 phase systems
Single phase gel
Continuous phase
separation between the insoluble matter and liquid vehicle is observed. This type contains inorganic materials
Single phase gel
Example of Single phase gel
Al(OH)3 Gel (aluminum hydroxide)
commonly aqueous where alcohol and gels may be use as continuous phase
Continuous phase
Example of Continuous phase which is Mineral oil + polyethylene resin =
oleaginous ointment base
for patch testing
Bases
for electrocardiography
NaCl
for anti- inflammatory corticosteroid
Fluocinonide Gel
dental care prophylactic
Na Fluoride & Phosphoric acid gel
treatment of acne
Tretinoin Gel
for intravaginal
Prostaglandin Gel
are semisolid preparations intended for application to the skin
paste
Contain a larger portion of solid material (25%)
paste
paste are prepared by
direct mixing or the use of heat
paste is suited for application of hairy parts of the body
False
Paste still used today:
Zinc Oxide paste: 25 % of Zinc oxide, starch and petrolatum
❑ are solid or semi-solid adhesive masses spread on a backing of paper, fabric, moleskin, or plastic.
❑ Applied to the skin to provide prolonged contact at site.
plasters
provide protection or mechanical support at the site of application
Unmedicated plasters
provide effects at the site of application.
Medical plasters
plasters few used today:
salicylic acid plaster
salicylic acid plaster used on
toes for removal of corns
Purpose of plasters
- To afford protection and mechanical support
- To furnish an occlusive macerating action
- To bring medication into close contact with surface of skin
Examples of Plaster
Adhesive plaster
Modern Plasters
Medicated plasters
Back Plasters
consisting of vinyl resin, plasticizers, and chemical additives
Adhesive plaster
are practically all machine made and are
available in colors such as flesh, striped, and others
Modern Plasters
Example of medicated plasters
Salicylic Acid Plaster, Salonpas
are made of heavy cotton or wool and cotton backing to
provide warmth and support.
Black plasters
Black plasters are usually use from
for backache, sore shoulders, sore arms, and other muscular aches
The active constituents of back plaster is
Chilli Plaster; Hot Salonpas
are unctuous preparations of such consistency that may be easily spread at ordinary temperature upon muslin cloth or similar material with spatula yet not soft to liquefy and run when applied to the skin
cerates
contents of cerates
oil, hard petrolatum and beeswax
Cerate example
Cantharides cerates; Rosin cerate; Camphor cerate; Cerate of lead acetate; Compound Rosin Cerate
Are viscous preparation intended for warm, external application to a body for purpose of reducing inflammation
CATAPLASM
Are soft semisolid, external applications which either stimulate a body surface or alleviate an inflamed area by supplying medication substance in the presence of heat and mixture
CATAPLASM
Are dental preparation employed primarily as temporary protective coverings for exposed pulps; also for holding medicinal agents in tooth cavities and rebasing of dentures
Cements
are melted prior to application, cooled to only slightly above body temperature, and applied to the affected area with a fine brush. After application this hardens, usually covered with bandage.
Glycerogelatins
Example of Glycerogelatins
Zinc Gelatin Boot
a firm, plastic mass containing 10% zinc oxide in a glycerogelatin base
Zinc Gelatin
treatment of varicose ulcers because of its ability to form pressure bandage
Zinc Gelatin
Zinc Gelatin is also known as
“gelatin boot”
are external application resembling ointments in consistency, but remaining semisolid at body temperature
dressings
dressings liquefy at ___ and remain pliable in thin films below __
50 degree C
28 degree C
Classes of Dressings
- Primary wound dressing or now as wet dressing
- Absorbents - surgical cotton and gauze
- Bandages
- Adhesive tapes
formerly official in the NF VI, was employed
as an air-excluding, soft, pliable, analgesic, splintlike covering for surface denuded by burns
Paraffin dressing
is absorbent gauze saturated with white petrolatum.
Petrolatum Gauze, USP
sterile antibacterial dressings containing nitrofurazone
Furazone gauze pads
any material used as covering, protective, or support for a diseased part
Surgical dressing
Surgical dressing examples
a. Adhesive bandage, USP
b. Gauze bandage
The most relevant studies are performed in ___.
humans
Animal models may be used insofar as they may be effective as predictors of human response such as
- Weanling pig
- Rhesus monkey
- Hairless mouse or rat
Skin penetration may be tested in vitro using:
Various skin tissues (human or animal) in a diffusion cell
Using human skin
Animal skin
Backing, adhesive, and protecting layers Examples of this technology:
TransdermNitro (Novartis)
and Transderm-Scop (Novartis)
MEMBRANE-CONTROLLED TRANSDERMAL SYSTEM Advantage over monolithic systems
release rate of drug
remains constant when the drug solution in the reservoir remains saturated
Prepared by preconstruction of the delivery unit filling the drug reservoir
sealing or lamination
Protects the system from environmental entry and from loss of drug from the system or moisture from
skin
Occlusive or blockade backing membrane
Stores and releases the drug at the skin site
Drug reservoir or matrix sytem
Removed before application and enables drug release
Release liner
Maintains contact with the skin after application
Adhesive layer
Adhesive layer example
Polybutyl acrylate
ADHESIVE LAYER
❑ Must be pressure sensitive
❑ Adheres to the skin with minimal pressure and remains in place for intended
period of wear
❑ Should be non-irritating, permit unimpeded drug flux to the skin, compatible
with all other systems, allow easy peel-off after use
Commonly used as adhesive
polybutyl acrylate
- Patch is worn (at least 4 hours before the anti-nausea effect is required) in a hairless area behind the ear
- Prevents motion sickness, nausea and
vomiting resulting from the use of certain anesthetics and analgesics used in surgery
Transdermal Scopolamine (transderm scop system)
For prophylactic treatment of angina
Transdermal Nitroglycerin
When taken sublingually use of Transdermal Nitroglycerin
relatively low dose, short plasma half-life, high peak plasma levels, and inherent side effects
First transdermal system for hypertension
Transdermal Clonidine (Catapres TTS)
- As adjunct in smoking cessation programs Effective aid in quitting smoking
- Provides sustain blood levels of nicotine replacement therapy
Transdermal Nicotine (Nicotrol)
Treatment of moderate to severe vasomotor symptoms associated with menopause, female hypogonadism, female castration, primary ovarian failure, and atrophic conditions caused by deficient endogenous estrogen production (atrophic vaginitis and kraurosis vulvae)
Transdermal Estradiol
Example of Transdermal Estradiol
Vivelle (Novartis)
For optimal absorption, applied to clean, dry scrotal skin that has been dry-shaved
Transdermal Testosterone
Placed on the scrotum (stretching the scrotal skin with one hand and pressing the adhesive side of the TDDS against the skin with the other hand, holding it in place for about 10 seconds)
Transdermal Testosterone
applied nightly to a clean, dry unabraded area of the skin of the back, abdomen, upper arms, or thighs
Androderm TDDS
intended for localized action are most frequently used to relieve constipation or pain, irritation, itching, and inflammation associated with hemorrhoids.
Rectal suppositories
Vaginal suppositories act as
antiseptic in feminine hygiene and as specific agents
to combat an invading pathogen
as antibacterial and as a local anesthetic preparatory
to urethral examination
Urethral Suppositories:
For system effects, the _____ of the rectum and vagina permits absorption of many soluble drugs
mucous membranes
used frequently as the site for the systemic absorption of drugs
Rectum
for the relief of nausea and vomiting and as a tranquilizer
Prochlorperazine & Chlorpromazine
for opioid analgesia
Morphine and oxymorphone
for the relief of migraine syndrome
Ergotamine tartrate
a nonsteroidal anti-inflammatory analgesic and antipyretic
Indomethacin
for the relief of nausea and vomiting
Ondansetron
Shape of modern rectal suppository
conical or torpedo shaped
length of rectal suppository
2 -3 centimeters
Suppositories for adults weigh
2 grams each
children suppositories weigh
1 gram each
Urethral suppositories for males weigh
4 grams each
Urethral suppositories for females weigh
2 grams each
Vaginal suppositories, also called
pessaries
Vaginal suppositories are usually in shape of
globular (ball), oviform or cone-shaped
Vaginal suppositories weigh
about 5 grams
are pencil-shaped suppositories similar in shape to urethral suppositories but shorter in length about ___
Aural suppositories
32mm long
a lipophilic drug that is distributed in a fatty suppository base in low concentration has loss of a tendency to escape to the surrounding aqueous fluids than would a hydrophilic substance present in fatty base to an extent approaching the saturation
Lipid-water solubility
“The smaller the particle size, the more readily the dissolution of the particle and the greater the chance for rapid absorption”
TRUE
Ability to melt, soften or dissolve at body temperature
Ability to release the drug substance
SUPPOSITORY BASE
SUPPOSITORY BASE is either __ character
hydrophilic or hydrophobic
When a base is not specified, ___is used
Cocoa Butter
Hydrogenated fatty acids of vegetable oils
palm, kernel oil, and cotton seed oil
Fat bases compounds
lycerin with the higher molecular weight fatty acids: palmitic and stearic acids
Water-soluble or water-miscible bases
- Glycerinated gelatin
* polyethylene glycols
Miscellaneous bases are combination of
lipophilic and hydrophilic
• Mixture of oleaginous and water-soluble materials Example
Polyoxyl 40 stearate (mixture of monostearate & distearate esters of mixed polyethylene diols & the free glycols)
Mixtures of many fatty acids (including Cocoa Butter) with emulsifying agents capable of forming W/O emulsion. Also referred to as
hydrophilic suppository base
are widely used today as they are easy to manufacture, more stable and less messy
Vaginal inserts (tablets)