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Pharmaceutics
Semi-Solid Preparations
60
Biology
Graduate
02/25/2012

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Term
creams
Definition
-semi-sold preparation in a o/w emulsion of other water washable base
Term
ointments
Definition
greasy semi-solid preparations often anhydrous containing dissolved or dispersed drug
Term
gels
Definition
-2 component semi-solid systems rich in liquid containing a continuous structure providing solid-like properties
Term
most semi-solid preparations are intended for
Definition
topical preparation
Term
antiseptic
Definition
-wound cleanse
Term
antipruritic
Definition
-for itch
Term
kerotolytic
Definition
-wort/corn remover
Term
astringent
Definition
ache/pores/blood vessels
Term
non medicated
Definition
-emollient (moisturizer)
-protectant
-lubricating
Term
topical preparations
Definition
-most used for localized effect
-drug penetrates INTO skin or mucous
-skin is target organ
-little systemic effect (concerns only during pregnancy)
Term
transdermal preparations
Definition
-intended for systemic delivery
-drug penetrates THROUGH skin
-skin is BARRIER not TARGET
Term
creams in detail
Definition
-thick emulsions
-o/w-rub into skin (vanishing cream)
-w/o-emollient and cleansing (water evaporates)
-used topically,rectally,vaginally
-patience preference (spreadability,washability,w/o emulsion over ointment)
Term
ointments in detail
Definition
-greasy appearance and feel
-can be medicated or not medicated
-used externally for skin or mucous membranes
-5 different base types
Term
5 ointment base types
Definition
-hydrocarbon (oleaginous bases)
-absorption
-w/o
-o/w (water removable)
-water-soluble
Term
hydrocarbon bases
Definition
-oleaginous
-emollient effect
-prevent loss of moisture
-difficult to wash off
-used in occlusive dressings (air and water tight)
Term
*hydrocarbon bases examples
Definition
-petrolatum
-yellow ointment (yellow wax and petrolatum)
-white ointment
Term
absorption bases
Definition
-permits aqueous media to be absorbed forming w/o *emulsion
-used as emollient
-oleaginous, not easily water washable
-useful for adding small amount of aqueous media into a hydrocarbon base
-NOT an emulsion to start with
Term
*absorption bases examples
Definition
-hydrophilic petrolatum
-AQUAPHOR
-lanolin (wool from sheep)
Term
w/o emulsion bases
Definition
-permits incorporation of additional amount of aqueous media
-used as emollients
-oleaginous, not easily water washable
-*emulsion to START with
Term
*w/o emulsion bases examples
Definition
-cold cream
-EUCERIN
-NIVEA
Term
o/w emulsion
Definition
-water removable bases
-o/w *emulsions resembling creams
-contain emulsifying agents (emulsifying bases)
-easily spreadable, water washable, can add aqueous media
-termed "water washable bases"
Term
*o/w emulsions bases examples
Definition
-hydrophilic ointment (prepared by heating oil phase and water phase and combine mixing until it congeals)
-DERMABASE
Term
water soluble bases
Definition
-do not contain oleaginous components (greaseless)
-water washable
-do not incorporate large amounts of aqueous media-will soften
-incorporates solid substances
Term
*water-soluble bases examples
Definition
-PEG
-POLYBASE
Term
PEG
Definition
-combine PEG 3350 and PEG 400
-number =MW
-less than 600=colorless
-600-1000=semi-solid
-greater than 1000=white, wax like
Term
selection of appropriate base
Definition
-desirability of occlusion of moisture from skin
-stability of drug in base
-desired release rate from base
-desriability for topical or percutaneous absorption
-effect of drug on base consistency
-desire for water-washability
Term
preparation of ointments: incorporation
Definition
-mixed until a uniform preparation is formed using a mortar and pestle or ointment slab and spatula
-use stainless steel spatula
-incorporate solid into a small amount of ointment then add additional ointment
-reduce particle size of powder to prevent grittiness
-may dissolve in a solvent
Term
*levigating agent
Definition
-used to disperse solid before incorporations
-*for oleaginous-mineral oil, cottonseed oil
-*for aqueous-glycerin, propylene glycol, PEG 400
Term
unguator
Definition
electronic mortar and pestle
Term
prep of ointments incorporation of a liquid
Definition
-use appropriate base
-only if base can accept liquid and quantity
-pile ointment and make hole in center to place liquid
-may use small amount of hydrophilic base to incorporate liquid, then add to hydrophobic base
-may add a co-solvent or levigating agents
Term
*preparation of ointments : fusion
Definition
-all or most components are melted,combined, and stirred until congealed (may need to head each phase separately)
-heat labile components added to cooling phase
-prepared in beaker or porcelain dish (pharmacy) or stem-jacketed kettle (industry)
-once congealed-pass thought ointment mill, ointment tile until spatula or mortar/pestle
Term
paste and examples
Definition
-semi-solids that generally contain larger proportion of solid material than ointments
-stiffer, higher drug content
-no levigating agent
-stay in place better, absorbs secretions
-ex.zinc oxide paste, toothpase
Term
plasters
Definition
-solids or semi-solids adhesive masses applied usually to skin
-provides prolonged contact at site
-ex. salicyclic acid plaster for corns
Term
gels in detail
Definition
-semi-solid systems consisting of dispersions of small or large molecules in an aqueous liquid vehicle
-particles form an interlacing network, providing rigidity to the product
-continuous phase is held within the meshes
-very small proportions are needed to form gel structure 1-5%
-can vary in rigidity due to gelling agent and quantity
-are often clear if all additives are soluble in dispersion medium
-jelly- a very thin consistancy
Term
mechanisms for gelling agents
Definition
-macromolecule entanglement
-attraction between particles-Van der Waals, hydrogen bonds
-cross-linking of macromolecules
Term
types of gelling agents
Definition
-thermal setting gels
-single-phase gels
-2-phase gels (magma)
-hydrogels
-organogels
-soluble macromolecules
Term
thermal setting gels
Definition
-gels that set by a change in heat to form the network or rigidity
Term
single phase gels
Definition
-soluble macromolecules distributed uniformly throughout media (colloidal dispersion)
Term
2-phase gels
Definition
-gel mass consists of floccules or distinct particles
-composed of water insoluble particles that hydrate
-thixotropic suspensions upon standing, liquid after shaking
-ex. milk of magnesia, Al hydroxide gel, bentonite magna
Term
hydrogels
Definition
-water as dispersion medium
-highly absorbant
Term
organogels
Definition
-organic solvent or oils as dispersion medium
Term
soluble macromolecules (one-phase)
Definition
-natural polymers
-semi-synthetic cellulose derivatives
-synthetic polymers
Term
natural polymers
Definition
-acacia (arabic gum)
-tragacanth
-xanthan gum
-sodium alginate
-natural gums
Term
acacia
Definition
-from stems of acacia tree
-advantages-sugar free, stable over pH range, unafffected by high ion concentrations
-disadvantages-palatablity (taste), promotes microbial growth, difficult to prepare
Term
semisynthetic polymers
Definition
-methylcellulose
-HPC
-HEC
-Na CMC
-HPMC
Term
methylcellulose
Definition
-methylation of cellulose
-water forms hydrogen bonds with cellulose
-disadvantages-must heat to prepare, difficult dispersion
Term
HPC
Definition
-thermosetting gel-heat then cool
Term
HEC
Definition
increase temp = increase thickness?
Term
Na CMC
Definition
-prepared hot or cold
Term
synthetic polymers
Definition
-carbomer
-poloxamer
Term
carbomer
Definition
-copolymer of acrylic acid
-most stable, less susceptible to microbial growth
-more solid (thick gels than celluloses)?
-creates low pH solutions
-most use a neutralizer to increase pH-gel?
-used primarily for topical (also approved for internal use)
-thickening agents (0.1%-0.5%)
-gel(0.5%-2%)
Term
poloxamer (PLURONICS)
Definition
-co-block polymer of ethylene oxide and propylene oxide
-forms clear, rigid gels at 20%
-viscosity based on type and grade
-forms clear, thermoreversibile gels (liquid at cool temp,gel at higher temp)
-ex. methimazole in PLO gel (for cats)
Term
characterisitcs of gels
Definition
-consistency from soft jelly to rigid breaking gelatin
-syneresis
-swelling
-imbibition
Term
syneresis
Definition
-liquid pressed out from a gel upon standing (bleeding)
Term
swelling
Definition
-taking up of a liquid by a gel with an increase in volume
-liquids that solvate a gel
Term
imbibition
Definition
-taking up of a liquid WITHOUT an increase in volume
Term
semi solid microbial requirements
Definition
-NOT required to be sterile (except opthalmic ointments)
-must contain preservatives
-some microbial limit tests stated by USP
-prevention of contamination (focus on good manufactuing process and environmental controls)
-special preparations may require additional tests (vaginal preps-yeasts,molds)
Term
semi solids packaging
Definition
-topical-large mouth jars or metal/plastic tubes
-nasal,vaginal,rectal-plastic/metal tubes
-airtight containers
-storage-protection from heat
Term
ointment jars packaging
Definition
-opaque plastic jar
-transfer to jar with spatula
-package at bottom or sides
-no trapped air
-curl on center surface of ointment
-lids or rim should no contain ointment
-nothing on inside cap
-fusion oints can be poured into jars to congeal
-pharmaceutically elegant
Term
tubes packaging
Definition
-composed of aluminum or plastic
-may include an applicator with product
-filled from back end, opposite the cap
-automatic filling with spatula
-can use glossy paper as a guide
-plastic tubes have hot sealer
-metal tubes are folded or crimped
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