SEMISOLID DOSAGE FORMS

● Ointments
● Creams
● Gels
● Suppositories
● Jellies
● Pastes
● Plasters
● Intended for topical application
● Unmedicated ones are used for physical effects as protectants or lubricants - without
an API

Topical or Dermatological Application

● Topical dermatological product
● Transdermal product

Ointments
● semisolid preparations of one or more therapeutic agents in any of the various
classes of bases and is intended for external uses (application to the skin or mucous
membranes)
● may be:
○ Medicated
○ Non-medicated
● Advantages
○ Easy to apply
○ Multiple effect - soothing, healing
● Limitations
○ Greasy
○ May cause irritation

Qualities of an Ideal Ointment Base

● compatible with the skin
● Stable
● permanent, smooth and pliable (spreadable flexible)
● Non-irritating, non-sensitizing
● Inert - should not affect the API
● able to release incorporated medication

Ointment Bases
● Hydrocarbon Bases (Oleaginous bases)
● Absorption Bases
● Water-Removable bases
● Water-Soluble Bases

Hydrocarbon Bases (Oleaginous Bases)

● Emollient effect - provides the highest occlusive properties
● Protects against escape of moisture
● Effective as occlusive dressings - hydrophobic in nature
 ● Can remain on the skin for long periods without drying out - it will not mix with sweat
● Difficult to wash off - immiscible in water
● Petrolatum USP- purified mixture of semi solid hydrocarbons obtained from
petroleum (semisolid hydrocarbon, melting point 38-68°C, yellow to light amber); also
known as Yellow Petrolatum or Petroleum Jelly)
● White petrolatum – petrolatum that has been wholly or nearly decolorized (not water
washable, occlusive)

● Yellow ointment (95% petrolatum + 5% Yellow wax)

● Yellow wax – purified wax obtained from honeycomb of the bee (Apis mellifera)
● White Ointment, USP – plain petrolatum and white wax (bleached and purified yellow
wax)
● Mineral oil (liquid hydrocarbon from petrolatum)
○

Absorption Bases
● Two Types:
○ Permit incorporation of aqueous solutions (to form water/oil emulsions) e.g.,
hydrophilic petrolatum
○ Water-in-oil emulsions (emulsion bases) that permit incorporation of
additional quantities of aqueous solutions e.g. lanolin
● May be used as emollients
● Do not provide the degree of occlusion afforded by oleaginous bases
● Not easily removed from the skin with water washing since external phase of
emulsion is oleaginous
● Hydrophilic petrolatum (cholesterol, stearyl alcohol, white wax, and white petrolatum)
● Aquaphor - refined hydrophilic petrolatum, takes up 3 times of its weight in water
● Lanolin, USP – obtained from the wool of sheep (Ovis aries), contains not more than
0.25% water

Water-removable base
● Oil-in-water emulsions resembling creams
● Called water washable bases because external phase of emulsion is aqueous, easily
washed from skin - miscible in water
● Example: Hydrophilic Ointment, USP
Water-soluble Base
● contain only water soluble components (water-washable, "greaseless")
● Soften greatly with the addition of water; large amounts of aqueous solutions are not
effectively incorporated, better for the incorporation of nonaqueous or solid
substances
● Polyethylene glycol

Selection of Appropriate Base

● Desired release rate
● Desirability for enhancement of percutaneous absorption - lower contact period on
the skin
● Advisability of occlusion - nt to be trapped
● Short-term or long-term stability of the drug in ointment base - stable API
● Influence of drug on consistency or other features of ointment base - API affects the
viscosity of the ointment base
● Patient factor - dry or weeping (oozing) skin - eczema
● Ability to be removed by water
● Characteristics of surface to which it is applied - surface of skin or mucosal
membrane

Preparation of Ointments
● Incorporation
● Fusion

Incorporation
● Components are mixed until a uniform preparation is attained
● For Solids
○ On small-scale (extemporaneous compounding)
○ Mortar and pestle
○ Spatula - figure of 8
○ To rub ingredients on an ointment slab or nonabsorbent parchment paper
● For Liquids
● Ointment base’s capacity to accept the volume required
○ Small amounts for oleaginous bases
○ Alcoholic solutions may be added
● Ointment or roller mills can be used to force coarsely formed ointments to produce
more uniform and smooth ointments

Fusion
● all or some components melted together and cooled with constant stirring until
congealed; components not melted are added as the ointment is being cooled and
stirred
● Small scale: porcelain or beaker
● Large scale: Steam-jacketed kettles
Preservation of Ointments
● determine and control microbial content
● Employ sterile techniques
● Add antimicrobial preservatives: p-hydroxybenzoates, phenols, benzoic acid, sorbic
acid, quaternary ammonium salts, organic mercury compounds, formaldehyde

Packaging, Storage, and Labeling

● Large-mouth jars or metal or plastic tubes - para madali makuha
● Well-closed containers to protect against contamination
● Store in cool place to protect against separation in heat
● Light resistant containers as needed
● Type of base used for certain ointments required by USP in product labels

Creams
● Semi-solid preparations containing one or more medicinal agents dissolved or
dispersed in a water-in-oil emulsion or oil-in-water emulsion or in another type of
water washable based
● Easier to spread and easier to remove than ointments

Gels
● Semisolid systems consisting of dispersions of small or large molecules in an
aqueous liquid vehicle rendered jelly-like by the addition of a gelling agent
● May be regarded as greaseless ointment

● Gelling agents
○ Synthetic macromolecules
○ Cellulose derivatives
○ Natural gums
Suppositories
● Solid dosage forms intended for insertion into body orifices where they melt, soften or
dissolve and exert local or systemic effects.
● Fusible dosage forms of various weights and shapes, usually medicated, for insertion
into the rectum, vagina, or the urethra where they melt to exert local or systemic
effect
● Advantages
○ Safe and painless administration
○ For drugs which are degraded when orally administered
○ For large dose drugs
○ Duration of action can be controlled
○ For uncooperative patients
○ For nauseous or vomiting patients
● Limitations
○ Unacceptability and poor compliance
○ Leaking - once nag-melt sa body temp, it may result into leaking
○ Problematic insertion

Types of Suppositories
● Rectal
● Vaginal
● Urethral

Rectal Suppository
● Tapered at one or both ends
● Shaped like a bullet
○ Adults = 2 g
○ Infants = 1 g
Vaginal Suppository
● Pessary
● Globular, conical or oviform in shape
● 5g

Urethral Suppository
● Bougie
● Slender, pencil-shaped

Qualities of an Ideal Suppository Bases

● nontoxic and nonirritating
● compatible with a variety of drugs
● melts or dissolves in body fluids - para deliver ang API and para maabsorb; para
hindi na kailangan tanggalin
● stable on storage
● does not interfere with the release and absorption of drug substances

Suppository Bases
● Fatty or Oleaginous bases
● Water-soluble and Water-miscible bases
 ● Miscellaneous bases

Fatty or Oleaginous Bases

● Theobroma oil - obtained from theobroma cacao (chocolate)
● At obtained from roasted seed of Theobroma cacao
● Melts between 30 and 36C (body temp and room temp -in other countries)
● Exhibits polymorphism
● When quickly chilled, turns into a form that has a melting point lower than normal

Cocoa Butter (Theobroma Oil)

● A solid fat expressed from the roasted seeds of Theobroma cacao.
● A pale yellow solid, becoming white on keeping, with a slight odour of cocoa and a
bland taste.
● It is sometimes deodorised.
● Slightly soluble in alcohol; soluble in benzene, chloroform. ether, light petroleum. and
boiling dehydrated alcohol.
Wille and Lutton Convention

Water-soluble and Water-miscible bases

● Glycerinated gelatin, polyethylene glycols, glycol-surfactant combinations
○ Polybase™
● does not need refrigeration
● Does not leak out of the body orifice
● Does not melt at room temp
● slow release of drug

Miscellaneous Bases
● Mixtures of oleaginous and water-soluble or water miscible materials
● Polyoxyl 40 stearate – mixture of monostearate and distearate esters of mixed
polyoxyethylene diols and free glycols

Glycerinated Gelatin
● slower to soften and mix with body fluids
● provides prolonged release
Methods of Preparing Suppositories
● Molding from a melt (fusion or melt-molding)
● Compression-molding
● Hand rolling and shaping

Fusion or Melt-molding
● most common method
● Molds
○ made from stainless steel, aluminum, brass, and plastic
○ Capacity: 6, 12 to 50 g
○ Steps in molding
■ Lubricate the mold - para di mag-stick sa mold
■ Calibrate the mold - for appropriate dose
■ Melt the base
■ Incorporate required medicaments
■ Pour melt into mold
■ Allow melt to cool and congeal into suppositories
■ Remove the suppositories from the mold

Suppository Molds

Compression-Molding
● forcing the suppository mixture into special molds using suppository-making
machines
● for drugs that are thermolabile and for drugs that are insoluble in the base

Hand Rolling and Shaping

● traditional method
● uses grated cocoa butter
● Steps:
1. Triturate cocoa butter with the other ingredients
2. roll into a ball using cooled hands - para di mag-melt sa hands
3. shape into a cylinder using a spatula
4. cylinder is cut into appropriate lengths
5. final shaping is done using the fingertips with the suppositories rolled in a
glassine powder
Packaging, Storage and Labelling of Suppositories
● Well-closed, screw-capped glass containers
● Cocoa butter-based suppositories are wrapped individually into partitioned boxes to
prevent contact and adhesion - magdidikit and melt at a given temp
● Suppositories containing light-sensitive drugs are individually wrapped in either foil or
polyvinyl chloride-polyethylene
● Strip-packaging of individual suppositories separated by tear-along perforations - for
individual dispensing
● Cool place but not frozen
○ Cocoa butter suppositories - below 30°C; preferably in a refrigerator
○ Glycerinated gelatin suppositories - below 35°C
○ Polyethylene glycol suppositories – room temperatures

Pastes
● Semi-solid preparations intended for application to the skin
● Contain a larger percentage of solid material than ointments
● Will not soften and flow after application

Jellies
● gels which contain a high proportion of liquid, usually water
● Usually contains an antimicrobial preservative due to its susceptibility to
contamination - due to water
● Stored in tubes which are tightly closed when not in use

Plasters
● adhesive masses spread on a backing of paper, fabric, moleskin or plastic
● Adhesive: rubber base or synthetic resin
● Applied to the skin to provide prolonged contact

Glycerogelatins
● plastic masses containing gelatin (15%), glycerin (40%), water (35%) and an added
medicinal substance (10%) such as zinc oxide.
● applied to the skin for the long term, melted before application, cooled to slightly
above body temperature, applied to affected area with a fine brush
 ● Ex: zinc gelatin used in the treatment of varicose ulcers

Compendial Requirements

Microbial Content
● Should meet acceptable microbial limits
● Ophthalmic preparations required to be sterile
● Preparations susceptible to microbial growth may contain antimicrobial preservatives
like methylparaben, propylparaben, phenols, benzoic acid, sorbic acid, and
quaternary ammonium salts
● Preparations that contain water tend to support microbial growth
● Microbial limits are set for certain articles in the USP
○ Betamethasone Valerate Ointment
■ absence of Pseudomonas aeruginosa and Staphylococcus aureus

Minimum Fill
● net weight or volume of the contents of filled containers to ensure proper contents as
against label claim

Additional Standards
● Manufacturer’s test for viscosity and in-vitro drug release
○ diffusion cell studies - Franz Cell Diffusion -