semisolid Flashcards
Are dosage forms intended for insertion into body orifices (rectum, vagina, urethra) where they melt,soften,or dissolve and exert a local or systemic
vagina, urethra) where they melt, soften, or dissolve and exert a local or systemic effect where the base plays an important role in this respect.
Suppositories
These are globular, oviform, or cone-shaped and typically weigh 5g with a cocoa butter base, though weight varies by base and manufacturer.
Vaginal Suppositories (Pessaries)
Used for vaginal yeast infections.
Clotrimazole
Treats bacterial vaginosis.
Metronidazole
Often used in hormone replacement therapy or fertility treatments.
Progesterone Suppositories
Are 32 mm long, cylindrical, with tapered or bullet-shaped ends. Adult
suppositories weigh 2g (cocoa butter base), while pediatric ones are smaller
(1g) and pencil-shaped. They are used for local or systemic effects.
Rectal Suppositories
For constipation relief.
Bisacodyl
Used to reduce fever or relieve pain.
Acetaminophen
For treating hemorrhoids or rectal inflammation.
Hydrocortisone
These are slender and pencil-shaped. Male versions are 140 mm long, 3–6 mm in diameter, and weigh 4 g. Female versions are 70 mm long and 2 g, both
typically using cocoa butter as the base
Urethral Suppositories (Bougies)
For erectile dysfunction; inserted directly into the urethra
Alprostadil
Problems in Formulation
• Water in Suppositories
• Hygroscopicity
• Drug-excipient Interactions
• Viscosity
• Brittleness
• Density
• Lubrication of Molds
• Volume Contraction
• Displacement Value
• Weight and Volume Control
• Rancidity
It may be defined as the number of parts by weight of medicament that displaces one part by weight of the base.
Displacement Value
It occurs when the active ingredients and excipients are not evenly dispersed within the base.
This can result from inadequate mixing time, improper use of mixing equipment, incorrect temperature control, or operator error.
Non uniformity of the mix
When the mixing time is too short, ingredients do not achieve uniform distribution, while overmixing can lead to overheating and degradation of sensitive components.
It occurs when active or excipient substances separate out from the
mixture, typically due to inadequate mixing, incorrect temperature control, or operator errors.
This often happens when the temperature drops below the solubility limit of certain components, or when mixing equipment fails to maintain proper agitation.
Precipitation of Components
It is a critical issue during mixing that can compromise the stability and efficacy of the product. This typically results from excessive temperatures during mixing, prolonged batching times, or the use of unsuitable equipment.
Decomposition of Components
This issue arises when the suppository splits or tears during removal from the mold. The primary causes include improper mold design, surface irregularities, or rapid cooling of the
suppository base, which leads to uneven shrinkage and stress.
Tearing and Splitting
It occurs when suppositories fail to close properly, often due to insufficient
filling of molds, overheating during sealing, or poor alignment of mold parts.
Improper Sealing
It manifest as imperfections like air bubbles or uneven textures on the
suppository’s exterior. They are commonly caused by trapped air during mixing or pouring, contamination in the base or molds, or incorrect pouring temperatures.
Surface Defects
These are common structural issues.
Soft suppositories, cracking, and granulation.
It typically occur due to inadequate solidification, which results from insufficient cooling time or
an improper base composition with a low melting point
Soft Suppositories
This often results from rapid cooling, which creates stress fractures in the
base. This can also occur due to poor compatibility between the base and the active ingredient.
Suppository Cracking
This may arise from poor mixing, leading to uneven dispersion of the active ingredient, or from recrystallization during storage.
Granulation
It is a critical issue in suppository production, as it affects dosage accuracy. This problem is caused by inconsistent filling of molds, improper mixing, or variations in base density.
Weight Variation
It refers to the separation or breaking of a molded solid or semi-solid dosage form into two or more parts. It often occurs along a visible plane or seam and
may compromise the product’s
structural integrity
Splitting
It involves the development of visible lines or fractures on the surface or throughout the bulk of the dosage form. It may result in partial or complete disintegration of the product.
Cracking
It is the formation of small, concave depressions or holes on the surface of the dosage form. It is typically a surface defect that does not penetrate deeply into the product.
Pitting
Are semi-solid preparations containing one or more medicinal agents dissolved or dispersed in either an oil- in-water emulsion or in another type of water-washable base.
Creams
Patients and physicians prefer creams to ointments because they are easier to spread and remove than many ointments.
These are oil-in-water emulsions containing large percentage of water and stearic acid or other oleaginous
components.
Vanishing Creams
It includes nonionic surfactants, detergents, and soaps.
Emulsifying agents
These are usually formed from a fatty acids in the oil phase hydrolyzed by a base dissolved in the aqueous phase in situ during the preparation of creams.
Soaps
Four (4) main ingredients of cold cream:
■ Water
■ Oil
■ Emulsifier
■ Thickening agent
Are semi-solid preparations intended for external applications to the skin or mucous membranes, usually but not always, they contain medicinal agents.
Ointments (Salve or Chrisma)
It makes the skin more pliable.
Emollients
In which to incorporate medication.
Vehicle
It prevents harmful substances from
coming in contact with the skin
Protective Barrier
Classification of Ointment Based on Composition
Oleaginous bases
Absorption bases
Water-removable bases
Water-soluble bases
Classification of Ointment Based on Penetration
Epidermic ointments
Endodermic ointments
Diadermic ointments
On the application to the skin, they have an emollient effect, protect against the
escape of moisture, effective as occlusive dressings, can remain on the skin for long periods without drying out, and because of their immiscibility with water, and are difficult to wash off.
Oleaginous Bases (Hydrocarbon Bases)
Examples of Oleaginous Bases
• Petrolatum, USP (Yellow Petrolatum and Petroleum Jelly)
• White Petrolatum, USP (White Petroleum Jelly)
• White Ointment, USP
These bases may be used as emollients, although they do not provide the degree of occlusion afforded by the oleaginous base, and are not easily removed from the skin with water washing, because the external phase of the emulsion is oleaginous.
Absorption Bases
Examples of Absorption Bases
• Hydrophilic Petrolatum, USP
• Lanolin, USP (Anhydrous Lanolin/Wool Fat)
• Modified Lanolin, USP
They may be diluted with water or aqueous solutions. They can absorb serous discharges.
Water-removable Bases
Examples of Water-removable Bases
Hydrophilic Ointment, USP
Cold Cream
Vanishing Cream
Dermovan
Unibase
They do not contain oleaginous components. They are completely water washable and often referred to as greaseless.
Because they soften greatly with the addition of water, large amounts of aqueous solutions are not effectively incorporated into these bases.
Water-Soluble Bases
Examples of Water-Soluble Bases
• Polyethylene Glycol (PEG)
• Propylene Glycol and Propylene Glycol-Ethanol
Demonstrate no or at the most very slight penetration.
Epidermic Ointment
Possess some powers of penetration into the deeper layers of the skin
Endodermic Ointments
Which penetrates the skin thus offering a better opportunity for absorption of the medicaments.
Diadermic Ointment
Creams or Ointments products are:
Emulsion
containing of waxes, emollients and lubricants dispersed in it.
Oil phase
containing emulsifying, stabilizing and thickening agents, preservatives and in
some cases, colorant
Water phase
These are dispersed in either phase or added when the emulsion has been formed and allowed to cool.
Active Ingredients
