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Semisolid Excipients
Semisolid Excipients
Semisolid Excipients
• Semi solids are the topical dosage form used for the therapeutic, protective or
cosmetic function. They may be applied to the skin, or used nasally, vaginally
or rectally.
• Pharmaceutical semisolid dosage preparations include:
• Ointments
• Pastes
• Creams
• Gels
• They contain one or more active ingredients dissolved our uniformly dispersed
in a suitable base and any suitable excipients such as emulsifiers, viscosity
increasing agents, anti-microbial agents, anti-oxidants, or stabilizing agents
etc.
SEMISOLID DOSAGE FORM
• Advantages:
• It is used externally
• Probability of side effect can be reduced
• Local action
• First pass gut and hepatic metabolism are avoided.
• Patient compliance is increased; the drug termination is problematic cases is
facilitated as compared with other routes of drug administration.
• Disadvantages:
• There is no dosage accuracy in this type of dosage form
• The base which is used in the semi-solid dosage form can be easily oxidized.
• If we go out after using semi-solid dosage form problems can occur.
Different Types of Semi-Solid - Ointment
• TYPES:
• Hydrophobic Ointments
• Water-Emulsifying Ointments
• Hydrophilic Ointments
Different Types of SemiSolid - Ointment
• Hydrophobic Ointments:
• Hydrophobic (lipophilic) ointments are usually anhydrous and can absorb only small amounts
of water.
• Typical bases used for their formulation are water-insoluble hydrocarbons such as hard, soft
and liquid paraffin, vegetable oil, animal fats, waxes, synthetic glycerides, and
polyalkylsiloxanes.
• Water-Emulsifying Ointments:
• Water-emulsifying ointments can absorb large amounts of water.
• They typically consist of a hydrophobic fatty base in which a w/o agent, such as wool fat,
wool alcohols, sorbitan esters, monoglycerides, or fatty alcohols can be incorporated to render
them hydrophilic.
• They may also be w/o emulsions that allow additional quantities of aqueous solutions to be
incorporated.
• Such ointments are used especially when formulating aqueous liquids or solutions.
• Hydrophilic Ointments:
• Hydrophilic ointment bases are miscible with water.
• The bases are usually a mixture of liquid and solid polyethylene glycols (macrogols).
Different Types of Semi-Solid - creams
• Types:
• Hydrophobic Gels:
• Hydrophobic gel (oleogel) bases usually consist of liquid paraffin with polyethylene or
fatty oils gelled with colloidal silica or aluminum or zinc soaps.
• Hydrophilic Gels:
• Hydrophilic gels (hydrogel) bases usually consist of water, glycerol, or propylene glycol
gelled with suitable agents such as tragacanth, starch, cellulose derivatives, carboxyvinyl
polymers, and magnesium aluminium silicates.
Different Types of Semi-Solid - pastes
• Paste is a substance that behaves as a solid until a sufficiently large load
or stress is applied, at which point it flows like a fluid.
• Types:
• Fatty Pastes:
• These formulations consist of fatty or oleaginous bases.
• Ex : Zinc oxide paste.
• Aqueous Gel Pastes:
• These are prepared with water miscible bases.
• Ex : Sodium hydromethyl cellulose paste, Titanium dioxide paste.
• Hydrocolloid Pastes:
• These preparations consist of hydrocarbon bases.
• Ex : Tooth paste, Zinc oxide gelatin paste.
EXCIPIENTS USED IN PREPARATION OF
SEMI SOLIDS
• Bases
• Preservative
• Humectants
• Anti-oxidants
• Emulsifier
• Gelling agent
• Permeation enhancer
• Buffers
EXCIPIENTS USED IN PREPARATION OF SEMI SOLIDS
• Bases:
• It is one of the most important ingredients used in the formulation of semisolid
dosage form.
• Ointment bases do not really act as the carriers of medicaments, but they also control
the extent of absorption of medicaments incorporated in them.
• Ideal properties of base:
• They should be.,
• Inert, non-irritating and non-sensitizing.
• Compatible with skin pH and drug.
• Good solvent and/or emulsifying agent.
• Emollient, protective, non-greasy and easily removable.
• Release medicament readily at the site of application.
• Pharmaceutically elegant and possess good stability.
EXCIPIENTS USED IN PREPARATION OF
SEMI SOLIDS
• Preservative:
• To inhibit the growth of contaminating microorganisms, so require the
addition of chemical antimicrobial preservatives to the formulation.
• Eg: Para-hydroxybenzoates (parabens), phenols, benzoic acid, sorbic acid,
quaternary ammonium salts and other compounds.
• Humectants:
• A humectant is a hygroscopic substance.
• Humectants are used to,
• Increase the solubility of active ingredient.
• To elevate its skin penetration.
• Elevate the hydration of skin.
EXCIPIENTS USED IN PREPARATION OF
SEMI SOLIDS
• Anti-Oxidants:
• Oxygen is a highly reactive atom that is capable of becoming part of
potentially damaging molecules commonly called "free radicals".
• Free radicals are capable of attacking the healthy cells of the body, causing
them to lose their structure and function. To prevent this anti-oxidants are
used.
• Eg: Butylated hydroxy anisole, Butylated hydroxy toluene.
• Emulsifier:
• An emulsifier (emulgent) is a substance that stabilizes an emulsion by
increasing its kinetic stability.
• Must reduce surface tension for proper emulsification.
• Prevents coalescence.
• Ability to increase the viscosity at low concentration.
EXCIPIENTS USED IN PREPARATION OF
SEMI SOLIDS
• Gelling Agents:
• Gelling agents are the gel-forming agents when dissolved in a liquid phase as a colloidal
mixture forms a weakly cohesive internal structure.
• They are organic hydrocolloids or hydrophilic inorganic substances.
• In semisolid dosage form, gelling agents are used at a concentration of 0.5%–10%.
• Eg: Tragacanth, pectin, starch, carbomer, sodium alginate, gelatin etc.
• Permeation Enhancers:
• Skin can act as a barrier.
• With the introduction of various penetration enhancers, penetration of the drug through skin
can be improved.
• Eg: Oleic acid
EXCIPIENTS USED IN PREPARATION OF
SEMI SOLIDS
• Buffers:
• Buffers are added for various purposes such as,
• Compatibility with skin.
• Drug solubility.
• Drug stability.
• Influence ionization of drug. Skin, due to its weak acidic nature, tolerate weak acidic
preparations.
• Eg: Sodium acetate, sodium citrate
SEMISOLID EXCIPIENTS EXAMPLES