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Questions and Answers
What is the primary role of wetting agents in a suspension?
What is the primary role of wetting agents in a suspension?
Which of the following wetting agents is specifically noted for parenteral use?
Which of the following wetting agents is specifically noted for parenteral use?
What is a disadvantage of using surfactants as wetting agents?
What is a disadvantage of using surfactants as wetting agents?
What effect do trivalent ions have when added to a flocculated suspension?
What effect do trivalent ions have when added to a flocculated suspension?
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Which hydrophilic polymer is NOT listed among those used as wetting agents?
Which hydrophilic polymer is NOT listed among those used as wetting agents?
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How do solvents like glycerol contribute to wetting in a suspension?
How do solvents like glycerol contribute to wetting in a suspension?
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When might the use of excessive electrolyte in a suspension lead to problems?
When might the use of excessive electrolyte in a suspension lead to problems?
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What is the function of hydrophilic polymers when added to a solid in a liquid medium?
What is the function of hydrophilic polymers when added to a solid in a liquid medium?
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What is the maximum concentration of Carbapol that can be used mainly for external applications?
What is the maximum concentration of Carbapol that can be used mainly for external applications?
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How do hydrated silicates like Bentonite need to be processed prior to use in external preparations?
How do hydrated silicates like Bentonite need to be processed prior to use in external preparations?
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Which of the following cellulose derivatives is used as a suspending agent?
Which of the following cellulose derivatives is used as a suspending agent?
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What is the potential issue arising from high concentrations of sweetening agents in a suspension?
What is the potential issue arising from high concentrations of sweetening agents in a suspension?
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Which suspending agent can be used in both internal and external applications?
Which suspending agent can be used in both internal and external applications?
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What role do buffers play in suspension formulations?
What role do buffers play in suspension formulations?
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Which of the following substances can be used as humectants in suspension formulations?
Which of the following substances can be used as humectants in suspension formulations?
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What is the purpose of preservatives in suspension formulations?
What is the purpose of preservatives in suspension formulations?
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What is the effect of non-ionic surfactants on particle charge density?
What is the effect of non-ionic surfactants on particle charge density?
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What happens to the positive zeta potential when monobasic potassium phosphate is added to bismuth subnitrate particles?
What happens to the positive zeta potential when monobasic potassium phosphate is added to bismuth subnitrate particles?
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Which statement correctly explains the correlation between zeta potential and sedimentation volume?
Which statement correctly explains the correlation between zeta potential and sedimentation volume?
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What type of agent is dibasic potassium phosphate when used with bismuth subnitrate suspension?
What type of agent is dibasic potassium phosphate when used with bismuth subnitrate suspension?
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Which of the following polymeric flocculating agents creates a gel-like network in the dispersed phase?
Which of the following polymeric flocculating agents creates a gel-like network in the dispersed phase?
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What occurs to the sedimentation volume when the zeta potential becomes sufficiently negative?
What occurs to the sedimentation volume when the zeta potential becomes sufficiently negative?
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Why does acacia gum become acidic upon storage?
Why does acacia gum become acidic upon storage?
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What is a disadvantage of sodium alginate when used in dispersions?
What is a disadvantage of sodium alginate when used in dispersions?
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What happens when the sedimentation volume 'F' is equal to 1?
What happens when the sedimentation volume 'F' is equal to 1?
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How is the degree of flocculation 'β' calculated?
How is the degree of flocculation 'β' calculated?
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What is the likely result of using large particles in ophthalmic suspension?
What is the likely result of using large particles in ophthalmic suspension?
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What does a sedimentation volume 'F' greater than 1 indicate?
What does a sedimentation volume 'F' greater than 1 indicate?
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Which is NOT a method of preparing suspensions?
Which is NOT a method of preparing suspensions?
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What parameter is considered more fundamental than sedimentation volume in suspension analysis?
What parameter is considered more fundamental than sedimentation volume in suspension analysis?
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What term describes the final sediment volume of deflocculated suspension?
What term describes the final sediment volume of deflocculated suspension?
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What is the outcome of particle size growth during storage of a drug?
What is the outcome of particle size growth during storage of a drug?
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Study Notes
Pharmaceutical Suspension
- Suspensions are pharmaceutical preparations where solid particles are dispersed in a liquid medium
- Sedimentation parameters are used to assess suspension stability.
- Sedimentation volume (F): The ratio of final sediment volume (Vf) to the original suspension volume (Vo). A value of F < 1 indicates the final sediment volume is less than the original suspension volume. F = 1 indicates the final sediment volume equals the original suspension volume. If F > 1, the final sediment volume exceeds the original suspension volume.
- Degree of flocculation (β): A more fundamental parameter relating the volume of flocculated sediment to a deflocculated system. It is calculated as β = Ff/Fα = Vf/Vα, where Fα and Vα represent the sedimentation volume and final sediment volume of a deflocculated system, respectively.
Preparation of Suspensions
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Particle Size Control:
- Large particles (greater than 5 µm) in ophthalmic suspensions cause irritation.
- Large particles in parenteral suspensions can block needles.
- Changes in temperature can cause drug crystallization, increasing particle size during storage. Drug solubility can be affected, and smaller particles may have higher solubility than larger ones.
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Use of Wetting Agents:
- Wetting agents reduce interfacial tension between solid particles and liquid medium.
- This allows displacement of air from the solid surfaces.
- Adequate wetting of the particles throughout the liquid is achieved.
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Types of Wetting Agents:
- Surfactants (HLB value 7-9) at concentrations of up to 0.1%
- Tweens and Spans (oral use)
- Sodium lauryl sulfate, Sodium dioctylsulphosuccinate (external use)
- Tweens, Pluronics, Lecithin (parenteral use)
- Disadvantages of surfactant use: excessive foaming, and the creation of a deflocculated system.
- Surfactants (HLB value 7-9) at concentrations of up to 0.1%
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Hydrophilic Polymers and Hydrocolloids:
- Materials that coat hydrophobic particles with a multimolecular layer, changing the solid from hydrophobic to hydrophilic
- Examples: acacia, bentonite, tragacanth, alginates, cellulose derivatives.
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Solvents:
- Alcohol, glycerol, and glycols reduce liquid/air interfacial tension, aiding wetting in the dispersion medium
Use of flocculating agents
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Electrolytes:
- Sodium salts of acetates, phosphates, and citrates are common electrolytes
- Addition of electrolytes reduces zeta potential of dispersed particles, promoting flocculation
- Flocculating ability of electrolytes depends on the valence of their counter-ions. Trivalent ions are more effective but less used due to toxicity. If hydrophilic polymers are present, these polymers may be precipitated if using trivalent ions
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Surfactants:
- Ionic surfactants help by neutralizing the charge on each particle
- Non-ionic surfactants may affect the charge density of a particle but form a loose structure through linear configuration adsorption.
Viscosity Modifiers (Suspending Agents)
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Polysaccharides:
- Acacia gum: acidification and potential oxidation-related problems
- Tragacanth: better thickening agent than acacia
- Alginates: Sodium alginate is the most used, but its anionic character makes it incompatible with heavy metals. Large increase in viscosity when calcium chloride is added
- Starch: Sodium starch glycollate, a starch derivative, is used.
- Water-soluble cellulose: Derivatives like Methyl cellulose, Hydroxyethyl cellulose, Carboxymethyl cellulose and Microcrystalline cellulose
- Hydrated silicates: Bentonite, Magnesium aluminum silicate (Veegum), Hectorite, and Carbopol
Other Formulation Additives in Suspensions
- Buffers: Maintain chemical stability and control tonicity
- Density Modifiers: Glycerol, propylene glycol, and sucrose keep suspension particles at a consistent density to prevent sedimentation.
- Flavours, colours, and perfumes: Improve organoleptic properties of the suspension
- Humectants: Prevent drying to skin after application
- Preservatives: prevent microbial growth, e.g. heating dry powder, autoclaving
- Sweeteners: Sorbitol, glycerol, or sucrose can negatively impact the suspension's properties and need to be accounted for
Stability Testing of Suspension
- Physical stability: Analyzed through sedimentation rate, initial/final volume, flocculation value, and redispersion ease.
- Chemical stability: Assessed by concentration of active ingredients over time.
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Description
Test your knowledge on pharmaceutical suspensions, including their preparation and stability parameters. This quiz covers key concepts such as sedimentation volume and degree of flocculation. Challenge yourself to understand the intricacies of suspension formulations.