Pharmaceutical Suspensions Overview
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Questions and Answers

What is one primary purpose of formulating suspensions for parenteral administration?

  • To increase the solubility of the drug
  • To prolong the action of the drug (correct)
  • To enhance the drug's absorption rate
  • To create a more palatable form of the drug

Which vehicle is advantageous for prolonging the activity of parenteral suspensions?

  • Fixed oils such as arachis oil (correct)
  • Alcohol-based vehicles
  • Glycerin-based vehicles
  • Aqueous vehicle

What is a significant factor in controlling the duration of activity in parenteral suspensions?

  • The color of the suspension
  • pH level of the suspension
  • Varying particle size (correct)
  • Temperature of storage

Which of the following is NOT a characteristic of small particles in suspensions?

<p>They can block hypodermic needles over 25 µm (A)</p> Signup and view all the answers

Which of these features is important for the selection of particle sizes in suspensions?

<p>Maintaining a narrow particle size range (D)</p> Signup and view all the answers

What role do polymorphic forms of a drug play in suspensions?

<p>They affect solubility and stability (B)</p> Signup and view all the answers

What is the purpose of optimizing the particle size in aerosol suspensions?

<p>To control the rate of drug release (D)</p> Signup and view all the answers

Which ingredient is included in Betolvex® for enhancing Vitamin B12 preparations?

<p>Aluminium monostearate (C)</p> Signup and view all the answers

What characteristic defines flocculated systems in the context of suspension formulation?

<p>Loose sediments that are easily redispersed (C)</p> Signup and view all the answers

Which component is primarily responsible for increasing viscosity in a deflocculated suspension?

<p>Suspending agent (D)</p> Signup and view all the answers

What is the ideal outcome of formulating suspensions for optimum physical stability?

<p>Flocculated particles in a structured vehicle (D)</p> Signup and view all the answers

What initial step is necessary for preparing a suspension from a powder?

<p>Wetting the powder in a vehicle (A)</p> Signup and view all the answers

What potential issue arises from the fast sedimentation rate in flocculated systems?

<p>Accurate dosage becoming challenging (D)</p> Signup and view all the answers

Which combination is suggested for optimum physical stability in suspensions?

<p>Wetting agent, flocculating agent, and suspending agent (D)</p> Signup and view all the answers

What is the purpose of using a flocculating agent in suspension formulation?

<p>To produce easily resuspended clumps that settle rapidly (C)</p> Signup and view all the answers

In the context of suspension formulation, what challenge is posed by air-adsorbed layers on particles?

<p>They cause particles to float on the surface (B)</p> Signup and view all the answers

What is the primary use of Bentonite?

<p>For external use (B)</p> Signup and view all the answers

Which of the following can be used both internally and externally?

<p>Veegum (C)</p> Signup and view all the answers

What property do Laponites exhibit compared to natural products?

<p>Consistency in composition (B)</p> Signup and view all the answers

What is the role of buffers in formulation additives?

<p>To stabilize pH (D)</p> Signup and view all the answers

Which of the following is NOT a function of density modifiers?

<p>Increase viscosity (D)</p> Signup and view all the answers

What role does Tween 80 serve in the Metronidazole Oral Suspension formulation?

<p>Wetting agent (C)</p> Signup and view all the answers

Which ingredient is commonly used to prevent formulations from drying out after application to the skin?

<p>Glycerol (C)</p> Signup and view all the answers

Which of the following corresponds to the role of Methyl paraben in the suspension?

<p>Preservative (D)</p> Signup and view all the answers

What is the primary purpose of preservatives in formulations?

<p>To prevent microbial growth (A)</p> Signup and view all the answers

Which of the following sweetening agents is considered a synthetic sweetener that may affect flocculation?

<p>Saccharine (A)</p> Signup and view all the answers

According to Stokes' Law, which factor does NOT influence the velocity of sedimentation?

<p>Color of the particle (C)</p> Signup and view all the answers

The sedimentation volume, F, is defined as which of the following?

<p>The ultimate volume of sediment to the original volume (A)</p> Signup and view all the answers

Which ingredient in the formulation primarily acts as a thickening agent?

<p>Acacia (B)</p> Signup and view all the answers

Which factor is inversely proportional to the velocity of sedimentation?

<p>Viscosity of the dispersion medium (C)</p> Signup and view all the answers

Which ingredient in the Metronidazole Oral Suspension contributes to sweetness?

<p>Sucrose (C)</p> Signup and view all the answers

Which of the following tests would be used to assess the physical stability of a suspension?

<p>Sedimentation parameters (A)</p> Signup and view all the answers

What happens if excessive electrolyte is added to a system containing bismuth subnitrate suspension?

<p>Charge reversal may occur (C)</p> Signup and view all the answers

Which of the following is a potential consequence of using high concentrations of polymeric flocculating agents?

<p>Complete coating of particles surface (B)</p> Signup and view all the answers

What is the primary role of suspending agents in a suspension?

<p>To retard sedimentation of flocs (B)</p> Signup and view all the answers

Why is tragacanth considered a better thickening agent than acacia gum?

<p>It can be used for both internal and external products (D)</p> Signup and view all the answers

Which polysaccharide is cited as a commonly used suspending agent?

<p>Sodium carboxymethyl cellulose (D)</p> Signup and view all the answers

What is the effect of avoiding excessive blending during the manufacture of flocculating agents?

<p>Promotes cross-linking between particles (D)</p> Signup and view all the answers

What characteristic of hydrated silicates affects their use in formulations?

<p>They are naturally occurring materials (B)</p> Signup and view all the answers

What can result from the swelling of bentonite in a formulation?

<p>Improved suspending properties (D)</p> Signup and view all the answers

What effect does average particle size have on the viscosity of a suspension?

<p>It can increase or decrease viscosity depending on the distribution. (D)</p> Signup and view all the answers

Which measurement technique is suitable for ensuring that individual particles are assessed in a suspension?

<p>Microscopic examination (D)</p> Signup and view all the answers

What type of behavior do flocculated systems exhibit under shear stress?

<p>Pseudoplastic or plastic behavior (A)</p> Signup and view all the answers

What happens to the viscosity of a flocculated suspension when shear stress is applied slowly?

<p>The viscosity decreases and the structure breaks down. (C)</p> Signup and view all the answers

What is the likely impact of temperature cycling on a suspension?

<p>It allows for the assessment of physical stability. (B)</p> Signup and view all the answers

What behavior do deflocculated systems demonstrate?

<p>Newtonian behavior due to absence of structures. (C)</p> Signup and view all the answers

How does the shape of the particles influence the viscosity of suspensions?

<p>Different shapes can lead to varying degrees of viscosity. (B)</p> Signup and view all the answers

What is thixotropy in the context of suspensions?

<p>Time-dependent reversibility of viscosity loss due to shear. (B)</p> Signup and view all the answers

Flashcards

Wetting agent

A wetting agent that helps solubilize ingredients by encapsulating them within micelles.

Polymer

A large molecule that can interact with other ingredients to help stabilize the suspension.

Suspended solids

These can bind to preservatives, making them less effective.

Sedimentation volume (F)

The amount of space occupied by the settled particles compared to the original volume of the suspension.

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Degree of flocculation (β)

A measure of how well particles are clumped together.

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Rheological assessment

A measure of how easily a suspension flows.

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Temperature cycling

Exposing the suspension to different temperatures to assess its stability.

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Particle size assessment

Measuring the size of particles in the suspension to understand their stability and effectiveness.

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Depot suspension

A suspension formulated for injection that releases the drug slowly, extending its effects over a longer period.

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Controlled-release suspension

A suspension formulated for injection that is designed to release the drug at a controlled rate, allowing for a consistent therapeutic effect over time.

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Vehicle selection for injectable suspensions

The use of different vehicles (liquids) to suspend the drug in an injectable suspension to modify its release rate and duration of action.

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Long-acting suspension

A specific form of an injectable suspension designed to release the drug at a controlled rate, offering extended therapeutic benefits.

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Selection of particle size for suspensions

The process of determining the ideal size of drug particles for a suspension to ensure its efficacy, stability, and safety.

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Control of particle size distribution

Maintaining consistent particle size in a suspension to prevent clogging of needles or other delivery systems.

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Polymorphism in drug formulations

The tendency of a drug to exist in multiple forms with varying solubility, potentially affecting its stability and release characteristics.

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Stable Polymorphic Form

The use of a specific form of a drug that is chemically stable and demonstrates predictable solubility, leading to optimal suspension performance.

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Deflocculated suspension

A state where particles in a suspension are dispersed and repel each other, leading to a stable system.

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Flocculated suspension

A state where particles in a suspension clump together, forming larger aggregates, leading to a less stable system.

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Charge reversal in suspensions

The addition of electrolytes to a suspension can lead to charge reversal, shifting the system from flocculated to deflocculated, or vice versa.

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Flocculating agents

Substances that promote particle aggregation, leading to flocculation in a suspension. They can be inorganic salts like phosphates or organic polymers.

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Polymeric flocculating agents

A type of flocculating agent consisting of large, chain-like molecules that form a network within the suspension, holding particles together.

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Viscosity modifiers (suspending agents)

Substances used to increase the viscosity of a suspension, slowing down sedimentation of the dispersed particles. They help to maintain a stable suspension by preventing particles from settling.

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Polysaccharides as suspending agents

Natural or synthetic polymers that act as viscosity modifiers, increasing the viscosity of the suspension and preventing sedimentation.

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Bentonite

A type of hydrated silicate that forms a gel-like structure when mixed with water, contributing to viscosity and suspension stability.

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Hydrated Silicates

Clay-like substances that absorb water and swell, forming a gel. Used externally for various applications.

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Veegum

Another type of hydrated silicate. Can be used internally or externally. Often used in medications.

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Laponites

Synthetic clay created in a lab. Has consistent quality and lower risk of contamination. Used both internally and externally.

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Carbopol

A synthetic polymer that helps thicken liquids, creating gels. Used primarily for external application, though some grades are safe for internal use.

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Buffers

A substance that, when dissolved in water, resists changes in pH. Helps keep products stable and compatible with our bodies.

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Density Modifiers

Substances used to adjust the density of liquids. Helps prevent settling in suspension.

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Preservatives

Substances that prevent the growth of microorganisms in medications or personal care products.

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Suspending agent

A substance added to suspensions to increase viscosity, slowing down sedimentation rate and keeping particles suspended.

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Sedimentation of suspensions

This happens when a suspension settles too quickly and separates, making it difficult to re-suspend and leaving a layer of solid particles.

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Optimum physical stability of a suspension

A suspension formulated with a combination of a suspending agent, wetting agent, and flocculating agent, creating a balance between viscosity and sedimentation rate.

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Formulation of a suspension

The process of preparing a physically stable suspension by choosing and combining the right types and amounts of suspending agent, wetting agent, and flocculating agent.

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Particle Size and Viscosity

The smaller the particle size, the higher the viscosity, as more particles interact with the suspending medium.

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Zeta Potential and Viscosity

Zeta potential is the electrical charge on a particle's surface. A higher zeta potential means particles repel each other, resulting in lower viscosity.

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Particle Shape and Viscosity

Particles with more complex shapes have greater surface area, leading to more interaction with the suspending medium and higher viscosity.

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Viscosity of Flocculated vs. Deflocculated

The viscosity of a flocculated suspension is higher than a deflocculated suspension due to the presence of floccules (clumps) and the interaction of these clumps with the suspending medium.

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Thixotropy

A suspension shows thixotropy when it behaves like a solid at rest but flows easily when shaken, due to broken-down floccules.

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Yield Value

The point at which a plastic system starts to flow under shear stress.

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Study Notes

Pharmaceutical Suspensions

  • Pharmaceutical suspensions are liquid preparations where solid particles are dispersed in a liquid phase.
  • Suspensions are used when a drug is poorly soluble or difficult to swallow as a solid dosage form.
  • Suspensions need to be prepared to remain homogeneous after shaking and while removing the required dose.
  • The sediment produced on storage should be easily resuspended using moderate agitation.
  • The viscosity needs to be suitable, not too high to make the suspension difficult to remove from the container, or too low so it doesn't remain homogenous.
  • Suspended particles' size should be uniform.
  • Suspensions must resist microbial contamination.
  • Different types of suspensions exist;
    • Aqueous suspensions (dispersion medium is water)
    • Oily suspensions (dispersion medium is oil)
    • Ready-to-use suspensions (for stable drugs)
    • Reconstituted powder suspensions (for non-stable drugs)
    • Flocculated suspensions
    • Deflocculated suspensions
    • Oral, Parenteral, Topical, or Ocular eye drops (based on intended use)

Liquid Dosage Forms

  • Solutions are homogeneous mixtures made by dissolving one or more solutes in a solvent.
  • Emulsions are dispersion systems that contain two immiscible liquids.
  • Suspensions are dispersions containing solid particles in a liquid.

Coarse Suspensions

  • Coarse suspensions are systems where the solid particles are larger than colloidal size (1µm).
  • The dispersion medium in the system could be aqueous or oily liquid.
  • Solid particles are typically insoluble.

Intended Learning Outcomes

  • Understand the physical and chemical principles affecting suspensions' formulation and performance.
  • Independently formulate pharmaceutical suspensions.
  • Evaluate information from various sources specific to pharmaceutical suspensions.

Reasons for Preparing Suspensions

  • Difficulty swallowing solid dosage forms (if drug is insoluble).
  • Drugs with poor solubility.
  • Bad taste drugs (suspensions can masks tastes that are undesirable).
  • Drugs that degrade in the presence of water (suspensions can provide a more stable dosage form).

Preformulation of Suspensions

  • Selecting suitable particle size.
  • Controlling particle size and distribution to avoid changes that alter the drug.
  • Ensuring small particle sizes (less than 5μm), to prevent gritty texture/irritation from injections or instillation into eyes and to prevent clogging of needles.
  • Using appropriate particle size ranges to control drug release rate and bioavailability.
  • Selecting stable polymorphic forms to avoid changes in solubility or precipitation.
  • Preventing crystal growth during manufacture and storage.
  • Controlling crystal growth by careful manufacturing processes and storage conditions. This ensures that the particle size of the suspended drug is maintained.

Formulation of Suspensions

  • Deflocculated systems use agents to reduce particle-particle attraction, leading to evenly distributed particles and minimal settling.
  • Flocculated systems use agents that create small aggregates of particles, which lead to settling but can be easily redissolved/resuspended, improving ease of dispensing.
  • Selection of appropriate wetting agents, which assists drug dispersal.
  • Adjusting solvents to improve wetting and dispersal.
  • Selecting hydrophilic colloids to coat solid particles to improve wetting.
  • Using appropriate flocculation and suspending agents for ideal stability and redispersion.
  • Using substances like buffers, density modifiers, flavors, colors, perfumes, humectants, and preservatives, adding desired properties.

Stability Testing of Suspensions

  • The testing ensures particles remain uniformly distributed.
  • Sedimentation parameters: assessing the volume of the sediment, its rate, and the degree of flocculation.
  • Rheological assessments (using a Brookfield viscometer) are used to evaluate viscosity at various stages of storage, giving the change in the structure/stability of the products with time.
  • Temperature cycling tests help maintain stability under varying temperatures and conditions, by causing variations that can occur in the suspension during use.
  • Particle size assessment to analyze potential crystal growth/particle size changes.

Preparation of Suspensions on Large Scale

  • Suitable equipment should be used for particle size reduction.
  • Concentrated dispersions with suspending agents should be prepared on large scale, to ensure that agglomerates are fully broken up in a homogenizer.
  • Precautions should be taken to prevent the structure of suspending agents from being destroyed.
  • Wetting the drug to be suspended using the wetting agent.
  • Dissolving other ingredients in a portion of the vehicle.
  • Homogenization to make a homogeneous final suspension.

Rheology of Suspensions

  • Ideal suspensions display high viscosity at low shear rates during storage and low viscosity at higher shear rates during shaking.
  • Flocculated systems exhibit time-dependent properties like thixotropy (reversible viscosity change).
  • Deflocculated suspensions display Newtonian behavior (constant viscosity regardless of shear rate), though highly concentrated systems might show dilatancy (increased viscosity at higher stress levels).

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Pharmaceutics I Lecture 7-8 PDF

Description

This quiz explores the fundamentals of pharmaceutical suspensions, including their preparation, types, and characteristics. Learn about the significance of viscosity, particle size, and microbial resistance in creating effective suspensions for drug administration.

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