Poorly Water-Soluble Drug Formulation

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12 Questions

What effect does reducing the particle size of griseofulvin have on its solubility and dissolution rate?

Increases solubility and dissolution rate

Why is it important to optimize the particle size of dispersed phases in cosmetic cream formulations?

To achieve the desired sensory attributes

Which type of particles tend to pack more closely and have less air space between them, affecting flowability?

Denser particles

How can electrostatic charge affect the flowability of a material?

Reduce flowability

What is the role of moisture in powder flowability?

Acts as a binder or a lubricant depending on the amount and type of moisture

What happens to cement's flowability when it is hydrated?

Decreases due to chemical bonds

How does particle size affect the solubility and dissolution rate of a drug?

Smaller particles have higher solubility and dissolution rate due to increased surface area.

What technique can be employed to reduce the particle size of a drug?

Micronization or nanosizing

Why does reducing the particle size of griseofulvin enhance its solubility and dissolution rate?

It increases surface area.

What is a drawback of smaller particles compared to larger particles in terms of stability?

Smaller particles have lower stability due to increased aggregation tendency.

How does reducing particle size affect the flowability of a drug?

Smaller particles have better flowability as they can slide past each other more easily.

Which drug is provided as an example in the text that is affected by particle size?

Griseofulvin

Study Notes

Poorly Water-Soluble Drug Formulation

  • Larger particle size is associated with poor dissolution and reduced bioavailability of a drug.
  • Smaller particles have higher solubility and dissolution rates due to increased surface area.
  • Techniques like micronization or nanosizing can be used to reduce particle size and enhance dissolution rates.
  • Example of a drug affected by particle size is griseofulvin, which has low solubility and dissolution rate, but reducing its particle size increases its surface area, enhancing solubility and dissolution rate.
  • Smaller particles have lower stability due to increased susceptibility to aggregation, oxidation, or degradation.
  • Smaller particles may have better flowability due to their ability to slide past each other more easily.

Cosmetic Cream Formulation

  • Particle size of dispersed phases in emulsions affects the sensory attributes of creams and lotions.
  • Larger particles can result in a gritty or unpleasant texture.
  • Optimizing particle size of emulsifying agents and active ingredients ensures a smooth and aesthetically pleasing product.

Particle Flowability

  • Flowability is the ability of a solid material to move or flow smoothly and easily.
  • Particle size, shape, density, surface area, moisture content, electrostatic charge, and interparticle interactions affect flowability.
  • Irregular or angular particles have lower flowability due to interlocking, whereas spherical or smooth particles have higher flowability.
  • Denser particles have lower flowability due to less air space, while less dense particles have higher flowability.
  • Electrostatic charge and interparticle interactions, such as van der Waals forces or chemical bonds, affect the cohesion and flowability of the material.
  • Moisture can act as a binder or lubricant between particles, affecting flowability.

Explore preformulation studies for a poorly water-soluble drug, focusing on assessing particle size and its impact on dissolution rate and bioavailability. Learn how smaller particles enhance solubility due to increased surface area exposed to the solvent.

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