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Pharmaceutics > T1 - Week 4 > Flashcards

T1 - Week 4 Flashcards

1
Q

Which is the most convenient route of drug delivery?

A

Oral

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2
Q

What is the disadvantage of oral dosage forms?

A

Poor bioavailability due to poor solubility and permeability

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3
Q

Define solubility

A

The amount of a solid solute that can dissolve in a given solvent at equilibrium

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4
Q

Define equilibrium solubility

A

The concentration of the solute in its saturated solution, where the saturated solution exists in a state of equilibrium with pure solid solute

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5
Q

Define kinetic solubility

A

The amount of the solute in solution prior to reaching equilibrium solubility

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6
Q

What are the steps of the solubility process?

A
  1. Solute-solute intermolecular bonds breakup
  2. Solvent-solvent intermolecular bonds breakup
    • Formation of cavity for solute
    • Transfer of solute into cavity
  3. Solute solvent intermolecular bond formation
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7
Q

What happens if solvent-solvent forces are greater than solvent-solute?

A

Solvent molecules will not want to dissociate the solute will be excluded

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8
Q

What happens if solute-solute forces are greater than solvent-solute?

A

The solvent will not be able to break and bind to solute

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9
Q

What happens if solvent-solute forces are greater than solvent-solvent or solute-solute?

A

Solute will form a solution

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10
Q

What are the USP classifications of solubility?

A
  1. Very soluble: less than 1mL/g
  2. Freely soluble: 1-10
  3. Soluble: 10-30
  4. Sparingly: 30-100
  5. Slightly sparingly: 100-1,000
  6. Very slightly soluble: 1,000-10,000
  7. Practically insoluble/insoluble: more than 10,000
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11
Q

Define miscibility

A

A homogenous solution of a liquid state in another liquid solvent at any concentration

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12
Q

What is dielectric property?

A

The ability of a molecule to store/carry a charge

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13
Q

What type of dielectric constant solvent can dissolve a highly polar or ionic compound?

A

High or a polar solvent

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14
Q

What type of dielectric constant solvent can dissolve a nonpolar compound?

A

Low

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15
Q

What is hydrogen bonding?

A

H bonds with electronegative elements that create partial polarity

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16
Q

What atoms would interact with hydrogen for bonding?

A

O, N, and S

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17
Q

Which is more soluble amorphous or crystalline nature of drugs?

A

Amorphous

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18
Q

Which is more soluble hydrous or anhydrous in water?

A

Anhydrous

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19
Q

Would high solubility have a high or low melting point?

A

Low due to molecular instability

20
Q

Why would branched molecules have increased solubility?

A

Branching will reduce size of the molecule making it easier to solvate the molecules

21
Q

What particle size would be the most soluble?

A

Small, to increase surface area to volume ratio

22
Q

What occurs when solute is being dissolved?

A

Intramolecular forces of solute are being overcome

23
Q

What happens to solubility when temperature increases?

A

Increases

24
Q

What happens if the solubilization process is endothermic?

A

Increasing temperature improves solubility

25
Q

What happens if the solubilization process is exothermic?

A

Increasing the temperature will decrease in solubility

26
Q

How can you improve solubility of ionizable solutes?

A

Adjusting of the solution’s pH

27
Q

How can you improve solubility of non-ionizable solutes?

A

Lowering the dielectric constant of the solvent with a co-solvent

28
Q

Describe the solubility of weak acids?

A

Solubility increases if pH is above pKa

29
Q

Describe the solubility of weak bases?

A

Solubility decreases as pH is above pKa

30
Q

What are the general rules of water solubility?

A
  1. Water solubility of a solute can be enhanced by forming H-bonding
  2. Water solubility decreases with an increase number of carbons in a solute
  3. High melting point solids largely have low water solubility
31
Q

What is comminution?

A

Using mechanical stress to disaggregate solid particles, however, may cause degradation of drug product

32
Q

What is micronization and nanonization?

A

Reducing particle size to micron and nano level, increasing surface area of lipophilic drug to improve solubility

33
Q

How do you enhance solubility of the drug by altering solid state?

A

Crystalline to amorphous

Selecting the highest soluble polymorphic form

34
Q

What is a pharmaceutical solid dispersion?

A

A mixture of a solid drug with diluents (carriers)

A hydrophilic carrier and a hydrophobic drug

35
Q

What is the inclusion complexes method?

A

Formed by the insertion of a nonpolar molecule (guest) into the cavity of another molecule or group (host)

36
Q

What is a common host molecule?

A

Cyclodextrin: Hydrophobic cavity and hydrophilic outer surface

37
Q

What are cosolvents?

A

Water-miscible organic solvent (lipophilic) that enhance aqueous solubility of poorly water soluble drugs

38
Q

What are examples of cosolvents?

A
  1. Ethanol
  2. Glycerol
  3. Propylene glycol (400)
39
Q

What are liposomes?

A

Vesicles obtained either from natural phospholipids or synthetically that carry poorly water soluble drugs while the hydrophilic compartments can load hydrophilic drugs

40
Q

What is a prodrug?

A

Covalently bound drug where the inactive moiety will be cleaved upon administration to regenerate the parent drug in the body enhancing solubility of parent drug

41
Q

What forms a salt?

A

Poorly water soluble weak acid or base + counterion

42
Q

What is dissolution?

A

The process which a solid substance enters the solvent phase to yield a solution

43
Q

What is the process of dissolution?

A
  1. Removal of the solute from the solid phase
  2. Accommodation of the solute in the liquid phase
  3. Diffusion of the solute away from the solid/liquid interface into the bulk phase
44
Q

What factors are proportional to drug dissolution rate?

A
  1. Drug solubility
  2. Surface area of drug particles
  3. The concentration gradient of drug between the diffusion layer and bulk solution
45
Q

What factors are inversely proportional to drug dissolution rate?

A
  1. The thickness of the diffusion layer surrounding the drug
  2. The volume of solution

Pharmaceutics (27 decks)

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