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168 Cards in this Set
- Front
- Back
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Patients assume that pharmaceuticals are safe and effective as required by law, and they judge the products you dispense based on what?
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- Appearance
- Color - Flavor - Odor - Package Design |
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What should match in your dosage form?
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Flavor and color!
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Whats more sensitive, odor or flavor?
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Odor
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What does umami mean?
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Taste enhancer
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What are the four primary tastes?
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Sweet, bitter, sour, salty
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How many people are in a taste panel? What are the characteristics of these people?
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12 people with no impairment of smell and taste
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In a taste panel, list the steps used to taste. How are the formulations evaluated?
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1) Rinse mouth with teaspoonful of water
2) Rinse mouth with formulation to be tested 3) Rinse mouth with water again 4) evaluate characteristics on a scale of 0 to 8 (with 0 being a lack of the characteristics for bitterness, sweetness, sourness, saltiness). |
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Who can pharmaceutical companies submit their drug to for tasting? Why?
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American tasting institute.
As an extra, for better marketing. |
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What kinds of characteristics does the American Tasting Institute look for?
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1) Appearance
2) Aroma 3) Flavor 4) Freshness 5) Taste 6) Texture |
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What are the purposes of flavoring agents?
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Mask the unpleasant flavor of a drug
Import a well-balanced flavor to the product |
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What are the purposes of coloring agents?
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Improve appearance
Aid in identification Facilitate associated taste response |
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What characteristics must a flavor and color agent have to be used with a drug?
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Must not interfere with therapeutic effect of the drug!
i.e. pH, alcohol concentration, etc |
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Flavoring and coloring agents must consider what?
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Age of the patient
Patient preferences |
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What flavors do young patients prefer?
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Sour or sweet
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What flavors do older patients prefer?
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Salty
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What are some of the patient preferences?
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1) Remove the "yuck"
2) Repeated administration 3) Let patient select flavor 4) Danger of making it taste TOO good. |
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What are the five flavoring techniques?
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1) Blending
2) Overshadowing 3) Physical 4) Chemical 5) Physiological |
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Describe the blending flavoring technique.
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Blend of multiple flavors. More effective than a single flavor.
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Describe the overshadowing flavoring technique.
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Addition of a flavor with a stronger intensity then the drug.
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Examples of some overshadowing flavors?
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Methyl salicylate (winter green)
Glycyrrhiza (licorice) |
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Describe the physical flavoring technique.
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Formation of insoluble compounds
1) Emulsification of oils 2) Effervescence (fizzing) 3) High viscosity fluid 4) Coating |
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Describe the chemical flavoring technique.
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Adsorption, complexation
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Describe the physiological flavoring technique.
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Anesthetic effects (menthol, mint)
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List some of the sweetening agents?
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Sucrose
Saccharin Aspartame Sucralose Dextrose Sorbitol Xylitol |
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Describe sucrose
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Safe, natural, can be heated.
Has calories. Not good for diabetics |
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Describe saccharin
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Sweet 'n low (pink pack.
No calories Can be used in diabetics Has aftertaste Cannot be heated Bad history |
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Describe aspartame
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Nutrasweet, equal (blue packet)
Can be used in diabetics No calories Cannot be heated Health concerns |
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Describe sucralose
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Splenda (yellow packet)
No Calories Can be used by diabetics Can be heated |
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Describe dextrose
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Not very sweet
Cannot be used by diabetics |
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Describe sorbitol
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Sweet
Can be used by diabetics Has a laxitive effect |
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Describe xylitol
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Commercial sweetener
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What does FD&C, D&C, Ext. D&C mean?
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FD&C = dyes that can be used in food, drug, and cosmetics
D&C = dyes that can be used in drugs and cosmetics Ext. D&C = dyes that can be used in external drugs and cosmetics (topical use) |
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Which one requires more dye, liquid or solid?
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Solid.
Liquids require less dye. |
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What do you need to know about dyes?
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Dyes have a common name, color, and FD&C
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Describe the FlavorX System
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- Post-manufacturing flavoring system for pharmacies
- Allows patient to select the flavor for their liquid medication using the "favorable flavors" guide - Flavor medications according to the "smart formulary" |
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Solid -> Liquid
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Melt
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Liquid -> Gas
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vaporize
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Gas -> Liquid
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Condense
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Liquid -> Solid
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Freezing
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Solid -> Gas
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Sublimation
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Describe the attributes of a solid.
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- Most are solid
- Most do not mix to form ONE solid - Eutecnic mixtures are the exception - Has an ordered structure - Molecules are tightly bound |
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Describe the attributes of a liquid
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- May or may not mix (Miscible and immiscible)
- Less ordered structure then a solid - Molecules less tightly bound then a solid |
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Describe the attributes of a gas
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- Mixes spontaneously
- Disordered structure - Molecules are loosely bound |
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What are the variables that affect the phase in which a chemical or chemicals exist?
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Temperature
Pressure Concentration Etc. |
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What is the MOST IMPORTANT variable that affects the phase in which a chemical or chemicals exist?
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temperature
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Gibb's Phase Rule is:
F = C - P + X What do each of these symbols mean? |
F = degrees of freedom
C = number of components P = number of phases X = 1, 2, or 3 depending on the phase diagram considered. |
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What does degrees of freedom mean in the gibb's phase rule?
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Number of independent variables that must be specified to define the complete system.
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What does components mean in the gibb's phase rule?
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Minimum number of chemical components that need to be specified to define the phases present
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What does phases mean in the gibb's phase rule?
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Number of distinct states of matter (solid, liquid, gas) present.
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How do you determine X in gibb's phase rule?
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if c = 1, x = 2
if c = 2, x = 1 C = components, minimum number of chemical components that need to be specified to define the phases present. |
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Use gibb's phase rule to compute the following..
Camphor + Menthol Gibb's Phase Rule: F = C - P + X |
Camphor and menthol
F = C - P + X Components (C) = 2 Phases (P) = 1 (liquid) X = 1 (because c = 2) F = 2 - 1 + 1 F = 0 |
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Know the diagram on page 36 and 37
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Know the diagram on page 36 and 37
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What are the uses of eutectics?
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Decreases grittiness
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What is a eutectic?
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Two solids forming liquid dosage form
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What are some disadvantages of a eutecnic, what can you do about it?
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2 solids forming a liquid will make solid powder sticky/clumpy.
Add diluent to reduce contact of eutecnic substance |
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What does comminution mean?
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The process of reducing the particle size of a solid to a finer state of subdivision.
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What are the four main objectives of comminution, describe them?
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1) To increase the dissolution rate of drugs
2) To aid in the formulation process 3) To enhance absorption 4) To facilitate crude drug extraction |
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What are the manual comminution techniques?
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Trituration
Spatulation Pulverization by intervention Levigation |
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What is trituration?
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Manual comminution method
Process of grinding a drug using a mortar and pestle to reduce particle size. To rub to pieces. |
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What is spatulation?
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Manual comminution method
The process of grinding a small amount of powder using a pill tile and spatula |
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What is pulverization by intervention?
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Manual comminution method
Use of a liquid in which the solid is SOLUBLE to aid in particle size reduction |
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What is levigation?
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Manual comminution method
Using a liquid in which the solid is INSOLUBLE to aid in particle size reduction. Not evaporating off liquid in this one (in contrast to pulverization by intervention) |
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What are the mechanical methods of comminution?
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Mills
Lyophilization Spray drying |
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Describe mills
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Mechanical comminution method
Any type of mechanical devices that breaks down particles. |
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Describe lyophilization
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Mechanical comminution method
Freeze-drying Lower temperature, increase airflow, leaves behind particles and sucks out moisture. Vacuum used to create airflow |
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Describe spray drying
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Heated glass column with airflow.
Drugs sprayed into column Solvent is dissolved Beaker collects small particles |
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Which mechanical comminution methods are based off pulverization by intervention?
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Lyophilization (freeze-drying)
Spray drying |
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Which mechanical comminution methods are based off of trituration?
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Mills.
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Particle sizes should be ___________. Reduction in particle sizes greatly increases _______ _______ ______.
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Particle sizes should be UNIFORM. Reduction in particle sizes greatly increases SPECIFIC SURFACE AREA.
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Look at cube problem page 39.
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Look at cube problem page 39.
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Example of a gas in liquid?
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Tap water with air trapped in it
Carbonated beverages |
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Examples of liquid in liquid?
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Alcohol and water mixed.
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Examples of solid in liquid?
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Solid in liquid....pretty much any clear mixture
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What are the chracteristics of solutions?
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- They are all transparent (suspension = cloudy)
- Solids are in their smallest particle size - Form spontaneously |
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What does solute mean?
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substance being dissolved
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What does solvent mean?
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Substance in which the solute is dissolved
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What must overcome what to form a solution?
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Solute's intermolecular forces of attraction must be overcome by attractive forces between solute and solvent molecules.
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What is the general rule for whether or not something will dissolve in another?
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Like dissolves like.
Polar dissolves polar Nonpolar dissolves nonpolar |
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What is a dielectric constant?
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Assigned to every solvent.
The higher it is, the more polar it is. |
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Describe the characteristics of a polar solvent.
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1) High dielectric constant
2) Breaks bonds 3) Has hydrogen bonds and/or dipole forces |
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What does it mean for a polar solvent to break bonds?
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example: Water breaks up NaCl and produces Na+ and Cl- (ionization).
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Describe the characteristics of nonpolar solvents.
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1) Low dielectric constant
2) Dipole interactions/van der waals forces |
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What is the definition of a dissolution rate?
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Time required for the solute to completely dissolve in the solvent
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What are the three factors affecting dissolution rate?
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1) Surface area
2) Length of stagnant layer 3) Solubility |
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How do changes in surface area affect dissolution rate?
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A decrease in particle size increases surface area. Increases dissolution rate.
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How do changes in stagnant layer affect dissolution rate?
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Agitating mixtures decreases the stagnant layer and increases dissolution rate.
Increased viscosity increases the stagnant layer and decreases dissolution rate. |
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In the rate of dissolution formula:
Rate of solution = (DA/l) x S What do each of the symbols mean? |
D = diffusion coefficient (cm2/sec) GIVEN THIS EXPERIMENTALLY
A = surface area of the solid (cm2) GIVEN OR CALCULATED l = length of stagnant layer (cm) GIVEN THIS S = solubility (g/mL) |
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Know how to calculate solubility page 41!
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Know how to calculate solubility page 41!
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What is the definition of solubility?
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The maximum concentration of solute in a solution for a specified set of conditions.
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Solubility depends on what?
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Chemical characteristics of the solvent and solute.
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What are the factors that affect solubility?
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1) Temperature
2) pH 3) Presence of other compounds 4) Cosolvents |
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What is a cosolvent?
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An additional solvent that is added to a primary solvent to increase solubility.
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Know how to use temperature and pH formula on page 42!
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Know how to use temperature and pH formula on page 42!.
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In general, the presence of other compounds does to solubility? Why?
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In general other compounds in a solution will decrease solubility of the drug because of the competition for solvent binding.
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Sometimes, presence of other compounds can do what to solubility? How can these happen?
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Sometimes, compounds added to the solution increase the solubility.
Solubilization Complexation |
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What does solubilization mean?
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Physical phenomenon where the compound surrounds the drug.
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What does complexation mean?
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Chemical phenomenon, chemical reaction between solute and complexing agent.
i.e. KI + I2 = K + I3 (helps K dissolve) |
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What are the ways you can express the strength of a solution, give examples.
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- Percent strength (% w/v, % w/w, % v/v)
- Ratio strength (w/v, w/w, w/v) - Molarity (moles/L) - Molality (moles/kg) kg of solvent - Normality (Eq/L) - Mole fraction (moles of solute per moles of solute + solvent) |
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What is molality?
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moles/kg of solvent
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What is normality?
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Eq/L
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What is mole fraction?
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Moles of solute / moles of solute + solvent
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Know how to calculate strength of a solution on page 43!
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Know how to calculate strength of a solution on page 43!
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Know how to calculate ionic strength on page 44!
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Know how to calculate ionic strength on page 44!
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What are the colligative properties?
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1) Osmotic pressure
2) Vapor pressure 3) Boiling point elevation 4) Freezing point depression |
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What do colligative properties depend on?
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The number of solute particles in solution.
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What is osmosis?
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Solvent passes from the compartment that has pure solvent (or less concentration solution) into a more concentrated solution, through a semipermeable membrane.
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What is osmotic pressure?
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The pressure needed to stop the passage of the solvent through the semipermeable membrane.
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Osmotic pressure is:
Pi = RTc What do each one of these mean? |
Pi = 3.14...
R = gas constant (0.082 Lxatm/kxmol) T = temperature KELVIN c = molar concentration DO NOT FORGET i, its invisible!!! dissociation factor (i, van't hoff term!) |
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Know how to calculate osmotic pressure on page 44!!
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Know how to calculate osmotic pressure on page 44!!
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Know how to calculate vapor pressure lowing on page 44!
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Know how to calculate vapor pressure lowing on page 44!
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Know how to calculate boiling point elevation and freezing point depression on page 45!
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Know how to calculate boiling point elevation and freezing point depression on page 45!
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Solvents for liquid preparations must be what?
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Must be safe for route of administration
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What are some examples of common solvents used for liquid preparations?
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Alcohol USP (95% ethanol)
Diluted Alcohol NF diluted 1:1 with water (47.5% ethanol Rubbing alcohol (70% ethanol or 70% isopropanol) Glycerin USP Propylene Glycol USP Purified water USP |
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What are the ways to purify water?
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Distillation
ion exchange Reverse osmosis |
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Describe distillation.
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Heat up water and collect as steam, leaves behind impurities.
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Describe ion exchange.
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Put water through a charged column, pulls ions out.
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Describe reverse osmosis.
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High concentration --> Low concentration using pressure. Leaves behind impurities.
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Is purified H2O sterile?
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No, you have to do one more step to sterilize it to make...
Sterilized H2O USP |
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What are the simple dissolution methods?
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Heating
Decrease particle size Agitate |
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What must you consider when heating something for simple dissolution?
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Stability of drug
Evaporation of solvent Must have a positive heat of solution |
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What is a saturated solution?
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No more solute can be dissolved in the solvent.
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What routes of administration can solutions be used for? Give examples
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- Oral (syrups, elixirs, tinctures)
- Topical (sprays, tinctures, liniments, collodions, rectal, vaginal, nasal, otic, inhalation, topical oral (mouthwash) - Parenteral (must be sterile solution!) |
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What is a syrup?
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Concentrated, aqueous preparation of sugar or sugar-substitute with or without added flavoring agent and medicinal substances
Can be medicated or non-medicated |
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What does a syrup contain?
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- Sucrose or sugar substitute
- Antimicrobial preservatives - Flavorant - Colorant - Adjunct solvents |
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What syrup does not need antimicrobial preservatives? Why?
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If your syrup is 60-85% sucrose, it is self preserving due to low water content.
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What are the methods of preparation for syrup?
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1) solution with aid of heat
2) solution by agitation without the aid of heat 3) addition of sucrose to a prepared liquid 4) percolation |
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What are the advantages of syrup?
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Viscous
Taste masking |
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What are the disadvantages of syrup?
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High sucrose content
Sticky |
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What is an elixir?
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Clear, sweetened, HYDROALCOHOLIC solutions intended for oral use, and are usually flavored to enhance their palatability.
Can be medicated or non medicated. |
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What does an elixir contain?
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- ALCOHOL
- Sweetener - Colorant - Flavoring - Adjunct solvents |
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What are the methods for preparing elixirs?
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1) Solution with agitation
2) Admixture of two or more liquid ingredients |
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What does it mean by admixture of two or more liquid ingredients to prepare an elixir?
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Dissolving alcohol soluble components in alcohol
Dissolving water soluble components in water Water solution is added to alcohol solution Alcohol solution may precipitate out! |
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What are the advantages of elixirs?
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Contain both H2O soluble and OH soluble components
Stable Ease of preparation |
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What are the disadvantages of elixirs?
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OH Content
Less effective in taste masking |
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What is a tincture?
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Alcoholic or hydroalcoholic solution prepared from vegetable materials or from chemical substances
i.e. iodine tincture |
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What is an aromatic water?
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Clear, aqueous solutions generally saturated with volatile oils or other aromatic or volatile substances
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What are spirits?
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Alcoholic or hydroalcoholic solutions of volatile substances
Alcohol > 60% Used for perfuming and flavoring agents or for therapeutic values |
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What are diluted acids?
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Prepared by diluting concentrated acid with purified water.
Mostly used topically Strength is % w/v or % w/w |
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What is a liniment?
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Alcoholic or oleaginous solution or emulsion intended for external application to the skin generally with rubbing.
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What are some consultations for liniments?
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Do not apply to broken or bruised skin.
Store in tight container because the alcohol will evaporate off. |
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What is a collodion?
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Liquid preparation composed of pyroxylin dissolved in a 3:1 mixture of ether:alcohol
Evapration of the solven leaves an occlusive film of pyroxylin |
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What are some things you should know about collodions?
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Pyroxylin precipitates in H2O
Do not weigh in glassware! Highly flammable! Store in tight containers, away from heat and light. |
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What does extraction mean?
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Withdrawal of the desired constituents from crude drugs by using selected solvents in which the desired constituents are soluble.
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What is a crude drug?
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Vegetable or animal drug
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What does extractives mean?
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Constituents removed from extraction (hopefully wanted drug)
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What is the Marc?
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Leftovers, after all desired constituents have been removed.
You can use this for a second extraction. |
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What does menstruum mean? What characteristics should this have?
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Solvent used for extraction
Should dissolve the maximum amount of desire active constituents and the minimum amount of undesired constituents. |
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What are the methods of extraction?
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Maceration - Process M
Percolation - Process P Combination of maceration and percolation |
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What is maceration?
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Drug is placed in a tight container and allowed to soak in the menstruum from 2-14 days with occasional agitation.
Marc is removed by filtration Performed at room temperature |
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What is percolation?
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Solvent (menstruum) is passed through a column of the drug.
Percolator = the column Percolate = collected extractive (active ingredient) |
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Most extractions are performed via what method?
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Percolation
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What are fluid extracts?
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Liquid preparations of vegetable drugs prepared by percolation
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What are extracts?
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Concentrated preparation of vegetable or animal drugs obtained by removal of the active constituents of the respective drugs with suitable menstrua, evaporation of the solvent under pressure, and adjustment of residual mass to prescribed standards.
This leaves behind a powder/paste in which you can add a diluent to form a solid dosage form. FIRST solid dosage form made this way. |
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What is an example of a strong acid?
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HCl
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What is an example of a strong base?
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NaOH
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A strong acid does what?
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completely ionizes in water
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A weak acid does what?
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does NOT completely ionize in water
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A high Ka means what? A low Ka?
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High Ka = stronger acid
Low Ka = weak acid |
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A base is what?
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A proton acceptor
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A high Kb means what? A low Kb?
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High Kb = higher base strength
Low Kb = weak base |
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What is a buffer?
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A system, usually an aqueous solution, that resists changes in pH upon addition of acid or base.
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What is a buffer composed of?
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Composed of a weak acid and conjugate base or weak base and conjugate acid.
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How do you prepare a buffer?
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Add weak acid and conjugate base together or weak base and conjugate acid together.
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How do you form a conjugate base from a weak acid?
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To form a conjugate base from a weak acid, add a strong base to the weak acid.
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How do you form a conjugate acid from weak base?
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To form a conjugate acid from weak by, add a strong acid to weak base.
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Know calculations for Kb and Ka and pH on page 53-55!
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Know calculations for Kb, Ka, pH and buffer capacity on page 53-55!
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What is the definition of buffer capacity?
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The amount of acid or base to add to 1L of a buffer to change pH by one unit.
The ability of a buffer solution to resist changes in pH upon addition of acid or base. |
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Why do we care about buffer capacity?
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- Drug stability, buffer formulation where rate constant (k) is the lowest
- Drug solubility, pH can effect solubility. - Drug activity, some drugs aren't active at certain pH - Drug absorption - Patient comfort, can't use certain pH in eyes. |
