Liquid Dosage Forms 10

Question 1

Liquid Dosage Forms

Answer 1

• Solutions
  
  • ​Clear / in solution
  • *solubility
• Colloids
• Suspensions
  
  • ​not soluble
  • matrix, suspends unsoluble drug
• Emulsions
• Other
  
  • ​Parenteral products

Question 2

Pharmaceutical principles

Answer 2

• Solvents and solubility
  
  • ​Non-Polar Solvents = MINERAL OIL
  • Semi-Polar Solvents = Ethanol / GLycols
  • Polar solvents = water
• Solvent Categories
  
  • ​based on their dipole moment / polarity of solvent
• Solubility Generalizations
  
  • ability of sulute to form HYDROGEN BONDS with solvent is very important in determining solubility
  • soluble drugs desirble for GI obsorption
• Solubility application to dosage form design /prep
• Dispersion size

Question 3

Solvent Categories

Answer 3

• Polar Solvents = Water
  
  • High Polarity / High Dielectric Constant / High Dipole Moment
• Semipolar Solvents = Ethanol / Glycols
  
  • Intermediate everything
• NON-polar Solvents = Mineral Oil
  
  • ​low everything

Question 4

Solutions Plus What =

Answer 4

• • Surfactant
    
    • = micellular dispersion
• + Surfactant & insoluble drug
  
  • = liposome
• + Surfactant & Oil
  
  • ​= emulsion
• ​+ Insoluble drug
  
  • ​= Suspension

Question 5

Solutions

Answer 5

• Molecular dispersions that may be components of other dispersions
  
  • Colloids / Suspension / Emulsions
• Preformulation Studies - properties of drugs
• Problem Solving –> Know properties of ACTIVE INGREDIENT
• Solution Dosage Forms design & Characteristics
• Solution Product Components
  
  • ​Include Packages / Devices / Supporting Ingredients

Question 6

Solution Product Components

Answer 6

• API (active Drug)
• Supporting Inactive Ingredients
  
  • ​Cosolvent / Inactive ingredients for stabilization
  • Chelant ~EDTA
  • Inactive ingredients for bioavailibility / APplication
  • Inactive ingredients for Compliance
    
    • ​viscosity / flavor / Color / Small
• Packages
• Processes for specific applications
  
  • ​ex. aseptic facility
• ​Administration device

Question 7

Oral Solutions

Answer 7

• Syrups
  
  • ​Sweeteners / flavors / colors / preservatives
• Elixers
  
  • ​+Alcohol
• Mouthwashes / Laxatives
• Oils / Capsules
• Flavoring / Parenteral Solutions
• Irrigation Solutions / Enemas
• Opthalmics / Otics
• Nasal Solutions / SPrays
• Meter Dose Inhalers / Inhalation Solutions

Question 8

Colloids

Answer 8

• Dispersions w/ particle size BELOW VISIBLE LIMITS
  
  • LyoPHILIC colloids
    
    • ​cellulosics / large ORGANICs
  • LyoPHOBIC colloids
    
    • ​inorganics
  • Association Colloids
    
    • ​surfactants! –> form micelles / liposomes
• Solubilized but not dissolved

Question 9

Suspensions

Answer 9

• Stoke’s Law
  
  • ​Determines velocity of SEDEMENTATION
• Brownian Motion
  
  • only affects particles <5 um in size
• Inactive Ingredients
  
  • ​Suspending agents / gelling agnets
  • Viscosity enhancers (Cellulosics / Polymers)
  • FLocculating Agents
  • Anti-Microbial Preservatives
  • Buffer System
  • Wetting Agent (surfactant/anti-foaming agents)
  • Sweeteners/flavor/color/fragrance

Question 10

Suspension Dosage Forms

Answer 10

• Oral Suspensions
  
  • ​Antacids, antidiarrheals, antibiotics
• Granules for reconstitution
• Opthalmic / otic / Nasal suspensions
• Rectal Suspensions
• Topical Suspensions
• Inhalation Suspensions
• Patenteral Suspentions

Question 11

Aerosol Inhalation

Flovent

Answer 11

• Considered a SUSPENSION even WITHOUT SUSPENDING AGENT
  
  • bc powder is MICRONIZED ~1um
  • does not need suspension
  • Due to BROWNIAN MOTION

Question 12

Types of Emulsions

Answer 12

1. O/W
2. W/O
3. Multiple emulsions - w/o/w
4. Microemulsions
   
   1. ​100um max
5. Nanoemulsions
   
   1. ​<.1um
6. ​In Vivo emulsions

Question 13

HLB Chart

Answer 13

• Micellization / Solubilization
  
  • ​18+ HLB
• ​Detergents
  
  • ​13-16
• ​O/W Emulsions
  
  • ​12
• ​Wetting / Spreading Agents
  
  • ​7-9
• ​W/O Emulsions
  
  • ​3-8
• ​Anti-Foaming Agents
  
  • ​<3

Question 14

Emulsion Dosage Forms

Answer 14

• Oral Emulsions
• Opthalmic Emulsions
• Topical
• Parenteral

Question 15

Inactive Ingredients in Emulsions

Answer 15

• Supporting inactive ingredients
  
  • ​Oil to dissolve API
• ​Inactive Ingredients to STABILIZE API
  
  • ​Buffer system
  • Chelant
  • Antioxidant
• ​Emulsifying Agent
• Aqueouss Phase

Question 16

SEDDS

Answer 16

• Self Emulsifying drug delivery system
  
  • ​Semipolar solvents
    
    • ​Ethanol / Propylene glycol / PEG400
  • Surfactants
    
    • Polysorbate 80
  • Oils
    
    • ​corn / safflower oil
• Commercial SEDDS formulations
  
  • ​Norvir
  • Neoral / Sandimmune (Cyclosporine)
  • -AVIR’s

Question 17

Parenteral Products

Answer 17

• Have Additional Requirements to the properties of non-parenteal products
  
  • STERILITY
  • ABSENCE OF PYROGENS
  • minimize particulates
  • stability / ISOTONICITY
  • compatability
  • Safety

Question 18

Adding Surfactant to Solution

Answer 18

1. Solution
   
   1. more surfactant
2. MICELLE
3. LIPOSOME
4. EMULSION