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COMPUTERS IN
PHARMACEUTICAL
FORMULATIONS
Presented By
Sujitha Mary
M Pharm
St Joseph College Of Pharmacy
1
CONTENTS
 Computers in pharmaceutical formulations
 Development of pharmaceutical emulsions
 Microemulsions as drug carriers
 Reference
2
INTRODUCTION
Formulation and development is a process
of selection of component and processing
 Various technique such as design of experiments are
implemented for optimization of formulation and
processing parameter
 Traditionally optimization refers to changing one
variable at a time
 Many times finding the correct answer is not simple .
In such cases use of computer tools is the best way
to solve problem
3
DEVELOPMENT OF
PHARMACEUTICAL EMULSIONS
 Definition
An emulsion is a thermodynamically
unstable system containing mixture of two or more
immiscible liquids which is stabilized by adding
emulsifying agent.
 Phases of emulsion
Discontinuous phase
Continous phase
4
TYPES OF EMULSIONS
 Based on dispersed phase
Oil in water(o/w)
Water in oil (w/o)
Water in oil in water(w/o/w)
 Based on size of liquids
Macroemulsions
Microemulsions
5
EMULSIFYING AGENTS
An emulsifying agent is any material
that enhances the stability of an emulsion
 Mainly 3 types
Surfactants- Eg: SLS, Cetrimide
Hydrocolloids- Eg: Acacia, Tragacanth
Finely divided solids- Eg : Bentonite
6
THEORIES OF
EMULSIFICATION
 Film theory:
The added emulsifying agent forms a mechanical film
by getting adsorption
 Viscosity theory:
↑in viscosity,↑in stability
 Wedge theory:
Monovalent soap gives o/w emulsion,divalent soap
gives w/o emulsion
 Interfacial theory:
The added emulsifying agent reduces the interfacial
tension
7
STABILITY OF EMULSIONS
Most common stability problems are
 Creaming and sedimentation:
As the droplets are subjected to gravity
force,they tend to move upward (creaming) or
downward(sedimentation)
 Cracking or coalescence:
Is the fusion of 2 or more droplets of the
disperse phase forming one droplet
 Phase inversion:
Emulsion changes from one type to another
8
METHODS TO ENHANCE
STABILITY
 Globule size:
smaller particles have slower creaming or
sedimentation
 Viscosity of continuous phase:
↑in viscosity ↑stability
 Using emulsifying agent:
Enhance viscosity,reduce interfacial tension
 Storage of temperature:
↑ in temp,↓ stability
9
METHODS FOR EVALUATION OF
STABILITY OF EMULSIONS
 Size frequency analysis by microscopy
 Velocity of craming
 Globule size analysis
 Turbidimetric analysis
 Conductivity testing
10
METHODS OF
PREPARATION
 Dry gum method
• Triturate emulsifier+oil
• Add water
• Triturate and form primary emulsion
• Add remaining qty of water
 Wet gum method
• Triturate gum+water
• Add oil and form primary emulsion
• Add remaining qty of water
11
METHODS OF
PREPARATION
 Bottle or Forbes bottle method
Gum+oil
↓
shake
↓
Add water
↓
Shake to form primary emulsion
↓
Add remaining qty of water
12
APPLICATIONS OF
EMULSIONS
 Oral administarion of water insoluble liquids
 IV administration of API as an emulsion(Taxol)
 For external use(lotions,liniments)
 Emulsions in aerosol can be used to produce
foam
13
MICROEMULSIONS AS DRUG
CARRIERS
14
MICROEMULSIONS
Microemulsions are
thermodynamically stable,optically
transparent,isotropic dispersions of
aquous and hydrocarbon liquids stabilized
by an interfacial film of surfactants
molecule
15
MICROEMULSION AS A DRUG
CARRIER SYSTEM
 Improved drug solubilization
 Long shelf life
 Ease of preparation
 Improved bioavailability
16
DISADVANTAGES
 Stability is influenced by environmental
parameters such as temperature and ph
 Limited solubilizing capacity for high melting
substances
17
TYPES OF
MICROEMULSIONS
 Direct microemulsion:
Droplets are dispersed in the
continuous aquous phase
 Reversed microemulsion:
Water droplets are dispersed in the
continuous oil phase
 Bicontinuous microemulsion:
Micro domains of oil and water are
interdispersed within the system
18
THEORIES OF
MICROEMULSION
 Thermodynamic theory
The free energy of microemulsion formation can be
dependent on the extent to which surfactant lowers the surface
tension of oil-water interface
DGF=ˠDA-TDS
 Solubilization theory
Formation of microemulsion by micelles gradually
become larger and swells to a certain size range results
 Interfacial theory
Microemulsion is capable of forming negative
interfacial tension
19
COMPONENTS OF
MICROEMULSION
 Oil – Eg:Isopropylmyristate,olive oil
 Surfactant –Eg:Tween80,Tween20
 Cosurfactants-Eg:Propyleneglycol,Ethanol
20
PREPARATION
 Drug has to dissolve in to oil phase of microemulsion
 Water phase is combined with surfactant and cosurfactant
 The amount of surfactant and cosurfactant to be added in the oil
phase is determined with the help of pseudoternary phase diagram
 Ultrasonicator can finally used to achieve the desired range for the
dispersed phase
 It is then allow to equilibrate
 Gel may be prepared by the addition of gelling agent to above
microemulsion
21
APPLICATIONS
 Dry cleaning process
 Pesticide formulation
 Floor polishers and cleaners
 Cutting oils
 In industry for the synthesis of polymers
22
REFERENCE
 www.slideshare .com
 Textbook of Industrial Pharmacy by
Liebermann
23

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Emulsions and microemulsions- computer in pharmaceutical formulatation

  • 1. COMPUTERS IN PHARMACEUTICAL FORMULATIONS Presented By Sujitha Mary M Pharm St Joseph College Of Pharmacy 1
  • 2. CONTENTS  Computers in pharmaceutical formulations  Development of pharmaceutical emulsions  Microemulsions as drug carriers  Reference 2
  • 3. INTRODUCTION Formulation and development is a process of selection of component and processing  Various technique such as design of experiments are implemented for optimization of formulation and processing parameter  Traditionally optimization refers to changing one variable at a time  Many times finding the correct answer is not simple . In such cases use of computer tools is the best way to solve problem 3
  • 4. DEVELOPMENT OF PHARMACEUTICAL EMULSIONS  Definition An emulsion is a thermodynamically unstable system containing mixture of two or more immiscible liquids which is stabilized by adding emulsifying agent.  Phases of emulsion Discontinuous phase Continous phase 4
  • 5. TYPES OF EMULSIONS  Based on dispersed phase Oil in water(o/w) Water in oil (w/o) Water in oil in water(w/o/w)  Based on size of liquids Macroemulsions Microemulsions 5
  • 6. EMULSIFYING AGENTS An emulsifying agent is any material that enhances the stability of an emulsion  Mainly 3 types Surfactants- Eg: SLS, Cetrimide Hydrocolloids- Eg: Acacia, Tragacanth Finely divided solids- Eg : Bentonite 6
  • 7. THEORIES OF EMULSIFICATION  Film theory: The added emulsifying agent forms a mechanical film by getting adsorption  Viscosity theory: ↑in viscosity,↑in stability  Wedge theory: Monovalent soap gives o/w emulsion,divalent soap gives w/o emulsion  Interfacial theory: The added emulsifying agent reduces the interfacial tension 7
  • 8. STABILITY OF EMULSIONS Most common stability problems are  Creaming and sedimentation: As the droplets are subjected to gravity force,they tend to move upward (creaming) or downward(sedimentation)  Cracking or coalescence: Is the fusion of 2 or more droplets of the disperse phase forming one droplet  Phase inversion: Emulsion changes from one type to another 8
  • 9. METHODS TO ENHANCE STABILITY  Globule size: smaller particles have slower creaming or sedimentation  Viscosity of continuous phase: ↑in viscosity ↑stability  Using emulsifying agent: Enhance viscosity,reduce interfacial tension  Storage of temperature: ↑ in temp,↓ stability 9
  • 10. METHODS FOR EVALUATION OF STABILITY OF EMULSIONS  Size frequency analysis by microscopy  Velocity of craming  Globule size analysis  Turbidimetric analysis  Conductivity testing 10
  • 11. METHODS OF PREPARATION  Dry gum method • Triturate emulsifier+oil • Add water • Triturate and form primary emulsion • Add remaining qty of water  Wet gum method • Triturate gum+water • Add oil and form primary emulsion • Add remaining qty of water 11
  • 12. METHODS OF PREPARATION  Bottle or Forbes bottle method Gum+oil ↓ shake ↓ Add water ↓ Shake to form primary emulsion ↓ Add remaining qty of water 12
  • 13. APPLICATIONS OF EMULSIONS  Oral administarion of water insoluble liquids  IV administration of API as an emulsion(Taxol)  For external use(lotions,liniments)  Emulsions in aerosol can be used to produce foam 13
  • 15. MICROEMULSIONS Microemulsions are thermodynamically stable,optically transparent,isotropic dispersions of aquous and hydrocarbon liquids stabilized by an interfacial film of surfactants molecule 15
  • 16. MICROEMULSION AS A DRUG CARRIER SYSTEM  Improved drug solubilization  Long shelf life  Ease of preparation  Improved bioavailability 16
  • 17. DISADVANTAGES  Stability is influenced by environmental parameters such as temperature and ph  Limited solubilizing capacity for high melting substances 17
  • 18. TYPES OF MICROEMULSIONS  Direct microemulsion: Droplets are dispersed in the continuous aquous phase  Reversed microemulsion: Water droplets are dispersed in the continuous oil phase  Bicontinuous microemulsion: Micro domains of oil and water are interdispersed within the system 18
  • 19. THEORIES OF MICROEMULSION  Thermodynamic theory The free energy of microemulsion formation can be dependent on the extent to which surfactant lowers the surface tension of oil-water interface DGF=ˠDA-TDS  Solubilization theory Formation of microemulsion by micelles gradually become larger and swells to a certain size range results  Interfacial theory Microemulsion is capable of forming negative interfacial tension 19
  • 20. COMPONENTS OF MICROEMULSION  Oil – Eg:Isopropylmyristate,olive oil  Surfactant –Eg:Tween80,Tween20  Cosurfactants-Eg:Propyleneglycol,Ethanol 20
  • 21. PREPARATION  Drug has to dissolve in to oil phase of microemulsion  Water phase is combined with surfactant and cosurfactant  The amount of surfactant and cosurfactant to be added in the oil phase is determined with the help of pseudoternary phase diagram  Ultrasonicator can finally used to achieve the desired range for the dispersed phase  It is then allow to equilibrate  Gel may be prepared by the addition of gelling agent to above microemulsion 21
  • 22. APPLICATIONS  Dry cleaning process  Pesticide formulation  Floor polishers and cleaners  Cutting oils  In industry for the synthesis of polymers 22
  • 23. REFERENCE  www.slideshare .com  Textbook of Industrial Pharmacy by Liebermann 23