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SOLID DISPERSION
A Seminar
By
Mr.Hanmant A.Galande.
Under the Guidance of
Dr. P.K. Pawar
Head of Pharmaceutics Department
Gourishankar Institute of Pharmaceutical Education &
Research Limb, Satara.
(2016-17)
 Introduction of Solid Dispersion
 Definition & Need
 Selection of The Carrier
 Types of Solid Dispersion
 Preparation Techniques
 Characterization of Solid Dispersion
 Advantages of Solid Dispersion
 Disadvantages of Solid Dispersion
 Application of Solid Dispersion
 References
CONTENTS
INTRODUCTION
 The concept of solid dispersion was originally
proposed by Sekiguchi & obi.
 Increasing solubility in water.
 Increasing the dissolution, absorption & therapeutic
efficacy of drugs in dosage forms.
 Improving the oral absorption and bioavailability of
BCS Class II drugs.
Definition & Need
 Definition: The technology is the science of
dispersing one or more active ingredients in an
inert matrix in the solid stage.
 Need of solid dispersion:
 Improved the solubility & stability.
 Enhanced release of drugs from ointment.
 Increased dissolution rate.
 Increases Oral bioavailability of a drug
SELECTION OF A CARRIER
 Freely water-soluble.
 Non-toxic and pharmacologically inert.
 Thermal stability
 Soluble in a variety of solvents.
 Enhances solubility of drug
 Chemically compatible with drugs.
 Eg.PVP,PEG,HPMC,CMC,CMEC,Urea
TYPES OF SOLID DISPERSION
PREPARATION TECHNIQUES
 Melting method
 Solvent evaporation method
 Melt extrusion method
 Super Critical Fluid (SCF) Technology
 Melting solvent method
 Spray drying
 Lyophilization technique
 Kneading method
1) Melting method
Physical mixture of a drug & water soluble carrier
heat directly until it get melted
cooled & solidified rapidly-ice bath-vigorous stirring.
solid mass was crushed, pulverized & sieved.
2) Solvent evaporation method
Drug + matrix ( both dissolve in solvent)
Solution
Evaporate The Solvent
Solid Mass is Sieved & Dried
Solid Dispersion
E.g..Atrovastatin + Neem gum
Temperatures
used for solvent
evaporation
generally lie in
the range 23-
65°C.
The solvent
evaporation can be
done by spray
drying or freeze
drying.
High rotating speed Drug + carrier mix
small period of time
using co-rotating twin- screw extruder.
Simultaneously melted & homogenized
extruded and shaped as tablets, granules, pellets
3) Melt extrusion method
4) Supercritical fluid technology
 These process involves the spaying of the solution
of solute and organic solvent into continuous
Supercritical phase flowing concurrently
 Eg. Carbon dioxide ,Nitrogen etc.
5) Melting solvent method
Drug dissolve in suitable solvent
Add melt of PEG
Evaporation of solvent
left clear film
Drying of film to get const.wt
6) Spray Drying
 polymeric fluid stream solution or melt delivered
through a millimeter-scale nozzle
 Rapid drying
 Produces fine dust free powder with specific size &
shape
SOLID DISPERSION-CHARACTERIZATION
1.Drug -carrier miscibility
• Hot stage microscopy
• Differential scanning calorimetry
• Powder X-ray diffraction
• NMR 1H Spin lattice relaxation time
2.Drug carrier interactions
• FT-IR spectroscopy
• Raman spectroscopy
• Solid state NMR
 Physical Structure
• Scanning electron microscopy
• Surface area analysis
• Surface properties
• Dynamic vapor sorption
• Inverse gas chromatography
• Atomic force microscopy
• Raman microscopy
 Amorphous content
• Polarized light optical microscopy
• Hot stage microscopy
• Humidity stage microscopy
• DSC (MTDSC)
• Powder X-ray diffraction
Stability
• Humidity studies
• Isothermal Calorimetry
• DSC (Tg, Temperature recrystallization)
• Dynamic vapor sorption
• Saturated solubility studies
Dissolution enhancement
• Dissolution
• Intrinsic dissolution
• Dynamic solubility
• Dissolution in bio-relevant media
APPLICATIONS
 To increase the solubility, dissolution rate ,
absorption and bioavailability.
 Improved the solubility & stability.
 To formulate a fast released dosage form.
 To reduce side effect of certain drugs.
 Masking of unpleasant taste and smell of drugs
 Improvement of drug release from ointment,
creams .
ADVANTAGES
 To reduced particle size.
 To improve wettability.
 To improve porosity of drug.
 To decrease the crystalline structure of drug in to
amorphous form.
 To improve dissolution in water of a poorly water-
soluble drug.
DISADVANTAGES
 Instability
 Not easy handling because of tackiness.
 The scale up of manufacturing processes.
REFERENCES
1. Singh Sameer, Raviraj Singh Baghel., Yadav Lalit, 2011.A
review on solid dispersion. International Journal of
pharmacy & life sciences.
2. Rajni Sharma, Rupa Mazumder, Archana Sharma and
Praveen Verma A review on: Solid dispersion
International Journal Of Pharmacy & Life Sciences.
3. L.Nikghalb1 ,G. Singh ,Gaurav Singh, and K.Kahkeshan
Solid Dispersion: Methods and Polymers to increase the
solubility of poorly soluble drugs Journal of Applied
Pharmaceutical Science Vol. 2 (10), pp. 170-175.
1.solid dispersion  1 st sem

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1.solid dispersion 1 st sem

  • 1.
  • 2. SOLID DISPERSION A Seminar By Mr.Hanmant A.Galande. Under the Guidance of Dr. P.K. Pawar Head of Pharmaceutics Department Gourishankar Institute of Pharmaceutical Education & Research Limb, Satara. (2016-17)
  • 3.  Introduction of Solid Dispersion  Definition & Need  Selection of The Carrier  Types of Solid Dispersion  Preparation Techniques  Characterization of Solid Dispersion  Advantages of Solid Dispersion  Disadvantages of Solid Dispersion  Application of Solid Dispersion  References CONTENTS
  • 4. INTRODUCTION  The concept of solid dispersion was originally proposed by Sekiguchi & obi.  Increasing solubility in water.  Increasing the dissolution, absorption & therapeutic efficacy of drugs in dosage forms.  Improving the oral absorption and bioavailability of BCS Class II drugs.
  • 5. Definition & Need  Definition: The technology is the science of dispersing one or more active ingredients in an inert matrix in the solid stage.  Need of solid dispersion:  Improved the solubility & stability.  Enhanced release of drugs from ointment.  Increased dissolution rate.  Increases Oral bioavailability of a drug
  • 6. SELECTION OF A CARRIER  Freely water-soluble.  Non-toxic and pharmacologically inert.  Thermal stability  Soluble in a variety of solvents.  Enhances solubility of drug  Chemically compatible with drugs.  Eg.PVP,PEG,HPMC,CMC,CMEC,Urea
  • 7. TYPES OF SOLID DISPERSION
  • 8. PREPARATION TECHNIQUES  Melting method  Solvent evaporation method  Melt extrusion method  Super Critical Fluid (SCF) Technology  Melting solvent method  Spray drying  Lyophilization technique  Kneading method
  • 9. 1) Melting method Physical mixture of a drug & water soluble carrier heat directly until it get melted cooled & solidified rapidly-ice bath-vigorous stirring. solid mass was crushed, pulverized & sieved.
  • 10. 2) Solvent evaporation method Drug + matrix ( both dissolve in solvent) Solution Evaporate The Solvent Solid Mass is Sieved & Dried Solid Dispersion E.g..Atrovastatin + Neem gum Temperatures used for solvent evaporation generally lie in the range 23- 65°C. The solvent evaporation can be done by spray drying or freeze drying.
  • 11. High rotating speed Drug + carrier mix small period of time using co-rotating twin- screw extruder. Simultaneously melted & homogenized extruded and shaped as tablets, granules, pellets 3) Melt extrusion method
  • 12. 4) Supercritical fluid technology  These process involves the spaying of the solution of solute and organic solvent into continuous Supercritical phase flowing concurrently  Eg. Carbon dioxide ,Nitrogen etc.
  • 13. 5) Melting solvent method Drug dissolve in suitable solvent Add melt of PEG Evaporation of solvent left clear film Drying of film to get const.wt
  • 14. 6) Spray Drying  polymeric fluid stream solution or melt delivered through a millimeter-scale nozzle  Rapid drying  Produces fine dust free powder with specific size & shape
  • 15. SOLID DISPERSION-CHARACTERIZATION 1.Drug -carrier miscibility • Hot stage microscopy • Differential scanning calorimetry • Powder X-ray diffraction • NMR 1H Spin lattice relaxation time 2.Drug carrier interactions • FT-IR spectroscopy • Raman spectroscopy • Solid state NMR
  • 16.  Physical Structure • Scanning electron microscopy • Surface area analysis • Surface properties • Dynamic vapor sorption • Inverse gas chromatography • Atomic force microscopy • Raman microscopy  Amorphous content • Polarized light optical microscopy • Hot stage microscopy • Humidity stage microscopy • DSC (MTDSC) • Powder X-ray diffraction
  • 17. Stability • Humidity studies • Isothermal Calorimetry • DSC (Tg, Temperature recrystallization) • Dynamic vapor sorption • Saturated solubility studies Dissolution enhancement • Dissolution • Intrinsic dissolution • Dynamic solubility • Dissolution in bio-relevant media
  • 18. APPLICATIONS  To increase the solubility, dissolution rate , absorption and bioavailability.  Improved the solubility & stability.  To formulate a fast released dosage form.  To reduce side effect of certain drugs.  Masking of unpleasant taste and smell of drugs  Improvement of drug release from ointment, creams .
  • 19. ADVANTAGES  To reduced particle size.  To improve wettability.  To improve porosity of drug.  To decrease the crystalline structure of drug in to amorphous form.  To improve dissolution in water of a poorly water- soluble drug.
  • 20. DISADVANTAGES  Instability  Not easy handling because of tackiness.  The scale up of manufacturing processes.
  • 21. REFERENCES 1. Singh Sameer, Raviraj Singh Baghel., Yadav Lalit, 2011.A review on solid dispersion. International Journal of pharmacy & life sciences. 2. Rajni Sharma, Rupa Mazumder, Archana Sharma and Praveen Verma A review on: Solid dispersion International Journal Of Pharmacy & Life Sciences. 3. L.Nikghalb1 ,G. Singh ,Gaurav Singh, and K.Kahkeshan Solid Dispersion: Methods and Polymers to increase the solubility of poorly soluble drugs Journal of Applied Pharmaceutical Science Vol. 2 (10), pp. 170-175.