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SEMISOLID
DOSAGE FORMS-2
Presented By:
K. Arshad Ahmed Khan
M.Pharm
Departmernt of
Pharmaceutics
RIPER.
Ingredients :
Active pharmaceutical ingredients
Bases
Preservatives
Humectants
Anti oxidants
Emulsifier
Gelling agent
Permeation enhancer
Buffers
It is one of the most important ingredient used in
the formulation of semisolid dosage form
Ointments and suppository base do not merely
acts as the carrier of the medicaments, but they also
control the extent of absorbtion of medicaments
incorporated with them
They should be:
 Compatible with skin ph and drug
 Inert ,non irritating and non sensitizing
 Good solvent and/or emulsifying agent
 Emollient , protective , non greasy and easily
removable
 Release medicaments easily at the site of
administration
 Pharmaceutical elegant and possess good stability.
BASES
OLEAGENOUS
BASE
ABSORBTION
BASE
EMULSION
BASE
WATER
SOLUBLE
BASE
1. Oleaginous ( hydrocarbon) bases:
They consist of a combination of more than one oleaginous
material such as water insoluble hydrophobic oils and fats
They are highly compatible ; occlusive ; good emollients
They are anhydrous, do not absorb water, readily(hydrophobic)
insoluble in water, non washable
Example : Vaseline,hard parafin, liquid paraffin,white ointment.
Uses : protective, emollient and vehicle for solid drugs.
2. Absorption (Emulsifiable) base:
Have capacity to absorb considerable quantities of
water or aqueous solution and turns to w/o without
marked changes in the consistency.
They are anhydrous, water insoluble and water
unwashable.
They have good emollient but poor occlusive
property.
Uses: protective, emollient and vehicle for aqueous
solutions and solid drug.
3. Emulsion bases:
According to the type of emulsion these bases are
classified as either W/O or O/W.
W/O EMULSION
BASE
O/W EMULSION
BASE
Hydrous Hydrous
Will absorb water Will absorb water
Insoluble in water Insoluble in water
Not washable washable
4. Water soluble Bases:
 These include both hydrous and non hydrous
dermatological non- emulsion bases which are water
soluble and contain no oil phase.
 Water soluble, water washable, non greasable
 Because they softens with the addition of water, large
amount of aqueous solutions are not effectively
incorporated into the bases.
Example : carbowax compounds such as the poly
ethylene glycol bases containing pectin, cellulose,
bentonite and gelatin.
Some bases , although, resist microbial attack but
because of their high water content, it require an anti
microbial preservative.
Commonly used preservative include:
Methyl hydroxy benzoate
Propyl hydroxy benzoate
Chlorocresol
Benzoic acid
Phenyl mercuric nitrate
Oxygen is highly reactive atom that is capable of
becoming of potentially damaging molecules
commonly called “free radicals”.
Free radicals are capable of attacking the healthy
cells of the body, causing them to loose their structure
and functions
To prevent this an anti oxidant are added.
Example : Butylated hydroxy anisole , Butylated
hydroxy toluene
CLASSIFICATION OF ANTIOXIDANT
ANTIOXIGENS REDUCING
AGENT
ANTIOXIDANT
SYNERGIST
Acts by reacting with
the free radicals.
e.g.
•Butylated hydroxy
anisole (BHA)
•Butylated hydroxy
tocopherols (BHT)
(used for oil system)
Have lower redox
potential than
drug,hence gets
oxidized first.
e.g.
•Ascorbic acid
•Potassium and
sodium metabisulfite
•Thiosulfite
(used for aqueous
system)
Chelating or
sequestering agents,
enhance the effect of
anti oxidants.
e.g.
•Citric acid
•Tartaric acid
•Lacithin
Gelling agents
 Gelling agent forms a gel dissolves in a liquid phase as a
colloid mixture that forms a weakly cohesive internal
structure.
 These are organic hydro colloids or hydro phillic
inorganic substances.
Example : tragacanth, sodium alginate, pectin, gelatin,
cellulose derivatives.
Material % Brook field
viscosity
Carbomer 94 1 resin NF 0.15 2900
Carbomer 94 1 resin NF 0.25 6300
Guar gum 1.50 8040
Methyl cellulose 2.00 5200
Sodium alginate 2.50 10400
Permeation enhancer
Skin can acts as a barrier with the introduction of
various penetration enhancers, penetration of the
drug through the skin can be improved.
Permeation enhancer Drug used
Methanol,carvacrol,
linalool
Propranolol
hydrochloride
Limonene Indomethacin ,
ketoprofin
Geraniol
Nerolidol
Diclofenic sodium
Oleic acid Piroxicam
Anionic Cationic Non ionic
•Alkyl sulphates
•Soaps
•D odecyl benzene
•Sulfonates
•Lactylates
•Sulfosuccinates
•Monoglycerides
•Sulfonates
•Phosphate esters
•Silicones
•Taurates
•Quaternary
ammonium
compounds
•alkoxyalkylamines
•Polyoxyethylene
•Alkyl-aryl ethers
•Polyoxy ethylene
•Sorbitan esters
•Sorbitan fatty acid
esters
•Glyceryl fatty acid
esters
A humectant is a hygroscopic substance . It is
often a molecule with several hydrophilic groups,
most often hydroxyl group.
Humectants are used to:
 Increase the solubility of active ingredients
 To elevate its skin preparation
 Elevate the hydration of the skin.
Buffers are added to variopus purpose such as:
 Compatibility with skin
 Drug solubility
 Drug Stability
 Influence on ionization of drug
Example: Sodium acetate , Sodium Citrate , Potassium meta
phosphate
Purified water
Water for Injection
Water for injection may be used in
ophthalmic semi solid preparation like eye
ointments , gels etc
PREPARATION OF SEMI SOLIDS
Trituration
method
Fusion
method
Chemical
reaction
method
Emulsificatio
n method
Ex. Ointments
creams
pastes
Ex. Ointments
creams
pastes
Ex. Ointments
creams
Ex. Ointments
creams
(Ointments, creams, pastes)
PREPARATION METHODS FOR
SUPPOSITORIES
Hand molding Heat molding
Automatic
machine
molding
Compression
molding
Ex. Rotary machine
linear machine
SIZE REDUCTION
LEVIGATION
MIXING WITH BASE
SPATULATION OR
TRITURATION
MIXING BASE TO
PRODUCE FINAL WEIGHT
HOMOGENIZATION
FILLING
Thank
you…..

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semisolid dosage form-2

  • 1. SEMISOLID DOSAGE FORMS-2 Presented By: K. Arshad Ahmed Khan M.Pharm Departmernt of Pharmaceutics RIPER.
  • 2. Ingredients : Active pharmaceutical ingredients Bases Preservatives Humectants Anti oxidants Emulsifier Gelling agent Permeation enhancer Buffers
  • 3. It is one of the most important ingredient used in the formulation of semisolid dosage form Ointments and suppository base do not merely acts as the carrier of the medicaments, but they also control the extent of absorbtion of medicaments incorporated with them
  • 4. They should be:  Compatible with skin ph and drug  Inert ,non irritating and non sensitizing  Good solvent and/or emulsifying agent  Emollient , protective , non greasy and easily removable  Release medicaments easily at the site of administration  Pharmaceutical elegant and possess good stability.
  • 6. 1. Oleaginous ( hydrocarbon) bases: They consist of a combination of more than one oleaginous material such as water insoluble hydrophobic oils and fats They are highly compatible ; occlusive ; good emollients They are anhydrous, do not absorb water, readily(hydrophobic) insoluble in water, non washable Example : Vaseline,hard parafin, liquid paraffin,white ointment. Uses : protective, emollient and vehicle for solid drugs.
  • 7. 2. Absorption (Emulsifiable) base: Have capacity to absorb considerable quantities of water or aqueous solution and turns to w/o without marked changes in the consistency. They are anhydrous, water insoluble and water unwashable. They have good emollient but poor occlusive property. Uses: protective, emollient and vehicle for aqueous solutions and solid drug.
  • 8. 3. Emulsion bases: According to the type of emulsion these bases are classified as either W/O or O/W. W/O EMULSION BASE O/W EMULSION BASE Hydrous Hydrous Will absorb water Will absorb water Insoluble in water Insoluble in water Not washable washable
  • 9. 4. Water soluble Bases:  These include both hydrous and non hydrous dermatological non- emulsion bases which are water soluble and contain no oil phase.  Water soluble, water washable, non greasable  Because they softens with the addition of water, large amount of aqueous solutions are not effectively incorporated into the bases. Example : carbowax compounds such as the poly ethylene glycol bases containing pectin, cellulose, bentonite and gelatin.
  • 10. Some bases , although, resist microbial attack but because of their high water content, it require an anti microbial preservative. Commonly used preservative include: Methyl hydroxy benzoate Propyl hydroxy benzoate Chlorocresol Benzoic acid Phenyl mercuric nitrate
  • 11. Oxygen is highly reactive atom that is capable of becoming of potentially damaging molecules commonly called “free radicals”. Free radicals are capable of attacking the healthy cells of the body, causing them to loose their structure and functions To prevent this an anti oxidant are added. Example : Butylated hydroxy anisole , Butylated hydroxy toluene
  • 12. CLASSIFICATION OF ANTIOXIDANT ANTIOXIGENS REDUCING AGENT ANTIOXIDANT SYNERGIST Acts by reacting with the free radicals. e.g. •Butylated hydroxy anisole (BHA) •Butylated hydroxy tocopherols (BHT) (used for oil system) Have lower redox potential than drug,hence gets oxidized first. e.g. •Ascorbic acid •Potassium and sodium metabisulfite •Thiosulfite (used for aqueous system) Chelating or sequestering agents, enhance the effect of anti oxidants. e.g. •Citric acid •Tartaric acid •Lacithin
  • 13. Gelling agents  Gelling agent forms a gel dissolves in a liquid phase as a colloid mixture that forms a weakly cohesive internal structure.  These are organic hydro colloids or hydro phillic inorganic substances. Example : tragacanth, sodium alginate, pectin, gelatin, cellulose derivatives. Material % Brook field viscosity Carbomer 94 1 resin NF 0.15 2900 Carbomer 94 1 resin NF 0.25 6300 Guar gum 1.50 8040 Methyl cellulose 2.00 5200 Sodium alginate 2.50 10400
  • 14. Permeation enhancer Skin can acts as a barrier with the introduction of various penetration enhancers, penetration of the drug through the skin can be improved. Permeation enhancer Drug used Methanol,carvacrol, linalool Propranolol hydrochloride Limonene Indomethacin , ketoprofin Geraniol Nerolidol Diclofenic sodium Oleic acid Piroxicam
  • 15. Anionic Cationic Non ionic •Alkyl sulphates •Soaps •D odecyl benzene •Sulfonates •Lactylates •Sulfosuccinates •Monoglycerides •Sulfonates •Phosphate esters •Silicones •Taurates •Quaternary ammonium compounds •alkoxyalkylamines •Polyoxyethylene •Alkyl-aryl ethers •Polyoxy ethylene •Sorbitan esters •Sorbitan fatty acid esters •Glyceryl fatty acid esters
  • 16. A humectant is a hygroscopic substance . It is often a molecule with several hydrophilic groups, most often hydroxyl group. Humectants are used to:  Increase the solubility of active ingredients  To elevate its skin preparation  Elevate the hydration of the skin.
  • 17. Buffers are added to variopus purpose such as:  Compatibility with skin  Drug solubility  Drug Stability  Influence on ionization of drug Example: Sodium acetate , Sodium Citrate , Potassium meta phosphate
  • 18. Purified water Water for Injection Water for injection may be used in ophthalmic semi solid preparation like eye ointments , gels etc
  • 19. PREPARATION OF SEMI SOLIDS Trituration method Fusion method Chemical reaction method Emulsificatio n method Ex. Ointments creams pastes Ex. Ointments creams pastes Ex. Ointments creams Ex. Ointments creams (Ointments, creams, pastes)
  • 20. PREPARATION METHODS FOR SUPPOSITORIES Hand molding Heat molding Automatic machine molding Compression molding Ex. Rotary machine linear machine
  • 21. SIZE REDUCTION LEVIGATION MIXING WITH BASE SPATULATION OR TRITURATION MIXING BASE TO PRODUCE FINAL WEIGHT HOMOGENIZATION FILLING
  • 22.