SEMI – SOLIDS
Shekinah Faith S. Balindan
BSPharmacy 4B
Learning Objectives
• Uses
• Factors Influencing Absorption
• Raw Materials For Semisolids
• Type Of Vehicle
• Factors Which Influence The
Choice Of Semisolid Vehicles
• Classes Of Semisolid – Usp
• Ophthalmic Ointment
• Preparation Of Ointment
• Semisolids
• Manufacture Of Emulsified
Semisolid
Pharmaceutical dosage form with
viscous consistency intended for
application on the skin
- Vehicle for topically applied drugs
- Emollients-soothing or softening's effect on surface
tissue
- Protective or occlusive dressings on the skin
- Partition coefficient of the drug
- Moisture and temperature in the environment
of the skin
- Pathologic injury to the skin
Vehicle used
PARTITION COEFFICIENT
Substance processing both water and lipid
solubility are favorable absorbed through the
skin
MOISTURE AND TEMPERATURE
- The moisture balance on the stratum corneum
(horny layer of the epidermis) of the skin has been
due to the presence of a combination of compounds
known as “natural moisturizing factor”.
MOISTURE AND TEMPERATURE
- The fat in the skin provides a protective film to
prevent this factor from being removed from the skin
during excessive contact with water as a bathing
PATHOLOGIC INJURY TO THE SKIN
- Skin penetration has been enhanced by abrasions or
stripping the skin of its barrier layer
- Skin penetration of the drug substances can be the
use of suitable vehicles
HYDROCARBONS
Petrolatum and mineral oil are perhaps the widely used substance in
semisolids next to water
Petrolatum – a complex mixture of semisolids containing
hydrocarbon alipathic, cyclic, saturated, unsaturated branch and
unbranched substance in varying proportions
Mineral oil – obtained from petroleum acid. Lower viscosity is more
preferred since it is less tacky.
HYDROCARON WAXES
Employed to increase the viscosity of mineral oil to prevent
separation from ointment.
Paraffin and ceresin wax
OLEAGINOUS SUBSTANCES
Vegetable oil such as peanut, almond oil, almond oil, sesame
oil and olive oil and glycerides of mixtures of unsaturated
fatty acids
FATTY ACIDS AND ALCOHOLS
Stearic acids – used in water removable creams as an emulsifier to
develop a certain consistency in the cream
Stearyl alcohol and cetyl alcohol (palmityl alcohol) – used in
creams as auxiliary emulsifiers and emollients; in sufficient stearyl
alcohol produces a firm cream which maybe softened by cetyl
alcohol.
EMULSIFIERS
- The water soluble soaps (triethanolamine stearate soap) were
among the first emulsifiers used for semisolid oil in water
emulsions. The viscosity of the cream or emollient prevents
coalescence of the emulsified phases and helps to stabilize the
emulsion. The interfacial film formed around the dispersed phase
globules is generally solid making emulsified preparation more
rigid.
POLYOLS
Glycerin, propylene glycol, sorbitol 70% and the
lower molecular weight polyethylene glycols are used
as humectants (prevent drying up) and prevent
formation of crust on the top of the cream
INSOLUBLE POWDERS
Insoluble powders must be uniformly dispersed
throughout the vehicle to assure homogeneity of the
product. The solid must be impalpable to touch. Particles
less than 74 microns in size equivalent to the mesh
openings in a number 200 mesh sieve of the US standard
sieve series are considered impalpable to most people
- The vehicle used for semisolid pharmaceutical
preparation differs from that used for cosmetics because
with a cosmetic, penetration to the skin is not desired.
- A well formulated pharmaceutical semisolid should be
both effective therapeutically and cosmetically appealing
but in major effort must be in medicinal direction
- Nature of the skin lesion
- Solubility and stability of the drug
Hydrocarbon base
Adsorption base
Water removable base
Water soluble base
HYDROCARBON BASE
Petrolatum and white ointment (petrolatum with 5% beeswax) are
typical lipophilic vehicles
Petrolatum is the most commonly used in ointment vehicles
because of its consistency, bland and neutral characteristics and its
ability to spread easily on the skin
These vehicle is difficult to wash off and are used as occlusive
dressings which produces sensation of warmth because of the
normal evaporation of perspiration is inhibited
ABSORPTION BASES
Hydrophilic mixtures formed by the addition of substances
miscible with hydrocarbons and possessing polar groupings
such as SO4, sulfonate, carboxyl, hydroxyl or an ether
linage.
E.g. lanolin, cholesterol, sterols, sorbitan monostearate,
sorbitan monooleate
ABSORPTION BASES
- Mineral oil is added to these bases to reduce tackiness of the
base
- Cold cream type w/o emulsion belongs to this type of the
base. This is a borax-beeswax combination with mineral oil or
vegetable oil as the continuous phase. A protective oil film
remains on the skin and slow evaporation of water gives the
skin a cooling effect.
WATER REMOVABLE BASE
- They are oil in water emulsions
- Upon application and rubbing into the skin, there is
little or no visible evidence of its presence
- The vanishing cream - o/w emulsion but with
absorption base which is w/o emulsion
WATER SOLUBLE BASE
- Prepared from mixtures of high and low molecular weight polyethylene glycols
- Characteristics:
• Low molecular weight are liquids; moderately higher molecular are unctuous,
high molecular weight are solids
• No water is required for their preparation
• Combination of high and low molecular weight polyethylene glycols yield
products having ointment like consistency which softens or melts when applied
to the skin
• Have polar group
• Also known as greaseless ointment base
- Semisolid ophthalmic vehicles frequently contain soft
petrolatum, a brand adsorption base or water soluble base
- Material used should avoid the eye discomfort and irritation
- Should be sterile when used in injure eye
Fusion method (anhydrous ointments) – dissolving the
active ingredients in the melted fats and waxes or in the
vehicle and then mixed with the base.
• Melted mass must be mixed while cooling to ensure
homogenous distribution of the ingredients
PRESERVATION
Preservation is evaluated to:
- Stability with regard to other components of
the formula
- Container to be used
CHARACTERISTICS OF PRESERVATIVES
• Some preservatives becomes inactive in the presence
of other ingredients
- 5% tween 80 in activates 80% of the total methyl
paraben – higher conc. of preservatives is required
• Boric acid may be used in ophthalmic preparation
ANTIOXIDANTS
-Added whenever oxidative deterioration is anticipated.
-Choice of antioxidants depends on:
Toxicity
Irritating potency
Compatibility
Odor
Discoloration
Solubility
Stability
 Aeration should be prevented for stability and
consistency in density. This can be done by introducing
one phase below the surface of the other liquid or
phase and mixing carefully
 In filling into tubes, the hopper should be filled with the
product to prevent incorporation of air
RHEOLOGICAL CHANGES
 Rheology – study of deformation and flow property of liquid and
semisolid; when subjected to stress (homogenization) tend to deform
in shape and flow
 Rheological changes in semisolid increases the consistency due to
increase of the number of emulsified droplets but may decrease
viscosity due to electrolyte effect
 Consistency is also affected by the number of times the preparation
is passed through a homogenizer
3 factors to be controlled during manufacturing:
Time of mixing
Temperature
Mechanical works including rate of agitation
Equipment should be automatically controlled as to
regulation on temperature by jacket around tank. Regulation
of mixing time and rate of agitation
STEPS IN MANUFACTURING
 Preparation of oil and aqueous phase
 Mixing of phases
 Cooling of semisolid emulsions
 Homogenization
 Storage while awaiting test
 Transfer of material for packaging

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Semi solids ppt

  • 1. SEMI – SOLIDS Shekinah Faith S. Balindan BSPharmacy 4B
  • 2. Learning Objectives • Uses • Factors Influencing Absorption • Raw Materials For Semisolids • Type Of Vehicle • Factors Which Influence The Choice Of Semisolid Vehicles • Classes Of Semisolid – Usp • Ophthalmic Ointment • Preparation Of Ointment • Semisolids • Manufacture Of Emulsified Semisolid
  • 3. Pharmaceutical dosage form with viscous consistency intended for application on the skin
  • 4. - Vehicle for topically applied drugs - Emollients-soothing or softening's effect on surface tissue - Protective or occlusive dressings on the skin
  • 5. - Partition coefficient of the drug - Moisture and temperature in the environment of the skin - Pathologic injury to the skin Vehicle used
  • 6. PARTITION COEFFICIENT Substance processing both water and lipid solubility are favorable absorbed through the skin
  • 7. MOISTURE AND TEMPERATURE - The moisture balance on the stratum corneum (horny layer of the epidermis) of the skin has been due to the presence of a combination of compounds known as “natural moisturizing factor”.
  • 8. MOISTURE AND TEMPERATURE - The fat in the skin provides a protective film to prevent this factor from being removed from the skin during excessive contact with water as a bathing
  • 9. PATHOLOGIC INJURY TO THE SKIN - Skin penetration has been enhanced by abrasions or stripping the skin of its barrier layer - Skin penetration of the drug substances can be the use of suitable vehicles
  • 10. HYDROCARBONS Petrolatum and mineral oil are perhaps the widely used substance in semisolids next to water Petrolatum – a complex mixture of semisolids containing hydrocarbon alipathic, cyclic, saturated, unsaturated branch and unbranched substance in varying proportions Mineral oil – obtained from petroleum acid. Lower viscosity is more preferred since it is less tacky.
  • 11. HYDROCARON WAXES Employed to increase the viscosity of mineral oil to prevent separation from ointment. Paraffin and ceresin wax
  • 12. OLEAGINOUS SUBSTANCES Vegetable oil such as peanut, almond oil, almond oil, sesame oil and olive oil and glycerides of mixtures of unsaturated fatty acids
  • 13. FATTY ACIDS AND ALCOHOLS Stearic acids – used in water removable creams as an emulsifier to develop a certain consistency in the cream Stearyl alcohol and cetyl alcohol (palmityl alcohol) – used in creams as auxiliary emulsifiers and emollients; in sufficient stearyl alcohol produces a firm cream which maybe softened by cetyl alcohol.
  • 14. EMULSIFIERS - The water soluble soaps (triethanolamine stearate soap) were among the first emulsifiers used for semisolid oil in water emulsions. The viscosity of the cream or emollient prevents coalescence of the emulsified phases and helps to stabilize the emulsion. The interfacial film formed around the dispersed phase globules is generally solid making emulsified preparation more rigid.
  • 15. POLYOLS Glycerin, propylene glycol, sorbitol 70% and the lower molecular weight polyethylene glycols are used as humectants (prevent drying up) and prevent formation of crust on the top of the cream
  • 16. INSOLUBLE POWDERS Insoluble powders must be uniformly dispersed throughout the vehicle to assure homogeneity of the product. The solid must be impalpable to touch. Particles less than 74 microns in size equivalent to the mesh openings in a number 200 mesh sieve of the US standard sieve series are considered impalpable to most people
  • 17. - The vehicle used for semisolid pharmaceutical preparation differs from that used for cosmetics because with a cosmetic, penetration to the skin is not desired. - A well formulated pharmaceutical semisolid should be both effective therapeutically and cosmetically appealing but in major effort must be in medicinal direction
  • 18. - Nature of the skin lesion - Solubility and stability of the drug
  • 19. Hydrocarbon base Adsorption base Water removable base Water soluble base
  • 20. HYDROCARBON BASE Petrolatum and white ointment (petrolatum with 5% beeswax) are typical lipophilic vehicles Petrolatum is the most commonly used in ointment vehicles because of its consistency, bland and neutral characteristics and its ability to spread easily on the skin These vehicle is difficult to wash off and are used as occlusive dressings which produces sensation of warmth because of the normal evaporation of perspiration is inhibited
  • 21. ABSORPTION BASES Hydrophilic mixtures formed by the addition of substances miscible with hydrocarbons and possessing polar groupings such as SO4, sulfonate, carboxyl, hydroxyl or an ether linage. E.g. lanolin, cholesterol, sterols, sorbitan monostearate, sorbitan monooleate
  • 22. ABSORPTION BASES - Mineral oil is added to these bases to reduce tackiness of the base - Cold cream type w/o emulsion belongs to this type of the base. This is a borax-beeswax combination with mineral oil or vegetable oil as the continuous phase. A protective oil film remains on the skin and slow evaporation of water gives the skin a cooling effect.
  • 23. WATER REMOVABLE BASE - They are oil in water emulsions - Upon application and rubbing into the skin, there is little or no visible evidence of its presence - The vanishing cream - o/w emulsion but with absorption base which is w/o emulsion
  • 24. WATER SOLUBLE BASE - Prepared from mixtures of high and low molecular weight polyethylene glycols - Characteristics: • Low molecular weight are liquids; moderately higher molecular are unctuous, high molecular weight are solids • No water is required for their preparation • Combination of high and low molecular weight polyethylene glycols yield products having ointment like consistency which softens or melts when applied to the skin • Have polar group • Also known as greaseless ointment base
  • 25. - Semisolid ophthalmic vehicles frequently contain soft petrolatum, a brand adsorption base or water soluble base - Material used should avoid the eye discomfort and irritation - Should be sterile when used in injure eye
  • 26. Fusion method (anhydrous ointments) – dissolving the active ingredients in the melted fats and waxes or in the vehicle and then mixed with the base. • Melted mass must be mixed while cooling to ensure homogenous distribution of the ingredients
  • 27. PRESERVATION Preservation is evaluated to: - Stability with regard to other components of the formula - Container to be used
  • 28. CHARACTERISTICS OF PRESERVATIVES • Some preservatives becomes inactive in the presence of other ingredients - 5% tween 80 in activates 80% of the total methyl paraben – higher conc. of preservatives is required • Boric acid may be used in ophthalmic preparation
  • 29. ANTIOXIDANTS -Added whenever oxidative deterioration is anticipated. -Choice of antioxidants depends on: Toxicity Irritating potency Compatibility Odor Discoloration Solubility Stability
  • 30.  Aeration should be prevented for stability and consistency in density. This can be done by introducing one phase below the surface of the other liquid or phase and mixing carefully  In filling into tubes, the hopper should be filled with the product to prevent incorporation of air
  • 31. RHEOLOGICAL CHANGES  Rheology – study of deformation and flow property of liquid and semisolid; when subjected to stress (homogenization) tend to deform in shape and flow  Rheological changes in semisolid increases the consistency due to increase of the number of emulsified droplets but may decrease viscosity due to electrolyte effect  Consistency is also affected by the number of times the preparation is passed through a homogenizer
  • 32. 3 factors to be controlled during manufacturing: Time of mixing Temperature Mechanical works including rate of agitation Equipment should be automatically controlled as to regulation on temperature by jacket around tank. Regulation of mixing time and rate of agitation
  • 33. STEPS IN MANUFACTURING  Preparation of oil and aqueous phase  Mixing of phases  Cooling of semisolid emulsions  Homogenization  Storage while awaiting test  Transfer of material for packaging

Editor's Notes

  • #4: A semisolid thing is something that is not really a solid or a liquid. Mayonnaise is an example. Mayonnaise does not hold its shape like a solid but does not flow like a liquid. Normally semisolids are covalent things. Covalent substances get softer and softer until they melt.