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COMPONENTS FOR AEROSOL
FORMULATION
Presented by- Moriyom Akhter
World University of Bangladesh
Aerosols
Aerosol are the products that depend on the power
of a compressed or liquefied gas to expel the
contents from the container. Aerosols are termed
also pressurized package.
Pharmaceutical aerosols:
Aerosol products containing therapeutically active
ingredients dissolved, suspended or emulsified in a
propellant or a mixture of solvent and propellant and
intended for topical administration, for administration into
one of the body cavities (ear, rectum and vagina) or
intended for administration orally or nasally as fine solid
particles or liquid mists through the pulmonary airways,
nasal passages or oral cavity.
Aerosol
Components of aerosols:
Propellant
Container
Valve and actuator
Product concentrate
PROPELLANTS
A propellant is a chemical with a vapor pressure
greater than atmospheric pressure at 40°C (105°F).

Function:
1) It is responsible for developing the vapor pressure
2)
3)

within the container
Expel the product when the valve is opened and in the
atomization or foam production of the product.
When the propellant is a liquefied gas or a mixture of
liquefied gases, it can also serve as the solvent or
vehicle for the product concentrate.
Types:

1. Compressed Gas

Propellants

Inert gases

Hydrocarbons(HC)
2. Liquefied gas
propellants

Chloroflourocarbon
(CFC)

Fluorinated
hydrocarbons(FHC)
Ethers

Carbon Dioxide
Nitrous Oxide
Nitrogen
Liquefied Petroleum
Gases(Propane,
Isobutane, n-Butane)
Isopentane, n-Pentane.
Trichloro-mono-flouro
methane (11), Dichloro-diflouromethane (12) , Dichloro-tetra-flouromethane (114)
1,1 Diflouroethane
(152a)
Dimethyl ether
Propellants
Compressed Gas Propellants


Gases such as nitrogen, nitrous oxide, and carbon dioxide have been used
as aerosol propellants for products dispensed as fine mists, foams, or
semisolids. Compressed gas propellants only occupy the head space
above the liquid in the can. When the aerosol valve is opened the gas
'pushes' the liquid out of the can. The amount of gas in the headspace
remains the same but it has more space, and as a result the pressure will
drop during the life of the can.

Liquefied gas


Liquefied propellants are gases that exist as liquids under pressure.
Because the aerosol is under pressure the propellant exists mainly as a
liquid, but it will also be in the head space as a gas. As the product is used
up as the valve is opened, some of the liquid propellant turns to gas and
keeps the head space full of gas.
Compressed gas propellants
Advantages

Low inhalation toxicity

High chemical stability

High purity

Inexpensive

No environmental problem
Disadvantages

Require use of a nonvolatile
co-solvent

Produce course droplet sprays

Pressure falls during use
Liquefied gas propellants
Hydrocarbons



It is mainly used for the preparation of topical preparation, chemically
stable, no hydrolysis, Inflammable , low toxicity.
They are lighter than water.

Chlorofluorocarbon (CFC) propellants
P-11, P-12, and P-114 are the CFCs of
choice for oral, nasal,
and inhalation aerosols.






Advantages
Low inhalation toxicity
High chemical stability
High purity
CFC-11 is a good solvent
Liquefied gas propellants
Hydrochlorofluorocarbons (HCFC) and Hydrofluorocarbons (HFC)
The hydrochlorofluorocarbons (HCFC) and hydrofluorocarbons (HFC) differ
from CFCs in that they may not contain chlorine and have one or more
hydrogen atoms. P-22, 142b, and 152a are used in topical pharmaceuticals.
These three propellants have a greater miscibility with water and therefore
are more useful as solvents. They are also slightly more flammable than the
other propellants.

Ether
Di Methyl Ether - This is an alternative liquefied propellant, and is more
common in personal care products, and some air fresheners. DME is
significantly higher in price than hydrocarbon propellants. Classified as a
flammable gas. It is a very strong and aggressive solvent. An advantage of
DME is its solubility in and compatibility with aqueous formulas.
Disadvantage of DME is that in aqueous formulas at levels at or above 19%,
the DME will attack the can lining thus requiring a corrosion inhibitor.
Formulation :
Contains two essential components:

Product concentrate : contains ingredients or mixture of active
ingredients and other such as solvents, antioxidants and
surfactants.

Propellant : Propellant May be single or blend of various
propellants
The type of the system
selected depends on many
factors such as

Physical, chemical and
pharmacological properties
of active ingredients
 Site of application
Formulation
Depending on the type of aerosol system utilized, the pharmaceutical
aerosol may be dispensed as a fine mist, wet spray, quick-breaking
foam , stable foam, semisolid or solid.

Type of systems are
1. Solution system :


Consist of a solution of active ingredients in pure propellant or
a mixture of propellant and solvents.
 Easy to formulate, provided that the ingredients are soluble in
the propellant
Aerosol solutions have been used

To make foot preparations

Local anesthetics

Spray on protective films

Anti-inflammatory preparations and

Aerosols for oral and nasal applications
2. Suspension or Dispersion systems
Active ingredients are suspended or dispersed throughout the propellant or
propellant and solvent phase.

Anti-asthmatic drugs, steroids, and antibiotics are delivered as suspension
aerosols. When the valve is actuated, the suspension formulation is emitted
as an aerosol and the propellant rapidly vaporizes and leaves a fine
dispersion of the product concentrate.
 There are some problem arise for suspension aerosols that are include
agglomeration, particle size growth, valve clogging, moisture content, and
particle size of the dispersed aerosolized particles.


To overcome these problems:

lubricants:
isopropyl myristate , oleic acid

Provide slippage between particles

Lubricate components parts of the valve

Surfactants: to disperse particles
3.Water based system ( Emulsion, dispersion ):
Relatively large amounts of water can be used to replace all part or part of the
non aqueous solvents used in aerosol. These products are generally referred to
as water-based aerosols and depending on the formulation are emitted as a
spray or foam.
To produce a spray the formulation must consist of a dispersion of active
ingredients and the solvents in an emulsion system in which the propellants is
external phase.
In this way when the product is dispensed, the propellants vaporizes and
disperses the active ingredients into many particles. Since propellant and water
are not miscible a three phase forms (propellants phase, water phase and
vapor phase) are used. To increase the solubility of propellants in water, ethyl
alcohol can be added to the system. Ethanol has been used as a co solvent to
solubilize some of the propellant in the water.
4. Foam system:




Foams are produced when the product concentrate is dispersed
throughout the propellant and the propellant is in the internal phase; i.e.,
the emulsion behaves like o/w emulsion.
Aqueous stable foams-The techniques used in preparing an aerosol
emulsion are the same as those used for non aerosol emulsions. This is
generally used for steroid antibiotics.



Non-aqueous stable foams-Various medicinal agents can be formulated by
this way.



Quick breaking foams-These type of system is specially applicable to
medication, which can be applied to limited or to large areas without the
use of mechanical force to dispense the active ingredients. Quick
breaking foams aerosol may be formulated by ethyl alcohol, surfactant,
water and hydrocarbon propellant.



Thermal foams - These are used when the warmness is required.
5. Intranasal aerosol:






Drug delivery systems intended for the deposition of the
medication into the nasal passageways has long been used as a
most effective, means of administering drugs intended to produce
either a local action of systemic effect.
The Intranasal aerosol offers numerous disadvantage including the
delivery of a measured dose of drug , excellent depth of
penetration into the nasal passageways with minimal intervertent
penetration into lungs, reduce droplet of particle size , lower
dosage than a comparable system preparation maintenance of
sterility from dose to dose.
The modes of administering of intranasal preparations have been
limited to nasal drops, non-pressurized nasal sprays (mist),
inhalants, intranasal gel, creams, ointments.
Wherever the medicament is needed, there the
product can be delivered in the required form like
foam, spray etc.
It have rapid onset of action. It will act on targeted
area without any contamination.
In conclusion, aerosol dosage form is a dosage form
with an easy administration. It’s main advantage is it
requires lesser amount of active ingredients or
medicaments.
THANK YOU

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Aerosol , components for aerosol formulation by mariomakhter@yahoo.com

  • 1. COMPONENTS FOR AEROSOL FORMULATION Presented by- Moriyom Akhter World University of Bangladesh
  • 2. Aerosols Aerosol are the products that depend on the power of a compressed or liquefied gas to expel the contents from the container. Aerosols are termed also pressurized package. Pharmaceutical aerosols: Aerosol products containing therapeutically active ingredients dissolved, suspended or emulsified in a propellant or a mixture of solvent and propellant and intended for topical administration, for administration into one of the body cavities (ear, rectum and vagina) or intended for administration orally or nasally as fine solid particles or liquid mists through the pulmonary airways, nasal passages or oral cavity.
  • 4. PROPELLANTS A propellant is a chemical with a vapor pressure greater than atmospheric pressure at 40°C (105°F). Function: 1) It is responsible for developing the vapor pressure 2) 3) within the container Expel the product when the valve is opened and in the atomization or foam production of the product. When the propellant is a liquefied gas or a mixture of liquefied gases, it can also serve as the solvent or vehicle for the product concentrate.
  • 5. Types: 1. Compressed Gas Propellants Inert gases Hydrocarbons(HC) 2. Liquefied gas propellants Chloroflourocarbon (CFC) Fluorinated hydrocarbons(FHC) Ethers Carbon Dioxide Nitrous Oxide Nitrogen Liquefied Petroleum Gases(Propane, Isobutane, n-Butane) Isopentane, n-Pentane. Trichloro-mono-flouro methane (11), Dichloro-diflouromethane (12) , Dichloro-tetra-flouromethane (114) 1,1 Diflouroethane (152a) Dimethyl ether
  • 6. Propellants Compressed Gas Propellants  Gases such as nitrogen, nitrous oxide, and carbon dioxide have been used as aerosol propellants for products dispensed as fine mists, foams, or semisolids. Compressed gas propellants only occupy the head space above the liquid in the can. When the aerosol valve is opened the gas 'pushes' the liquid out of the can. The amount of gas in the headspace remains the same but it has more space, and as a result the pressure will drop during the life of the can. Liquefied gas  Liquefied propellants are gases that exist as liquids under pressure. Because the aerosol is under pressure the propellant exists mainly as a liquid, but it will also be in the head space as a gas. As the product is used up as the valve is opened, some of the liquid propellant turns to gas and keeps the head space full of gas.
  • 7.
  • 8. Compressed gas propellants Advantages  Low inhalation toxicity  High chemical stability  High purity  Inexpensive  No environmental problem Disadvantages  Require use of a nonvolatile co-solvent  Produce course droplet sprays  Pressure falls during use
  • 9. Liquefied gas propellants Hydrocarbons  It is mainly used for the preparation of topical preparation, chemically stable, no hydrolysis, Inflammable , low toxicity. They are lighter than water. Chlorofluorocarbon (CFC) propellants P-11, P-12, and P-114 are the CFCs of choice for oral, nasal, and inhalation aerosols.     Advantages Low inhalation toxicity High chemical stability High purity CFC-11 is a good solvent
  • 10. Liquefied gas propellants Hydrochlorofluorocarbons (HCFC) and Hydrofluorocarbons (HFC) The hydrochlorofluorocarbons (HCFC) and hydrofluorocarbons (HFC) differ from CFCs in that they may not contain chlorine and have one or more hydrogen atoms. P-22, 142b, and 152a are used in topical pharmaceuticals. These three propellants have a greater miscibility with water and therefore are more useful as solvents. They are also slightly more flammable than the other propellants. Ether Di Methyl Ether - This is an alternative liquefied propellant, and is more common in personal care products, and some air fresheners. DME is significantly higher in price than hydrocarbon propellants. Classified as a flammable gas. It is a very strong and aggressive solvent. An advantage of DME is its solubility in and compatibility with aqueous formulas. Disadvantage of DME is that in aqueous formulas at levels at or above 19%, the DME will attack the can lining thus requiring a corrosion inhibitor.
  • 11. Formulation : Contains two essential components:  Product concentrate : contains ingredients or mixture of active ingredients and other such as solvents, antioxidants and surfactants.  Propellant : Propellant May be single or blend of various propellants The type of the system selected depends on many factors such as  Physical, chemical and pharmacological properties of active ingredients  Site of application
  • 12. Formulation Depending on the type of aerosol system utilized, the pharmaceutical aerosol may be dispensed as a fine mist, wet spray, quick-breaking foam , stable foam, semisolid or solid. Type of systems are 1. Solution system :  Consist of a solution of active ingredients in pure propellant or a mixture of propellant and solvents.  Easy to formulate, provided that the ingredients are soluble in the propellant Aerosol solutions have been used  To make foot preparations  Local anesthetics  Spray on protective films  Anti-inflammatory preparations and  Aerosols for oral and nasal applications
  • 13. 2. Suspension or Dispersion systems Active ingredients are suspended or dispersed throughout the propellant or propellant and solvent phase.  Anti-asthmatic drugs, steroids, and antibiotics are delivered as suspension aerosols. When the valve is actuated, the suspension formulation is emitted as an aerosol and the propellant rapidly vaporizes and leaves a fine dispersion of the product concentrate.  There are some problem arise for suspension aerosols that are include agglomeration, particle size growth, valve clogging, moisture content, and particle size of the dispersed aerosolized particles.  To overcome these problems:  lubricants: isopropyl myristate , oleic acid  Provide slippage between particles  Lubricate components parts of the valve  Surfactants: to disperse particles
  • 14. 3.Water based system ( Emulsion, dispersion ): Relatively large amounts of water can be used to replace all part or part of the non aqueous solvents used in aerosol. These products are generally referred to as water-based aerosols and depending on the formulation are emitted as a spray or foam. To produce a spray the formulation must consist of a dispersion of active ingredients and the solvents in an emulsion system in which the propellants is external phase. In this way when the product is dispensed, the propellants vaporizes and disperses the active ingredients into many particles. Since propellant and water are not miscible a three phase forms (propellants phase, water phase and vapor phase) are used. To increase the solubility of propellants in water, ethyl alcohol can be added to the system. Ethanol has been used as a co solvent to solubilize some of the propellant in the water.
  • 15. 4. Foam system:   Foams are produced when the product concentrate is dispersed throughout the propellant and the propellant is in the internal phase; i.e., the emulsion behaves like o/w emulsion. Aqueous stable foams-The techniques used in preparing an aerosol emulsion are the same as those used for non aerosol emulsions. This is generally used for steroid antibiotics.  Non-aqueous stable foams-Various medicinal agents can be formulated by this way.  Quick breaking foams-These type of system is specially applicable to medication, which can be applied to limited or to large areas without the use of mechanical force to dispense the active ingredients. Quick breaking foams aerosol may be formulated by ethyl alcohol, surfactant, water and hydrocarbon propellant.  Thermal foams - These are used when the warmness is required.
  • 16. 5. Intranasal aerosol:    Drug delivery systems intended for the deposition of the medication into the nasal passageways has long been used as a most effective, means of administering drugs intended to produce either a local action of systemic effect. The Intranasal aerosol offers numerous disadvantage including the delivery of a measured dose of drug , excellent depth of penetration into the nasal passageways with minimal intervertent penetration into lungs, reduce droplet of particle size , lower dosage than a comparable system preparation maintenance of sterility from dose to dose. The modes of administering of intranasal preparations have been limited to nasal drops, non-pressurized nasal sprays (mist), inhalants, intranasal gel, creams, ointments.
  • 17. Wherever the medicament is needed, there the product can be delivered in the required form like foam, spray etc. It have rapid onset of action. It will act on targeted area without any contamination. In conclusion, aerosol dosage form is a dosage form with an easy administration. It’s main advantage is it requires lesser amount of active ingredients or medicaments.