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 Aerosols are pressurized dosage forms containing one or more


active drug dissolved, suspended, or emulsified in a propellant or
a mixture of solvent and propellant, which is released on actuation
of the valve as a fine dispersion of liquid or solid in a gaseous
medium.

 Used for either topical, oral or nasal administration in the form


fine particles or mist or fog.

 Mainly used for the treatment of Asthma and COPD disease

 Designed to expel their contents as a fine mist, a coarse wet or


dry spray, a steady stream or a stable or fast breaking foam.
ADVANTAGES

       


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TYPES OF AEROSOL SPRAY

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º Space sprays

 ?hese products are delivered as a fine mist.


 It contains not more than 50 ȝm of particle.
eg. Room sprays

 Surface coating spray

 Aerosols intended for carrying active ingredients to surface are


termed as surface sprays or surface coating spray.
eg. ?opical Aerosol

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|OMPONENT OF AEROSOL

Aerosol consist of

1. Product concentrate

2. Propellant

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consist of API, additives like suspending
agent , emulsifying agent,antioxidant, aqeous and non aqueous
sovents, cosolvent etc«
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 It is responsible for developing the vapour pressure


with in the container and also expel the product when
the valve is opened and aids in the atomization or foam
production of the product.

It is classified in to mainly two types

º Liquified gas system

a) Flourinated hydrocarbon(FH|)
b) Hydrocarbons (H|)

 |ompressed gas system ² eg |   


 FH| find widespread use in aerosols for oral and inhalation use
 H| and compressed gas find widespread use in aerosols for topical
use
Liquified gas system

 ?hese compounds are gases at room temperature and atmospheric pressure


.However they can be liquified easily by lowering the temperature (below the
boiling point or by increasing pressure )

?hese compounds are chosen generally have B.Pt below Ú R and vapour
pressure between 14 and 85 psia at Ú R.

ïhen it is placed into sealed container it immediately separartes


into a liquid and a vapour phase

 

  



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R  Chemically stable
  Inflammable
 mow toxicity
 mow inhalation toxicity  ?hey are lighter than
 High chemical stability water
 High purity  c 


 

  High chemical stability
 High purity
 Destructive to  Inexpensive
atmospheric Ozone  No environmental
 High cost problems
 Produce course droplet
sprays
 Pressure falls during use
 
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(b/w portion of liqified propllent and which


vaporizes and occupies the upper portion
of aerosol container)

        



    
  
     

 
  
     

 
  
    

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Containers must withstand pressure as high as 140 to 180 psig
  


  

(a) Side-seam (three pieces)
(b) ?wo-piece or drawn
(c) ?in free steel


 


(a) ?wo-piece
(b) One-piece (extruded or drawn)







 

1. Uncoated glass
2. Plastic coated glass

 
?ypes of containers:



 
 
 
 Sheet of steel plate that has been electroplated on both sides with tin.
 ïelded side seam are done using 2 processes:   


   


 

 
 
 reater resistance to corrosion
 might weight, not fragile
 ood for light sensitive drugs





 
 
 mimited for smaller size
 Extremely strong and resistant to most materials


 
 
 
 Available with plastic or without plastic coating
 Compatible with many additives
 No corrosion problems
 Can have various shape because of molding
 Fragile
 Not for light sensitive drugs
|OMPONENT OF AEROSOLS

 Actuator
 Ferrule or mounting cup
 Valve body or housing
 Stem
 asket
 Spring
 Dip tube
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Actuators:

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 Spray Actuators
 Foam Actuators
 Solid Stream Actuators
 Special Actuators
FERRULE/ mounting cup
 It is used to attach the valve in proper position to the container.
 Made from tin-plate steel although aluminium also can be used.
 ?o increase resistance to corrosion a single or double epoxy or
vinyl coating can be added.

Valve body / housing


 ?he part of the valve which holds the stem, gasket and spring in
place and to which the dip tube is attached.
 It is made of    
 and contains an opening at the point
of attachment of the diptube which ranges from 0.013 to 0.080
inch.
 ?he housing may or may not contain another opening ±  

 Produce fine particle size
 Prevents valve clogging with products containing insoluble
materials
 Reduce the chilling effect of propllent on skin
Stem:
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Gasket :
 It is made of Buna ±N, Neoprene rubber


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 It is used to hold the gasket in a place and when actuator is
depressed and released, it returns the valve to its closed position
 It is made of stainless steel




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 It is made up of poly propylene material / poly ethylene
 Inside diameter (0.120 ± 0.125 inch) for capillary tubes -0.050
inch and Viscous product - 0.195
? PES OF AEROSOm S S?EM

 Solution system / ?wo phase system

 ïater based system / ?hree phase system

 Suspension or Dispersion system

 Foam system
Solution system / Two phase system
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Liquid phase 1  2  3   


Vapor phase

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A layer of water- immisible liquid propellent
A layer of highly aqueous product concentrate
A vapour phase

          


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A |ontrol of moisture content- must be below - ppm
A Use of derivatives of AI having minimum solubility in propellent
A Reduction of initial particle size to less than 5microns
A Adustment of density difference
A Use of surfactants (HLB < º  º ² º %)
Foam system

  2  2     


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Stable foam

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†uick breaking foam

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 Cold filling apparatus

 Pressure filling apparatus

 Compressed gas filling apparatus


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 Pressure filling is carried out at R T under high pressure

 The apparatus consists of a pressure burette capable of metering small


volumes of liquefied gas under pressure into an aerosol container

 The propellant is added through the inlet valve located at the


bottom or top of the burette

 The desired amount of propellant is allowed to flow through the


aerosol valve into the container under its own vapor pressure

hen the pressure is equalized between the burette and the


container (thus happens with low pressure propellant), the
propellant stops flowing

 To help in adding additional propellant, a hose leading to a


cylinder of nitrogen or compressed is attached to the upper valve
and the added nitrogen pressure causes the propellant to flow
Pressure filling apparatus
ADVAN?AES

It is the preferred method for solutions, emulsions and


suspension.

mess chances for contamination of product


with the moisture.

mess propellant is lost

No refrigeration is required, can be carried out at R?


 
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 ?he principle of cold filling method requires the chilling


of all components including concentrate and propellant
to a temperature of -30 to -40 º F.

 ?his temprature is necessary to liquify the propellant


gas.

 ?he cooling system may be a mixture of dry ice and


acetone or refergiration system.

 First, the product concentrate is chilled and filled into


already chilled container followed by the chilled liquefied
propellant.
Cold filling apparatus


 Easy process




 Aqueous products, emulsions and those products


adversely affected by cold temperature cannot be filled
by this method.

 For nonaqueous systems, some moisture usually


appear in the final product due to condensation of
atmospheric presure
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 Compressed gases are present under high pressure in
cylinders. ?hese cylinders are fitted with a pressure reducing
valve and a delivery gauge.
 ? he concentrate is placed in the container
 ?he valve is crimped in place
 Air is evacuated by means of vacuum pump

?he filling head is inserted into the valve opening, valve


depressed and gas is allowed to flow into the container

 For those products requiring an increased amount of gas or


those in which the solubility of gas in the product is necessary,
carbon dioxide and nitrous oxide can be used.

 ?o obtain maximum solubility of the gas in the product, the


container is shaken manually during and after the filling
operation by mechanical shakers.
 


 

 

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 Flame extension
 Flash point


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 Vapour pressure
 Density
 Moisture content
 Identification of propellant(s)


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 Aerosol valve discharge rate
 Spray pattern
 Dosage with metered valves
 Net contents
 Foam stability
 Particle size determination





 



  




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 ?his test indicates the effect of


an aerosol formulation on the
extension of an open flame.

 Product is sprayed for 4 sec.


into flame.

 Depending on the nature of


formulation, the flame is extended,
and exact length was measured
with ruler.
FmASH POIN?

 Determined by using 



 

 

PROCEDURE:
 Aerosol product is chilled to temperature of - 25 0 F and
transferred to the test apparatus.

 ?emperature of test liquid increased slowly, and the


temperature at which the vapors ignite is taken a flash point.

 Calculated for flammable component, which in case of


topical hydrocarbons
 
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 ?o determine pressure variation from container to


container.

 Determined by pressure gauge or Can puncturing


device.

 Variation in pressure indicates the presence of air in


headspace.
MEASUREMEN? OF DENSI?

 Determined by    


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Procedure:
 A pressure tube is fitted with metal fingers and
hoke valve, which allow for the introduction of
liquids under pressure.
 ?he hydrometer is placed in to the glass
pressure tube.
 Sufficient sample is introduced through the
valve to cause the hydrometer to rise half way up
the length of the tube.
 ?he density can be read directly.
  
 

 
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 as Chromatography

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 as Chromatography
 I.R spectrophotometry

 
  


Expressed as gram per seconds.

 Determined by taking an aerosol known weight and discharging


the contents for given time using standard apparatus.

 By reweighing the container after time limit has expired, the


change in weight per time dispensed is discharge rate.

Spray pattern

 Spray the product on the coated (dye +talc ) paper.

 Depending upon the nature of aerosol water /oil soluble dye is


used.
Dosage with metered valves

   




 




 


  

  

 


 
 
 





NE? CON?EN?

ïeight of empty container = gm


ïeight of the filled container = gm
net content

FOAM S?ABImI? :
 Visual evaluation
 ?ime for a given mass to penetrate the foam
 Rotational viscometer
Particle size
 cascade impactor
    

 
     

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