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Therapeutic Aerosols
Dr. Basavaraj K. NanjwadeM. Pharm., Ph. D
Department of Pharmaceutics
Faculty of Pharmacy
Omer Al-Mukhtar University
Tobruk, Libya.
E-mail: nanjwadebk@gmail.com
2014/05/18 1
Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobruk, Libya.
CONTENTS
1. Definition and uses, model of operation.
2. Deposition in human respiratory tract.
3. Formulation aspects,
4. Propellants.
5. Packages and containers.
6. Absorption and clearance.
7. Applications.
8. References.
2014/05/18 2
Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobruk, Libya.
Definition and uses
• Aerosols may be defined as disperse phase system, in
which very fine solid particles or liquid droplets get
dispersed in the gas which acts as continuous phase.
Uses:
1. The medicament can be delivered directly to the
affect area such as burnt skin and wound.
2. So it minimises the discomfort caused by mechanical
or manual application
2014/05/18 3
Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobruk, Libya.
Model of operation
• Drugs are generally delivered to the respiratory tract
for the treatment or prophylaxis of airways diseases,
such as bronchial asthma and cystic fibrosis.
• The administration of a drug at its site of action can
result in a rapid onset of activity.
• Additionally, smaller doses can be administered
locally compared to delivery by the oral or parenteral
routes.
• The pulmonary route is also useful where a drug is
poorly absorbed orally.
2014/05/18
Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobruk, Libya.
4
Deposition in human
respiratory tract
• Casts of the upper airways have been constructed in
an attempt to predict aerosol deposition in the lungs.
• Most lung deposition models are based on the
influence of particle size on aerosol deposition.
• Breathing parameters, such as breathing frequency
and tidal volume, play a key role in lung deposition.
2014/05/18 5
Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobruk, Libya.
2014/05/18
Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobruk, Libya.
6
Site of Deposition in human
respiratory tract
Formulation aspects
• The formulation of pharmaceuticals as therapeutic
aerosols is continually increasing.
• Thus antiseptic materials can be sprayed onto abraded
skin with a minimum of discomfort to the patient.
• One product, ethyl chloride, cools sufficiently on
expansion so that when sprayed on the skin, it freezes
the tissue and produces a local anesthesia.
• This procedure is sometimes used in minor surgical
operations.
2014/05/18 7
Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobruk, Libya.
Propellants
• Propellants develops a pressure in the container.
• Compressed gases such as carbon dioxide or nitrogen
and liquified gases like methane or ethane can be
used as propellants.
• These days propellants like trichloro-fluoro-methane,
dichloro-difluoro-methane, dichloro-tetrafluoro-
ethane and difluoro-ethane are used in
pharmaceutical aerosols.
• The medicaments to be propelled may be solid or
liquid.
2014/05/18
Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobruk, Libya.
8
Packages
1. They are used for spray bandages and for
application of drugs meant for topical use.
2. They are used for spray administration of drugs into
various body cavities.
3. They are used for administration of drugs such as
local anesthetics, local antiseptic, local analgesics
and anti-inflammatory drugs.
4. They are used to spray cosmetics preparations such
as perfumes.
5. They are used to spray disinfectants, deodorizers
and air sanitizers.
2014/05/18 9
Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobruk, Libya.
Containers
• The containers are made from metal, glass and plastic.
• Pharmaceutical aerosols may be packaged in tinplated
steel, plastic-coated glass or aluminium containers.
• MDIs (Metered-Dose Inhalers) are generally presented
in aluminium canisters, produced by extrusion to give
seamless containers with a capacity of 10-30 mL.
• Aluminium containers with an internal coating of a
chemically resistant organic material, such as an epoxy
resin, can be used.
2014/05/18
Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobruk, Libya.
10
2014/05/18
Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobruk, Libya.
11
Container
Absorption
• Hydrophilic materials are poorly absorbed through
membrane pores at rates inversely proporational to
molecular size.
• Some drugs, such as sodium cromoglycate, are partly
absorbed by a saturable active transport mechanism.
• The rate of drug absorption, and consequently drug
action, can be influenced by the formulation.
• Prolonged absorption may be achieved using
suspension formulations or novel drug delivery
systems such as liposomes and microspheres.
2014/05/18 12
Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobruk, Libya.
Clearance
• Particles deposited in the ciliated conducting airways
are cleared within 24 hours and ultimately swallowed.
• Insoluble particles penetrating to the alveolar regions,
and which are not solubilized in situ, are removed
more slowly.
• Alveolar macrophages engulf such particles and may
then migrate to the bottom of the mucociliary
escalator, or alternatively particles may be removed
via the lymphatics.
2014/05/18
Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobruk, Libya.
13
Applications
1. The use of aerosols as a dosage form is particularly
important in the administration of drugs via the
respiratory system.
2. In addition to local effects, systemic effects may be
obtained if the drug is absorbed into the bloodstream
from the lungs.
3. Topical preparations are also well suited for
presentation as aerosols.
2014/05/18
Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobruk, Libya.
14
THANK YOUe-mail: nanjwadebk@gmail.com
2014/05/18 15
Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobruk, Libya.

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Therapeutic aerosols

  • 1. Therapeutic Aerosols Dr. Basavaraj K. NanjwadeM. Pharm., Ph. D Department of Pharmaceutics Faculty of Pharmacy Omer Al-Mukhtar University Tobruk, Libya. E-mail: nanjwadebk@gmail.com 2014/05/18 1 Faculty of Pharmacy, Omer Al-Mukhtar University, Tobruk, Libya.
  • 2. CONTENTS 1. Definition and uses, model of operation. 2. Deposition in human respiratory tract. 3. Formulation aspects, 4. Propellants. 5. Packages and containers. 6. Absorption and clearance. 7. Applications. 8. References. 2014/05/18 2 Faculty of Pharmacy, Omer Al-Mukhtar University, Tobruk, Libya.
  • 3. Definition and uses • Aerosols may be defined as disperse phase system, in which very fine solid particles or liquid droplets get dispersed in the gas which acts as continuous phase. Uses: 1. The medicament can be delivered directly to the affect area such as burnt skin and wound. 2. So it minimises the discomfort caused by mechanical or manual application 2014/05/18 3 Faculty of Pharmacy, Omer Al-Mukhtar University, Tobruk, Libya.
  • 4. Model of operation • Drugs are generally delivered to the respiratory tract for the treatment or prophylaxis of airways diseases, such as bronchial asthma and cystic fibrosis. • The administration of a drug at its site of action can result in a rapid onset of activity. • Additionally, smaller doses can be administered locally compared to delivery by the oral or parenteral routes. • The pulmonary route is also useful where a drug is poorly absorbed orally. 2014/05/18 Faculty of Pharmacy, Omer Al-Mukhtar University, Tobruk, Libya. 4
  • 5. Deposition in human respiratory tract • Casts of the upper airways have been constructed in an attempt to predict aerosol deposition in the lungs. • Most lung deposition models are based on the influence of particle size on aerosol deposition. • Breathing parameters, such as breathing frequency and tidal volume, play a key role in lung deposition. 2014/05/18 5 Faculty of Pharmacy, Omer Al-Mukhtar University, Tobruk, Libya.
  • 6. 2014/05/18 Faculty of Pharmacy, Omer Al-Mukhtar University, Tobruk, Libya. 6 Site of Deposition in human respiratory tract
  • 7. Formulation aspects • The formulation of pharmaceuticals as therapeutic aerosols is continually increasing. • Thus antiseptic materials can be sprayed onto abraded skin with a minimum of discomfort to the patient. • One product, ethyl chloride, cools sufficiently on expansion so that when sprayed on the skin, it freezes the tissue and produces a local anesthesia. • This procedure is sometimes used in minor surgical operations. 2014/05/18 7 Faculty of Pharmacy, Omer Al-Mukhtar University, Tobruk, Libya.
  • 8. Propellants • Propellants develops a pressure in the container. • Compressed gases such as carbon dioxide or nitrogen and liquified gases like methane or ethane can be used as propellants. • These days propellants like trichloro-fluoro-methane, dichloro-difluoro-methane, dichloro-tetrafluoro- ethane and difluoro-ethane are used in pharmaceutical aerosols. • The medicaments to be propelled may be solid or liquid. 2014/05/18 Faculty of Pharmacy, Omer Al-Mukhtar University, Tobruk, Libya. 8
  • 9. Packages 1. They are used for spray bandages and for application of drugs meant for topical use. 2. They are used for spray administration of drugs into various body cavities. 3. They are used for administration of drugs such as local anesthetics, local antiseptic, local analgesics and anti-inflammatory drugs. 4. They are used to spray cosmetics preparations such as perfumes. 5. They are used to spray disinfectants, deodorizers and air sanitizers. 2014/05/18 9 Faculty of Pharmacy, Omer Al-Mukhtar University, Tobruk, Libya.
  • 10. Containers • The containers are made from metal, glass and plastic. • Pharmaceutical aerosols may be packaged in tinplated steel, plastic-coated glass or aluminium containers. • MDIs (Metered-Dose Inhalers) are generally presented in aluminium canisters, produced by extrusion to give seamless containers with a capacity of 10-30 mL. • Aluminium containers with an internal coating of a chemically resistant organic material, such as an epoxy resin, can be used. 2014/05/18 Faculty of Pharmacy, Omer Al-Mukhtar University, Tobruk, Libya. 10
  • 11. 2014/05/18 Faculty of Pharmacy, Omer Al-Mukhtar University, Tobruk, Libya. 11 Container
  • 12. Absorption • Hydrophilic materials are poorly absorbed through membrane pores at rates inversely proporational to molecular size. • Some drugs, such as sodium cromoglycate, are partly absorbed by a saturable active transport mechanism. • The rate of drug absorption, and consequently drug action, can be influenced by the formulation. • Prolonged absorption may be achieved using suspension formulations or novel drug delivery systems such as liposomes and microspheres. 2014/05/18 12 Faculty of Pharmacy, Omer Al-Mukhtar University, Tobruk, Libya.
  • 13. Clearance • Particles deposited in the ciliated conducting airways are cleared within 24 hours and ultimately swallowed. • Insoluble particles penetrating to the alveolar regions, and which are not solubilized in situ, are removed more slowly. • Alveolar macrophages engulf such particles and may then migrate to the bottom of the mucociliary escalator, or alternatively particles may be removed via the lymphatics. 2014/05/18 Faculty of Pharmacy, Omer Al-Mukhtar University, Tobruk, Libya. 13
  • 14. Applications 1. The use of aerosols as a dosage form is particularly important in the administration of drugs via the respiratory system. 2. In addition to local effects, systemic effects may be obtained if the drug is absorbed into the bloodstream from the lungs. 3. Topical preparations are also well suited for presentation as aerosols. 2014/05/18 Faculty of Pharmacy, Omer Al-Mukhtar University, Tobruk, Libya. 14
  • 15. THANK YOUe-mail: nanjwadebk@gmail.com 2014/05/18 15 Faculty of Pharmacy, Omer Al-Mukhtar University, Tobruk, Libya.