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TOPICAL AGENT
SUBMITTED BY: SAKSHI UPADHYAY
MPT 1ST SEM
DEFINITION
• The topical agents are those substances, which applied to body surface including applications
within the body cavities that open outside (e.g. the oral vaginal).
• These are the compound that act locally with skin or mucous membrane mainly by mechanical
or physical manner.
• Topical agents does not absorbed directly into the circulation.
• Compounds have little pharmacological effect.
• The facts of compounds are that when they are applied produces variety of effects like
adsorbent, astringent, demulcent , emollient or protective.
CLASSIFICATION
Protectives and
adsorbents
E.g. Talc
Silicone polymers
Titanium dioxide
Calamine
Zinc oxide.
Antimicrobial
agents
1.Hydrogen peroxide, Potassium
permanganate, Sodium per borate.
2.Iodine & iodine preparations,
Chlorinated lime, sodium hypochlorite
solution.
3.E.g. Boric acid, Borax, Silver & Silver
compounds, Mercury compounds.
Astringents
E.g. Zinc chloride, Zinc
sulphate, Aluminium
sulphate, Alum,
Aluminum sub acetate
solution.
Miscellaneous
compounds
E.g. sulphur & sulphur
compounds
PROTECTIVE'S AND ADSORBENTS
• Protective's are the agents that cover the skin or mucous membrane from possible
irritants.
MOA
• Some substance are of insoluble type & chemically inert, they act by forming a coat or
film on the skin.
• They absorb moisture decreases mechanical friction and irritation and also
discourages certain bacterial growth.
• Dusting powder is in the state of fine division form adherent continuous film on intact
skin & exhibit protective action.
ADSORBENTS
• Some chemically inert substances adsorb dissolved or suspended particles or gases, toxins etc.
are known as adsorbents.
MOA
• They are mainly used internally to prevent the irritant & unwanted effects on mucous
membrane.
• Some inorganic chemicals possesses both protective & adsorbent properties on topical
application.
• Protective action is generally nothing but the mechanical protection which is given from the
external environment by forming a film coat or layer on the skin.
SOME OF THE INORGANIC PROTECTIVE COMPOUNDS AND
PREPARATIONS ARE DESCRIBED HERE:
TALC
• Chemical formula :- 3Mgo. 4siO2.H20
• Synonym:- soapstone or French chalk, purified talc
 Talc is the softest material Properties:-
• Colour: White/greyish white
• Odour:-odourless.
• Nature:-fine powder
• Taste:-tasteless
• Touch:-greasy or unctuous & adheres to skin
• Solubility:-soluble in water, dil. acids & bases 9
• Storage:- In well closed container.
• PREPARATION
1. Prepared by boiling fine powered talc with Dil HCL & allowing to settle.
2. The supernatant liquid is removed
3. The talc is washed thoroughly with water to make it free from acid.
(Acid treatment remove impurities from talc.)
• USES
1. As pharmaceutical aid
2. Dusting powder.
3. It can be perfumed that is cosmetic or medicated with zinc oxide or boric acid.
4. It is greasy / untouched to touch therefore used as lubricant or protective.
5. It is used as excipient, lubricant& filler for tablet & pills
ZINC OXIDE
• Chemical formula:-ZnO
• Mol wt. : 81.38
Properties:-
• Colour: White/yellowish white
• Odour:- Odourless.
• Nature:-fine amorphous powder
• Solubility:-Insoluble in water & alcohol soluble in NH3
• PREPARATION
1. Commercially ZnO is obtained by heating metallic zinc in a current of air at
higher temperature the metal burns into oxides which is collected as fine white
powder.
2Zn + O2 2ZnO
2. Medicinal grade ZnO is obtained from zinc sulphate by double decomposition
sulphate is added to a boiling sol of sodium carbonate collected washed until free
from sulphate dried & ignited.
ZnSO4 + Na2CO3 ZnCO3 + Na2SO4
ZnCO3 ZnO + CO213
• ASSAY
ZnO is insoluble in water therefore cannot directly titrated with acid.
It is dissolved in excessive of acid & back titrated.
Ammonium chloride is used in titration to prevent ppt
White ppt interferes in end point
Methyl orange is used as an indicator
ZnO + H2SO4 ZnSO4 + H2O
H2SO4 ( Excess) + 2NaOH Na2SO4+ 2H2O 14
• USES
1. Mild Antiseptic & Astringent. in form of lotions, ointment paste or dusting
powder.
2. In treatment of urticaria, eczema, sunburns
3. In combinations with other antimicrobial agents E.g. Talc
4. Primary ingredient in calamine.
5. Pharmaceutical aid in mfg. of adhesive tapes, bandages.
6. It is used in the treatment of eczema, ring worm, pruritus and psoriasis.
CALAMINE
• Chemical formula:- ZnC03.Zn(OH)2·xFe2O3
• STD:- After ignition, it contains not less than 98.0% and not more than 100.5% of ZnO.
Properties
• Colour: pink or reddish brown powder
• Odour:-odourless.
• Nature:-fine powder & amorphous
• Taste :- tasteless
• Solubility:-Practically insoluble in water, almost completely soluble in
mineral acids with effervescence.
• NOTE The presence of ferric oxide gives the substance a pink colour
(for cosmetic reasons)
• Preparation
1. Calamine is obtained by calcination( powdered by heating) of the natural native zinc
carbonate.
2. Prepared by mixing zinc oxide with ferric oxide
3. Sieved & fine powder is collected.
• Assay
1. An ignited & cooled sample is dissolved in excess acid H2SO4 (1 N) & filter.
2. Residue washed with hot water to free from acidity.
3. Ammonium Chloride is added to prevent ppt of ferric hydroxide during titration) &
titrated with NaOH (1N) using methyl orange as indicator. 17
• USES
1. Topical protective
2. It is used in dusting powders, ointments and lotions (Calamine Lotion) is
applied on the skin for its soothing, adsorbent and protective properties.
3. It has better cosmetic acceptability than zinc oxide.
4. Various dermatological conditions including the exudation of fluids respond
reasonably well to calamine.
5. Mild astringent, antiseptic & protective for skin.
6. Phenolated calamine lotion contain 1% liquefied phenol which provides local
anesthetic antiseptic & antipruritic
ZINC STEARATE
• Chemical formula:- CH3 (CH2)16CO2) 2 Zn
• STD:- After ignition, it contains not less than12.5% and
not more than 14.0% of ZnO.
• Properties
1. Colour: White
2. Odour:-faint characteristic.
3. Nature:- light fine bulky powder free from grittiness
4. Taste :- tasteless
5. Solubility:-. practically soluble in water, alcohol & ether
Chemical Properties :- 1)Hydrolysed by heating in dil mineral acid to
form a soluble Zinc stearate 2)moistened to litmus paper.
ASSAY
1. Analyzed by complexometric method.
2. An ignited & cooled sample is dissolved in excess acid H2SO4 (1 N) by boiling.
3. Residue washed with water to free from acidity.
4. Combined the filtrate & titrated against disodium EDTA solution using ammonia, ammonium
chloride buffer &urochrome black T as an indicator.
USES
1. Astringent & Antimicrobial.
2. Soothing& protective agent & used in dusting powder ointment creams in treatment of
inflammatory condition.
3. Used in skin problems where large amount of water is exuded because it will not form
patches.
4. Used as lubricant in the processing of tablets.
NOTE:-causes pulmonary inflammation if inhaled .
TANIUM DIOXIDE
• Chemical formula:- TiO2 2) Mol. Wt. :-79.90
• STD:-It contains not less than 98% of TiO2 W.R.T.
to dried substance
• Properties
1. Colour: White
2. Odour:-odourless.
3. Nature:-Amorphous & fluffy powder
4. Taste :- tasteless
5. Solubility:-. practically soluble in water, & in dil mineral
acid it dissolves slowly in Hot H2SO4.22
• ASSAY
1. It is analysed by complex metric titration.
2. Sodium edetate back titration method.
3. Sample is dissolved in hot H2SO4 using ammonium sulphate with definite volume.
H2O2,strong ammonia solution, Hexamine buffer& excess disodium EDTA is added &
excess is back titrated.
• Storage:- Store in well closed container
• Uses
1. Topical preparation due to its opacity nature.
2. Due to its opacity nature it is used for screening out the UV radiations in various sun
creams & sunscreen product to prevent sunburn.
3. Due to its white color it is used in cosmetic preparation & in paints.
SILICON POLYMERS
• Synonyms:-Dimethicone, Simethicone, Dimethicone, polysiloxne , silicone oils.
• Properties & uses of Silicones
1. The silicone polymers are generally known as silicone oils.
2. The silicone polymers are prepared synthetically by polymerization reaction.
3. The oily nature of these compounds makes it useful as water repellent and protective to skin
from contact irritants.
4. The silicone oils, thus in general act as protective, it also act as an Antiflatulents and used in
varying amount in antacid preparations
• Dimethicone
1. It is an inert silicone, oily in nature, it is stable and has low surface tension.
2. It forms a protective layer on skin like plastic and acts as water protective agent.
3. It is mainly used in ointments, sprays, lotions and creams.
• Simethicone :
1. It occurs as a light gray, translucent liquid with greasy consistency.
2. It is prepared from dimethylpolysiloxane.
3. It is used as an Antiflatulents and is employed in antacid, antispasmodic, sedative
and digestant preparations in 40 - 80 mg dose at bed time
TOPICAL AGENT.pptx

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TOPICAL AGENT.pptx

  • 1. TOPICAL AGENT SUBMITTED BY: SAKSHI UPADHYAY MPT 1ST SEM
  • 2. DEFINITION • The topical agents are those substances, which applied to body surface including applications within the body cavities that open outside (e.g. the oral vaginal). • These are the compound that act locally with skin or mucous membrane mainly by mechanical or physical manner. • Topical agents does not absorbed directly into the circulation. • Compounds have little pharmacological effect. • The facts of compounds are that when they are applied produces variety of effects like adsorbent, astringent, demulcent , emollient or protective.
  • 3. CLASSIFICATION Protectives and adsorbents E.g. Talc Silicone polymers Titanium dioxide Calamine Zinc oxide. Antimicrobial agents 1.Hydrogen peroxide, Potassium permanganate, Sodium per borate. 2.Iodine & iodine preparations, Chlorinated lime, sodium hypochlorite solution. 3.E.g. Boric acid, Borax, Silver & Silver compounds, Mercury compounds. Astringents E.g. Zinc chloride, Zinc sulphate, Aluminium sulphate, Alum, Aluminum sub acetate solution. Miscellaneous compounds E.g. sulphur & sulphur compounds
  • 4. PROTECTIVE'S AND ADSORBENTS • Protective's are the agents that cover the skin or mucous membrane from possible irritants. MOA • Some substance are of insoluble type & chemically inert, they act by forming a coat or film on the skin. • They absorb moisture decreases mechanical friction and irritation and also discourages certain bacterial growth. • Dusting powder is in the state of fine division form adherent continuous film on intact skin & exhibit protective action.
  • 5. ADSORBENTS • Some chemically inert substances adsorb dissolved or suspended particles or gases, toxins etc. are known as adsorbents. MOA • They are mainly used internally to prevent the irritant & unwanted effects on mucous membrane. • Some inorganic chemicals possesses both protective & adsorbent properties on topical application. • Protective action is generally nothing but the mechanical protection which is given from the external environment by forming a film coat or layer on the skin.
  • 6. SOME OF THE INORGANIC PROTECTIVE COMPOUNDS AND PREPARATIONS ARE DESCRIBED HERE: TALC • Chemical formula :- 3Mgo. 4siO2.H20 • Synonym:- soapstone or French chalk, purified talc  Talc is the softest material Properties:- • Colour: White/greyish white • Odour:-odourless. • Nature:-fine powder • Taste:-tasteless • Touch:-greasy or unctuous & adheres to skin • Solubility:-soluble in water, dil. acids & bases 9 • Storage:- In well closed container.
  • 7. • PREPARATION 1. Prepared by boiling fine powered talc with Dil HCL & allowing to settle. 2. The supernatant liquid is removed 3. The talc is washed thoroughly with water to make it free from acid. (Acid treatment remove impurities from talc.) • USES 1. As pharmaceutical aid 2. Dusting powder. 3. It can be perfumed that is cosmetic or medicated with zinc oxide or boric acid. 4. It is greasy / untouched to touch therefore used as lubricant or protective. 5. It is used as excipient, lubricant& filler for tablet & pills
  • 8. ZINC OXIDE • Chemical formula:-ZnO • Mol wt. : 81.38 Properties:- • Colour: White/yellowish white • Odour:- Odourless. • Nature:-fine amorphous powder • Solubility:-Insoluble in water & alcohol soluble in NH3
  • 9. • PREPARATION 1. Commercially ZnO is obtained by heating metallic zinc in a current of air at higher temperature the metal burns into oxides which is collected as fine white powder. 2Zn + O2 2ZnO 2. Medicinal grade ZnO is obtained from zinc sulphate by double decomposition sulphate is added to a boiling sol of sodium carbonate collected washed until free from sulphate dried & ignited. ZnSO4 + Na2CO3 ZnCO3 + Na2SO4 ZnCO3 ZnO + CO213
  • 10. • ASSAY ZnO is insoluble in water therefore cannot directly titrated with acid. It is dissolved in excessive of acid & back titrated. Ammonium chloride is used in titration to prevent ppt White ppt interferes in end point Methyl orange is used as an indicator ZnO + H2SO4 ZnSO4 + H2O H2SO4 ( Excess) + 2NaOH Na2SO4+ 2H2O 14
  • 11. • USES 1. Mild Antiseptic & Astringent. in form of lotions, ointment paste or dusting powder. 2. In treatment of urticaria, eczema, sunburns 3. In combinations with other antimicrobial agents E.g. Talc 4. Primary ingredient in calamine. 5. Pharmaceutical aid in mfg. of adhesive tapes, bandages. 6. It is used in the treatment of eczema, ring worm, pruritus and psoriasis.
  • 12. CALAMINE • Chemical formula:- ZnC03.Zn(OH)2·xFe2O3 • STD:- After ignition, it contains not less than 98.0% and not more than 100.5% of ZnO. Properties • Colour: pink or reddish brown powder • Odour:-odourless. • Nature:-fine powder & amorphous • Taste :- tasteless • Solubility:-Practically insoluble in water, almost completely soluble in mineral acids with effervescence. • NOTE The presence of ferric oxide gives the substance a pink colour (for cosmetic reasons)
  • 13. • Preparation 1. Calamine is obtained by calcination( powdered by heating) of the natural native zinc carbonate. 2. Prepared by mixing zinc oxide with ferric oxide 3. Sieved & fine powder is collected. • Assay 1. An ignited & cooled sample is dissolved in excess acid H2SO4 (1 N) & filter. 2. Residue washed with hot water to free from acidity. 3. Ammonium Chloride is added to prevent ppt of ferric hydroxide during titration) & titrated with NaOH (1N) using methyl orange as indicator. 17
  • 14. • USES 1. Topical protective 2. It is used in dusting powders, ointments and lotions (Calamine Lotion) is applied on the skin for its soothing, adsorbent and protective properties. 3. It has better cosmetic acceptability than zinc oxide. 4. Various dermatological conditions including the exudation of fluids respond reasonably well to calamine. 5. Mild astringent, antiseptic & protective for skin. 6. Phenolated calamine lotion contain 1% liquefied phenol which provides local anesthetic antiseptic & antipruritic
  • 15. ZINC STEARATE • Chemical formula:- CH3 (CH2)16CO2) 2 Zn • STD:- After ignition, it contains not less than12.5% and not more than 14.0% of ZnO. • Properties 1. Colour: White 2. Odour:-faint characteristic. 3. Nature:- light fine bulky powder free from grittiness 4. Taste :- tasteless 5. Solubility:-. practically soluble in water, alcohol & ether Chemical Properties :- 1)Hydrolysed by heating in dil mineral acid to form a soluble Zinc stearate 2)moistened to litmus paper.
  • 16. ASSAY 1. Analyzed by complexometric method. 2. An ignited & cooled sample is dissolved in excess acid H2SO4 (1 N) by boiling. 3. Residue washed with water to free from acidity. 4. Combined the filtrate & titrated against disodium EDTA solution using ammonia, ammonium chloride buffer &urochrome black T as an indicator. USES 1. Astringent & Antimicrobial. 2. Soothing& protective agent & used in dusting powder ointment creams in treatment of inflammatory condition. 3. Used in skin problems where large amount of water is exuded because it will not form patches. 4. Used as lubricant in the processing of tablets. NOTE:-causes pulmonary inflammation if inhaled .
  • 17. TANIUM DIOXIDE • Chemical formula:- TiO2 2) Mol. Wt. :-79.90 • STD:-It contains not less than 98% of TiO2 W.R.T. to dried substance • Properties 1. Colour: White 2. Odour:-odourless. 3. Nature:-Amorphous & fluffy powder 4. Taste :- tasteless 5. Solubility:-. practically soluble in water, & in dil mineral acid it dissolves slowly in Hot H2SO4.22
  • 18. • ASSAY 1. It is analysed by complex metric titration. 2. Sodium edetate back titration method. 3. Sample is dissolved in hot H2SO4 using ammonium sulphate with definite volume. H2O2,strong ammonia solution, Hexamine buffer& excess disodium EDTA is added & excess is back titrated. • Storage:- Store in well closed container • Uses 1. Topical preparation due to its opacity nature. 2. Due to its opacity nature it is used for screening out the UV radiations in various sun creams & sunscreen product to prevent sunburn. 3. Due to its white color it is used in cosmetic preparation & in paints.
  • 19. SILICON POLYMERS • Synonyms:-Dimethicone, Simethicone, Dimethicone, polysiloxne , silicone oils. • Properties & uses of Silicones 1. The silicone polymers are generally known as silicone oils. 2. The silicone polymers are prepared synthetically by polymerization reaction. 3. The oily nature of these compounds makes it useful as water repellent and protective to skin from contact irritants. 4. The silicone oils, thus in general act as protective, it also act as an Antiflatulents and used in varying amount in antacid preparations
  • 20. • Dimethicone 1. It is an inert silicone, oily in nature, it is stable and has low surface tension. 2. It forms a protective layer on skin like plastic and acts as water protective agent. 3. It is mainly used in ointments, sprays, lotions and creams. • Simethicone : 1. It occurs as a light gray, translucent liquid with greasy consistency. 2. It is prepared from dimethylpolysiloxane. 3. It is used as an Antiflatulents and is employed in antacid, antispasmodic, sedative and digestant preparations in 40 - 80 mg dose at bed time