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TOPICAL AGENTS
By
Mr. Afroj Shaikh
M. Pharm
Institute of Chemical Technology, Mumbai
1
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) ,
īƒ˜These are the compound that act locally with skin or
mucous membrane mainly by mechanical or physical
manner.
īƒ˜Topical agents does not absorbed directly into the
circulation.
īƒ˜Compounds have little pharmacological effect.
TOPICALAGENTS
2
īƒ˜ The facts of compounds are that when they are applied
produces variety of effects like adsorbent, astringent,
demulcent , emollient or protective
īƒ˜ Some compounds also exhibit antimicrobial, astringent
activity topically.
īƒ˜ Some inorganic compounds are having topical local
activity .
3
īƒ˜ The inorganic compounds used topically are broadly
* categorized on the basis of their usual action or use e.g.
* (i) protective's and adsorbents,
* (ii) antimicrobial,
* (iii) astringent and
* (iv) Sulphur and its compounds
* (v) miscellaneous compounds.
4
Topical agents:-
1] Protectives and adsorbents.e.g.talc, silicone polymers,
titanium dioxide, calamine, zinc oxide.
2] Antimicrobial agents.
īƒ˜ Hydrogen peroxide, Potassium permanganate, Sodium
per borate.
īƒ˜ Iodine & iodine preparations, Chlorinated lime, sodium
hypochlorite solution,
E.g. Boric acid, Borax, Silver & Silver compounds,
Mercury compounds.
5
3] Astringents. E.g. Zinc chloride, Zinc sulphate,
Aluminium sulphate, Alum, Aluminum sub acetate
solution.
4] Miscellaneous compounds. E.g. sulphur & sulphur
compounds.
6
(i) Protective's and adsorbents :-
protective's are the agents that cover the skin or mucous
membrane from possible irritants.
MOA:-
o Some substance are of insoluble type & chemically inert,
they act by forming a coat or film on the skin.
o They absorb moisture decreases mechanical friction and
irritation and also discourages certain bacterial growth.
o Dusting powder is in the state of fine division form
adherent continuous film on intact skin & exhibit
protective action.
7
Adsorbents:-
â€ĸ Some chemically inert substances adsorb dissolved or
suspended particles or gases, toxins etc are known as
adsorbents .
MOA:-Adsorbents' are mainly used internally to prevent
the irritant & unwanted effects on mucous membrane.
ī‚§ Some inorganic chemicals possesses both protective &
adsorbent properties on topical application.
â€ĸ 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.8
Some of the inorganic protective compounds and preparations
are described here:
1) TALC
Chemical formula :- 3Mgo. 4siO2.H20
Synonym:- soapstone or French chalk, purified talc
īƒ˜ Talc is the softest material
Properties:-
īƒ˜Colour: White/greayish white
īƒ˜Odour:-odourless.
īƒ˜Nature:-fine powder
īƒ˜Taste:-tasteless
īƒ˜Touch:-greasy or unctuous & adheres to skin
īƒ˜Solubility:-soluble in water, dil. acids & bases
9
Storage:- In well closed container.
PREPARATION
a)prepared by boiling fine powered talc with Dil HCL &
allowing to settle.
b)the supernatant liquid is removed
c) the talc is washed thoroughly with water to make it free
from acid.
( Acid treatment remove impurities from talc.)
10
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 / untouch to touch therefore used as lubricant
or protective.
5)It is used as excipient, lubricant& filler for tablet & pills
11
2) ZINC OXIDE
1)Chemical formula:-ZnO
2) Mol wt : 81.38
3) Properties:-
īƒ˜Colour: White/yellowish white
īƒ˜Odour:- Odourless.
īƒ˜Nature:-fine amorphous powder
īƒ˜Solubility:-Insoluble in water & alcohol
soluble in NH3.
īƒ˜Storage:- Zinc oxide absorbs carbon dioxideâ€Ļ.
?
12
PREPARATION
a) 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
b) 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
īƒŧ ZnO is insoluble in water therefore cannot directly titrated
with acid.
īƒŧ it is dissolved in excessive of acid & back titrated.
īƒŧAmmonium chloride is used in titration to prevent ppt
īƒŧWhite ppt interferes in end point
īƒŧMethyl orange is used as an indicator
ZnO + H2SO4 ZnSO4 + H2O
H2SO4 ( Excess) + 2NaOH Na2SO4+ 2H2O
14
USES:-
â€ĸ Mild Antiseptic & Astringent.
in form of lotions, ointment paste or dusting powder.
â€ĸ in treatment of urticaria, aczema,sunburns
â€ĸ in combinations with other antimicrobial agents Eg Talc
â€ĸ primary ingredient in calamine.
â€ĸ pharmaceutical aid in mfg of adhesive tapes, bandages.
â€ĸ It is used in the treatment of eczema, ring worm, pruritus
and psoriasis
15
3) CALAMINE
1. Chemical formula:- ZnC03.Zn(OH)2¡xFe2O3
2. STD:- After ignition, it contains not less than 98.0% and
not more than 100.5% of ZnO.
3. Properties:-
īƒ˜Colour: pink or reddish brown powder
īƒ˜Odour:-odourless.
īƒ˜Nature:-fine powder & amorphous
īƒ˜Taste :- tasteless
īƒ˜Solubility:-Practically insoluble in water, almost
completely soluble in mineral acids with effervescence.
īƒ˜NOTE
The presence of ferric oxide gives the substance a pink
colour (for cosmetic reasons).
16
Preparation
ī‚§ Calamine is obtained by calcination( powdered by heating) of
the natural native zinc carbonate.
ī‚§ prepared by mixing zinc oxide with ferric oxide
ī‚§Sieved & fine powder is collected.
Assay
ī‚§An ignited & cooled sample is dissolved in excess acid
H2SO4 (1 N) & filter.
ī‚§ residue washed with hot water to free from acidity.
ī‚§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.
18
4) ZINC STEARATE
1)Chemical formula:- CH3 (CH2)16CO2) 2 Zn
2)STD:- After ignition, it contains not less than12.5% and not
more than 14.0% of ZnO.
3) Properties:-
īƒ˜Colour: White
īƒ˜Odour:-faint characteristic.
īƒ˜Nature:- light fine bulky powder free from grittiness
īƒ˜Taste :- tasteless
īƒ˜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. 19
ASSAY
īƒ˜Analyzed by complexometry method.
ī‚§An ignited & cooled sample is dissolved in excess acid
H2SO4 (1 N) by boiling.
ī‚§ residue washed with water to free from acidity.
ī‚§Combined the filtrate & titrated against disodium EDTA
solution using ammonia, ammonium chloride buffer
&eriochrome black T as an indicator.
20
USES
â€ĸ Astringent & Antimicrobial.
â€ĸ Soothing& protective agent & used in dusting powder
ointment creams in treatment of inflammatory condition.
â€ĸ Used in skin problems where large amount of water is
exuded becoz it will not form patches.
â€ĸ used as lubricant in the processing of tablets.
â€ĸ NOTE:-causes pulmonary inflammation if inhaled .
21
5) TANIUM DIOXIDE
1)Chemical formula:- TiO2
2)Mol.Wt :-79.90
3)STD:-It contains not less than 98% of TiO2 W.R.T. to dried
substance
Properties:-
īƒ˜Colour: White
īƒ˜Odour:-odourless.
īƒ˜Nature:-Amorphous & fluffy powder
īƒ˜Taste :- tasteless
īƒ˜Solubility:-. practically soluble in water, & in dil mineral
acid it dissolves slowly in Hot H2SO4.22
ASSAY
īƒ˜ It is analyzed by complex metric titration.
īƒ˜Sodium edetate back titration method.
īƒ˜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.
23
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 colour it is used in cosmetic
preparation & in paints.
24
6) Silicon Polymers
Synonyms:-Dimethicone, Simethicone, Dimethicone, polysiloxne ,
silicone oils.
Properties & uses of Silicones
â€ĸ The silicone polymers are generally known as silicone oils.
â€ĸ The silicone polymers are prepared synthetically by polymerization
reaction.
â€ĸ The oily nature of these compounds makes it useful as water
repellent and protective to skin from contact irritants.
â€ĸ The silicone oils, thus in general act as protective, it also act as an
Antiflatulents and used in varying amount in antacid preparations.
25
â€ĸ Dimethicone:
â€ĸ It is an inert silicone, oily in nature, it is stable and has low
surface tension.
â€ĸ It forms a protective layer on skin like plastic and acts as
water protective agent.
â€ĸ It is mainly used in ointments, sprays, lotions and creams.
Simethicone :
ī‚§ It occurs as a light gray, translucent liquid with greasy
consistency. It is prepared from dimethylpolysiloxane.
ī‚§It is used as an Antiflatulents and is employed in antacid,
antispasmodic, sedative and digestant preparations in
40 - 80 mg dose at bed time.
26
ANTIMICROBIAL AGENT
â€ĸ Is a broad terminology describing activity against microbes.
â€ĸ Antimicrobials are the chemical agents used to destroy or inhibit the
growth of pathogenic micro-organism.
â€ĸ They are normally ineffective in the sporing state of microorganism.
Disinfectants -are substances that are applied to non-living/inanimate
objects to destroy microorganisms that are living on the objects.
E.g. Chlorinated lime, potassium permanganate, formaldehyde, phenol
etc.
Antiseptic: They are antimicrobial substances that are applied to
living tissue/skin to reduce the possibility of infection, sepsis.
e.g. Hydrogen peroxide, potassium permanganate, Iodine, Povidone
iodine etc.
27
Sterilization:-the complete destruction living microorganism
including bacterial spores .it can be achieved by physical
methods or by chemical means.
Germicide:-the agents which are employed to kill M.O. it can
be broad form germicidal,virucide,fungicide etc.
Static:-stops the growth of M.O.
Bacteriostatic:- The agent which primarily function by
inhibiting the growth of bacteria. Thus, bacteriostatic drugs or
agents do not kill but arrest the growth of bacteria.
28
PROPERTIES
1.It should have antiseptic or germicide activity & not
bacteriostatic activity because if M.O are not killed , they
may grow & cause infection.
2.To reduce incidence of resistance it should have rapid
onset of
action & sustain activity.
3. Have good therapeutic index.
4.Should not produce local cellular damage or should not
interfere with body defense.
5. It should show no systemic toxicity from topical
application.
6. It should have in general broad spectrum of activity
against bacteria, fungi, protozoa, virus etc.29
MECHANISM OF ACTION
Antimicrobial is a broad terminology describing activity against
microbes. Specific terminology describes exact mode or
mechanism of action.e.g. Antiseptics, Disinfectant, Germicide
bactericide' (against bacteria), 'fungicide' (against fungi),
'virucide' (against virus) etc. denotes exact
action.),Bacteriostatic.
Inorganic compounds generally exhibit antimicrobial action by,
either of the three mechanisms viz.
(i) Oxidation
(ii) Halogenation
(iii) Protein binding or Precipitation.
30
1.Oxidation Mechanism :
īƒ˜Compounds acting by this mechanism belong to class of
peroxide, peroxy-acids, oxygen liberating compounds like
permanganate and certain oxo-halogen anions.
īƒ˜ They act on proteins containing sulphadryl group and
oxidizes free sulphadryl to disulphide bridge and inactivate its
function.
2. Halogenation Mechanisms:
īƒ˜ Compounds which liberate chlorine or hypochlorite or
iodine act by this mechanism.
īƒ˜ This category of agents act on peptide linkage and alter its
potential and property.
īƒ˜The destruction of specific function of protein results in
death of microorganisms.
. 31
3. Protein Precipitation :
ī‚§ Many metals in their cation form exhibit protein binding or
protein precipitation.
ī‚§ The nature of interaction with protein occurs through polar group
of protein which acts as ligands and metal ion acts as Lewis acid.
ī‚§ The complex formed may be a strong chelate leading to
inactivation of protein.
ī‚§ This action in general is non-specific. Protein precipitants do not
distinguish between the protein of microbes and that of host.
ī‚§ Germicidal action results when the concentration of ion is such
that reaction is restricted largely to the parasite cell
32
Various antimicrobials and astringents are classified as under:
īąOxidative Antimicrobial agents
e.g. Hydrogen Peroxide Solution, Zinc Peroxide, Sodium Perborate,
Potassium Permanganate, Sodium Hypochlorite Solution, Chlorinated Lime.
īą Iodine Preparations and Compounds
e.g. Iodine and Iodine Solutions, Povidone-Iodine.
īą Protein Precipitant Antimicrobial Agents
e.g. Silver Nitrate, Mild Silver Protein.
īą Mercury Compounds
e.g. Yellow Mercuric Oxide, Ammoniated Mercury, Mercuric Chloride.
īą Sulphur and Sulphur compounds
e.g. Sublimed Sulphur, Precipitated Sulphur, Sulphur Dioxide,
Sulphureted Potash, Selenium Sulphide, Cadmium Sulphide.
īą6. Boric acid and Borax.
Sodium Borate
īą7. Arsenic Compounds
e.g. Carbarsone, Glycobiarsol, Tryparsamide.
īą8. Antimony Compounds
e.g. Antimony Sodium Gluconate, Stibophen.33
Hydrogen Peroxide:-
1)Chemical formula:- H2O2
2)Mol. Wt :-34.02
Properties:-
īƒ˜Colour: colorless
īƒ˜Odour:-odourless.
īƒ˜Nature:- Clear liquid
īƒ˜Taste :- slightly acidic
īƒ˜Solubility:-. practically soluble in water, & in dil mineral acid it
dissolves slowly in Hot H2SO4
34
The Solution usually deteriorate upon standing upon agitation
Rapidly decomposes when in contact with many oxidizing or reducing sub.
2H2O2 2 H2O + O2
Solution is stabilized by
1) By addition of small qty of acid & by adjusting the pH between 2 to 3.
2) Some Stabilizers like acetanilide, quinine, sulphate, 8-
hydroxyquinoline & others complexing /chelating agents are used in
0.02 to 0.05% con range.
35
Principle:
īƒ˜This assay is based on Oxidation Reduction (Permanganate) type of
titration in which solution of potassium permanganate is acts as an
oxidizing agent and hydrogen peroxide also acts as an oxidizing
agent But in presence of strong oxidizing agent like potassium
permanganate hydrogen peroxide acts as reducing agent.
īƒ˜The ability of potassium permanganate solution to oxidize is due to
conversion of the MnO4 - ion to Mn++ in acidic solution but MnO4
- ion is reduced by reducing agent like hydrogen peroxide.
īƒ˜Solution containing MnO4 - ion are purple in color , solution of salt
containing Mn++ ions are colorless, hence permanganate solution is
decolorized by reducing agent as longer as MnO4 - is present in the
solution.
36
The moment there is an excess addition of potassium permanganate
solution becomes purple, thus potassium permanganate acts as a self
indicator.
Reactions:
In this assay dilute sulfuric acid is used for conversion of
MnO4- to Mn++
MnO4 - + 8H+ + 5e Mn+2 + 4H2O
Chemical reaction for assay:
2KMnO4 + 3H2SO4 + 5H2O2 2MnSO4 + K2SO4 + 8H2O +
5O2
37
Uses
1) The primary use is a mild oxidizing antiseptic. This action comes
when it comes in contact with abraded tissue It is a mild oxidizing
antiseptic action the antiseptic action is associated with
mechanical cleansing provides by rapid foaming release of
oxygen. Helps in removal of dirt , bacteria from cuts & wounds &
acts as cleaning antiseptic.
2) It destroy most pathogenic bacteria.
3) Its 1.6% solution is used as deodorant, gargle and mouth wash.
4) It is used as an antidote in phosphorous and cyanide poisoning.
5) It is used for bleaching the hair.
6) It is used in treatment as ear wash & vaginal douches.
38
Storage:-
â€ĸ It is stored in container protected from light, in bottles closed
with glass stoppered or plastic caps provided with vent for the
escape of oxygen.
â€ĸ Keep in cool place.
â€ĸ The label should indicate whether it contains stabilizing agent or
not.
39
2)Potassium Permanganate
Chemical Formula:-KMnO4
Mol Wt:-158.03
Physical Properties:-
īƒ˜ Colour: Dark Purple
īƒ˜Odour:-odourless.
īƒ˜Nature:- metallic prisms, almost opaque with blue metallic lustered
īƒ˜Taste :- sweet
īƒ˜Solubility:-. practically soluble in water, & more in boiling water.
40
Chemical properties:-
īƒ˜ When heated it decomposes at high temp ( 240°C)
2KMnO4 K2MnO4+MnO2+O2
īƒ˜ It is a powerful oxidizing agent
in acidic solution it is reduced from Mn+7 to Manganious
ion Mn+2 with evolution of O2.
2KMnO4 + 3H2SO4 K2SO4 + 2MnS04 + 3H20 + 5[O]
īƒ˜ In neutral or alkaline media also O2 is liberated .It brings
bleaching Action.
īƒ˜ KMnO4 oxidize alcohol to Aldehyde
īƒ˜ Sulphide to Sulphur
īƒ˜Ferrous Salt to Ferric
īƒ˜Nitrites to nitrates
īƒ˜Iodide to free iodine in acidic condition
41
Assay:- Oxidation Reduction Reaction
īƒ˜ known Wt of sample is dissolved in water & vol made to
250ml.
īƒ˜ To 25ml of 0.1N oxalic acid added 5ml H2SO4 &
warms to 70Âē C& titrated with prepared solution of KmNO4
(temp is not maintained at 70Âē C the reaction will be slow)
īƒ˜The permanganate should be taken in the burette and the end point
is appearance of a pale pink color.
42
īƒ˜ Incompatibility It is incompatible with iodides, reducing
agents and most organic matter.
īƒ˜Storage:- It should be stored in tightly-closed container &should
handled with care since explosion may occur when it comes in
contact with oxidisable substance
43
Uses:-
1. It is a topical anti-infective (antibacterial and anti-
fungal). (anti-infective due to the oxidizing property.)
2.It stains the skin & tissues.
Sol in 1:5000-1:15000 conc. it is used in cleaning wounds &
ulcers for skin infection caused by bacteria & fungi.
3. It is also used as an antidote in barbiturate & alkaloidal
poisoning. (A sol of 1: 5000 when used as gastric wash, oxidises
poison & prevents their absorption.)
44
Compound acting by Halogenation Mechanism:-
1.CHLORINATED LIME:-
Chemical formula Ca(ClO)2
Synonym Bleaching Powder, Chloride of Lime.
Physical Properties:
Colour:- white powder
Odour:- characteristic odour
Solubility:- slightly soluble in water and in alcohol.
Storage: It should be stored in tightly closed containers. It is
affected by moisture & heat.
45
īƒ˜Preparation:-
It is manufactured by the action of chlorine on calcium
hydroxide
i.e.. The slaked lime is spread on shelves in suitable container
Chlorine gas is introduced at the top of chamber & passed through
the contents of the shelves.
this is usually done at 25° thus minimizing the formation of calcium
chloride. when abs of chlorine is completed, powdered lime is
blown into the chamber to absorb the excess of chlorine.
46
USES:-
-It is used as disinfectant & bleaching agent.
-It shows bactericidal action.
-It is used to disinfect faeces, urine , sputum& other organic material.
-It is employed for disinfecting drainages.
-It is a powerful bleaching agent .Its powerful bleaching action
must be considered while disinfecting coloured materials.
-it is used as 1-2 g/l for sterilization of water.
The treated water should be exposed to air & allowed to settle
before use.
-Chlorinated lime is used in the preparation of surgical chlorinated
soda solution, employed as a wound disinfectant.
47
Properties of Boric acid-
1. It is a white, colorless crystalline powder, odorless, unctuous to
touch.
2. It has bitter, sweetish after taste
3. It is soluble in alcohol, freely soluble in glycerin, propylene
glycol and boiling water
4. Stable in air
5. On heating at 1000C it is converted in to Metaboric acid, at
1600Cin to tetra boric acid and at more than 1600C boric acid is
converted in to boron trioxide.
6. Boric acid is very weak acid, so it cannot be titrated accurately
with standard alkali.
Hence glycerin is added in its titration.
Storage of Boric acid- It should be stored in air-tight, well closed
container.
48
Uses of Boric acid-
1. It has weak bacterciostatic and fungi static action
2. It is used as local anti-infective drug in the form of cream,
ointment and lotion
3. Buffer in topical preparations
4. Vehicle for ophthalmic solution
5. Boric acid is useful as Suppositories base
6. It is also used to impregnate surgical dressings
49
BORAX
ī‚§ Chemical formula Na2B4O7. 10 H2O
īƒ˜ Synonym:- Sodium Borate
īƒ˜ Properties:-
īƒ˜Colour:-Colourless transparent crystals
īƒ˜Odour:-odourless,
īƒ˜Taste:- saline and alkaline taste
īƒ˜Solubility:- It is soluble in water and glycerin but insoluble
in alcohol.
īƒ˜Chemical Properties:-
īƒ˜ On heating loses all its water of hydration & swells to a
white porous powder.
īƒ˜ When heated to red hot & on cooling , forms a transparent
mass known as borax bead 50
īƒ˜ An aqueous sol of Na borate is alkaline to litmus .
īƒ˜Alkali borate are water soluble.
īƒ˜Borates of other metals undergo hydrolysis & forms insoluble ,
hydroxides or oxides.
Action & Uses:- It has been used externally in solutions
containing 1 to 2% of borax as an eyewash, gargle in
mouthwashes and as a wet dressing used in food preservative
īƒ˜ cosmetics, it is used as emulsifier & also in lotions. germicide
& bacteriostatic.
51
Iodine
īƒ˜ Chemical formula :-I2
īƒ˜ Mol wt : 253.8
Properties:-
īƒ˜ Colour:-grayish-violet or bluish-black
īƒ˜ Nature:-brittle plates or small crystals with a metallic luster.
īƒ˜ Odour:-It possesses a distinctive penetrating irritant
īƒ˜ Taste:-bitterly pungent taste.
īƒ˜Solubility:-It is very slightly soluble in water, soluble in
alcohol and dissolves freely in ether, chloroform and
carbon disulphide.
It dissolves readily in sol of KI & other iodides forming
compound as KI3.
52
Chemical Properties:-
1.It melts at 1400C but sublimes freely at temp below its MP.
2. It is volatile at R.T & its vapours attack both cork & rubber.
3.The imp chemical property of iodine in aqueous sol is that a mild
oxidizing action mediated through the formation of hypoiodous
acid.
Storage:- Should be stored in well- closed bottles fitted with glass
stoppers because I2 is volatile & its vapors attack both cork &
rubber.
Incompatibility:- with alkalis and alkali carbonates.
53
Uses:-
1) Topical anti-infective iodine has a powerful bactericidal
action and is used for disinfecting unbroken skin before operation.
2) Iodine ointments are applied as counter-irritants.
3)Its.2% solution in glycerol is used for application to mucous
membrane
4)compound iodine paint is used as a throat paint in pharyngitis
and follicular tonsillitis.
5) Iodine is an essential trace element in human diet.
Deficiency of iodine leads to development of goiter and in
many countries, common salt which is used for food
purpose is iodized mainly with iodides.
54
Solution Of Iodine:-
īƒ˜ The germicidal activity of free iodine is about six times
that of hypoiodous acid.
īƒ˜ Preparations providing free iodine are bactericidal,
fungicidal, amoebicidal and virucidal.
īƒ˜ Iodine is effective in very dilutions.
īƒ˜ Iodine Solutions and Iodine Tincture are most effective
topical agents available.
ī‚§ They have been used as antiseptics on the skin prior to surgery.
55
Some of the well-established solutions are:
ī‚§ 1)Aqueous Iodine Solution B.P./I.P. (1966) (Strong Iodine
U.S.P.)
īƒ˜ It is also known as Lugol's solution.
īƒ˜It does not contain any alcohol. It contains 5.0% w/v of
Iodine and 10.0% w/v of Potassium Iodide.
īƒ˜ The relative proportion of potassium iodide to iodine is much
higher than in weak solution.
īƒ˜Uses: Source ¡of Iodine.
56
2)Strong Iodine Solution I.P. (1966)
It contains 10.0% w/v of Iodine and 6.0% w/v of Potassium Iodide
in alcoholic solution, composition: Iodine 100 g, Potassium Iodide
60 g, Purified water 100 ml; Alcohol (90%) sufficient to produce
1000 ml'
Uses: Antiseptic.
57
3) Weak Iodine Solution B.P/I.P. (1966):-
It contains
2.0% w/v of Iodine
2.5% w/v of Potassium Iodide in water.
This solution is identical in composition with Tinctura
iodi Mitis B.P. 1914. es.
Uses: Antiseptic.
58
4) Iodine Tincture U.S.P. :
It contains 2.0% w/v of Iodine and 2.4% w/v of Sodium Iodide in
much diluted alcoholic solution.
Note-Iodine preparations of any type are contraindicated in
patients who have exhibited prior allergy or hypersensitivity to
iodine.
59
Povidone-Iodine
īƒ˜ Povidone-Iodine is a complex of iodine with Povidone
(a polymer) also known as polyvinylpyrrolidone or PVP.
īƒ˜ Products are available under different names in concentrations
of 0.1 to 1 % of available iodine. (usually 10% of the total
concentration of Povidone- Iodine).
īƒ˜Povidone-Iodine belongs to iodophors.
īƒ˜ Iodophors are complexes of iodine with carrier organic
compounds serving as a solubilizing agent, which slowly
liberate iodine in solution.
60
Properties
īƒ˜ Colour:-Yellowish brown
īƒ˜ Odour:- slight characteristic odour
īƒ˜Nature:- amorphous powder
īƒ˜ Solubility:-It is soluble in water and in alcohol, but practically
insoluble in organic solvents.
īƒ˜Chemical properties :-Aqueous solution is acidic to litmus.
īƒ˜ The Povidone-Iodine solution is reddish Brown colour, and a pH of
not more than 6.0.
īƒ˜ Its non-irritating effects on tissue, comparatively low oral toxicity,
its water solubility and its low iodine vapour pressure making it
stable to possible iodine loss makes it superior to Iodine Solutions.
īƒ˜ Solution in most of the applications. Solutions are nonstaining
and can be washed clear from skin and clothing.
Storage :-It should be stored in air-tight containers (tightly closed
containers), the materials of which are resistant to iodine.61
Uses
â€ĸ Antiseptics for surgical scrubs and pre-operative antisepsis of the
skin.
â€ĸ It is also used in gargles and mouthwashes for the treatment of
infections in the oral cavity.
â€ĸ Various preparations include an aerosol (0.5%), solutions (usually
1%), a surgical scrub (0.75%), a vaginal douche (1%) and a
vaginal gel (0.1%).
62
Protein precipitant Antimicrobial
SILVER NITRATE
Chemical formula:- AgNO3
Mol wt : 169.89
preparation:-
īƒ˜ It is prepared by the action of hot nearly concentrated nitric acid
on pure silver.
īƒ˜ 3 parts of silver are added to a sol 25% nitric acid ( about 10 parts)
heated to expel the nitrous fumes,filltered & evaporated until it is
dry.
īƒ˜ then the mass is fused to convert the copper nitrate into insoluble
oxide. So obtained product is dissolved in hot water, filtered it &
kept aside in dark place for crystallization.
īƒ˜ crystals are collected on sintered glass crucible & dried at 50°c
in dark.
īƒ˜Purified of AgNO3 is costly therefore pure silver & nitric acid free
from halogen & sulphur is used. 63
Properties
īƒ˜Colour:-White
īƒ˜ Odour:- odourless
īƒ˜ Nature:-Rhombic crystals
īƒ˜ Taste:- Bitter taste
īƒ˜ Solubility:-Very soluble in water
īƒ˜Sparingly soluble in alcohol, freely soluble in boiling alcohol It
becomes grey/greyish black .
īƒ˜ On exposure to light in presence of organic matter, due to liberated
silver.
Chemical Properties:-
īƒ˜ 1% sol has PH between 4.5- 6
īƒ˜ 4% sol has bet 5.4- to 6.4
īƒ˜ at 212° C it melts to a slightly yellow liquid which on cooling
congeals to a white crystalline mass.
īƒ˜ At high temp is slowly decomposes evolving oxides of nitrogen.
it produces chemical reaction of silver ion & nitrate ion.
64
īƒ˜ Sol of AgNO3 gives white- yellow –white ppt with HCL & other
halogen containing salts.
īƒ˜ The silver halide ppt is insoluble in dil acids but dissolve in
ammonia.
Storage :-
īƒ˜ Should be stores in tightly closed light resistant non metallic
containers .
īƒ˜ Sol should be freshly prepared & supplied in amber Coloured
bottles.
65
Incompatibility:-incompatible with reducing agent, Tartarates,
Sugar, Tannins, Alkali halogen acids & their salts.
Uses:-
1) Antibacterial in conc. from 0.01 to 0.5%
2) In higher conc 1% above it has astringent, irritant property on
tissues .
3) AgNO3 ophthalmic sol 1% is used in eyewash, 0.5% aq sol for
treating burns injuries & in wet dressings.
4)Its effective against coccol infections
66
Mild Silver Protein
Chemical formula :-Variable
It is a silver rendered colloidal by the presence of, or in combination
with protein .
Properties:-
Colour:- dark brown or almost black
Odour:- odourless
Nature:- shining scales or granules
Solubility:-It is freely soluble in water, but almost insoluble in
alcohol, chloroform and ether.
Storage:-It is affected by light therefore should be protected
from light.
67
Action & uses:-
1) 0.5% to 20% sol is used as antibacterial. the release of Ag+ ions tends to
increase with dilution & therefore more dilute sol becomes irritating. on
aging sol becomes more irritant & a ppt is formed. therefore sol of mild
silver protein should be always prepared freshly which contain suitable
stabilizers.
Uses:-
Uses:-
â€ĸ The Solution due to its low irritability usually employed as local
antibacterial on mucous membranes in nose, throat, & conjunctiva of eye.
â€ĸ for irrigation of urethra & bladder.
â€ĸ its major effectiveness in the treatment of gonococcal infection. Also used
in respiratory tract infections & also as prophylactic against respiratory
infection.
â€ĸ Mercury with chalk act as purgative due to irritant action of Hg ion.
â€ĸ As it is toxic it is not used medicinally.
â€ĸ best bacteriostatic.
note:- Prolonged use of mild silver protein may result in darkening of skin
due to the deposit of free silver below epidermis.68
Mercury
Synonym:-Hydragyrum , quick silver (Hg)
īƒ˜ Colour:- bright shiny silvery White
īƒ˜ Odour:- odourless
īƒ˜ Nature:-liquid at room temp
Storage :-
īƒ˜ Should be stores in tightly closed containers .
īƒ˜Action & uses:-
īƒ˜ Cathartic & parasiticide
īƒ˜Also used in the treatment of syphilis & as diuretic
īƒ˜ But it is extremely poisonous & prolonged inhalation in
minute quantity may be fatal.
69
Yellow Mercuric Oxide
Chemical Formula:-HgO
Mol.Wt: 216.6
īƒ˜ Colour:-Yellow to orange according to temp at time of preparation
īƒ˜ Odour:- odourless
īƒ˜ Solubility:- in Soluble in water& alcohol but soluble in acids
Storage :-
īƒ˜ Should be stores in tightly closed containers .protected fro light
īƒ˜ Chemical properties:-
īƒ˜ Stable in air
īƒ˜ form red oxide slowly develops on exposure to light.
70
Action & Uses:-
īƒ˜ local antibacterial.
īƒ˜ also mild antiseptic action used in ophthalmology for treating no.
of inflammatory conditions.
īƒ˜ also used for the treatment of fungal infection of the skin &
infestations of body lice.
71
Ammoniated Mercury
Chemical formula:-NH2 .HgCl
Synonym:- Amminochloride of mercury, white precipitate
īƒ˜ Mol.wt- 252.1
īƒ˜ Colour:- White
īƒ˜ Solubility:- Insoluble In water, alcohol, ether.
Storage :-
īƒ˜Should be the amber colored container (on exposure to light it darkens).
Action & uses:-
1) acts as mild antiseptiC (slow release of mercuric ions.)
2) topically used in treatment of various skin infections caused by
fungi, lice & other infestations.
3) Commonly employed in 5% strength as ointment & also as dusting
powder.
72
Sulphur & its compound
* Elemental Sulphur exist in various allotropic forms including several solid and
two liquid states namely:
*It occurs in free form & also sulphides & Sulphate Sulphur &
* its compound have many use p,’ceutical & medicinal fields.
*Solid as Rhombic (Îą-Sulphur, SÎą, Sublimed Sulphur or Flower of Sulphur), and
Monoclinic (β-Sulphur, Sβ); Liquid as Îģ-Sulphur Plastic Sulphur and Amorphous
Sulphur (formed on aging of "plastic" sulphur).
*Elemental Sulphur is little use internally
MOA:-but it is use topically as antibacterial. elemental sulphur acts either due to
the oxidation-reduction products of the element [e.g. sulphides)
*The sulphur "candles" when burned, give off sulphur dioxide for fumigation or
insecticide purposes.
* Sulphides are used as depilatories, due to the ability of sulphides in highly
alkaline solution (pH 10) to reduce the disulphide linkage in the amino acid
cysteine in hair. The reduction and softening of the hair help in its removal.
73
medicinally used Sulphur compound are
PRECIPITATED SULPHUR
īƒ˜ Chemical symbol S Atomic wt. : 32.6
īƒ˜ Synonym:- flower of Sulphur, milk of sulphur
Preparation:-
īƒ˜ By Sublimation process
(Any form of Sulphur is heated vapors produced which are condensed.)
īƒ˜ In refinery the molten Sulphur is placed in iron retorts which
communicate with the stone chambers.
īƒ˜ When Sulphur vapors enters the stone chambers they ignite &
convert into Sulphur dioxide.
īƒ˜ The subsequent vapor pass through relative cold gas &
condenses on walls & floors of the chambers in fine crystalline
form.
74
Properties:-
īƒ˜ Colour:-Yellow
īƒ˜ nature:- Fine crystalline powder
īƒ˜ Odour :-Odourless
īƒ˜Tasteless
īƒ˜ Solubility:-insoluble in water and in alcohol.
Uses:-
īƒ˜ Used as an ingredient in sulphur ointment & used as scabicide.
īƒ˜Used in the treatment of acne, pimples and psoriasis
īƒ˜Act as kerotolytic agent
75
Precipitated Sulphur U.S.P ( Solid allotropic form of Sulphur)
īƒ˜ properties:
īƒ˜ Colour:-pale yellow
īƒ˜ Odour:-odoureless
īƒ˜ Taste;- Tasteless
īƒ˜ nature:- very fine
īƒ˜ Solubility;- very slightly soluble in alcohol & slightly
soluble in olive oil.
76
Uses:-
1.Sulphur is a mild antiseptic and Parasiticide and has been
widely in the of lotions and 10% ointments for treatment of
scabies & acne . employed as fungicides in the treatment of
superficial fungal infections.
2) Sulphur is also used mainly as a dermatological agent to treat
seborrhea s , psoriasis.
3)It may be used alone or in conjunction with other keratolytics .
4) Precipitated Sulphur is converted in the small intestines into
alkali sulphides which produce a mild laxative effect due to their
irritant action.
5)also used in homoeopathic medicines.
Note-Some patients may be hypersensitive to sulphur and
should be observed for any allergic manifestations.
77
Selenium Sulphide
Chemical formula -SeS2
Synonym Selenium Disulphide
Mol.wt-143.09
Preparation;-
Prepared by passing H2S into selenious acid.by adding selenious acid
to a saturated solution of H2S PPT is collected & dry.
Properties.
colour;-orange to reddish brown
odour:- faint odour of hydrogen sulphide
nature:- powder
solubility:-in water & inorganic solvents in HNO3 with formation of
selenious & sulphuric acid
78
1 Selenium sulphide is used as antidandruff.
2. Selenium Sulphide used in 1 to 2.5 % as anti seborrheic
3. 5-10ml of 2.5% suspension to be applied on scalp. after
application it is allowed to remain in contact for 5 min & it is washed
off.
4.Longer exposure produce irritation care should be taken ,not to
introduce in eyes or mouth as it is highly toxic.
79
Astringent
īƒ˜Astringents are locally applied protein precipitants which
have a low cell permeability so that the action is limited essentially
to the cell surface and the interstitial spaces.
īƒ˜The action does not result in the death of the cell, only
the permeability of the cell membrane is reduced.
80
Astringents are therapeutically used as
(i) Styptic, to arrest haemorrhage (to stop bleeding from small cuts) by
promoting coagulation of blood and constricting small capillaries;
(ii) antiperspirant to decrease sweating by constricting pores at the surface of the
skin;
(iii) to reduce inflammation by restriction of the blood supply to the surface of
mucous membranes;
(iv) promote healing and toughen the skin;
(v) deodorant by virtue of interaction with odorous fatty acids liberated or
produced by the action of bacteria on lipids in sweat and by an action
suppressing bacterial growth, partly due to a decrease in pH; and
(vi) direct action on skin to remove unwanted tissue (this requires a higher
concentration or a stronger protein precipitant, often termed as corrosive).
81
Most topical astringents are salts of aluminium, zinc & to some
extent Zirconium.
Alum :-KAI(SO4)2 12H2O
Mol wt :- 474.33
(Aluminium Potassium Sulphate) Mol wt. 453.33
(Aluminium Ammonium Sulphate), Mol Wt:- 474.39
Alum can be either the ammonium or the potassium salt & should
be labeled on container which salt is present.
82
Preparation:-
official alums are prepared by adding a hot, concentrated
solution of either potassium or ammonium sulphate to a
hot solution of an equimolecular proportion of
aluminium sulphate.
The alums separate out as crystals on cooling.
Properties:-
Colour:- colourless
Nature:- large crystals, crystalline fragments or as a white
powder.
odour:- odourless
taste:-with a sweetish strongly astringent taste.
Solubility:- Alums are freely soluble in water, but slowly
dissolve in glycerin, and insoluble in alcohol.
83
Chemical properties:-
Acidic to litmus
When heated, it melts and at about 200°C looses its water
of crystallization with the formation of the anhydrous salt.
Storage:-To be stored in airtight containers.
84
Uses:-
īƒ˜ Alum precipitates proteins and is a powerful astringent.
īƒ˜ Dilute solutions (l to 4%) have been¡ used as astringent
mouthwashes and gargles but they have a destructive
action on teeth.
īƒ˜A 2% solution has been used for application to the skin to
reduce excessive perspiration.
īƒ˜ Stronger solutions (5 to 10%) are used to harden skin by
athletes, especially as footbath to toughen the skin of the
feet.
īƒ˜ strong solution is used as a styptic for minor cuts and
abrasions.
īƒ˜(0.5 to 5%), lotions and douches, some vulvovaginal
cleansing and deodorant preparations.
85
ZINC SULPHATE
Chemical formula :-ZnS04.7H20
Synonym:- White Vitriol
Preparations
īƒ˜ For industrial scale, zinc sulphide is heated in presence
of air under specified conditions.the heated mass is
dissolved in hot water, filter the solution concentrated for
crystallization.
īƒ˜ metallic zinc granules are digested with H2SO4.
īƒ˜ The sol is filtered & treated with chlorine to oxidize any
ferrous impurity into ferric sulphate which is then ppted
by hydroxide & removed.
the filtrate is concentrated & crystallized
86
Properties:-
īƒ˜ Colour:- colorless,
īƒ˜ Nature:-transparent crystals or as crystallline powder.
īƒ˜ Odour:- is odourless
īƒ˜ taste:- metallic and astringent.
īƒ˜ Solubility:- very soluble in water. It is freely soluble in
glycerin, but is insoluble in alcohol it
īƒ˜ Chemical Properties:-
īƒ˜ Aqueous solutions of zinc sulphate are acid to litmus
īƒ˜ It forms double salts with ammonium & Potassium Sulphate
īƒ˜ When strongly heated it decomposes
īƒ˜ Storage It should be stored in tightly closed containers.
īƒ˜ Incompatibility :-It is incompatible with alkali carbonates and
īƒ˜ hydroxides and with astringent infusions and decoctions.
87
uses:-
īƒ˜ Zinc ions exhibit mild germicidal astringent & styptic
action
īƒ˜ ( the action is dependent due to slow release of zinc ions
from salt or sol.)
īƒ˜ Insoluble zinc ions used in topical agents as protectives.
īƒ˜ ZnSO4 sol 0.1-1% used ophthalmic
īƒ˜ Internally it is used as an emetic
īƒ˜ Insoluble Zn complex are mainly used in bandages,
adhesive, tapes etc.
88

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Topical agents

  • 1. TOPICAL AGENTS By Mr. Afroj Shaikh M. Pharm Institute of Chemical Technology, Mumbai 1
  • 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) , īƒ˜These are the compound that act locally with skin or mucous membrane mainly by mechanical or physical manner. īƒ˜Topical agents does not absorbed directly into the circulation. īƒ˜Compounds have little pharmacological effect. TOPICALAGENTS 2
  • 3. īƒ˜ The facts of compounds are that when they are applied produces variety of effects like adsorbent, astringent, demulcent , emollient or protective īƒ˜ Some compounds also exhibit antimicrobial, astringent activity topically. īƒ˜ Some inorganic compounds are having topical local activity . 3
  • 4. īƒ˜ The inorganic compounds used topically are broadly * categorized on the basis of their usual action or use e.g. * (i) protective's and adsorbents, * (ii) antimicrobial, * (iii) astringent and * (iv) Sulphur and its compounds * (v) miscellaneous compounds. 4
  • 5. Topical agents:- 1] Protectives and adsorbents.e.g.talc, silicone polymers, titanium dioxide, calamine, zinc oxide. 2] Antimicrobial agents. īƒ˜ Hydrogen peroxide, Potassium permanganate, Sodium per borate. īƒ˜ Iodine & iodine preparations, Chlorinated lime, sodium hypochlorite solution, E.g. Boric acid, Borax, Silver & Silver compounds, Mercury compounds. 5
  • 6. 3] Astringents. E.g. Zinc chloride, Zinc sulphate, Aluminium sulphate, Alum, Aluminum sub acetate solution. 4] Miscellaneous compounds. E.g. sulphur & sulphur compounds. 6
  • 7. (i) Protective's and adsorbents :- protective's are the agents that cover the skin or mucous membrane from possible irritants. MOA:- o Some substance are of insoluble type & chemically inert, they act by forming a coat or film on the skin. o They absorb moisture decreases mechanical friction and irritation and also discourages certain bacterial growth. o Dusting powder is in the state of fine division form adherent continuous film on intact skin & exhibit protective action. 7
  • 8. Adsorbents:- â€ĸ Some chemically inert substances adsorb dissolved or suspended particles or gases, toxins etc are known as adsorbents . MOA:-Adsorbents' are mainly used internally to prevent the irritant & unwanted effects on mucous membrane. ī‚§ Some inorganic chemicals possesses both protective & adsorbent properties on topical application. â€ĸ 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.8
  • 9. Some of the inorganic protective compounds and preparations are described here: 1) TALC Chemical formula :- 3Mgo. 4siO2.H20 Synonym:- soapstone or French chalk, purified talc īƒ˜ Talc is the softest material Properties:- īƒ˜Colour: White/greayish white īƒ˜Odour:-odourless. īƒ˜Nature:-fine powder īƒ˜Taste:-tasteless īƒ˜Touch:-greasy or unctuous & adheres to skin īƒ˜Solubility:-soluble in water, dil. acids & bases 9
  • 10. Storage:- In well closed container. PREPARATION a)prepared by boiling fine powered talc with Dil HCL & allowing to settle. b)the supernatant liquid is removed c) the talc is washed thoroughly with water to make it free from acid. ( Acid treatment remove impurities from talc.) 10
  • 11. 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 / untouch to touch therefore used as lubricant or protective. 5)It is used as excipient, lubricant& filler for tablet & pills 11
  • 12. 2) ZINC OXIDE 1)Chemical formula:-ZnO 2) Mol wt : 81.38 3) Properties:- īƒ˜Colour: White/yellowish white īƒ˜Odour:- Odourless. īƒ˜Nature:-fine amorphous powder īƒ˜Solubility:-Insoluble in water & alcohol soluble in NH3. īƒ˜Storage:- Zinc oxide absorbs carbon dioxideâ€Ļ. ? 12
  • 13. PREPARATION a) 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 b) 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
  • 14. ASSAY īƒŧ ZnO is insoluble in water therefore cannot directly titrated with acid. īƒŧ it is dissolved in excessive of acid & back titrated. īƒŧAmmonium chloride is used in titration to prevent ppt īƒŧWhite ppt interferes in end point īƒŧMethyl orange is used as an indicator ZnO + H2SO4 ZnSO4 + H2O H2SO4 ( Excess) + 2NaOH Na2SO4+ 2H2O 14
  • 15. USES:- â€ĸ Mild Antiseptic & Astringent. in form of lotions, ointment paste or dusting powder. â€ĸ in treatment of urticaria, aczema,sunburns â€ĸ in combinations with other antimicrobial agents Eg Talc â€ĸ primary ingredient in calamine. â€ĸ pharmaceutical aid in mfg of adhesive tapes, bandages. â€ĸ It is used in the treatment of eczema, ring worm, pruritus and psoriasis 15
  • 16. 3) CALAMINE 1. Chemical formula:- ZnC03.Zn(OH)2¡xFe2O3 2. STD:- After ignition, it contains not less than 98.0% and not more than 100.5% of ZnO. 3. Properties:- īƒ˜Colour: pink or reddish brown powder īƒ˜Odour:-odourless. īƒ˜Nature:-fine powder & amorphous īƒ˜Taste :- tasteless īƒ˜Solubility:-Practically insoluble in water, almost completely soluble in mineral acids with effervescence. īƒ˜NOTE The presence of ferric oxide gives the substance a pink colour (for cosmetic reasons). 16
  • 17. Preparation ī‚§ Calamine is obtained by calcination( powdered by heating) of the natural native zinc carbonate. ī‚§ prepared by mixing zinc oxide with ferric oxide ī‚§Sieved & fine powder is collected. Assay ī‚§An ignited & cooled sample is dissolved in excess acid H2SO4 (1 N) & filter. ī‚§ residue washed with hot water to free from acidity. ī‚§Ammonium Chloride is added to prevent ppt of ferric hydroxide during titration) & titrated with NaOH (1N) using methyl orange as indicator. 17
  • 18. 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. 18
  • 19. 4) ZINC STEARATE 1)Chemical formula:- CH3 (CH2)16CO2) 2 Zn 2)STD:- After ignition, it contains not less than12.5% and not more than 14.0% of ZnO. 3) Properties:- īƒ˜Colour: White īƒ˜Odour:-faint characteristic. īƒ˜Nature:- light fine bulky powder free from grittiness īƒ˜Taste :- tasteless īƒ˜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. 19
  • 20. ASSAY īƒ˜Analyzed by complexometry method. ī‚§An ignited & cooled sample is dissolved in excess acid H2SO4 (1 N) by boiling. ī‚§ residue washed with water to free from acidity. ī‚§Combined the filtrate & titrated against disodium EDTA solution using ammonia, ammonium chloride buffer &eriochrome black T as an indicator. 20
  • 21. USES â€ĸ Astringent & Antimicrobial. â€ĸ Soothing& protective agent & used in dusting powder ointment creams in treatment of inflammatory condition. â€ĸ Used in skin problems where large amount of water is exuded becoz it will not form patches. â€ĸ used as lubricant in the processing of tablets. â€ĸ NOTE:-causes pulmonary inflammation if inhaled . 21
  • 22. 5) TANIUM DIOXIDE 1)Chemical formula:- TiO2 2)Mol.Wt :-79.90 3)STD:-It contains not less than 98% of TiO2 W.R.T. to dried substance Properties:- īƒ˜Colour: White īƒ˜Odour:-odourless. īƒ˜Nature:-Amorphous & fluffy powder īƒ˜Taste :- tasteless īƒ˜Solubility:-. practically soluble in water, & in dil mineral acid it dissolves slowly in Hot H2SO4.22
  • 23. ASSAY īƒ˜ It is analyzed by complex metric titration. īƒ˜Sodium edetate back titration method. īƒ˜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. 23
  • 24. 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 colour it is used in cosmetic preparation & in paints. 24
  • 25. 6) Silicon Polymers Synonyms:-Dimethicone, Simethicone, Dimethicone, polysiloxne , silicone oils. Properties & uses of Silicones â€ĸ The silicone polymers are generally known as silicone oils. â€ĸ The silicone polymers are prepared synthetically by polymerization reaction. â€ĸ The oily nature of these compounds makes it useful as water repellent and protective to skin from contact irritants. â€ĸ The silicone oils, thus in general act as protective, it also act as an Antiflatulents and used in varying amount in antacid preparations. 25
  • 26. â€ĸ Dimethicone: â€ĸ It is an inert silicone, oily in nature, it is stable and has low surface tension. â€ĸ It forms a protective layer on skin like plastic and acts as water protective agent. â€ĸ It is mainly used in ointments, sprays, lotions and creams. Simethicone : ī‚§ It occurs as a light gray, translucent liquid with greasy consistency. It is prepared from dimethylpolysiloxane. ī‚§It is used as an Antiflatulents and is employed in antacid, antispasmodic, sedative and digestant preparations in 40 - 80 mg dose at bed time. 26
  • 27. ANTIMICROBIAL AGENT â€ĸ Is a broad terminology describing activity against microbes. â€ĸ Antimicrobials are the chemical agents used to destroy or inhibit the growth of pathogenic micro-organism. â€ĸ They are normally ineffective in the sporing state of microorganism. Disinfectants -are substances that are applied to non-living/inanimate objects to destroy microorganisms that are living on the objects. E.g. Chlorinated lime, potassium permanganate, formaldehyde, phenol etc. Antiseptic: They are antimicrobial substances that are applied to living tissue/skin to reduce the possibility of infection, sepsis. e.g. Hydrogen peroxide, potassium permanganate, Iodine, Povidone iodine etc. 27
  • 28. Sterilization:-the complete destruction living microorganism including bacterial spores .it can be achieved by physical methods or by chemical means. Germicide:-the agents which are employed to kill M.O. it can be broad form germicidal,virucide,fungicide etc. Static:-stops the growth of M.O. Bacteriostatic:- The agent which primarily function by inhibiting the growth of bacteria. Thus, bacteriostatic drugs or agents do not kill but arrest the growth of bacteria. 28
  • 29. PROPERTIES 1.It should have antiseptic or germicide activity & not bacteriostatic activity because if M.O are not killed , they may grow & cause infection. 2.To reduce incidence of resistance it should have rapid onset of action & sustain activity. 3. Have good therapeutic index. 4.Should not produce local cellular damage or should not interfere with body defense. 5. It should show no systemic toxicity from topical application. 6. It should have in general broad spectrum of activity against bacteria, fungi, protozoa, virus etc.29
  • 30. MECHANISM OF ACTION Antimicrobial is a broad terminology describing activity against microbes. Specific terminology describes exact mode or mechanism of action.e.g. Antiseptics, Disinfectant, Germicide bactericide' (against bacteria), 'fungicide' (against fungi), 'virucide' (against virus) etc. denotes exact action.),Bacteriostatic. Inorganic compounds generally exhibit antimicrobial action by, either of the three mechanisms viz. (i) Oxidation (ii) Halogenation (iii) Protein binding or Precipitation. 30
  • 31. 1.Oxidation Mechanism : īƒ˜Compounds acting by this mechanism belong to class of peroxide, peroxy-acids, oxygen liberating compounds like permanganate and certain oxo-halogen anions. īƒ˜ They act on proteins containing sulphadryl group and oxidizes free sulphadryl to disulphide bridge and inactivate its function. 2. Halogenation Mechanisms: īƒ˜ Compounds which liberate chlorine or hypochlorite or iodine act by this mechanism. īƒ˜ This category of agents act on peptide linkage and alter its potential and property. īƒ˜The destruction of specific function of protein results in death of microorganisms. . 31
  • 32. 3. Protein Precipitation : ī‚§ Many metals in their cation form exhibit protein binding or protein precipitation. ī‚§ The nature of interaction with protein occurs through polar group of protein which acts as ligands and metal ion acts as Lewis acid. ī‚§ The complex formed may be a strong chelate leading to inactivation of protein. ī‚§ This action in general is non-specific. Protein precipitants do not distinguish between the protein of microbes and that of host. ī‚§ Germicidal action results when the concentration of ion is such that reaction is restricted largely to the parasite cell 32
  • 33. Various antimicrobials and astringents are classified as under: īąOxidative Antimicrobial agents e.g. Hydrogen Peroxide Solution, Zinc Peroxide, Sodium Perborate, Potassium Permanganate, Sodium Hypochlorite Solution, Chlorinated Lime. īą Iodine Preparations and Compounds e.g. Iodine and Iodine Solutions, Povidone-Iodine. īą Protein Precipitant Antimicrobial Agents e.g. Silver Nitrate, Mild Silver Protein. īą Mercury Compounds e.g. Yellow Mercuric Oxide, Ammoniated Mercury, Mercuric Chloride. īą Sulphur and Sulphur compounds e.g. Sublimed Sulphur, Precipitated Sulphur, Sulphur Dioxide, Sulphureted Potash, Selenium Sulphide, Cadmium Sulphide. īą6. Boric acid and Borax. Sodium Borate īą7. Arsenic Compounds e.g. Carbarsone, Glycobiarsol, Tryparsamide. īą8. Antimony Compounds e.g. Antimony Sodium Gluconate, Stibophen.33
  • 34. Hydrogen Peroxide:- 1)Chemical formula:- H2O2 2)Mol. Wt :-34.02 Properties:- īƒ˜Colour: colorless īƒ˜Odour:-odourless. īƒ˜Nature:- Clear liquid īƒ˜Taste :- slightly acidic īƒ˜Solubility:-. practically soluble in water, & in dil mineral acid it dissolves slowly in Hot H2SO4 34
  • 35. The Solution usually deteriorate upon standing upon agitation Rapidly decomposes when in contact with many oxidizing or reducing sub. 2H2O2 2 H2O + O2 Solution is stabilized by 1) By addition of small qty of acid & by adjusting the pH between 2 to 3. 2) Some Stabilizers like acetanilide, quinine, sulphate, 8- hydroxyquinoline & others complexing /chelating agents are used in 0.02 to 0.05% con range. 35
  • 36. Principle: īƒ˜This assay is based on Oxidation Reduction (Permanganate) type of titration in which solution of potassium permanganate is acts as an oxidizing agent and hydrogen peroxide also acts as an oxidizing agent But in presence of strong oxidizing agent like potassium permanganate hydrogen peroxide acts as reducing agent. īƒ˜The ability of potassium permanganate solution to oxidize is due to conversion of the MnO4 - ion to Mn++ in acidic solution but MnO4 - ion is reduced by reducing agent like hydrogen peroxide. īƒ˜Solution containing MnO4 - ion are purple in color , solution of salt containing Mn++ ions are colorless, hence permanganate solution is decolorized by reducing agent as longer as MnO4 - is present in the solution. 36
  • 37. The moment there is an excess addition of potassium permanganate solution becomes purple, thus potassium permanganate acts as a self indicator. Reactions: In this assay dilute sulfuric acid is used for conversion of MnO4- to Mn++ MnO4 - + 8H+ + 5e Mn+2 + 4H2O Chemical reaction for assay: 2KMnO4 + 3H2SO4 + 5H2O2 2MnSO4 + K2SO4 + 8H2O + 5O2 37
  • 38. Uses 1) The primary use is a mild oxidizing antiseptic. This action comes when it comes in contact with abraded tissue It is a mild oxidizing antiseptic action the antiseptic action is associated with mechanical cleansing provides by rapid foaming release of oxygen. Helps in removal of dirt , bacteria from cuts & wounds & acts as cleaning antiseptic. 2) It destroy most pathogenic bacteria. 3) Its 1.6% solution is used as deodorant, gargle and mouth wash. 4) It is used as an antidote in phosphorous and cyanide poisoning. 5) It is used for bleaching the hair. 6) It is used in treatment as ear wash & vaginal douches. 38
  • 39. Storage:- â€ĸ It is stored in container protected from light, in bottles closed with glass stoppered or plastic caps provided with vent for the escape of oxygen. â€ĸ Keep in cool place. â€ĸ The label should indicate whether it contains stabilizing agent or not. 39
  • 40. 2)Potassium Permanganate Chemical Formula:-KMnO4 Mol Wt:-158.03 Physical Properties:- īƒ˜ Colour: Dark Purple īƒ˜Odour:-odourless. īƒ˜Nature:- metallic prisms, almost opaque with blue metallic lustered īƒ˜Taste :- sweet īƒ˜Solubility:-. practically soluble in water, & more in boiling water. 40
  • 41. Chemical properties:- īƒ˜ When heated it decomposes at high temp ( 240°C) 2KMnO4 K2MnO4+MnO2+O2 īƒ˜ It is a powerful oxidizing agent in acidic solution it is reduced from Mn+7 to Manganious ion Mn+2 with evolution of O2. 2KMnO4 + 3H2SO4 K2SO4 + 2MnS04 + 3H20 + 5[O] īƒ˜ In neutral or alkaline media also O2 is liberated .It brings bleaching Action. īƒ˜ KMnO4 oxidize alcohol to Aldehyde īƒ˜ Sulphide to Sulphur īƒ˜Ferrous Salt to Ferric īƒ˜Nitrites to nitrates īƒ˜Iodide to free iodine in acidic condition 41
  • 42. Assay:- Oxidation Reduction Reaction īƒ˜ known Wt of sample is dissolved in water & vol made to 250ml. īƒ˜ To 25ml of 0.1N oxalic acid added 5ml H2SO4 & warms to 70Âē C& titrated with prepared solution of KmNO4 (temp is not maintained at 70Âē C the reaction will be slow) īƒ˜The permanganate should be taken in the burette and the end point is appearance of a pale pink color. 42
  • 43. īƒ˜ Incompatibility It is incompatible with iodides, reducing agents and most organic matter. īƒ˜Storage:- It should be stored in tightly-closed container &should handled with care since explosion may occur when it comes in contact with oxidisable substance 43
  • 44. Uses:- 1. It is a topical anti-infective (antibacterial and anti- fungal). (anti-infective due to the oxidizing property.) 2.It stains the skin & tissues. Sol in 1:5000-1:15000 conc. it is used in cleaning wounds & ulcers for skin infection caused by bacteria & fungi. 3. It is also used as an antidote in barbiturate & alkaloidal poisoning. (A sol of 1: 5000 when used as gastric wash, oxidises poison & prevents their absorption.) 44
  • 45. Compound acting by Halogenation Mechanism:- 1.CHLORINATED LIME:- Chemical formula Ca(ClO)2 Synonym Bleaching Powder, Chloride of Lime. Physical Properties: Colour:- white powder Odour:- characteristic odour Solubility:- slightly soluble in water and in alcohol. Storage: It should be stored in tightly closed containers. It is affected by moisture & heat. 45
  • 46. īƒ˜Preparation:- It is manufactured by the action of chlorine on calcium hydroxide i.e.. The slaked lime is spread on shelves in suitable container Chlorine gas is introduced at the top of chamber & passed through the contents of the shelves. this is usually done at 25° thus minimizing the formation of calcium chloride. when abs of chlorine is completed, powdered lime is blown into the chamber to absorb the excess of chlorine. 46
  • 47. USES:- -It is used as disinfectant & bleaching agent. -It shows bactericidal action. -It is used to disinfect faeces, urine , sputum& other organic material. -It is employed for disinfecting drainages. -It is a powerful bleaching agent .Its powerful bleaching action must be considered while disinfecting coloured materials. -it is used as 1-2 g/l for sterilization of water. The treated water should be exposed to air & allowed to settle before use. -Chlorinated lime is used in the preparation of surgical chlorinated soda solution, employed as a wound disinfectant. 47
  • 48. Properties of Boric acid- 1. It is a white, colorless crystalline powder, odorless, unctuous to touch. 2. It has bitter, sweetish after taste 3. It is soluble in alcohol, freely soluble in glycerin, propylene glycol and boiling water 4. Stable in air 5. On heating at 1000C it is converted in to Metaboric acid, at 1600Cin to tetra boric acid and at more than 1600C boric acid is converted in to boron trioxide. 6. Boric acid is very weak acid, so it cannot be titrated accurately with standard alkali. Hence glycerin is added in its titration. Storage of Boric acid- It should be stored in air-tight, well closed container. 48
  • 49. Uses of Boric acid- 1. It has weak bacterciostatic and fungi static action 2. It is used as local anti-infective drug in the form of cream, ointment and lotion 3. Buffer in topical preparations 4. Vehicle for ophthalmic solution 5. Boric acid is useful as Suppositories base 6. It is also used to impregnate surgical dressings 49
  • 50. BORAX ī‚§ Chemical formula Na2B4O7. 10 H2O īƒ˜ Synonym:- Sodium Borate īƒ˜ Properties:- īƒ˜Colour:-Colourless transparent crystals īƒ˜Odour:-odourless, īƒ˜Taste:- saline and alkaline taste īƒ˜Solubility:- It is soluble in water and glycerin but insoluble in alcohol. īƒ˜Chemical Properties:- īƒ˜ On heating loses all its water of hydration & swells to a white porous powder. īƒ˜ When heated to red hot & on cooling , forms a transparent mass known as borax bead 50
  • 51. īƒ˜ An aqueous sol of Na borate is alkaline to litmus . īƒ˜Alkali borate are water soluble. īƒ˜Borates of other metals undergo hydrolysis & forms insoluble , hydroxides or oxides. Action & Uses:- It has been used externally in solutions containing 1 to 2% of borax as an eyewash, gargle in mouthwashes and as a wet dressing used in food preservative īƒ˜ cosmetics, it is used as emulsifier & also in lotions. germicide & bacteriostatic. 51
  • 52. Iodine īƒ˜ Chemical formula :-I2 īƒ˜ Mol wt : 253.8 Properties:- īƒ˜ Colour:-grayish-violet or bluish-black īƒ˜ Nature:-brittle plates or small crystals with a metallic luster. īƒ˜ Odour:-It possesses a distinctive penetrating irritant īƒ˜ Taste:-bitterly pungent taste. īƒ˜Solubility:-It is very slightly soluble in water, soluble in alcohol and dissolves freely in ether, chloroform and carbon disulphide. It dissolves readily in sol of KI & other iodides forming compound as KI3. 52
  • 53. Chemical Properties:- 1.It melts at 1400C but sublimes freely at temp below its MP. 2. It is volatile at R.T & its vapours attack both cork & rubber. 3.The imp chemical property of iodine in aqueous sol is that a mild oxidizing action mediated through the formation of hypoiodous acid. Storage:- Should be stored in well- closed bottles fitted with glass stoppers because I2 is volatile & its vapors attack both cork & rubber. Incompatibility:- with alkalis and alkali carbonates. 53
  • 54. Uses:- 1) Topical anti-infective iodine has a powerful bactericidal action and is used for disinfecting unbroken skin before operation. 2) Iodine ointments are applied as counter-irritants. 3)Its.2% solution in glycerol is used for application to mucous membrane 4)compound iodine paint is used as a throat paint in pharyngitis and follicular tonsillitis. 5) Iodine is an essential trace element in human diet. Deficiency of iodine leads to development of goiter and in many countries, common salt which is used for food purpose is iodized mainly with iodides. 54
  • 55. Solution Of Iodine:- īƒ˜ The germicidal activity of free iodine is about six times that of hypoiodous acid. īƒ˜ Preparations providing free iodine are bactericidal, fungicidal, amoebicidal and virucidal. īƒ˜ Iodine is effective in very dilutions. īƒ˜ Iodine Solutions and Iodine Tincture are most effective topical agents available. ī‚§ They have been used as antiseptics on the skin prior to surgery. 55
  • 56. Some of the well-established solutions are: ī‚§ 1)Aqueous Iodine Solution B.P./I.P. (1966) (Strong Iodine U.S.P.) īƒ˜ It is also known as Lugol's solution. īƒ˜It does not contain any alcohol. It contains 5.0% w/v of Iodine and 10.0% w/v of Potassium Iodide. īƒ˜ The relative proportion of potassium iodide to iodine is much higher than in weak solution. īƒ˜Uses: Source ¡of Iodine. 56
  • 57. 2)Strong Iodine Solution I.P. (1966) It contains 10.0% w/v of Iodine and 6.0% w/v of Potassium Iodide in alcoholic solution, composition: Iodine 100 g, Potassium Iodide 60 g, Purified water 100 ml; Alcohol (90%) sufficient to produce 1000 ml' Uses: Antiseptic. 57
  • 58. 3) Weak Iodine Solution B.P/I.P. (1966):- It contains 2.0% w/v of Iodine 2.5% w/v of Potassium Iodide in water. This solution is identical in composition with Tinctura iodi Mitis B.P. 1914. es. Uses: Antiseptic. 58
  • 59. 4) Iodine Tincture U.S.P. : It contains 2.0% w/v of Iodine and 2.4% w/v of Sodium Iodide in much diluted alcoholic solution. Note-Iodine preparations of any type are contraindicated in patients who have exhibited prior allergy or hypersensitivity to iodine. 59
  • 60. Povidone-Iodine īƒ˜ Povidone-Iodine is a complex of iodine with Povidone (a polymer) also known as polyvinylpyrrolidone or PVP. īƒ˜ Products are available under different names in concentrations of 0.1 to 1 % of available iodine. (usually 10% of the total concentration of Povidone- Iodine). īƒ˜Povidone-Iodine belongs to iodophors. īƒ˜ Iodophors are complexes of iodine with carrier organic compounds serving as a solubilizing agent, which slowly liberate iodine in solution. 60
  • 61. Properties īƒ˜ Colour:-Yellowish brown īƒ˜ Odour:- slight characteristic odour īƒ˜Nature:- amorphous powder īƒ˜ Solubility:-It is soluble in water and in alcohol, but practically insoluble in organic solvents. īƒ˜Chemical properties :-Aqueous solution is acidic to litmus. īƒ˜ The Povidone-Iodine solution is reddish Brown colour, and a pH of not more than 6.0. īƒ˜ Its non-irritating effects on tissue, comparatively low oral toxicity, its water solubility and its low iodine vapour pressure making it stable to possible iodine loss makes it superior to Iodine Solutions. īƒ˜ Solution in most of the applications. Solutions are nonstaining and can be washed clear from skin and clothing. Storage :-It should be stored in air-tight containers (tightly closed containers), the materials of which are resistant to iodine.61
  • 62. Uses â€ĸ Antiseptics for surgical scrubs and pre-operative antisepsis of the skin. â€ĸ It is also used in gargles and mouthwashes for the treatment of infections in the oral cavity. â€ĸ Various preparations include an aerosol (0.5%), solutions (usually 1%), a surgical scrub (0.75%), a vaginal douche (1%) and a vaginal gel (0.1%). 62
  • 63. Protein precipitant Antimicrobial SILVER NITRATE Chemical formula:- AgNO3 Mol wt : 169.89 preparation:- īƒ˜ It is prepared by the action of hot nearly concentrated nitric acid on pure silver. īƒ˜ 3 parts of silver are added to a sol 25% nitric acid ( about 10 parts) heated to expel the nitrous fumes,filltered & evaporated until it is dry. īƒ˜ then the mass is fused to convert the copper nitrate into insoluble oxide. So obtained product is dissolved in hot water, filtered it & kept aside in dark place for crystallization. īƒ˜ crystals are collected on sintered glass crucible & dried at 50°c in dark. īƒ˜Purified of AgNO3 is costly therefore pure silver & nitric acid free from halogen & sulphur is used. 63
  • 64. Properties īƒ˜Colour:-White īƒ˜ Odour:- odourless īƒ˜ Nature:-Rhombic crystals īƒ˜ Taste:- Bitter taste īƒ˜ Solubility:-Very soluble in water īƒ˜Sparingly soluble in alcohol, freely soluble in boiling alcohol It becomes grey/greyish black . īƒ˜ On exposure to light in presence of organic matter, due to liberated silver. Chemical Properties:- īƒ˜ 1% sol has PH between 4.5- 6 īƒ˜ 4% sol has bet 5.4- to 6.4 īƒ˜ at 212° C it melts to a slightly yellow liquid which on cooling congeals to a white crystalline mass. īƒ˜ At high temp is slowly decomposes evolving oxides of nitrogen. it produces chemical reaction of silver ion & nitrate ion. 64
  • 65. īƒ˜ Sol of AgNO3 gives white- yellow –white ppt with HCL & other halogen containing salts. īƒ˜ The silver halide ppt is insoluble in dil acids but dissolve in ammonia. Storage :- īƒ˜ Should be stores in tightly closed light resistant non metallic containers . īƒ˜ Sol should be freshly prepared & supplied in amber Coloured bottles. 65
  • 66. Incompatibility:-incompatible with reducing agent, Tartarates, Sugar, Tannins, Alkali halogen acids & their salts. Uses:- 1) Antibacterial in conc. from 0.01 to 0.5% 2) In higher conc 1% above it has astringent, irritant property on tissues . 3) AgNO3 ophthalmic sol 1% is used in eyewash, 0.5% aq sol for treating burns injuries & in wet dressings. 4)Its effective against coccol infections 66
  • 67. Mild Silver Protein Chemical formula :-Variable It is a silver rendered colloidal by the presence of, or in combination with protein . Properties:- Colour:- dark brown or almost black Odour:- odourless Nature:- shining scales or granules Solubility:-It is freely soluble in water, but almost insoluble in alcohol, chloroform and ether. Storage:-It is affected by light therefore should be protected from light. 67
  • 68. Action & uses:- 1) 0.5% to 20% sol is used as antibacterial. the release of Ag+ ions tends to increase with dilution & therefore more dilute sol becomes irritating. on aging sol becomes more irritant & a ppt is formed. therefore sol of mild silver protein should be always prepared freshly which contain suitable stabilizers. Uses:- Uses:- â€ĸ The Solution due to its low irritability usually employed as local antibacterial on mucous membranes in nose, throat, & conjunctiva of eye. â€ĸ for irrigation of urethra & bladder. â€ĸ its major effectiveness in the treatment of gonococcal infection. Also used in respiratory tract infections & also as prophylactic against respiratory infection. â€ĸ Mercury with chalk act as purgative due to irritant action of Hg ion. â€ĸ As it is toxic it is not used medicinally. â€ĸ best bacteriostatic. note:- Prolonged use of mild silver protein may result in darkening of skin due to the deposit of free silver below epidermis.68
  • 69. Mercury Synonym:-Hydragyrum , quick silver (Hg) īƒ˜ Colour:- bright shiny silvery White īƒ˜ Odour:- odourless īƒ˜ Nature:-liquid at room temp Storage :- īƒ˜ Should be stores in tightly closed containers . īƒ˜Action & uses:- īƒ˜ Cathartic & parasiticide īƒ˜Also used in the treatment of syphilis & as diuretic īƒ˜ But it is extremely poisonous & prolonged inhalation in minute quantity may be fatal. 69
  • 70. Yellow Mercuric Oxide Chemical Formula:-HgO Mol.Wt: 216.6 īƒ˜ Colour:-Yellow to orange according to temp at time of preparation īƒ˜ Odour:- odourless īƒ˜ Solubility:- in Soluble in water& alcohol but soluble in acids Storage :- īƒ˜ Should be stores in tightly closed containers .protected fro light īƒ˜ Chemical properties:- īƒ˜ Stable in air īƒ˜ form red oxide slowly develops on exposure to light. 70
  • 71. Action & Uses:- īƒ˜ local antibacterial. īƒ˜ also mild antiseptic action used in ophthalmology for treating no. of inflammatory conditions. īƒ˜ also used for the treatment of fungal infection of the skin & infestations of body lice. 71
  • 72. Ammoniated Mercury Chemical formula:-NH2 .HgCl Synonym:- Amminochloride of mercury, white precipitate īƒ˜ Mol.wt- 252.1 īƒ˜ Colour:- White īƒ˜ Solubility:- Insoluble In water, alcohol, ether. Storage :- īƒ˜Should be the amber colored container (on exposure to light it darkens). Action & uses:- 1) acts as mild antiseptiC (slow release of mercuric ions.) 2) topically used in treatment of various skin infections caused by fungi, lice & other infestations. 3) Commonly employed in 5% strength as ointment & also as dusting powder. 72
  • 73. Sulphur & its compound * Elemental Sulphur exist in various allotropic forms including several solid and two liquid states namely: *It occurs in free form & also sulphides & Sulphate Sulphur & * its compound have many use p,’ceutical & medicinal fields. *Solid as Rhombic (Îą-Sulphur, SÎą, Sublimed Sulphur or Flower of Sulphur), and Monoclinic (β-Sulphur, Sβ); Liquid as Îģ-Sulphur Plastic Sulphur and Amorphous Sulphur (formed on aging of "plastic" sulphur). *Elemental Sulphur is little use internally MOA:-but it is use topically as antibacterial. elemental sulphur acts either due to the oxidation-reduction products of the element [e.g. sulphides) *The sulphur "candles" when burned, give off sulphur dioxide for fumigation or insecticide purposes. * Sulphides are used as depilatories, due to the ability of sulphides in highly alkaline solution (pH 10) to reduce the disulphide linkage in the amino acid cysteine in hair. The reduction and softening of the hair help in its removal. 73
  • 74. medicinally used Sulphur compound are PRECIPITATED SULPHUR īƒ˜ Chemical symbol S Atomic wt. : 32.6 īƒ˜ Synonym:- flower of Sulphur, milk of sulphur Preparation:- īƒ˜ By Sublimation process (Any form of Sulphur is heated vapors produced which are condensed.) īƒ˜ In refinery the molten Sulphur is placed in iron retorts which communicate with the stone chambers. īƒ˜ When Sulphur vapors enters the stone chambers they ignite & convert into Sulphur dioxide. īƒ˜ The subsequent vapor pass through relative cold gas & condenses on walls & floors of the chambers in fine crystalline form. 74
  • 75. Properties:- īƒ˜ Colour:-Yellow īƒ˜ nature:- Fine crystalline powder īƒ˜ Odour :-Odourless īƒ˜Tasteless īƒ˜ Solubility:-insoluble in water and in alcohol. Uses:- īƒ˜ Used as an ingredient in sulphur ointment & used as scabicide. īƒ˜Used in the treatment of acne, pimples and psoriasis īƒ˜Act as kerotolytic agent 75
  • 76. Precipitated Sulphur U.S.P ( Solid allotropic form of Sulphur) īƒ˜ properties: īƒ˜ Colour:-pale yellow īƒ˜ Odour:-odoureless īƒ˜ Taste;- Tasteless īƒ˜ nature:- very fine īƒ˜ Solubility;- very slightly soluble in alcohol & slightly soluble in olive oil. 76
  • 77. Uses:- 1.Sulphur is a mild antiseptic and Parasiticide and has been widely in the of lotions and 10% ointments for treatment of scabies & acne . employed as fungicides in the treatment of superficial fungal infections. 2) Sulphur is also used mainly as a dermatological agent to treat seborrhea s , psoriasis. 3)It may be used alone or in conjunction with other keratolytics . 4) Precipitated Sulphur is converted in the small intestines into alkali sulphides which produce a mild laxative effect due to their irritant action. 5)also used in homoeopathic medicines. Note-Some patients may be hypersensitive to sulphur and should be observed for any allergic manifestations. 77
  • 78. Selenium Sulphide Chemical formula -SeS2 Synonym Selenium Disulphide Mol.wt-143.09 Preparation;- Prepared by passing H2S into selenious acid.by adding selenious acid to a saturated solution of H2S PPT is collected & dry. Properties. colour;-orange to reddish brown odour:- faint odour of hydrogen sulphide nature:- powder solubility:-in water & inorganic solvents in HNO3 with formation of selenious & sulphuric acid 78
  • 79. 1 Selenium sulphide is used as antidandruff. 2. Selenium Sulphide used in 1 to 2.5 % as anti seborrheic 3. 5-10ml of 2.5% suspension to be applied on scalp. after application it is allowed to remain in contact for 5 min & it is washed off. 4.Longer exposure produce irritation care should be taken ,not to introduce in eyes or mouth as it is highly toxic. 79
  • 80. Astringent īƒ˜Astringents are locally applied protein precipitants which have a low cell permeability so that the action is limited essentially to the cell surface and the interstitial spaces. īƒ˜The action does not result in the death of the cell, only the permeability of the cell membrane is reduced. 80
  • 81. Astringents are therapeutically used as (i) Styptic, to arrest haemorrhage (to stop bleeding from small cuts) by promoting coagulation of blood and constricting small capillaries; (ii) antiperspirant to decrease sweating by constricting pores at the surface of the skin; (iii) to reduce inflammation by restriction of the blood supply to the surface of mucous membranes; (iv) promote healing and toughen the skin; (v) deodorant by virtue of interaction with odorous fatty acids liberated or produced by the action of bacteria on lipids in sweat and by an action suppressing bacterial growth, partly due to a decrease in pH; and (vi) direct action on skin to remove unwanted tissue (this requires a higher concentration or a stronger protein precipitant, often termed as corrosive). 81
  • 82. Most topical astringents are salts of aluminium, zinc & to some extent Zirconium. Alum :-KAI(SO4)2 12H2O Mol wt :- 474.33 (Aluminium Potassium Sulphate) Mol wt. 453.33 (Aluminium Ammonium Sulphate), Mol Wt:- 474.39 Alum can be either the ammonium or the potassium salt & should be labeled on container which salt is present. 82
  • 83. Preparation:- official alums are prepared by adding a hot, concentrated solution of either potassium or ammonium sulphate to a hot solution of an equimolecular proportion of aluminium sulphate. The alums separate out as crystals on cooling. Properties:- Colour:- colourless Nature:- large crystals, crystalline fragments or as a white powder. odour:- odourless taste:-with a sweetish strongly astringent taste. Solubility:- Alums are freely soluble in water, but slowly dissolve in glycerin, and insoluble in alcohol. 83
  • 84. Chemical properties:- Acidic to litmus When heated, it melts and at about 200°C looses its water of crystallization with the formation of the anhydrous salt. Storage:-To be stored in airtight containers. 84
  • 85. Uses:- īƒ˜ Alum precipitates proteins and is a powerful astringent. īƒ˜ Dilute solutions (l to 4%) have been¡ used as astringent mouthwashes and gargles but they have a destructive action on teeth. īƒ˜A 2% solution has been used for application to the skin to reduce excessive perspiration. īƒ˜ Stronger solutions (5 to 10%) are used to harden skin by athletes, especially as footbath to toughen the skin of the feet. īƒ˜ strong solution is used as a styptic for minor cuts and abrasions. īƒ˜(0.5 to 5%), lotions and douches, some vulvovaginal cleansing and deodorant preparations. 85
  • 86. ZINC SULPHATE Chemical formula :-ZnS04.7H20 Synonym:- White Vitriol Preparations īƒ˜ For industrial scale, zinc sulphide is heated in presence of air under specified conditions.the heated mass is dissolved in hot water, filter the solution concentrated for crystallization. īƒ˜ metallic zinc granules are digested with H2SO4. īƒ˜ The sol is filtered & treated with chlorine to oxidize any ferrous impurity into ferric sulphate which is then ppted by hydroxide & removed. the filtrate is concentrated & crystallized 86
  • 87. Properties:- īƒ˜ Colour:- colorless, īƒ˜ Nature:-transparent crystals or as crystallline powder. īƒ˜ Odour:- is odourless īƒ˜ taste:- metallic and astringent. īƒ˜ Solubility:- very soluble in water. It is freely soluble in glycerin, but is insoluble in alcohol it īƒ˜ Chemical Properties:- īƒ˜ Aqueous solutions of zinc sulphate are acid to litmus īƒ˜ It forms double salts with ammonium & Potassium Sulphate īƒ˜ When strongly heated it decomposes īƒ˜ Storage It should be stored in tightly closed containers. īƒ˜ Incompatibility :-It is incompatible with alkali carbonates and īƒ˜ hydroxides and with astringent infusions and decoctions. 87
  • 88. uses:- īƒ˜ Zinc ions exhibit mild germicidal astringent & styptic action īƒ˜ ( the action is dependent due to slow release of zinc ions from salt or sol.) īƒ˜ Insoluble zinc ions used in topical agents as protectives. īƒ˜ ZnSO4 sol 0.1-1% used ophthalmic īƒ˜ Internally it is used as an emetic īƒ˜ Insoluble Zn complex are mainly used in bandages, adhesive, tapes etc. 88