MAKAUT/SEM 1/ PHARMACEUTICAL INORGANIC CHEMISTRY/ UNIT 3/GASTROINTESTINAL AGENTS_ANTIMICROBIAL
BY
KUNAL DATTA
ASSISTANT PROFESSOR
B.PHARM , M.PHARM
NETAJI SUBHAS CHANDRA BOSE INSTITUTE OF PHARMACY
3. Defination :
Any agents which either kills or inhibit the growth
of microbes i.e bacteria, fungi , protozoa etc.
Classification of agents:
ļ±Antiseptic
ļ±Disinfectants
ļ±Germicides
ļ±Keratolytics
ļ±Chemotherapeutics
4. ļ± Agents which prevent infection , by killing or
inhibiting the growth of micro-organism when
applied topically at damaged tissue.
ļ±The drugs like phenol , iodine , chloroxylenol ,
Boric acid , zinc oxide, cetrimide are the examples
of antiseptics.
Antiseptic
5. Disinfectants
ļ±Disinfectants are antimicrobial agents that are
applied to the surface of non-living objects to destroy
microorganisms that are living on the objects.
ļ±Commonly used disinfectants include cresol , phenol.
6. ļ±These are the agents which kills microbes.
Sub classification:
ļ¶Bactericidal agents- those kill bacteria
ļ¶Fungicidal- those kill fungus
Germicides
7. ļ±These are the agents which are applied on the skin
to soften the keratin.
Eg: Sulphur, Aluminium oxide
Use : They are used to treat acne and other skin infection
Keratolytic Agents
8. ļ±These are the chemical agents which are used in
clinical application of antimicrobial agents to treat
infection diseases.
Chemotherapeutics Agents
9. ļ¼ Must have a broad spectrum of action;
ļ¼ Rapid onset of action;
ļ¼ Should have a small latency period;
ļ¼ Should have a high activity;
ļ¼ Must be chemically resistant;
ļ¼ High availability and low cost;
ļ¼ Lack of local irritant or allergic effects on tissues;
ļ¼ Minimal absorption from the place of their application;
ļ¼ Low toxicity ;
Characteristics of antimicrobials Agents
10. ā¢ Microorganism contain many important āprotein
structureā (e.g enzyme) to survive.
ā¢ If there is minute changes in protein structure , the
protein becomes non functioning and inactive.
ā¢ There are three types of mechanisms for changing
their protein structure.
ļOxidation
ļHalogenation
ļPrecipitation of Protein
Mechanism of action : Antimicrobial Agents
11. ā¢ Oxygen liberating compound (Oxidizing agents) like
peroxide and peroxyacids , permanganate give action by this
mechanisms.
ā¢ These antimicrobial agents cause oxidation of active
functional group present in protein or enzymes and
inactivate them.
Mechanism of Action : Oxidation
12. ā¢ The halide and hypohalide (Iodine and Hypochlorite)
compounds give action by this mechanisms.
ā¢ This category of agents act on peptide linkage present in
protein or enzymes and there by changing the
conformational structure of protein.
Mechanism of Action : Halogenation
13. ā¢ Metal containg (e.g., mercury, arsenic and antimony)
compounds give action by this mechanisms.
ā¢ Metal binds with important group present in protein. This
protein metal complexation (Chelation) inactivates the
protein or enzymes.
Mechanism of Action : Precipitation of Protein
17. Physical Properties
ā¢ Appearance : purplish-bronze-gray needles
ā¢ Odor: Odourless
ā¢ Taste: Bitter with metalic taste
ā¢ Density : 2.703 g/cm3
ā¢ Melting point: 240 Ā°C
ā¢ Solubility: Freely soluble in water and alcohol
18. Chemical Properties
ā¢ Solid potassium permanganate decomposes when
heated :
ā¢ Potassium acts as strong oxidizing agents. KMnO4
oxidizes potassium iodide to iodine in acidic medium.
2KMnO4 ā K2MnO4 + MnO2(s) + O2
2KMnO4 + 10KI + 8H2SO4 ā 6K2SO4 + 2MnSO4 + 5I2 + 8H2O
19. Preparation
ļ±On a large scale, potassium permanganate is
prepared by mixing a solution of KOH with
powdered manganese oxide and potassium
chlorate. The mixture is boiled and evaporated to
yield the residue which is heated in iron pans until
it has acquired a paste like consistency.
KOH + 3MnO2 + KClO3ā K2MnO4 + KCl + 3H2O
20. Preparation
ļ± Potassium manganate when treated with Hydrochloric acid
3 K2MnO4 + 4 HCl ā 2 KMnO4 + MnO2 + 2 H2O + 4 KCl
ļ± Potassium manganate when treated with Carbon dioxide
3 K2MnO4 + 2 CO2 ā 2 KMnO4 + 2 K2CO3 + MnO2
21. Assay
ļ± Its assay is based upon the oxidation - reduction reaction.
ļ± Potassium permanganate is a strong oxidizing agent so it will be titrated
against oxalic acid which is a reducing agent.
ļ± An accurately weighed amount of about 0.8 g of sample is dissolved in
water.
ļ± Then it is diluted with water to 250 ml and titrated with 25 ml of 0.1 N
oxalic acid which is mixed with 25 ml of water and 5 ml of sulphuric acid.
ļ± This solution is maintained at about 70Ā°C temperature throughout the
entire titration.
5H2C2O4 + 2H2O + 2KMnO4 + 3H2SO4 ā K2SO4 + 2MnSO4 + 18H2O + 10CO2
22. Uses
ļ± Antiseptics in mouth wash preparation
ļ± wounds and skin infection
ļ± Oxidizing agents
ļ± urethritis
ļ± water treatment
ļ± Bleaching agent
ļ± 1-5% hydro alcholic solution of potassium permanganate used
as wet dressing.
25. Physical Properties
ā¢ Appearance : White crystalline solid or granular
ā¢ Odor: Odourless
ā¢ Taste: Sweet
ā¢ Density : 1.435 g/cm3
ā¢ Melting point: 170.9 Ā°C
ā¢ Solubility: Sparingly soluble in water, Slightly soluble in
Alcohol and Freely soluble glycerine.
26. Chemical Properties
ā¢ Boric acid is soluble in boiling water. When heated
above 100Ā°C, it dehydrates, forming metaboric acid
(HBO2) .
ā¢ When metaboric acid heated at 160Ā°C it converted
into tetraboric acid or pyroboric acid (H2B4O7)
ā¢ When pyroboric acid is heated above 200Ā°C it
decompose into boron trioxide (B2O3).
27. Preparation
Na2B4O7Ā·10H2O + 2HCl ā 4H3BO3 + 2NaCl + 5H2O
ļ±Boric acid may be prepared by reacting borax
(sodium tetraborate decahydrate) with a mineral acid,
such as hydrochloric acid.
ļ±In the laboratory, boric acid is obtained by adding a
mixture of conc. H2SO4 and water to a boiling solution
of borax.
Na2B4O7 + H2SO4 + 5H2O ā Na2SO4 + 4H3BO3
28. Assay
ā¢ It is assayed by a titrimetric methods.
ā¢ An accurately weighed quantity of boric acid is
dissolved in a mixture of 50 ml of water, and 100 ml
glycerine.
ā¢ Now this solution is titrated with 1 N NaOH
solution using phenolphthalein as an indicator.
29. Uses
ļ± Boric acid can be used as an antiseptic for minor burns or
cuts.
ļ± Boric acid is applied in a very dilute solution as an eye wash.
ļ± It is also used as mouth washes, skin lotion for local anti-
infective action.
ļ± It is also used in preservation of grains such as rice and wheat.
ļ± Its use as an insecticide.
32. Properties
ā¢ Hydrogen peroxide is a colourless and odourless liquid
having a slightly acidic taste.
ā¢ Hydrogen peroxide is a strong oxidising agent and is
miscible in water.
ā¢ The solution decomposes when it comes in contact with
oxidisable matter or when made alkaline.
2H2O2 ā 2H2O + O2
33. Preparation
ā¢ From Barium peroxide:
When aqueous cream of barium peroxide treated
with cold dilute sulphuric acid forms hydrogen
peroxide.
BaO2 + H2SO4 ā BaSO4 + H2O2
ā¢ From Sodium Peroxide:
Sodium peroxide decomposed by addition of cold
dilute sulphuric acid forms hydrogen peroxide.
Na2O2 + H2SO4 ā Na2SO4 + H2O2
34. Assay
ļ±Assay of hydrogen peroxide depend on the
oxidation reduction titration.
ļ±10 ml the H2O2 is diluted with 10 ml distilled water,
then add 10 ml of 5N Sulphuric acid and then
titrated with 0.1N potassium permanganate
solution, until a faint pink color is obtained.
2 KMnO4 + 3H2SO4 + 5 H2O2 ā K2SO4 + 2 MnSO4 + 8 H2O + 5 O2
35. Uses
ā¢ It is a strong oxidising agent.
ā¢ It is used for bleaching.
ā¢ It acts as an antiseptic and a germicide and hence it
is used for cleaning cuts and wounds.
ā¢ It is an effective antidote for phosphorus and cyanide
poisoning.
ā¢ It also finds use for cleaning ears and during removal
of surgical dressings.
37. Preparation
ā¢ From Sea Weed Ash
ā¢ Sea water contains iodine as salts forms
ā¢ These salts are absorbed by seaweeds
ā¢ These seaweeds are dried , burnt and ash is collected
which is called kelp.
ā¢ Aqueous solution of kelp is prepared and
concentrated (Where the sulphates and chloride of
sodium and potassium crystallize out).
38. Preparation
ā¢ Crystals are removed by filtration
ā¢ The solution contains only salts of iodides of sodium
and potassium.
ā¢ Then the solution is treated with sulphuric acid and
then the manganese dioxide and heated.
ā¢ Synthesized iodine is purified and collected.
2NaI + 3H2SO4 + MnO2 ā MnSO4 + 2NaHSO4 + I2 + 2H2O
39. Physical Properties
ā¢ Iodine is in the form of heavy, bluish-black,
rhombic prism or plate having a metallic lustre.
ā¢ It has a peculiar odour and is volatile at ordinary
temperature.
ā¢ It is insoluble in water but soluble in alcohol.
ā¢ It is freely soluble in chloroform and solvent ether
and in aqueous solution of iodides.
40. Assay
ļ± It may be assayed by involving the oxidation - reduction
titration method.
ļ± About 0.5 gm of iodine is first dissolved in a solution of 1 gm
of potassium iodide (1 gm potassium iodide in 5 ml water) in
an iodine flask. It is diluted with 50 ml of water and acidified
with 1 ml of acetic acid.
ļ± Then the resulting solution is titrated with standard sodium
thiosulphate, using starch solution as an indicator.
2Na2S2O3 + I2 ā Na2S4O6 + 2NaI
41. Uses
ā¢ Iodine is used in medicine mainly as a counter irritant and
disinfectant.
ā¢ It is used as a local germicide.
ā¢ Used for preparation of various iodine solution.
ā¢ In the treatment of goitre iodine is supplied to the body either
in the elemental form or in the form of sodium or potassium
iodide.
42. Official Preparation Of Iodine solution
ā¢ Aqueous Iodine solution (Lugolās Solution)
ā¢ Weak Iodine Solution (tincture of Iodine)
ā¢ Strong Iodine solution