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PT 103 PHARMACEUTICAL INORGANIC
CHEMISTRY(THEORY)
KUNAL DATTA
UNIT III : Gastrointestinal Agents
Antimicrobial Agents
Antimicrobial Agents
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
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
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.
ļ±These are the agents which kills microbes.
Sub classification:
ļ¶Bactericidal agents- those kill bacteria
ļ¶Fungicidal- those kill fungus
Germicides
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
ļ±These are the chemical agents which are used in
clinical application of antimicrobial agents to treat
infection diseases.
Chemotherapeutics Agents
ļƒ¼ Must have a broad spectrum of action;
ļƒ¼ Rapid onset of action;
ļƒ¼ Should have a small latency period;
ļƒ¼ Should have a high activity;
ļƒ¼ Must be chemically resistant;
ļƒ¼ High availability and low cost;
ļƒ¼ Lack of local irritant or allergic effects on tissues;
ļƒ¼ Minimal absorption from the place of their application;
ļƒ¼ Low toxicity ;
Characteristics of antimicrobials Agents
ā€¢ Microorganism contain many important ā€˜protein
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.
ļƒ˜Oxidation
ļƒ˜Halogenation
ļƒ˜Precipitation of Protein
Mechanism of action : Antimicrobial Agents
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
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
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
Classification of Antimicrobial agents according to
their MOA
Some Commonly Used
Antimicrobial agents
Potassium permanganate
Molecular formula
KMnO4
Molar mass
158.034 g/mol
Synonym
Condy's crystals; Permanganate of potash
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
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
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
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
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
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.
Storage
ļ‚§ Store in well closed container and kept
in a cool place.
Boric Acid
Molecular formula:
H3BO3
Molar mass:
61.83 g/mol
Synonym :
Hydrogen borate
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.
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).
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
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.
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.
Storage
ā€¢ Store in well closed container and kept in
a cool place.
Hydrogen peroxide
Molecular formula
H2O2
Molar mass
34 g/mol
Synonym
Dioxidane; Oxidanyl; Perhydroxic acid
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
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
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
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.
Iodine Solution
Molecular formula
I2
Molar mass
126.9 gm/mol
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).
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
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.
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
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.
Official Preparation Of Iodine solution
ā€¢ Aqueous Iodine solution (Lugolā€™s Solution)
ā€¢ Weak Iodine Solution (tincture of Iodine)
ā€¢ Strong Iodine solution
Aqueous Iodine Solution
Weak Iodine Solution
Strong Iodine Solution
Storage
ā€¢ It is preserved in glass stoppered, amber
coloured bottles and kept in a cool place.
THANK YOU

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Gastrointestinal agents _ Antimicrobial.ppt

  • 1. PT 103 PHARMACEUTICAL INORGANIC CHEMISTRY(THEORY) KUNAL DATTA UNIT III : Gastrointestinal Agents Antimicrobial Agents
  • 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. ļƒ¼ Must have a broad spectrum of action; ļƒ¼ Rapid onset of action; ļƒ¼ Should have a small latency period; ļƒ¼ Should have a high activity; ļƒ¼ Must be chemically resistant; ļƒ¼ High availability and low cost; ļƒ¼ Lack of local irritant or allergic effects on tissues; ļƒ¼ Minimal absorption from the place of their application; ļƒ¼ Low toxicity ; Characteristics of antimicrobials Agents
  • 10. ā€¢ Microorganism contain many important ā€˜protein 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. ļƒ˜Oxidation ļƒ˜Halogenation ļƒ˜Precipitation 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
  • 14. Classification of Antimicrobial agents according to their MOA
  • 16. Potassium permanganate Molecular formula KMnO4 Molar mass 158.034 g/mol Synonym Condy's crystals; Permanganate of potash
  • 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.
  • 23. Storage ļ‚§ Store in well closed container and kept in a cool place.
  • 24. Boric Acid Molecular formula: H3BO3 Molar mass: 61.83 g/mol Synonym : Hydrogen borate
  • 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.
  • 30. Storage ā€¢ Store in well closed container and kept in a cool place.
  • 31. Hydrogen peroxide Molecular formula H2O2 Molar mass 34 g/mol Synonym Dioxidane; Oxidanyl; Perhydroxic acid
  • 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 (Lugolā€™s Solution) ā€¢ Weak Iodine Solution (tincture of Iodine) ā€¢ Strong Iodine solution
  • 46. Storage ā€¢ It is preserved in glass stoppered, amber coloured bottles and kept in a cool place.