Final U-III Content GI Tract

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Unit-3

Gastrointestinal agents

Content:

3.1 Introduction to Gastro intestinal tract (GIT)

3.1.1 Disorders of GIT

3.1.2 Acidifier.

3.1.2.1 Ammonium chloride.

3.1.2.2 Dilute hydrochloric acid.

3.1.3 Antacids.

3.1.3.1 Criteria of an Ideal antacid preparation:

3.1.3.2 Requirements of Combinations of antacids therapy.

3.1.3.3 Sodium bicarbonate.

3.1.3.4 Aluminium hydroxide gel.

3.1.3.5 Magnesium hydroxide mixture.

3.1.4 Cathartics.

3.1.4.1 Magnesium sulphate.

3.1.4.2 Sodium orthophosphate.

3.1.4.3 Bentonite.
3.1.5 Protectives and Adsorbents.

3.1.5.1 Diarrhea

3.1.5.2 Bismuth subcarbonate

3.1.5.3 Kaolin

3.2 Antimicrobials.

3.2.1 Classification.

3.2.2 Mechanism.

3.2.3 Potassium permanganate.

3.2.4 Boric acid.

3.2.5 Hydrogen peroxide.

3.2.6 Chlorinated lime.

3.2.7 Iodine and its preparation.


3.1 Introduction to the gastrointestinal tract (3D video-1)

 The gastrointestinal tract (GIT) also called as digestive tract or alimentary


canal is a part of the digestive system.
 It is a long pathway, where food enters the
− Mouth: Also known as the oral cavity, the mouth is the hollow cavity
that allows food and air to enter the body.
− Pharynx: The pharynx is a hollow tube that starts behind the nose, goes
down the neck, and ends at the top of the trachea and oesophagus. The
oral cavity proceeds into the oropharynx. It serves both respiratory and
digestive functions.
− Oesophagus: Muscular tube lined with mucous membrane which
connects throat to stomach
− Stomach: The stomach is a sac like muscular, J-shaped organ situated in
the upper part of the abdomen. It is a part of the digestive system,
which extends from the mouth to the anus.
− Small intestine: A long tube-like organ that connects the stomach
and the large intestine.
− Large intestine: The large intestine is also called as colon which is
connected to rectum and anus, where the undigested food is expelled.
− Each of the gastrointestinal organ has a definite functional role.
3.1.1 Disorders of GIT:
When the function of GIT is impaired it leads to many disorders a few of which
have been listed below.
1. Achlorhydria or hypochlorhydria (Video-2) 2D
 This occurs due to inadequate secretion of acid in the stomach.
 It's a more severe form of a hypochlorhydria, a deficiency of stomach acids.
 Both conditions can impair the digestive process and lead to damage of the
gastrointestinal system

2. Hyperacidity (Video-3) 2D:


 Hydrochloric Acid that is present in our stomach is a digestive juice that
breaks down the food particles into their smallest form to aid digestion.
 But when there is an increase in the amount of this hydrochloric acid in the
stomach, it leads to the condition of hyperacidity. 
3. Constipation – (Video-4) 2D
 Constipation is a symptom, not a disease, and can be caused by many
factors.
 It is defined as having hard, dry bowel movements, or going fewer than
three times a week.

4. Diarrhoea (Video-5) 2D
 Diarrhoea occurs when the contents in the digestive system moves quickly
through the digestive system such that the intestines don't have enough
time to absorb the fluids, or when the digestive system produces extra fluid.
 The result is stools that contain excess fluids, making them loose and
watery.

Gastrointestinal agents:

 Gastrointestinal agents are a different class of drugs used to


treat gastrointestinal disorders such as gastric acidity,
regulate gastrointestinal motility and water flow, and improve digestion.
 They are

1. Acidifiers or Acidifying agents


2. Antacid
3. Cathartics
4. Antimicrobials

3.1.2 Acidifiers:

What are Acidifiers or Acidifying reagents?

1. Acidifiers are inorganic chemicals that either produce or become acidic.


2. These are the drugs which are able to increase the acidity, in the
gastrointestinal tract, thus decreasing the stomach pH.
3. Some of these drugs are used to treat metabolic alkalosis whereas some
of these are used to increase gastric hydrochloric acid.

Types of acidifiers: (Video-6) 3D


There are four types of acidifiers:
1. Gastric acidifiers- Drugs which are used to restore the acidity of stomach
in patients suffering from achlorhydria or hypochlorhydria.
2. Urinary acidifiers- These are the drugs which are used to render urine
acidic to enable treatment of urinary tract infections.
3. Systemic acidifiers- These are the drugs which are able to combat the
alkalinity of body fluids particularly blood, in patients who are suffering
from systemic alkalosis.
4. Acids-These are widely used in synthesis of drugs and reagents/chemicals.

Two most common examples of acidifiers are:

1. Ammonium chloride
2. Hydrochloric acid

Now, the first drug among the acidifier group is Ammonium chloride.

3.1.2.1 Ammonium chloride:

What is Ammonium chloride?

 Ammonium Chloride is a systemic and urinary acidifying salt. Ammonium


chloride helps to maintain pH and exerts mild diuretic effect.
 It contains not less than 99.5% of NH4Cl, which is calculated with reference
to substance dried over silica gel for four hours.
Synonyms: Sal ammoniac, ammonium muriate.
Chemical Formula: NH4Cl
Description: (Video-9)2D: It is a white crystalline powder or colourless crystals,
odourless with saline taste

Chemical properties:

 It can decompose when heated back to hydrochloric acid and ammonia


(reaction I).
 Additionally, it can react with bases like sodium or potassium hydroxide
to produce ammonia gas. (reaction II)
 Other important reaction is the decomposition of carbonates and
bicarbonates, forming a salt and ammonia (reaction III).
NH4Cl → NH3 + HCl (reaction I)
NH4Cl + NaOH → NH3 + NaCl + H2O (reaction II)
2NH4Cl + Na2CO3 → 2 NaCl + CO2 + H2O + 2 NH3 (reaction III)

Preparation[video-7-2D]

• Ammonium chloride is made by reacting hydrochloric acid with ammonia,


the solution is evaporated to dryness
NH3 +HCl=NH4Cl
• The product is purified by re-crystallisation or by sublimation.
• Ammonium chloride is produced as one of the product during solvay
process used for the production of sodium carbonate.
• Industrially Ammonium chloride is prepared by neutralizing ammonia with
hydrochloric acid.
NH3 + HCl → NH4Cl

• Ammonium chloride is also produced by heating Ammonium Sulphate with


sodium chloride.
2NaCl +(NH4)2 SO4 → 2NH3 + HCl + Na2SO4
NH3 + HCl → NH4Cl

Assay: [video-8-2D]

• Assay of ammonium chloride can be performed by either Volhard’s


method or acid-base titration method.

Test for identity: It gives reactions characteristic of ammonium salts and


chlorides.

Test for purity:

It is tested for

• Arsenic, which is not more than 4 ppm,


• Heavy metals, not more than 10 ppm,
• Sulfated ash – not more than 0.1%
• Clarity and color of the solution – 10% w/v solution is clear and colorless,
• Reaction – 5% w/v solution has a pH between 4.5-6.0
• Test for barium – no turbidity is produced when dissolved in acidified water.
• Test for thiocyanate – no red colour is produced due to the formation of
ferrous thiocyanate when treated with ferric chloride solution.
• Loss on drying – not more than 1% determined on 1 g by drying in an oven
at 105oC.
Uses:

1. Used as an expectorant, diuretic and systemic acidifier.


3.1.2.2 Dilute hydrochloric acid:
 It contains 10% w/w of HCL, not less than 9.5% and not more than 10.5%
 It is commonly known as spirit of salt because it was first prepared by
distillation of sea salt with sulphuric acid.

Chemical Formula: HCl

Synonyms: Hydrochloric acid, muriatic acid,

Description:

It is a colourless liquid. It is strongly acidic with distinct pungent smell and has
a specific gravity of about 1.04 – 1.05 g

Chemical properties:

 HCL is a strong acid and is highly stable.


 It is monoprotic therefore it can only release one proton (H+).
 In water, it completely dissociates to form hydrogen and chloride ions.
The reason hydrochloric acid dissociates into hydrogen and chloride ions
are because it is a polar covalent compound and therefore when added
to water it ionizes.
 Concentrated HCL dissolves metals and form oxidized metal chlorides
and liberates hydrogen gas.
 HCL is very corrosive it attacks many metals like mercury, gold platinum,
tantalum, silver, and certain alloys are an exception.
 Non-corrosive in presence of glass.

General method for preparation of Hydrochloric acid: (Video-9-2D)

 Hydrochloric acid is prepared by warming NaCl crystals with


concentrated H2SO4 (Sulphuric acid).

NaCl+H2SO4→NaHSO4+HCl

 Usually, most of the hydrogen chloride/hydrochloric acid formed is a co-


product of some other chemical reactions.
 HCl is also formed by the chlorination of hydrocarbons.
 Preparation of Dilute Hydrochloric acid:
 It contains 10% W/W of HCl (limits 9.5 to 10.5 %)
 274.0g of Hydrochloric acid is added gradually to 726.0g of water and
mixed

Assay: (Video-10-2D)

Each ml of 1 N NaOH = 0.03646 g of hydrochloric acid.

Test for Purity:

It is tested for Arsenic, heavy metals, sulphate, sulphite.

Free chlorine, bromide and iodide and residue on ignition (not more than
0.01%).
Identification:

1. After neutralization, it gives reactions which are characteristic of


chloride.
2. When it is added to KMnO4 solution, chlorine gas is liberated.
3. Weight per ml at 250C is 1.18g.

Uses of Hydrochloric acid

1. It is used as gastric acidifier.


2. It is used as pharmaceutical aid or as an acidifying agent.

3.1.3 Antacids

What are Antacids? (video-11-3D)

 Antacids are drugs used for neutralizing excess hydrochloric acid in the
stomach.

 They contain ingredients such as aluminium, calcium, magnesium, or


sodium bicarbonate which act as bases (alkalis) to counteract stomach acid
and make its pH more neutral.

What are antacids used for?

Antacids are used to relieve the symptoms of gastroesophageal reflux disease


(GERD) also called acid reflux  ,heartburn or indigestion (also called dyspepsia).

Classification of Antacids: (Video 12-2D)

Based on pharmacological properties antacids are classified into two main types

Systemic antacids:

Examples:

1. Sodium bicarbonate (baking soda),


2. Magnesium oxide (magnesia),
3. Magnesium carbonates,
4. Calcium carbonates,
5. Bourget mixture (sodium bicarbonates, sulphate, phosphate).

Non-systemic antacids:

Examples:

1. Aluminium hydroxide

2. Aluminum Phosphate

3. Magnesium hydroxide

4. Magnesium Silicate,

5. Aluminum-Magnesium Combination

Source:
https://www.researchgate.net/publication/321938715_PHARMACEUTICAL_INORGANIC_CH
EMISTRY_Gastrointestinal_agents_ANTACID

3.1.3.1 Criteria of an Ideal antacid preparation:


• It should not be absorbable or cause systemic alkalosis.
• It should be able to exert its effect gradually and over a long period of time.
• It should not be a laxative or cause constipation.
• It should not cause any side effects because they are used on long term
basis.
• It should be stable and readily available.

No single antacid substance will possess all the required properties, so


generally a combination of antacid substances is used in formulations.

3.1.3.2 Requirements of Combinations of antacids therapy.


 Combination antacids may overcome the side effects of the commonly
used drugs.
 The constipating effect of calcium and aluminium containing antacids
can be corrected with co administration of a magnesium containing
antacid which acts as laxative.

 Non-systemic antacids are more potent and effective as compared to


systemic antacids.
 In Magnesium salt, Magnesium carbonate is most water soluble and
reacts with HCl at a slow rate, while Magnesium hydroxide has low
solubility and has the power to absorb and inactivate pepsin and to
protect the ulcer base.
 Aluminium hydroxide is a weak and slow reacting antacid. But the
aluminium ions relax smooth muscles and cause constipation.
 Calcium carbonate is a potent antacid with rapid acid neutralizing
capacity, but on long term use, it can cause hypercalcemia,
hypercalciuria and formation of calcium stone in kidney.
 Every single compound among antacid have some side effect especially
when used for longer period or used in elderly patients. To avoid certain
side effects associated with antacids, combinations of antacids are used
such as
i) Magnesium and aluminium containing preparation e.g.
magnesium hydroxide a fast acting antacid with aluminium
hydroxide which is a slow acting antacid.
ii) Magnesium and calcium containing preparation where one is
laxative and the other one is constipative in nature.

3.1.3.3 SODIUM BICARBONATE:


 It contains not less than 99% and not more than 100.5% of NaHCO3 with
reference to the dried substance.
 Sodium bicarbonate is a salt that breaks to form sodium and bicarbonate
in water.
 This breakdown makes the solution alkaline, means it is able to
neutralize acid.
 Because of this, sodium bicarbonate is often used to treat conditions
caused by high acidity in the body, such as heartburn.

Synonyms: Baking soda, Bread soda, Cooking soda, Bicarbonate of soda

Preparation of sodium bicarbonate: (video-13) (2D)

 On a small scale, it is prepared by passing carbon dioxide gas through a


solution of sodium hydroxide.
 On an industrial scale, it is obtained by the Solvay process.
 However, I.P grade sodium bicarbonate cannot be obtained by this
method and it is obtained from a sodium carbonate solution.

Assay of sodium bicarbonate: (video-14) (2D)

 Assay of sodium bicarbonate is based on acid base titration.


 Each ml of 1 N H2SO4 ≅ 84.01 mg of NaHCO3.

Description:

 It occurs in white crystalline or amorphous powder having a saline taste.


It is freely soluble in water but practically insoluble in alcohol.
 When heated to 1000C it gets converted into sesquicarbonate (Na2CO3,
NaHCO3 2H2O). It gives an effervescence with acids. Its solution is
alkaline in nature.
 Identification: It gives the reactions of sodium and carbonate. Its 1%
w/v solution has a pH not more than 8.6.
 Tests for purity: It is tested for alkalinity, Al, Ca, insoluble matter, As, Fe,
heavy metals, chloride, sulphate and ammonium compounds.

Uses:

One of the most important application is used as systemic antacid.


Indications:

Sodium Bicarbonate (sodium bicarbonate 5% injection) Injection may be


indicated in the treatment of metabolic acidosis which occurs in severe renal
disease.

Dosage and administration:

 As directed by a physician. Dosage is dependent upon the age, weight and


clinical condition of the patient as well as laboratory determinations.
 For mild acidosis, the usual dosage is 1 to 2 mEq per kg of body weight,
administered slowly.

3.1.3.4 Aluminium hydroxide gel: (colloidal aluminium hydroxide)

 It is aqueous white suspension of hydrated aluminium oxide having varying


amounts of basic aluminium carbonate and bicarbonate.
 It contains not less than 3.55 and not more than 4.4 % w/w of aluminium
oxide (Al3O3).
 It also contains methyl oil, peppermint oil, glycerine, sucrose, saccharin etc.
as flavouring and sweetening agents and up to 0.05%, sodium benzoate, as
a preservative.

Molecular formula: Al(OH)3

Synonyms: Hydrated alumina, Ortho Aluminic acid, Aluminic acid.

Preparation of aluminium hydroxide gel: (Video-15-2D)

It is prepared by adding sodium carbonate to a solution of aluminium sulphate


and by subsequent hydrolysis of aluminium carbonate, aluminium hydroxide is
formed.

Assay of aluminum hydroxide gel: (Video-16) (2D)

Each ml of 0.05 M disodium edetate is equivalent to 0.002549 g of Al2O3.


Tests for identity: A solution in dil.HCl gives reactions which are characteristic
of aluminium. When an equal volume of gel is diluted with distilled water the
pH of the solution should not be more than 7.5.

Tests for purity: It is tested for alkalinity, ammonium salts, arsenic, chloride,
sulphate and acid consuming capacity.

Description:
• It is a white viscous suspension. A clear liquid gets separated when it is
kept standing for some time.
• Aluminium hydroxide gel gives astringent aluminium chloride when it
reacts with gastric hydrochloric acid. This results into nausea, vomiting
and constipation.

Uses:

 Used as antacid in management of


o peptic ulcer,
o gastritis,
o peptic oesophagitis,
o gastric hyperacidity.

Dose: 5 to 30 ml upto 12 times daily.


Normal adult dose:15ml four to six times a day

3.1.3.5 Magnesium hydroxide mixture:

• It is having not less than 95% and more than 100.5 % of magnesium
hydroxide.

Formula: Mg (OH)2
Preparation: (Video -17-2D)
Sodium hydroxide and magnesium sulphate interact to form magnesium
hydroxide.

MgSO4(aq) + 2NaOH(aq) → Mg(OH)2(s) + Na2SO4(aq)


magnesium sulfate sodium hydroxide Megnesium hydroxide sodiumsulfate

Assay: (Video -18-2D)


 Its assay is based on acid -base titrations.
 Each mL of per g. 0.05 M edetate disodium is equivalent to 2.916 mg of
Mg(OH)2.

Properties:

It is colourless, odourless, amorphous powder

 It decomposes into Magnesium Oxide and water.


Mg (OH)2 → MgO + H2O
 It is moderately basic, which helps in neutralizing mild acids.
 Moreover, it has an active disassociation in water to give hydroxyl ions and
Mg ions.

Uses: (video-19-2D)

Magnesium hydroxide mixture is used as an antacid or a laxative.

Product information:

Generic Name: magnesium hydroxide

Brand Name: Ex-Lax Milk of Magnesia®, Milk of Magnesia, Pedia-Lax


Chewable, Phillips Milk of Magnesia, Concentrated Phillips Milk of Magnesia.

 MILK OF MAGNESIA
• Milk of Magnesia is a suspension of Magnesium Hydroxide.
• It is having not less than 7 percent w/w and not more than 8.5% w/w of
magnesium hydroxide Mg(OH)2 in purified water.
• Milk of Magnesia, Double-Strength Milk of Magnesia, and Triple-
Strength Milk of Magnesia contain not less than 90.0 percent and not
more than 115.0 percent of the labelled amount of Mg(OH)2, the
labelled amount being 80, 160, and 240 mg of Mg(OH)2 per mL,
respectively as per USP Monographs.

Description: It is white uniform suspension.

Varying proportion of water may separate out on standing.

Identification: A solution of 1 ml in 2 ml diluted hydrochloric acid gives


reactions which are characteristic of magnesium.

Tests for purity: It is tested for soluble alkalies, soluble salts carbonates and
acid insoluble matter besides As, Ca and heavy metals.

Packaging and storage: Preserve in tight containers, preferably at a


temperature not exceeding 350C. Avoid freezing.

Labelling:

(i) Double- or Triple-Strength Milk of Magnesia is so labelled, or may be


labelled as 2× or 3× Concentrated Milk of Magnesia, respectively.
(ii) “SHAKE WELL BEFORE USE”.

Uses:

• Milk of Magnesia is used as antacid and Laxative.


• Used to treat symptoms caused by too much stomach acid such as
heartburn, upset stomach or indigestion.

https://www.youtube.com/watch?v=7rHk9PO4XHU
https://www.youtube.com/watch?v=JBjgLfW1wZ4

https://www.youtube.com/watch?v=QsXAWC1rw-Y

https://www.youtube.com/watch?v=7rHk9PO4XHU

https://www.youtube.com/watch?v=JBjgLfW1wZ4

https://www.youtube.com/watch?v=QsXAWC1rw-Y

https://www.slideshare.net/AdarshKhilawdiya/cathartics-by-adk

3.1.4 Cathartics
What are Cathartics?
Laxatives and cathartics are medications that bring about the defecation.
 Laxatives ease the passage of fully formed fecal matter from the rectum
 Cathartics have a stronger effect, and causes the evacuation of the
entire colon, usually in the form of watery, unformed stool.
 Purgatives are also cathartics which act similarly but are generally mild
in their nature.
 Laxatives are the mild type of purgatives.
 Some medications can function both as a laxative and as cathartics,
depending on the dosage.
In normal habits, peristalsis causes defecation. The peristaltic waves are able
to stimulate bowel and relieve its contents.

Common indications of Cathartics and Laxatives:


 To relieve acute constipation and for expulsion of intestinal parasites.
 To ease defaecation in patients with painful haemorrhoids, hernias and
other rectal disorders.
 To avoid excessive straining during defecation, and resultant potentially
hazardous rises in blood pressure in patients with hypertension,
cerebral, coronary, or other arterial disease.
 To evacuate bowels before surgery.
 To remove solid material from the intestinal tract prior to certain
roentgenographic studies.

Cathartics are classified into 4 different types where each category of


cathartics has its own mechanism of action.
1. Bulk forming Cathartics: (Video-20)
Stimulate evacuation of the bowel by increasing the bulk of the feces
(stool).
Examples: Methylcellulose, psyllium husk, Isapgol and dietary fiber such
as wheat and oat bran.
2. Stool Softener/Emollient/Lubricant (Stool Softeners): (Video-21)
These are fecal softening agents which act like a detergent by helping to
permit water and fatty material to mix with fecal contents and make
them soft.
Examples: dioctyl sodium sulfosuccinate—docusate sodium and dioctyl
calcium sulfosuccinate— docusate calcium.
Ex: Liquid paraffin, glycerine
3. Stimulant or Irritant Purgatives. (Video-22)
These stimulants act by local irritation on the intestinal tract which
increase peristaltic activity.
Examples include phenolphthalein, aloin, cascara extract, rhubarb
extract, senna extract, podophyllum, castor oil, bisacodyl, calomel etc.
4. Saline cathartics/Osmotic laxatives: (Video-23)
They are salts of poorly absorbable anions biphosphate, phosphate,
sulphates, tartarates, and soluble magnesium salt.
They are water soluble and are taken with large quantities of water to
prevent excessive loss of fluids from the body.
Examples: Magnesium sulpahte, sodium tartrate, sodium biphosphate,
sodium phosphate, potassium sodium tartrate, magnesium hydroxide,
magnesium citrate and magnesium sulphate.

 Constipation is the infrequent


or difficult evacuation of the
faeces.
Various inorganic compounds that are used as cathartics and laxatives are
 Magnesium sulphate
 Sodium phosphate
 Sodium potassium tartrate
 Potassium bitartrate
 Mercurous chloride
3.1.4.1 MAGNESIUM SULPHATE:
Molecular formula: MgSO4. 7H2O
 Magnesium sulfate, commonly known as Epsom salt, is a mineral. It
works by replacing magnesium in the body and increasing water in the
intestines.
 Magnesium sulfate can be used orally as a laxative to relieve
occasional constipation, and to treat low levels of magnesium.
I.P Limit:
It is having not less than 99% and not more than 100.5% of MgSO4
calculated with reference to dried substance.
Synonyms: Epsom salt

Properties of Magnesium sulphate


It occurs as colourless crystals having cool, saline bitter taste.
 It effloresces in warm dry air.
 It is soluble in water and sparingly soluble in alcohol.
 When gently heated it loses some of its water of hydration and gets
converted into the monohydrate (white powder) which becomes
anhydrous at 2000C.
Preparation (video-284-2D)
It is obtained by the action of dilute sulphuric acid on magnesium oxide.
Assay: (video-25-2D)
Each ml of 0.05 m disodium ethylene diamine tetraacetate = 0.00602 g of
MgSO4
Action and Uses:
 It is used as a saline cathartic.
 Magnesium sulphate is given orally in dilute solutions. About 5 g gives rise
to laxative effect. Due to bitter and nauseating taste it is given in fruit
juices.
 The mechanism of action is that magnesium sulphate does not get
absorbed from intestinal tract and thus retains sufficient water within the
lumen.
 The hydrostatic pressure is able to promote motor activity or peristalsis of
bowel.

Description:

 Magnesium Sulphate Injection, USP (50%) for IV and IM use is a sterile


concentrated solution of magnesium sulphate USP.
 Each ml contains: magnesium sulphate (magnesium sulphate injection)
(heptahydrate) 500 mg, which provides 4.06 mEq each of magnesium (Mg+
+) and sulphate (SO4+), water for injection.

Chemical properties of Magnesium sulphate


Let us see a few of the chemical properties of magnesium sulphate

 In the anhydrous form, it readily absorbs moisture from the air,


making it hygroscopic. 
 MgSO4 is highly soluble in water.
 It is stable at normal conditions but when heated to high temperatures,
it decomposes to give toxic fumes of sulfur oxides.
https://sciencing.com/physical-chemical-properties-epsom-salt-
7217842.html

DOSE: 10-15g/day
Identification: It gives reactions which are characteristic of magnesium and
sulphate.
Tests for purity: It has to be tested for As,Fe,Zn, heavy metals, and loss on
drying.
3.1.4.2 SODIUM ORTHOPHOSPHATE
It is dodecahydrate of disodium hydrogen phosphate.
I.P Limit:
It contains not less than 98% and more than the equivalent of 101.0% of
Na2HPO4 calculated with reference to the dried substance.
Molecular formula: Na2HPO4.12H2O
Synonym: Disodium hydrogen phosphate.
Preparation: (video-26-2D)
It is prepared by neutralization of phosphoric acid under controlled conditions
with sodium hydroxide or sodium carbonate.
Assay: (video-27-2D)
It is based on acid base titration.
Each 1 ml of 0.5 N H2SO4= 0.07098 g of Na2HPO4
Description:
 It occurs in the form of colourless transparent crystals, having saline taste.
 It is odourless and effervescent.
 It in soluble in water but insoluble in alcohol.
 Its aqueous solution has a pH between 8.0 – 11.0; moderately basic.

 On heating over 3000C it is converted into sodium pyrophosphate.


2 Na2HPO4→ Na2P2O7 + H2O
Uses:

 It is used to treat constipation or to clean the bowel before a colonoscopy.


 It is used as a saline laxative.
 It is a cathartic and buffering agent.

Storage: It should be stored in tightly closed container.


Dose: 2-16g in divided dose daily.
3.1.4.3 Bentonite (Al2O3 .4SiO2 .H2O)
 It is a colloidal hydrated aluminium silicate which occurs naturally.
 It is obtained from the naturally occurring sources.
 Bentonite is having SiO2, Al2O3, Fe2O3, CaO, MgO and some sodium and
potassium.

Properties:
 It occurs as a very fine, pale or cream coloured powder.
 It is odourless, free from grit and has slightly earthy taste.
 It is almost insoluble in water but swells to about 12 times its volume
after neutralisation.
 The special properties of bentonite are swelling, the extracted bentonite
is distinctly solid, with a moisture content of approximately 30%.

Uses:
 It is a good pharmaceutical aid and is used as a protective colloid to
stabilise emulsions.
 Mainly it is used to suspend other insoluble powders.
 It is also used as a base for many pharmaceutical preparations including
plasters and ointments.
 It is an ingredient of calamine lotion which is used as a protective.

3.1.5 Protectives and Adsorbents.

Protectives and adsorbents are gastrointestinal agents commonly used for the
treatment of mild diarrhea.

3.1.5.1 Diarrhea:

 Abnormal frequent passage of loose stool or passage of stools with


increased frequency, fluidity, and weight, or with increased water
content in stool.
 It is a symptom and not a disease.
 It may be caused by bacterial toxins, chemical poisons, drugs, allergy,
disease, gastrointestinal surgery, carcinomas, chronic inflammatory
conditions and various absorptive defects.
 Products used in the treatment of diarrhea may include
o adsorbents – substances that adsorb toxins, bacteria and viruses
from the intestines.
o protectives- provides protective coating of intestinal lining.
o Antispasmodics- to relieve the intestinal spasms that result from
increased intestinal motility
o and possibly an antibacterial agent.
 They include bismuth salts, special clays and activated charcoal.

3.1.5.3 KAOLIN:

Heavy Kaolin, Al2O3, 2SiO2, 2H20

 Kaolin is a native, hydrated aluminum silicate, powdered and freed from


gritty particles by elutriation.
 It may contain a suitable dispersing agent.

Preparation: Heavy kaolin is prepared by powdering the natural substances,


which is freed from most of its impurities by elutriation and dried.

Properties:

 It is soft, whitish odourless and tasteless powder, free from particles.


 It is insoluble in water, in cold dilute acids and in solutions of alkali
hydroxides.

Storage : Store in well closed containers. Medicinal and Pharmaceutical

Uses:

1. It is used as pharmaceutical aid.


2. Used as anti-inflammatory and counter irritant (Kaolin Poultice, I.P.’66
contains 50.5% of Heavy Kaolin).

LIGHT KAOLIN, Al2O3, 2SiO2, 2H20

 Light kaolin is nothing but finely divided form of kaolin, which is lighter
and is used for internal administration.

Preparation:

 It is prepared from the natural substance by electrical sedimentation. It


must be free from gritty and other impurities.

Properties:

 It is light, odorless, tasteless white powder.


 It is insoluble in water and mineral acids.

Storage: Store in well-closed containers.

Medicinal and Pharmaceutical Uses:

1. It is used in the symptomatic treatment of colitis, cholera, dysentery and


diarrhoea and in the treatment of food and alkaloidal poisoning.
2. It is given orally to adsorb toxins and other substances from
gastrointestinal tract thereby helps to increase the bulk of faeces, which
improves the consistency of stool resulting in decreased frequency of
defeacation.

Dose: 15 – 60 g orally.

3.2. Antimicrobial Agents

What are microbes? :(video-28-2D)


Microbes are tiny living things that are found all around us and are too small
to be seen by the naked eye. They live in water, soil, and in the air.

What are antimicrobials agents?

1. The chemical substances that destroy or inhibit the growth of micro-


organisms and especially pathogenic organisms are called antimicrobials.
2. The word antimicrobial was derived from the Greek words ‘Anti’-
Against, ‘mikros’-little and bios-life.
3. It refers to all agents that act against microorganisms.
4. The most common targets for action of antimicrobial drugs fall into 5
basic categories:
i) Inhibition of cell wall synthesis.
ii) Inhibition of protein synthesis
iii) Inhibition of nucleic acid synthesis
iv) Effects on cell membrane sterols (antifungal agents)
v) Inhibition of unique metabolic steps.

 Mechanism of action antimicrobial agents: The mechanism of action of


antimicrobial agents may range from mild astringent to powerful
oxidative processes.
 Inorganic compounds are generally used as anti-infectives topically but
not for systemic infections
 They are not administered internally like antibiotics or sulphonamides
except in a very few cases, for topical application they may be used with
caution.

Inorganic compounds generally exhibit antimicrobial action by either of the


three mechanisms. They are

Oxidation
Halogenation
Protein binding or precipitation.

Oxidation mechanism. (Video-29-2D)


Compounds acting by this mechanism belong to classes of
1. peroxides,
2. oxygen liberating like permanganate and
3. certain oxo-halogen anions.
Halogenation mechanism: (Video-30-2D)
Compounds which are able to liberate chlorine or hypochlorite or iodine act by
this mechanism.
Protein precipitation. (Video-31-2D)
 Metal ions and protein react together forming a complex i.e protein
precipitation resulting in inactivation of the protein.

3.2.2. Classification of antimicrobial agents.


 Antimicrobial agents are classified into different types based on the
mechanism of action and the effect they show on various
microorganisms:
- Antiseptic
- Disinfectants
- Germicides
- Bacteriostatic
- Sanitizers

Antiseptics: (Video-32-2D)

 These are substances that stop or slow down the growth of micro-
organism.
 An antiseptic is applied to living tissue.
 An ideal antiseptic should destroy bacteria, spores, fungi, viruses, or any
other infective agent without causing any harm to the tissues of the
host.
 They are applied to all tissues of the body and may be used in the form
of
o mouth washes,
o soaps,
o deodorants,
o throat and nasal sprays
o vaginal douches.
 Example: tincture of iodine.
Disinfectants:(video-33-2d)

 These are substances that prevent infection by destroying pathogenic


microorganisms, generally applied to inanimate objects.

Germicides:(Video-34-2d)

 These are the substances which kill micro-organisms.


There are three types of germicides
Bactericide -Which kills bacteria
Fungicide – Which kills fungi
Viricide – which kills Virus

Bacteriostatic: (video-35-2D)

“Bacteriostatic” means that the agent prevents the growth of bacteria i.e., it
keeps them in the stationary phase of growth.

Sanitizers (Video-36-3D)

 Sanitizer is a substance or fluid designed to kill germs on skin and


objects.
 Sanitizers are of specific use to remove the germs without the use of
water.
 Most popular hand sanitizers are alcohol based and kills 99.99% of
germs.
 Sanitation is mainly concerned with cleaning or washing away the
organic matter on skin and objects.
 The active ingredient is around 70% alcohol depending on the
formulation.
 The alcohol can be either ethanol or isopropanol.
https://www.youtube.com/watch?v=245jz3ZqZqM

3.2.3 POTASSIUM PERMANGANATE:

Chemical formula: KMnO4

 It contains NLT 99.0% of KMnO4


 It is a potassium salt of manganic acid.

Synonyms: chameleon mineral, Condy’s crystals, permanganate of potash and


hypermagan.

Preparation: (Video-37-2D)

Potassium permanganate is prepared by using a solution of potassium


hydroxide with powdered manganese oxide and potassium chlorate.

Assay: (Video-38-2D)

 Its assay is based upon oxidation-reduction reaction.


 Potassium permanganate is a strong oxidising agent and oxalic acid is a
reducing agent.
 The reaction between KMnO4 and oxalic acid tends to proceed slowly.
 Hence, warming at 700C is required.
Each ml of 0.1N oxalic acid = 0.00316 of KMnO4

Description:

 It is a dark purple, slender, prismatic crystals with metallic lustre.


 It has no odour but sweet astringent taste.
 It decomposes at higher temperature.

It is a powerful oxidizing agent.

Mode of Action:

Potassium permanganate releases the nascent oxygen that is [O], which by


oxidative mechanism inhibits the actions of microorganism and their growth.

Tests for purity:

It is tested for Cl and SO4

Tests for purity:

 It is tested for Cl and SO4.


 To remove the colour of KMnO4(since colour may interfere with the
test of purity), KMnO4 is boiled with 95% alcohol, and the precipitated
MnO2 is removed by filtration.
 Limit test for chlorides and sulphates is carried out.

Uses:
 It is used in the treatment of Urethritis
 Used as anti-infective in Mouthwash, and in cleaning ulcers or abscesses.
 Because of its ability to oxidize drugs and venoms, used as an antidote in
poisoning by barbiturates, chloral hydrate and alkaloids. It oxidises the
excess drug substance in the stomach, but should be removed from the
stomach subsequently.
 It is also used as an acute solution for the treatment of fungal infections
like athlete’s foot, where the affected foot is soaked in a potassium
permanganate solution in water for about 15 minutes.

Storage: stored in tightly closed containers.

3.2.4 BORIC ACID:

 It is having not less than 99.5% of H3BO3 which is calculated with reference
to the substance and dried over sulphuric acid for five hours.
 Occurrence: Free boric acid occurs in sea water, many plants and nearly all
fruits so far.

Chemical Formula: H3BO3 


Synonyms: Orthoboric acid, hydrogen borate.
Description:

Boric acid is a solid which is available in three forms

1. Colourless, odourless pearly scales


2. Six sided triclinio crystals.

3. White odourless powder which is unctuous to touch.


4. It is slightly acidic or bitter in taste, soluble in water and alcohol.

Chemical properties:

 Boric acid is a weak acid. Heating boric acid to certain temperatures,


yields various dehydration products.
 Boric acid on heating to 100°C loses one molecule of water, to give
metaboric acid HBO2.
H3BO3 → HBO2 + H2O
 Heating to approximately 160°C, causes a further loss of water from
metaboric acid to produce tetraboric acid, H2B4O7.
 4 HBO2 →H2B4O7 + H2O
 Heating to still higher temperatures tetraboric acid produces the
anhydride of boric acid, boron trioxide, B2O3 which is a glassy solid.

H2B4O7 →2B2O3+H2O

Preparation: (Video-39-2D)

 Boric acid is prepared from native borax and borates by reacting them
with hydrochloric or sulphuric acid.

Assay: (Video-40-2D)

 It is assayed by titrimetric method. Being a very weak acid it cannot be


directly titrated accurately with a strong alkali.
 When it is dissolved in a mixture of water and glycerin, it behaves like a
strong monobasic acid and then it can be titrated with alkali using
phenolphthalein as an indicator.

Each ml of 1 N NaOH = 0.06183 g of H3BO3

Uses:
 Has varied uses in the pharmaceutical industry where a few of them have
been mentioned below.
 Boroglycerine, prepared from boric acid is used as a suppository base.
 Its anti-fungal properties are useful to treat vaginal yeast infections or
candidiasis.

Storage: It is stored in a well closed container.


Test for identity:
1. Solution of boric acid in alcohol on igniting in a porcelain dish burns with
green tinged flame.
2. An aqueous solution of boric acid on addition of HCl turns the turmeric
paper to pink or brownish red which upon being moistened with NH3
solution changes to blue or greenish black.
Test for purity:
It has to be tested for arsenic; heavy metals; sulphate and alcohol- insoluble
substances.
3.2.5 HYDROGEN PEROXIDE:

 Hydrogen Peroxide Solution is an aqueous solution of hydrogen peroxide


and contains NLT 6% w/v of H2O2
 It is used as an oxidizer, bleaching agent, and antiseptic.
Synonyms: Dioxidane, Oxidanyl, dihydrogen dioxide, oxygenated water,
peroxaan.
Chemical formula: H2O2
Preparation: (Video-41-2D)
Acidifying Barium peroxide and Removing excess water by evaporation under
reduced pressure gives Hydrogen peroxide.
BaO2.8H2O(S)+H2SO4(Aq) BaSO4(S)+H2O2(Aq)+8H2O(I)
Description

 In the pure state hydrogen peroxide is an almost colourless


odourless liquid.
 It has slightly acidic taste.
 It is miscible with water in all proportions and forms a hydrate
H2O2.H2O
 A 30% solution of H2O2 is marketed as “100 volume” hydrogen
peroxide (perhydrol).
Chemical properties
Its Acts as an Oxidizing as well as reducing agent in both acidic and alkaline
medium.

 https://www.vedantu.com/chemistry/hydrogen-peroxide

Assay (Video-42-2D) This assay is based upon volumetric titration method.


 Hydrogen peroxide and acidified potassium permanganate, both are
oxidizing agents.
 These two oxidizing agents reduce one another with the evolution of
gaseous oxygen.
 Hydrogen peroxide reduces KMnO4 solution and causes its discoloration.
 At the end point, excess drops of KMnO4 gives pink colour.
 Potassium permanganate itself acts as an indicator.
Each ml of 0.1 N kMnO4 ≡ 0.001701 g of H2O2
3.26 CHLORINATED LIME

 It is an inorganic compound which principally consists of calcium


hypochlorite [Ca(OCl)2], dibasic calcium hypochlorite [Ca3(OCl)2(OH)4],
and dibasic calcium chloride [Ca3Cl2(OH)4].
 It is made from slightly moist slaked lime.

 It is having not less than 30.0 % w/w of available chlorine.


 It is the main active ingredient of commercial products called bleaching
powder, chlorine powder, or chlorinated lime.
Synonyms: Hypochlorous acid; Bleaching powder; Calcium oxychloride;
Calcium hypochlorite.
Molecular Formula: Ca(ClO)2.
Description:

 It is a dull white powder with characteristic odour.


 When exposed to air, it absorbs moisture and gradually decomposed.
 It is slightly acidic in water and alcohol.

Chemical properties:

When bleaching powder is put in water, hypochlorite goes out in solution,


because of which it gets bleaching and oxidizing property.

2Ca (OCl)Cl + CO2+ H2O→ CaCO3 + CaCl2 + 2HOCl


Chlorinated lime Calcium carbonate

Preparation: (Video-43-2D)
Chlorinated lime is a compound which is obtained by the action of chlorine on
calcium hydroxide.
Ca (OH)2 + Cl2 → Ca (OCl) Cl + H2O
Assay: (Video-44-2D)

 Its assay is based on redox titration method.


 Chlorinated lime liberates the available chlorine as Cl2 gas by the action
of acid.
 Then this free chlorine is allowed to react with potassium iodide to
liberate iodine, the quantity of liberated iodine is then estimated by
titration with sodium thiosulphate.

 Each ml of o.1 mol/L sodium thiosulphate is equivalent to 3.5453 mg of


Chlorine.
Identification tests: when HCl is treated with sample, chlorine gas is evolved.

 Tests for purity: It has been tested for its stability by heating it at 1000c
for 2 hours, it must not lose more than 3% w/w of available chlorine.
 Storage: stored in a well closed container in a cool place.

Uses:
 Calcium hypochlorite has rapid bactericidal action.
 It works by chlorination of microorganism’s protein, which ultimately leads
to the destruction of protein and cell death.
 It kills most of bacteria, some fungi, yeast, algae, viruses and protozoa.
3.27 IODINE :

 Iodine of I.P. Standards Contains NLT 99.5% of I2

 Sea water is contains traces of combined iodine, which is absorbed by some


specific plants and sea weeds, like Laminaria digitate, Fucus vesiculosus.
 The body needs iodine to make thyroid hormones, which control the body's
metabolism and many other important functions
Synonyms:  iodine-131 I, iodine -125
Chemical Formula: I2.

Preparation: (Video-45-2D)

 Iodine is manufactured by extracting Kelp (seaweed’s ash).


 More recently iodine has been reported to be found in the brine of
oil wells and this source is used nowadays for getting iodine in some
countries.
 Impurities like iodine monochloride (ICl), iodine monobromide (IBr)
and Cyanogen iodide (ICN) present in iodine are removed by heating
crude iodine with potassium iodide.
ICI + KI → KCI + I2

IBr + KI → KBr + I2

ICN + KI → KCN +I2

Properties:
1. Iodine occurs as bluish black small crystals with metallic luster.
2. It possesses a different irritating odour and bitterly pungent in taste.
3. It is volatile at room temperature and its vapour attack both cork and
rubber.
4. It is slightly soluble in water, but insoluble in alcohol, either chloroform.
5. At higher temperature, the density of iodine decreases as it dissociates.
I2⇋ 2I-
6. It reacts directly with some non-metals and with heavy metals.
2P + 3I3 → 2PI3
Fe +I2 → FeI2
7. With an alkali, iodine reacts to form an iodine and iodate with heat.
3I2 + 6NaOH → 5NaI+ NaIO3+3H2O

8. Potassium iodide is able to dissolve large quantity of iodine due to the


formation of I3 ions.
KI + I2 →KI3

Mode of Action:
 Iodine in aqueous solution act as a mild oxidizing agent which is mediated
through the formation of hypoiodous acid (HIO), which further releases
nascent oxygen [O], which help in the oxidation of microorganism’s
proteins.
I2 +H2O ⇋ HI +HIO
HIO → HI+[O]

Various official preparations of Iodine:

1. Aqueous iodine solution (Lugol’s splution)

2. Weak iodine solution (tincture of iodine)

3. Strong iodine solution

1. Aqueous iodine solution (Video-46)

Synonym: Lugol’s solution

 It contains 5.0 % W/V of iodine and 10 % w/v of Potassium iodide in


water.

Description:

- Transparent, brown liquid with smell of iodine

Uses:

- As a germicide and fungicide agent.


- It does not cause irritation when applied on cuts like tincture of iodine.

2.Weak iodine solution (Video-47)

Synonyms: Iodine tincture

 Weak iodine solution contains 2.0 % w/V of iodine and 2.5 % w/w of
Potassium iodide in water.

Description:

Transparent, brown liquid with smell of iodine and alcohol.


Uses:

It is a popular antiseptic agent.

3.Strong iodine solution (Video-)

Strong iodine solution contains 10.0 % W/W of iodine and 6.0 % w/w of
Potassium iodide in alcohol-water mixture.

Description:

Transparent, brown liquid with smell of iodine and alcohol.

Use:

Used as an antiseptic agent.

Dosages of Iodine:

Recommended Daily Allowance (RDA)

 Adult: 150 mcg/day


 Pregnancy: 220 mcg/day
 Lactation: 290 mcg/day
 Children 1-8 years: 90 mcg/day
 Children 8-13 years: 120 mcg/day
 Children 13-18 years: 150 mcg/day

Storage: “It should be stored in dark coloured amber containers with a glass
stopper in a Cool Place.”
Incompatibility : With hypophosphite, sulphite - Some metal - Reducing
agent - With alkalis, alkali carbonates

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