Gastro Intestinal (GIT) Agents

and Related Compounds

Drugs which act in the GIT are known as
Gastro Intestinal (GIT) Agents

ACIDIFIERS
STOMACH AND ACIDITY
Acid environment kills bacteria that comes in
with food, is optimum for activity of digestive
enzymes.
It is unusual compared to other organs as its
pH is as low as 1-2 due to production of
hydrochloric acid from structures in lining of
walls from gastric glands.
Acidity in the stomach is normal, but excess
acidity is potentially harmful
 The Stomach
• The walls of the
stomach are lined
with cells that
secrete mucus,
pepsinogen and
hydrochloric acid.

3
 The Stomach
• The hydrochloric acid
of the stomach which
corresponds to a pH
range of about 1.5 to
2.5 (concentration
ranges from 0.03 M
to 0.003 M )

4
 The Stomach
• The mucus lining of
the stomach protects
the stomach walls
from the action of
stomach acid

5
 Gastro Intestinal (GIT) Agents and Related
Compounds
 Acidifiers
 Antacids
 Protectives & Adsorbents
 Saline Cathartics

ACIDIFIERS
 ACIDIFIERS
• In patients suffering from achlorhydria, there
is deficient secretion of hydrochloric acid in
the stomach.
• In such cases acidifiers are useful in providing
the necessary acidity for the proper digestion
of food.

ACIDIFIERS
 ACIDIFIERS
Classification of Acidifiers:
1. Systemic Acidifiers – Given usually by inj, act
by reducing the alkali reserve in the body. Ex:
Sodium phosphate & Ammonium chloride

2.Non–Systemic Acidifiers – usually

administered orally which act directly on the
GIT. Ex: Hydrochloric acid, Dil. Hydrochloric
acid
ACIDIFIERS
 ACIDIFIERS
Hydrochloric Acid
SYNONYM: Muriatic acid
Mol. Formula: HCl
Preparation:
A. It is prepared by reacting sodium chloride with sulphuric
acid. This reaction takes place in two steps
NaCl + H2SO4 NaHSO4 + HCl
Common salt Sodiumbisulphite pan acid
NaHSO4 + NaCl Na2SO4 + HCl
Salt cake Muriatic acid
The HCl in Ist step – pure, II step - impure

ACIDIFIERS
 Hydrochloric Acid

Preparation:
B. In this method the hydrogen and chlorine
obtained in the electrolysis of sodium chloride
in the manufacture of caustic soda are burnt
preferably using quartz Bunsen burners.
H2 + Cl2 2 HCl

100 % pure HCl is formed by this method

ACIDIFIERS
 Hydrochloric Acid

• Hcl is
– A colourless gas
– An acrid irritating odour
– an acid taste
– Heavier than air
– Very soluble in water (460 ml of gas in 1 ml of
water) Soluble in water and in ethanol
– Hydrochloric acid is a clear, colourless fuming liquid
with pungent taste
– Neutralization reaction (with alkali)
NH3 + HCl NH4Cl
With metal 2Na + 2HCl 2 NaCl + H2
ACIDIFIERS
 Hydrochloric Acid

It releases CO2 from carbonates and bicarbonates

• Na2CO3 + 2 HCl 2NaCl + H2CO3
• H2CO3 H2O + CO2
• AgNO3 + HCl AgCl + HNO3
• Na2SO3 + 2 HCl 2 NaCl + H2SO3
• H2SO3 SO2 + H2O
Identification Tests:
1. Sample + water – neutralized - gives reactions of
chlorides
2. When the sample is added to potassium
permanganate, chlorineACIDIFIERS
is evolved
Tests for PURITY
• Non-volatile residue - Not more than 0.5%
• Transfer 1 g into a tared glass dish, evaporate to
dryness on a steam bath, dry at 110º for 1 h, cool in
a desiccator and weigh. The weight of the residue
does not exceed 5 mg.
• Reducing substances - Not more than 70 mg/kg as sulfur dioxide ; Transfer 1 ml
of reagent grade hydrochloric acid into a 30-ml test tube, dilute to 20 ml with
freshly boiled and cooled water, and add 1 ml of potassium iodide TS, 1 ml of
starch TS and 2 ml of 0.001N iodine. Stopper the test tube and mix thoroughly.
The blue colour produced is not discharged by 1 ml of the sample.

• Oxidizing substances - Not more than 30 mg/kg as chlorine Transfer 1 ml of the

sample into a 30-ml test tube, dilute to 20 ml with freshly boiled and cooled water,
and add 1 ml of potassium iodide TS and 1 ml of starch TS. Stopper the test tube
and mix thoroughly. The intensity of any blue colour developed does not exceed
that produced in a control prepared similarly but containing 1 ml of 0.001N iodine
(instead of potassium iodide TS) and 1 ml of reagent grade concentrated
hydrochloric acid (instead of sample).

ACIDIFIERS
• Sulfate - Not more than 0.5%
Dilute 1 g of the sample to 100 ml with water, transfer 5 ml of this dilution to a
50-ml tall-form Nessler tube and dilute to 20 ml with water. Add a drop of
phenolphthalein TS, neutralize the solution with ammonia TS, and then add 1 ml
of hydrochloric acid TS prepared from reagent grade hydrochloric acid. To the
clear solution (filtered if necessary) add 3 ml of barium chloride TS, dilute to 50
ml with water and mix. Prepare a control consisting of 1 ml of reagent grade
concentrated hydrochloric acid and 250 μg of sulfate (SO 4 ) and the same
quantities of the reagents as used for the sample. Any turbidity shown in the
sample does not exceed that in the control.
• Total organic compounds - Total organic compounds (non-fluorine): Not more
than 5 mg/kg Benzene: Not more than 0.05 mg/kg Fluorinated organic
compounds (total): Not more than 25 mg/kg See description under TESTS
• Iron - Not more than 5 mg/kg
Dilute 5 g (4.3 ml) of the sample to 40 ml and add about 40 mg of ammonium
persulfate and 10 ml of ammonium thiocyanate TS. Any red colour developed
does not exceed that in a control prepared by mixing 2.5 ml of Iron standard
solution in an equal volume of a solution containing the same quantities of
reagent grade hydrochloric acid and the reagents as used in the test.

ACIDIFIERS
• Lead - Not more than 1 mg/kg
Determine using an atomic absorption technique
appropriate to the specified level.
Free chlorine, Bromide & Iodide and sulphite
Standard: not  35% w/w and not  38% w/w of
HCl
Storage: Glass-stoppered container securely closed
at a temperature not exceeding 30C

ACIDIFIERS
Assay of HCl:
Acid – Base Titration method
An accurately weighed sample is diluted with
water and titrated with 1M NaOH using
methyl red as an indicator. End point is the
appearance of faint yellow colour.

ACIDIFIERS
 Medicinal Uses:
 Used as an acidifier / acidfying agent in
cases of achlorhydria (Lack of HCl in the
gastric juice)
 Used in the manufacture of glucose from
corn starch
 For extracting glue (gelatin) from bones
 Used as a Reagent in the laboratory

ACIDIFIERS
 Dilute Hydrochloric Acid
Preparation: By diluting 274 g of the acid with
726 g of purified water
Pps:
- Clear colourless liquid with an acid taste
- Same
Standard: not  9.5% w/w not > 10.5% w/w
Assay – same
Medicinal Uses:
- Acidifier ( dose 0.6- 8 ml)
- Laboratory reagent
ACIDIFIERS
 Sodium Phosphate
SYNONYMS : Dibasic sodium phosphate, disodium phosphate, disodium acid
phosphate, secondary sodium phosphate, Disodium hydrogen phosphate
Chemical formula - Anhydrous: Na 2 HPO 4
Hydrated: Na 2 HPO 4 · 12 H 2 O
Molecular weight: 141.98 (anhydrous)
Preparation:
1. From sodium carbonate
sodium carbonate + boiling phosphoric acid - until slightly alkaline – Pdt Crytals
Na2CO3 + H3PO4 Na2HPO4 + CO2 + H2O
2. Prepared from calcium phosphate by reacting with sulphuric acid
Ca3(PO4)2 + 2 H2SO4 Ca (H2PO4)2 + 2 CaSO4
The monophasic calcium phosphate is added with boiling water – filter – Filterate
+ sodium carbonate – Pdt cryatls

Ca (H2PO4)2 + Na2CO3 Na2HPO4 + CO2 + H2O

ACIDIFIERS
Description
Anhydrous: White, hygroscopic, odourless powder
Dihydrate: White crystalline, odourless solid
Heptahydrate: White, odourless, efflorescent crystals or granular powder
Dodecahydrate: White, efflorescent, odourless powder or crystals
When heated at 40C – colourless liquid, at 100C – anhydrous, at 300C – coverted to
sodium pyro phosphste ( Na2P4O7 )
Aqueous solution – alkaline to litmus
Combines with barium, ferric and led salts to form corresponding insoluble phosphates
BaHPO4 , FePO4 & Pb3(PO4)2

Identification
Solubility: Freely soluble in water; insoluble in ethanol pH (Vol. 4) 9.0- 9.6 (1 in 100
soln)
Test for sodium - Passes test
Test for phosphate - Passes test
Test for orthophosphate Dissolve 0.1 g of the sample in 10 ml water, acidify slightly
with dilute (acetic acid TS, and add 1 ml of silver nitrate TS. A yellow precipitate is
formed.

ACIDIFIERS
Purity
Clarity of the solution, Heavy metals, Cl-, SO42-
Loss on drying : Anhydrous: Not more than 5.0% Dihydrate: Not more than
22.0%
• Water insoluble substances : Not more than 0.2%
• Fluoride : Not more than 50 mg/kg (Method I or III)
• Arsenic: Not more than 3 mg/kg (Method II)
• Lead : Not more than 4 mg/kg , Determine using an atomic absorption
technique appropriate to the specified level.
• Reducing subsatnces: tested by adding a dilute solution of potassium
permanganate and heating on as water bath for 5 min. The red colour
should not be completely discharged
Standard:
Between 98 -101% w/w of anhydrous substance

ACIDIFIERS
Assay of Sodium phosphate:
Potentiometric titration method
1. Into a 250-ml beaker transfer about 6.5 g of the dried sample accurately
weighed.
2. Add 50 ml of 1N hydrochloric acid and 50 ml of water, and stir until the
sample is completely dissolved.
3. Place the electrodes of a suitable pH meter in the solution and titrate the
excess acid with 1N sodium hydroxide to the inflection point occurring at
about pH 4.
4. Record the burette reading and calculate the volume (A) of 1N
hydrochloric acid consumed by the sample.
5. Continue the titration with 1N sodium hydroxide until the inflection point
occurring at about pH 8.8 is reached, record the burette reading, and
calculate the volume (B) of 1N sodium hydroxide required in the titration
between the two inflection points (pH 4 to pH 8.8).
6. When (A) is equal to, or less than, (B), each ml of the volume (A) of 1N
hydrochloric acid is equivalent to 142.0 mg of Na2HPO4 . When (A) is
greater than (B), each ml of the volume 2(B) -(A) of 1N sodium
hydroxide is equivalent to sodium phosphate
ACIDIFIERS
Storage:
Storgly efflorescent – tightly closed container
Medicinal Uses:
Systemic acidifier
Buffering agent
Saline laxative
Cathartic

ACIDIFIERS
 Ammonium Chloride
Mol. Formula: NH4Cl
Preparation: HCl with ammonia
NH3 + HCl NH 4Cl
PPS:
- Pure white crystalline powder.
- odourless with saline taste
- Freely soluble in water
When heated – Volatalizes – ammonia+Hcl  cool - NH4Cl (due to this it is used as a
flux in soldering for removing the film of oxide from the surface of the metal. The
HCl formed converts the metallic oxide into chloride which, being volatile , is driven
off easily at the high temperature)
Id Tests:
Gives positive results for ammonium and chlorides
Tests for Purity
• Arsenic, Heavy metals, Iron, Sulphate
• Thiocyanate:
By adding HCl and ferric chloride solution. No red colour is produced
• Loss on Drying: drying the sample in an oven at 105C
ACIDIFIERS
Standard: not < 99.5 % w/w of NH4Cl
Storage: Tightly closed container
Assay of NH4Cl
Two methods – a) Acid-Base titration method
b) Modified Volhard’s Method
a) Acid-Base titration method
Formaldehyde previously neutralized to phenolphthalein, is added to a solution
of the substance. It fixes the ammonia in ammonium chloride as hexamine .The
liberated hydrochloric acid is titrated against 0.1M NaOH using
phenolphthalein as indicator.

4 NH4Cl + 6 HCHO (CH2)6 N4 + 4HCl + 6H2O

Ammonium chloride Hexamine

HCl + NaOH NaCl+H 2O

ACIDIFIERS
b) Modified Volhard’s Method
In modified volhard’s method a solution of the substance, acidified with nitric
acid, is shaken with the measured volume of N/10 silver nitrate, nitrobenzene
being previously added. Nitrobenzene is added to coagulate the precipitate of
silver chloride, so that it will not interfere with the titration later of excess of
silver nitrate which is determined by titration with N/10 ammonium
thiocyanate, using ferric ammonium sulphate as indicator

AgNO3 + NH4Cl AgCl + NH4NO3

AgNO3 + NH4SCN AgSCN + NH4NO3
Silver nitrate Ammonium thiocyanate Silver thiocyanate

FeNH4(SO4)2 + 3 NH4SCN Fe(SCN)3 + 2 (NH4)2SO4

Ferric ammonium sulphate Ferric thiocyanate

Medicinal Uses:
Systemic acidifier
Expectorant
Acidifier ACIDIFIERS