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ANTACIDS
Authored By:
Dr. Alex Martin
Ph.D, M.Pharm, FAGE
GASTRIC ACIDITY
High amounts of HCl in stomach is referred to as Gastric Acidity
SYMPTOMS
Abdominal pain Burping Bloating
Bad Breath
Heartburn
Gastric Reflux
Acidic state in mouth
Nausea Vomiting
Decreased appetite
Unexplained Weight Loss
Diarrhea
Gastric Ulcer Stomach Cancer
COMPLICATONS
CAUSES OF HIGH ACIDITY IN STOMACH
MECHANISM OF ACTION OF ANTACIDS
1. Is converted into its soluble salts after being acted upon by stomach HCl.
3. Raises the pH above 4.
2. Acts as weak base, it neutralizes the gastric HCl.
4. Relives acidity and associated symptoms.
The efficiency of an antacid is determined by its neutralizing capacity.
Antacids should have minimum neutralizing capacity of 5 mEq of HCl
per unit dose.
Fine particle size.
Should not cause
systemic alkalosis.
Should not act as
laxative
Should not cause
constipation
Should not cause any
side effects
Stable and readily
available
Should not evolve
large quantities of
gas on reaction
with stomach HCl.
Should produce a
pH of 4 to 6
Gradual onset and
prolonged action
Should inhibit
pepsin
IDEAL CHARACTERISTICS OF AN ANTACID
SYSTEMIC ANTACIDS
Soluble in water
Readily absorbed through GIT to blood to produce
Systemic Alkalosis and Electrolytic alterations.
Suggested in conditions of acidemia (i.e. pH of blood is below 7.35).
CKD, diabetic ketoacidosis, loss of bicarbonate ions through diarrhea
and vomiting.
NON-SYSTEMIC ANTACIDS
They produce local action by neutralizing stomach HCl.
They are not absorbed into bloodstream through
stomach and thus produce local action.
Antacids should be taken after meals to achieve
prolonged action.
I. Calcium Antacids II. Magnesium Antacids III. Aluminum Antacids
I. Calcium
containing
Antacids
II. Magnesium
containing
antacids
III. Aluminum
Containing
antacids
IV. Combination
Antacids
i) Calcium
carbonate
ii) Tribasic
Calcium
phosphate
i) Magnesium
Carbonate
ii) Magnesium
hydroxide
iii) Magnesium
phosphate
iv) Magnesium
oxide
v) Magnesium
citrate
vi) Magnesium
trisilicate
i) Aluminium
hydroxide
ii) Aluminium
phosphate
iii) Aluminium
carbonate gel
iv) Aluminum
Phosphate
v)
Dihydroxyalumini
um sodium
carbonate
vi)
Dihydroxyalumini
um aminoacetate
i) Aluminium
hydroxide gel +
Magnesium
hydroxide
ii) Aluminuim
hydroxide gel +
Magnesium
trisilicate
iii) Simethicone
containing antacids
iv) Calcium
Carbonate
containing antacids
v) Magaldrate:
Monoalium hydrate
+ hydrated
magnesium
aluminate
Simethicone is also used as an
additive in many antacids.
FAMOUS BRANDS AND THEIR INGREDIENTS
1. GELUSIL
Ingredients : Al(OH)2 +
Mg(OH)2 + Simethicone
2. DIGENE
Ingredients : Al(OH)2 +
Mg(OH)2 +
Simethicone + Sodium
carboxy
methylcellulose
SODIUM BICARBONATE
Physical Properties
MEDICINAL USES OF SODIUM BICARBONATE
1. SYSTEMIC ANTACID
Indicated in:-
1. Loss of Bicarbonate ion due to diarrhea/vomiting
2. Chronic Kidney Disease/ Dialysis
3. Diabetic ketoacidosis
2. NON-SYSTEMIC ANTACID
It provides quickest relief from stomach acidity. However, it is rapidly
absorbed into the bloodstream where it produces alkalosis.
As action is not prolonged, it is generally not used for this purpose
3. GASTRIC LAVAGE AND LAXATIVE
4. HYPERKALEMIA
5. AS AN ANTIDOTE
6. AS ADDITIVE IN LOCAL ANAESTHETICS AND COMPONENT IN MOFFET’S SOLUTION
In Moffet’s Solution(used prior to nasal surgeries)
ASSAY OF SODIUM BICARBONATE
PRINCIPLE: ACID-BASE TITRATION (ACIDIMETRY)
1.5 g NaHCO3 + 50 ml CO2
free water + Indicator
(Methyl orange)
1 M HCl solution
REACTION:
NaHCO3 + HCl NaCl + CO2 + H20
COLOUR
CHANGE
Methyl Orange in Basic solution
(YELLOW)
Methyl Orange in Mildly Acidic Solution
(ORANGE)
Ionized
Methyl
orange
Non-ionized methyl
orange
Repeat Titration to get concordant value.
Calculate the percentage purity of NAHCO3 by following equation:
% purity = Titre Value x Normality of HCl x Eq. Wt. Factor x 100
Sample Weight
Colourless
Odourless
Insoluble in water
Soluble in acidic/ alkaline
solutions
M.P. = 300°C
Amorphous powder
MEDICINAL VALUE OF ALUMINIUM HYDROXIDE
1. AS AN ANTACID
Al(OH)3 gel neutralizes the acid in the stomach. Thereby, it relieves
acidity, heartburn and abdominal discomfort.
However, because it inhibits smooth muscle cell
contraction of GIT/ Peristalsis, it can result in
constipation.
3. AS VACCINE ADJUANT
2. HYPERPHOSPHOTEMIA
In this condition, excess of phosphates builds up in the
blood due to insufficient excretion of phosphates from
kidneys.
Al(OH)3 is used as phosphate binder in hyperphosphotemia.
MAGNESIUM HYDROXIDE
Color: Silvery white Slightly soluble in water
Density: 2.345 g/cm3
Forms MgO when
heated to 360°C
Odorless
1. Extemporaneous
preparation/ Readily
available
Light Magnesium Oxide
2. Also known as Milk of Magnesia
2. As a laxative, for relief from occasional constipation
3. Owing to its ability to adsorb water, it is used as an antiperspirant in
talcum powders
THANK YOU….

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Antacids (Pharmaceutical Inorganic Chemistry)

  • 1. ANTACIDS Authored By: Dr. Alex Martin Ph.D, M.Pharm, FAGE
  • 2. GASTRIC ACIDITY High amounts of HCl in stomach is referred to as Gastric Acidity SYMPTOMS Abdominal pain Burping Bloating Bad Breath Heartburn Gastric Reflux Acidic state in mouth Nausea Vomiting Decreased appetite Unexplained Weight Loss Diarrhea Gastric Ulcer Stomach Cancer
  • 3. COMPLICATONS CAUSES OF HIGH ACIDITY IN STOMACH
  • 4. MECHANISM OF ACTION OF ANTACIDS 1. Is converted into its soluble salts after being acted upon by stomach HCl. 3. Raises the pH above 4. 2. Acts as weak base, it neutralizes the gastric HCl. 4. Relives acidity and associated symptoms. The efficiency of an antacid is determined by its neutralizing capacity. Antacids should have minimum neutralizing capacity of 5 mEq of HCl per unit dose.
  • 5. Fine particle size. Should not cause systemic alkalosis. Should not act as laxative Should not cause constipation Should not cause any side effects Stable and readily available Should not evolve large quantities of gas on reaction with stomach HCl. Should produce a pH of 4 to 6 Gradual onset and prolonged action Should inhibit pepsin IDEAL CHARACTERISTICS OF AN ANTACID
  • 6. SYSTEMIC ANTACIDS Soluble in water Readily absorbed through GIT to blood to produce Systemic Alkalosis and Electrolytic alterations. Suggested in conditions of acidemia (i.e. pH of blood is below 7.35). CKD, diabetic ketoacidosis, loss of bicarbonate ions through diarrhea and vomiting. NON-SYSTEMIC ANTACIDS They produce local action by neutralizing stomach HCl. They are not absorbed into bloodstream through stomach and thus produce local action. Antacids should be taken after meals to achieve prolonged action. I. Calcium Antacids II. Magnesium Antacids III. Aluminum Antacids
  • 7. I. Calcium containing Antacids II. Magnesium containing antacids III. Aluminum Containing antacids IV. Combination Antacids i) Calcium carbonate ii) Tribasic Calcium phosphate i) Magnesium Carbonate ii) Magnesium hydroxide iii) Magnesium phosphate iv) Magnesium oxide v) Magnesium citrate vi) Magnesium trisilicate i) Aluminium hydroxide ii) Aluminium phosphate iii) Aluminium carbonate gel iv) Aluminum Phosphate v) Dihydroxyalumini um sodium carbonate vi) Dihydroxyalumini um aminoacetate i) Aluminium hydroxide gel + Magnesium hydroxide ii) Aluminuim hydroxide gel + Magnesium trisilicate iii) Simethicone containing antacids iv) Calcium Carbonate containing antacids v) Magaldrate: Monoalium hydrate + hydrated magnesium aluminate
  • 8. Simethicone is also used as an additive in many antacids.
  • 9. FAMOUS BRANDS AND THEIR INGREDIENTS 1. GELUSIL Ingredients : Al(OH)2 + Mg(OH)2 + Simethicone 2. DIGENE Ingredients : Al(OH)2 + Mg(OH)2 + Simethicone + Sodium carboxy methylcellulose SODIUM BICARBONATE Physical Properties
  • 10. MEDICINAL USES OF SODIUM BICARBONATE 1. SYSTEMIC ANTACID Indicated in:- 1. Loss of Bicarbonate ion due to diarrhea/vomiting 2. Chronic Kidney Disease/ Dialysis 3. Diabetic ketoacidosis 2. NON-SYSTEMIC ANTACID It provides quickest relief from stomach acidity. However, it is rapidly absorbed into the bloodstream where it produces alkalosis. As action is not prolonged, it is generally not used for this purpose
  • 11. 3. GASTRIC LAVAGE AND LAXATIVE 4. HYPERKALEMIA 5. AS AN ANTIDOTE 6. AS ADDITIVE IN LOCAL ANAESTHETICS AND COMPONENT IN MOFFET’S SOLUTION In Moffet’s Solution(used prior to nasal surgeries)
  • 12. ASSAY OF SODIUM BICARBONATE PRINCIPLE: ACID-BASE TITRATION (ACIDIMETRY) 1.5 g NaHCO3 + 50 ml CO2 free water + Indicator (Methyl orange) 1 M HCl solution REACTION: NaHCO3 + HCl NaCl + CO2 + H20
  • 13. COLOUR CHANGE Methyl Orange in Basic solution (YELLOW) Methyl Orange in Mildly Acidic Solution (ORANGE) Ionized Methyl orange Non-ionized methyl orange
  • 14. Repeat Titration to get concordant value. Calculate the percentage purity of NAHCO3 by following equation: % purity = Titre Value x Normality of HCl x Eq. Wt. Factor x 100 Sample Weight Colourless Odourless Insoluble in water Soluble in acidic/ alkaline solutions M.P. = 300°C Amorphous powder
  • 15. MEDICINAL VALUE OF ALUMINIUM HYDROXIDE 1. AS AN ANTACID Al(OH)3 gel neutralizes the acid in the stomach. Thereby, it relieves acidity, heartburn and abdominal discomfort. However, because it inhibits smooth muscle cell contraction of GIT/ Peristalsis, it can result in constipation.
  • 16. 3. AS VACCINE ADJUANT 2. HYPERPHOSPHOTEMIA In this condition, excess of phosphates builds up in the blood due to insufficient excretion of phosphates from kidneys. Al(OH)3 is used as phosphate binder in hyperphosphotemia. MAGNESIUM HYDROXIDE Color: Silvery white Slightly soluble in water Density: 2.345 g/cm3 Forms MgO when heated to 360°C Odorless
  • 17. 1. Extemporaneous preparation/ Readily available Light Magnesium Oxide 2. Also known as Milk of Magnesia 2. As a laxative, for relief from occasional constipation 3. Owing to its ability to adsorb water, it is used as an antiperspirant in talcum powders