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Experiment No. 04
Name of the Experiment: Formulation and preparation of Antacid Suspension.
(Each 5 mL contains Aluminum Hydroxide 200 mg and Magnesium Hydroxide 400 mg)

Introduction:
Suspensions may be defined as a coarse dispersion in which finely divided insoluble drug
particles (the suspensoid) generally greater than 1µm in diameter are dispersed uniformly
throughout a liquid medium in which the drug exhibits a minimum degree of solubility.
A coarse suspension is a dispersion of finely divided, insoluble solid particles (the disperse phase)
in a fluid (the dispersion medium or continuous phase). Most pharmaceutical suspensions consist of
an aqueous dispersion medium, although in some instances it may be an organic or oily liquid.
A gastric antacid is a chemical substance introduced into the stomach for the purpose of
lowering the hydrogen ion concentration, or acidity, of the gastric contents; resulting in an
increase in the pH of stomach and duodenum. Gastric acidity occurs due to excessive secretion of
HCl in stomach due to various reasons. The suspension form of antacids is given for faster
absorption, because the rate of dissolution is higher than tablets. It is because of resulting from
higher surface area provided by smaller fine particles.
Such antacids are in common use in medical practice, mostly in the treatment of peptic ulcer.
They react with gastric HCl and neutralize the acids as follows:
Al (OH) 3+3HCl⭢AlCl3+3H2O
Mg(OH)2+2HCl→MgCl2+2H2O
Classification:

a. Systemic Antacid:

Systemic antacids are antacids which get systemically absorbed. They are capable of producing
metabolic alkalosis because the certain moiety does not form insoluble basic compound in the
intestine e.g. NaHCO3, KHCO3, Na-citrate etc.

b. Non Systemic Antacid:

A non- insoluble basic systemic antacid is one which forms insoluble basic compound in the
intestine and is not subsequently absorbed. So these antacids do not produce systemic alkalosis.
e.g. Al(OH)3,Ca(OH)2 Mg(OH)2, Ca3(PO4)2,Mg-trisilicate.

Apparatus:
1. Beaker 3.Stirrer 5. Measuring cylinder 7. Droppers

2. Mortar 4.Pestle 6. Funnel 8. Electric balance

Recipe:
Note: Actual 5 mL formulation contains dried Al (OH) 3 Gel USP equivalent to 200 mg Al2O3,
400mg Mg(OH)2 BP and 30 mg Simethicone USP (which is omitted here).

For 60 mL Antacid Suspension (Calculation is only for Al(OH)3):

Each 5 mL contains 200 mg Al(OH)3

Then 60 mL contains = 200  60 mg of Al(OH)3

5
=2400 mg of Al(OH)3
=2.4 gm of Al(OH)3

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Formula:
Each 5 mL suspension contains 200 mg of Al(OH)3 & 400 mg of Mg(OH)2

Name of the Weight Purpose/Justification Working

ingredient Formula (40mL)
Dried Aluminium 2.4 gm API. Gastric antacid. 1.6 gm
Hydroxide
Magnesium hydroxide 4.8 gm API. Gastric antacid. 3.2 gm
Na-CMC BP 0.4 gm Suspending agent 0.268 gm
Retard crystallization 2 Ml
Glycerin BP 3 mL
of sucrose;Sweetener,
Humectant.
Viscosity imparting agent; 6.7 mL
Sorbitol Solution (70%) 10
Humectant,Sweetener; Anti-
BP mL
crystallization Agent
Methyl 4- 100 mg / 0.1 gm Antimicrobial Preservative. 0.067 gm/ 67 mg
Hydroxybenzoate BP
Propyl 4- 10 mg / 0.01 gm Antimicrobial Preservative. 0.0067 gm/ 6.7mg
Hydroxybenzoate BP
Saccharine Sodium BP 15 mg / 0.015 gm Sweetening agent. 500 × more 0.01 gm/ 10 mg
sweet than sucrose
Sodium Citrate BP 50 mg / 0.05 gm Flocculating agent. 0.33gm/ 33.5 mg
Flavour Q.S.
Improving organoleptic Q.S.
Colour Q.S properties.
Purified Water BP Q.S. to 60 mL Solvent/Vehicle. Q.S. up to 40 mL
Method of Preparation:

1. Take 2.4 gm Al (OH) 3 & 4.8 gm Mg(OH)2 in a mortar. Crush them properly and then dissolve
them in 10 mL DW with continuous trituration by pestle in order to get a uniform mixture.

2. Then take 0.4 gm Na-CMC along with 10 mL DW in a 50 mL beaker. Mix it slowly to make
uniform mucilage.

3. Now mix the Al(OH)3 & Mg(OH)2 solution (previously made in the step one) and Na-
CMC mucilage (from the step two) in a 250 mL beaker. Appropriately blend these two solutions to
get a homogenous mixture.

4. Afterwards add 10 mL Sorbitol solution, 3 mL Glycerine, 0.1 gm Methyl Hydroxybenzoate,

0.01 gm Propyl Hydroxybenzoate, 0.015 gm Saccharine sodium and 0.05 gm Na-Citrate. Mix them
thoroughly with continuous stirring.

5. Finally add organic oil (Flavor) with triturate to mix it with the preparation properly.

6. Take the final solution in a measuring cylinder and adjust the volume to 60 mL by adding
sufficient quantity of purified water.

7. From the cylinder, transfer the final preparation in a well-polished bottle. Finally cork & label
the bottle.
Function of ingredients:

1. Al(OH)3 and Mg(OH)2: Al(OH)3 and Mg(OH)2 are the active part of the preparation. They
act as antacid and serve to reduce acidity.

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Properties: Al(OH)3
√ Physical form : Amorphous powder
√ Color : White
√ Odor : Odorless
√ Solubility : Soluble in dilute mineral acids and aqueous solutions of Alkali
hydroxides. Insoluble in water.

Properties: Mg (OH)2
√ Physical form : Fine amorphous powder
√ Color : White
√ Odor : Odorless
√ Solubility : Soluble in dilute acids. Insoluble in water.

2. Na-CMC: Carmellose sodium

Carboxymethylcellulose Sodium is widely used in oral and topical pharmaceutical formulations,

primarily for its viscosity-increasing properties.

Properties:

i. It occurs as a white to almost white

ii. Odourless and tasteless
iii. Granular powder
iv. It is hygroscopic after drying
v. Easily dispersed in water at all temperatures, forming clear, colloidal solutions.
The aqueous solubility varies with the degree of substitution.

Function:
🞛 Suspending agent 🞛 Stabilizing agent
🞛 Viscosity-increasing agent 🞛 Water-absorbing agent

3. Glycerin:( Glycerol; Glycerine)

Glycerin is used in a wide variety of pharmaceutical formulations including
oral, otic, ophthalmic, topical, and parenteral preparations.
Glycerin has preservative qualities and is often used as a stabilizer and as an auxiliary solvent in conýunction with water or
alcohol.

Properties:
i. Clear, colorless, odorless iii. Viscous
ii. Hygroscopic liquid iv. Sweet in taste (App. 0.6 times as sweet as sucrose)

Functions:
🞛 Solvent, Co-solvent 🞛 Humectant
🞛 Antimicrobial preservative 🞛Viscosity increasing agent
🞛 Sweetening agent 🞛 Retard crystallization of sucrose
4. Sorbitol Solution
Sorbitol is D-glucitol. It is a hexahydric alcohol related to mannose and is isomeric with mannitol.

Sorbitol: Sorbitol is widely used as an excipient in pharmaceutical formulations.

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Properties:
i. Odorless, white or almost colorless iii. Crystalline
ii. Hygroscopic powder iv. Sweet in taste

Functions:
🞛 Prevent crystallization of sugar around the cap of bottles 🞛Sweetener
🞛 Vehicle in sugar-free formulations 🞛 Stabilizing agent 🞛 Humectant

5. Methyl & Propylparaben: (parabens : Alkyl esters of p-hydroxybenzoic acid )

Methylparaben is widely used as an antimicrobial preservative in cosmetics, food products, and pharmaceutical formulations.

Methylparaben
Properties:
i. Colorless crystals or a white crystalline powder
ii. Odorless or almost odorless .
iii. Slight burning taste.
Propylparaben
Properties:
i. White iii. Odorless
ii. Crystalline powder iv. Tasteless

Function
i. Methylparaben & Propylparaben (10:1) exhibit antimicrobial activity over the pH range 4–8.
ii. They are also more active against Gram-positive than against Gram-negative bacteria.
Activity may be improved by using combinations of parabens, as synergistic effects occur.

6. Saccharine Sodium Saccharinum

Properties:
i . White crystalline powder.
ii. Odorless or faintly aromatic.
iii. Efflorescent. SACCHARIN-Na SACCHARIN
iv. It has an intensely sweet taste, with a metallic or bitter aftertaste.

Functions:
♦ Sweetening agent (approximately 300–600 times sweet than sucrose).
♦ Saccharin sodium enhances flavor systems and may be used to mask some unpleasant
taste characteristics.

7. Sodium Citrate (dihydrate) Trisodium citrate; C6H5Na3O7.2H2O

Properties:
i. Monoclinic crystals or a white crystalline powder.
ii. Odorless, colorless.
iii. Cooling, saline (sour) taste.
iv. It is slightly deliquescent in moist air and efflorescent in warm dry air.

Functions:
♦ Buffering agent ♦ Sequestering agent ♦ Preservatives and Antioxidants
♦ Alkalizing agent ♦ Emulsifying agent ♦ Processing Aids and Additives

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Other ingredient(s) used:
Peppermint Oil : It is used as flavouring agent. Green banana flavour

Indications: Antacid Suspension is indicated for-

🞛 Dyspepsia, 🞛 Hyperacidity, 🞛 Gastric and duodenal ulcer,

🞛 Gastritis; 🞛 Relief of flatulence, 🞛 Abdominal distention and
🞛 Windy colic.

Dosage & Administration:

1-2 teaspoonfuls one hour after meals and at bed time or as directed by the physician.

Warning & Precautions:

Drugs containing Al(OH)3 shouldn’t be taken concomitantly with any form of Tetracycline, as the
absorption of the later may be affected. Al(OH)3 may also reduce the absorption of Digoxin.

Side effects:
1. Theoretically, if the gastric pH is raised too much, acid rebound may occur, since an effort to
maintain a lower pH, the stomach secretes additional HCl acid which consumes the antacid.

2. A second potential problem is systemic alkalosis. If the antacid is sufficiently water soluble
and is composed of readily absorbable ions, the antacid may be absorbed and exert its alkaline
effort on the body’s buffer system.

3. Another problem is sodium content of antacid. Those patients who are sodium restricted, diet
should be advised of this when antacid is recommended.

4. The 4th side effect is the local effect is the GIT. Antacid containing calcium and aluminum salts,
after being converted to soluble salt by gastric acid, tend to constipating, while containing
magnesium salts tend to have a laxative effect.

Market preparation: Antacid Suspension

SL. Trade/Brand Name Manufacturer Dosage form

01 Ancid Plus Renata Limited Suspension
02 Avlocid ACI Limited Suspension
03 Entacyd Square Pharmaceuticals Ltd. Suspension
04 Epazel Edruc Ltd Suspension
05 Pentocil Albion Pharmaceuticals Suspension

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