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Файл:Ординатура / Хирургия / Библиотека им академика М.И. Перельмана / Книга_5265_Библиотеки_им_академика_М_И_Перельмана.pdf
Inorganic Pharmaceuticals 77
Marketed Preparations of Ferric Ammonium Citrate:
Brand Name
Dosage Form
Company
Feriop
Feriop syrup formulation containing: (Ferric
Ammonium Citrate, Folic Acid & Cyanocobalamin)
• Ferric ammonium citrate – 160 mg
• Folic acid – 0.5 mg
• Cyanocobalamin (Vitamin B
12
)
– 7.5 mcg
• Cupric sulphate – 30 mcg
• Manganese sulphate – 30 mcg
.
Wellmed Pharma
Ricson
Remedies
Syrup: Composition: Each 5 ml contains:
• Ferric Ammonium Citrate I.P. – 200
mg (equivalent to elemental iron 40 mg)
• Cyanocobalamin I.P. – 7.5 mcg
• Folic Acid I.P. – 0.5 mg
• Zinc Sulphate I.P. – 7 mg
• Pyridoxine HCL I.P. – 1.5 mg
• Sorbitol Solution (70%) I.P. – 750 mg
(Non-crystallising)
• Flavored syrupy base
• Color: Caramel
Rickson Remedies
Xenado
Oral Drops: Each 15 ml contains:
Vitamin A 5000 IU + Vitamin D
3
400 IU + Vitamin
B
12
5 mcg + Folinic acid 0.2 mg + Ferric Ammonium
Citrate 25 mg + Lysine 100 mg + Vitamin B
1
1 mg +
Vitamin B
2
1 mg + Vitamin B
6
1 mg + Niacinamide 5
mg + D-Panthenol.
Seagull
Laboratories (I)
Pvt. Ltd.
Storage: Keep Ferric ammonium citrate in a tightly closed container. Store it in a cool, dry and
ventilated area. Protect it from light and physical damage. Observe all warnings and precautions
listed for the product. Properly discard this product when it is expired or no longer needed.
3.1.4 Ferrous Ascorbate
Molecular formula: C
12
H
14
FeO
12
Molecular weight: 406.08
Synonym: L-ascorbate, ferrous cevitamate
Ferrous ascorbate is the organic compound which belongs to the class of butenolides. These
are dihydrofurans with a carbonyl group at the C2 carbon atom. It is a synthetic chelate of iron in
the ferrous state with ascorbic acid.
78 Text Book of Pharmaceutical Chemistry
Preparation: Ferrous ascorbate is prepared by the reaction of ferrous sulphate with barium
ascorbate in water under nitrogen atmosphere. After the completion of the reaction, solid ferrous
ascorbate is separated out, filtered and collected.
Uses of Ferrous Ascorbate:
➢ Ferrous ascorbate is used as an iron supplement, used to treat or avoid low iron levels in
the blood.
➢ Ferrous ascorbate is used in the treatment of anaemia due to chronic kidney failure.
➢ It is used to treat iron deficiency-related haemoglobin disorders.
➢ Ferrous ascorbate + Folic acid are also important in pregnancy because of its role in the
brain and spinal cord development of the unborn baby.
➢ Ferrous ascorbate acts as a catalyst, stimulates the transport and use of oxygen, and
helps in cell growth and proliferation.
➢ It increases the production of red blood cells and haemoglobin.
➢ Vitamin C present in ferrous ascorbate aids in the effective and maximum absorption of
dietary iron.
➢ Ferrous Ascorbate acts as a health supplement for those with low iron content in their
diet.
Pharmaceutical Formulations: It is used in range of nutraceutical and health care preparations
like liquid, capsule and tablet, etc.
➢ Tablet: 100 mg (equivalent to elemental iron)
➢ Suspension: 30 mg/5 ml,
➢ Syrup: 30 mg/5 ml, 35 mg/5 ml
➢ Capsule (Soft gelatin): 100 mg
1. Ferrous Ascorbate Tablet
➢ Ferrous ascorbate – 100 mg
➢ Folinic acid – 1.5 mg
➢ Zinc sulphate – 61.5 mg
2. Ferrous Ascorbate Film Coated Tablet with Folic Acid
➢ Ferrous ascorbate – Equivalent to elemental iron 100 mg
➢ Folinic acid – 15 mg
➢ Excipients – q.s.
➢ Vitamin – Appropriate dose
➢ Color – Red oxide of iron and titanium dioxide
Inorganic Pharmaceuticals 79
3. Ferrous Ascorbate Syrup 200 ml with Folic Acid and Zinc Sulphate
➢ Ferrous ascorbate – 30 mg
➢ Folinic acid – 550 mg
➢ Zinc sulphate – 7.5 mg
Marketed Preparations of Ferric Ammonium Citrate:
Brand Name
Dosage Form
Company
Ferojin-XT
Tablets: Ferrous Ascorbate, Folic Acid and Zinc
• Ferrous Ascorbate – 100 mg
• Folinic acid – 1.5 mg
• Zinc sulphate – 61.5 mg
J.P. Biotech
Iromits-XT
Syrups:
• Ferrous Ascorbate, Folic Acid – 200 ml
MITS Healthcare Pvt.
Ltd.
I-BAR XT
Soft Gelatin Capsules:
• Ferrous Ascorbate – 100 mg
• Folinic Acid – 5 mg
• Adenosylcobalamin – 100 mg
Soigner Pharma
Orofer-XT
Tablets:
• Ferrous Ascorbate – 100 mg
• Folic Acid – 1.5 mg
Emcure
Pharmaceuticals
Limited
Tab Feromind
Tablets:
• Ferrous Ascorbate – 100 mg
• Folic Acid – 1.5 mg
Medi Mind Drugs and
Chemicals
Storage:
➢ Ferrous Ascorbate avoids direct contact with heat, air and light; it may damage
medicines. The exposure to medicine may cause some harmful effects.
➢ It must be kept in a safe place and out of children’s reach.
➢ It should be kept at room temperature between 68ºF and 77ºF (20ºC and 25ºC).
➢ Follow the prescription and follow doctor advice whenever you take Ferrous Ascorbate.
3.1.5 Carbonyl Iron
Molecular Formula: Fe(CO)
5
Molecular Weight: 195.9 g/mol
Synonym: Iron pentacarbonyl
Brand Names: Feosol Caplet, Icar, Iron Chews
80 Text Book of Pharmaceutical Chemistry
Preparation: Iron carbonyl is a compound of iron and carbon monoxide (CO) in which carbon
monoxide ligands are coordinated to an iron atom or a plurality of iron atoms. Iron carbonyl is
prepared by reacting carbon monoxide with solid reactive iron, at a pressure of from 5 to 30 MPa,
and from 150 to 200°C. To this end, carbon monoxide is passed over the iron in a reactor; the iron
carbonyl which form is removed in a condenser from the gas is a free-flowing, straw-colored
liquid with a pungent odor.
FeI
2
+ 4CO → Fe(CO)
4
I
2
5Fe(CO)
4
I
2
+ 10Cu → 10CuI + 4Fe(CO)
5
+ Fe
Properties: Liquid iron carbonyl occurs as yellow liquid, with the formula Fe(CO)
5
, boiling is at
102°C. It is straw-colored liquid with a pungent odor and the salts of iron have usually only a
feeble color. Its higher boiling point is due to the introduction of more carbon monoxide. It is
insoluble in cold water, hot water, alkali, ethanol and ether; soluble in hydrochloric acid, sulfuric
acid and dilute nitric acid; and insoluble in concentrated acid and dilute alkali solution.
Uses of Iron Carbonyl:
➢ Iron carbonyl used in the treatment of iron-deficiency anemia.
➢ Carbonyl iron powder is used as an iron dietary supplement.
➢ It is used as a reducing agent; for the electronics industry, powder metallurgy and the
production of iron salts.
➢ It needs to produce red blood cells and keep person in good health.
➢ Carbonyl iron is safe for use during pregnancy and is prescribed as a component of
prenatal vitamin/mineral supplements.
Pharmaceutical Formulations: Carbonyl iron is available under the following different brand
names: Feosol (Carbonyl Fe), Icar C, Icar Pediatric, and Irco.
➢ Tablet: 45 mg (Feosol), 66 mg (Ircon)
➢ Oral Suspension: 15 mg/1.25 ml (Icar Pediatric)
➢ Tablet, Chewable: 15 mg (Icar Pediatric, Wee Care)
➢ Tablet with Vitamin C: 100 mg iron/250 mg vitamin C (Icar C)
1. Carbonyl Iron Syrup 200 ml with Folic Acid and Zinc Sulphate
➢ Carbonyl Iron – 60 mg
➢ Folic Acid I.P. – 1 mg
➢ Zinc Sulphate – 11 mg
2. Carbonyl Iron Hard Gelatin Capsule with Folic Acid and Zinc Sulphate
Each CARISTA hard gelatin capsule contains:
Inorganic Pharmaceuticals 81
➢ Carbonyl Iron (equivalent to elemental iron) – 100 mg
➢ Folic Acid – 1.5 mg
➢ Vitamin B
12
– 15 mcg
➢ Vitamin C – 75 mg
➢ Zinc Sulphate Monohydrate (equivalent to elemental zinc) – 61.8 mg
3. Carbonyl Iron, Folic Acid and Zinc Sulphate Capsules
Each hard gelatin capsule contains:
➢ Carbonyl Iron – 50 mg (equivalent to elemental Iron)
➢ Zinc Sulphate Monohydrate I.P. – 61.8 mg (equivalent to elemental Zinc)
➢ Folic Acid I.P. – 0.5 mg
➢ Excipients – q.s.
Marketed Preparations of Carbonyl Iron:
Brand Name
Dosage Form
Company
Cofol-Z
capsule
Cofol-Z capsule:
• Folic Acid (Vitamin B
9
) – 0.5 mg
• Zinc Sulphate – 61.8 mg
• Carbonyl Ferrous – 50 mg
Cipla Limited
Forbon
Syrup 200 ml:
• Carbonyl Iron – 50 mg
• Folic Acid I.P. – 1.5 mg
• Cyanocobalamine – 10 mcg
• Zinc Sulphate Monohydrate (Elemental) –22.5 mg
Gynae Range
Irolash
Capsules:
• Carbonyl Iron + Folic Acid + Zinc Sulphate
Kenvish Healthcare
Feri-Max
Capsules:
• Elemental Iron – 100 mg
• Folic Acid I.P. – 1 mg
• Zinc Sulphate Monohydrate I.P. – 61.8 mg
Max Qure Labs
Storage:
➢ Store at room temperature.
➢ Keep away from moisture and heat.
➢ Overdose of iron accidentally in children can be fatal.
➢ Keep the medicine out of the reach of children.
82 Text Book of Pharmaceutical Chemistry
3.2 GASTROINTESTINAL AGENTS
Digestive system is made up of the gastrointestinal tract (alimentary canal) and other organs,
such as the liver, pancreas and gallbladder. The GI tract contains all the major organs of the
digestive system, including the mouth, pharynx (throat), esophagus, stomach, small intestine
(consists of three parts: the duodenum, the jejunum and the ileum) and large intestine (consists of
cecum, the ascending (right) colon, the transverse (across) colon, the descending (left) colon, and
the sigmoid colon, which connects to the rectus), food taken in through the mouth is digested to
extract nutrients and absorb energy, and the waste expelled at the anus as feces.
A number of different conditions or diseases can affect the GI tract and have an impact on the
digestive system includes:
➢ Achlorhydria is a condition in which the stomach does not produce hydrochloric acids
(HCl). It is a more severe form of hypochlorhydria; a deficiency of stomach acids.
➢ Hyperacidity: Acidity, sometimes known as hyperacidity, is a common medical problem
in which the stomach produces excessive acid. Hyperacidity is a condition that occurs
when the stomach has an excessive amount of hydrochloric acid. It can lead to a wide
range of symptoms such as stomach pain discomfort, vomiting, loss of appetite,
flatulence, and heartburn.
➢ Diarrhoea caused by infections of the bowels by various bacteria, viruses or parasitic,
diarrhoea caused by any of these infections is referred to as gastroenteritis. It is
characterized by abnormally loose or watery stools.
➢ Infrequent bowel movements or difficult passage of stools that persists for several
weeks or longer is called constipation.
Gastrointestinal (GI) agents are the classes of drugs that are used to treat gastrointestinal
disorders. It includes 5-aminosalicylates, antacids, antidiarrheals, digestive enzymes, functional
bowel disorder agents, gallstone solubilizing agents, GI stimulants, H. pylori eradication agents,
H2 antagonists, laxatives and proton pump inhibitors.
Classification of Gastrointestinal (GI) Agents:
1. Acidifying agents: Drugs that increase the gastric acidity, e.g., dil. HCl.
2. Antacids: Drugs that neutralize the excess HCl, e.g., Aluminium hydroxide gel, Sodium
Bicarbonate, Calcium carbonate, etc.
3. Protective and adsorbent: These drugs are used in the treatment of diarrhea, e.g.,
Bismuth subcarbonate, Kaoline, etc.
4. Saline cathartics: These drugs are used to relieve constipation, e.g., Magnesium
sulfate, Sodium potassium tartrate, etc.
Inorganic Pharmaceuticals 83
Antacids
Antacids are a class of drugs that help to reduce the amount of acid in the stomach. They are
commonly used to treat symptoms including stomach distress, heartburn, acid reflux and acid
indigestion caused by too much stomach acid.
Antacids act by neutralizing stomach acid and lowering the amount of acid refluxed into the
esophagus or duodenum. Antacids are bases (alkalis) that are the opposites of acids
(neutralization is the reaction between an acid and a base).
They also work by inhibiting the activity of pepsin, a digestive enzyme secreted in the
stomach that is responsible for normal meal digestion.
The most common antacids that are commonly used include aluminium hydroxide,
magnesium hydroxide and magnesium trisilicate. Sodium bicarbonate is a rapidly acting antacid,
but it should not be used for long-term treatment in peptic ulcer disease as it is absorbed in the
intestines and may cause metabolic alkalosis.
Ideal Properties of Antacids
➢ It should be cheaper.
➢ It should exert action gradually and have longer duration of action.
➢ It should be insoluble in water and have fine particle size.
➢ It should not be absorbable in water and cause systemic alkalosis.
➢ It should inhibit pepsin/proteolytic enzyme.
➢ It should not be a laxative or cause constipation.
➢ It should not cause any side-effects.
➢ It should be stable and readily available.
➢ It should not evolve large quantities of gas on reacting with hydrochloric acid.
➢ The antacid should buffer in the pH range 4 to 6.
Classification of Antacids
Antacids are classified into two categories: (a) Systemic (absorbable) antacids and (b) Non-
systemic (non-absorbable) antacids.
(i) Systemic antacids: These types of antacids are compounds which get systemically
absorbed and produce systemic alkalosis, e.g., Sodium bicarbonate, Potassium citrate,
etc.
(ii) Non-systemic antacids or Non-absorbable antacids: These compounds are
insoluble, poorly absorbed systemically, and does not produce systemic alkalosis. These
types of compounds are again divided into following sub-categories:
➢ Calcium containing antacid: e.g., Calcium carbonate, Calcium hydroxide, Tribasic
Calcium phosphate, etc.
84 Text Book of Pharmaceutical Chemistry
➢ Magnesium containing antacid: e.g., Magnesium carbonate, Magnesium trisilicate,
Magnesium oxide, etc.
➢ Aluminium containing antacids: e.g., Aluminium hydroxide, Aluminium phosphate,
etc.
➢ Combination antacid preparation: e.g., Aluminium hydroxide gel and
Magnesium hydroxide, Aluminium hydroxide gel and Magnesium trisilicate,
Aluminium hydroxide gel, Calcium carbonate and Magnesium hydroxide,
Aluminium hydroxide gel and Calcium carbonate, etc.
3.2.1 Aluminium Hydroxide Gel
Chemical Formula: Al(OH)
3
Molecular Weight: 78.0
Synonym: Aluminic acid, hydrated alumina, Orthoaluminic acid.
Properties: Aluminium hydroxide is an aqueous white, light odorless, tasteless amorphous
powder. It is soluble in dilute mineral acids and in solution of alkali hydroxides but practically
insoluble in water. It forms gel on prolonged contact with water at pH 5.5-8.0. It absorbs acids
and carbon dioxide. The aluminium hydroxide gels are ideal buffers in the pH 3-5 range due to its
amphoteric nature. Aluminum hydroxide is accepted in two forms in USP.
1. Gel USP XVIII: White viscous suspension, small amount of clear liquid may separate
on standing. It has a pH USP which permits inclusion of flavoring and antimicrobial
agent.
2. Dried Gel USP XVIII: Dried aluminium hydroxide gel is white, odorless, colorless,
tasteless, amorphous powder, soluble in dilute mineral acids but insoluble in water and
alcohol. It is a common antacid drug that is used in pharmaceutical preparations. Al
2
O
3
content is between 47.0% to 60.0%.
Preparation: It is prepared by dissolving sodium carbonate in not water & the solution is filtered.
To the filtrate add clear solution of alum in water with constant stirring. Add more of water and
remove all gas. The Aluminium Hydroxide precipitate out, collect the precipitate, wash and
suspend in sufficient purified water.
3NaCO
3
+ 2KAl(SO4)
2
+ 3H
2
O → 3NaSO
4
+ K
2
SO
4
+ 2AI(OH)
3
+ 3CO
2
Potash alum
If sodium carbonate solution is added to potash alum solution, then it is difficult to wash out the
sulphate completely. Due to adsorption by aluminum hydroxide, some carbonate may be present.
Test for Identification: A solution in 2N HCl gives the characteristic reactions of aluminum
salts. To the sample, add 5 drops of freshly prepared 0.05% w/v solution of quinalizarin in 1%
w/v solution of NaOH. When heated to boiling, cooled and acidified with excess of acetic acid, a
reddish violet color is produced.
Inorganic Pharmaceuticals 85
Medicinal and Pharmaceutical Uses:
➢ It is used as an active medicament in antacid formulations.
➢ It is used in manufacturing of colored lakes, inks, catalysts carrier, etc.
➢ It is used as protective in treating peptic ulcers.
➢ It is used to treat symptoms of increased stomach acid such as heartburn, upset stomach,
sour stomach, or acid indigestion.
➢ It is used in cases of acute hyperacidity.
➢ It is used to reduce phosphate levels in people with certain kidney conditions.
Pharmaceutical Formulations:
➢ Aluminum hydroxide/magnesium hydroxide systemic – Brand names: Alamag, Maalox
TC, ConRx AR, Rulox
➢ Aluminum hydroxide/magnesium hydroxide/simethicone systemic – Brand names:
Mylanta, Maalox, Mylanta Maximum Strength
Storage Conditions: Store it in a tightly closed container, in a cool, dry, well-ventilated area
away from incompatible substances. It is stable under normal temperatures and pressures. It
absorbs carbon dioxide from the air. It gels on prolonged contact with water. It absorbs acids.
When co-precipitated with bismuth hydroxide and reduced by hydrogen, it becomes violently
flammable in air.
Market Preparations:
➢ Aluminium Hydroxide (Gel) I.P.
➢ Dried Aluminium Hydroxide Gel Magnesium Hydroxide – Milstein Pharma
➢ Aluminium Hydroxide Gel, 250 mg – Iva Healthcare Pvt. Ltd.
3.2.2 Magnesium Hydroxide
Chemical Formula: Mg(OH)
2
Molecular Weight: 58.3197 g/mol
Synonym: Magnesium hydroxide, Hydroxide, Hydrated oxide
Magnesium hydroxide is naturally occurring as the mineral brucite. In the chemical structure,
the central Mg is bonded to the two hydroxyl groups. The compound is ionic, existing mainly as
Mg
2+
and OH
–
ions.
Preparation of Magnesium Hydroxide: Magnesium hydroxide is prepared by the following
methods:
1. It is prepared by the reaction between the aqueous solution of magnesium chloride and
sodium hydroxide by precipitation. The chemical equation for the reaction is given
below:
MgCl
2
(aq) + 2NaOH (aq) → Mg(OH)
2
(s) + 2NaCl (aq)
86 Text Book of Pharmaceutical Chemistry
2. Magnesium hydroxide is precipitated when a solution of magnesium salts is combined
with alkaline water. The net ionic equation for such reaction can be given as:
Mg
2+
+ 2OH
−
→ Mg(OH)
2
3. Commercially, Magnesium hydroxide is produced by treating lime and seawater.
Approximately, one ton of magnesium hydroxide is obtained from 600 m
3
of seawater.
Calcium hydroxide is more soluble in magnesium hydroxide. Therefore, Mg(OH)
2
precipitates as a solid. The reaction is as follows:
MgO + H2O → Mg(OH)
2
Properties: Magnesium hydroxide occurs as a white, odorless, crystalline solid with a density of
2.34 g/ml, and a melting point of 350°C. It is almost insoluble (very low solubility) in water and
ethanol, but dissolves dilute acid.
Uses: The list of uses of Magnesium Hydroxide is given below:
➢ It is used as a laxative to improve bowel movements and to loosen the stool.
➢ It is widely used in wastewater treatment, as acidic waste water can be neutralized by
adding magnesium hydroxide.
➢ A suspension of magnesium hydroxide is widely used as an antacid which is called milk
of magnesia.
➢ It is used as a food additive, generally recognized as a safe food additive by FDA.
➢ Brucite, which is naturally occurring mineral of magnesium hydroxide, is widely used as
a fire retardant.
➢ It is used in wet plate collodion process as a photographic fixer.
➢ In the cosmetic industry, magnesium hydroxide is used as a pH controlling agent.
➢ It is also used as a fuel additive to treat heavy oil fuels and crude oils.
➢ Magnesium hydroxide is used as an antiperspirant.
Storage Conditions: MgOH
2
must not exceed 100°F during delivery storage. It should be kept in
original containers, in indoor storage areas away from humidity and at least one meter away from
heating devices.
Dosage Forms: Oral concentrate (24%); oral suspension (8%); oral tablet, chewable (400 mg).
Pharmaceutical Formulations:
1. Milk of Magnesia I.P. 340ml
Ingredient with quantity:
Magnesium hydroxide I.P. – 8.0% w/w
(Hydrated Magnesium oxide calculated as Magnesium hydroxide I.P.)
Water: Up to 340 ml
Dose: Laxatives: 15-30 ml
Antacids: 5-15 ml