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Файл:Ординатура / Хирургия / Библиотека им академика М.И. Перельмана / Книга_5265_Библиотеки_им_академика_М_И_Перельмана.pdf
Inorganic Pharmaceuticals 97
Topical agents mainly classified into various categories based on their usual action:
➢ Protectives and adsorbents
➢ Antimicrobial and astringent compounds
➢ Antiseptics
➢ Germicides
➢ Protectives
➢ Astringents
➢ Emollients
➢ Demulcents
➢ Cleaning agents
Protectives and Adsorbents
Protective referred to as any agent that protects the exposed surface (skin or other
membranes) from harmful or annoying stimuli by mechanical or other physical means. Protective
and adsorbents adsorb toxins, bacteria, viruses and provide a protective coating along intestinal
mucosa. These drugs are commonly used for the treatment of mild diarrhea.
Diarrhoea is defined as the abnormal frequent passing of loose, watery and unformed stool
with increased frequency, fluidity, and weight. The majority of cases of acute diarrhoea are
caused by a bacterial, viral, or parasitic infection of the intestines. Chronic diarrhoea can also be
caused by digestive system problems. Diarrhoea can be either acute or chronic in nature.
Acute diarrhoea is defined as the sudden onset of three or more loose stools per day over a
period of one to two weeks. The most common causes of acute diarrhoea include viral infections,
bacterial toxins, chemical poisons, medicines, allergies, and illness.
Chronic diarrhoea or persistent diarrhea can result from gastrointestinal surgery,
carcinomas, chronic inflammatory conditions, and various absorptive defects.
Most antidiarrheal medications will only cure the symptoms of diarrhea, and in certain cases,
the cause, but not the complications. The adsorbent-protectives adsorb toxins, bacteria, and
viruses along with providing a protective coating of the intestinal mucosa. They include bismuth
salts, special clays, and activated charcoal.
3.3.1 Antimicrobials
Antimicrobials are topical medications that are used to destroy or inhibit the growth of
microorganisms, particularly pathogenic organisms, on the body’s surface. Their effect is focused
on the area where they are applied. Antimicrobial comes from the Greek words anti (against),
micro (small), and bios (life). There are several terms used in describing antimicrobial activity.
98 Text Book of Pharmaceutical Chemistry
Antiseptics
These are the chemical agent used to kills or inhibit the growth of microorganism. The
characteristics of an ideal antiseptic is to destroy bacteria, spores, fungi, viruses, or any other
infective agent without causing any harm to the tissues of the host.
Germicides
These are the agents which kill microorganism, Therefore, thay can be applied to the names
of various classes of microorganisms to provide terms for more specific agents, e.g., bactericide
(against bacteria), fungicide (against fungi), ‘viricide’ (against virus), etc.
Bacteriostatics
These are biological or chemical agents that primarily work by inhibiting the growth of
bacteria, stops bacteria from reproducing, while not necessarily killing them.
Sanitizers
Disinfectants, used to maintain general public health standards, are termed as sanitizers.
Sanitizers are mainly concerned with cleaning or washing away the organic matter (e.g., saliva).
Disinfectants
These are the chemical agents that prevent infection by the destruction of pathogenic
microorganisms. These agents are generally applied on inanimate objects (non-living) germicidal
activity, e.g., equipments, room or instruments.
The ideal disinfectant kills a wider range of microorganisms (than sanitizers), and would
rapidly destroy bacteria, fungi, viruses, and protozoan.
Astringents
An astringent is group of chemical substances that cause the contraction or shrinkage of the
body tissues and dry up secretions. Astringents are generally categorized into three groups on the
basis of their mode of action.
• Agents that decrease the blood supply by narrowing the small blood vessels, e.g., cocaine,
epinephrine, etc.
• Agents that abstract water from the tissue, e.g., glycerol and alcohol.
• Agents that coagulate the superficial tissue layers into a crust, e.g., metallic astringents,
such as calamine or alum.
3.3.2 Silver Nitrate
Molecular Formula: AgNO
3
Molecular Weight: 169.9 gm/mol
Brand Name: Grafco Silver Nitrate
Silver Nitrate contains not less than 99.5% of AgNO
3
.
Inorganic Pharmaceuticals 99
Preparation: Silver Nitrate is prepared by dissolving silver in hot and concentrated nitric
acid followed by evaporation of the solution.
Ag + 2HNO
3
→ AgNO
3
+ H
2
O + NO
2
Physical Properties: Silver nitrate appears as a colorless, odorless and white crystalline solid
becoming black on exposure to light or organic material. The melting and boiling points of silver
nitrate are 482.8 K and 713 K respectively. Its aqueous solution may decompose on exposure to
light. It dissolves readily in water. Its solubility in water corresponds to 122 g/100 ml at 0ºC and
256 g/100 ml at a temperature of 25ºC.
Uses: The uses of Silver Nitrate are listed below:
➢ It is used in many ways in organic synthesis, e.g., for deprotection and oxidations.
➢ It is used as a precursor to other silver-containing compounds.
➢ It is used in making photographic films.
➢ This compound is also known to be used for the treatment and removal of unwanted
warts in human beings.
➢ Mixtures of alkenes can be separated with the help of this compound since the silver
cation binds with alkenes in a reversible fashion.
➢ When diluted with water to a concentration of 0.5%, silver nitrate can serve as an
antiseptic in many medical set-ups.
Medicinal Uses of Silver Nitrate:
➢ Silver salts have antiseptic properties.
➢ It is used as a cauterizing (technique of burning a part of a body to remove or close off a
part of it) agent.
➢ Dilute solutions of AgNO
3
used in newborn babies’ eyes at birth to prevent contraction
of gonorrhea from the mother
➢ Dentists use silver nitrate-infused swabs to heal oral ulcers.
➢ It can be used for sterilization procedures.
Storage: It should be stored in sealed containers or packages and not exposed to light. Because of
its strong oxidizing properties, silver nitrate must be stored away from flammable materials and
ammonia, and in a cool, well ventilated area, and kept in a tightly closed container.
Pharmaceutical Formulations: It is available in the following formulations:
➢ Topical ointment (10%)
➢ Topical solution (0.5%; 10%; 25%; 50%)
➢ Topical stick (–)
1. Silver nitrate eye drop 1% w/w
➢ Silver nitrate – 1% w/w
➢ Benzalkonium chloride – 0.01%
➢ Sodium chloride – 0.01%
➢ Purified water I.P. – q.s.
100 Text Book of Pharmaceutical Chemistry
2. Silver nitrate gel 0.2% w/w
➢ Silver nitrate – 0.2% w/w
➢ Ethyl alcohol I.P. – 4% v/v
➢ Gel base – q.s.
Marketed Preparations of Silver Nitrate:
Brand Name
Dosage Form
Company
Chemsavers
Silver Nitrate, 5% Solution
Chemsavers
Silver Nitrate
Silver Nitrate Topical Solution 50%
Gordon Laboratories
Neon (Agneon)
Neon Silver Nitrate Gel, 20 g
Shree Sai Healthcare
3.3.3 Ionic Silver
Ionic Silver is the topical antimicrobial agent used in burn wound treatment. It is a solution of
silver ions and water. The solubility of silver ions is due to the missing electron. It is the outer
electrons of an atom that determine its physical properties. The solubility of ionic silver can be
determined by means that it can pass through a membrane without leaving any residue behind.
Ionic silver is different from colloidal silver because it contains silver ions as opposed to their
particles. The silver ions in ionic silver are atoms or molecules chemically dissolved in water,
whereas silver particles in the colloidal silver are suspended as colloids in a solution.
Unlike ionic silver, colloidal silver is effective when applied topically and on taken orally.
The body does not metabolize the tiny silver particles found in colloidal silver.
Pharmaceutical Formulations:
➢ Aqueous solution: 0.1%
➢ Ointment/gel: 0.2%
1. Ionic Silver Nitrate Solution 100 ml
➢ Ionic silver – 0.1%
➢ Methanol – q.s.
➢ Glycerol – q.s.
➢ Sodium chloride solution – Upto 1 ml
2. Ionic Silver Nitrate Gel 0.2% w/w 10 gm
➢ Ionic silver – 0.2%
➢ Ethyl alcohol I.P. – 4% v/v
➢ Gel base – q.s.
Inorganic Pharmaceuticals 101
Marketed Preparations of Ionic Silver:
Brand Name
Dosage Form
Company
Silverex Ionix
Silver Nitrate Gel, 10 g
Devankit Medical Agency
Sulfhex Ionic
Sulfhex Ionic Silver Nitrate Gel 0.2% w/w,
20 gm
M/s Glowide Pharmaceuticals
Pvt. Ltd.
Ionsil
Ionic Silver Nitrate Gel 0.2%
Virchow Biotech Pvt. Ltd.
Storage: Use dark glass bottles for storage. Silver is very light-sensitive. So, store it in dark
container or have access to dark glass bottles. It should be stored at room temperature (i.e.,
between 68-85 degrees).
Uses:
➢ Ionic silver water is used as a topical antimicrobial agent.
➢ It is used to heal open sores and also having drinking benefits.
➢ It has been used as antibiotic, antifungal and antiviral alternative.
➢ Silver particles block the infection by viruses.
➢ It is effective in healing wounds.
3.3.4 Chlorhexidine Gluconate
Molecular Formula: C
34
H
54
Cl
2
N
10
O
14
Molecular Weight: 897.8
Brand Name: Grafco Silver Nitrate
Chlorhexidine Gluconate is derived from chlorhexidine. It is a gluconate salt form of
chlorhexidine, a biguanide compound used as an antiseptic agent with topical antibacterial
activity.
Properties: The gluconate salt form of chlorhexidine, a biguanide compound Chlorhexidine
gluconate, is positively charged and reacts with the negatively charged microbial cell surface,
thereby destroying the integrity of the cell membrane. Subsequently, chlorhexidine gluconate
penetrates into the cell and causes leakage of intracellular components leading to cell death. Since
gram positive bacteria are more negatively charged, they are more sensitive to this agent.
Uses:
➢ Topical chlorhexidine used as disinfectant, as well as oral rinses for dental use, carries
activity against a broad range of pathogens including bacteria, yeasts, and viruses.
➢ Promotes gingival healing following periodontal surgery.
➢ Chlorhexidine Gluconate is used as a disinfectant and antiseptic that is used for skin
disinfection before surgery and to sterilize surgical instruments.
➢ It is used to disinfect the skin of the patient and the hands of the healthcare providers.
➢ It is used for cleaning wounds and preventing dental plaque.
➢ Chlorhexidine eye drops have been used as a treatment for eyes affected by
Acanthamoeba keratitis.
102 Text Book of Pharmaceutical Chemistry
Pharmaceutical Formulations: Chlorhexidine Gluconate available in the following
formulations:
➢ Oral rinse – 0.12% w/v
➢ Mouth gel – 1% w/w
➢ Aqueous solution – 4% w/v
1. Chlorhexidine Gluconate Mouth Gel: 1% w/w (15 gm)
➢ Chlorhexidine Gluconate solution I.P. – 1% w/w
➢ Gel base – q.s.
2. Chlorhexidine Gluconate and Cetrimide Antiseptic Liquid 50 ml
➢ Chlorhexidine Gluconate Solution I.P.: 15% v/v
➢ Cetrimide BP: 30% v/v
➢ Coloring agent: q.s.
Marketed Preparations of Chlorhexidine Gluconate:
Brand Name
Dosage Form
Company
Hexidine
Chlorhexidine Gluconate Solution I.P.
ICPA Health
Hexigel
Chlorhexidine Gluconate Gel 15 gm
ICPA Health
Gargilin
Chlorhexidine Gluconate Mouthwash I.P., Liquid
Trio Life Science Pvt. Ltd.
Storage: Chlorhexidine Gluconate should be stored below 25°C. It is stable under ambient
warehouse conditions to moisture and simulated sunlight.
3.3.5 Hydrogen Peroxide
Molecular Formula: H
2
O
2
Molecular Weight: 34.02
Brand Names: Eskata, Orajel Mouth Sore Rinse
Hydrogen peroxide is a non-planar molecule containing two oxygen atoms joined by a
single covalent connection known as the peroxide bond. It is a water molecule with one extra atom
of oxygen.
There are various methods for the preparation for hydrogen peroxide:
1. From Barium Peroxide
(i) When barium peroxide is acidified and the excess water is removed by the process of
evaporation under reduced pressure, we obtain hydrogen peroxide. The following
reaction will clarify this:
BaO
2
+ H
2
SO
4
(aq) → BaSO
4
+ H
2
O
2
+ H
2
O
Inorganic Pharmaceuticals 103
(ii) Reaction of ice cold paste of barium peroxide with carbon dioxide produced hydrogen
peroxide. Precipitated hydrogen peroxide then filtered off.
BaO
2
+ CO
2
+ H
2
O → BaCO
3
+ H
2
O
2
(iii) Hydrogen peroxide can also be prepared by decomposing barium peroxide with
phosphoric acid.
3BaO
2
+ 2H
3
PO
4
→ Ba
2
(PO
4
)
2
+ 3H
2
O
2
2. From Sodium Peroxide
The calculated amount of sodium peroxide is decomposed by addition of ice-cold dilute
solution of sulphuric acid. Upon reaction of these two, we get crystals of sodium sulphide and a 30%
solution of hydrogen peroxide.
Na
2
O
2
+ H
2
SO
4
→ Na
2
SO
4
+ H
2
O
2
Properties: Hydrogen Peroxide is an almost clear, colorless, pale blue liquid in its pure state with
a bitter taste and has pungent, irritating odor. It is miscible in water, i.e., it forms a homogeneous
solution when mixed with water. It has a viscosity higher than water and denser than water about
40%. Hydrogen Peroxide is a very strong oxidizing agent. It also acts as a reducing agent.
Uses:
➢ Hydrogen Peroxide is used in the laboratory for detecting the presence of chromium,
titanium, etc.
➢ It is peroxide and oxidizing agent with disinfectant, antiviral and anti-bacterial activities.
➢ It is used as a bleaching and deodorizing agent for textiles, wood pulp, hair, fur, etc. It is
a good bleaching agent for hair since its byproducts (water and oxygen) are not harmful.
➢ It is used as an antiseptic for minor cuts, bruises, laceration, etc.
➢ It is used in air pollution control where it is used to treat effluents from industrial waste.
➢ It is used to sterilize cosmetic brushes and sanitize toothbrushes.
➢ It is used as a mouthwash to clear mucus and soothe minor mouth discomfort.
➢ It is used in the production of epoxides and inorganic chemicals like sodium per borate.
Storage: Hydrogen peroxide should be stored in tightly closed container and well-ventilated
place. When containers are opened, they must be carefully resealed and kept upright to prevent
leakage. It is stored at temperature 2ºC to 8ºC. To confirm greater stability, the inside surfaces of
containers should be as free as possible from rough points since these promote decomposition.
Topical solution of hydrogen peroxide should be stored in tight, light-resistant containers at 15ºC
to 30ºC.
Pharmaceutical Formulations: Hydrogen peroxide is available in the following dosage forms
and strength:
Topical solution: 40% (w/w) hydrogen peroxide.
104 Text Book of Pharmaceutical Chemistry
1. Hydrogen peroxide USP 3% w/v solution 100 ml
➢ Hydrogen peroxide USP – 3% w/v
➢ Purified water I.P. – q.s. upto 100% v/v
2. Hydrogen peroxide 6% w/v solution 100 ml
➢ Hydrogen peroxide I.P. – 6% w/v
➢ Sodium citrate (stabilizing agents) – q.s.
➢ Purified water – q.s. upto 100% v/v
3. Hydrogen peroxide 1.5% w/v mouthwashes 200 ml
➢ Hydrogen peroxide I.P. – 1.5% w/v
➢ Glycerine I.P. – 2% v/v
➢ Sodium citrate (stabilizing agents) – q.s.
➢ Purified water – q.s. upto 100% v/v
Marketed Preparations of Hydrogen Peroxide:
Brand Name
Dosage Form
Company
Labogens
Lobogens Hydrogen Peroxide (20 Vol.)
Solution (6% w/v H
2
O
2
)
Labogens Fine Chem Industry
Peroxyl
Hydrogen Peroxide + Tigo SML + Menthol
Panax Pharm
Equate 3%
Hydrogen Peroxide Topical Solution
Vi-Jon Laboratories
3.3.6 Boric Acid
Molecular Formula: H
3
BO
3,
(or B(OH)
3
)
Molecular Weight: 61.83 g·mol
−1
Brand Names: Hylafem, Borofax
Synonyms: Ortho-Boric acid
Preparation:
1. Boric acid is prepared by reacting borax with strong acids like hydrochloric acid (HCl).
The chemical equation for this reaction can be written as:
Na
2
B
4
O
7
.10H
2
O + 2HCl → 4H
3
BO
3
+ 5 H
2
O + 2NaCl
2. It can be prepared by hydrolysis of diborane.
B
2
H
6
+ 6H
2
O → 2 B(OH)
3
+ 6H
2
3. Boric acid can also be prepared by the hydrolysis of boron trihalides (such as BBr
3
).
BBr
3
+ 3H
2
O → B(OH)
3
+ 3HBr
Inorganic Pharmaceuticals 105
Properties: Boric acid occurs as a white crystalline, odorless solid with a density of 1.435 g/ml,
melting point of 170.9°C and boiling point of 300°C. It is soluble in water and does not have any
characteristic odor. The structure of boric acid consists of planar sheets of planar trigonal B(OH)
3
molecules linked by hydrogen bonds.
Uses: The following are some of the applications for boric acid.
➢ Boric acid used as an antiseptic, insecticide, antibacterial and for acne treatment.
➢ Boric acid used as a source of B
2
O
3
in glasses and other vitreous products like fiberglass,
heat-resistant borosilicate glasses, ceramic glazes, porcelain, ceramics, crockery,
enamels, artificial gemstones, and sealing optical glasses.
➢ It is used in preservative, pH buffer, swimming pool chemicals, flame retardant, and a
precursor to many useful chemicals.
➢ It is used industrially for the manufacture of fiberglass, household glass products and the
glass used in LCD displays.
➢ It is a weekly acidic hydrate of boric oxide with mild antifungal and antiviral properties.
➢ It is used in carom boards as a dry lubricant.
➢ It is also used in the jewellery industry.
➢ It is used to preserve grains like wheat and rice.
Storage: Boric acid should be stored in well closed container under cold to warm conditions
between 2 to 40°C (36 to 104°F). Store in carbon steel or aluminum containers; stainless steel is
needed for moist conditions. Protect the container against physical damage. It is stable under
ordinary conditions of use and storage. If moisture is present, boric acid can be corrosive to iron.
Dosage Forms:
Vaginal Suppository:
➢ Eye ear drop – 0.3% w/v
➢ Eye drop – 0.3 g/15 ml
➢ Dusting powder – 400 gm
➢ Ointment – 4.5% w/w
Boric Acid:
➢ Eye drop – 15 ml
➢ Boric acid I.P. – 0.3 gm
➢ Alcohol – 3 ml
➢ Purified deionized water – 15 ml
Boric Acid Gentamycin Eye/Ear Drop (30 × 10 ml)
➢ Boric acid I.P. – 1.5% w/v
➢ Gentamycin – 0.3% w/v
➢ Benzalkonium chloride – 0.02% w/v
➢ Sterile aqueous vehicle – q.s.
106 Text Book of Pharmaceutical Chemistry
Marketed Preparations of Boric Acid:
Brand Name
Dosage Form
Company
Borexa
Boric acid Eye/Ear Drops 2%
Schwitz Biotech
Mylan
Borax /Boric Acid 10 Single-dose Ophthalmic
12 mg/18/mg/mL
Mon Pharmacien Conseil
Gentavol
Gentamicin and Boric Acid Eye/Ear Drops
(30 × 10 ml)
Srinivasa Associates
3.3.7 Bleaching Powder
Molecular Formula: Ca(OCl)
2
Molecular Weight: 142.98 g/mol
Synonyms: Chlorinated lime, Calcium hypochlorite
Bleaching powder is a solid combination of chlorine and slaked lime. It is often referred to as
a chloride of lime. It is the by-product to the reaction of calcium hydroxide and chlorine gas. It is
generally made of slaked lime that has moisture in it.
Preparation of Bleaching Powder: Bleaching powder is prepared by the action of chlorine gas
(produced from the chlor-alkali process) on dry slaked lime (Ca(OH)
2
).
Ca(OH)
2
+ Cl
2
→ Ca(OCl)
2
+ CaCl
2
+ 2H
2
O
Properties: Bleaching powder occurs as a pale yellow powder having a strong smell of chlorine.
It is soluble in water but does not form a clear solution as impurities are present in it; the small
insoluble portion left behind on dilution is the lime present in it. It slowly decomposes on its own
and forms calcium chloride and calcium chlorate. When bleaching powder is treated with an
excess of dilute sulphuric acid, all the chlorine present in it is liberated.
Uses:
➢ It is used for bleaching of various cotton and linen in textile industry and for bleaching
wood pulp in paper industry.
➢ It is used for disinfecting drinking water supply to make it potable, i.e., for making
drinking water free from germs.
➢ It is used as a bactericide and in the preparation of some compounds.
➢ It is mixed in water and can be used to clean and sanitize the doors, windows and floors
in households, offices, hospitals, malls and other places.
➢ It is used to prepare for the manufacture of chloroform (CHCl
3
) in laboratories.
➢ It is used for making wool unshrinkable.
➢ It is used in the bleaching of various materials (clothing, furniture, paper, etc.). That is
why it is called bleaching powder.
Storage: Bleaching powder should store in a tightly closed container in a cool, dry and well-
ventilated place. Keep it away from combustible material and sunlight.