PHARMACEUTICAL INORGANIC CHEMISTRY OF MEDICINALS

Dr. Althea Rodriguez Arenajo

Oxygen,Ozone,Hydrogen,WaterHydrogen Peroxide

OXYGEN

A particular gas present in the atmosphere was consumed during oxidation and respiration (Mayow)

The Chinese named the gas yne Steven Hales was able to obtained the

gas by heating minium (lead tetroxide) Joseph Priestley obtained the gas by

heating mercuric oxide and named it dephlogisticated air

In 1774, Priesley published the properties of

the gas he discovered Karl Wilhelm Scheele, a Sweedish

apothecary, discovered oxygen using nitrates in 1773 and named it empyreal air

Antoinne Laurant Lavoisier, a French chemist, made correct interpretations of Priestley’s

work and the role played by oxygen in combustion and respiration

OXYGEN

OXYGEN Lavoisier named the gas oxygen , from the

Greek word meaning “sour” and “I produce”

• Oxygen then is an “acid former” Official test

A glowing splinter will burst into flame when placed near a container with the gas Pharmacologic action 1.Oxygenation of the blood 1.0 minute- normal oxygenation of the blood 10-15 seconds – when the body is exerted

The processes by which oxygen reaches the tissues

1.Diffusion from alveolar air to blood plasma

2. Surrender from blood plasma to red blood corpuscles to form oxyhemoglobin

3. Abstraction of oxygen from oxyhemoglobin by the tissues via complex physiochemical processes and by diffusion

15gm/ml - hemoglobin in the blood 1 gm of hemoglobin canhold 1.34 mL

of oxygen 100mL of blood can hold 20 mL of

oxygen

OXYGEN

Calassification of oxygen once in the by

1. Anorexic – supply of O2 to the tissue is inadequate, blood arrives at a lower tension

2. Anemic – O2 tension is normal, amount of hemoglobin is inadequate

3. Stagnant – general circulation is inadeqaute or when circulation is locally retarded

4. Histotoxic – the tissue cell oxidation may be interferred within several ways:

a. Dehydration b. Cyanide poisoning

OXYGEN

2. Neutralization of toxic materials 2.5 atm – counters the lethal dose of

cyanide It is a routine procedure, together

with sodium nitrite and sodium thiosulfate, in the antidotal treatment of cyanide posoning

The efficient utilization of oxygen by the body in its normal process demands a smooth functioning of oxygen transport from inspired air to utilization in the tissue

OXYGEN

Important preparations1. Oxygen USP – has not less than 99% of

Oxygenuses:

a. in medical practice and surgery.b. in all pathological conditions, e.g.

pneumonia, angina, bronchitis etc., that are accompanied by cyanosis and dyspnea

c. in chloroform poisoning and in threatened death from inhalation of coal gas or nitrous oxide

OXYGEN

OXYGENd. in the resuscitation drowned individuals

e. in conditions where there is scarcity of

oxygen like: airplanes in high altitudes,

diving bells and submarines 20% Oxygen with Helium for

therapeutic purposes is stored in brown-green colored cylinders

Oxygen and Carbon dioxide mixture is stored in gray-green cylinders

2. Liquid Oxygenuses:a. in treating growths such as wartsb. in industry such as: steel industry, steel

fabrication and industrial maintenance

c. as ingredient in the fuel of rockets

OXYGEN

OZONE Van Marum, a Dutch chemist, has observed the peculiar irritating odor when electric

spark is passed over oxygen or air Schonbein named the gas ozone from the

Greek word which means “to smell” It is an allotrope of oxygen O3 is stable at very low tempt , at ordinary

tempt it slowly decompose to oxygen More O3 is formed, higher O2 is heated

OZONE

The transformation of O2 into O3 involves

the changing of electrical energy into

chemical energy It needs 68,820 cal to change O2

into O3 Ozone is a more active chemical

agent than is oxygen, therefore, O3 is an

ideal and a powerful oxidizing agent Ozone has a bluish tinge and an

irritating garli-like odor

Uses of Ozone:1. Oxygen or air containing ozone is used as bleaching agent for oils, waxes, delicate silk or wool fabrics, flour, starch, ivory etc.2. As disinfectant for drinking water 3. As deodorant of foul animal matter esp in

large public halls and food warehouses4. Inhibitor of molds and bacteria on meats

and fruits in cold storage

OZONE

OZONE

5. Manufacture of synthetic camphor, and many other organic

compounds Ozone is a highly lethal and toxic

substance in acute exposure Individuals in continued exposure to

about 0.1 ppm, experienced headache

and throat dryness Studies show that less than 5.0 ppm

is fatal to 50% of exposed rats

OZONE

Ozonides are subs of ozone dissolved in turpentine, cinnamon and olive

oils some of which are antisepticsOzonide preparations with olive oil :1. Oilzo – liquid2. Ozettes –vaginalppository Ozonide air is the one containing 1-

2% ozone

HYDROGEN

Paracelsus was the first to recognized hydrogen in the 16th century

Turquet de Mayenne payed attention to its combustible nature Cavendish was the first to experiment on H2 by the action of dil HCl upon metals He named the gas “inflammable air” Lavoisier named the gas “hydrogen”

from the Greek word which means “water” and “to produce”

HYDROGEN H2 occurs in volcanic gases in the free state In combined form it is in the air, meteorites, stars and nebulae and also occurs in the sun H2 is found in acids and in anaerobic

fermentation A colorless, tasteless, and odorless gas, soluble

in water & occluded by many metals H2 is a powerful reducing agent, burns with a

pale blue, non-luminous flame

HYDROGEN

Uses:1. Nitrogen fixation and inflating

balloons2. Production of high temperatures

when burned in oxygen3. Hydrogenation of oils used for

edible such as oleomargarine and hydrogenated

fats4. As a laboratory agent in the

preparation of many chemical compounds

H2 is never used in pharmacy or medicine

WATER

Lavoisier decomposed water, he proved that it is composed of 1 part by weight of hydrogen and 8 parts by weight of oxygen

The ocean is the most abundant of all

natural sources of water Mineral waters are natural spring or

well waters containing minerals or

gaseous matter to render it unfit for domesic use

WATER

Waters with medicinal constituents:1. Alkaline waters – contains Na & Mg

sulfates with calcium carbonate2. Carbonated waters – while in the

earth, they are charged with CO2, effervesce on

coming to the surface3. Chalybeate water – containing iron

in soulution or suspension and are characterized by a ferruginous taste

WATER

4. Lithia waters – no appreciable amount of lithium, Li occurs in carbonates or chlorides

5. Saline waters – also known as “purgative waters”, contain large amount of Na & Mg

sulfates with NaCl6. Sulfur waters – contain H2S, deposit sulfur upon exposure to the atmosphere7. Siliceous waters – contain very small

quantities of soluble alkali silicates

WATERS

Green plants contain 75-80% water Fresh fruits contain 80-98% water The animal body contains 70% water Water is a tasteless, odorless and

limpid Colorless in small quantities but

greenish-blue in deep layers Only slightly compressible and a

poor conductor of heat and electricity

WATER

H2O exists as liquid between zero and

100 degrees at 760 atm Its greatest density is at 4 degrees

celcius It is solid below zero degrees and

vapor above 100 Viscosity decreases rapidly with rise

of temperature (8X greater at zero degrees

as at 100 degrees)

WATER This is an important property of filtering and washing precipitates As water passes from one state to another,

heat (energy) is consumed or liberated 79.71 cal of heat are needed to effect the

change of 1 gm of ice to 1 gm of water at zero degrees

539.55 cal are consumed to change 1 gm of water to 1 gm of steam at 100 degrees

WATER

Melting-or freezing points – the temp at

which solids to liquids or vice versa occurs

Boiling points – the temp at which liquid are transformed to vapor

Specific heat – quantity of heat, in calories required to raise 1 gm, 1 degree celcius

The specific heat of water at 14.5 degrees is 1

Calorie (cal) – the unit quantity of heat

Kilocalorie – is a large calorie, 1000X larger

WATER

Methods of removing particles in water:

1. Chlorination-

2. Coagulation-

3. Filtration-

4. Sidementation

WATER

A pharmacuetical can be altered in clarity,

color, taste, and in therapeutic effect by

the water used Hardness is a property of water that

determines its value for domestic and commercial purposes

Hard water is water containing varying amounts of calcium, iron and magnesium

salts

WATER

Kinds of hardness in water:I. Temporary – is caused by the

presence of ion soluble calcium or magnesium

carbonates Methods to soften temporary

hardness: a. Boiling b. Clark’s lime process – addition of

slaked lime (calcium hydroxide) c. Addition of Soluble Alkali

Carbonates or hydroxides

WATER

d. Addition of ammoniae. Zeolite process – softens both temporary

and hard water. This makes use of sodium aluminum silicate by ion exchange

f. De-ionized or Demineralized Water- the latest method for softening both types of water. This makes use of resinous ion-exchange (Hresin-for cation; amine formaldehyde resin-for anion)

WATER

II. Permanent - caused by the presence in solution of the sulfates chlorides or hydroxides of calcium or magnesium

Ways to soften permanently hard water

1. Addition of soluble carbonates- precipitation of calcium and magnesium occurs

2. Zeolite process3. De-ionized or Demineralized Water

WATER

4. Sequestration and chelationsequestration- the act of removing or withdrawing or to take possession of byconfiscating or appropriating

Sequestering agent decreases the concen-

tration of a multivalent positve ion (Cu,Ca, Fe 2+,3+ ) in solution, by combining wit it to form a complex negative ion

WATER Graham salt or Sodium metaphosphate, the most widely used sequestering agent is coverted to a polymer known as Calgon Calgon is a very effective water- softener by acting to remove the calcium ions as a

very slightly ionized complex Trilon B (Versene) is the sodium salt of

ethylene diamine tetraacetic acid (EDTA), this is more described as chelating agent

WATER

Recognized water by USP1 . Water USP- is Water USP; Purified

water; Water for Injection; Sterile Water

for Injection Requirements: a. Clear, colorless, odorless liquid b. pH range of not less than 6.3 and

not more than 8.3 c. Freedom from bacteriological

impurities

WATER

2. Purified Water USP/Distilled Water USP-

water obtained by distillation or by ion-exchange treatment

requirements: a. Clear, colorless, odorless liquid b. pH approaches neutrality Not to be used for parenterals but

as solvent Carbon dioxide –free water is

Purified water

WATER

that has been boiled for 5 minutes or more and protected from reabsorption of CO2

3. Water for Injection USP- is purified by distillation and contains no added subs

Water for injection is intended for use as a

solvent for parenteral solutions For parenteral solutions prepared

under aseptic conditions and not sterilized by appropriate filtration or not in the final

WATER

container, first render the water for injection and therafter protect it from

contamination Water for Injection should be free of

pyrogens (bacterial decomposition products causing fever) It is to be preserved in tight containers,

stored at a temperature below/above the range when microbes grow/occurs

WATER

4. Sterile Water for Injection/Water for Parenterals- is water for injection sterilized

and packaged for pharmaceutical use

Requirements:a. clear, colorless and odorless liquidb. contains no bacteriostatic agentc. absent of pyrogens d. chlorine content does not exceed

0.5ppme. stored insingle dose containers

HYDROGEN PEROXIDE

Thenard discovered hydrogen peroxide and and called it”oxygenated acid”

Later it was called “oxygenated water” – as we now know as hydrogen peroxide

Its use in medicine as well as hair bleach began in 1873 in Berlin

It occurs naturally in small quantities in air,

dew, rain and snow It is an unstable colorless,

astringent and

HYDROGEN PEROXIDE

syrupy liquid at room temperature Pure hydrogen peroxide will decompose very slowly with explosive violence to form water and hydrogen peroxide It is miscible in all proportions with water but is more soluble in ether Aluminum tanks are good storage containers because it does not catalyze decomposition of H2O2

HYDROGEN PEROXIDE

H2O2 is stable in solutions of high purity, contaminants will decompose it unless

a stabilizer is present For pharmaceuticals of hydrogen peroxide,

an excellent stabilizer is 0.02 % quinine Acetanilid 0.03% is present in H2O2,protects

the peroxide from the effects of sunlight Alkalis increase the decomposition of

peroxide

HYDROGEN PEROXIDE

An evalescent blue color will appear on the equeous layer of H2O2 with dil sulfuric acid,

ether and pot dichromate test solution

A blue color is produced when a solution of

H2O2 is added to a mixture of tincture of guiac and malt infusion

A better test to identify H2O2in the blood is benzidine (p,p’ - diaminodiphenyl)

HYDROGEN PEROXIDE

Physiological properties:a. H2O2 solutions and vapors are

nontoxicb.The 30% sol’n is causticc. Ingestion and injection into body

cavities is dangerous, evolution of too much

O2 that may cause irritation and

bleeding d. Vapor is irritating to the nose and

eyes e. It gives an stinging sensation with

the skin and cause to whiten

HYDROGEN PEROXIDE

Important Compounds:1. Hydrogen Peroxide USP a clear, colorless , having the odor of ozone stored in tight, light resistant containers

below 350 C contains preservative(acetanilid) that not to exceed 50mg/100mL sol’n as antiseptic, it liberates O2 when comes

with tissues and referred as” auto-oxidation”

HYDROGEN PEROXIDE

its mechanical cleansing action is impt

in removing surgical dressings and earwax

used in treating Vincent’s stomatitis and as

mouth wash several times daily may cause “hairy

tongue”(hypertrophied filiform papillae), disappears if discontinue

use as hair (6%) and fabric bleaches 0.1% retards bacterial flora in milk

thus, souring is extended

HYDROGEN PEROXIDE

Volume strenghts of H2O23% = 10 volumes 9% = 30

volumes6% = 20 volumes 12% = 40

volumes9% = 30 volumes 15% = 50

volumes 30% ( 100 volumes) – a common

commercial strenght (Superoxol and Perhydrol) 2. Urea Peroxide (Perhydrit or

carbamide peroxide) showed greater

bacteriostatic action against Cl. welchii and Cl.tetani