Biological and Pharmaceutical Significance

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Classifications Examples/Preparations

Acids Strong acids Weak acid


Hydrochloric acid HCl Citric acid C6H7O8
Hydrobromic acid HBr Tartaric acid C4H6O6
Hydroiodic acid HI Acetic acid CH3OOH
Nitric acid HNO3 Hydrocyanic acid HCN
Sulfuric acid H2SO4 Ammonium ion NH4
Phosphoric acid H3PO4 Boric acid H3BO3
Bases Strong bases Weak bases
Sodium hydroxide NaOH Ammonium hydroxide NH4OH
Potassium hydroxide KOH Ammonia NH3
Rubidium hydroxide RbOH Water H2O
Magnesium hydroxide Mg(OH)2
Calcium hydroxide Ca(OH)2
Strontium hydroxide Sr(OH)2
Barium hydroxide Ba(OH)2
Buffer Sorensen phosphate buffer – pH range of 5.8 to 8. Has greatest buffer capacity at pH6.7.
Composted of Sodium acid phosphate and disodium phosphate in purified water with addition of
sodium chloride to render the solution isotonic. Has Valuable buffer system for ophthalmic drugs,
as the ions present are normally found in the eye and the pH range includes the isohydric point of
tears.
Gifford’s buffer – composed of boric acid and sodium carbonate with potassium chloride in
purified water.
Atkin’s and Pantin buffer – composed of boric acid and sodium carbonate with sodium chloride in
purified water.
Feldman’s buffer – composed of boric acid and sodium borate with sodium chloride in purified
water.
Antioxidants Prevents oxidative decomposition of pharmaceutically active components.
Naturally Mineral water – contains minerals; from natural sources.
occurring water Alkaline water - contains alkalines such as sodium bicarbonate.
Carbonated water – contains carbonates.
Chalybeate water – contains iron; tastes like rust or has a ferruginous taste.
Lithia water – contains lithium.
Saline water – contains salts like NaCl.
Sulfur water – contains sulfur; used as therapy for hypertension or rheumatoid arthritis (not
clinically proven).
Siliceous water – contains silicas.
Potable water – “fit to drink”
Official water Water USP – used as solvent; used to make several official solution, tinctures, and extracts.
Purified water USP – obtained by distillation or by ion exchange treatment.
Method of preparation must be indicated on the label of the container.
Not intended for parenteral administration. Used in preparation of most USP test reagents. Water
of choice for extemporaneous compounding (lotions, creams or any other preparations).
Water for injection USP – purified by distillation. Must pass PYROGEN TEST (determines if a
solution may cause fever). Intended for use as solvent for the preparation of parenteral solutions.
Mut be stored below 4oC or above 37oC. Requires sterilization before administration.
Bacteriostatic Water for injections USP – sterile water for injection containing one or more
suitable antimicrobial agents (benzyl alcohol). Inhibits growth of bacteria.
Used for compounding small volumes of parenterals for IM injections.
Sterile water for injection USP – water for injection sterilized and suitably packaged which
contains no antimicrobial agents. Used for extemporaneous compounding of parenterals for either
intravenous or intramuscular injections. No further sterilization required.
Glass – for storage Glass type Composition Use
and as dispensing Type 1 Borosilicate Glass It is ideal for containing all injectable preparations with acid,
container for most
drug products.
neutral and alkaline pH. It has good resistance to thermal
Boron: decreases shocks and can be sterilized before or after filling.
coefficient of Type 2 Soda-lime Silica This type of glass is a soda-lime glass which, by means of a
expansion in Pyrex Glass with special treatment, reaches the hydrolytic stability of type I
glass.
Potassium gives
treatment on the glass on its surface layer of 0.1-0.2 um. It is suitable for acidic
brown light resistant inner surface to and neutral parenteral preparations. Type II glass container
glass. increase hydrolytic can be sterilized before or after filling.
Lead is added to resistance
increase refractive
index Type 3 Soda-lime Silica This type of glass has average hydrolytic resistance. It is
Glass suitable for containing non-aqueous injectable preparations
Glass contains and those in powder form. It can also be used for non-
sodium silicate. parenteral preparations. Type III glass container should be
sterilized by dry heat before filling.
In water produces
NaOH that increases
alkalinity in drugs.

Vitreous material= a
material that softens
gradually over a
temperature rather
than melting sharply.

Type II glass makes


use of water attack
test.
Physiological Chloride – major extracellular anion.
ions Phosphate – principal anion of the intracellular fluid component.
Bicarbonate – 2nd most prevalent anion in the extracellular fluid.
Sulfate - second most abundant intracellular anion.
Sodium – principal cation in the extracellular fluid.
Potassium - major intracellular cation.
Calcium – 1% is found in intracellular fluid especially for blood clotting.
Magnesium – 2nd most plentiful cation in the intracellular fluid.
Essential ions – Iron – constituent of hemoglobin.
not produced by Iodine – constituent of thyroxin & triiodothyronine.
our own bodies, Zinc – constituent of insulin, carbonic anhydrase & lactic dehydrogenase.
from food. Copper – for the formation of hemoglobin & constituent of oxides enzymes (tyrosinase).
Cobalt – constituent of vitamin B12
Manganese – cofactor for a number of enzymes like arginase, carboxylase & kinases
Sulfur – constituent of proteins, mucopolysaccharides, heparin, biotin, thiamine & lipoic acid.
Chromium – involved in carbohydrate utilization
Molybdenum – constituent of xanthine oxidase & aldehyde oxidase.
Selenium – constituent of factor 3 acts with Vitamin E to prevent liver necrosis.
Non-essential Fluoride – anticariogenic agent
ions Mercury – cathartic, diuretic, antiseptic, disinfectant
Bromide – sedative (0.2 – 2g) & CNS depressant, Hypnotic (4 - 8g)
Arsenic – depressant for epilepsy
Lithium – treatment of hypomanic and manic states
Gold – treatment of lupus erythematosus or rheumatoid arthritis
Aluminum – astringent, antiseptic and deodorant
Silver – antiseptic, astringent, protein precipitant
Strontium – as bromide- sedative; as chloride – desensitizing agent
Gastrointestinal agents
Antacids – weak Local antacids – effect occurs only in the stomach
BASES that Aluminum Hydroxide Al(OH)3
neutralizes Systemic antacids – antacids that can be absorbed into the systemic circulation.
stomach acid. Sodium Bicarbonate NaHCO3 – systemic alkalinizer; causes flatulence or bloating.
Calcium carbonate CaCO3 – may cause flatulence or bloating; may also cause constipation. Source
of calcium.
Sodium Bicarbonate – highly water soluble; rapid onset, short duration; sharp increase of gastric
pH; evolution of CO2; Found in many effervescent antacid preparations; sparkling flavor.
Examples of Aluminum Hydroxide USP 31 – ideal buffers in the pH 3-5 region but can cause constipation,
Antacids nausea/vomiting. Loss of antacid properties on aging.
Uses: Gastric antacid, treatment of hypochlorhydria and peptic ulcer, and indicated for intestinal
toxemia.
MOA:
Capable of adsorbing HCl, toxins and bacteria
Can adsorb pepsin
Can interfere with the absorption of other drugs
2 Physical forms (USP 26)
Aluminum Hydroxide Gel – white viscous suspension
Dried Aluminum Hydroxide Gel – white amorphous powder; very fine colloidal particles, large SA,
great adsorptive powers.
Calcium Carbonate USP 31 – “Precipitated Chalk”; One of the most popular antacids
Action is limited by the amount of salt that will go in solution; has constipative effect
needed to be mixed with Mg.
USP 26 – CaCO3 Lozenges and Oral Suspension
Tribasic Calcium Phosphate NF 26 – Variable mixture of Calcium Phosphates
Found abundantly in nature (Phosphorite or Phosphate Rock and Apatite)
Uses:
Antacid – treatment of hyperacidity
Diminishes the H+ concentration of gastric HCl
No gas produced – no flatulence
Does not alkalinize the system
Magnesium- Magnesium Carbonate USP 31 – Carbonate of Magnesia, Heavy Magnesium Carbonate
Containing Properties: White, bulky, odorless powder that has a slightly earthy taste.
Antacids – Uses:
Poorly soluble Antacid properties due to hydroxides and carbonates
salts Dissolves only as carbonate and hydroxide is being consumed
As the pH of the Magnesium Hydroxide USP 31 – Efficient antacid and laxative in high doses – formation of MgCl2
stomach or “salt action”.
approaches into Milk of Magnesia – Suspension of Mg(OH)2; NLT 7% and NMT 8.5%; Very popular antacid and
neutrality, laxative that has suitable flavoring agents.
rate of Contains Citric Acid – minimizes interaction with glass containers.
dissolution of Magnesium Oxide USP 31 – “MgO Magnesia”; Absorb CO2 and moisture upon exposure to air;
Mg salt slows Administered in about 29x its weight of water; addition order: Magnesia to water
down and stop Uses: Laxative, Diuretic, Antacid, Arsenic Antidote
at neutrality 2 varieties:
Light Magnesium Oxide – 5 g occupies 40-50 mL; hydrolyzes more easily
Anion – confers Heavy Magnesium Oxide – 5 g occupies 10-20 mL;
the antacid Magnesium Trisilicate USP 31 – 2MgO∙3SiO2∙xH2O
Contains NLT 20% of MgO and NMT 45% of SiO2
properties. Has definite ratio; Amount of SiO2 ↑ - ↓ antacid capability
Mg Cation – Properties: Fine, white, odorless, tasteless powder, free from grittiness
Laxatives. Uses:
Gastric antacid – peptic ulcer
Combination Colloidal Silicic Acid or Hydrous Silica
with Ca and Al protective/adsorptive
Magnesium Phosphate USP 31 – Mg3(PO4)2∙5H2O
Tertiary Magnesium Phosphate; Used as an antacid
Combination Al(OH)3 Gel – Mg(OH)2
Antacid Aludrox®, WinGel®, Maalox®, Cremalin®
Preparations – Al(OH)3 Gel – Mg Trisilicate
No single antacid Gelusil®, Tricreamalate®, Triosgel®
meets all the Magaldrate – Al(OH)3 and Mg(OH)2
criteria of an Riopan®
ideal antacid. Simethicone Containing Antacids
Rapid onset of Simethicone – defoaming agent; removes complaints of being “gassy”.
action and Di-Gel®, Mylanta®
longer duration Alginic Acid- NaHCO3 – Symptomatic relief of reflux esophagitis.
of action Gaviscon®, Foamtab®
Protective and Bismuth-Containing Products
adsorbents Water insoluble – small amounts go into solution
*Diarrhea – Soluble Bi+3 – mild astringent and antiseptic
Symptom and Causes black stool – formation of Bi2S3
not a disease;
impairs digestion 1. Bismuth Subnitrate USP 31 – Basic Bismuth Nitrate, White Bismuth
and/or Incompatible with Tragacanth; Will precipitate as hard mass; Fixed with addition of Na
absorption. Biphosphate or Trisodium Phosphate
Can lead to Uses: Effective non-irritant intestinal antiseptic, lessens gastric secretion and reduce acidity,
dehydration. Treatment for gastric ulcers and inflammations, Common remedy for diarrhea

Acute-Bacterial 2. Bismuth Subcarbonate USP 31 – Basic Bismuth Carbonate


toxins, chemical Uses:
poisons, drugs, Protective and antacid effect in inflammations of the stomach and bowels
allergy, and Large doses (60g) – rendering the alimentary canal opaque to x-ray
disease. Astringent and adsorbent
Chronic – GI Treatment of diarrhea and dysentery
surgery,
carcinomas, 3. Milk of Bismuth USP 31 – Bismuth Magma, Bismuth Cream
chronic Bismuth hydroxide and Bismuth carbonate in suspension in water
inflammatory Uses: Astringent, Antacid
conditions, Kaolin USP 31 – Native hydrated aluminum silicate
various Freed from gritty particles by elutriation; Contains 20.9% of Al
adsorptive Formed by weathering of Feldspar (KAlSi3O8); Earthly and clay-like taste; assumes a darker color
defects. and develops a marked clay-like color
Ideal Uses:
antidiarrheal Usually found together with pectin (vegetable carbohydrate) – Kaopectate, Kao-Con
act directly on Protective and adsorbent in diarrheal disorders
the smooth Interfere materially with the intestinal absorption of Lincomycin
muscle of the Activated Charcoal USP 31 – Adsorbent in the treatment of diarrhea and antidote in certain types
gut – spasm like of poisoning.
effect.
Saline cathartics Monobasic Sodium Phosphate USP 31 – NaH2PO4∙H2O; Sodium Dihydrogen Phosphate, Sodium
– increase Acid Phosphate, Primary Sodium Phosphate, Sodium Biphosphate
osmotic load; Uses:
body relieves Official category – Urinary acidifier
hypertonicity by Cathartic
secreting Render the urine acidic in case of cystitis with hexamethylenetetramine (Methenamine)
additional fluids. Dibasic Sodium Phosphate USP 31 – Na2HPO4∙7H2O; Disodium Hydrogen Phosphate, Secondary
Sodium Phosphate
Poorly absorbed Solutions are alkaline to litmus and phenolphthalein
anions that are Uses:
used as saline Saline cathartic – poor intestinal permeability
cathartics Caution:
biphosphate, Should never be confused with the commercial tribasic sodium phosphate – very alkaline and
phosphate, caustic
sulfate and Potassium Sodium Tartrate USP 31 – KNaC4H4O6.4H2O; Rochelle’s or Seignette Salt
tartrate. Uses:
Cathartic
Water soluble Mild laxative to Hydragogue – depending on the dose
and taken with Ingredient of Seidlitz Powder
large amounts of Effervescent preparation and Palatable product
water. Component of Fehling’s Solution (Alkaline Cupric Tartrate)
Chelate Complexation
Magnesium Sulfate USP 31 – MgSO4∙7H2O; Epsom Salt, Bitter Salt
Preparation:
Magnesite (MgCO3)
Kierserite (MgSO4∙H2O)
Dolomite (MgCO3∙CaCO3)
Uses: Active cathartic – with little pain or nausea, produce watery stools
Chief objection: Disagreeable bitter taste
Parenteral: As anticonvulsant
Saturated solution – used locally for anesthetic effect
Magnesium Citrate USP 31 – Citrate of Magnesia, Purgative Lemonade
Preparation:
Reacting MgCO3 with Citric Acid
Added with flavoring agents
NaHCO3 or KHCO3 is added to react with remaining Citric Acid
Product: Palatable, carbonated, lemon flavored solution
Sterilized or pasteurized.
Topical agents
Protectives applied to the skin to protect certain areas from irritation, usually of mechanical origin.
Talc and Zinc
Antimicrobials – Mechanism of Antimicrobials
agents that Oxidation Halogenation Protein precipitant
inhibit the Oxidizing Agents Hypochlorous Acid Silver Nitrate
growth or kill Hydrogen Peroxide Toughened Silver Nitrate
microorganisms. Zinc Acetate
Sodium Hypochlorite
Iodine as Zinc Sulfate
Zinc Undecylenate
Boric acid
Sodium Borate
Antimony Potassium Tartrate USP
Antimony Sodium Tartrate USP
Astringents are protein precipitants which results to contraction of tissues and later on wrinkling.
Examples are styptics, antiperspirants, and deodorants.

Dental Agents
Anticaries used for the prevention of caries (tooth decay) caused by the action of acids on the tooth
Agents enamel.
Dentifrices These are powders or pastes used for cleaning and polishing the teeth.
Pumice
MISCELLANEOUS PHARMACEUTICAL AGENTS
Inhalants Gases which can pass into the nasal passage where they can exert their effect.
O2, CO2, N2O, artificial air 80% He, and 20% O2
Respiratory Carbon dioxide – used as a respiratory stimulant, usually containing 5 to 7% oxygen
Stimulants – Ammonium Carbonate NF – at room temperature it decomposes to ammonia and carbon dioxide,
used to revive an two respiratory stimulants.
unconscious Aromatic Ammonia Spirit USP – prepared from ammonium carbonate, strong ammonia solution,
person which various aromatic oils, alcohol and water (light- resistant containers must be used).
cause reflex
action of the
patient taking a
sudden deep
breath (Aromatic
Spirit of
Ammonia)
Expectorant are used orally to stimulate the flow of respiratory tract secretions.
Emetics are used to induce vomiting in low doses.
Antidotes – are Physiological – NaNO2 convert hemoglobin into methemoglobin.
agents that Chemical - Na2S2O3 react with CN to produce their cyanate.
counteract a Mechanical – activated charcoal (MgSO4 & CuSO4 – inactivation)
poison.
Carbon Dioxide Particles formed must be:
Absorbers – must be large enough to allow free passage of air, but small enough to give a large surface area for
Used as general absorption must be hard to prevent dust formation with handling.
anesthesia, a
patient A colored indicator is included in the preparation to indicate when the carbon dioxide capacity is
rebreathes air, depleted. Soda Lime NF and Barium hydroxide Lime USP
dangerous levels
of carbon
dioxide build up.
Enemas PEG 3350 and Electrolytes for Oral Solution USP (polyethyleneglycol 3350, NaHCO3,NaCl, Na2SO4
and KCl) – is a dry mixture that is to be dissolved at the time of use and then consumed within a
prescribed time; accomplish oral colonic lavage in preparation for a barium enema or a colonospic
examination.
Sulfur - it is thought to be reduced to hydrogen sulfide by reducing agents present in the intestinal
fluid.
Sodium Phosphates Enema USP – is a mixture of dibasic and monobasic sodium phosphates or
dibasic sodium phosphate and phosphoric acid in water to give a pH of 5 to 5.8.
Irrigating A sterile solution that, after the chemical reactions between citric acid and the other two
Solutions – compounds are completed and the resulting solution is sterilized: suitable for use as a urinary
bladder irrigant.
Its acidic pH is conductive to dissolving any bladder calculi in patients such as those using
indwelling catheter.
Examples:
Citric acid irrigation
Magnesium oxide irrigation USP
Sodium Carbonate Irrigation USP

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