PHARMA AIDS Flashcards
1
Q
Agents that are important in the:
-preparation
-preservation, &
-storage of pharmaceutical products
-are not API
-have little to NO pharmacological activity
A
pharmaceutical aids and necessities
2
Q
adsorb fluids and moisture and keep pharmaceutical products dry
A
Adsorbents
3
Q
inert substances and vehicles used in pharmaceutical to dilute and decrease the concentration of the API or increase the bulk of formulation
A
Diluents
4
Q
are substances added for overcoming agglomeration of the dispersed particles and for increasing the viscosity of the medium so that particle settle down very slowly
A
Suspending Agents
5
Q
substances used in the clarification process
A
Filter Aids
6
Q
compound that are used to prevent chemical and physical degradation of liquid or semi-solid preparations against antimicrobial contamination
A
Preservatives
7
Q
frequently employed in the conversion of drugs to chemical forms
A
Acids & Bases
8
Q
maintain the pH of various formulations within prescribed limits
A
Buffers
9
Q
prevent oxidative decomposition of pharmaceutically active components
A
Antioxidants
10
Q
primary solvent or liquid phase in most liquid pharmaceutical preparations
A
Water
11
Q
used for storage and as dispensing container for most drug products
A
Glass
12
Q
Acid forms what in water?
A
H+
13
Q
Base forms what in water?
A
-OH
14
Q
can donate 2 or more H+ per molecule
A
Polyprotic acid
15
Q
can only donate 1 H+ per molecule
A
Monoprotic acid
16
Q
Brønsted-Lowry Theory
A
Acids: H+ donors
Bases: H+ acceptors
17
Q
substances that can act as an acid or base
A
Amphoteric
18
Q
Lewis Theory
A
Acids: electron pair acceptor
Bases: electron pair donor
19
Q
- taste sour (lemons, vinegar)
- turn blue litmus paper red.
- solutions: pH <7
- can conduct electricity in solution.
A
Acids
20
Q
are strong electrolytes.
A
Strong acids and bases
21
Q
- taste bitter and feel slippery.
- turn red litmus paper blue.
- solutions: pH > 7
- can conduct electricity in solution.
A
Bases
22
Q
Strong Acids (7):
A
- HCl (hydrochloric acid)
- HNO3 (nitric acid)
- H2SO4 (sulfuric acid)
- HBr (hydrobromic acid)
- HI (hydroiodic acid)
- HClO3 (chloric acid)
- HClO4 (perchloric acid)
23
Q
Strong Bases (8):
A
- LiOH (lithium hydroxide)
- NaOH (sodium hydroxide)
- KOH (potassium hydroxide)
- Ca(OH)2 (calcium hydroxide)
- RbOH (rubidium hydroxide)
- Sr(OH)2 (strontium hydroxide)
- CsOH (cesium hydroxide)
- Ba(OH)2 (barium hydroxide)
24
Q
is the potential of hydrogen ions.
A
pH
25
is the potential of hydroxide ions.
pOH
26
As pH increases, pOH increases.
As pH decreases, pOH decreases.
| TRUE OR FALSE
FALSE
| As pH increases, pOH decreases.
As pH decreases, pOH increases.
27
OFFICIAL INORGANIC ACIDS
* Boric acid (H3BO3)
* Hydrochloric acid (HCl)
* Diluted Hydrochloric acid
* Nitric acid (HNO3)
* Phosphoric acid (H3PO4)
* Diluted Phosphoric acid
* Sulfuric acid
28
Found in seawaters, certain plants, in nearly all fruits and in some volcanic steam jets.
## Footnote
Uses: Antiseptic, since it is a weak bacteriostatic acid agent; in 2% w/v concentration as eyewash and as buffer in ophthalmic solutions
Boric acid (H3BO3)
| Synonyms: Hydrogen borate, Boracic acid, and Orthoboric acid.
29
Boric acid Available in three crystalline forms:
a. colorless, odorless, pearly scales
b. six-sided triclinic crystals
c. white, odorless powder with a soapy feel
| The toxicity of boric acid makes it unfit to be taken orally.
30
* Prepared/ obtained from NaCl or rock salt
* When hydrogen chloride is dissolved in water it is formed. It is a simple diatomic molecule.
* Use: A pharmaceutical aid as an acidifying agent
Hydrochloric acid (HCl)
| Synonyms: Chlorhydric acid,
Spirit of Sea Salt, Muriatic acid
31
Uses:
1. Aiding in the conversion of pepsinogen into pepsin
and of proteins into peptones;
2. Serves as a gastric antiseptic; and,
3. It is also used in the management of gastric
achlorhydria and hypochlorhydria.
Diluted Hydrochloric acid
32
is the absence of HCl in the stomach
Achlorhydria
33
deficiency of HCl production of the stomach
Hypochlorhydria
34
* Prepared from a mineral or a salt, knowns as Potassium nitrate.
* Colourless but as it gets older it turns into a yellow cast.
* Highly corrosive and toxic.
* Causes severe skin burn.
* Reacts with hydroxides, metals, and oxides to form nitrate salts.
## Footnote
Uses:
* Manufacture of sulfuric acid
* Coal tar dyes and explosives
* Nitrating agent in Pyroxylin USP XVII
* Source of nitrate ion in the preparation of milk of bismuth
* Externally, for the elimination of chancres and warts
Nitric acid (HNO3)
Aqua Fortis, Aqua Fuerte
| Synonyms: Spirit of Nitre,
35
* is a weak acid with the chemical formula H3PO4.
* Present in teeth and bones and helps in metabolic processes
* In its liquid form, it appears as a clear, colourless solution
* In its solid form, it appears as a transparent, crystalline solid
Phosphoric acid (H3PO4)
| Synonyms: Orthophosphoric acid, Acido Orthofosforico
36
* The most important -oxy acid of phosphorus
* Used to make phosphate salts for fertilizers.
* Used in dental cement, albumin derivatives preparation and in the sugar and textile industries.
Phosphoric acid (H3PO4)
37
Uses:
* A tonic and stimulant to the gastric mucous membranes;
* A synergistic substance to pepsin and acids to the formulation of peptones.
Diluted phosphoric acid
38
* At higher concentrations, it acts as an oxidizing agent and dehydrating agent.
* A syrupy liquid which is odourless and has no colour.
* Water-soluble and releases heat when dissolved in water.
* Widely used in the manufacturing of fertilizers.
* used in chemical synthesis and wastewater processes.
Sulfuric acid (H2SO4)
39
OFFICIAL INORGANIC BASES
* Strong Ammonia Solution
* Diluted Ammonia Solution
* Calcium Hydroxide
* Potassium Hydroxide
* Sodium Hydroxide
* Sodium Carbonate
* Soda Lime
* Potassium Bicarbonate
* Sodium Bicarbonate
40
Uses:
* Bronsted base
* Manifacture of nitric acid and sodium bicarbonate
* Preparation of aromatic spirit and ammonia cal silver nitrate solution
Strong Ammonia Solution (NH4OH)
| Synonyms: Ammonium hydroxide, Stronger Ammonia Water
41
is used to treat or prevent syncope
Aromatic Ammonia Spirit
42
is an alkaline solution of ammonia cal silver nitrate and is used to test for aldehydes
Tollens' reagent
43
* Prepared from strong ammonia solution
* Known as ammonia water or household ammonia
* Employed as circulatory inhalant through inhalation of vapors
| Use:
Externally, it is used as counter-irritant agent
Diluted Ammonia Solution (NH4OH)
44
Preparation: Manufactured from lime or calcium oxide through the addition of water in limited amounts in slaking process, characterized by the avid absorption of water by the oxide lumps, and by the final disintegration into fine powder.
Calcium Hydroxide Ca(OH)2
| Synonyms: Slaked lime,
Calcium hydrate
45
Uses:
* Medicinally used as fluid electrolyte and topical astringent
* Utilized for its high hydroxide ion concentration in pharmaceutical preparations
* Utilized for it's potentially high hydroxide ion concentration
* Form calcium soaps, which have emulsifying properties
* Combined with NaOH or KOH in a mixture known as soda lime
Calcium Hydroxide Ca(OH)2
46
Properties:
* Deliquescent
* Very strong base with caustic/ corrosive effect on tissues (handle carefully)
Uses:
* A caustic in veterinary practice
* A saponifying agent to hydrolyze esters of fatty acids into their constituent alcohols and potassium salt
Potassium Hydroxide (KOH)
| Synonyms: Caustic potash, Potassa
47
Properties:
* It attacks soft glass (containers should be made of hard glass with rubber stoppers
* Glass-stoppered bottles can be used if a little petroleum or paraffin is spread around the stopper
* Not borosilicate, a soft glass has high coefficients of thermal expansion; thus it does not require a high temperature to make them soft.
Sodium Hydroxide (NaOH)
| Synonyms: Caustic soda , Soda lye
48
Use:
Same as potassium hydroxide but has more advantage since it is less deliquescent, milder, and cheaper
Sodium Hydroxide (NaOH)
49
Uses:
In pharmaceutical preparations, its basicity forms sodium salts of acidic drugs
Sodium Carbonate (Na2CO3.H2O)
| Synonyms: Monohydrated Sodium Carbonate
50
A mixture of Ca(OH)2 and NaOH or KOH or both intended for metabolism tests, anesthesia & O2 therapy.
Soda Lime (NaOH + Ca0)
51
Uses:
Buffering agent for pharmaceutical preparations
Potassium Bicarbonate (KHCO3)
52
Use:
Preferred in the preparation of effervescent mixtures containing sodium bicarbonate and organic acids such as tartaric or citric. These additives react to liberate CO2 that acts as a disintegrator producing effervescence when in water.
Sodium Bicarbonate (NaHCO3)
| Synonym: Sodium Hydrogen Carbonate
53
is a solution of a weak acid and its salt (conjugate base) or weak base and its salt (conjugate acid), that resists drastic changes in pH when small amounts of acid or base are added to it.
buffer
54
Buffers control the pH of pharmaceutical products within certain specified limits for these reasons:
* Chemical stability,
* Solubility of the drug, and
* Patients comfort.
55
Characteristics of a Buffer:
* It has a definite pH value.
* Its pH value doesn’t change on keeping for a long time.
* Its pH value doesn’t change on dilution.
* Its pH value doesn’t change even with the addition of a small amount of a strong acid or a base.
56
Factors which can produce alterations in pH includes the following:
* Alkali in certain inexpensive containers;
* Gases present in air such as CO2 and NH3;
* Effects of temperature, light, humidity, radiation and solvent used; &
* Presence of other chemicals resulting from contamination or from the unintentional/intentional mixing of different products.
57
# How to make buffers?
A buffer must contain a weak acid and its conjugate base. There are several ways a solution containing these two components can be made:
* Buffers can be made from weak acids or base and their salts.
* Buffers can be made from two salts that provide a conjugate acid-base pair.
* Buffers can be made by adding a strong acid or base to a weak acid or base.
58
Mechanism of Action of a Buffer
* Acid / Its salt
* Base / Its salt
59
# Important Considerations in Selecting or Choosing a Buffer
The selected buffer should not:
A. Participate in oxidation-reduction reaction
B. Alter the solubility of other components
C. Form complexes with active ingredient
60
Consider the following when choosing a buffer:
1. Volatile species should not be used as buffers
2. It should not have any influence on the pharmacological activity of the API
3. The use of pharmaceutical should be considered in choosing a buffer for a product. If it is to be ingested, buffers containing borates should not be used as they are toxic systematically.
61
Two Inorganic Buffer Systems
* Phosphate Buffer System
* Borate Buffer System
62
Uses :
It is included in preparation containing metals that would otherwise precipitate in the presence of phosphate. Since borates are toxic, this buffer system is suitable in external preparations, opthalmic, and nasal solutions but is contraindicated in parenteral solutions.
Borate Buffer System
63
Three Primary Borate Buffer Systems
1. FELDMAN'S BUFFER SYSTEM
2. ATKIN'S AND PANTIN BUFFER SYSTEM
3. GIFFORD BUFFER SYSTEM
64
boric acid+NaCl (to make it isotonic) + sodium borate
FELDMAN'S BUFFER SYSTEM
65
sodium carbonate + boric acid + NaCl
ATKIN'S AND PANTIN BUFFER SYSTEM
66
boric acid + KCl (to make it hypotonic) + sodium borate
GIFFORD BUFFER SYSTEM
67
Two Categories of Buffer System in Pharmacy
* Standard Buffer Systems
* Actual Pharmaceutical Buffer
68
designed to provide a solution having a specific pH for analytical purposes
Standard Buffer Systems
69
designed to maintain pH limits in drug preparation
Actual Pharmaceutical Buffer
70
Standard buffer solutions having pH ranges between 1.2 and 10.0 can be prepared by the appropriate combinations of :
* boric acid and sodium chloride, 0.2M
* hydrochloric acid, 0.2M
* potassium chloride, 0.2M
* potassium phosphate, monobasic 0.2M
* potassium biphthalate, 0.2M
* sodium hydroxide, 0.2M
* acetic acid, 2N
71
50 mL potassium chloride solution with a specified volume of 0.2M HCI and water
hydrochloric
acid buffer
| pH= 1.2 - 2.2
72
50 mL of potassium biphthalate solution with a specified volume of 0.2M HCl and water
acid phthalate
buffer
| pH= 2.2 - 4.0
73
a specified amount of sodium acetate solutions with a specified volume of the acetic acid solution and water
acetate buffer
| pH= 4.1 - 5.5
74
50 mL of potassium biphthalate solution with a
specified volume of NaOH and water
neutralized phthalate buffer
| pH= 4.5-5.8
75
50 mL of monobasic potassium phosphate solution with a specified volume of NaOH and water
phosphate buffer
| pH= 5.8 - 8.0
76
50 mL of boric acid and potassium chloride solution with a specified volume of NaOH and water
alkaline
borate
buffer
| pH= 8.0 - 10.0
77
* A chemical compound consisting of two hydrogen atoms and one oxygen atom forming a polar covalent bond.
* Odorless, tasteless, and a colorless liquid that is in small quantities and greenish blue in deep layers.
* One of the most important molecules to humanity.
* A crucial pharmaceutical agent due to its solvent powers and physiological inertness.
WATER
78
PROPERTIES OF WATER:
* Water is polar.
* Water is an excellent solvent.
* Water has a high heat capacity.
* Water has high heat vaporization.
* Water has cohesive and adhesive properties.
* Water is less dense as a solid than as a liquid.
79
WHY IS WATER THE SOLVENT OF CHOICE?
* Water is extensively used as a raw material, ingredient, and solvent in the processing, formulation, and manufacture of pharmaceutical products, active pharmaceutical ingredients (APIs), and intermediates.
* Water can dissolve much more substances than any other liquid found in nature. However, water cannot dissolve every substance.
* Water can be used in a variety of applications, some requiring extreme microbiological control and others requiring none.
* Water may be present as an excipient or used for reconstitution of products, during synthesis, during production of the finished product or as a cleaning agent for rinsing vessels, equipment, primary packaging materials, etc.
80
MAJOR CLASSIFICATIONS OF WATER
* NATURAL WATER
* POTABLE WATER
* PURIFIED WATER
* HEAVY WATER
81
All forms of water, including any river, stream, dam, lake, pond, swamp, marsh, canal, whether natural or artificial or other body of water forming part of that water course. The purest natural water is rain water.
NATURAL WATER
82
Water that is already filtered properly and is finally free from all contaminants and harmful bacteria. Purified water is fit to drink, or it can be called ‘drinking water after the purification processes, and is safe for both cooking and drinking.
It can be used during the manufacture of active substances and early stages of cleaning pharmaceutical manufacturing equipment.
POTABLE WATER
83
Prepared by distillation, ion exchange, and reverse osmosis. Purified water is widely used for oral and topical products and in granulation processes for tablets and capsules.
First, it must meet the requirements for ionic and organic chemical purity and must be protected from microbial contamination before being used in pharmaceutical applications.
PURIFIED WATER
84
* Water that has high mineral contents (Ca2+ and Mg2+ ions) also bicarbonate and sulfates.
* Calcium usually enters the water as either CaCO3, in the form of limestone and chalk, or calcium sulfate (CaCO4).
* Slightly heavier than normal water and is not harmful to one’s health. (Formula of D2O)
HEAVY WATER
85
TYPES OF NATURAL WATER
ALKALINE WATERS
CARBONATED WATERS
SALINE WATERS
SULFUR WATERS
CHALYBEATE WATERS
SILICEOUS WATERS
LITHIA WATERS
86
Usually contain appreciable quantities of sodium and magnesium sulfates.
Alkaline Waters
87
Those have been charged with carbon dioxide under pressure while in the Earth.
Carbonated Waters
88
Have iron in solution or in suspension and are characterized by a ferruginous taste.
Chalybeate Waters
89
Occur in the form of carbonate or chloride.
Lithia Waters
90
Also called "Purgative Waters". Hold relatively large amounts of magnesium and sodium sulfates with sodium chloride.
Saline Waters
91
Have hydrogen sulfide.
Sulfur Waters
92
Include very small amounts of soluble alkali silicates.
Siliceous Waters
93
Description: clear, colorless, odorless liquid; purified by distillation or reverse osmosis.
Use: ingredient in official preparations and it tests and assays unless otherwise specified.
PURIFIED WATER
94
Description: clear, colorless, odorless liquid; purified by distillation or reverse osmosis and contains no added substances.
Use: Pharmaceutic aid as a vehicle for dilution and reconstitution of suitable medicinal products for parenteral administration.
WATER FOR INJECTION
95
Description: It is prepared from Water for Injection that is sterilized and packaged in prefilled syringes or in vials containing not more than 30 mL. It also has one or more suitable antimicrobial agents.
Use: to dilute or dissolve medications
## Footnote
NOTE: Label should state: " NOT FOR USE IN NEONATES" as there were problems encountered with neonates and the toxicity of the bacteriostatic, benzyl alcohol
BACTERIOSTATIC WATER FOR INJECTION
96
Description: clear, colorless, odorless liquid; water for parenteral; sterilized; no antimicrobial agent or other added substances.
Use: for fluid replacement only after suitable additives are introduced to approximate isotonicity and to serve as a vehicle for suitable medications.
STERILE PURIFIED WATER FOR INJECTION
97
Description: clear, colorless liquid; water for injection that has been sterilized; no antimicrobial agent or other substance.
Use: an irrigating solution
STERILE WATER FOR IRRIGATION
## Footnote
NOTE: Label must say: "For irrigation only and NOT for injection"
98
Description: It is prepared from Water for Injection, sterilized and suitably packaged with no added microbial agents.
Use: May relieve symptoms of inflamed, swollen blood vessels in your nasal passages.
STERILE WATER FOR INHILATION
99
Are compounds that have the capability of functioning chemically as reducing agents.
They are pharmaceutical necessities since their addition prevents oxidative decomposition in the products.
Antioxidants
100
Mechanism of Action of Antioxidants
* An antioxidant is oxidized in place of an active compound.
* The antioxidant reduces the already oxidized active constituent back to its normal oxidation state.
* Inorganic antioxidants act through redox reactions. Redox reaction is when the oxidation-reduction reaction takes place simultaneously.
101
Uses:
The formation of free iodine is prevented in diluted hydriodic and syrup.
Its presence in ferrous iodide syrup ensures the non-formation of both ferric ions and molecular iodine.
Hypophosphorous Acid (H2P02)
102
Uses:
Salt of hypophosphorous acid are antioxidants
Sodium hypophosphite is a preservative in certain foods.
Ammonium hypophosphite is likewise a preservative in many preparations
Hypophosphorous Acid (H2P02)
103
Uses:
It will protect many susceptible compounds from oxidation by reducing the oxidized form back to its original compounds or by reacting with oxygen before the susceptible compounds do.
Sulfur Dioxide (S02)
| Synonym: Sulfurous Anhydride
104
Uses:
It is usually in injectable preparations in impulses or vials.
It is used in industry to bleach wood pulp, fumigate grains, and arrest fermentation.
Sulfur Dioxide (S02)
105
Synonyms:
Sodium hydrogen sulfite
Sodium acid sulfate
Leucogen
Uses:
It prevents oxidation of the compounds of phenol and catechol nucleus to quinones.
Sodium bisulfite (NaHSO3) or
Sodium metabisulfite (Na2S2O5)
106
Uses:
It prepares water-soluble derivatives of normally insoluble drugs.
Bisulfite and metabisulfite can be found in ascorbic acid injections as reducing agents.
Sodium bisulfite (NaHSO3) or
Sodium metabisulfite (Na2S2O5)
107
Uses:
As an inert atmosphere, it retards oxidation in oxidation-sensitive products and replaces air in containers for parenteral and solutions for topical applications.
Nitrogen (N2)
108
Uses:
It contains sulfur in two different oxidation states.
> the oxidized sulfur atom is in a +6 state resisting further oxidation.
> the remaining sulfur atom is in a zero oxidation state.
Sodium thiosulfate (Na2S2O3)
109
Uses:
This oxidation polarity allows the compound to act as a reducing agent.
It also act as an antidote for cyanide poisoning.
Sodium thiosulfate (Na2S2O3)
110
Uses:
Nitrite can act as both a reducing and oxidizing agent. Reduction of compounds with sodium nitrite results in the formation of nitrates.
It is an antidote for cyanide poisoning.
Sodium nitrite (NaNO2)
111
Uses:
Nitrites in brine solutions are curing ingredients of meats and fish for they are excellent color developers, enhance flavor production, and prevent microbial growth. However, nitrite ions remain in cured meats and react with organic amines to form potentially carcinogenic N-nitrosamines.
Sodium nitrite (NaNO2)
