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Chapter 6 Topical Agents Pharmaceutical Chemistry Lecture (Reviewer)

Matias, Charmaine Joyce M. Page 1



Topical places the use of these compounds on body surfaces.
Topical application of drugs may be accomplished within body cavities that open to the outside (e.g. the oral,
nasal, otic, vaginal and colonic activities).
The compound will exert local or surface activity

2 broad categories based on their usual action or use:
1. Protectives
2. Antimicrobials and Astringent compound

PROTECTIVES
- Applied to the skin to protect certain areas from irritation, usually from mechanical origin.

Desirable properties of Protectives:
1. Insolubility property that limits the absorption of the compounds through the skin; makes it difficult to wash
them off and diminish metallic properties on tissues.
2. Chemically Inert This property is necessary in order to prevent the interaction between the protective
substance and the tissue; biologically inactive.

Small particles offer larger surface area allowing them to adhere to each other, adhere better to the surface of
the skin and absorb moisture more efficiently.
Fine state of subdivision of the particles also offers a smooth substance which is soothing to apply and aids in
preventing irritation due to rubbing or friction.
Generally applied as dusting powders, suspensions containing the insoluble protective substance or ointments.
Protective substances are available for use internally for gastrointestinal irritations.

PROTECTIVE PRODUCTS

TALC USP 31 * 3MgO4SiO
2
H
2
O ]
Synonyms: French Chalk, Soapstone, Piedra Grassa, Creta Gallica
Definition: a native, hydrous magnesium silicate sometimes containing a small proportion of aluminum silicate.
Properties:
- Unctuous, adheres readily to the skin and is free from grittiness.
- Softest mineral known
- Lump form (stealite); is known as Soapstone.
- Form most desirable for cosmetic and pharmaceutical purposes is known as foliated talc and has a plate-like
structure.
- Very low adsorptive properties which is an important consideration for its use as filtering aid, allowing filtration
without danger or removing important constituents (e.g. alkaloids, dyes).

USES:
- Useful lubricating, protective dusting powder.
- Used to prevent irritation due to friction and to protect areas from further irritation.
- When used on broken skin, talc can produce sterile abscesses or granulomas ( a nodule of inflamed tissue in
which granulation is occurring).
- Absorbable dusting powders are recommended for surgical gloves rather than talc-containing dusting powders.




Chapter 6 Topical Agents Pharmaceutical Chemistry Lecture (Reviewer)

Matias, Charmaine Joyce M. Page 2

ZINC OXIDE USP 31 [ ZnO ]
Synonym: Zinc White, Lana o Algodon Filosoficos, Flores de Zinc
Preparations: by heating strongly in a furnace a mixture of coke and a zinc mineral (e.g):
Calamine (Zn
2
SiO
4
H
2
O)
Willemite (Zn
2
SiO
4
)
Smithsonite (ZnCO
3
)
Franklinite (ZnO, admixed with oxides of iron and manganese)
Zincite (ZnO, red variety)
free metallic zinc is liberated and vaporized.
- Medicinal grade of zinc oxide is also made by calcinations of zinc carbonate in a shallow vessel until a small
amount of the heated product no longer gives effervescence when treated with dilute mineral acid.

Properties:
- Gradually absorbs carbon dioxide from the air to form a basic zinc carbonate.
- Reacts with dilute acids and aqueous solutions of ammonium compounds to form water soluble products.
- When treated with dilute HCl, the oxide forms the Lewis acid, zinc chloride.
USES:
- Mild astringent
- Weak antimicrobial compound
- Used as a protective in ointment, pastes and dusting powders in the treatment of skin ulceration and other
dermatological problems.
- As a dusting powder, frequently found in combination with other protective and antimicrobial agents (talc and
boric acid).
- Primary ingredient of Calamine USP.

CALAMINE USP 31 * ZnOxFe
2
O
3
]
- Zinc oxide with a small proportion of ferric oxide.
- The presence of ferric oxide gives the substance a pink color which varies according to the method of
preparation and the amount of ferric oxide present.
- Fine powder, odorless, and practically tasteless
- Official forms are ointment, paste, and the Zinc oxide with salicylic acid paste.

USES:
- Classified as a topical protective
- Used as dusting powders, ointments and lotion where it is applied to the skin for its soothing, adsorbent,
protective properties.
- Calamine has better cosmetic acceptability than zinc oxide.
- Exudation of fluids, respond reasonably well to the application of products containing Calamine.
Calamine Lotion USP most widely used preparations containing calamine; is a protective with a good drying
effect and a mild astringent action.
Phenolated Calamine Lotion contains 1% liquefied phenol which provides a local anesthetic and antipruritic
action.







Chapter 6 Topical Agents Pharmaceutical Chemistry Lecture (Reviewer)

Matias, Charmaine Joyce M. Page 3

ZINC STEARATE USP 31
Properties:
- Mixture of solid organic acids obtained from fats and consists chiefly of variable proportions of zinc stearate and
zinc palmitate.
USES:
- Mild astringent and antimicrobial properties
- Employed in dusting powders and ointments as protective.
- As well as magnesium stearate, is widely used as a lubricant in the manufacture of tablets.
ADVANTAGE: it is not wetted by moisture.
- This property makes the material more desirable in dermatological problems where large amounts of fluids are
exuded, because it will not form crusty patches over the areas being treated.
DISADVANTAGE: inhalation of zinc stearate dust can cause pulmonary inflammation.
- For this reason, its route use as dusting powder for infants and children should be strongly discouraged.

TITANIUM DIOXIDE USP 31 [ TiO
2
]
Properties:
- White amorphous, odorless, tasteless, infusible powder.
- 1:10 aqueous suspension of the compound is neutral to litmus paper.

Official Identification of the compound:
- Reaction of TiO
2
with H
2
O
2
in dilute H
2
SO
4
produces Titanium Peroxide (TiO
3
) which imparts an orange-red color
to the solution.
USES:
Official Category: Topical protective
- Used primarily for its opacity (unique property not allowed to pass) due to its high refractive index (useful for
screening out ultraviolet reaction).
- Used in various sun creams and sun screen products.
- As a solar ray protective, it is used in concentrations of 5% to 25% in ointments or lotions.
- Organic sun screen agents (e.g. p-aminobenzoic acid) act chemically by absorbing ultraviolet radiation.
- Used as a white pigment in cosmetic and paints.

SILICON POLYMERS
Properties:
- Inert protective substances occurring in liquid form and known generally as silicone oils.
- Primarily dimethylsilicone ethers.
- Dimethicone or Simethicone USP 26 (polymer) is used in ointments and creams for application to the skin as a
water repellent and protectives against contact irritants.
- Silicone oils adhere very well to the skin and exclude contact with air; they should not be applied over broken or
abraded skin or wounds requiring drainage.
- Primary use: prophylactic agent against chemical irritants.









Chapter 6 Topical Agents Pharmaceutical Chemistry Lecture (Reviewer)

Matias, Charmaine Joyce M. Page 4

ANTIMICROBIALS AND ASTRINGENTS

MECHANISM OF ACTIONS:
- Represent the primary chemical interactions or reactions that occur between the agent and the microbial
protein can result in the death of the microbe or inhibition of its growth.

1. Oxidation
- Compounds capable of functioning as antimicrobial agents through oxidative mechanisms are generally non-
metals and certain types of anions (H
2
O
2
, metal peroxides, permanganates, halogens (Cl
-
, I
-
) and certain
oxohalogen anions.
- The overall change or destruction of function in specific proteins is responsible for the ultimate destruction of
the microorganism.
- The chemical result of oxidizing the protein is reduction of the antimicrobial agent.

2. Halogenation
- Reaction occurring with antiseptics of the hypohalite type (ClO
-
).
- The reaction is ultimately destructive to the function of specific proteins because the substitution of the Cl
-
for
the hydrogen produces changes in the forces (hydrogen bonding) responsible for the proper conformation of
the protein molecule, the changes in conformation will result to the destruction of function.

3. Protein Precipitation
- Involves the interaction of proteins with metallic ions having large charge/radius ratio or strong electrostatic
fields (transition metal cations, metals of Group I B and Group II B, Al).
- The complexation of the metal results in the radical change in the properties of the protein or protein
precipitant.
- By increasing concentrations, antimicrobial, astringent, irritant and corrosive properties are successively
available.

ASTRINGENT
- Its effect can be observed or felt, when applied to the skin or mucous membrane.
- The effect can be generally described as shrinkage or firming of tissues.

CONTROL OF ANTIMICROBIAL/ ASTRINGENT ACTION
Inorganic antimicrobial agents are largely non-specific in their actions or proteins
The action on microbial versus host cells is determined by concentrations.

a. Water soluble compounds
- Control of activity is accomplished by making solutions of the appropriate concentration for the desired use.
e.g. Higher concentrations may be used on the skin than in the eye.
- Controlled by placing them in a vehicle which will slow their release to the site of action.
e.g. placing them in a solutions containing glycerin ( glycerite of hydrogen peroxide) or polyethylene glycol.

b. Complexation with a ligand
- Provides a controlled release of some of these agents, minimizing toxicity and activity at host cells (e.g.
Povidone-Iodine)

c. Synthesized into an insoluble form and used in suspensions, ointments and creams for microbial actions
- This will slow the release of the active ingredient.

Chapter 6 Topical Agents Pharmaceutical Chemistry Lecture (Reviewer)

Matias, Charmaine Joyce M. Page 5

HYDROGEN PEROXIDE SOLUTION USP 31 [ H
2
O
2
]
Synonyms: Hydrogen Peroxide, Aqua Oxigenada

Properties:
- Suitable preservatives totaling not more than 0.05% may be added.
- Acid to litmus
- Pure hydrogen peroxide, at room temperature is a colorless, syrupy liquid with astringent properties (not use on
the skin in this form).
- Heated to 100C pure hydrogen peroxide decomposes explosively to form water and oxygen.
- The solution will usually deteriorate upon standing and rapidly decomposes when in contact with many oxidizing
or reducing substances.
- Unstable on prolonged exposure to light and may decompose suddenly when rapidly heated.

DIFFERENT WAYS TO RENDER H
2
O
2
:
a. It should be kept in a cool place protected from light and dust.
b. Amber-colored bottles are used as containers.
c. Preservatives such as acetanilide is added
d. It may be stabilized with any organic and inorganic acids, complexing agents or adsorbents.

- Complexing or chelating agents will chelate trace amounts of abundant metals, thereby making them
unavailable to catalyze decomposition.

USES:
- Primary use: Mild oxidizing antiseptic
- In theory, the oxygen acts as an oxidizing agent on bacteria, providing antiseptic action particularly on those
organisms obliges to survive through anaerobic metabolism.
- Destroy most pathogenic bacteria ( Escherichia coli, Staphylococcus aureus, Typhoid bacilli).
- Mechanical cleansing action provided by the foaming release of oxygen.
- Effervescent action aids in the removal of dirt, bacteria and debris from the surface of a wound or difficult-to-
reach areas, e.g. the ear canal.
- Official solution: containing 3% H
2
O
2
is referred to as a 10 volume solution, indicating that 1 mL of the solution
will liberate a total of 10 mL of oxygen at the standard temperature and pressure. (one with medicinal use)
- 6% solution (20 volumes) is used as a hair and fabric bleach.
- Used undiluted for its antiseptic and cleansing effect on wounds.
- Diluted, used as a gargle or mouthwash in the treatment of bacterial infections of the throat and mouth.
- Half-strengths may also be used as a vaginal douche
- Diluted to less than half-strength, tends to lose its antiseptic property.












Chapter 6 Topical Agents Pharmaceutical Chemistry Lecture (Reviewer)

Matias, Charmaine Joyce M. Page 6

POTASSIUM PERMANGANATE USP 31 [ KMnO
4
]
Synonym: Mineral Chameleon
Properties:
- Odorless, dark purple crystalline compound.
- Crystals are almost opaque in transmitted light and of blue metallic luster in reflected light.
- Concentrated solutions have a deep violet-red color and highly diluted solutions are pink.
- Sweetish astringent taste
- Chemically, a strong oxidizing agent both in the dry state and in solution.
CAUTION: Observe great care in handling KMnO
4
, as dangerous explosions may occur if brought in contact with organic
or other readily oxidizable substances, either in solution or in the dry state.
- The compound in dry state forms explosive mixtures with charcoal
- Will produce fore when mixed with glycerin
- Oxidize alcohol
- Acid solution, react to reduce the MnO
4
-
to the Mn
2+
with the evolution of oxygen.
- Neutral or alkaline solution produces a similar reaction (above) with the characteristic brown ppt. of MnO
2.
(therapeutic importance; permanganate are applied to the skin in neutral solutions)
- Antimicrobial action is dependent upon its oxidation of protein or other bio-organic substances in neutral media.
- It oxidizes all organic matter

USES:
- Not used for both their antibacterial and antifungal actions.
- Primarily used today for skin infections (dermatitis) caused by bacteria and fungi and for poisoning produced by
plant and animal toxins.
- Wet dressings, are used in the treatment of vesicular (presence of small blisters or raised areas containing fluid)
stage of eczema, athletes foot (Tinea pedis) and fungal infections on other portions of the body, e.g. groin (Tine
curries).
- Better results may be achieved through direct applications of dilute solutions.

SODIUM HYPOCHLORITE SOLUTION USP 31 [ NaOCl ]
Synonyms: Dakins solution, Chlorinated Soda Solution
Properties:
- Used as disinfectant for inanimate objects only
- Clear pale greenish yellow liquid having an odor of chlorine.
- Alkaline pH coloring red litmus paper blue (chlorine will later bleach the color).
- USP 26 classifies Sodium Hypochlorite Solution as a disinfectant and makes the following statement: CAUTION:
This solution is not suitable for application to wounds.
- The alkalinity and oxidizing action of this solution is too strong for use on tissues.
- The solution dissolves blood clots and delay healing.
- Diluted form is known as Labarraquess solution and consists of NaOCl which has been diluted with an equal
volume of water.
- Upon exposure to air, it loses active chlorine and the product as useless for the purpose it is intended.
USES:
- Useful as disinfectant and laundry bleach
- Effective germicidal agent





Chapter 6 Topical Agents Pharmaceutical Chemistry Lecture (Reviewer)

Matias, Charmaine Joyce M. Page 7

DILUTED SODIUM HYPOCHLORITE SOLUTION
- Colorless or light yellow liquid having a slight odor suggesting chlorine
- pH 8.3 or less
- dilution of household bleach does not normally meet the USP standards as an antiseptic because of the lack of
pH adjustment.
USES:
- Used in the past as an antiseptic on pus-forming wounds
- As an irritation solution for infections inside certain body openings.
- Removing necrotic tissue.
DISADVANTAGE: dissolving certain types of sutures and of dissolving blood clots and prolonging clotting time.
- Used as a foot bath in the prevention of various fungal infections (athletes foot).

OTHER CHLORINE-CONTAINING COMPOUNDS

1. CHLORINATED LIME Bleaching Powder, Chlorine of Lime
- Chemically, Calcium Chloride Hypochlorite CaOCl(Cl)2H
2
O
- Product obtained by passing chlorine gas over slaked lime.
- Distinct odor of chlorine and decomposes in the air to release hypochlorous acid.
- Used as an disinfectant in swimming pools and sterile rooms
- Bleaching agent

2. CHLORAMINES
- Organic amines with one or two Cl
-
bonded to the nitrogen.
- Dissolved in water they slowly hydrolyze to release hypochlorous acid.
- Used as disinfectants
- Used in purification of drinking water supplies. (e.g. Chloramine-T and Halazone)
- The antimicrobial action is due to the presence of HOCl.

IODINE USP 31 [ I ]
Synonyms: Iodinum, Jodum
Properties:
- Heavy, grayish black plates or granules, having metallic luster and a characteristic penetrating odor.
- The solubility in solutions of iodide (e.g. Sodium Iodide) is due to the formation of triiodide (I
3-
).
- Both of the iodide and triiodide ions are devoid (absence) of antibacterial activity.
- Most notable chemical property of iodine in aqueous solution is that of mild oxidizing agent.
- Free iodine is about six times more effective than hypoiodous acid, HIO.
- Iodine will oxidize iron to form ferrous iodide.
- Toxicity of preparations containing free iodine is frequently mentioned and somewhat overstated; iodine is
easily inactivated by organic materials in the GI tract, producing abdominal pains, gastroenterititis and possibly
bloody diarrhea.
- Treatment involves gastric lavage with soluble starch solutions or administration of a 5% sodium thiosulfate
solution.
- Most frequently used preparations which contain iodine for antimicrobial purposes are Iodine Solution and
Iodine Tincture (solvent: alcohol).
- Both solutions are transparent, have a reddish brown color and have the characteristic odor of iodine.
- Iodine Tincture also has the odor of alcohol.



Chapter 6 Topical Agents Pharmaceutical Chemistry Lecture (Reviewer)

Matias, Charmaine Joyce M. Page 8

USES:
- Iodine Tincture and Iodine Solution are the most effective topical antiseptic agents available.
- Used as antiseptics on the skin prior to surgery
- Iodine Tincture, more suitable for antiseptic prior surgery, since the alcohol seems to improve the penetration of
the iodine due to a wetting or spreading effect.
- Both preparations can be diluted with water to provide effective solutions of reduced concentrations for
application to wounds because of alcohol in the Tincture is very irritating to open wounds.
- The official solution and Tincture are effective against bacterial and fungal infections of the skin.
- Iodine Tincture may be used t disinfect drinking water. Treatments of water supplies with three drops per quart
will amoebae and bacteria in 15 minutes.
- Both Iodine Solution and Tincture are available in official concentration (2%) and can be dilutes to 0.5% to 1%
concentration for application to wounds and to 0.1% for irrigation.

POVIDONE-IODINE USP 31
- Complex of iodine with Povidone which is a polymer also known as polyvinylpyrrolidone or PVP.
- Yellowish brown amorphous powder and has a slight characteristic odor
- Aqueous solution acid to litmus
- Member of a class of compounds referred to as iodophors (complexes of iodine with carrier organic molecules
serving as a solubilizing agent)
USES:
- Iodine solution and Tincture is more effective
MAJOR ADVANTAGE: the lack of tissue irritation which makes them useful for application to sensitive areas and mucous
membranes.
- Solutions are recommended for surgical scrubs
- Preoperative antisepsis
- Used in gargles and mouthwashes for the treatment of infections in the oral activity (Vincents agina).
- Preparations include as aerosol (0.5%), solutions (1%), surgical scrub (0.75%) and a vaginal douche (1%).

SILVER NITRATE USP 31 [ AgNO
3
]
Synonyms: Azotas Argenticus, Crystales Lunares
Properties:
- Colorless or white crystals which becomes gray or grayish black on exposure to light in the presence of organic
matter
- Very soluble in water.
- The protein precipitant action of silver is not selective and will precipitate both bacterial and human protein.
- Silver presents an interesting property referred to as oligo-dynamic action, meaning it is active in small
quantities.
- Extended use of silver preparations is likely to cause a darkening of the skin due to the deposition of free silver
below the epidermis; termed as argyria.
USES:
- Employed as an antimicrobial in solutions ranging in concentraton from 0.01% to 10% recognizing that the
higher concentration present astringent and irritant properties to the tissues.
- External use only






Chapter 6 Topical Agents Pharmaceutical Chemistry Lecture (Reviewer)

Matias, Charmaine Joyce M. Page 9

SILVER NITRATE OPHTHALMIC SOLUTION USP 31b
- 1% solution for instillation into the eyes of the newborn babies.
- Quite effective against gonococcal organisms and two drops are placed in each eye as a prophylactic measure
against infections produced by these organisms (Ophthalmia Neonatorum).
- More effective than antibiotics such as penicillin.
- Treatment of choice because the silver ion seemed to be particularly effective at reducing infection due to
Staphylococcus aureus, various species of Proteus and Pseudomonas aeruginosa.
- Common side effects associated with this treatment involves electrolyte imbalance due to precipitation of
chloride.

TOUGHENED SILVER NITRATE USP 31
Synonym: Lunar Caustic, Silver Nitrate Pencils
- Made by adding to silver nitrate 4% of its weight of HCl
- Melting the mixture at a low temperature as possible and casting in silver molds.
- The presence of about 5% silver chloride toughens the silver nitrate and thus lessens the friability of pencils.
- Used as escharotics (substances that kills tissue) and germicide especially for small septic wounds and ulcers.

AMMONIATED MERCURY USP 31 [ Hg(NH
2
)Cl) ]
Synonym: White Precipitate
Properties:
- White, pulverized (easily powdered) pieces or as a white, amorphous powder, is odorless and stable in air, but
darkens on exposure to light.
- The antiseptic action of mercury on microorganisms and body tissues is due primarily to the mercuric ion, which
will react with many polar groups.
USES:
- Local anti-infective
- Topically as a 5% ointment to skin
- 3% ophthalmic ointment to conjunctivas
- Not given internally because of toxicity.
Acrodynia red skin due to mercury.

SUBLIMED SULFUR USP 31 [ S ]
Synonym: Flowers of Sulfur, Azufre
Properties:
- Fine, yellow, crystalline (rhombic) powder having a faint odor and taste.
- Obtained by condensing the sulfur vapors produced by heating any form of sulfur.
- Topical scabicide












Chapter 6 Topical Agents Pharmaceutical Chemistry Lecture (Reviewer)

Matias, Charmaine Joyce M. Page 10

PRECIPITATED SULFUR USP 31
Synonym: Milk of Sulfur
Properties:
- Slaking sulfur with metal hydroxides to form mixtures of metal sulfides and thiosulfates.
- Very fine, pale yellow, amorphous or rhombic powder without odor or taste.
- Carbon disulfide is the same as Sublimed Sulfur.
USES:
- Categorized as scabicides
- Used in Sulfur Ointment USP
- Treatment of scabies, in which it kills the mite Sarcoptes scabiei
- Effective against live parasite but has no effect on the eggs.
- Dermatological agent in the treatment of seborrhea (an abnormal secretion of sebum from the sebaceous
glands, giving an oily or scaly appearance to the skin), acne, psoriasis, etc.
- Keratolytic agent
- Symptomatic treatment for many dermatological problems

SULFURATED POTASH
Synonym: Liver of Sulfur
Properties:
- Composed chiefly of potassium polysulfides and potassium thiosulfate
- Occurs as irregular, liver brown pieces when freshly made, changing to a greenish yellow color.
USES:
- Official as a pharmaceutical aid as a source of sulfide
- Used in the preparation of White lotion
- Used as a parasiticide (scabicide)
- Treatment of acne and psoriasis.

SELENIUM SULFIDE
Synonym: Selenium Disulfide
Properties:
- Bright orange powder having no more than a faint odor.
- Toxic in large quantities
- Topical application to limited areas of unbroken, unirritated skin will not usually result in selenium toxicity.
USES:
- Used in shampoos in concentration of 1% to 2.5% as an anti-seborrheic
- The hands should be thoroughly washed and the fingernails meticulously cleansed after using selenium sulfide.

ANTIMONY POTASSIUM TARTRATE USP 31 [ (SbO) KC
4
H
4
O
6
1/2H
2
O ]
Synonym: Tartar Emetic
USES:
- Used as an emetic and expectorant (Brown Mixture)
- Treatment of schistosomiasis (intestinal worms)
- Example: Stibophen which is effective against Schistosoma haematobium and Schistosoma mansoni but less
effective against Schistosoma japonicum.
- Given orally but intravenous doses are more effective.




Chapter 6 Topical Agents Pharmaceutical Chemistry Lecture (Reviewer)

Matias, Charmaine Joyce M. Page 11

ASTRINGENTS
- Protein precipitant of limited penetrative power.
- To coagulate protein primarily on the surface of cells
- General constriction of tissue e.g. small blood vessels then occurs under the influence of the astringent but the
action is controlled by virtue of being topical, lacking deeper effects.
- Firming of tissues.

Some of the uses for astringent compounds include:
1. Styptic to stop bleeding from small cuts by promoting coagulation of blood and constriction of small
capillaries.
2. Antiperspirant to decrease secretion of perspiration by constricting pores at the surfaces of skin.
3. Restriction of the supply of blood to the surface of mucous membrane as a means of reducing inflammation.
4. Direct actions on skin to remove unwanted tissues. Sometimes termed as corrosives.

ALUM USP 31 [ AlNH
4
(SO
4
)
2
12H
2
O ] [ AlK(SO
4
)
2
12H
2
O ]
Properties:
- Can be either aluminum ammonium sulfate or aluminum potassium sulfate
- The label in the container must indicate which salt is being dispensed.
- Freely soluble in water, slowly soluble in glycerin and insoluble in water.

USES:
- Source of aluminum ion
- Useful as a topical astringent
- High astringency of the compounds makes it possible for certain preparations to be used as irritants or caustics.
- Used in footbaths
- Active ingredient in styptic pencils
- Used to stop bleeding from small cuts.
- Used in the preparation of several biological products (e.g. precipitated diphtheria and tetanus toxoids).

ALUMINUM CHLORIDE USP 31 [ AlCl
3
6H
2
O ]
Properties:
- White or yellowish white, deliquescent, crystalline powder.
USES:
- Local external astringent
- Mild antiseptic
- Used as an antiperspirant but was found to be irritating to sensitive tissues and also damaged to clothing due in
part to the formation of HCl by hydrolysis.
- Replaced by aluminum hydroxychloride which is less acidic and less irritating as antiperspirant. (e.g. Aluminum
hydroxychloride as Arrid, Right Guard, etc.)

OTHER ALUMINUM-CONTAINING ASTRINGENTS

ALUMINUM SULAFTE USP 31 [ Al
2
(SO
4
)
3
14H
2
O ]
Synonyms: Cake Alum, Pickle Alum, Pearl Alum, Papermakers Alum

ALUMINUM ACETATE SOLUTION USP 31
Synonym: Burrows Solution


Chapter 6 Topical Agents Pharmaceutical Chemistry Lecture (Reviewer)

Matias, Charmaine Joyce M. Page 12

ZINC CHLORIDE USP 31 [ ZnCl
2
]
Synonym: Butter of Zinc
Properties:
- White, odorless, crystalline powder or granules
- Very deliquescent salt
- Its solution in water or in alcohol is usually slightly turbid but the turbidity disappears when a small quantity of
HC is added.

USES:
- Astringent and dentin desensitizer (drug that reduces pair)
- Strong astringent properties
- Useful as escharotics, this is more of a caustic than astringent action.

ZINC SULFATE USP 31 [ ZnSO
4
7H
2
O ]
Synonym: White Vitriol
Properties:
- Colorless, transparent prisms or as small needles
- Acid to litmus

USES:
- Externally as an ophthalmic astringent in 0.25% solution.
- Acidic nature of Zinc Sulfate Solutions requires buffering which can be achieved by additions of borate buffer
systems, e.g. Gifford Buffer System