The document discusses various dental products used for oral health including antiplaque agents like chlorhexidine and povidone-iodine, anticaries agents like fluorides, and dentifrices. It provides details on the composition, mechanisms of action, uses, and side effects of these agents. The goal of these products is to inhibit plaque formation, prevent dental caries, and promote oral hygiene.

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Md. Saiful Islam
Dept. of Pharmaceutical Sciences
North South University
Facebook Group: Pharmacy Universe
Dental Products

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Dental Products
 Antiplaque agents
 Anticaries agents
 Dentifrices
 Mouthwash

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Antiplaque agents
Dental plaque: Dental plaque is a whitish soft accumulation of
bacteria and their substrate which deposits on the teeth while not
cleaned adequately.
Plaque formation: Plaque formation does not take place
haphazardly but in a reasonably orderly manner.
A pellicle derived from the saliva or gingival fluid first forms
on the teeth. This pellicle is a thin, clear cuticle and is composed
mainly of glycoproteins.
Very soon after its formation, bacteria of the coccus type
(streptococci largely) are attached to the pellicle which has a
‘sticky’ surface, i.e. one which enables colonies of organisms to be
anchored. These organisms divide and form colonies.
Attachment of the microorganisms is further enhanced by the
production of dextrans by the bacteria as by-products of metabolic
activity. Later other types of organisms are attracted to the mass
and a dense mixed flora of filamentous forms i.e. plaque results.
Plaque may attach to the teeth supragingivally, or
subgingivally in the gingival crevice, or in periodontal pockets.

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Antiplaque agents: Antiplaque agents are the agents or drugs that
are used to prevent or inhibit plaque formation in the mouth, e.g.
chlorhexidine, povidone iodine etc.
Ideal properties of an antiplaque agent:
1. It should be non-toxic, non-allergic and non-irritating.
2. It should have a broad spectrum of antimicrobial activity
3. It should specifically affect only the pathogenic flora.
4. It should not have any induced drug resistance.
5. It should have an acceptable taste.
6. It should possess sufficient chemical stability, so that it can
be stored for a reasonable length of time.
7. It should be of low price and available.

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Chlorhexidine
Chemistry: It is a chlorophenyl bisbiguanide that has been used as
the acetate and more commonly the gluconate salt in mouth rinses,
gels and dentifrice for control of plaque and gingivitis. It is highly
cationic antiseptic. It has fungicidal activity and bactericidal action
against both gram positive and gram negative microorganisms.
Mechanism of action: Due to its high cationic nature
chlorhexidine binds the anionic groups on the bacterial surface, i.e.
phosphate group of terchoic acid in gram-positive bacteria and
phosphate group of lipopolysaccharides in gram negative bacteria.
When the bisbiguanide binds to the organism, the cell
membrane becomes permeable allowing the cytoplasmic contents
to leak out of the cell. At higher concentration chlorhexidine
causes precipitation of cytoplasmic proteins.
By virtue of their cationic properties the bisbiguanides also
bind electrostatically to the hydroxy-apatite of teeth and forms a
pellicle (film or surface) against plaque and to buccal mucosa. This
is how it acts as an anti-plaque agent.

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Uses: Chlorohexidine is used in the following vehicles:
1. Mouth rinse:
a. 0.12% chlorhexidine gluconate solution is used as a
mouthwash for oral hygiene and oropharyngeal infections,
especially aphthous ulcers. .
b. 0.2% chlorhexidine gluconate solution prevents the
accumulation of plaque. It is absorbed onto tooth enamel, where it
exerts a persisting action to decrease the growth of dental plaque.
2. Irrigator: 400 ml of a 0.02% soluition of chlorhexidine (80 mg
totally) applied once daily in an oral irrigator will give complete
plaque inhibition.
3. Gels: 1% gel of chlorhexidine gluconate applied for a period of
five minutes, once or twice a day is effective in the inhibition of
bacterial plaque particularly in the treatment of denture stomatitis.
4. Antiseptics: 4% aqueous solution of chlorhexidine is effectively
used as a surgical scrub, it decreases the cutaneous bacterial
population more than either hexachlorophene or povidone iodine.

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Clinical indication of chlorhexidine:
1. Short term application:
a) Healing phase in periodontal surgery
b) Healing phase in oral surgery
i) Mandibular fracture
ii) Third molar extraction
c) Pre-surgical use to reduce bacteremia (bacteria in the
blood)
d) Therapy for apthus ulceration
e) Therapy for denture stomatitis
f) Therapy for acute necrotizing ulcerative gingivitis.
2. Intermediate short term application
a) Repeated denture stomatitis
b) Adjunct to periodontal maintenance care.
c) Dental implants

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Side effects or adverse reaction of chlorhexidine:
1. The most common side effect of chlorhexidine is the
formation of staining or an extrinsic yellowish or brownish
discoloration of the tooth surface and gum. Stain may appear
on the natural teeth, artificial teeth and composite filling
though it depends on the concentration and varies greatly
from one individual to another.
2. It has an unpleasant bitter taste and may cause irritation to the
oral mucosa and disturbance in the taste buds.
3. Regular use of chlorhexidine may sometimes block the
salivary duct of the parotid gland and lead to a painful
condition
4. Local tissue damage may occur if the drug is applied to
abraded epithelium.
5. Hypersensitivity reaction may occur in some individuals.
Precaution: (i) Chlorhexidine rinses should be performed after
meals to minimize taste alteration.
(ii) Patients should not rinse with water following a
chlorhexidine rinse.

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Povidone-iodine:Povidone-iodine is a stable chemical complex of
polyvinylpyrrolidone (PVP) and elemental iodine. It shows broad
spectrum germicidal action and acts as bactericide (both gram-
positive and gram-negative). It is effective in dilute solution and
does not develop resistance in microorganisms.
It is safer and easier to use than classic iodine preparations and has
low systemic toxicity. Unlike iodine solutions, it does not cause
pain when applied to wounds or mucous membranes. It is less
irritating to the skin than conventional iodine preparations. It will
not permanently stain skin or hard surfaces.
Use: Povidone-iodine containing mouth-wash and gargle is used
for the treatment of acute mucosal infections of the mouth and
pharynx. It is also used for oral hygiene prior to, during and after
oral surgery.

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References:
1. A manual of paediatric dentistry – R.J. Andlaw, W. P Rock
2. Dental pharmacology- dr. A.N.M Nazmul Islam
3. Handbook of paediatric dentistry- Editor Angus C.
Cameeron.
4. Preventive dentistry- John O. Forrest
5. Remington’s pharmaceutical sciences (EighteenthEdition-
page 1965)

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Anticaries agents
Dental caries: Dental caries is gradual decay and disintegration of
tooth tissues, i.e. progressive decalcification of the enamel and
dentin of a tooth.
The ultimate effect of caries is to break down enamel and
dentine and thus open a path for bacteria to reach the pulp. The
consequences are inflammation of the pulp and, later, of the
periapical tissues. Infection can spread from the periapical region
to the jaw and beyond.
Types of carries according to location:
(i) Pits and fissure caries
(ii) Smooth surface caries
(iii) Root caries
(iv) Deep dentinal caries

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Factors involved in the initiation of dental caries/ Essential
requirements for development of dental caries: Dental caries is
a multifactorial disease and the following four factors are involved
in the initiation of dental caries:
1. Susceptible tooth surface to acid attack: Generally caries is
initiated in the enamel but it may also begin in dentine or
cementum.
2. Plaque attached to the tooth surface: Plaque is a
tenaciously adherent deposit that forms on tooth surface. It
consists of an organic matrix containing a dense
concentration of bacteria.
3. The bacterial activity in the plaque: Plaque contains
bacteria that are acid producing. Mutans streptococci are
believed to be the most important bacteria in the initiation
and progress of dental caries.

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4. Substrates: Bacteria utilize fermentable carbohydrates for
energy and the end-points of the glycolytic pathway in
bacterial metabolism are acids. Sucrose is the fermentable
carbohydrate most frequently implicated but bacteria can use
all fermentable carbohydrates, including cooked starches.
The interaction of these factors is illustrated by the simplified
equation:
Plaque
Bacteria + Sucrose = Acid + Susceptible tooth surface = Caries
Caries initiation is the action by microorganisms in the
plaque which is in intimate relationship with the tooth surface.
These organisms act on sucrose products entering the plaque after
carbohydrate ingestion, and form acids which at the critical pH
level (below 5.5) bring about enamel dissolution.

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Prevention of dental caries/ Preventive efforts relative to
caries:
(i) Increasing the resistance of the tooth surface enamel against
acid products: The resistance of the tooth surface enamel to acid
attack can be very greatly enhanced by the incorporation of minute
amounts of fluoride ion so that the hydroxyapatite crystals become
fluoroapatite. The principal mode of action of all fluorides (tooth
pastes, rinses, gels and community water fluoridation) is its topical
effect on enamel.
(ii) Diet modification: Minimizing intake of dietary refined
carbohydrates and good dental hygiene prevent growth of bacteria
that contribute to the development of caries. Sweets etc. should be
limited to mealtimes.
Frequency of intake is more important than overall quantity.
‘Grazing’ or ‘snacking’ between meals should be avoided.
The frequent consumption of soft drinks is a major problem,
these being not only cariogenic but extremely erosive.

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(iii) Plaque removal: Proper brushing of the teeth is effective in
preventing and removing dental plaque in all areas except those
between the teeth and deep fissures. Ideally, tooth brushing should
be carried out twice a day and emphasis should be placed on
brushing just before bed.
Use of dental floss or tape removes plaque from between adjacent
tooth surfaces; deep pits and fissures may be sealed by the
application of resins. The sealant may need to be replaced
periodically.
Parents should be advised to begin cleaning their children’s teeth
from when they first erupt. Gauze or a cloth on a finger, or a small
very soft toothbrush may be used to remove the plaque.
(iv) Early detection and dental restorations offer the best form of
control once caries has formed.

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Fluorides in the prevention of dental caries/Effects of fluorides/
Mechanism of action of fluorides:
The principal mode of action of all fluorides (tooth pastes, rinses,
gels and community water fluoridation) is its effect on enamel. The
resistance of the tooth surface enamel to acid attack can be very
greatly enhanced by the incorporation of minute amounts of
fluoride ion so that the hydroxyapatite crystals become
fluoroapatite.
The formation of this solubility resistant form explains the
mode of action of fluorides as preventive agents.

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Fluoride therapy (Systemic fluoridation and topical
fluoridation): In the child, the developing tooth will receive its
necessary building materials from the blood plasma and thus the
enamel fluorine content will at this point be completely dependent
on systemically absorbed fluorine. After tooth eruption, maturation
of the enamel takes place and a great deal of fluoride uptake is a
topical one. Hence it may be assumed that that fluoride acts in two
complementary ways- by systemic action and by its topical action.
Fluoride therapy for the prevention of dental caries is
considered under the two main headings:
1. Systemic fluoridation
2. Topical fluoridation.

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1. Systemic fluoridation:
A. Fluoridation of public water supplies: An optimal level of
fluoride in the water supply provides significant protection against
caries. The optimal concentration depends on the annual average
temperature of the community as temperature influences the
amount of daily water intake.
Temperature ranging between 14.70
C to 17.70
C, the optimal level
of fluoride is 1 part per million (ppm). The adjustment of the
fluoride concentration of public water supplies to 1 ppm is
necessary in low-fluoride areas. Most commonly, fluoride is added
in the form of hexafluorosilicic acid or sodium hexafluorosilicate,
but sodium silicofluoride and sodium fluoride have also been used.
In a warmer climate slightly less than 1 ppm is sufficient.
The effect of fluoride in drinking water persists in between 8 to 18
years of age i.e. during tooth formation and mineralization.

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B. Fluoride supplement: Fluoride supplements like tablet, drops,
lozenges, table salt etc. offer an alternative source of systemic
fluoridation where water fluoridation is not feasible. These
supplements are usually administered continuously on a daily basis
from birth to the pre-eruptive maturation of permanent teeth.
• If fluoride tablets are prescribed they should be chewed rather
than swallowed whole. This will increase the topical benefit of
fluoride.

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2. Topical fluoridation: A lifetime protection against dental caries
results from the continuous use of low-concentration fluoride. In
addition to their use in caries prevention, topical fluorides may be
used to control established caries lesions. This is effective for both
adults and children.
(a) Fluoride tooth paste: The use of fluoride toothpastes has led
to a 25% reduction in the prevalence of caries in industrialized
countries.
Conventional tooth pastes
• Contain approximately 1 mg F / g paste (1000-1100 ppm of
fluoride).
• Added as sodium fluoride such as sodium monofluorophosphate
(MFP) or stannous fluoride.
(b) Fluoride mouth rinses: Studies showed that supervised
fluoride-rinse programs reduce caries by 20-50%. Weekly 0.2%
NaF and daily 0.05% NaF rinses were considered to be ideal public
health measures.

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(c) Fluoride varnishes: Fluoride varnishes were developed to
prolong contact times between fluoride and enamel with a view to
increasing the formation of fluoroapatite. Although fluoride
varnishes firmly bind fluoride in enamel more than other topical
fluoride preparations, the reduction of caries has been of the same
order (approximately 30%).
Example: Duraphat- An alcoholic solution of natural varnishes
containing 50 mg NaF/mL. This varnish remains on the teeth for
up to 12 hours and there is still fixation of fluoride evident up to 48
hours after application.
(d) Concentrated fluoride gels and solutions
APF gels: Acidulated phosphate fluoride (APF) gels, containing
1.23% fluoride are used for professional applications and consist of
a mixture of NaF, HF and orthophosphoric acid. The incorporation
of a water-soluble polymer (i.e. sodium carboxymethyl cellulose)
into aqueous APF produces a viscous solution that improves the
ease of application.
APF gels are mainly used for the prevention of caries
development.

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Dental fluorosis: Dental fluorosis is chronic fluorine poisoning,
sometimes marked by mottling of tooth enamel. It may result from
excessive exposure to fluorides from a wide variety of dietary,
water-borne, and supplemental sources.
There is evidence to show that mild fluorosis will occur with
ingestion of 2 mg or more of fluoride per day.

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Sodium fluoride (NaF)
Preparation-By interaction of 40% HF with an equivalent quantity
of NaOH or Na2CO3.
Stannous fluoride (SnF2)
Preparation- Stannous oxide is dissolved in 40% HF and the
solution is evaporated out of contact with air.
Uses of NaF / SnF2: NaF or SnF2 is used as a dental carries
prophylactic. Ingested fluoride is effective only while teeth are
being formed. The fluoride is incorporated into tooth salts as
fluoroapatite. Topical application results in changes only in the
outer layers of enamel or exposed dentin. It alters the composition
and crystalline structure of the hydroxyapatite-like salts that make
up the bulk of enamel and dentin, so that the tooth material is more
resistant to acidic erosion and dental caries (decay).

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Dentifrices
References:
1. Accepted Dental Therapeutics – 40th
edition
2. Dental Pharmacology- Dr. A.N.M Nazmul Hussain
3. Remington’s Pharmaceutical Sciences (9th
edition – page
1965)
4. Inorganic Medicinal and Pharmaceutical Chemistry-Jhon H.
Block (page 366)

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Dentifrices: Dentifrices are the substances used with a toothbrush
for the removal of bacterial plaque, food debris, stain and calculus
only from the accessible surfaces of the tooth.
Ideal properties of a dentifrice:
1. It should not be harmful to the oral tissue and fluid.
2. If it is ingested it should not be harmful to the G.I.T.
3. It should not stain teeth.
4. It should not be scratching to the enamel surface of tooth.
5. It should have pleasant odour and taste.

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Types of dentifrices
Commercial dentifrices are generally available in two forms:
1. Powder
2. Paste or gel.
Ingredients of powder dentifrices:
• Abrasives
• Foaming agent
• Flavoring agent
Ingredients of paste dentifrices:
• Abrasive
• Foaming agent
• Humectants
• Binders or thickening agents
• Preservatives
• Therapeutic agents
• Flavoring agent
• Sweetening agents
• Coloring agents
• Water

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Abrasives: Abrasives are the solid cleansing materials. It gives
mechanical aids to the dentifrice and helps to remove debris and
stains from the tooth surface. These agents must be nontoxic and
should provide a maximum cleansing action with a minimum of
abrasion to the dental hard tissues.
In general dentifrice abrasives are inorganic salts that are relatively
insoluble. CaCO3 is widely used as abrasive. Other abrasives used
are: insoluble sodium metaphosphate (NaPO3), anhydrous and
hydrous calcium monohydrogen phosphate (CaHPO4 and
CaHPO4.2H2O), calcium pyrophosphate (Ca2P2O7), magnesium
carbonate, hydrated aluminum oxides, silicates or dehydrated silica
gels.

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Foaming agents: Foaming agents flushes and cleanses the cavity.
Consumers prefer to use foaming dentifrices. Synthetic detergents
which not only blend well with other constituents of dentifrice
preparations but also provide optimal foaming capabilities are
incorporated in the dentifrice formulations. Sodium lauryl sulfate
is the most commonly used foaming agent. Other foaming agents
shown to be useful include sodium N-lauryl sarcosinate and
sodium coconut monoglyceride sulfonate.
Humectants: Humectants are incorporated into tooth paste
formulations to prevent loss of water and subsequent hardening of
the preparation upon exposure to air. The most frequently
employed agents include sorbitol, glycerol and propylene glycol.

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Binders: Binders or thickening agents are used to stabilize
dentifrice formulations to prevent separation of the liquid and solid
phases, especially upon storage. Binders increase the viscosity of
the preparation and help to keep it on the brush. The most widely
used thickening agents are the natural gums such as gum
tragacanth and gum karaya, sodium alginate, synthetic celluloses
such as sodium carboxymethylcellulose and methylcellulose.
Preservatives: Preservatives are used to inhibit bacterial
proliferation in the preparation. Aqueous solutions of humectants
support the growth of bacteria and molds and, therefore, a
preservative such as benzoic acid or esters of p-hydroxy benzoic
acid is commonly added to dentifrices containing these agents.

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Therapeutic agents: The majority of dentifrices contain
therapeutic agents such as fluoride salts. Fluoride salts inhibit
caries. Common fluoride salt, which are used in the paste are-
i. Sodium monofluoro phosphate (SMFP)
ii. Monofluoro phosphate (MFP)
iii. Stanous fluoride.
Triclosan: Triclosan (trichloro hydroxydiphenyl ether, C12H7Cl3O2)
is white or off-white, crystalline powder. It has broad-spectrum
antibacterial activity.

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Flavoring agents: For most people, the flavor is an extremely
important factor in choosing a dentifrice. The flavoring agents used
in dentifrices must be compatible with other dentifrice constituents
and yet provide a smooth pleasant flavor both during brushing and
as an aftertaste. Principal flavor ingredients, usually spearmint,
peppermint, wintergreen or cinnamon-mint, are blended with other
essential oils to produce a distinctive flavor.
Sweetening agents: Sweeteners are added to almost all flavors.
The most frequently used synthetic sweetener is saccharin.
Coloring agents: Red, green, chocholate or blue coloring agents
are used.

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Composition of “Crest” tooth paste:
Stanous fluoride 0.4%
Stanous pyrophosphate 1%
Calcium pyrophosphate (Ca2P2O7) 39%
Glycerin 10%
Sorbitol (70% solution) 20%
Water 29.6%
Miscellanous formulating agents

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Composition of “Colgate” tooth paste:
Sodium monofluorophosphate (MFP) 0.76%
Insoluble sodium metaphosphate 41.85%
Anhydrous dicalcium phosphate 5%
Sorbitol 11.9%
Glycerol 9.9%
Sodium N-lauroyl sarcosinate 2%
Water 24.4%
Miscellanous formulating agents 4.2%

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Mouthwash
References:
1. Dental pharmacology- Dr. A.N.M Nazmul Islam
2. Remington’s pharmaceutical sciences (EighteenthEdition-
page 1965)

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Mouthwash is a medicated solution used to cleanse or treat
diseases of the oral mucosa, reduce halitosis (bad breadth), or add
fluoride to the teeth for control or prevention of dental caries.
In dental practice mouthwashes may also be employed as a part of
postoperative treatment, and during the course of certain operative
procedures- when such use adds to the comfort or oral hygiene of
the patient.
Some mouthwashes have a topical anesthetic effect on oral mucosa
and are useful for relieving pain associated with denture sore spots,
herpetic infections and aphthous ulcers. In patients with painful
lesions, these mouthwashes should be used prior to eating to
improve comfort.
Some materials used as mouthwash:
1. Chlorhexidine 2. NaCl 3.Povidone iodine 4. Sodium
fluoride 5. Cetylpyridinium chloride 6. Na borate 7. Hydrogen
peroxide

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Halitosis (bad breadth): Halitosis is a condition in which the
breath smells unpleasant.
The most common cause of bad breath (halitosis) is accumulation
of plaque and food debris on oral hard or soft tissues. Bacteria in
these plaque accumulations produce odoriferous sulfate substances
which contribute significantly to bad breadth. Halitosis may also
be caused by a number of other local and systemic factors.
Until the causative factors are removed, a commercial mouth wash
may be recommended to mask bad breadth. Mouthwashes flush
loose debris from the mouth, provide a pleasant taste and mask bad
breadth for 15 to 30 minutes.
The most commonly studied mouthwashes associated with a
reduction in bad breadth are Listerine (thymol and essential oils),
Cepacol (Cetylpyridinium chloride) and Scope (Cetylpyridinium
chloride and domiphen bromide).