What should we know about

Chlorhexidine

Chalermpong SAENJUM, Ph.D.

Faculty of Pharmacy, Chiang Mai University
November 11, 2016
 Chlorhexidine (digluconate)
=NH+ =NH+
=NH+ =NH+

Chlorhexidine
Chlorhexidine digluconate

Retrived on 19-April-2013 from http://en.wikipedia.org/wiki/Chlorhexidine 2

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 Gram positive bacteria
• Long acting topical antiseptic and
remains active for hours after
application (residual effect more
than alcohol).
• Water soluble form: Chlorhexidine
gluconate
• It strongly adsorbs to bacterial
membranes, causing leakage of Gram negative bacteria
small molecules (low
concentration, 0.2%) and
precipitation of cytoplasmic
proteins (high concentration,
2.0%)
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• Bind to negatively charged bacterial cell wall (phosphate
group), causing osmotic changes and finally destroying the
organism
• Activity against: Gram positive bacteria
Gram negative bacteria
Yeast, Fungi, and Viruses
• Does not become inactivated in the presence of organic
material

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Retrieved on 2013-05-28 from http://www.chlorhexidinefacts.com/mechanism-of-action.html
Solubility of Chlorhexidine and salts in Water
CHX & Salts %w/v at 20 C
CHX base 0.008
Di-acetate 1.90
Di-hydrobromide 0.07
Di-hydrochloride 0.06
Sulphate 0.01
Carbonate 0.02
Gluconate > 70
Digluconate > 70
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Applications of Chlorhexodine (di) Gluconate
Products CHG Concentration
Topical solution 2% or 3.15% with 70%
isopropanol
Scrub solution 2% or 4% aqueous
Washcloth 2% aqueous
Dental solution 0.12%
Gauze dressing 0.5% with paraffin
Catheter dressing 2% gel pad
Hand rub 1% alcohol based with emollients
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 Pharmaceutical Incompatibility (1)

1.Physical
incompatibility

2.Chemical 3.Therapeutic
incompatibility incompatibility

• Visible incompatibility
• Hidden incompatibility 10 10
 Pharmaceutical Incompatibility (2)
Some instance, there is no visible signs
of incompatibility, but the antimicrobial activity may
be significantly reduced

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 1 2 3 4 5 6 7 8 9 10 11
2.0% CHG + NaOCl; 1: 6.0%, 2: 3.0%, 3: 1.5%, 4: 0.75%,
5: 0.38%, 6: 0.19%, 7: 0.094%, 8: 0.047%, & 9: 0.023%
10: 6.0% NaOCl & 11: 2.0% CHG (Control) 12
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 The precipitate is most likely a salt form by the electrostatic
neutralization of the cationic chlorhexidine by the anionic EDTA.
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2.0% CHG + Water 2.0% CHG + NaOCl 2.0% CHG + EDTA

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Effect of Hand Sanitizing Gel/Rub on Antibacterial
Activity of Chlorhexidine (di) Gluconate Solution

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 Purpose of the study (1)
To study the physical and chemical
incompatibilities of chlorhexidine (di) gluconate with
alcohol hand sanitizing gels.

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 Methods
8 samples of alcohol hand Measurement of 2%w/v
sanitizing gel were collected Chlorhexidine gluconate

The reaction mixture compose of 2 mL chlorhexidine

gluconate solution and 1 g alcohol hand sanitizing gel

The amount of chlorhexidine gluconate was measured by

reversed-phase HPLC at 5, 10, 30, & 60 mins of exposure time
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 Results (1): Physical incompatibility

1 2 3 4 5 6 7 8 9 10

1: Control; 2: Sample 1; 3: Sample 2; 4: Sample 3; 5: Sample

4; 6 Sample 5; 7: Sample 6; 8: Sample 7; 9: Sample 8; and
10: Sample 9

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 Results (2): Chemical incompatibility
50

40
5 mins
%Reduction of CHG

30 10 mins
15 mins
20 30 mins
60 mins
10

0
Sample-1 Sample-2 Sample-3 Sample-4 Sample-5 Sample-6 Sample-7 Sample-8
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Effect of Lubricating Gel on Antibacterial Activity
of Chlorhexidine (di) Gluconate Solution

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 Purpose of the study
To study the physical, chemical, and
therapeutic incompatibilities of chlorhexidine (di)
gluconate with lubricating gels.

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 Methods
5 samples of lubricating gel Measurement of 2%w/v
were collected Chlorhexidine gluconate

The reaction mixture compose of 5 mL chlorhexidine

gluconate solution and 1 g lubricating gel

- The amount of chlorhexidine gluconate was measured by

reversed-phase HPLC at 10 mins of mixture time
- Determination for antimicrobial activity
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Results (1): Physical incompatibility

Control Sample-1 Sample-2 Sample-3 Sample-4 Sample-5

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Results (2): Chemical incompatibility

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Results (3): Therapeutic incompatibility

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 Effect of Different Solvents on Antibacterial
Activity of Chlorhexidine (di) Gluconate Solution

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 Purpose of the study
To study the chemical, and therapeutic
incompatibilities of chlorhexidine (di) gluconate in
different solvents.

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 Methods
3 samples of different Measurement of 4%w/v
solvents were collected Chlorhexidine gluconate

The reaction mixture compose of 1 mL chlorhexidine

gluconate solution and 1 mL solvent

- The amount of chlorhexidine gluconate was measured by

reversed-phase HPLC at 0, 1, 2.5, 5, 10, 20, & 30 mins of
mixture time
- Determination for antimicrobial activity 21
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Results (1): Chemical incompatibility

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Results (2): Therapeutic incompatibility

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Results (3): Therapeutic incompatibility

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 Discussion (1)
Chemical incompatibility
Anionic – cationic interaction
(Charge neutralization)

Reduce/loss activity
Inorganic/organic anionic substances

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 Incompatibility of
Discussion (2) CHX

Inorganic/organic anionic substances

- Soaps
- Surface active agents: sodium lauryl sulfate
- Anionic polymers: sodium carboxymethyl
cellulose, alginates
- Pharmaceutical coloring agents
Some instance, there is no visible signs
of incompatibility, but the antimicrobial activity may be
significantly reduced 26
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ขอบคุณครับ

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