Ideal ointment base
Factors affecting the selection of an ideal ointment base
A- dermatological factors
B-
Pharmaceutical factors
A-dermatological factors
A-dermatological factors
1- Absorption and penetration
Absorption: entry in the blood stream
i.e systemic absorption
Penetration: transfer through the skin
The problems of absorption and
penetration are:
a- only oint. Base penetrate deep into
the skin
b- mainly medicament absorbed into blood
stream
c-
paraffins don't penetrate the skin
Animal and vegetable fats and oils normally penetrate the skin
Animal and vegetable fats and oils normally penetrate the skin
d- substances which are soluble in both
oil and water are readily absorbed
e- water soluble drugs are absorbed from water soluble bases
e- water soluble drugs are absorbed from water soluble bases
f-
o/w emulsion release the medicament more readily than the greasy w/o
2- Effect on skin function
2- Effect on skin function
Greasy bases interfere with skin
function such as heat radiation and sweat. o/w emulsion and other water
miscible bases produce cooling effect rather than heating effect and readily
mixed with skin secretions
3- Miscibility with skin secretion
Bases miscible with skin secretion
rapid release of the medicament
4- Compatibility with skin secretion
Used
bases should have pH about 5.5 because this the normal pH of the skin
5- Free from irritant effect
5- Free from irritant effect
Used bases should be non irritant and of
high standard purity specially for eye ointments
6- Emollient properties
Ointments should keep the skin moisture
7- Ease of application and removal
The
applied ointments should be easily applied as well as removed from the skin.
Emulsion bases are more preferable as they are softer and spread more readily
over the skin. They can be easily removed by simple washing with water
B-Pharmaceutical factors
B-Pharmaceutical factors
1- Stability
To increase the stability antioxidant
and antiseptic should be added according to the need depending upon the
constituent of the preparation.
2- Solvent properties
Insoluble
medicaments should be finely powdered and distributed uniformly inside the base
using small portion of oils.
3- Emulsifying properties
3- Emulsifying properties
Depends upon the amount of water that
must be added to the formulation.
4- Consistency
the
consistency can be adjusted by using suitable proportion of high melting
substances and low melting point substances
Preparation of ointments
Preparation of ointments
By either trituration or fusion
1- Trituration method
The most common method used for
preparation of ointments. The medicament is finely powdered and triturated with
small amount of the base till homogenous dispersion is obtained. Then followed
by addition of the remaining base with good mixing
2- Fusion method
It
is used when the ointment contains a number of solid ingredients such as bees
wax, cetyl alcohol….etc
In this case it is necessary to melt these ingredients. The melting of ingredient take place in decreasing order of melting points. The medicament is then added to the melted ingredients and stirred thoroughly until cooling and formation of homogenous product.
In this case it is necessary to melt these ingredients. The melting of ingredient take place in decreasing order of melting points. The medicament is then added to the melted ingredients and stirred thoroughly until cooling and formation of homogenous product.
Liquid
should be heated to nearly the same temperature of the melted base before
adding it the melted bases.
Other additive in ointments
Other additive in ointments
Preservatives, antioxidants, perfumes
and chelating agents may be incorporated in the ointment.
The commonly used preservatives are :
1) Phenolics: phenol (0.2-0.5%) ,
chlorocresol ( 0.075- 0.12%) .
2) Methyl parapen (0.02-0.03%), propyl
parapen (0.02-0.3%).
3) Benzyl alcohol (< or = 3%).
preservatives prevent the bacterial
growth when ointments stored for long time.
Antioxidants prevent the oxidation
decomposition of the ingredients such as:
a) Lipophilic antioxidants: e.g., BHA
& BHT
b) Hydrophilic antioxidants (dissolved
in aqueous phase) such as sodium metabisulfite or sodium Sulfite.
Humectants such as glycerin and
propylene glycol and sorbitol may be added to prevent the loss of moisture.
Pigments such as iron oxide may be added
to give ointments a cosmetic like appearance specially in formulation intended
for application to the face.
Perfumes
may be also incorporated to give ointment a pleasant odour.
Packaging and storage of ointments
Packaging and storage of ointments
Packaging
Ointment jar and collapsible tubes of
different sizes, shapes and capacities are used for storage of ointments. Amber
glass containers are used for light sensitive preparations.
Storage
Ointments must be stored at an optimum
temperature otherwise separation of phases may take place which is very
difficult to remix to get uniform product