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Department of «Industrial pharmacy»

National pharmaceutical university

SEMISOLID DOSAGES
Questions

1. Classification of semisolid drug forms (SSDF)


2. Types of ointments bases
3. Types of instability of emulsive bases
4. Auxiliary substances
5. Technology of SSDF
6. Reactor for preparation of ointment
7. Packing of ointment

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Characteristics

Semisolid dosage forms are traditionally used for treating topical


ailments.
The vast majority of them are meant for skin applications.
They are also used for treating ophthalmic, nasal, buccal, rectal,
and vaginal ailments.
Various categories of drugs such as antibacterials, antifungals,
antivirals, antipruritics, local anesthetics, anti - inflammatories,
analgesics, keratolytics, astringents, and mydriatic agents are
incorporated into these products. Drugs incorporated into semisolids
either show their activity on the surface layers of tissues or penetrate
into internal layers to reach the site of action.

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Classification of SSDF
•on affinity to water: Hydrophobic (lypophilic) and Hydrophilic;
• on ability to absorb water and to the mechanism of absorption;
• on the class of dispersible system:
 homogenous (solutions, alloys),
 biphasic (emulsions of class are oil/water (o/w) and w/o,
suspensions, colloid dispersions)
 and multiphase systems (plural emulsions of o/w/o and w/o/w,
and also the combined systems);
•on reological characteristics at the set temperature of storage and
usage;
• on a concentration and dispersible condition of auxiliary and/or
medicinal substances.

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Classification of semisolides

according to consistence

liniments
ointments gels creams pastes

ointments

homogeneous heterogeneous

alloys solutions combined


suspensions 5
emulsions
Classification of SSDF
• Ointments are semisolid medicinal form for local application, the dispersing
environment of which at the set temperature of storage has a non-
newtonian class of current and high values of reological characteristics.
• Creams are semisolid medicinal form for local application, being bi- or
multiphase disperse systems, the dispersing environment of which at the set
temperature of storage, as a rule, has a newtonian class of current and low
values of reological characteristics.
• Gels are semisolid medicinal form for local application, being mono- bi- or
multiphase disperse systems with a liquid dispersing environment, the flow
characteristics of which are conditioned being of gel-forming substances in
comparatively small concentrations.
• Pastes are semisolid medicinal form for local application, which are
suspensions with more than 20 % of hard dispersible phase, evenly up-
diffused in a base. As a base for pastes can be used bases for ointments,
creams and gels.
• Liniments are semisolid medicinal form for local application, melting at a
bodies temperature. To liniments can be concern ointments, creams, gels
and pastes, characterized this criterion.

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The main requirements to the semi-solid medicines

effectiveness safety
first of all they are defined by active substances

Other requirements to the semi-solid medicines


The release of active substances should be quite well Easy and suitable application

Stability during the hypoallergenicity


shelf-life

Moistening and softening Osmotic activity ensuring skin’s


of skin gas- and
heat exchange

Hermetic packing,
Use of hydrophilic basis, absence of microbiological
Using water-soluble
absorption penetrators contamination, production Exclusion of basis
according to GMP possible
principles allergens

Including wet moisture-


Including osmotic
retaining substances to
activity substances to
the composition
the composition 7
Ointment basis

hydrocarbon absorbtion water-removable water-soluble

vaseline, Can oil-in-water macrogol,


petrolatum, incorporate emulsion poloxamers,
fats, until 50% carbomers,
mineral oil of water: pectin, gelatin,
starch, alginic acid
Na CMC
lanolin,
anhydrous Basis with
lanolin, propylene glycol
lanosterol glycerin

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!!! Ointment = basis + active substances
Requirements to ointment bases
•Ointment basis are the carrier of medicinal substance and provides
volume and necessary physical properties of ointment. The basis
ensuring maximal therapeutical effect should answer the following
requirements:
To have necessary structural - mechanical properties
 To have absorbing ability,
To not change under action of external environment and not react
with medicinal substances, entered into it,
 To not render irritating action on a skin and to promote
preservation of initial meaning of skin or mucous environment рН ,
 To not be exposed microbe contamination.
The properties of a basis should correspond to the purpose of
ointment assignment.
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Auxiliary substances
soft bases (mineral oils, lanolin and other);
Substances increased the melting temperature and
viscosity of bases (paraffin, spermacet, hydrogenated
vegetable oils, beeswaxes, polyethylenglykol with high
molecular mass and other);
Hydrophobic e solvents (mineral and vegetable oils,
isopropylpalmitat, isopropylmiristat, polyalkilsiloksans,
Benzylbenzoath and other);
water and hydrophilic solvents (ethyl and isopropyl
alcohols, polyethylenglykols 200-600, propylenglykols,
propylencarbonate, glycerin, dymeksid and other);

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Auxiliary substances
emulsifying agents of o/w type (sodium laurilsulfate,
emulsifying agent № 1, twin, polyoxyethylenglykol ethers of
higher oily alcohols, cetilpyridin chloride, salts of higher fatty
acids, oxyethylated castor oil, polyoxyethylenglykol ethers of
stearinic acid and other);
 emulsifying agents of w/o type (higher oily alcohols,
cholesterol, spens, glyceryl monooleate, a glyceryl
monostearat and other);
Gel-formers (karbomer, norgine and its salts, derivative
celluloses, polyethylene, poloxamers, polyethulenglkols 1500-
8000, bentonite, kaolin, colloid silex, Arabic gum, tragacanth,
gelatin and other);

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Auxiliary substances

•antimicrobial preservatives (benzalkon chloride, miramistin,


cetrimid, cetilpiridiniya chloride, chlorhexidine, benzoynic and sorbic
acids and their salts, parabens, an benzil alcohol, krezol, chlorkrezol,
propylenglycol, ethyl alcohol and other);
• antioxidants ( α-tokoferol, ascorbic acid and its derivates, tetrine
and its salts, lemon acid, propylgallat, sodium metabisulfite and other);
• solyubilazers (β-cyklodekstrin, hydrophobic surface active
agents and other);
 smell improvers (Menthol, essential oils, and other);
• рН regulators (lemon acid, phosphorusacids salts of sodium and
other).

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Technological process of ointment production:
3

1
4 4

1. Preparation of active substances 2

2. Preparation of ointment basis


3. Introduction active substances into ointment basis
4. Homogenization
5. Standardization
6. Packing and marking

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Reactor-gomogenisator

3 types of mixers:

plate-and-frame,
turbine,
paddle

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Preparation of ointment

•. Blade and frame mixers are revolved to meet to each


other. Effective horizontal and vertical interfusion is
provided with a moving action.
•The form of blades of blade mixer provides direction of
product downward to the center of turbine mixer.
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Types of high-speed turbine
mixer
universal emulsifier
emulsifier

dispersor (intended for


interfusion of product with
powder)
dispersor- homogenizer
(at treatment of product of
type of paste)
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Transfer

Discharge of intermediate
products (ointment, liniment, gel,
suppozitory mass) is carried out
under the pressure of filtered
compressed air or nitrogen into
the hermetically closed movable
capacities made from alloy
stainless steel, so-called “muller’s
barrels", of different capacity.

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Homogenization

Chart of rotor-pulsation vehicle.


Colloid mill 1 – rotor; 2 – stator; 3 – corps;
4 – spinner; 5, 6 – inlet and outlet pipe

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Packing of ointment

Screw machine
•Bunker with ointment (1),
screw (2), faucet for ointment
feeding (3) jet (4).
A faucet is closed at stated
intervals, and ointment from a jet
is pushed in a jar or tube. Packing
is carried out at times closing and
openings of faucet. Jars with the
packed up ointment close by caps.

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Packing of ointment

Packing of ointment into


tubes is carried out on automatic
tubefilling machines. Sequence
of operations:
•orientation of tube on a label;
•filling with of tube by
ointment;
•folding of tube;
•printing of series, storage
term.
1- bunker, 2 – pipelines, 3 – jet, 4 - tubes

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Line for filling and packing of
tubes

1 – unit for feeding of empty tubes; 2 – tubefilling machine; 3 –


cartoning machine; 4 – boxing machine; 5 – film overwrapping machine

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Quality control:

1. organoleptic property

2. Identification

3. Homogeneity

4. рН

5. microbial cleanness

6. quantitation

7. hermetic of tube
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Thank you
for your attention!

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