Department of «Industrial pharmacy»

National pharmaceutical university

Industrial technology of rektal

medicinal forms
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Questions
• Determination. Classification. Properties.
• Description of bases and auxiliary matters.
• Methods of suppositories obtaining .
• Technological equipment for the production of
suppositories.
• Quality control of suppositories, their packing and terms of
storage.
• Basic directions of improvement of suppositories
medications.

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 Determination. Classification.
Properties.
Medications for rektal application are intended for introduction
to the rectum with the purpose of receipt of system or local
action.

Classification
• Rektal suppositories
• Rektal capsules
• Rektal solutions and suspensions
• Powders and tablets for preparation of rektal solutions or
suspensions
• Semisolids for rektal application
• Rektal suds
• Rektal tampons

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 The positive characteristics of a rectal way of
medicinal forms introduction into human body
• Increased speed of their suction (approximately equal to speed of
intraskin, underskin, intramuscular introduction of medicines) and
expressed organism pharmacological reaction on medicines with
strong physiological action give a possibility to use rectal medicine for
rendering of first aid;
• Gastric enzymes does not have an action on active substances;
• Opportunity of assignment of substances with unpleasant taste and
aggressive concerning to a stomach mucous covers;
• Sufficient reduction of an allergic reactions level, reduction or complete
absence of side effects;
• High efficiency of rectal preparations in treatment of the infants and
elderly patient;
• The opportunity of rectal medicines use in case of a nausea,
infringement in swelling process, liver diseases.
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 Suppositories
• Suppositories are solid at room temperature and
melting or dissolving at body temperature
dosage medicinal form for entering into a body
cavity. Distinguish rectal suppositories, vaginal
and stick.
• Rectal suppositories can have the form of a
cone, cylinder with the pointed end or other form
with the maximal diameter 1,5 sm.
• Weight of one suppository should be in limits
from 1 till 4. Weight of one suppository for
children should be from 0,5 up to 1,5 g.
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 Classification of suppositories
bases and requirement to them
• More than a hundred substances of a natural and
synthetic origin used as suppositories bases are known
today.
Requirements to bases:
• Melting temperature or dissolution should be close to
temperature of a human body;
• The basis should not irritate a mucous straight line
intestine or cause other undesirable actions, i.e. it should
be physiologically inert;
• The basis should not interfere to releasing and
therapeutical action of medicinal substance;
• The basis should not cooperate with medicinal
substances entered into suppositories mass.

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 Technological requirements to
bases
• Chemical and physical stability during
suppositories manufacturing and storage;
• The ability of easy formation and keeping
necessary hardness during the introduction;
• Ability to emulsify necessary amount of
solutions;
• To have the certain plasticity, viscosity, time of
deformation, i.e. certain structural - mechanical
properties.

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 Production of potable water
There are no prescribed methods for the treatment of raw
water to produce potable water from a specific raw water
source.
Typical processes employed at a user plant or by a water
supply authority include:
• filtration;
• softening;
• disinfection or sanitization (e.g. by sodium hypochlorite
(chlorine) injection);
• iron removal;
• precipitation;  and
• specific inorganic/organic reduction.

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 Classifications of bases
By physical and chemical features

lipophylic emulsion water soluble

By origin

natural products of synthetic (PEO)

(oil, fats, processing
waxes (collagen,
hydrogenise
fats,
gelatineglycer
ine mass)

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 Classifications of bases
By ratio of solubility in water

water-soluble basis insoluble in water basis

(hydrophilic) PEO, gelatin-
glycerin, collagen carbovax
(USA), skurol (France),
postonal, suppopharm
(Germany)
(lipophilic) fats, their alloys,
products of fats processing,
vitepsol, estranium, lasupol

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 Preparation of suppositories
• Suppositories are made by the following
methods:
 by pouring out of mass in the forms;
 by rolling out;
 by pressing on the special equipment.

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 Method of pouring out
• Preparation of a basis The components are weighted out, and
then alloyed together in reactor with steam jacket and mixer at
temperature 60-70C. The base is filtered through druck-filter.
• Preparation of medicinal substances and reception of a
concentrate Water-soluble components are dissolved in heated
at 45 C water, fat-soluble – in melted fat base. Received
concentrates are filtrated through filter, and then are mixed with
the rest of base. Insoluble in water and base components enter
as a suspension.

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 Method of pouring out
• Introduction of medicinal substances
into a basis Ready concentrate enter into
the reactor for mixing with the base.
Operation of suppositories mass preparing
is going with mixing and heating to the 45-
50C. And after positive results of quality
analyses (uniformity of mix, cooling and
melting temperature, time of complete
deformation) suppositories are pouring
out.
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 Method of pouring out
• Suppositories forming
(pouring out) For
suppositories forming use
different automatic and
semiautomatic devices, the
most widespread of them are
“Sarong 200 S”, “Farmo Dui
FD 22/U”, “Franco-Krepsi”.
After forming suppositories
are sorting on appearance.
Suppositories are dried at
temperature 10-15С within 2-
3 hours with additional
airflow for removal of cooling
and greasing components.
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 Method of pressing
•By method of pressing on eccentric tablet machines with
punch cooling, the matrixes and casing can be received from
40 up to 100 thousand of suppositories at one hour.
Suppository mass usually cool in the refrigerating chamber up
to 3-5С, grind and sift. Into a granulate structure enter
lactose, sucrose, aerosol, starch for updating certain
technological properties.
•The advantage of this method consists in an opportunity of
prevention of thermolabel medicinal substances destruction,
absence of active substance sedimentation and prevention of
its possible incompatibility with melted suppositories basis.

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Quality control of suppositories

• form and weight uniformity,

• hardness,
• quantitative content and dosage uniformity
of active substances.
• For suppositories prepared on lipophilic
bases melting temperature is determinate.
• For suppositories prepared on hydrophilic
bases dissolving time is determinate

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 Development of rectal medicinal
forms
• One of the perspective medicinal forms is a rectal capsule. They
represent capacities from gelatinous film in the form of suppository,
filled by an expendable doze of medicinal substance as liniment,
ointment, emulsion or solution.
• It is known the application of rectal tampons which are represented
by the plastic core which has been wrapped up by cotton wool with
adsorbed on it medicinal substances. Wadded tampon is covered
with a thin layer of alginate. Before the use tampon on some time
immerse in water, due to what the cover from alginate swell and
does not interfere to medicinal substance diffusion process.
Tampons enter into a straight line intestines at 2 hours. Apply
mainly to treatment hemorrhoid.

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 Development of rectal medicinal
forms
• Now receive wide application foam forming preparations in aerosol
packing. The foams favorably differ from other medicinal forms used
in proctology. The ointments and creams will not penetrate in
mucous and into deeper zones intestines. Suppositories do not
provide treatment of sites of anal channel, is characteristic for them
more short-term therapeutical effect in comparison with foams.
• It is known, that from water solutions entered in a direct intestines in
the form of enema, the medicinal substances are soaked up very
quickly. However part of a solution is poured out outside. In such
cases medicinal solution it is more convenient to enter with the help
of rectal dropper - rectioles which consist from elastic vessel with a
tip. Vessel is executed as the goffered container of capacity 1,5 - 5
ml. The tip is rigidly attached to it and is executed from polythene.
Use for rectioles filling oleogels, liniments, and ointments opens
ample opportunities of expansion of assortment proctological
medicinal forms.

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 Thank you
for your attention!

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