57) Abstract:

Suppositories with glycerin is used as a laxative for constipation of various

etiologies. Glycerin is distilled pre-mixed with polyethylene oxide of molecular
weight 400 to obtain 86% glycerin solution. In glycerol solution spend the
interaction of sodium carbonate and stearic acid when heated. Glyceric weight
stand. Then formed into suppositories at 68-75oC. a New method to produce
suppositories with glycerin has improved their quality, appearance, to increase
the use of packaging material, in particular livinallongo film, and to make the
soup of positories on automatic lines "Sarong" and "Colindex".

The invention relates to the pharmaceutical industry and for the manufacture of
a medicinal product, namely with suppositories glycerin, used as a laxative for
constipation of various etiologies: functional (the usual), psychogenic, aged,
sedentary patients, associated with a decrease in the sensitivity of the receptor
apparatus of the rectum.

A method of obtaining suppositories with glial bath to 15-120oC. Add sodium

stearate and the mixture is well stirred, maintaining the specified temperature
to melt the sodium stearate.

Then add distilled water, mixed well and the hot mixture is poured into the form
and leave until cool. When using a metal mold, it is heated to 80-90oC and the
hot mixture is poured. After this form is cooled, candles extract and pack.

Used sodium stearate in this way receive a separate technology.

Suppositories with glycerin obtained in a known manner to have a good texture

and form, they are also quite satisfactory and pharmacological side.
Although suppositories obtained by the method described in the article Hohner-
Mechaninc, good quality, its use in an industrial environment is technologically
difficult to implement. Therefore, the known method can be used primarily for
small test batches.

Also known is a method of obtaining with glycerin suppositories comprising the

reaction of interaction of sodium uglekislogo crystal with stearic acid in the
environment 86% glycerol [2].

Yes the result.

Way to get with glycerin suppositories consists of the following stages.

In a reactor loaded distilled glycerol density above 1,223 and there serves
distilled water to obtain 86% glycerol. The contents of the reactor are stirred
and a solution of glycerol 86% served in the reactor preparation suppozitornoj
mass.

The process is conducted in a reactor equipped with a jacket with steam

heating, anchor stirrer and outlet pipe for removing carbon dioxide. The
glycerin solution in the reactor is heated up to 90-94oC and it loads sodium
carbonate crystal. After loading the contents of the reactor is stirred until the
salt is completely dissolved in glycerine. Then the temperature of the solution
increased to 94-98oC and portions gradually charged to the reactor stearic
acid. At the same time provide the output of carbon dioxide from the reactor.

The reaction of interaction of sodium carbonate with stearic acid is heat, so the
temperature in the reactor automatically support within 94-110oC.

Once downloaded, stearic acid mass is stirred and stand up to full subsidence
foam: 2.5 to 4 h in the manufacture of Melk the RNA mass transfer at the
formation stage of suppositories. In the process of forming support temperature
mass within 95-105oC. Molded candles immediately Packed in
poliatilenzellofana film (PC-2).

However, in the known method temperature (94-100oC) at the stage of

formation of suppositories allows the use of mainly one type of packaging
material, namely, poliatilenzellofana film.

Conducted a study on the use of other packaging materials showed that the high
temperature at the stage of formation of suppositories does not allow their
packaging, in particular, polyvinyl chloride film (PVC). At this temperature, is
full of its deformation.

In addition, due to the fact that suppositories with glycerin possess strong
hygroscopicity, water that is used for pre-dilution of glycerol leads to a
deterioration in their quality and appearance. When storing suppositories is the
dilution of the surface layer, making it difficult to release them from the
packaging material and the introduction to recto.

The technical result that can be obtained by carrying out the present invention,
is expressed in the expansion, and all other types of candles in our country, and
abroad, and improve the quality of the final product.

To obtain this technical result in the method of producing suppositories with

glycerin, including the interaction of sodium carbonate and stearic acid in 86%
solution of glycerol distilled by heating with subsequent maturation glycerol
mass and formation, according to the invention glycerin mixed with
polyethylene oxide of molecular weight 400 to obtain 86% glycerin solution,
and the formation of suppositories is carried out at 68-75oC.

Use glycerin distilled according to GOST 68-24-76 (dynamite, the highest or

first grade).
The polyethylene oxide - 400 (FS 42-1242-79), posted by Pharmacological
Committee for medical use as an integral part of the bases for suppositories
(Protocol No. 6 of 10.04.64 and letter of FC for N 211-15-1787 from 30.07.93).

Preliminary mixture of glycerol and polyethylene oxide - 400 to obtain the 86%
solution helped to reduce temperature suppozitornoj mass at the stage of
formation of the candles before 68-75oC. With this comes the ability to make
the packaging of suppositories with glycerin in polivinilhloridnyi film brand EP
is valila significantly improve the quality of the final product. Suppositories
with glycerin, obtained by the claimed method, have a good consistency,
without light surface, a hundred and improves their appearance and creates
convenience in their introduction to recto.

The selected temperature range, the formation stage within 68-75oC is optimal
and the deviation from it results in poor quality of suppositories.

The results showed that when the temperature drops below 68oC glycerol mass
solidifies above the 75oC mass yellower, and the PVC film in the formation of
deformed and lose their properties.

A comparison of the proposed technical solutions with the characteristics of the

prototype allowed us to establish compliance with a criterion of "novelty".
Analysis of the known technical solutions in this area showed that the
polyethylene oxide - 400 permitted Pharmacological Committee as a
component of the basis (together with the polyethylene oxide - 1500) for the
manufacture of suppositories, as Anestesiol", candles with diprophylline or
candles with theophylline.

However, in the known processes for the manufacture of suppositories

polyethyleneoxide - 400 is one of the main parts of the hydrophilic base and
soobshchenie polyethyleneoxide - 400 performs the role of glycerol diluent and
at the same time enhances the laxative action.
As a result of the research it was found that the use of polyethylene oxide - 400
dilution of glycerol to 86%, with no impact on the course and the course of the
chemical reaction between the crystalline sodium carbonate with stearic acid.
The process occurs at the same temperature and in the same sequence as in the
prototype.

The required amount of polyethylene oxide - 400 calculated by the formula:

X=A-A/B86%,

where X is the number of polyethylene oxide - 400;

A number of 86% glycerol;

B - concentration source glycerin;

86% - the optimal concentration of glycerol in the solution.

The method of producing suppositories with glycerol as follows.

The quantity of raw materials is calculated from the composition for 1 candle.

Part 1 candle, g: - Children

Glycerin - 1,32
Stearic acid - 0,12

Sodium carbonate crystal - 0,06

The polyethylene oxide - 400 - 0,12

Part 1 candle, Mr. Adult

Glycerin - 2,95

Stearic acid - 0,205

The sodium in the SS="ptx2">

The process is conducted in a reactor equipped with a jacket with steam

heating, anchor stirrer and outlet pipe for removing carbon dioxide.

In the reactor mix glycerine distilled premium grade with a density above 1,223
with polyethylene oxide - 400 with anchor stirrer within 10-15 minutes the
Mixture is heated up to 90-94oC and injected sodium carbonate crystal. After
loading the contents of the reactor is stirred until the salt is completely
dissolved. Then bring the temperature up 94-98oC and injected into several
stages stearic acid. Each subsequent dose is administered after the subsidence
of the foam from the previous one. At the same time provide the output of
carbon dioxide from the reactor. Once downloaded, stearic acid mass is stirred
for 40-60 min and stand for 3-6 h at 94-100oC without stirring.

The end of the reaction myeloablative determine the full settling of the foam and
the transparency or translucency of drops of mass during freezing.
Suppozitornyj mass is cooled to 68-75oC and poured at this temperature in
blister packaging made of PVC film marks EP-73C. Suppositories is formed
into two dosages: weighing not more than 1.65 g and not more than 2,88,

Thus, studies have shown that a new method to produce suppositories with
glycerin has the following techno-economic advantages:

Replacement of distilled water on polyethylene oxide - 400 at the stage of

dilution of glycerol distilled allowed:

1. To improve the quality of suppositories in comparison with the previously

produced the prototype. They have a good consistency, without spotting the
surface, which improves their appearance and creates a comfortable
introduction to recto.

2. To carry out their production on automatic lines "Sarong" and "Colindex" in

blister packaging made of PVC film marks EP-73C.

Currently received resolution Pharmacological state Committee on the issue

with glycerin suppositories by the present method.

Way to get with glycerin suppositories, including the interaction of sodium

carbonate and stearic acid in 86% solution of glycerol distilled by heating with
subsequent veterinarium mol. m 400 with getting 86% glycerin solution, and
forming suppositories carried out at 68 75oC.
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