USE OF DIMETICONE FOR TREATING CONSTIPATION

UTILISATION DU DIMETICONE DANS LE TRAITEMENT DE LA CONSTIPATION

English Abstract

The invention disclosed relates to the use of dimeticone as an agent for treating constipation.

French Abstract

L'invention se rapporte à l'utilisation du diméticone comme agent de traitement de la constipation.

Claims

6
Claims:
1. ~Use of dimethylpolysiloxane as the active ingredient
for the preparation of a pharmaceutical composition for
treating constipation.
2. ~The use according to claim 1 wherein the
dimethylpolysiloxane is used in combination with a
dispersed silicon dioxide.
3. ~The use according to claim 1 or 2 wherein the
dimethylpolysiloxane is used in combination with a
biologically acceptable fat emulsifier.
4. ~The use according to claim 3, wherein the emulsifier
is glycerine stearate.
5. ~The use according to any one of claims 1 to 4 for
treating constipation in a child, immobile or geriatric
patient, or a pregnant woman.
6. ~A pharmaceutical composition for the treatment of
constipation comprising dimethylpolysiloxane as the active
ingredient in admixture with a pharmaceutically acceptable
carrier or diluent.

Description

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1
Use of Dimeticone for Treating Constipation
The invention relates to the use of dimet.icone for treating
constipation.
Constipation means a delay in the discharge of dry and hard
feces. It is caused either by a delayed passage of the
stomach contents through the intestine or' a disorder of the
evacuation reflex. Possible reasons for the delayed
passage through the intestine are dietetic factors, changes
in the intestinal walls or a functional or organic disorder
of the nervous system. Also, pharmaceuticals may have a
constipating effect. A defect in the defecation mechanism
is found in disorders of the anal channE=_l, in the case of
loss of the rectal dilation reflex or a weakness in the
abdominal muscles used to apply abdominal pressure.
Patients complain about symptoms such as a sensation of
pressure, flatulence and pains during the discharge of
feces.
Constipation is treated with laxatives which on the one
hand soften the hard feces and on the other hand prompt
defecation.

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2
Laxatives either act as lubricants, fillers or swelling
agents, have saline or csmotic properties, or produce an
anti-absorptive or secretagogue effect. The substances of
the afore-mentioned groups are combined in commercial
preparations in many ways.
When used in long-term therapy, almost all laxatives, except
for the swelling agents, increasingly cause disorders of the
electrolyte metabolism and in particular cause a potassium
loss, which in turn increases constipation. The sodium loss
can be so high as to cause a secondary hyperaldesteronism.
The potassium losses so caused may lead to a reduced
intestine motility and may increase constipation. Moreover,
hypokalaemias are above all dangerous when used in therapy
together with cardiac glycosides. Concomitant calcium losses
can promote the occurrence of osteoporosis, especially in
women.
The administration of a swelling agent involves the danger
that the stomach contents might stick together, from which
the danger of an ileus ensues.
Moreover, many laxatives are resorbed, with the result that
they can have a large number of systemic side effects.
Hence, there has been a need for an effective agent far
treating constipation which does not produce the afore-
mentioned side effects and consequently lends itself for use
in problem patients, for instance children, immobile or
geriatric patients and women, in particular during
pregnancy.
According to the invention, dimethylpolysiioxane
(dimeticone) was found to be effective in the treatment of
constipation, without producing the usual side effects.

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PCT/EP94/04024 ~ ~' ~ ~ ~ ~~ V~~S~US & PARTNER
-~HMIDT, Alfred et al. . PATENTANYIIALTc
~r Ref. : H 839 PCT 51SBE~tTSTR. a
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Commercial dimeticone-containing prepazations are used to
treat indications such as flatulence, sensation of repletion
(bloating) and meteorism. Moreover, the use of dimeticone
for heating inflammatory and ulcerous diseases of the
esophagus, the stomach and the duodenum has been described.
In FR-5.549M, Therapiewoche 1975, Nr. 25, pp. 1509-1512,
Med. J. Aust. Vol. 150, No. 11, 1989, p. 667, J. Indiana
Med. Ass. Vol. 66, No. 12, 1973, pp. 1083-1084, DE-A-38 07
712 and Radiologie VoI. 30, No. 1, 1990 various compositions
or therapeutic regimens for the treatment of constipation
are disclosed which comprise in addition to a conventional
laxative component either dimaticvne or simethicone based on
their deflatulent properties.
Dimethylpolysiloxane may be administered to a human or
animal in the form of tablets, capsules, emulsions,
suspensions and powders for oral administration or in
combination with foodstuffs and dietary supplements. Such
compositions may be administered to humans and animals in a
safe and effective amount to elicit the desired result. The
compositions used for this invention typically comprise an
affective amount of dimethylpolysiloxane and a biologically
acceptable carrier. Such carriers may be solid or liquid,
such as, for example, highly dispersed silicon dioxide,
cornstarch, lactose, sacchaross, glucose, sucrose, water,
water and fat emulsions such as glycerin stearate emulsions
and flavoring agents. If a solid carrier is used, the dosage
forms may ba tablets, capsules or lozenges. Liquid dosage
forms include soft gelatine capsules, syrup or Iiguid
suspension. The dimsticone-containing compositions may ba
employed according to this invention in a conventional
manner for the tramtment and prevention of constipation.
Their dosage levels may be chosen by those of ordinary skill
in the art from the available methods and techniques.
Specific dosage and treatment ragim~ns will depend. upon
factors such as health status and the severity and course of
constipation and disposition thereto.
In order that this imrention be more fully understood, the
following example is set forth. Thi example is for the
:y
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purpose of illustration only, and is not to be construed as
limiting the scope of the invention in any way.
Example
Preparation of treatment composition
2 kg of dimethylpolysiloxane containing approximately 60 g
of highly dispersed silicon dioxide was heated in a water
bath to about 70'C. 1 kg of solid, finely triturated
glycerin stearate (a mixture of mono- and diglycerin
stearate) was then added thereto and the mixture was left in
the water bath until the entire mass had melted. The mixture
was then stirred to form an emulsion to which 3 liters of
Water were slowly added at a temperature of about 70'C.
After further stirring and gradual cooling, a stable aqueous
emulsion formed which had a stiff, lard-like composition at
room temperature. This composition could now be finely
dosed, admixed with an inert tabletting mass consisting of
saccharose, glucose, lactose and flavoring agents, and made
into tablets. It is also possible to dilute the resulting
mass with water to prepare a liquid preparation for
administration as drops.
Application of treatment composition
sex: female
age: 2 years
diagnosis: constipation
additional symptoms: tibia fracture (left side)
resulting in a bed-ridden
condition
duration of constipation: three days
concomitant symptoms: non-specific symptomatic pains
therapy: one teaspoon of the dimeticone
suspension
result: complete evacuation of the feces
(bowels) after two hours

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a
As the patient was required to remain immobilized, the
situation after three further days was the same as before
treatment. Again, about 40 drops (one teaspoon) of the
dimeticone suspension was administered. after the suspension
was allowed to act for 2 hours, it produced a complete
evacuation of the bowels.
While we have described an embodiment of this invention, it
is apparent that our embodiment may be altered to provide
other embodiments which utilize the method of this
invention. Therefore, it will be appreciated that the scope
of this invention is to be defined by the appended claims,
rather than by the specific embodiment which has been
presented by way of example.