DE2943031A1 - THIOL DERIVATIVE FOR CELLULITIS TREATMENT - Google Patents

Description

PATENT LAWYERS 29 ^ 3031

DR.- ING. H. H. WILHELM - D I PL. - IHMG. H. DAUSTER D-7000 STUTTGART 1 - GYMNASIUMSTRASSE 31B - TELEPHONE (0711) 291133

Applicant: Stuttgart, October 23, 1979

P5786 / 7a

PROTEK S.p.A. Dr. W / S

38, Via Lambro

I-Opera (Milan)

Thiol derivative for the treatment of cellulite

The invention relates to a thiol derivative useful for treating, i.e. eliminating or reducing, cellulite.

As is well known, the term cellulite is commonly used denotes that abnormal subcutaneous layer which has the typical aspect of orange peel and which is the result of an agglomeration of hypertrophic adipocytes arises within the polymeric structure of acidic, hydrophilic glycoproteins.

The formation of cellulite arises from both an aesthetic and a therapeutic point of view the problem of eliminating or at least substantially reducing this cellulite. Always stronger and forever broader groups of people feel the need to find a solution to this problem.

The conventional and most widely used cellulite reduction treatment is based on a mechanical localized action (Massage); parallel to this treatment, which is known to be carried out by qualified personnel for a longer period of time is to be carried out, special diets are generally to be followed and constant gymnastics exercises to be carried out.

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It is also known that the "effort" and the economic The burden that such treatment entails on the patient very often tempted to interrupt the treatment after the first reduction results, despite these results are not entirely satisfactory and although such an interruption practically and quickly wipes out the results obtained.

Other cellulite treatments were suggested, such as a treatment based on ultrasound or special enzymes; these suggestions have (but not to any widespread The reason for this application is that such treatments require the use of highly qualified personnel and / or complex ones and equipment that is not easy to use is required, as well as because it does not give completely satisfactory results be achieved.

The invention is based on the object of an anti-cellulite To provide highly effective interconnection that is affordable and incorporated into suitable forms of transportation can be so that a direct application by the patient is possible.

These and other tasks, which are explained in more detail in the following description, are achieved by a connection, which is intended for the treatment of cellulite and is essentially in accordance with the present invention - from a thiol derivative with the following formula:

K *

R-CH-NH-CO-CH

COOH \

R "

where M is hydrogen, as well as alkali metal or alkaline earth metal atoms is,

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- R is H or -CH ₂ SH

- R ¹ is H or -SH

- R "is H, -CH ₃ or -C ₂ H ₅ ;

if R ¹ is also -SH, R must be hydrogen and R "must be -CH _{1, -C 2} H ₅ and if R is -CH ₂ SH, R ¹ must be hydrogen and R" must be hydrogen or -CH ; ,, or -C ₂ Hj- be.

The thiol derivatives corresponding to the above formula wherein M, R, R * and R "occupy the meanings listed above, have shown that si ^e possess a substantial antizellulitische effect. Namely, when a local application or administration of appropriate with thiol derivatives equipped If preparations are made in a different way (e.g. by rectal or oral route, by means of local infiltration, etc.), there is always a clear softening of the subcutaneous cellulite nodules, as well as their reduction or elimination, while the cutaneous and subcutaneous tissue retains its elasticity and suppleness This rapid and striking effect is essentially due to the ability of the thiol derivatives corresponding to the above formula to depolymerize the acidic, hydrophilic glycoproteins; in this way the adipocytes described above, which are within the polymeric chain of the glycoproteins mentioned have accumulated, released. As a result, these adipocytes are quickly absorbed and eliminated.

The anti-cellulite effect reaches its maximum value when the thiol derivative used as such or as a component a suitable form of transport from a 2-thiol-propionamide-acetic acid or of one of their salts, in particular of their sodium salt. This acid has the formula:

SH

H-CH-NH-CO-CH
COOH

CH,

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Another significant advantage is that the thiol derivatives mentioned are easily and economically available for local use intended carrier substances, e.g. in ointments, creams, lotions and the like can be incorporated or that they can be incorporated rectally (suppositories), by means of local infiltration (sterile solutions) or by the oral route, e.g. in the form of tablets, capsules. Granules, syrups, etc. can be administered. This results in the possibility that the patient can carry out an effective and economical cellulite treatment directly. Next some non-limiting exemplary embodiments of carrier substances are listed which are incorporated by the present invention Contain provided thiol derivative, in particular the 2-thiol-propionamide-acetic acid or one of their salts which have been found to be useful in the treatment of cellulite.

example 1

There are 6g of 2-thiol-propionamide-acetic acid in about 20 ml of WassBr dissolved and heated to approx. 5> O C; the pH is increased by adding of alkaline solutions (e.g. sodium or potassium hydroxide) checked for neutrality. The resulting solution then becomes 74-g added melted lanolin. This gives an ointment that is massaged into the areas to be treated for a long time will. Active ingredient dose 200-300 mg per treatment. Duration of treatment: 6-8 weeks.

Example 2

There are 6 g of 2-thiol-propionamide-acetic acid in the form of sodium salt dissolved in 200 ml of distilled, sterile, pyrogen-free water.

The resulting solution is filtered and put into ampoules with predetermined Capacity, which are sterilized in the autoclave, filled.

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The ampoules are used for local subcutaneous infiltrations several syringes in. the active ingredient dose of 100-2 30 mg per treatment used.

Example 3

There are 10 g of 2-thiol-propionamide-acetic acid in about 4 ml of water mixed, and sodium carbonate is added to pH 5-6.

The solution is heated to approx. 40 C and in a suppository suitable molten mass (consisting e.g. of glycerine esters with saturated vegetable fatty acids) is introduced.

The hate that contains the active ingredient is used to manufacture Divided suppositories with a predetermined capacity. The suppositories are dosed with active ingredient, the content of which is between 50 and 500 mg can vary; the treatment dose is 1-2 suppositories at 250 mg per day for 15-30 days.

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Claims (3)

PATENTANWÄLTE 29 A 30 DR.-ING. H. H. WILHELM - DIFL.-ING. H. DAUSTER D-7000 STUTTGART 1 - GYMNASIUMSTRASSE 31B - TELEPHONE (0711) 291133 Applicant: Stuttgart, October 23, 1979 ρρπφτγρ ς - ^ δ -P 5786 / 7a J ^ KUlU1K b.p.A. / 38, Via Lambro 1-Opera (Milan) Claims 1. Connection to cellulite treatment, thereby marked · - · '' that it essentially consists of a thiol derivative with the following formula: R-CH-KH-CO-CH
COOM where M is hydrogen or alkali metal or Alkaline earth metal atom is - R is H or -CH ₂ SH - R ¹ is H or -SH - R "is H, -CH ₃ or -C ₂ H ₅ ; in addition, when R ¹ is -SH, R is hydrogen and R "is -CH ₅ , C ₂ H ₅ and when R is -CH ₂ SH, R 'is hydrogen and R" is hydrogen or -CH, or -C ₂ H ₁ -. 2. A compound according to claim 1, characterized in that this thiol derivative consists of a 2-thiolpropionamide vinegar 030020/0630 acid or one of its salts with the following formula: QTT COOM CH, 3. A compound according to claim 2, where this thiol derivative is the sodium salt of 2-thiol-propionamide-acetic acid. 030020/0630