GB2033748A - A thiol derivative for the treatment of cellulitis - Google Patents
A thiol derivative for the treatment of cellulitis Download PDFInfo
- Publication number
- GB2033748A GB2033748A GB7936936A GB7936936A GB2033748A GB 2033748 A GB2033748 A GB 2033748A GB 7936936 A GB7936936 A GB 7936936A GB 7936936 A GB7936936 A GB 7936936A GB 2033748 A GB2033748 A GB 2033748A
- Authority
- GB
- United Kingdom
- Prior art keywords
- hydrogen
- cellulitis
- treatment
- thiol
- thiol derivative
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Withdrawn
Links
- 206010007882 Cellulitis Diseases 0.000 title claims abstract description 17
- 125000003396 thiol group Chemical class [H]S* 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract description 16
- 239000001257 hydrogen Substances 0.000 claims abstract description 16
- 150000003573 thiols Chemical class 0.000 claims abstract description 14
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims abstract description 8
- 229910052784 alkaline earth metal Inorganic materials 0.000 claims abstract description 8
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract description 8
- 239000003513 alkali Substances 0.000 claims abstract description 4
- 150000001342 alkaline earth metals Chemical class 0.000 claims abstract description 4
- 125000004429 atom Chemical group 0.000 claims abstract description 4
- 150000001875 compounds Chemical class 0.000 claims abstract description 4
- 125000004055 thiomethyl group Chemical group [H]SC([H])([H])* 0.000 claims abstract 3
- 108010058907 Tiopronin Proteins 0.000 claims description 7
- 239000000203 mixture Substances 0.000 claims description 4
- 150000003839 salts Chemical class 0.000 claims description 3
- 159000000000 sodium salts Chemical class 0.000 claims description 3
- 239000004480 active ingredient Substances 0.000 claims 1
- 239000000829 suppository Substances 0.000 description 5
- 239000000546 pharmaceutical excipient Substances 0.000 description 4
- 102000003886 Glycoproteins Human genes 0.000 description 3
- 108090000288 Glycoproteins Proteins 0.000 description 3
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 description 3
- 239000002253 acid Substances 0.000 description 3
- 210000001789 adipocyte Anatomy 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 230000008595 infiltration Effects 0.000 description 3
- 238000001764 infiltration Methods 0.000 description 3
- 239000002674 ointment Substances 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- 238000007920 subcutaneous administration Methods 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 2
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 2
- 150000007513 acids Chemical class 0.000 description 2
- 230000001969 hypertrophic effect Effects 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 229920000642 polymer Polymers 0.000 description 2
- 230000002829 reductive effect Effects 0.000 description 2
- HEMHJVSKTPXQMS-UHFFFAOYSA-M sodium hydroxide Inorganic materials [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 2
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- 238000009825 accumulation Methods 0.000 description 1
- 239000012670 alkaline solution Substances 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- JYYOBHFYCIDXHH-UHFFFAOYSA-N carbonic acid;hydrate Chemical compound O.OC(O)=O JYYOBHFYCIDXHH-UHFFFAOYSA-N 0.000 description 1
- 239000006071 cream Substances 0.000 description 1
- 235000005911 diet Nutrition 0.000 description 1
- 230000037213 diet Effects 0.000 description 1
- 235000014113 dietary fatty acids Nutrition 0.000 description 1
- 230000008034 disappearance Effects 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 239000000194 fatty acid Substances 0.000 description 1
- 229930195729 fatty acid Natural products 0.000 description 1
- 150000004665 fatty acids Chemical class 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 235000011187 glycerol Nutrition 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000006210 lotion Substances 0.000 description 1
- 230000007935 neutral effect Effects 0.000 description 1
- 206010033675 panniculitis Diseases 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 1
- 235000017557 sodium bicarbonate Nutrition 0.000 description 1
- 239000008174 sterile solution Substances 0.000 description 1
- 210000004304 subcutaneous tissue Anatomy 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 238000002604 ultrasonography Methods 0.000 description 1
- 235000013311 vegetables Nutrition 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
- A61Q19/06—Preparations for care of the skin for countering cellulitis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/46—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing sulfur
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Birds (AREA)
- Dermatology (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
As a compound active in the treatment of cellulitis a thiol derivative having the general formula: <IMAGE> in which M denotes hydrogen or an atom of an alkali or alkaline earth metal, R is H or CH2SH R' is H or -SH R'' is H or -CH3 or -C2H5 and in which, when R' is -SH, R is hydrogen and R'' is -CH3 or -C2H5 and when R is -CH2SH, R' is hydrogen and R'' is hydrogen or -CH3 or -C2H5.
Description
SPECIFICATION
A thiol derivative for the treatment of cellulitis
DESCRIPTION
The invention relates to a thiol derivative of use for eliminating or reducing cellulitis.
As is known, the term cellulitis is conventionally used for the abnormal subcutaneous layer, having the typical appearance of orange peel, which forms as a result of an accumulation of hypertrophic adipocytes in the polymer structure of hydrophilic glycoprotein acids.
Both for aesthetic and for therapeutic reasons, cellulitis must be eliminated or substantially reduced. This problem is becoming progressively more urgent and widespread.
The conventional, most widely-used reductive treatment of cellulitis is based on localized mechanical action (massage). This treatment which, as is known, has to be performed by skilled personnel for very long periods, generally has to be associated with special diets and constant physical exercise. It it also known that, as a result of "fatigue" and the expense of treatment, the patient often breaks it off after the first reduction in cellulitis, even though this reduction is not completely satisfactory and will rapidly be made useless by the interruption in treatment.
Other methods of treating cellulitis have been suggested, e.g. based on ultrasound or particular enzymes, but these suggestions have not been widely applied in practice since, as before, they require highly-trained personnel and/or complicated apparatus which is not easy to operate or monitor, and the results are not completely satisfactory.
The main object of the invention is to provide a compound which is highly efficient against cellulitis, widely available and easily incorporated in excipients which can be directly applied to the patient.
This object, and others which will be more clearly understood from the description hereinafter, are obtained by a compound for treating cellulitis according to the invention, mainly comprising a thiol derivative having the general formula:
in which M denotes hydrogen or an atom of an alkali or alkaline earth metal,
R is H or -CH2SH R' is H or -SH
R" is H or -CH3 or -C2H5 and in which, when
R' is -SH, R is hydrogen and R" is -CH3 or -C2H5 and when R is -CH2SH, R' is hydrogen and R" is hydrogen or -CH3 or -C2H5.
Thiol derivatives according to the aforementioned general formula, in which M, R, R' and
R" have the meanings given, have been shown to have a considerable anti-cellulitis effect in that, after appropriate preparations containing the aforementioned thiol derivatives have been locally applied or administered by other methods (e.g. by rectal or oral application or local infiltration) considerable softening of the subcutaneous cellulitis nodules is always observed, followed by their gradual reduction and disappearance, whereas the cutaneous and subcutaneous tissue recovers its elasticity and plasticity.This relatively fast, surprising effect is mainly due to the capacity which the thiol derivatives according to the aforementioned general formula have of depolymerizing hydrophilic glycoprotein acids, thus releasing the hypertrophic adipocytes which have previously accumulated in the polymer chains of the glycoproteins. The adipocytes can consequently be rapidly reabsorbed and eliminated.
More particularly, the aforementioned anticellulitis activity is at a maximum when the thiol derivative, used either alone or in an appropriate excipient, is 2-thiol-propionamidoacetic acid or a salt thereof, more particularly the sodium salt. This acid has the following formula:
Another important advantage is the ease and cheapness with which the aforementioned thiol derivatives can be incorporated in excipients for local use, e.g. in ointments, unguents, cream, lotions or the like, or suppositories for rectal administration or for local infiltration (a sterile solution) or oral administration, e.g. in the form of tablets, capsules, granulates, syrups and the like. Cellulitis can thus be effectively and economically treated, directly by the patient.
The following are some non-limitative examples of some formulations and excipients incorporating a thiol derivative according to the invention, more particularly 2-thiol propionamido-acetic acid or a salt thereof, of use in the treatment of cellulitis.
EXAMPLE I
6 g of 2-thiol-propionamido-acetic acid were dissolved in about 20 ml water and heated to about 50,C, keeping the pH neutral by adding alkaline solution (e.g. sodium or potassium hydroxide). The resulting solution was then added to 74 g melted lanoline. The resulting ointment was applied by prolonged massaging of the region under treatment.
Dose of active principles: 200-300 mg per application. Duration of treatment: 6-8 weeks.
EXAMPLE 2 6 g of 2-thiol-propionamido-acetic acid in the form of the sodium salt was dissolved in 200 ml distilled sterile apyrogenic water. The resulting solution was filtered and distributed in bottles having a predetermined capacity, which were sterilized in an autoclave.
The bottles were used for local subcutaneous infiltration by repeated injections, the dose being 100-200 mg active principle per treatment.
EXAMPLE 3 10 g of 2 thiol-propionamido-acetic acid were dissolved in about 4 ml water and sodium bicarbonate was added until the pH was 5-6.
The solution was heated to 40"C and incorporated in melted suppository material (e.g.
esters of glycerine with saturated vegetable fatty acids).
The material containing the active principle was distributed in suppository containers having a given capacity.
The suppositories contained 50-500 mg of active principle. The dose for application was 1 or 2 250 mg suppositories per day, for 15-30 days.
Claims (4)
1. A composition for the treatment of cellulitis, characterised in that it comprises as active ingredient a thiol derivative having the following general formula:
in which M denotes hydrogen or an atom of an alkali or alkaline earth metal,
R is H or CH2SH
R' is H or -SH R" is H or - CH3-or - C2H5 and in which, when R' is - SH, R is hydrogen and R" is -CH3 or -C2H5 and when R is -CH2SH, R' is hydrogen and R" is hydrogen or -CH3 or -C2 H5.
2. A composition according to Claim 1, characterised in that the thiol derivative is 2thiol propionamido acetic acid or a salt thereof having the general formula:
3. A composition according to Claim 2 in which the thiol derivative is the sodium salt or 2-thiol-propionamido acetic acid.
4. As a new compound active in the treatment of cellulitis a thiol derivative having the general formula:
in which M denotes hydrogen or an atom of an alkali or alkaline earth metal,
R is H or CH2SH
R' is H or -SH
R" is H or CH3 or -C2H5 and in which, when
R' is -SH, R is hydrogen and R" is -CH3 or -C2H5 and when R is -CH2SH, R' is hydrogen and R" is hydrogen or -CH3 or -C2H5.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IT29292/78A IT1101261B (en) | 1978-10-31 | 1978-10-31 | THYOLIC DERIVATIVE FOR THE TREATMENT OF CELLULITE |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| GB2033748A true GB2033748A (en) | 1980-05-29 |
Family
ID=11226698
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| GB7936936A Withdrawn GB2033748A (en) | 1978-10-31 | 1979-10-24 | A thiol derivative for the treatment of cellulitis |
Country Status (5)
| Country | Link |
|---|---|
| BE (1) | BE874915A (en) |
| DE (1) | DE2943031A1 (en) |
| FR (1) | FR2440355A1 (en) |
| GB (1) | GB2033748A (en) |
| IT (1) | IT1101261B (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2750332B1 (en) * | 1996-06-28 | 1998-09-11 | Sincholle Daniel Paul | COMPOSITION FOR THE PREVENTION AND TOPICAL TREATMENT OF CELLULITE |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2470M (en) * | 1962-03-13 | 1964-04-20 | Mead Johnson & Co | Therapeutic composition. |
| FR1491204A (en) * | 1962-08-10 | 1967-08-11 | Santen Pharmaceutical Co Ltd | Processes for the preparation of alpha- and beta mercaptopropionylglycocoll and their derivatives |
-
1978
- 1978-10-31 IT IT29292/78A patent/IT1101261B/en active
-
1979
- 1979-03-16 BE BE0/194080A patent/BE874915A/en unknown
- 1979-10-24 DE DE19792943031 patent/DE2943031A1/en not_active Withdrawn
- 1979-10-24 GB GB7936936A patent/GB2033748A/en not_active Withdrawn
- 1979-10-30 FR FR7926904A patent/FR2440355A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| BE874915A (en) | 1979-07-16 |
| IT7829292A0 (en) | 1978-10-31 |
| DE2943031A1 (en) | 1980-05-14 |
| FR2440355A1 (en) | 1980-05-30 |
| IT1101261B (en) | 1985-09-28 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US4442125A (en) | Process for detaching or preventing attachment of microorganisms to a surface | |
| US5324746A (en) | Method of treating damaged mucosal and epithelial tissues with misoprostol | |
| EP0300100A1 (en) | Method and compounds for reducing dermal inflammations | |
| CA1333179C (en) | Method and compounds for reducing dermal inflammations | |
| GR3026530T3 (en) | Terfenadine metabolites and their optically pure isomers for treating allergic disorders | |
| JPH01311030A (en) | Angiogenesis inhibiting collagen metabolism control drug | |
| EP0423929A1 (en) | Skin whitening agent | |
| EP0822816B1 (en) | Dermatological preparation for treating actinic keratoses | |
| EP0746313B1 (en) | Use of a composition comprising alpha hydroxy organic acid for the manufacture of a medicament for the treatment of small mouth ulcers | |
| US4708873A (en) | Method of chemically debriding uncerated necrotic tissue | |
| Sealock et al. | Administration of Ascorbic Acid to an Alkaptonuric Patient. | |
| CA2070468A1 (en) | Fatty acid treatment | |
| NO950518D0 (en) | Use of terpene compounds for reduced release of arachidonic acid and assay mediators | |
| JP2004501195A (en) | Neuroprotective 7-β-hydroxy steroid | |
| GB2033748A (en) | A thiol derivative for the treatment of cellulitis | |
| US20040097587A1 (en) | Compositions and methods of treatment of ulcerating diseases, burns, and related conditions | |
| Sassolas et al. | Nocturnal continuous infusion of growth hormone (GH)-releasing hormone results in a dose-dependent accentuation of episodic GH secretion in normal men | |
| WO2014117056A1 (en) | Therapeutic compounds | |
| JP2557241B2 (en) | Anti-pigmenting agent | |
| TJ286B (en) | A method for treatment or prevention of obesity | |
| EP2810641B1 (en) | Topical pharmaceutical and medical device preparations containing combinations of sucralfate, hyaluronic acid, arginine and a natural moisturizing agent | |
| JPH0559092B2 (en) | ||
| Myren et al. | Effects of colchicine on intestinal mucosal dehydrogenases: I. Histochemical observations | |
| CN115040501B (en) | Application of cis-13-octadecenoic acid or salt compound thereof in preparation of drugs for promoting healing of damaged skin and/or mucous membrane | |
| US3720773A (en) | Method and composition for the topical treatment of herpetic keratitis |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| WAP | Application withdrawn, taken to be withdrawn or refused ** after publication under section 16(1) |