DD234612B1 - OINTMENT BASE AND SKIN CARE IN THE FORM OF A WATER IN LIPID EMULSION - Google Patents

Description

Field of application of the invention

The invention relates to a new ointment base of type F, which can be used as a skin care product or in which dermatologically active ingredients can be incorporated. Field of application of the invention are the pharmaceutical industry and medicine.

Characteristic of the known technical solutions

The normal functional state of the epidermis of human skin is essentially determined by the intensity and timing of the proliferation, differentiation, maturation and keratinization of the epidermis cells and by the relationship of these processes to one another. External or internal skin effects may affect one or more of these parameters, which in turn may retroactively affect the course of other processes in the skin. The result of these processes, depending on the presence or absence of the basic disposition of the skin, are various skin diseases such as desiccation dermatoses, aging skin, various forms of eczema, psoriasis, ichthyosis and the like. a. m.

The starting point for any successful external therapy of this disease is the selection of an optimal basis, the most appropriate vehicle. For each active substance, a corresponding vehicle must be selected in the respective desired pharmaceutical form. The following requirements must be placed on these vehicles: No irritative effects on the skin Lack of sensitizing properties Favorable liberation of the active substance Favorable influence on the functional structure of the skin according to the respective disease Supports the respective penetration kinetics of the active substance

The ointment base is not only to select as a carrier for drugs, but it also affects the skin due to their physicochemical properties. This is especially true in the prophylaxis and metaphylaxis of many skin diseases. So z. B. psoriatiker a corresponding, the normal functional structure of the skin supportive, drug-free skincare in the eruption-free interval or a therapy-supporting Externum after or before the various forms of phototherapy.

The attending physician is on individual; Dependent on formulations to be prepared by the pharmacist, which seldom meet all the requirements listed above. On the other hand, the interaction of skin condition, vehicle and drug under the influence of numerous auxiliaries is a problem of dermatopharmacology manageable only for the specialist. In addition, in selecting an appropriate basis in external therapy, the skin type, the degree of manifestation of the disease and the morphology of the disease must be taken into account, so that different bases must be applied.

In summary, it can be stated that at present there are no salve bases or skincare products meeting these requirements.

Object of the invention

The object of the invention is to develop a skin care product adapted to the basic type of skin which supports the normal functional structure of the skin

Explanation of the essence of the invention

The invention is based on the object; to develop a skin care or ointment base type F with penetration-promoting properties, which can serve as a vehicle for different drugs.

According to the invention, the new ointment base of the type F in the form of a water in lipid emulsion of f to 10% with 5 to 20% urea occupied polysaccharide, 0.05 to 5% adipic acid, 2 to 15% yellow vaseline, Paraffinum pertiquidum, Paraffinum molle and emulsifiers, preferably RofetanF, 1 to 10% sorbitol solution and 40 to 80% water. This composition is well adapted to the basic skin types and is galenically and chemically stable.

The microbiological purity of this emulsion type is preferably achieved by addition of methyl hydroxybenzoate and propyl hydroxybenzoate

In this vehicle, drugs, preferably corticosteroids, dithranol, antimycotics, photoprotective or antiviral substances and necessary stabilizers and excipients can be incorporated.

The application of the fat-rich ointment base type F usually takes place in sebostatic skin types (about 10 to 20% of the population}.

embodiment

The invention will be explained in more detail below using an example:

According to the invention, a urea phase is first prepared by dissolving urea in water and stirring it with a polysaccharide, preferably corn starch, to give a thin suspension, which is then dried at 60 to 80 ° C. A water phase is prepared by dissolving sorbitol, adipic acid and methyl hydroxybenzoate in water at a maximum of 80 ° to 90 ° C. with stirring. In a melt phase, yellow vaseline, rofetan F, paraffinum perliquidum, paraffin molle and propylhydroxybenzoate are added to the melt kettle with continuous stirring maximum 70 ° C mixed to clear liquid melt. The mixture of the individual phases is carried out in a Frymal®) plant by initially introducing the melt phase and mixing the urea phase with constant stirring. Subsequently, the emulsion is formed by adding the water phase with intensive stirring (homogenizing) for 10 to 20 minutes. Subsequently, the emulsion is cooled with continuous stirring to about 37 ° C until emptying of the system.

As an example of a composition of the F-type sebum base can be listed:

Vaseline, yellow 9.00

Rofetan F 5.00

Paraffin perliquidum 7.00

Paraffinum molle 5.00

Sorbitol 2.00

Urea 10.00

Cornstarch 4.00

Adipic acid 0.20

Methyl hydroxybenzoate 0.12

Propyl hydroxybenzoate 0.08 * -

Water 57,60 100,00

The galenic stability of the ointment base according to the invention proved to be sufficient in the cold, heat, swing and centrifuge tests usually used for stability reports.

For chemical stability, the following urea concentrations could be found with respect to the urea content of the example given above:

After storage for 1 year at room temperature at + 40 ° C

Ointment base F type 9.45% 8.90%

A comparably very good skin compatibility results from the epidermal reaction after short-term and long-term contact with the __

Ointment base type F in animal experiments (guinea pig ear) for biometric and 3-H thymidine autoradiographic examinations.

Contact duration AF PI DNA-SI 1 week 1.20 0.99 1.68 4 weeks 1.16 1.03 1.03 (AF = acanthosis factor, PI = papillomatosis index, DNA-SI = DNA synthesis index)

Claims (2)

1. ointment base for dermatologically active agents and skin care agents in the form of a water in üpid emulsion, characterized in that they contain from 1 to 10% with 5 to 20% urea occupied Polysaccharidteifchen, 0.05 to 5% adipic acid, 2 to 15% yellow Vaseline, Paraffinum perliquidum, Paraffinum molle and emulsifying alcohols, preferably Rofetan F, 1 to 10% sorbitol solution and 40 to 80% water. 2. ointment base and skin care agent according to claim 1, characterized in that preferably 0.01 to 1% of methyl hydroxybenzoate and propyl hydroxybenzoate are included. Field of application of the invention / The invention relates to a new ointment base type F, which can be used as a skin care product or in the £ Dermatologically active agents can be incorporated. Field of application of the invention are the pharmaceutical industry and medicine. Characteristic of the known technical solutions The normal functional state of the epidermis of human skin is essentially determined by the intensity and timing of the proliferation, differentiation, maturation and keratinization of the epidermis cells and by the relationship of these processes to one another. External or internal skin effects may affect one or more of these parameters, which in turn may retroactively affect the course of other processes in the skin. The result of these processes, depending on the presence or absence of the basic disposition of the skin, are various skin diseases such as desiccation dermatoses, aging skin, various forms of eczema, psoriasis, ichthyosis and the like. a. m. The starting point for any successful external therapy of this disease is the selection of an optimal basis, the most appropriate vehicle. For each active substance, a corresponding vehicle must be selected in the respective desired pharmaceutical form. The following requirements must be met for these vehicles: - no irritative effects on the skin - lack of sensitization properties - favorable liberation of the active substance - Favorable influence on the functional structure of the skin according to the particular disease - Support of the respective penetration kinetics of the drug The ointment base is not only to be selected as a carrier for drugs, but it also affects the skin itself because of their physicochemical properties. This is especially true in the prophylaxis and metaphylaxis of many skin diseases. So z. B. psoriatiker a corresponding, the normal functional structure of the skin supportive, drug-free skincare in the eruption-free interval or a therapy-supporting Externum after or before the various forms of phototherapy. The attending physician relies on individual recipes to be prepared by the pharmacist, which rarely meet all the requirements listed above. On the other hand, the interaction of skin condition, vehicle and drug under the influence of numerous auxiliaries is a problem of dermatopharmacology manageable only for the specialist. In addition, in selecting an appropriate basis in external therapy, the skin type, the degree of manifestation of the disease and the morphology of the disease must be taken into account, so that different bases must be applied. In summary, it can be stated that at present there are no salve bases or skincare products meeting these requirements. Object of the invention The invention has the goal to develop a Hautgrundtypen adapted skin care product or an ointment base, the normal skin function structure supported. * Explanation of the essence of the invention The invention has for its object to develop a skin care product or an ointment base type F with penetration-promoting properties, which can serve as a vehicle for different drugs. According to the invention, the new ointment base type fin form of a water in lipid emulsion from 1 to 10% with 5 to 20% urea-occupied polysaccharide, 0.05 to 5% adipic acid, each 2 to 15% yellow vaseline. Paraffinum perliquidum, Paraffinum molle and emulsifiers, preferably Rofetan F, 1 to 10% sorbitol solution and 40 to 80% water. This composition is well adapted to the basic skin types and is galenically and chemically stable. The microbiological purity of this emulsion type is preferably achieved by addition of methyl hydroxybenzoate and propyl hydroxybenzoate. In this vehicle, drugs, preferably corticosteroids, dithranol, antimycotics, photoprotective or antiviral substances and necessary stabilizers and excipients may be incorporated. The application of the fat-rich ointment base type F usually takes place in sebostatic skin types (about 10 to 20% of the population). embodiment The invention will be explained in more detail below using an example: According to the invention, a urea phase is first prepared by dissolving urea in water and stirring it with a polysaccharide, preferably corn starch, to give a low-viscosity suspension which is then dried at 60 to 80 ^° C. A water phase is prepared by sorbitol, adipic acid and methyl hydroxybenzoate are dissolved with constant stirring at a maximum of 80 to 90 ⁰ C in water. In a melting phase, yellow Vaseline, Rofetan F, Paraffinum perliquidum, Paraffinum molle and Propylhydroxybenzoat be mixed in a melting vessel with continuous stirring at a maximum of 70 ° C to a clear liquid melt. The mixture of the individual phases takes place in a Fryma ^{| B)} plant by initially introducing the melt phase and mixing the urea phase with constant stirring. Subsequently, the emulsion is formed by adding the water phase with intensive stirring (homogenizing) for 10 to 20 minutes. Subsequently, the emulsion is cooled with constant stirring to about 37 ⁰ C until emptying of the system. As an example of a composition of the ointment base of F-type can be listed: 100.00 The galenic stability of the ointment base according to the invention proved to be sufficient in the cold, heat, swing and centrifuge tests usually used for stability reports. For chemical stability, the following urea concentrations could be found with respect to the urea content of the example given above: After storage for 1 year at room temperature at + 40 ° C Ointment base F type 9.45% 8.90% A comparatively very good skin compatibility results from the epidermal reaction after short-term and long-term contact with the ointment base type F in animal experiments (guinea pig ear) after biometric and ³ -H-thymidine autoradiographic studies. Contact duration AF PI DNS-SI 1 week 1.20 0.99 1.68 4 weeks 1.16 1.03 1.03 (AF = acanthosis factor, Pl = papillomatosis index, DNA-SI = DNA synthesis index)