CS223370B1 - Hydrophilic ointment base - Google Patents

Abstract

The invention relates to a hydrophilic butter base based on an oil-in-water emulsion, intended for dermal pharmaceutical or cosmetic preparations, but especially for pharmacies, for magistraliter prescribed external preparations. This base is characterized in that the aqueous phase is a gel containing a neutralized carboxyvinyl polymer. The stability of the emulsion is achieved by adding a minimum amount of a suitable emulsifier with an HLB value of 6 to 20, preferably 10 to 18.

Description

The invention relates to a hydrophilic butter base based on an oil-in-water emulsion, intended for dermal pharmaceutical or cosmetic preparations, but especially for pharmacies, for magistraliter prescribed external preparations. This base is characterized in that the aqueous phase is a gel containing a neutralized carboxyvinyl polymer. The stability of the emulsion is achieved by adding a minimum amount of a suitable emulsifier with an HLB value of 6 to 20, preferably 10 to 18.

The invention relates to a hydrophilic ointment base based on an oil-in-water emulsion. This base is intended for dermal pharmaceutical or cosmetic preparations, but especially for medical purposes, for magistraliter prescribed external preparations. It differs from conventional bases of a similar type primarily in the nature of the aqueous phase, which is a gel, without the final form having the character of a gel.

There is information in the literature about the use of various gelling agents. An overview of the history, recipes, structure and prospects of gels is given by D. L. Courtney (Amer. Perfum. Cosmet 87, 31, 1972). The structure and properties of some natural hydrocolloids used in cosmetic production are reported by G. Brigand (Riechst. Aromen, Korperpflegemittel 23, 1973, No. 2, p. 32). The preparation of a transparent gel containing polyoxyethylene cetyl stearyl ether and polyoxyethylene oleyl ether is also known (Swiss Pat. No. 500 715).

The definition, theory and recipes of emulsions were dealt with, for example, by K. Gúttinger (Kosmet. Aerosole 1972, 45 /6/, 148), E. Nůrnberg (Deutsche Apotheker Ztg. 108, 26, 907, 1968) and K. Khristov et al. (Pharmazie 1972, 27 /1/, 46);

In the production of emulsions, gelling agents have been used to a limited extent only as thickeners, i.e. as emulsion stabilizers, but not as basic components. Through systematic research of the individual ingredients required for the production of emulsions and gels, it has been possible to create a new original system that summarizes the advantages of both types of consistencies, i.e. emulsion and gel, and eliminates their disadvantageous properties. It is a system that forms a transition between gel and emulsion, with properties desirable for a hydrophilic massage base. This system is chemically and physically stable, even at maximum temperature loads, there is no phase separation. It is able to accommodate a significant amount (at least 100% vol.) of hydrophilic and hydrophobic liquids without compromising its stability. Its consistency and rheological properties change little in the temperature range of 5 to 60 °C. The base is very easy to spread and washable with water. It is compatible with many active ingredients, both solid and liquid, making it suitable for the formulation of a number of industrially produced dermal preparations of both pharmaceutical and cosmetic nature. This base is particularly advantageous for pharmacies.

The invention therefore relates to a hydrophilic butter base based on an oil-in-water emulsion, the essence of which is that it contains 5 to 50% by weight of a fat phase, 40 to 90% by weight of an aqueous phase, 0.01 to 2.0% by weight, preferably 1.0 to 1.5% by weight of an emulsifier with a hydrophilic-lipophilic balance value of 6 to 20, preferably 10 to 18, 0.4 to 0.8% by weight, preferably 0.5 to 0.6% by weight of a gel-forming substance, in particular a neutralized carboxyvinyl polymer, 0.02 to 0.5% by weight of an antimicrobial and/or preservative and/or stabilizing active substance, the aqueous phase forming a gel. If necessary, the butter base may contain a perfume and/or colorant additive.

All raw materials that form part of the base are non-toxic, pharmacologically indifferent, mostly commonly listed in pharmacopoeias. The content of fatty substances can be adjusted as needed to create emulsions with different resorption and penetration characteristics. The amount of emulsifier with a high value of hydrophilic-lipophilic balance is insignificant; in extreme cases, the emulsifier could be omitted, but as experience has shown, the addition of even a very small amount of emulsifier significantly improves the properties of the final product, in particular, guarantees its stability.

From an economic and technological point of view, the base according to the invention is also advantageous in that a simple homogenization device is sufficient for its production.

For use in a hydrophilic oil base, physiologically harmless nonionic emulsifiers such as ethoxylated fatty acid esters of sorbitol, alkyl polyglycol ethers, alkyl aryl polyglycol ethers, sulfates of substituted polyglycol ethers, sulfosuccinates and phosphoric acid esters are particularly suitable.

If a carboxyvinyl polymer is used as a gelling agent, there are a number of substances suitable for its neutralization, for example alkali metal hydroxides, especially sodium hydroxide, hydroxyalkylamines, especially triethanolamine, diisopropylamine or triethylamine, or borax, etc.

Commonly known liquid and solid substances can serve as components of the fat phase, such as solid and liquid paraffin, white and yellow vaseline, vegetable oils, purcelin, stearin, cetyl alcohol, stearyl alcohol, beeswax, lanolin, ceresin, cetaceum, isopropyl palmitate and many others, if they suit the intended purpose.

Solid and liquid, hydrophilic and lipophilic, organic and inorganic active ingredients can be incorporated into the base; however, care must be taken to ensure that when using active ingredients that lower the pH value, hydroxyethyl cellulose is used as a gelling agent.

The aqueous phase, in addition to water itself, may also include polyhydric alcohols, such as glycerol, propylene glycol, sorbitol, etc.

The base met the given conditions in the basic tests of microbiological safety and dermal irritation. The pH value of the 20% aqueous emulsion ranged from 6.60 to 6.90.

When evaluating the stability using alternating tests (24 hours at 40°C, 24 hours at 5°C and 24 hours at room temperature), performed 13 times in succession, no changes in the character of the tested samples were detected.

β

Example 4

Further details can be seen from the following examples of embodiments, which indicate some of the application options of the hydrophilic ointment base according to the invention. Regenerating cream with collagen

to. Collagen 1.0 Liquid paraffin 20.0 Example 1 Cetylstearyl alcohol 1.5 Emulsifier as in example 1 1.5 Dry base for pharmacies (quantity in gj: Carboxyvinylpolymer 0.5 Triethanolamine 0.8 Liquid paraffin 10.0 Ethanol 96% 5.0 Cetylstearyl alcohol 1.5 to 2.0 Preservative or antimicrobial Alkyl poly-type emulsifier substance 0.2 to 0.3 glycol ether (HLB 15 to 16) 1.0 to 1.5 Perfume 0.4 to 0.5 Carboxyvinylpolymer 0.5 Water up to 100.0 Triethanolamine 0.8 Preservative or Example 5 antimicrobial substance 0.2 Water up to 100.0 Massage Cream I Workflow for examples 1 to 15: Nicotinic acid benzyl ester 0.05 Menthol 1.0 First, all the components of the liquid phase are Camphor 1.0 sterilized at a temperature of 120 to 130 °C, after o- Liquid paraffin 30.0 cooling to a temperature of around 100 °C is added Cetylstearyl alcohol 1.5 carboxyvinyl polymer, pre-swollen in Emulsifier as in example 1 1.5 water and emulsifier, the mixture is homogenized, Carboxyvinylpolymer 0.5 neutralizes with triethanolamine while stirring Triethanolamine 0.8 to create a gel consistency, after which Ethanol 96% 10.0 gradually adding other ingredients, such as anti- Antimicrobial substance 0.2 microbial or preservative agents, perfume, Water up to 100.0 optionally dye. Permanent mixing the base cools to room temperature. According to Example 6 its character (dry or semi-oily) by adding active ingredients, the appropriate Massage Cream II a basis for the desired final product, i.e. medicinal or cosmetic product. Benzyl ester of acid nicotine 0.05 Example 2 Liquid paraffin 30.0 Solid paraffin 15.0 Semi-oily base Cetyl alcohol 1.0 Alkylaryl-type emulsifier Liquid paraffin 30.0 to 40.0 polyglycol ether (HLB 15 to 17) 2.0 Cetylstearyl alcohol 1.5 to 2.0 Carboxyvinylpolymer 0.5 Emulsifier as in example 1 1.5 to 2.0 Triethanolamine 0.8 Carboxyvinylpolymer 0.5 Antimicrobial substance 0.2 Triethanolamine 0.8 Lavender oil 0.25 Preservative or antimicrobial Water up to 100.0 substance 0.2 Water up to 100.0 Example 7 Example 3 Vitamin cream Regenerative cream hormonal Axerophthol acetate 0.05 Tocopherol acetate 0.1 Pregnenolone base 0.25 Tocopherol 100% 0.1 Liquid paraffin 20.0 Pyridoxine dipalmitate 0.2 Cetylstearyl alcohol 1.5 Panthenol 0.5 Emulsifier as in example 1 1.5 Allantoin 0.2 Carboxyvinylpolymer 0.5 Liquid paraffin 15.0 Triethanolamine 0.8 Cetylstearyl alcohol 1.5 Ethanol 96% 5.0 Emulsifier as in example 1 1.5 Preservative or antimicrobial Carboxyvinylpolymer 0.5 substance 0.2 to 0.3 Triethanolamine 0.8 Perfume 0.4 to 0.5 Antimicrobial substance 0.2 Water up to 100.0 Perfume 0.5 Water up to 100.0

Example 8 Liquid paraffin Carboxyvinyl polymer 5.0 0.8 Sunscreen Triethanolamine 0.4 Emulsifier as in example 1 1.0 cANapthylcetyl ether 5.0 Butylhydroxyanisole 0.04 Theophylline 2.0 Butylhydroxytoluene 0.03 Liquid paraffin 20.0 Ascorbyl palmitate 0.03 Solid paraffin 5.0 Antimicrobial substance 0.2 Cetylstearyl alcohol 1.0 Water up to 100.0 Emulsifier as in example 1 1.5 Carboxyvinylpolymer 0.5 Example 13 Triethanolamine 0.8 Antimicrobial substance 0.2 Disinfectant ointment Perfume 0.5 Water up to 100.0 Carbethoxypentadecyltrimethyl- ammonium bromide 0.2 Example 9 Liquid paraffin 12.0 Cetylstearyl alcohol 2.0 Refreshing cream Emulsifier as in example 1 1.0 Carboxyvinylpolymer 0.6 Menthol 1.0 Triethanolamine 0.9 Camphor 1.0 Antimicrobial substance 0.2 Ethanol 96% 5.0 Water up to 100.0 Liquid paraffin 15.0 Purcelin rigid 5.0 Example 14 Carboxyvinylpolymer 0.5 Triethanolamine 0.8 Heparinoid ointment Polyoxyethylene glycol sorbitan oleate 1.5 Antimicrobial substance 0.2 Heparin S 0.2 Water up to 100.0 Liquid paraffin 13.0 Solid paraffin 5.0 Example 10 Cetylstearyl alcohol 2.0 Emulsifier as in example 1 1.5 Liquid powder Carboxyvinyl polymer Triethanolamine 0.5 0.8 Zinc oxide 5.0 Antimicrobial substance 0.2 Talc 10.0 Water up to 100.0 Titanium dioxide 10.0 Liquid paraffin 20.0 Example 15 Carboxyvinylpolymer 0.8 Triethanolamine 1.0 Antifungal cream Emulsifier as an example 1 0.5 Antimicrobial substance 0.2 Iodopropargyloxypyrimidine subst. 0.5 Water up to 100.0 Liquid paraffin 15.0 Cetylstearyl alcohol 1.5 Example 11 Emulsifier as in example 1 1.0 Carboxyvinylpolymer 0.5 Oxine paste Triethanolamine 0.8 Antimicrobial substance 0.2 Dichlorooxyquinoline subst. 5.25 Water up to 100.0 Titanium dioxide 15.0 Zinc stearate 5.0 Example 16 Japanese wax 0.5 White wax 1.0 Neutral protective cream Liquid paraffin 20.0 Solid paraffin 5.0 Liquid paraffin 20.0 Emulsifier as in example 1 1.0 Cetyl alcohol 5.0 Carboxyvinylpolymer 0.7 Sunflower oil 5.0 Triethanolamine 1.0 Carboxyvinylpolymer 0.6 Water up to 100.0 Triethanolamine 0.8 Antimicrobial substance 0.25 Example 12 Water up to 100.0

Ketophenylbutazone ointment

Claims (2)

SUBJECT An oil-in-water emulsion-based hydrophilic ointment base comprising 5 to 50 wt. % fat phase, 40 to 90 wt. 0.01 to 2.0 wt.%, preferably 1.0 to 1.5 wt. % of an emulsifier having a hydrophilic-lipophilic balance value of 6 to 20, preferably 10 to 18, 0.4 to 0.8 wt.%, preferably 0.5 to 0.6 wt. 0.02 to 0.5% by weight of a gelling agent, in particular a neutralized carboxyvinyl polymer; antimicrobial and / or preservative and / or stabilizing agents, the aqueous phase being a gel. Second ^hydrophilic: the ointment base according to claim 1, characterized in that it contains an addition of perfume and / or dyes.