Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Patent
1987-03-26
1991-02-05
Griffin, Ronald W.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
424401, 514 57, 514777, 514781, 514859, 514871, 514943, 514844, A61K 748, A61K 4700, A61K 3170
Patent
active
049905015
DESCRIPTION:
BRIEF SUMMARY
This invention relates to compositions and more particularly concerns compositions which have medical application.
More specifically, the invention relates to compositions which are useful for the treatment of human and animal tissue surfaces, for example skin. Compositions have been found particularly useful for the treatment of skin ailments such as acne and also for injuries where the skin has been damaged, such as burns.
According to one aspect of the present invention we provide a composition for application to human and animal tissue surfaces, said composition comprising an aqueous medium and a film-forming component at least partially soluble or dispersible in said aqueous medium, said film-forming component comprising an ester or mixture of esters, at least one being an ester of a polyol.
In a preferred embodiment, the aqueous medium comprises water and the film forming component comprises a sucrose ester or mixture of sucrose esters, wherein the quantity or sucrose ester of mixture of sucrose esters is 40% to 80% (w/w) of the composition excluding the water.
The film-forming component is preferably soluble in water to an extent of at least 5% by weight at 25.degree. C., more preferably at least 10% by weight.
In preferred compositions according to the invention mixtures of esters are employed, mixtures containing saturated and unsaturated fatty acid esters being particularly preferred. Ratios in the range 20 to 100% by weight saturated to 0-80% unsaturated can be employed. Generally however it is advantageous to include at least 10% by weight unsaturated fatty acid ester in the ester mixture comprising the film-forming component.
It is believed that the presence of unsaturated fatty acid ester helps to solubilise saturated fatty acid esters which if used above would be insoluble. The at least partial solubility or dispersibility of the ester mixture is believed to be necessary in order to achieve a coherent film on a tissue surface being treated with the composition.
The choice of fatty acid esters depends to some extent on the solubility or dispersibility. Thus saturated fatty acid esters which are insoluble in water are suitable only if used in mixtures with esters which have a solubilising effect.
Saturated fatty acid esters in the range C.sub.8 to C.sub.22 can be employed but esters in which the fatty acid is in the range C.sub.12 to C.sub.22 are generally insoluble and thus require to be used in mixtures with solubilising esters. In such mixtures saturated fatty acids in the range C.sub.12 to C.sub.20 are preferred, especially C.sub.16 to C.sub.18.
The esters of unsaturated fatty acids are preferably derived from fatty acids in the range C.sub.16 to C.sub.22, preferably C.sub.16 to C.sub.18.
The polyol may be a sugar, especially sucrose, but other polyols may be used, including lactitol, sorbitol, sorbitan and polyglycerol.
Mixtures of sucrose esters have been found to be advantageous, especially mixtures of sucrose stearates, palmitates and/or oleates.
The composition may include further ingredients to improve its properties or ease of application. The addition of a thickening agent has been found to give desirable properties, suitable thickening agents being cellulose and cellulose derivatives, such as carboxymethyl celluloses.
An additive which improves the "feel" of the composition when applied to the tissue surface may also be included. One such additive is a mixture of mono and diglycerides although other materials could be employed for this purpose, such as lanolin, jojoba oil, coconut oil and similar materials.
The composition may be in the form of a solution, suspension or emulsion. Where the composition is to be used as a treatment for skin ailments or as an application to tissue it is often preferable for the composition to be in the form of an emulsion and to this end it is desirable to add one or more emulsifying agents.
The choice of sucrose ester or esters will to some extent depend upon the end use of the compound. The amount of saturated fatty acid ester may be from 20% to 10
REFERENCES:
patent: 4151304 (1979-04-01), Evans
patent: 4298730 (1981-11-01), Galleymore et al.
patent: 4334061 (1982-06-01), Bossier
patent: 4379755 (1983-04-01), Yamada et al.
patent: 4611055 (1986-09-01), Yamamoto et al.
patent: 4797300 (1989-01-01), Jandacek et al.
patent: 4822601 (1989-04-01), Goode et al.
The Merck Index, 10th edition, published by Merck & Co., Inc., Rahway, N.J., U.S.A., 1983, p. 771, item 5191.
Imrie Frazer K. E.
James Ken
Griffin Ronald W.
Sempernova PLC
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