MXPA00003316A - &bgr;-D GLUCAN TOPICAL COMPOSITION - Google Patents
&bgr;-D GLUCAN TOPICAL COMPOSITIONInfo
- Publication number
- MXPA00003316A MXPA00003316A MXPA/A/2000/003316A MXPA00003316A MXPA00003316A MX PA00003316 A MXPA00003316 A MX PA00003316A MX PA00003316 A MXPA00003316 A MX PA00003316A MX PA00003316 A MXPA00003316 A MX PA00003316A
- Authority
- MX
- Mexico
- Prior art keywords
- composition
- approx
- topical composition
- glucan
- cereal
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 130
- 230000000699 topical Effects 0.000 title claims abstract description 65
- 229920001503 Glucan Polymers 0.000 title claims abstract description 25
- 235000013339 cereals Nutrition 0.000 claims abstract description 54
- 200000000019 wound Diseases 0.000 claims abstract description 24
- 239000006071 cream Substances 0.000 claims abstract description 22
- 239000000499 gel Substances 0.000 claims abstract description 21
- 239000004480 active ingredient Substances 0.000 claims abstract description 12
- 210000003491 Skin Anatomy 0.000 claims abstract description 11
- 230000035876 healing Effects 0.000 claims abstract description 4
- 230000037390 scarring Effects 0.000 claims abstract description 3
- FYGDTMLNYKFZSV-WFYNLLPOSA-N (2S,3R,4S,5S,6R)-2-[(2R,4R,5R,6S)-4,5-dihydroxy-2-(hydroxymethyl)-6-[(2R,3S,4R,5R,6S)-4,5,6-trihydroxy-2-(hydroxymethyl)oxan-3-yl]oxyoxan-3-yl]oxy-6-(hydroxymethyl)oxane-3,4,5-triol Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1OC1[C@@H](CO)O[C@@H](O[C@@H]2[C@H](O[C@H](O)[C@H](O)[C@H]2O)CO)[C@H](O)[C@H]1O FYGDTMLNYKFZSV-WFYNLLPOSA-N 0.000 claims description 55
- 229920002498 Beta-glucan Polymers 0.000 claims description 37
- PEDCQBHIVMGVHV-UHFFFAOYSA-N glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 33
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- 239000002904 solvent Substances 0.000 claims description 21
- LXCFILQKKLGQFO-UHFFFAOYSA-N Methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 claims description 19
- 239000003795 chemical substances by application Substances 0.000 claims description 19
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- 235000007319 Avena orientalis Nutrition 0.000 claims description 14
- NIXOWILDQLNWCW-UHFFFAOYSA-N acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 claims description 14
- GSEJCLTVZPLZKY-UHFFFAOYSA-N Tris Chemical compound OCCN(CCO)CCO GSEJCLTVZPLZKY-UHFFFAOYSA-N 0.000 claims description 12
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- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims description 8
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 claims description 8
- 239000004292 methyl p-hydroxybenzoate Substances 0.000 claims description 8
- 229960002216 methylparaben Drugs 0.000 claims description 8
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- 235000019333 sodium laurylsulphate Nutrition 0.000 claims description 8
- BXWNKGSJHAJOGX-UHFFFAOYSA-N Cetyl alcohol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 claims description 7
- 241000209219 Hordeum Species 0.000 claims description 7
- 235000007340 Hordeum vulgare Nutrition 0.000 claims description 7
- QELSKZZBTMNZEB-UHFFFAOYSA-N Propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 claims description 7
- 206010040844 Skin exfoliation Diseases 0.000 claims description 7
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 7
- 235000010948 carboxy methyl cellulose Nutrition 0.000 claims description 7
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- 229960000541 cetyl alcohol Drugs 0.000 claims description 7
- KCXVZYZYPLLWCC-UHFFFAOYSA-N edta Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 claims description 7
- 239000003906 humectant Substances 0.000 claims description 7
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 claims description 7
- 239000004405 propyl p-hydroxybenzoate Substances 0.000 claims description 7
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- 229940100611 Topical Cream Drugs 0.000 claims description 5
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- 239000003351 stiffener Substances 0.000 claims description 5
- 239000003871 white petrolatum Substances 0.000 claims description 5
- 210000004400 Mucous Membrane Anatomy 0.000 claims description 4
- IPCSVZSSVZVIGE-UHFFFAOYSA-N Palmitic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 claims description 4
- 235000021314 Palmitic acid Nutrition 0.000 claims description 4
- 239000004141 Sodium laurylsulphate Substances 0.000 claims description 4
- 229940072056 alginate Drugs 0.000 claims description 4
- 235000010443 alginic acid Nutrition 0.000 claims description 4
- 229920000615 alginic acid Polymers 0.000 claims description 4
- 239000003974 emollient agent Substances 0.000 claims description 4
- 239000002674 ointment Substances 0.000 claims description 4
- DNLDXOPTFYQILE-UHFFFAOYSA-N 2-[bis(2-hydroxyethyl)amino]tetradecan-1-ol Chemical compound CCCCCCCCCCCCC(CO)N(CCO)CCO DNLDXOPTFYQILE-UHFFFAOYSA-N 0.000 claims description 3
- QFOHBWFCKVYLES-UHFFFAOYSA-N Butylparaben Chemical compound CCCCOC(=O)C1=CC=C(O)C=C1 QFOHBWFCKVYLES-UHFFFAOYSA-N 0.000 claims description 3
- NUVBSKCKDOMJSU-UHFFFAOYSA-N Ethylparaben Chemical compound CCOC(=O)C1=CC=C(O)C=C1 NUVBSKCKDOMJSU-UHFFFAOYSA-N 0.000 claims description 3
- 229920002907 Guar gum Polymers 0.000 claims description 3
- 240000008529 Triticum aestivum Species 0.000 claims description 3
- 229940067596 butylparaben Drugs 0.000 claims description 3
- 229960001617 ethyl hydroxybenzoate Drugs 0.000 claims description 3
- 235000010228 ethyl p-hydroxybenzoate Nutrition 0.000 claims description 3
- 239000004403 ethyl p-hydroxybenzoate Substances 0.000 claims description 3
- 239000000665 guar gum Substances 0.000 claims description 3
- 235000010417 guar gum Nutrition 0.000 claims description 3
- 229960002154 guar gum Drugs 0.000 claims description 3
- 239000003883 ointment base Substances 0.000 claims description 3
- 235000021307 wheat Nutrition 0.000 claims description 3
- 229940039717 Lanolin Drugs 0.000 claims description 2
- 239000004166 Lanolin Substances 0.000 claims description 2
- 239000002738 chelating agent Substances 0.000 claims description 2
- 239000003026 cod liver oil Substances 0.000 claims description 2
- 235000012716 cod liver oil Nutrition 0.000 claims description 2
- 235000019388 lanolin Nutrition 0.000 claims description 2
- 239000006210 lotion Substances 0.000 claims description 2
- 239000002480 mineral oil Substances 0.000 claims description 2
- 235000010446 mineral oil Nutrition 0.000 claims description 2
- 239000012188 paraffin wax Substances 0.000 claims description 2
- 230000002708 enhancing Effects 0.000 claims 5
- 229940042129 Topical Gel Drugs 0.000 claims 2
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- 210000004877 mucosa Anatomy 0.000 claims 1
- 235000019422 polyvinyl alcohol Nutrition 0.000 claims 1
- 239000010686 shark liver oil Substances 0.000 claims 1
- 240000004808 Saccharomyces cerevisiae Species 0.000 description 12
- 244000052616 bacterial pathogens Species 0.000 description 10
- 239000000306 component Substances 0.000 description 9
- 125000005640 glucopyranosyl group Chemical group 0.000 description 7
- 229920001282 polysaccharide Polymers 0.000 description 7
- 210000002421 Cell Wall Anatomy 0.000 description 6
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- 150000004676 glycans Polymers 0.000 description 6
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- 210000004027 cells Anatomy 0.000 description 4
- 229920000642 polymer Polymers 0.000 description 4
- 238000003756 stirring Methods 0.000 description 4
- WPYMKLBDIGXBTP-UHFFFAOYSA-N Benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 3
- 239000004464 cereal grain Substances 0.000 description 3
- 238000006116 polymerization reaction Methods 0.000 description 3
- 206010016807 Fluid retention Diseases 0.000 description 2
- 206010023330 Keloid scar Diseases 0.000 description 2
- 206010028980 Neoplasm Diseases 0.000 description 2
- 208000003251 Pruritus Diseases 0.000 description 2
- 230000001139 anti-pruritic Effects 0.000 description 2
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- 230000001419 dependent Effects 0.000 description 2
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- LFQSCWFLJHTTHZ-UHFFFAOYSA-N ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- 239000000727 fraction Substances 0.000 description 2
- -1 germicides Substances 0.000 description 2
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- HVYWMOMLDIMFJA-DPAQBDIFSA-N (3β)-Cholest-5-en-3-ol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 description 1
- FYYGCTQPBDNICZ-UHFFFAOYSA-N 2-tetradecyloctadecanoic acid Chemical compound CCCCCCCCCCCCCCCCC(C(O)=O)CCCCCCCCCCCCCC FYYGCTQPBDNICZ-UHFFFAOYSA-N 0.000 description 1
- 229940035674 ANESTHETICS Drugs 0.000 description 1
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- 102000008186 Collagen Human genes 0.000 description 1
- 108010035532 Collagen Proteins 0.000 description 1
- WQZGKKKJIJFFOK-QTVWNMPRSA-N D-mannopyranose Chemical compound OC[C@H]1OC(O)[C@@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-QTVWNMPRSA-N 0.000 description 1
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- LYCAIKOWRPUZTN-UHFFFAOYSA-N glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 1
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- ZCTXEAQXZGPWFG-UHFFFAOYSA-N imidurea Chemical compound O=C1NC(=O)N(CO)C1NC(=O)NCNC(=O)NC1C(=O)NC(=O)N1CO ZCTXEAQXZGPWFG-UHFFFAOYSA-N 0.000 description 1
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Abstract
A topical composition for healing treatment of burns and wounds and scarring therefrom has as the active ingredient cereal-derived (1-3) (1-4)&bgr;-D-glucan at about 0.5-15 w/w percent. The composition may be formulated in various forms with creams and gels being preferred for application to the skin.
Description
TOPICAL COMPOSITION OF ß-D-GLUCANO
BACKGROUND OF THE INVENTION
Field of the Invention: This invention relates generally to topical compositions for the treatment of burns and superficial wounds and partial thickness of the skin and mucous membranes. More particularly, the invention pertains to the formulations of topical creams and gels that provide cleansing, wetting, calming action and antipruritic activity for the therapeutic treatment of wounds and burns and other damages and conditions of skin loss.
STATE OF THE ART: A group of complex polysaccharides known as glucans are found in the cell walls of yeast and bacteria. Although the structures of the glycans derived from microbes have not been completely elucidated, it is known that these include long chain carbohydrate polymers composed solely of β-D-glucan residues with 1,3-linkages or a combination of 1,3-linkages and 1.6.
In the cell walls of the yeast Sa cch aromyces cerevi si a, glucans may also be associated with mañano, another complex polysaccharide. Studies have indicated that 1,3-glucan derived from yeast activates macrophages, including phages with immunological activity against tumor development. It was found that 1,6-glucans are inactive relative to macrophages. This is reported by di Luzio et al. in THE MACROPHAGE IN NEOPLASIA, Mary A. Pitik, editox, "1976, Academic Press, New York, pp 181-182. In the United States Patent No. 5,158,772 to Davis, the incorporation of a β-type polysaccharide is described. 1, 3-glucan derived from microbes, in a topical composition The polysaccharide is produced by a bacterial microorganism known as Cel l ul omona s fl a vi gena The functions of the polysaccharide in the topical composition are described as triples, for example ( a) its effectiveness as a water retention agent, by which it controls the fluidity, appearance and "feel" of a composition, (b) its viscosity-elevating effect, (c) its ability to suspend others cosmetic and therapeutic agents such as dyes, drugs, germicides, anesthetics, etc., as a carrier. In a North American Patent Application of Williams and Lawin, which bears serial number 08 / 423,838 and commonly assigned with this application, is described in a mesh matrix wound dressing incorporating cereals-derived β-D-glucan and collagen, in a bandage for burns. Do you need a topical healing ointment for the treatment of burns and wounds? & skin and mucous membranes where a wound dressing is not indicated.
BRIEF DESCRIPTION OF THE INVENTION
The invention comprises a topical composition for multiple purposes for application to the skin and mucous membranes. This is designed for use as a topically applied cream or gel to provide cleansing and soothing relief of superficial and partial thickness burns, such as a humectant to improve water retention of the stratum corneum, and to relieve itching associated with scarring hypertrophic or keloid.
The active ingredient of the topical composition of the invention is being investigated as a possible modifier of the biological response and macrophage stimulator. The main active component of the topical composition is the β-D-glucan derived from cereals, which chemically comprises a large number of glucopyranosyl units which are determined to be linked by links (1-3) and (1-4). The preferred active ingredient is ß-D-glucan derived from oats, "although glucans from barley, wheat and other cereal grains can be used for topical composition, with the proviso that (1-4) (1-3 ) ß-D-glucan can be extracted economically As is generally formulated, the composition of the topical cream of the invention comprises the following, wherein the indicated concentration of each component is uniformly given as a percentage of the total of all the components:
ß-D-glucan derived from cereal approx. 0.5 - 15% (active agent) p / p base for ointment ca. 10 - 20% w / w humectant (s) approx. 2 - 6% w / w increase agent (s) of approx. 0.01 - 8.0 suspension / viscosity% w / p stiffening agent (s) approx. 0.5 - 6% w / w emulsifying agent (s) / approx. 0.1 - 8% solubilization w / w antimicrobial agent (s) approx. 0.1 - 2% w / w plasticizer (s) approx. 5 - 15% solvent (s) the rest
Some ingredients can have several functions. For example, glycerol can serve as a solvent and a plasticizer, and propylene glycol can serve as a solvent, humectant and plasticizer. A general formulation for a gel composition of the invention is:
ß-D-glucan derived from cereal approx. 0.5 - 15% p / p
(active agent) water approx. 80 - 98% w / w increasing agent (s) of approx. 0.5 - 8% p / p suspension / viscosity emulsification agent (s) / approx. 0.5% p / p solubilization antimicrobial agent (s) approx. 0.05 - 1% p / p
The β-D-glucan derived from cereal in this composition is significantly different from the glucans obtained from other sources, including ß-D-glucans derived from yeast, such as Sa cch aromyces cerevi si a e and bacteria such as Cell ul omonas flavi gena. - - The main source of ß-glucan has historically been yeast and bacterial cells. However, (1-4) (1-3) ß-D-glucan derived from cereals, useful in the invention, is different from glycans derived from microbes in that all have links (1-3) or mainly bonds ( 1-3) with a few links (1-6). The molecular weight of the ß-D-glucan derived from mixed-bond cereals used in this invention is much higher than that of glycans derived from microbes.
BRIEF DESCRIPTION OF THE DRAWINGS
Figure 1 is a drawing of a generalized chemical structure of (1-3) of the β-glucan derived from microbes used in a composition of the prior art;
Figure 2 is a drawing of a generalized chemical structure of (1-3) (1-6) of the β-D-glucan; Y
Figure 3 is a drawing of a generalized chemical structure, proposed, of (1-3) (1-4) of the ß-D-glucan derived from mixtures-binding cereals, "used in a topical composition of the invention.
DETAILED DESCRIPTION OF THE INVENTION
According to the invention, the new compositions for the multi-purpose topical treatment are presented wherein the active ingredient is a β-D-glucan derived from cereals, identified herein as * CDG. "The invention pertains to the various compositions The invention includes topical compositions variously known as ointments, creams, gels, emollients, lotions and oils, each with a generally characteristic solvent composition, and having a solvent base varying from essentially all water to essentially all oil. a form in the liquid-to-semi-solid range The compositions classified as β-glucans comprise a large group of high molecular weight polymers containing glucopyranosyl units in β-linked chains ß-glucans are found essentially in all living cells, which are enclosed in cell walls, with structural variation considerable dependent on the source. These are highly unbranched homopolysaccharides and isomerically placed to alpha-D-glucan (eg, starch) which is typically non-functional as a structural support component of the cell. As described in Figure 1, glycans derived from microbes have been generally characterized as possessing essentially linked (1-3) chains of glucopyranosyl units. With recent advances in test identification methods, yeast-derived glucans that have mainly linkages (1-3) with a relatively small number of links (1-6) (Figure 2), have been identified. The glucan polymers derived from yeast are frequently associated with the mannose, and typically have a helically wound chain shape. The mixed link glucan polymers found in cereals are very different from the polymers derived from yeast and from bacteria. Glucans derived from cereal grains, as shown in Figure 3, have bonds (1-3) and (1-4) and generally have a twisted linear or linear chain. The cereal derived glucan (CDG) can be characterized as follows: a. CDG is a long chain unbranched polysaccharide, typically comprising about 3 to 4 percent oat and barley grains. The concentration of CDG is higher, for example 7-10 percent, in the crushed fiber fraction of oats. b. CDG is found in the endosperm and the aleurone cell walls of most cereal grains. Glucans derived from microbes appear in the cell wall of yeast or bacteria. c. CDG is a mixed link molecule that contains approximately 70 percent bonds (1-4) and approximately 30 percent bonds (1-3). The linked units (1-3) appear mainly in a simple manner wherein the linked units (1-4) typically appear in groups of three or four glucopyranosyl units. In this way, the resulting structure is a series of short runs of 3 or 4 glucopyranosyl units (1-4) linked with adjacent runs connected by links (1-3). The frequencies of the groups of three (celotriosyl) and four (celotetraosyl) glucopyranosyl units also tend to be characteristic of the source, being affected by the variety of cereal, the age of the tissue, and the stage of maturity. Typically CDG derived from oats has more than the groups of three glucopyranosyl units (1-4) linked consecutively than the CDG derived from barley. The proportion of the trisaccharide groups to tetrasaccharides is approximately 2: 1 for oats and closer to 3: 1 for barley. CDG differs from glycans derived from microbes, which have all links (1-3) or mainly links (1-3) with some links (1-6). d. CDG is a linear molecule, while glucan derived from yeast has a helical shape.
and. The degree of polymerization of CDG is in the range of about 1200-1800. On the other hand, the ß-D-glucan derived from yeast has a much lower degree of polymerization, for example about 60-80. Cellulose, the main constituent of plant cell walls, has all ß (1-4) bonds and a degree of polymerization of approximately 10,000 to 15,000. F. CDG forms viscous solutions in hot water. On the other hand, the glucan derived from yeast is insoluble in water but dispersible in aqueous systems. g. CDG appears within the grain with a clearly broad range of molecular weight, for example from about 200,000 to 700,000. It is believed that the molecular weight is dependent on the grain species, the grain source, the glucan extraction conditions and the particular laboratory. The glucan derived from microbes has a much lower molecular weight, in the range of about 10,000 to 14,000. Cellulose has a molecular weight of about 700,000. The use of CDG as a food component has been studied extensively by various researchers; Studies have included the use of CDG in the regulation of glucose metabolism, the hypoglycemic response, the reduction in serum cholesterol, and the like. Thus, in terms of chemical structure and molecular weight, CDG is much more cellulose-like than glucan-derived microbe. Each of the components of the new composition serves a particular function or functions, and is available in purities leading to use in particular applications. In this way, a component can comprise the USP grade
(United States Pharmacopoeia), National Formulary (NF), or other grade of purity appropriate for topical use on skin burns and wounds. In addition to cereal-derived ß-D-glucan, the components of the cream formulation include: a. an ointment base, preferably white petrolatum. An alternative but somewhat less desirable substance for this purpose is lanolin. b. a solvent, principally or completely water. Additional solvents that can be added to generally low concentrations including natural oils such as cod liver oil, mineral oil, etc., and glycerol or propylene glycol. The water content of the cream formulation is at least about 50 percent. c. a plasticizer, preferably glycerol. Propylene glycol or other glycol can also be used as a plasticizer. d. a humectant, preferably propylene glycol. and. a suspension or viscosity improving agent, such as carrageenan. Other possible agents include polyvinyl alcohol, xanthan gum, agarose, alginate, guar gum, Carbopol 940 RM carbomer (B.F. Goodrich), and carboxymethylcellulose (CMC), as well as mixtures thereof. A variation in the concentration of suspending agents is compensated by the variation of the concentration of water (solvent). F. an emulsifying or solubilizing agent or agents. Exemplary agents are sodium lauryl sulfate and triethanolamine. In the preferred formulation, a combination of sodium lauryl sulfate and triethanolamine is used. g. a stiffening agent, preferably cetyl alcohol (hexadecanoic acid). Paraffin can also be used.
h. An antimicrobial agent, preferably one or more parabens. The paraben may be methylparaben, propylparaben, ethylparaben, butyl-paraben, or mixtures thereof. Other possible antimicrobial agents are imidurea, benzoic acid and benzoic alcohol. A preferred formation of the cream composition of the invention is:
ß-D-glucan derived from cereal approx. 0.5 - 15% w / w ^ "petrolatum (white) about 0.5 - 15% w / w glycerol about 5 - 15% w / w propylene glycol about 2 - 6% w / w cetyl alcohol (approx. 6% w / w hexadecanoic) triethanolamine approx 0.1 - 5% w / w sodium lauryl sulfate approx 0.1 - 5% w / w parabens approx 0.01 - 2% w / w carrageenan approx 0.01 - 1.0% w / w water the rest (at least 50%)
A currently most preferred composition of the topical cream is as follows:
ß-D-glucan derived from cereal approx. 2% p / p petrolatum (white) approx. 15% w / w glycerol approx. 10% w / w propylene glycol approx. 4% p / p alcohol, cetyl (hexadecanoic acid) approx. 2% w / w triethanolamine approx. 2% w / w sodium lauryl sulphate approx. 1% p / p i-carrageenan approx. 0.3% w / w methyl paraben, approx. 0.2% p / p propyl-parabeno approx. 0.2% p / p xanthan gum approx. 0.15% p ^ p-water the rest (approximately 63.15% p / p)
Another preferred embodiment of the composition is as follows
ß-D-glucan derived from cereal approx. 2% p / p petrolatum (white) approx. 15% w / w glycerol approx. 10% w / w propylene glycol approx. 4% w / w cetyl alcohol (hexadecanoic acid) approx. 2% w / w triethanolamine approx. 2% w / w sodium lauryl sulphate approx. 1% p / p parabens approx. 0.25% p / p carrageenan ca. 0.1% p / p water the rest (approx 62.75% p / p
EXAMPLE A
A batch of 100 g of a topical cream of the invention having the following ingredients, given as g per 100 g of total cream composition, was prepared:
water 63-75 g / 100 g white petrolatum, m.p. 38-60 ° C 15.0 g / 100 g glycerol 10.0 g / 100 g propylene glycol 4.0 g / 100 g ß-D-glucan cereal derivative (oat) 2.0 g / 100 g cetyl alcohol 2.0 g / 100 g triethanolamine 2.0 g / 100 g laurilsulf ato 1.0 g / 100 g i-carrageenan 0.3 g / 100 g methylparaben 0.2 g / 100 g propylparaben 0.2 g / 100 g
Xanthan gum 0.15 g / 100 g
A stock solution of 4% ß-D-glucan was prepared by dissolving 4.0 g of ß-D-glucan derived from purified oat (powder) in 96 ml of distilled water in an autoclave bottle. The solution was stirred vigorously and then heated in an autoclave at 121 ° C with stirring until the glucan was completely dissolved. To 50 ml of the stock solution of the β-D-glucan the remaining ingredients were added to the weights indicated above. Additional water was added to put the components of the mixture to the desired final concentrations. The mixture 'at 85-90 ° C) was liquefied with constant stirring until all the ingredients dissolved and the mixture was homogeneous. The solution was then homogenized in a Polytron homogenizer for 45 seconds at a speed adjustment of 3. The cream composition, once homogenized, was cooled to approximately 50 ° C and homogenized • a second time at the same speed and at the same conditions weather. The cream composition was then assorted in individual containers and cooled to room temperature. When applied topically, the cream composition had a soft, non-greasy, desired feel to the touch, with a consistency similar to that of whipped cream. The cream composition provided very good skin moisturization and emolliency. Alternatively, a water-soluble, fat-free version of the cream may also be provided. In a composition of this type, the levels of ß-D-glucan and the other water-soluble components would be increased, and the petrolatum base would not be present. The concentration ranges of the examples given above would remain applicable. A useful gel composition of the invention, including the active ingredient, the β-D-glucan derived from cereal, is as follows:
ß-D-glucan derived from cereal approx. 0.5 - 15% water approx. 80 - 98% polyvinyl alcohol approx. 0.5 - 4% xanthan gum and / or CMC approx. 0.5 - 4% other suspension agent (s) approx. 0 - 4% antimicrobial agent (s) approx. 0.1 - 1%
Other agent (s) for increase in suspension / viscosity that can be added include carrageenan, agarose, alginate, carbomer thickener 940MR, and guar gum, at concentrations of each individual agent at approximately 0.01-4%. The use of xanthan gum and / or CMC is particularly advantageous to produce a clear, colorless gel. In addition, one or more emulsifying / solubilizing agents such as triethanolamine may be added at about 2 percent each. In addition, a chelating agent such as the ethylenediamine tetraacetic acid (EDTA) can be added to approximately 0.1-0.5 percent, generally as its tetrasodium salt. Thus, a more preferred embodiment of the gel composition comprises:
ß-D-glucan derived from cereal approx. 2.0% p / p polyvinyl alcohol approx. 2.0% w / w triethanolamine approx. 2.0% w / w carboxymethylcellulose (CMC) approx. 2.0% w / w additional suspension agent approx. 0.4% p / p
EDTA ca. 0.2% p / p methylparaben approx. 0.2% p / p propylparaben approx. 0.2% w / w water (at least 80%) the remainder A preferred additional suspending agent is Carbopol ™ 940 carbomer, added at approximately 0.5 percent.
EXAMPLE B
HE. prepared a batch of 100 g of a gel composition of the invention, which has the following ingredients:
water (distilled) 92.9 g / 100 g ß-D-glucan derived from cereal (oats) 2.0 g / 100 g triethanolamine 2.0 g / 100 g carboxymethylcellulose (CMC) 1.0 g / 100 g polyvinyl alcohol 1.0 g / 100 g carbomer Carbopolm 940 0.5 g / 100 g (homopolymer of acrylic acid) ethylenediaminetetraacetic acid (EDTA) 0.2 g / 100 g methylparaben 0.2 g / 100 g propylparaben 0.2 g / 100 g
43.9 g of water (at room temperature) were placed in a vessel and stirred rapidly to produce a vortex at the bottom of the vessel. The heavy carbomer was then siphoned into the stirred water until it completely dissolved. The remaining dry ingredients were then added to the container while stirring, to achieve a uniform mixture / solution. The appropriate amount (50.0 g) of the cereal-derived β-D-glucan solution (oat) of Example A was added to the vessel, and the mixture was liquefied at 85-90 ° C with constant stirring until all the ingredients they dissolved and the solution was homogeneous. The gel composition was allowed to cool to room temperature, and was dispensed into individual containers. The gel composition produced by this method had a soft feel to the touch with high wetting properties and emollient properties. An oil-based topical composition containing the cereal-derived β-D-glutane can be formulated. In this composition, the solvent of the basic cream or of the gel formulation is changed to mainly make an oil or a mixture of oils. The water content is reduced to compensate for the increased concentrations of the oils. The other ingredients can remain the same or be varied, as desired. In the oil composition, the solvent may comprise, for example, all or all of the oils, or a mixture of oil and water, where the oily fraction is generally greater than the aqueous fraction. However, the preferred forms of topical compositions for the treatment of burns and wounds are, to this date, the cream and gel formulations. In a method of the invention, for the management of burns and wounds, the composition can be topically applied to the area of the damaged tissue. the glucan-containing cream or gel of the invention provides emollient, soothing, moisturizing, anti-pruritic and softening dermal protection, and biologically derived, to aid during the skin recovery process. The treatment comprises: 1. the perfect cleaning of the burned area or site of tissue destruction; 2. the topical liberal application of the topical composition to the affected area; and 3. the repeated application of the composition until the cure is complete. The method is useful for managing scars due to burns, wounds or surgery, and the cream or gel is applied topically to the affected hypertrophic or keloid scar. The topical composition provides faster healing of burns or wounds, moisturizing relief for skin dryness and irritation, and a reduction in itching. The active ingredient, the β-D-glucan derived from the cereal, can also be a biological response modifier, for example a macrophage stimulator.
Claims (47)
1. A topical composition for application to the skin and mucosa for burns and wounds and other damages and skin loss conditions, comprising the β-D-glucan derived from cereal as an ingredient in one of a cream base, base of gel and oil base.
2. The topical composition of claim 1, wherein the β-D-glucan derived from cereal is derived from one of oats, wheat and barley.
3. The topical composition of claim 1, wherein the β-D-glucan derived from cereal is derived from oats.
4. The topical composition of claim 1, wherein the cereal derived β-D-glucan is characterized as (1-3) (1-4) -β-D-glucan.
5. The topical composition of claim 1, wherein the β-D-glucan derived from cereal comprises about 0.5 to 15 percent w / w, of the topical composition.
6. The topical composition of claim 1, wherein the cereal derived β-D-glucan comprises about 2-8 percent w / w of the topical composition.
7. The topical composition of claim 1, wherein the composition is a "cream, the composition comprising: β-D-glucan derived from cereal at about 0.5-1.5 percent w / w; a solvent including at least about water 50 percent w / w of the composition, an ointment base of at least about 10 percent w / w, a humectant, a stiffening agent, an emulsifying / solubilizing agent, a suspending agent / viscosity, an antimicrobial agent and a plasticizer.
8. The topical composition of claim 7, wherein the solvent comprises at least 50 percent w / w of the topical composition.
9. The topical composition of claim 7, wherein the solvent includes oil, at a concentration of up to about 20 percent w / w of the topical composition.
10. The topical composition of claim 7, wherein the oil comprises one or more of cod liver oil, mineral oil, shark liver oil, and glycerol.
11. The topical composition of claim 7, wherein the ointment base comprises one of white petrolatum and lanolin.
12. The topical composition of claim 7, wherein the humectant comprises propylene glycol.
13. The topical composition of claim 7, wherein the stiffening agent is selected from a group comprising cetyl alcohol and paraffin.
14. The topical composition of claim 7, wherein the emulsifying / solubilizing agent is selected from a group including sodium lauryl sulfate and triethanolamine.
15. The topical composition of claim 7, wherein the suspending agent / viscosity is selected from the group consisting of polyvinyl alcohol, agarose, alginate, xanthan gum, gum gum, carboxymethylcellulose, and Carbopol 940MR carbomer.
16. The topical composition of claim 7, wherein the antimicrobial agent is selected from the group comprising methylparaben, ethylparaben, butylparaben, and propylparaben.
17. The topical composition of claim 7, wherein the plasticizer is selected from some of glycerol and propylene glycol.
18. A composition of a topical cream for multiple purposes, comprising: water at least 50% w / w white petrolatum approx. 10-20% w / w glycerol approx. 5-20% w / w propylene glycol ca. 2 - 6% w / w cetyl alcohol (approx 0.5 - 6% w / w hexadecanoic acid) ß-D-glucan derived from cereal approx. 0.5 - 15% w / w triethanolamine approx. 0.5% w / w sodium lauryl sulphate approx. 0.1 - 5.0% p / p antimicrobial agent approx. 0.1 - 2% w / w, and i-agarose approx. 0.01 - 0.5% p / p
19. The composition of claim 18, further comprising xanthan gum at about 0.1-4.0%.
20. The composition of claim 18, wherein the antimicrobial agent is selected from the group of parabens including methylparaben, ethylparaben, butylparaben and propylparaben.
21. A composition of a topical cream for the treatment of burns and wounds, which comprises: white petrolatum approx. 15% w / w glycerol approx. 10% w / w propylene glycol approx. 4% w / w cetyl alcohol (hexadecanoic acid) approx. 2% p / p ß-D-glucan derived from cereal approx. 1 - 15% w / w triethanolamine approx. 2% w / w sodium lauryl sulphate approx. 1% p / p parabens approx. 0.4% w / w suspension enhancing agent / approx. 0.1 - 8.0% viscosity p / p solvent the remainder wherein the solvent comprises approximately 50-70 percent w / w of water and. about 0-20 percent w / w oil of the composition; and wherein the suspension / viscosity enhancing agent includes at least one of polyvinyl alcohol and xanthan gum.
22. The topical composition of claim 1, wherein the composition is a cream, the composition comprises: β-D-glucan derived from cereal of about 0.5 - 15 percent w / w; a solvent that includes water, at about at least 50 percent w / w of the composition; a humectant; a stiffening agent, an emulsifying / solubilizing agent; a suspension / viscosity increasing agent; an antimicrobial agent; and a plasticizer.
23. The topical composition of claim 1, wherein the composition is a gel having a gel base including water and at least one suspending agent / viscosity.
24. The topical composition of claim 1, wherein the composition is a gel having a water base including at least about 80 percent w / w of water.
25. The topical composition of claim 23, wherein the topical composition includes: water ca. 80 - 98% w / w increasing agent (s) of approx. 0.5 - 8.0% suspension / viscosity p / p.
26. The topical composition of claim 25, wherein the suspension / viscosity enhancing agent (s) comprises at least one of a group including polyvinyl alcohol, carboxymethyl cellulose, and xanthan gum.
27. The topical composition of claim 25, wherein the suspension / viscosity enhancing agents comprise polyvinyl alcohol plus another.
28. The topical composition of claim 25, further comprising triethanolamine at about 0.1-5.0% w / w.
29. The topical composition of claim 25, further comprising a chelating agent at about 0.01-1.0% w / w.
30. The topical composition of claim 25, further comprising an antimicrobial agent.
31. The topical composition of claim 27, wherein the other suspension enhancing agent / Viscosity comprises one of xanthan gum, agarose, alginate, guar gum, carboxymethylcellulose, and CarbopolMR 940 carbomer.
32. A multi-purpose topical gel composition, comprising: water ca. 80 - 98% p / p ß-D-glucan derived from cereal approx. 0.5 - 15% w / w triethanolamine approx. 0.1 - 5.0% w / w carboxymethylcellulose approx. 0.01 - 2.0% w / w polyvinyl alcohol approx. 0.5 - 4% w / w carbomer approx. 0.01 - 2.0% p / p EDTA ca. 0.01 - 1.0% p / p paraben (s) approx. 0.1 - 2.0% p / p
33. The composition of claim 33, wherein the β-D-glucan derived from cereal is derived from one of oats and barley.
34. The composition of claim 32, wherein the β-D-glucan derived from cereal is characterized as (1-3) (1-4) -β-D-glucan.
35. The composition of claim 32, wherein the β-D-glucan derived from cereal is characterized by having a number of (1-4) -glucopyranosyl bonds equal to about 1.5 to 3.0 times the number of bonds (1-3) - glucopyranosyl.
36. A multi-purpose topical gel composition, comprising: water ca. 92.9% p / p ß-D-glucan derived from cereal approx. 2.0% w / w triethanolamine approx. 2.0% p / p carboxymethylcellulose approx. 1.0% w / w polyvinyl alcohol approx. 1.0% p / p carbomer Carbopol 940 approx. 0.5% p / p EDTA ca. 0.2% p / p methylparaben approx. 0.2% p / p propylparaben approx. 0.2% p / p
37. The composition of claim 36, wherein the glucan derived from cereal is oat derived.
38. The composition of claim 36, wherein the cereal derived glucan is characterized as (1-3) (1-4) -β-D-glucan.
39. A topical composition for burns, wounds and scarring of the skin and mucous membranes, wherein the composition contains 0.5-15% w / w of β-D-glucan derived from cereal, said composition is selectively formulated as one of the group comprising a ointment, cream, gel, emollient, oil and lotion.
40. A method for the treatment of burns and wounds, and other damages and conditions of skin loss, comprising the step of applying to the affected area of a patient's skin, a topical composition comprising cereal-derived β-D-glucan as an active ingredient.
41. The method of claim 40, wherein the topical composition comprises one of a cream base, a gel base and an oil base. - -
42. The method of claim 40, wherein the β-D-glucan derived from cereal is derived from one of barley, oats and wheat.
43. A method for the treatment of burns and wounds and other damages and conditions of skin loss, comprising the step of applying to the affected area of a patient's skin, a topical composition comprising ß-D-glucan derived from cereal, characterized as (1-3) (1-4) -β-D-glucan as the active ingredient.
44. A method for the treatment of burns and wounds and other damages and conditions of skin loss, comprising the steps of: perfectly cleaning a wound area of damaged tissue; applying to the wound a topical composition comprising a β-D-glucan derived from cereal as the active ingredient; and the repetition of the application of the topical composition until the healing is complete.
45. A method of treating burns and wounds and other damages and loss conditions of the skin, comprising the steps of: perfectly cleaning a wounded area of damaged tissue; the application of a topical composition comprising a β-D-glucan derived from cereal, characterized as (1-3) (1-4) -β-D-glucan as the active ingredient; and the repeated application of the topical composition until the cure is complete.
46. A method of treating burns and wounds and other damages and conditions of skin loss, comprising the steps of: perfectly cleaning a wounded area of damaged tissue; applying to the wound, a topical composition comprising a β-D-glucan derived from cereal as the active ingredient; and the repetition of the application of the topical composition.
47. A method of treating burns and wounds and other damages and conditions of skin loss, comprising the steps of: perfectly cleaning a wounded area of damaged tissue; applying a topical composition comprising a β-D-glucan derived from cereal; characterized as (1-3) (1-4) -β-D-glucan as the active ingredient; -and repeat the application of the topical composition.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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US08957529 | 1997-10-24 |
Publications (1)
Publication Number | Publication Date |
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MXPA00003316A true MXPA00003316A (en) | 2002-02-26 |
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