US2221139A - Preparation of medicaments - Google Patents

Preparation of medicaments Download PDF

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Publication number
US2221139A
US2221139A US265203A US26520339A US2221139A US 2221139 A US2221139 A US 2221139A US 265203 A US265203 A US 265203A US 26520339 A US26520339 A US 26520339A US 2221139 A US2221139 A US 2221139A
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composition
skin
cellulose
oil
ester
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US265203A
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Gordon D Hiatt
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Eastman Kodak Co
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Eastman Kodak Co
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Priority to US265203A priority Critical patent/US2221139A/en
Priority to US337677A priority patent/US2249523A/en
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Publication of US2221139A publication Critical patent/US2221139A/en
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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38Cellulose; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/29Titanium; Compounds thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/37Esters of carboxylic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/73Polysaccharides
    • A61K8/731Cellulose; Quaternized cellulose derivatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/70Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7015Drug-containing film-forming compositions, e.g. spray-on
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings

Definitions

  • This invention relates to the preparation of medicaments and more particularly to a protective composition for coating the skin to prevent dermatitis, and for improving the appearance of the skin.
  • Dermatitis may be'caused by mechanical abrasions, exposure to physical conditions such as extremes of heat or cold, or exposure to chemicals such as solvents, desiccants, dissociation solutions, protein precipitating chemicals and those which cause interference with intracellular metabolism.
  • a protective cream or coating refers to a substance which is applied to the individuals skin for the purpose of giving an impermeable coating thus preventing actual contacts with the substance or substances to which he is exposed.
  • a protective cream or coating usually the hands and forearms are the parts of the body so protected, but occasionally other portions require this type of coating. In some instances gloves are worn over the protective coating.
  • the compound to prevent dermatitis that it is an excellent undercoating for make up and may be colored corresponding to the color of the skin taken with the oil or fat will dissolve the cellulose to form a composition for covering skin blemishes such as birth marks or other disfigurements. It also appears that the composition may be employed in war times to offset the harmful effect on the skin caused by poison gas such as mustard I gas or other such irritating gases.
  • An object of the present invention is a composition for preventing dermatitis.
  • Another object of the invention is a composition for preventing dermatitis caused by aqueous 10 photographic developer solutions.
  • Still another object is a protective coating composition to prevent mustard gas and similar gases from attacking the skin.
  • a still further object is such a composition 18 which will be relatively non-greasy as well as waterproof and will contain no substances which would fog or otherwise damage photographic film if maintained out of actual contact therewith.
  • Still another object is a composition which may be employed as an undercoating for make up.
  • Another object is a composition which when suitably colored may be employed to cover skin blemishes.
  • a gel composition in the form of a salve containing as the basic ingredients a cellulose ester, the acyl radical of which contains four or more carbon atoms such as butyryl or higher or if there is some acetyl in the cellulose derivative, it will be in the minority, and a skin softening vegetable oil or animal fat.
  • the composition also contains a suitable high boiling solvent and may also contain suitable pigments.
  • the composition may be prepared by heating the particular oil or fat up to a point at which the cellulose organic acid ester becomessolubletherein and then causing the ester'to become thoroughly mixed in the oil. If a high boiling solvent and/or a pigment is required it may also be suitably incorporated in the composition at this time.
  • the cellulose organic acid esters employed must be those which will dissolve in the oil or fat, or mixture of the oil or fat and high boiling solvent, at higher temperatures and the mixture must gel on cooling. If a high boiling solvent is employed it must, therefore, be one which when 50 derivative at an elevated temperature, and form the gel or salve-like composition at room temperatures. Of course the solvent, when mixed in with the remaining compositions should have no harmful effects on the skin.
  • the preferred skin softening and protecting oils are those having an iodine number less than 125 such as olive oil, cotton seed oil, palm oil, corn oil and peanut oil and fish oils and fats such as lard and tallow.
  • suitable oils or fats having such properties may be employed.
  • the preferred cellulose compounds are cellulose organic acid esters containing higher v acyl groups of four or more carbon atoms, such as cellulose butyrate, or mixed esters such as cellulose acetate stearate and cellulose acetate palmitate stearate, cellulose acetate caproate the total acyl content in all cases being not less than about 50%.
  • the mixed esters contain from approximately 20 to 55% of the higher acyl.
  • the preferred high boiling solvents are: methyl stearate, butyl stearate, diglycol laurate, and di-' butyl phthalate.
  • other high boiling solvents which have a solvent action on the above described cellulose esters may be employed.
  • the greaslness may be further reduced by adding pigments such as zinc oxide and titanium dioxide to the composition.
  • Example I 1 part of cellulose tributyrate is heated with three parts of butyl stearate to a temperature of 160 C. in a suitable receptacle. After thorough incorporation, the mixture is cooled to room temperature and a smooth firm gel results. This gel or salve may be freely used on the hands to prevent dermatitis from aqueous developer solutions.
  • Example II The following composition is particularly 50 valuable for prevention of dermatitis caused by aqueous developer solutions.
  • a mixture of 33 pounds of olive oil and 22 pounds of butyl stearate is stirred in a 15 gallon stainless steel tank and heated with two internal 55 electric coils. At a temperature of 130 0., 11
  • heating and mixing period extends over about 3 hours.
  • the mixture gels at about 90 C. and is easily spread at normal room temperatures and when in contact with the warmth oi. the skin.
  • Example IV Example V The following composition which can also be made by the method described in Example III is also a very good preparation for prevention of dermatitis.
  • Example VI A composition suitable for use as a base for make up or to cover up skin blemishes or as a lip stick preparation may be made by replacing a portion or all of the zinc oxide in Example V by suitable colored pigments such as ochres, umbers and siennas. If other colored compositions are desired pigments such as the ultramarines or various colored lakes may be employed.
  • suitable colored pigments such as ochres, umbers and siennas. If other colored compositions are desired pigments such as the ultramarines or various colored lakes may be employed.
  • Example VII The following compositions may also be made by the method described in Example III and may be employed to protect the skin from chemical irritants.
  • a salve-like composition for coating the skin essentially consisting of a cellulose organic acid ester having an acyl content of at least 50% of the weight of the cellulose ester of which a major portion is fatty acid groups of at least 4 carbon atoms and a.- miscible vegetable oil having an iodine number not greater than 125.
  • a salve-like composition for coating the skin essentially consisting of a cellulose organic acid ester having an acyl content of at least 50% of the weight of the cellulose ester of which a major portion is fatty acid groups of at least 4 carbon atoms, a miscible vegetable oil, a high boiling solvent for the ester, and a pigment.
  • a salve-like composition for coating the skin essentially consisting of a cellulose organic acid ester having an acyl content of at least 50% of the weight of the cellulose ester of which a major portion is fatty acid groups of at least 4 carbon atoms and olive oil.
  • a salve-like composition for coating the skin essentially consisting of a cellulose organic acid ester having an acyl content of at least 50% of the weight of the cellulose ester of'which a major portion is fatty acid groups of at least 4 carbon atoms and cottonseed oil.
  • a salve-like composition for coating the skin essentially consisting of a cellulose organic acid ester having an acyl content of at least 50% of the weight of the cellulose ester of which a major portion is fatty acid groups of at least 4 carbon atoms and palm oil.
  • a salve-like composition for coating the skin essentially consisting of a cellulose organic acid ester having an acylcontent of at least 50% of the weight of the cellulose ester of which a major portion is fatty acid groups of at least 4 carbon atoms, cottonseed oil, a high boiling solvent for the ester and a pigment.
  • a salve-like composition for coating the skin essentially consisting of a cellulose butyrate having a butyryl content of at least 50% of the weight of the ester, butyl stearate, olive oil and titanium dioxide.
  • a salve-like composition for coating the skin essentially consisting of a cellulose butyrate having a butyryl content of at least 50% of the weight of the ester, butyl stearate, olive oil and a colored pigment.
  • a salve-like composition for coating the skin essentially consisting of cellulose acetate stearate having an acyl content of at least 50% of the weight of the cellulose ester and a stearyl content of 20 to 55% of the weight of the cellulose ester, butyl stearate, cottonseed oil and zinc oxide.
  • a salve-like composition for coating the skin essentially consisting of cellulose acetate stearate having an acyl content of at least 50% of the weight of the cellulose ester and a stearyl content of 20 to 55% of the weight of the cellulose ester, butyl stearate, olive oil and titanium dioxide.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Birds (AREA)
  • Inorganic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Emergency Medicine (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Cosmetics (AREA)

Description

Patented Nov. 12, 1940 UNITED STATES PATENT or ice PREPARATION OF MEDIOAMENTS Gordon D. Hiatt, Rochester, N. Y., assignor to Eastman Kodak Company, Rochester, N. Y., a corporation of New Jersey No Drawing.
Application March 81, 1939,
Serial No. 265,203
10 Claims This invention relates to the preparation of medicaments and more particularly to a protective composition for coating the skin to prevent dermatitis, and for improving the appearance of the skin.
Dermatitis or inflammation of the derma or true skin is a serious industrial problem. Industrial dermatitis, according to various Compensation Board Reports, accounts for 50 to 60% of the industrial diseases (excluding accidents). The obvious cause of industrial dermatitis in the majority of instances is contact of some industrial product such as a solid, liquid or vapor with the skin surface. Prevention of dermatitis, in those instances, therefore, depends largely upon preventing this harmful contact.
Dermatitis may be'caused by mechanical abrasions, exposure to physical conditions such as extremes of heat or cold, or exposure to chemicals such as solvents, desiccants, dissociation solutions, protein precipitating chemicals and those which cause interference with intracellular metabolism.
In large photographic plants where one group of people may spend a considerable part of their day working with photographic developers, dermatitis caused by the developers is a serious problem, unless proper precautions are observed. Obviously this is undesirable since it lowers the emciency of the employee and may provide the entrance for a more serious disease.
One of the important methods used in preventing contact with harmful chemicals is the employment of a protective cream or coating. This refers to a substance which is applied to the individuals skin for the purpose of giving an impermeable coating thus preventing actual contacts with the substance or substances to which he is exposed. Usually the hands and forearms are the parts of the body so protected, but occasionally other portions require this type of coating. In some instances gloves are worn over the protective coating.
There are several commercial preparations available on the market, but most of these compositions were found to be inadequate to protect the skin against exposure to aqueous developer solutions, and the present invention, therefore, is the outcome of considerable experimental work and study to discover a composition suitable for this purpose.
I have also found that in addition to employing I the compound to prevent dermatitis that it is an excellent undercoating for make up and may be colored corresponding to the color of the skin taken with the oil or fat will dissolve the cellulose to form a composition for covering skin blemishes such as birth marks or other disfigurements. It also appears that the composition may be employed in war times to offset the harmful effect on the skin caused by poison gas such as mustard I gas or other such irritating gases.
An object of the present invention is a composition for preventing dermatitis.
Another object of the invention is a composition for preventing dermatitis caused by aqueous 10 photographic developer solutions.
Still another object is a protective coating composition to prevent mustard gas and similar gases from attacking the skin.
A still further object is such a composition 18 which will be relatively non-greasy as well as waterproof and will contain no substances which would fog or otherwise damage photographic film if maintained out of actual contact therewith.
Still another object is a composition which may be employed as an undercoating for make up.
Another object is a composition which when suitably colored may be employed to cover skin blemishes.
In accordance with the invention these and other objects are accomplished by preparing and employing a gel composition in the form of a salve containing as the basic ingredients a cellulose ester, the acyl radical of which contains four or more carbon atoms such as butyryl or higher or if there is some acetyl in the cellulose derivative, it will be in the minority, and a skin softening vegetable oil or animal fat. Preferably the composition also contains a suitable high boiling solvent and may also contain suitable pigments.
The composition may be prepared by heating the particular oil or fat up to a point at which the cellulose organic acid ester becomessolubletherein and then causing the ester'to become thoroughly mixed in the oil. If a high boiling solvent and/or a pigment is required it may also be suitably incorporated in the composition at this time.
The cellulose organic acid esters employed must be those which will dissolve in the oil or fat, or mixture of the oil or fat and high boiling solvent, at higher temperatures and the mixture must gel on cooling. If a high boiling solvent is employed it must, therefore, be one which when 50 derivative at an elevated temperature, and form the gel or salve-like composition at room temperatures. Of course the solvent, when mixed in with the remaining compositions should have no harmful effects on the skin.
The preferred skin softening and protecting oils are those having an iodine number less than 125 such as olive oil, cotton seed oil, palm oil, corn oil and peanut oil and fish oils and fats such as lard and tallow. However, other suitable oils or fats having such properties may be employed.
Since these oils and fats have rather poor solvent power, the preferred cellulose compounds are cellulose organic acid esters containing higher v acyl groups of four or more carbon atoms, such as cellulose butyrate, or mixed esters such as cellulose acetate stearate and cellulose acetate palmitate stearate, cellulose acetate caproate the total acyl content in all cases being not less than about 50%. Preferably the mixed esters contain from approximately 20 to 55% of the higher acyl.
The preferred high boiling solvents are: methyl stearate, butyl stearate, diglycol laurate, and di-' butyl phthalate. However, other high boiling solvents which have a solvent action on the above described cellulose esters may be employed.
If the composition appears too greasy for the purpose desired, the greaslness may be further reduced by adding pigments such as zinc oxide and titanium dioxide to the composition.
The invention will be further understood by referring to the following examples whichdescribe preferred compositions for preventing dermatitis.
Example I 1 part of cellulose tributyrate is heated with three parts of butyl stearate to a temperature of 160 C. in a suitable receptacle. After thorough incorporation, the mixture is cooled to room temperature and a smooth firm gel results. This gel or salve may be freely used on the hands to prevent dermatitis from aqueous developer solutions.
Example II The following composition is particularly 50 valuable for prevention of dermatitis caused by aqueous developer solutions.
A mixture of 33 pounds of olive oil and 22 pounds of butyl stearate is stirred in a 15 gallon stainless steel tank and heated with two internal 55 electric coils. At a temperature of 130 0., 11
pounds of cellulose butyrate of 56% butyryl content is slowly added and the temperature is raised to 160 to 170 C. to complete the solution. The temperature may be allowed to rise to 190 to in- 60 sure homogeneity. The heat is then reduced, and 33 pounds of titanium dioxide ('fitanox) is added slowly with suitable mixing. The resulting creamy solution is drained into containers when the temperature has fallen to 120-130 C. The
heating and mixing period extends over about 3 hours. The mixture gels at about 90 C. and is easily spread at normal room temperatures and when in contact with the warmth oi. the skin.
Example IV Example V The following composition which can also be made by the method described in Example III is also a very good preparation for prevention of dermatitis.
Parts Cellulose acetate stearate 1 Butyl stearate 2 Cottonseed oil 2 Zinc oxide 2 The use of these compositions to prevent dermatitis from aqueous developer solutions has proved extremely satisfactory. The salve can be used on the hands with or without rubber gloves, and it will not fog the film being developed, provided it does not come in actual contact with it. This composition entirely lacks the greasy feel of the original oil or of the commercial compositions made with petrolatum, mineral oil, or lanolin. It also has excellent moisture resistance .and covering power as well as extended life on the skin.
Example VI A composition suitable for use as a base for make up or to cover up skin blemishes or as a lip stick preparation may be made by replacing a portion or all of the zinc oxide in Example V by suitable colored pigments such as ochres, umbers and siennas. If other colored compositions are desired pigments such as the ultramarines or various colored lakes may be employed.
Example VII The following compositions may also be made by the method described in Example III and may be employed to protect the skin from chemical irritants.
Parts Cellulose acetate stearate 1 Butyl stearate 2 Lard 2 Titanium dioxide 2 What is claimed is:
1. A salve-like composition for coating the skin essentially consisting of a cellulose organic acid ester having an acyl content of at least 50% of the weight of the cellulose ester of which a major portion is fatty acid groups of at least 4 carbon atoms and a.- miscible vegetable oil having an iodine number not greater than 125.
2. A salve-like composition for coating the skin essentially consisting of a cellulose organic acid ester having an acyl content of at least 50% of the weight of the cellulose ester of which a major portion is fatty acid groups of at least 4 carbon atoms, a miscible vegetable oil, a high boiling solvent for the ester, and a pigment.
3. A salve-like composition for coating the skin essentially consisting of a cellulose organic acid ester having an acyl content of at least 50% of the weight of the cellulose ester of which a major portion is fatty acid groups of at least 4 carbon atoms and olive oil.
4. A salve-like composition for coating the skin essentially consisting of a cellulose organic acid ester having an acyl content of at least 50% of the weight of the cellulose ester of'which a major portion is fatty acid groups of at least 4 carbon atoms and cottonseed oil.
5. A salve-like composition for coating the skin essentially consisting of a cellulose organic acid ester having an acyl content of at least 50% of the weight of the cellulose ester of which a major portion is fatty acid groups of at least 4 carbon atoms and palm oil.
6. A salve-like composition for coating the skin essentially consisting of a cellulose organic acid ester having an acylcontent of at least 50% of the weight of the cellulose ester of which a major portion is fatty acid groups of at least 4 carbon atoms, cottonseed oil, a high boiling solvent for the ester and a pigment.
7. A salve-like composition for coating the skin essentially consisting of a cellulose butyrate having a butyryl content of at least 50% of the weight of the ester, butyl stearate, olive oil and titanium dioxide.
8. A salve-like composition for coating the skin essentially consisting of a cellulose butyrate having a butyryl content of at least 50% of the weight of the ester, butyl stearate, olive oil and a colored pigment.
9. A salve-like composition for coating the skin essentially consisting of cellulose acetate stearate having an acyl content of at least 50% of the weight of the cellulose ester and a stearyl content of 20 to 55% of the weight of the cellulose ester, butyl stearate, cottonseed oil and zinc oxide.
10. A salve-like composition for coating the skin essentially consisting of cellulose acetate stearate having an acyl content of at least 50% of the weight of the cellulose ester and a stearyl content of 20 to 55% of the weight of the cellulose ester, butyl stearate, olive oil and titanium dioxide.
GORDON D. HIA'IT.
US265203A 1939-03-31 1939-03-31 Preparation of medicaments Expired - Lifetime US2221139A (en)

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US337677A US2249523A (en) 1939-03-31 1940-05-28 Medicament

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Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2618584A (en) * 1942-03-20 1952-11-18 Ralph L Evans Dichloramine compound solution
US2630399A (en) * 1946-05-31 1953-03-03 Marion B Sulzberger Chloramide skin protecting ointment
US2725335A (en) * 1945-11-02 1955-11-29 Wilbur A Lazier Chloroamide containing camouflage ointment
US20060062749A1 (en) * 2004-09-16 2006-03-23 Shelton Michael C personal care products incorporating cellulosic fatty acid esters
US20070053855A1 (en) * 2004-09-16 2007-03-08 Shelton Michael C Personal care products incorporating cellulosic fatty acid esters

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2618584A (en) * 1942-03-20 1952-11-18 Ralph L Evans Dichloramine compound solution
US2725335A (en) * 1945-11-02 1955-11-29 Wilbur A Lazier Chloroamide containing camouflage ointment
US2630399A (en) * 1946-05-31 1953-03-03 Marion B Sulzberger Chloramide skin protecting ointment
US20060062749A1 (en) * 2004-09-16 2006-03-23 Shelton Michael C personal care products incorporating cellulosic fatty acid esters
WO2006034071A1 (en) * 2004-09-16 2006-03-30 Eastman Chemical Company Personal care products incorporating cellulosic fatty acid esters
US20070053855A1 (en) * 2004-09-16 2007-03-08 Shelton Michael C Personal care products incorporating cellulosic fatty acid esters
JP2008513480A (en) * 2004-09-16 2008-05-01 イーストマン ケミカル カンパニー Personal care products containing cellulose fatty acid esters

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