US 2114370 A
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Patented Apr. 19, 1938 UNITED STATES PATENT OFFICE .AGENT FOR. THE TREATMENT OF MUCOUS SURFACES Frank J. Bickenheuser,
Tulsa, Okla", assignor, by
Application May 26, 1937,
serial No. 144,961
The present invention relates to topical medicines containing, as a vehicle, a liquid oily material which has the property of mixing with water or with moist secretions of the mucous surfaces 5 of the human body, to produce a jelly-like mass,
which will be capable of readily adhering to wet mucous surfaces, for any desired period of time.
vehicle, a suitable antiseptic material, and a widevariety of antiseptic materials can be used, and
in widely varying amounts, so long as the said antiseptic can be gotten into solution in the said vehicle.
The following is given as the for use in the present case- 2 preferred vehicle Volume Triethanolamine 1 26 Oleic arid 3 Purified mineral oil 3.5
,The amount of the oleic acid can be varied, usually between 2.5. and 3.5 volumes, and the amount of the mineral oil can be varied, usually between 3 and 4 volumes. But even somewhat wider variation in the proportions may be advantageous in some instances. In place of the above mineral oil, it is often advisable to employ 35 a mixture of mineral oil and a fatty oil, to thereby iorm jellies of different consistencies, suitable for some specific purpose. substitution. one part of mineral oil can readily be replaced by about 1.2 to 1.4 parts of fatty oil.
In general the ratio of the total amount of the oil used (petroleum oil with or without fatty oil) to the combined amount of triethanolamine and free oleic acid (or triethanolamine oleate) is between 0.75:l and 1.2:1. Variation in these ratios 45 modifies the properties of the Jelly, i. e. softness,
toughness, adherence to mucous surfaces, elasticity. The petroleum oil is in excess over the fatty oil, it the latter is used, preferably in large excess.
I give the following classification of antiseptic components, as the term-is employed in the present' case, the term including substances which are directly antiseptic, as well as substances which when used in mixtures of the type set forth 5 become antiseptic or which liberate or form or In making this generate or produce or are converted into substances which have antiseptic activity. In this classification I also give a convenient mode of putting the said antiseptic material into solution, dispersion or quasi-solution, and I also give a convenient safe, effective and practical percentage of the antiseptic substances, based on the amount of the vehicle (these being illustrative, without limiting the invention thereto, except as specified in the appended claims) (1) Elemental sulphur (in triethanolamine at 120 F.). 10%.
(2) Elemental iodine (in triethanolamine at 120 F.). 0.02%.
(3) Phenolic bodies, suitable effective examples being phenol (carbolic. acid) and cresol (or cresylic acid). These'can be dissolved in triethanolamine at 90 to 120? F. 0.1% to 0.2%.
(4.) Resorcin and its derivatives, e. 3. highamples being bismuth beta naphtholate and blsmuth tribromphenate and potassium sodium bismutho-tartrate which can be dissolved in oleic acid at 105 F. to 110 F. 2%.
(5d) Metallo-organic aluminum compounds,-
examples being aluminum phenol-sulphonate and aluminum betaenaphthol-disulphonate, which can be dissolved in oleic acid at 105 F. 1%.
(5e) Metallo-organic compounds of antimony,' an example being antimony thio-glycol-amide,
which can be dissolved in the mineral oil at room temperature, say 75 F. 0.2% is suitable.
(6) Such chlorine compounds as para-sulphondichlor-amido-benzolc acid or para-toluene-sulphon-dlchlor-amide, which can be dissolved in triethanolamine at 80 F. 2%.
(7) As compounds of oxy-quinolin, suitable for use, I mention the sulphate or benzoates of oxyquinolin, which can be dissolved in the oleic acid at 84 F. 2%.
(8) Typical of the sulphur compounds effective for the purpose is ammontium sulpho-ichthyolate which can be dissolved in triethanolamine at 120 F. Or it can be dissolved in the mineral oil. Up to about 10% can be used.
(9) Trichloro-organic compounds containing an OH group, examples being trichioro-butyl alcohol and trichloro-phenol. These can be dissolved in triethanolamine at 80 F. 2%.
(10) Antiseptically active dyes containing the methyl group, examples being 3:6 diamino-IO- methyl-acridinum chloride mono-hydrochloride and pentaand hexa-methyl-para-rosaniline. These can be dissolved in oleic acid at 80 C. 0.1%.
(11) Organic iodine compounds other than iodo-benzoic acid, an example being di-iodohydroxy-propane or diiodhydrine, or also iothion, which can be dissolved in triethanolamine at 120 F. .2%.
(12) Fatty acid esters of phenolic bodies, such as cresyl acetate can be used, dissolved in the mineral oil at room temperature. 0.1%.
All of the above mentioned compositions, can be used for the treatment of vaginal disorders, one or the other being more suitable, depending upon the organisms present, causing the trouble. Thus for instance the arsenic compounds are highly suitable for the treatment of tricomonas vaginalis, the elemental iodine and the organic iodine compounds would be suitable to use in cases of cervical erosion and vaginalis, the resorcin derivatives being suitable as hygienic cleansers, and for application against minor infections.
The preferred way of compounding the medicines is similar in all cases, namely first dissolve the antiseptic in the particular one of the components referred to above, after which the oleic acid is well mixed with the mineral oil, and the triethanolamine subsequently added and well mixed. In producing the medicine, the following hasbeen found to be the most advantageous procedure. The oleic acid may first be warmed up, say to about 120 F., and the mineral oil is then added, and the mixture well stirred for 10 or 15 minutes. After this the triethanolamine is added and well stirred, for 10 minutes or up to onehalf hour. The addition of the triethanolamine first gives a somewhat milky mixture, and upon continuing the stirring, the mass becomes thoroughly clear; The stirring is preferably continued until the solution has become clear, and the reactions will have been sufllciently completed when the solution has become clear. The fatty oil, if this is to be employed, can be previously mixed with the mineral oil, or can be added to the mixture after addition of the mineral oil. -It will be understood that in the above formula, for the preparation of the medicine, it is immaterial (from the standpoint of procedure) which one of the components of the vehicle contains the antiseptic, and it will be further understood that water is not added to the material or to the finished medicine, and it is important that the components be free from moisture. In making up the medicine, it is advisable particularly in wet weather or when the atmosphere is highly charged with moisture, to put the completed medicine into a sealed receptacle, for example into the collapsible metal tube in which it is to be shipped and sold promptly after preparation. It is important also that the components be used in a substantially or completely anhydrous condition, in or-= .acids such as stearic.
der to get a mixed oil having a considerable ailinity for moisture, and freely liquid.
The completed medicine is in all cases a viscous oily liquid, the color depending upon the particular antiseptic employed.
In the above formula, oleic acid was referred to. It will be understood that for producing a mixture of higher viscosity, a small amount of the oleic acid can be substitutedby solid fatty I would not ordinarily recommend substituting more than one-fifth of the oleic acid by stearic.
The medicinal mineral oil can be the widely used variety sold as a mild laxative, being a water-white liquid, having a specific gravity of about 0.84, and a Saybolt viscosity at 100 C. about 150, and free from unsaturated constituents. Other similar oils can be used.
The fatty oil, e. g. cottonseed oil or olive oil if used, may be the usual well refined dehydrated edible grades. In place of these oils, other well refined liquid fatty oils can be used, for example soybean oil, peanut oil, sesame oil, perilla oil or the like, all preferably in the well refined dehydrated condition and substantially free from odors. If the fatty oil used contains considerable free fatty acid, slightly more of the said oil and slightly less of the oleic acid can be suitably employed. The use of the well refined oil and of the well refined free fatty acid are however more desirable, as giving a product more free forms a mass of jelly-like consistency which strongly adheres to wet mucous surfaces,
The action of the oily medicine when it is brought into contact with water (or aqueous liq uids) containing bacteria or other living vmicroorganisms, has been carefully studied, under the microscope. The oily material bursts into the aqueous liquid forming billows of soft jelly-like consistency drawing into-itself these micro-organisms, to completely envelop the same. Following this action, the jelly stiffens somewhat imprisoning the said micro-organisms, which are thereby destroyed. This action takes place irrespective of what forms of micro-organisms are whether coll-bacillus, staphylococci, spirochaetae, streptococci, spores, spermatazoa or various mixed cultures, or in fact any living organisms. The oily mixture made in substantially the above proportions, has an affinity for water, or in other words, is hydrophilic" and the Jelly formed is a hydrophilic colloid.
The medicine is particularly advantageous for application to mucous surfaces of the vagina from which liquids are being exuded, whether in normal healthy condition or in a diseased condition.
In the above description of the complete medicine I have described the use of one or more of a considerable number of antiseptic substances, which are suitable for use, as antiseptics. In some instances, the vehicle alone without the addition of the antiseptic substances, or any of them, can be employed. Thus for instance, the vehicle alone, i. e. without the addition of any antiseptic substances thereto, can be used as a vaginal cleanser, or for clearing up minor conditions where there is no deep-seated infection. For this purpose, a small quantity of the oily material, for example 3 to 10 cc. of the same can be introduced into the vagina, and allowed to read:
with the secretion therein, and form the'jellylike mass as referred to above. of the said jelly of course picks up any bacteria or other organisms present or introduced, as well' as solid materials, debris or other foreign matter, all of which would be removed on flushing out with a warm water douche, the jelly of course carrying away with it any solids or bacteria contained therein.
The vehicle itself, either with or without the addition of antiseptic substances, is also suitable for application to burns or to other skin affections in which there is a more or less great amount of discharge of watery excretions. The use of the material for this purpose is particularly suitable in cases where it is not desired to use bandages or the like, because the jelly-like mass formed will readily adhere to the skin, as well as to mucous surfaces, without the aid of any bandages, tampons, or the like. For this purpose, it will be obvious that no large amounts of water, or aqueous liquids are to be applied. This gives a protection over tender surfaces where there is an aqueous secretion.
No claim is made herein specifically on the use of iodobenzoic acid as the antiseptic in a vehicle containing fatty ofl, as described above, that subject matter being claimed in a copending case. Serial No. 124,135.
1. The herein described topical antiseptic medicine suitable for the treatment of vaginal disorders, which is iree from water and adapted, upon coming into contact with aqueous secretions on mucous surfaces, to draw said secretions into itself, thereby forming a jelly-like mass which will readily adhere to said mucous surfaces, said medicine being in the form of a mobile oily liquid, having the appearance and consistency of a substantially clear liquid oil, and the vehicle of which medicine is composed essentially of an oil and the reaction product of triethanolamine and a higher fatty acid, the oil in said vehicle being composed in major part at least of a well purifled liquid petroleum oil, and the amount of said oil being over 0.75 and less than 1.2 times the combined amount of triethanolamine and said higher fatty acid, said vehicle carrying dissolved therein an antiseptic component other than iodobenzoic acid, such topical medicine, when applied to a mucous surface of the vagina form-.
ing thereon an adherent Jelly-like clinging mass. 2. The herein described topical antiseptic medicine suitable for treating vaginal disorders, which is free from water and adapted, upon coming into contact with aqueous secretions on mucous surfaces, to draw said secretions into itself, thereby forming a Jelly-libs mass which will readily adhere to Q medicinebeingintheformofamobilooilyliquid,
The formation having the appearance and consistency of a substantially clear liquid OH, and the vehicle of which medicine is composed essentially of an oil and the reaction product of triethanolamine and a higher fatty acid, the oil in said vehicle being composed in-major part at least of a well purified liquid petroleum oil, and the amount of said oilbeing over 0.75 and less than 1.2 times the combined amount of triethanolamine and said higher fatty acid, said vehiclev carrying dissolved therein a metallo-organic compound of mercury as an antiseptic, such topical medicine, when applied to a mucous'surface of the vagina forming thereon an adherent jelly-like clinging mass.
3. The herein described topical antiseptic medicine suitable for the treatment of vaginal disorders, which'is free from water and adapted, upon coming into contact with aqueous secretions on mucous surfaces, to draw said secretions into itself, thereby forming a jelly-like mass which will readily adhere to said mucous surfaces, said medicine being in the form of a mobile oily liquid,
' having the appearance and consistency of a substantially clear liquid oil, and the vehicle of which medicine is composed essentially of an oil and the reaction product of triethanolamine and a higher fatty acid, the oil in said vehicle being composed in, major part at least of a well purified liquid petroleum oil, and the amount of said oil being over 0.75 and less than 1.2 times the combined amount oftriethanolamine and said higher fatty acid, said vehicle carrying dissolved therein a phenolic body as an antiseptic, such topical medicine, when applied to a mucous surface of the vagina forming thereon an adherent jelly-like clinging mass. v
4. A topical antiseptic medicine as covered in claim 1, in which the oil present is a mixture of a well purified petroleum oil and a fatty oil, theformer being in excess over the latter.
5. The herein described topical agent adapted for the treatment of vaginal disorders, which is free from water and adapted, upon coming into contact with aqueous secretions on mucous surfaces of the vaginal cavity, to draw said secretions into itself together with any extraneous solids and organisms therein, thereby forming a jelly-like mass which will readily adhere to said mucous surfaces, said agent being in the-form of a mobfle oily liquid, having the appearance and consistency of a substantially clear liquid oil, and composed at least largely of an oil and the reaction product of trietbanolamine and a higher fatty acid, the oil in said agent being composed in major part at least of a well purified liquid petroleum oil, and the amount of said oil being over 0.75 and below 1.2 times the combined amount of triethsnolamine and'said higher fatty FRANK J. BICKENI-IEUSER.
said mucous surfaces, sci