US007575.

739B2

(12) United States Patent (10) Patent No.: US 7,575,739 B2

Tamarkin et al. (45) Date of Patent: Aug. 18, 2009

(54) FOAMABLE IODINE COMPOSITION 3,993,224. A 1 1/1976 Harrison

4,110,426 A 8, 1978 Barnhurst
(75) Inventors: Earl May,("Egon 4,124,149 A 1 1/1978 Spitzer et al.
riedman, Karmei Yosef (IL); Meir
Eini, Ness Ziona (IL)
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(58) Field of Classification Search .................... 424/43
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 US 7,575,739 B2
1. 2
FOAMABLE ODINE COMPOSITION U.S. Pat. No. 5,071,648 discloses a composition contain
ing acetalized polyvinyl alcohol complexed with iodine,
RELATED APPLICATIONS which releases free iodine in the presence of water.
WO 01/70242 discloses a composition including molecu
This application claims priority under 35 U.S.C. S 119(e) 5 lar iodine and tetraglycol (TG) that facilitates the dissolution
to co-pending U.S. application Ser. No. 60/466,094, filed Apr. of iodine, enhances its antiseptic effect, and remains stable in
28, 2003, and entitled "Foamable Iodine Compositions, the presence of water, in contrast to other iodine solvents,
which is incorporated in its entirety by reference. Such as ethanol, in which iodine precipitates after water addi
tion. Povidone-iodine complex (PVP-I) may also be dis
FIELD OF THE INVENTION 10 solved in TG or a TG water system. A pharmaceutically
acceptable vehicle according to WO 01/70242 includes an
The present invention relates to a foamable composition of oil/water or a water/oil emulsion, a solution, a Suspension, a
matter comprising iodine. The invention further relates to gel, an ointment, a patch, or an aerosol, preferably solutions,
compositions that, when provided in a Suitable foaming sys gels and washable ointments.
tem, evolve into foam, effective in the topical treatment of 15 Despite many years of usage in topical therapy, iodine
various skin conditions. compositions are still restricted to the conventional list of
dosage forms, consisting of water/oil emulsions, Solutions,
BACKGROUND OF THE INVENTION Suspensions, gels, ointments, patch, or aerosols. All these
preparations comprise liquid or semi-liquid Substances, hav
Iodine and iodine complex preparations are widely ing continuous texture and consistency and possessing spe
employed as disinfectants in human and Veterinary medicine. cific gravity of 0.7-1.1. Such preparations are disadvanta
Iodine has a powerful bactericidal and fungicidal action and is geous, when intended to treat relatively large areas. They are
also active against viruses. It is used as topical antiseptic even more disadvantageous when the area to be treated is
agents for treatment of Small wounds, abrasions and other sensitive, such as area with burns or open wounds, where
skin lesions such as herpes simplex. Iodine containing com 25 rubbing a liquid or semi-solid formulation is difficult and
positions are used for protective treatment of a skin area to be painful.
dissected. Certain foamable formulations are known in the art.
Iodine preparations are used in Veterinary medicine as U.S. Pat. No. 5,716,611 discloses a topical formulation
post-milking disinfecting treatment of the udders. Iodine is comprising an anti-microbially effective amount of povi
also effectively used for disinfection of drinking water and 30 done-iodine and from 2% to about 30% of a water-soluble
Swimming pool water (Martindale, The extra pharmaco emollient comprising from about 1 to about 99% ethoxylated
poeia, 28 THI edition, Eds. Reynolds, J. E. F. and Prasad, A. higher aliphatic alcohol and from about 1 to about 99%
B. The Pharmaceutical Press, London, 1982, pp. 862-864). ethoxylated cholesterol derivative. The composition includes
Topical iodine preparations possess counter-irritating thickening agents and Surfactants that provide foaming upon
activity in rheumatism, tenosynovitis and in inflammatory 35 rubbing on the applied surface.
diseases of the peripheral nervous system and muscles. Addi U.S. Pat. No. 6,258,374 provides a pharmaceutical com
tional pronounced counter-irritating activity of iodine was position for rectal or vaginal application containing at least
demonstrated against skin irritation caused by chemical and two parts wherein the composition comprises (i) two or more
thermal stimuli. Iodine is also effective against other skin physiologically acceptable Substances each in separate parts
irritants such as mechlorethamine, divinylsulfone, iodoacetic 40 of the composition which are such that on admixture they
acid and cantharidine (Wormser et al. Arch. Toxicol. (1997) react to produce a physiologically acceptable gas; (ii) in at
71, 165-170). least one part of the composition a polymer stabilizer which is
Molecular iodine (I) is practically water insoluble unless adapted to facilitate the formation of a water-soluble collaps
iodide (sodium or potassium salts) is present in the solution to ible foam structure; and (iii) in at least one part of the com
form the water-soluble ion (IT). Iodine can be dissolved in 45 position a pharmaceutically active Substance. One of the
ethanol but precipitates in the presence of water. Thus, iodine optional active Substances is iodine.
tincture (which contains ethyl alcohol and water) must also International patent application WO 96/19921 discloses a
contain iodide to form I for proper dissolution. composition having biocidal activity comprising an active
Iodine formulations using other solvents or carriers are agent selected from iodine or a compound or complex thereof
known. In some cases, these formulations are shown to have 50 and a polymeric solubilizing agent. The composition may be
greateriodine solubility or improved iodine release. In some a foam.
cases, the iodine formulations are demonstrated to be more U.S. Pat. No. 6,187.290 teaches physiologically acceptable
potent as antiseptics than currently available commercial foam including a foamable carrier separately packaged from
iodine preparations. an active ingredient. The active ingredient may be, among
Post-exposure treatment with topical povidone (polyvi 55 others, povidone-iodine. Surfactants, humectants and plasti
nylpyrolidone)-iodine preparation has been shown to provide cizers may be optionally included.
significant protection against mustard gas (Sulfur mustard, U.S. Pat. No. 5,951,993 discloses a composition including
SM)-induced skin lesions (Wormser et al. Arch. Toxicol. a lower alcohol and water in a weight ratio of about 35:65 to
(1997) 71, 165-170). Studies also have shown the counter 100:0, and a thickener system. The thickener system includes
irritating activity of povidone-iodine against thermal stimuli 60 at least two emulsifiers, each emulsifier containing at least
in humans (Wormser, Burns (1998) 24, 383). The experience one hydrophobic group and at least one hydrophilic group.
with patients after accidental heat burns (mostly of grade I: The composition optionally contains iodine or a complexed
caused by hot water or oil or by hot steam) has shown that form of iodine. The composition is useful as a presurgical
topical application of povidone-iodine ointment immediately scrub replacement, a lotion or other hand preparation.
after the stimulus reduced the degree of skin lesions. The 65 U.S. Pat. No. 5,672,634 describes a rigid, cellular PVP-I
shorter the interval between stimulus and treatment the better foam product, useful as an iodophor, containing about 0.1-2%
the protection achieved. cross linker and about 16-18% total inorganic iodine.
 US 7,575,739 B2
3 4
U.S. Pat. No. 5,545.401 teaches a foaming gel consisting compressed gas propellant, for example, at a concentration of
essentially of water, povidone and iodine. In one embodiment about 3% to about 25% of the total composition.
water is added to the gel in a closed container pressurized at According to one or more embodiments of the present
between 1 and 3 atmospheres with pentane so that when the invention, the foamed composition has specific gravity of
mixture is returned to atmospheric pressure it spontaneously about 0.02 gr/ml to about 0.35 gr/ml.
forms a foam. According to one or more embodiments of the present
U.S. Pat. No. 5.254.334 describes an anhydrous cream invention, iodine is selected from molecular iodine and com
composition comprising (a) glycerin in an amount from about plexed iodine. Complexed iodine may be selected from
40% to about 60% by weight based on the weight of the total cadexomer-iodine, diiodhydrin, domiodol, hydriodic acid,
composition; (b) sodium cocoyl isethionate in an amount 10
iodinated glycerol, iodoform, iodide and povidone-iodine
from about 10 to about 19% by weight based on the weight of According to one or more embodiments of the present
the total composition; (c) emollients in an amount from about invention, the solvent is water or a water miscible organic
10 to about 40% by weight based on the weight of the total Solvent, Such as a polyhydroxy compounds and poly-ethoxy
composition; and (d) sodium lauryl Sulfate in an amount from lated compounds. In one embodiment the composition has a
about 1 to about 5% by weight based on the weight of the total 15
water-to-water miscible organic solvent ratio of about 1:10 to
composition. The composition may further comprise a foam about 10:1. Due to the skin irritability of lower alkyl alcohols,
booster or active ingredients such as PVP-iodine. the water miscible compound is not a lower alkyl, e.g., C-Cs.
U.S. Pat. No. 4,271,149 discloses a germicidal iodine com alcohol.
position containing an aqueous solution of elemental iodine In one or more embodiments, the polyhydroxy compound
and at least one organic Substance which slowly reacts with is selected from ethylene glycol, propylene glycol, glycerol,
iodine selected from the group consisting of iodine complex butanediols and isomers thereof, pentaerythritol, sorbitol,
ing polymers, Surface active agents, alcohols, polyols and mannitol, dimethyl isosorbide, polyethylene glycol, polypro
water soluble solvents. The iodine composition is stable for pylene glycol, diethylene glycol monoethyl ether and mix
extended storage by providing balanced sources of iodide ion tures thereof.
25
in the range of about 0.025% to 0.5% and iodate ion in the In one or more embodiments, the poly-ethoxylated com
range of about 0.005% to 0.2% while maintaining a pH within pound is selected from polyethylene glycol, tetrahydrofurfu
the range of pH 5-7. Foam stabilizers are optional compo ryl alcohol and polyethyleneglycol. The solvent can be mix
nents of the composition. tures of water, polyhydroxy compounds and/or poly
New topical dosage forms are desired to deliver iodine and 30 ethyoxylated compounds.
to treat skin conditions that respond to iodine topical appli
cation. A simple-to-use breakable foam, having low specific According to one or more embodiments, a Surface active
gravity and being easily spreadable on large skin areas, is agent may be an anionic Surface active agent, a cationic
particularly desirable. Surface active agent, a nonionic Surface active agent, a Zwit
terionic Surface active agent, an amphoteric Surface active
SUMMARY OF THE INVENTION 35 agent, an ampholytic Surface active agent and mixtures
thereof.
The present invention provides a foamable composition In one or more embodiments, the Surface-active agent
including iodine, water, a foam adjuvant, a Surface-active includes at least a non-ionic agent. In one or more embodi
agent and a gelling agent that is easily applied and provides ments, the Surface active agent is a mixture of a non-ionic
high availability of iodine to the applied surface. 40 Surface active agent and an anionic Surface active agent pro
According to one aspect the present invention, a foamable vided at a weight ratio of about 4:1 to about 1:4 more prefer
composition includes iodine, water, a foam adjuvant, a Sur ably a weight ratio of about 2:1 to about 1:2. In one or more
face active agent and a gelling agent, in the following con embodiments, the Surface-active agent has a HLB value
centrations: higher than about 8.
45
about 0.1% to about 5% by weight iodine: According to one or more embodiments, the foam adjuvant
about 80% to about 99.6% by weight of at least one solvent; is selected from a fatty alcohol, a fatty acid mixtures thereof,
about 0.1% to about 5% by weight of at least one foam and is provided at a concentration between about 0.4% and
adjuvant; about 2.5% of the composition.
about 0.1% to about 5% by weight of at least one surface 50
Another aspect the present invention provides a method of
active agent; and treating, alleviating or preventing a human or veterinary dis
about 0.1% to about 5% by weight of at least one gelling order by topically administering to a surface afflicted with the
agent. disorder an effective amount of the composition according to
one or more embodiments of the present invention.
The % values presented herein are provided on a weight 55 The method of the invention, according to one or more
(w/w) basis of the total composition. embodiments, provides for the prophylaxis, or treatment of or
The composition according to one or more embodiments of alleviation of the symptoms of a variety of infectious derma
the present invention, when provided in a suitable foaming tological disorders, including for example heat burns, chemi
device, forms a foam that is effective in the topical treatment cal burns, infections, wounds, cuts and ulcers and radioactive
of various skin conditions. 60 radiation damage, and burns and infections resulting from
According to one or more embodiments of the present chemical and biological warfare agents.
invention, the composition is provided in a plastic or glass
propellant free foaming dispenser and forms a breakable or BRIEF DESCRIPTION OF THE DRAWING
collapsible foam when dispensed from the propellant free
foaming dispenser. 65 The invention is described with reference to the FIGURE,
According to one or more embodiments of the present which is provided for the purpose of illustration only and is
invention, the composition further includes a liquefied or not intended to be limiting of the invention.
 US 7,575,739 B2
5 6
The FIGURE is an illustration of a foam dispenser used in way of non-limiting examples, is a polyhydroxy compound
one or more embodiments of the present invention. and/or a poly-ethoxylated compound.
Suitable polyhydroxy solvents (polyols) include small
DETAILED DESCRIPTION OF THE INVENTION organic molecules having two or more hydroxy groups on
their carbon skeleton, Such as ethylene glycol, propylene
Composition glycol, glycerol, butanediols and isomers thereof, pentaeryth
According to one aspect, the present invention provides a ritol, sorbitol, mannitol, dimethyl isosorbide, polyethylene
foamable composition of matter includes iodine, water, a glycol, polypropylene glycol, diethylene glycol monoethyl
foam adjuvant, a Surface active agent and a gelling agent, in ether (TranscutolR) and mixtures thereof.
the following concentrations, reported as percent by weight: Poly-ethoxylated compounds can enhance the effective
iodine: about 0.1% to about 5%; ness of iodine significantly by dissolving the I. Examples of
at least one solvent: about 80% to about 99.6%; Suitable poly-ethoxylated compounds include polyethylene
at least one foam adjuvant: about 0.1% to about 5%; glycol (e.g., PEG 400), tetrahydrofurfuryl alcohol polyethyl
at least one surface active agent: about 0.1% to about 5%; eneglycol ether (glycofurol, tetraglycol (TG)). Among the
and 15 above-mentioned water miscible solvents, suitable com
at least one gelling agent: about 0.1% to about 5%. pounds include transcutol, polyethylene glycol and TG and
mixtures thereof. The ratio between water and the water mis
The % values presented herein are provided on a weight cible solvents is in the range of about 1:10 to about 10:1. In
(w/w) basis of the total composition. one or more embodiments, the ratio is between about 1:4 and
The composition according to one or more embodiments of about 4:1. Due to the skin irritability of lower alkyl (C1-C5)
the present invention is applied to the Surface as a foam. That alcohols, and the tendency of Such alcohols to impair the
is, the foamed composition is applied to the Substrate and is natural skin barrier by dissolving and removing the oily com
not generated by rubbing or lathering. The foamed composi ponents of the skin, lower alkyl alcohols are not included as a
tion, according to one or more embodiments of the present miscible organic solvent.
invention, is dispensed from a glass or plastic container that 25 Foam Adjuvant
dispenses foam in the absence of a gas or liquid propellant. A foam adjuvant is included in the composition to improve
Alternatively, the composition of the present invention fur the stability and reduce the specific gravity of the foamed
ther includes a liquefied or compressed gas propellant at a composition. In one or more embodiments of the present
concentration of about 3% to about 25% of the total compo invention, foam adjuvants include fatty alcohols, fatty acids,
sition. Examples of suitable propellants include volatile 30 and mixtures thereof. The foam adjuvant can include at least
hydrocarbons such as butane, propane, isobutane or mixtures one fatty alcohol and at least one fatty acid.
thereof, and fluorocarbon gases. Suitable fatty alcohols include alcohols having 15 or more
The foamed composition, according to one or more carbons in their carbon chain, such as cetyl alcohol and
embodiments of the present invention, is of exceptionally low stearyl alcohol (or mixtures thereof). Other examples offatty
specific gravity, for example, the foamed composition has a 35 alcohols are arachidyl alcohol (C20), behenyl alcohol (C22),
specific gravity in the range of about 0.02 gr/ml to about 0.35 1-triacontanol (C30), as well as alcohols with longer carbon
gr/ml. Although of low specific gravity, the foam is highly chains (up to C50). The concentration of the fatty alcohol
stable and will remain without collapse for several minutes. required to Support the foam system is inversely related to the
Nonetheless, the foam collapses readily upon application of length of its carbon chains. Fatty alcohols that are derived
mild shear stress. Low specific gravity, high foam stability 40 from beeswax, including a mixture of alcohols, a majority of
and ready collapsibility all contribute to a foamed composi which has at least 20 carbonatoms in their carbon chain, are
tion that is easily applied and administered over large areas especially well Suited as foam adjuvants according to the
without rubbing or chaffing of the affected area. present invention. The concentration of the fatty alcohol
Iodine required to Support the foam system is inversely related to the
“Iodine' and “iodine species' include iodine in its native 45 length of its carbon chains.
form or released from a compound. In its native form, iodine Suitable fatty acids include acids having 16 or more car
(I) is provided as bluish-black crystals, having density of bons in its carbon chain, such as hexadecanoic acid (C16)
about 5 g/cm. When used as is, the iodine concentration in stearic acid (C18), arachidic acid (C20), behenic acid (C22),
the total composition ranges between 0.1% and 5% and more octacosanoic acid (C28), as well as fatty acids with longer
preferably, between 0.5% and 1.5%. In other embodiments of 50 carbon chains (up to C50), or mixtures thereof. As for fatty
the present invention molecular iodine is released from an alcohols, the concentration of fatty acids required to Support
iodine-containing and/or producing compound. Non-limiting the foam system is inversely proportionate to carbon chain
examples of Such compounds include cadexomer-iodine, length.
diiodhydrin, domiodol, hydriodic acid, iodinated glycerol, Optionally, the carbonatom chain of the fatty alcohol or the
iodide, iodoform, and povidone-iodine. When provided as an 55 fatty acid may have at least one double bond. A further class
iodine-containing and/or producing compound, the com of foam adjuvant agent includes a long chain fatty alcohol or
pound concentration in the total composition is calculated to fatty acid, wherein the carbon atom chain is branched. The
achieve a final iodine concentration ranging between about carbon chain of the fatty acid or fatty alcohol can be substi
0.1% and 5% by weight and more preferably, between about tuted with a hydroxyl group. Such as 12-hydroxy Stearic acid.
0.5% and about 1.5% by weight. 60 The foam adjuvant of the present invention may include a
Solvent mixture of fatty alcohols, fatty acids and hydroxy fatty acids
According to one or more embodiments, the composition and alcohols in any proportion. The total amount of foam
includes about 80% to about 99.6% solvent, and typically adjuvants is about 0.1% to about 5% (w/w) of the carrier
includes water. Iodine is not highly soluble in water and thus, mass, and typically, the total amount is about 0.4% to about
formulation stability and effectiveness is limited. In a one or 65 2.5% (w/w) of the carrier mass.
more embodiments of the present invention, the solvent In one or more embodiments of the present invention, a
includes wateranda water miscible organic solvent, which by fatty alcohol possesses a therapeutic properties perse. Long
 US 7,575,739 B2
7 8
chain Saturated and mono unsaturated fatty alcohols, e.g., mers sold, for example, by the B.F. Goodrich Company under
Stearyl alcohol, erycyl alcohol, arachidyl alcohol and the trademark of CarbopolR) resins. These resins include a
docosanol have been reported to possess antiviral, anti infec colloidal water-soluble polyalkenyl polyether cross linked
tive, anti-proliferative and anti-inflammatory properties (U.S. polymer of acrylic acid cross linked with from 0.75% to 2%
Pat. No. 4,874,794). Longer chain fatty alcohols, e.g., tetra of a cross linking agent such as polyallyl Sucrose or polyallyl
cosanol, hexacosanol, heptacosanol, octacosanol, triacon pentaerythritol. Examples include Carbopol 934, Carbopol
tanol, etc. are also known for their metabolism modifying 940, Carbopol 950, Carbopol 980, Carbopol 951 and Car
properties and tissue energizing properties. Long chain fatty bopol 981. Carbopol 934 is a water-soluble polymer of
acids have also been reported to possess anti-infective char acrylic acid cross linked with about 1% of polyallyl ether of
acteristics. Thus, the iodine foamable composition of the 10 Sucrose having an average of about 5.8 allyl groups for each
present invention, containing the foam adjuvant provides a Sucrose molecule.
synergistic therapeutic benefit in comparison with currently Methods of Evolving and Releasing the Foam
used vehicles, which are inert and non-active. Any customary method of evolving foam is applicable
Surface-active Agent according to the present invention. By way of example, in one
According to one or more embodiments of the present 15 optional configuration, the composition according to one or
invention, the Surface-active agent includes any agent linking more embodiments of the present invention is preferably
oil and water in the composition, e.g., the agent can be a placed, together with a liquefied or compressed gas propellant
Surfactant. In one or more embodiments of the present inven in the amount of about 3% to about 25% of the total compo
tion, the composition includes about 0.1% to about 5% of the sition, in an aerosol container. Upon pressing the actuator, a
Surface-active agent. breakable foam, suitable for topical administration is
Suitable Surface-active agents include anionic, cationic, released. Due to the oxidizing nature of iodine, containers
nonionic, Zwitterionic, amphoteric and ampholytic Surfac that are coated with highly durable lacquers of coatings are
tants, as well as mixtures of these surfactants. Such surfac used.
tants are well known to those skilled in the pharmaceutical In an alternative exemplary configuration, the composition
and cosmetic formulation art. Non-limiting examples of use 25 according to one or more embodiments of the present inven
ful surfactants include sucrose esters, sorbitan esters, PEG tion is placed in a plastic or glass container, equipped with a
esters or ethers of fatty chains, mono or diglycerides, isocet foaming dispenser that works without gas propellants. Such
eth-20, sodium methyl cocoyl taurate, sodium methyl oleoyl dispensers are described, for example, in U.S. Pat. No. 6,536,
taurate, sodium lauryl Sulfate, triethanolamine lauryl Sulfate 629, in which the dispenser includes a container and a dis
and betaines (e.g., cocamidopropyl betaine and laurami 30 pensing assembly coupled in liquid-tight manner. The dis
dopropyl betaine), which are known to contribute to foam pensing assembly can have a liquid pump with a liquid inlet
stability (foam boosters). and a liquid outlet. An exemplary foam dispenser is shown in
While any surface-active agent may be used in the present the FIGURE.
invention, a Surface-active agent having an HLB (hydro Foam Characteristics
philic-lipophilic balance) higher than 8 is used in one or more 35 The foam that is released from the aerosol container or
embodiments of the present invention. from the propellant-free foaming dispenser is well aerated. It
Non-ionic Surfactants are particularly well Suited as Sur has specific gravity of about 0.02 gr/ml to about 0.35 gr/ml.
face-active agents. A combination of a non-ionic Surfactant When applied onto a surface, specifically a skin Surface, and
and an anionic Surfactant (such as Sodium lauryl Sulfate) may rubbed gently, it spreads easily over the area, without the need
also be used. A ratio of non-ionic Surfactant to anionic Sur 40 of extensive rubbing.
factant between around 4:1 and about 1:4, or between about A foam composition of one or more embodiments of the
2:1 and about 1:2, provides a foam, which upon rubbing onto present invention is advantageous over formulation options.
the skin collapses easily, to allow facile spreading and absorp A foamed composition may possess one or more of the fol
tion. A Surface-active agent mix is even further improved lowing properties. The foam is lightweight and thus, eco
when a foam stabilizing Surfactant, such as cocamidopropyl 45 nomical. The foam is easily spreadable, allowing treatment of
betaine, is added. large areas such as the arms, back, legs and the breast. The
flow properties provide a foam that spreads effectively into
Gelling Agent folds and wrinkles, providing uniform distribution of the
In one or more embodiments of the present invention, the active agent without the need of extensive rubbing and
composition includes about 0.1% to about 5% of a gelling 50 absorbs into the skin. The low specific gravity, e.g., fluffy,
agent. Suitable gelling agents include, in a non-limiting man nature of the foam renders application of the foam on large
ner, naturally-occurring polymeric materials such as locust skin areas very easy, irritation-free and painless.
bean gum, guar gum, Sodium alginate, Sodium caseinate, egg Foam Applications
albumin, gelatin agar, carrageenin gum, Sodium alginate, The compositions according to one or more embodiments
Xanthan gum, quince seed extract, tragacanth gum, starch, 55 of the present invention are useful in the various medicinal
chemically modified Starches and the like, semi-synthetic disciplines including human and Veterinary medicine. More
polymeric materials such as cellulose ethers (e.g. hydroxy generally, the compositions according to the present inven
ethyl cellulose, methyl cellulose, carboxymethyl cellulose, tion can be used in situations where use of iodine is preferred
hydroxy propylmethyl cellulose), hydroxypropyl guar gum, including, but not limited to, medicine, industrial processes,
soluble starch, cationic celluloses, cationic guars and the like 60 diagnostics and environmental purposes.
and synthetic polymeric materials such as carboxyvinyl poly Specifically, the compositions according to one or more
mers, polyvinylpyrrolidone, polyvinyl alcohol, polyacrylic embodiments of the present invention are useful as antiseptic
acid polymers, polymethacrylic acid polymers, polyvinyl compositions. The compositions may be further used to pro
acetate polymers, polyvinyl chloride polymers, polyvi tect from, prevent, alleviate the symptoms of or cure a variety
nylidene chloride polymers and the like. 65 of infectious dermatological disorders, including: bacterial
Also useful herein are gelling agents such as the acrylic Infections including cellulitis, acute lymphangitis, lymphad
acid/ethyl acrylate copolymers and the carboxyvinyl poly enitis, erysipelas, cutaneous abscesses, necrotizing Subcuta
 US 7,575,739 B2
9
neous infections, staphylococcal scalded skin syndrome, fol
liculitis, furuncles, hidradenitis Suppurativa, carbuncles, -continued
paronychial infections, erythrasma; fungal infections includ
ing dermatophyte infections, yeast infections; parasitic infec Ingredient % (w.fw) Function
tions including scabies, pediculosis, creeping eruption and Sodium Lauryl Sulfate 1% Surface active agent
viral infections. Sucrose Ester 70 1% Surface active agent
The treatment of heat burns, chemical burns (caused by Cocamidopropyl Betaine 0.5% Surface active agent
Methocel LV15 0.8% Gelling agent
chemicals such as acids, bases, caustic materials and warfare (Hydroxypropylmethyl cellulose)
chemicals), wounds, cuts and ulcers using the composition Xanthan Gum 0.4% Gelling agent
according to one or more embodiments of the present inven 10
tion is particularly advantageous. Upon application, the foam
spreads easily, covering the Surface of the affected area, and Iodine was dissolved in a mixture of glycofurol and Stearyl
without causing pain. alcohol and the mixture was heated to -60C until homoge
The composition of the invention is also useful as a pro neity was obtained. Methocel was dispersed in one third
tectant in case of exposure to radiation and radioactive iso 15 portion of water, preheated to 80°C., and sucrose ester was
topes. added. The remaining two-third portion of water at room
According to another aspect the present invention provides temperature was added under vigorous stirring; and Xanthan
a method of treating, alleviating or preventing a human or gum and sodium lauryl Sulfate and cocamidopropyl betaine
Veterinary disorder by topically administering to a Surface were added mixing continuously for 15 minutes under vigor
afflicted with the disorder an effective amount of the compo ous stirring. The iodine mixture was added carefully to aque
sition including: ous mixture and was stirred for an additional 5 minutes for
about 0.1% to about 5% by weight iodine: complete homogeneity. The resultant product was cooled to
about 80% to about 99.6% by weight of at least one solvent; room temperature and filled into bottles.
about 0.1% to about 5% by weight of at least one foam EXAMPLE 2
adjuvant; 25
about 0.1% to about 5% by weight of at least one surface Pressurized Foam Comprising Iodine
active agent; and
about 0.1% to about 5% by weight of at least one gelling The composition of Example 1 (50 ml) at ambient tem
agent.
30 perature was added to a 125 ml aerosol container, the con
The present invention provides for the prophylaxis, or treat tainer was sealed with an aerosol valve and abutane/propane
ment of oralleviating the symptoms of a variety of infectious propellant (about 16% of the composition mass) was com
dermatological disorders, including heat burns, chemical pressed into the container. Upon pressing the aerosol valve, a
burns, infections, wounds, cuts and ulcers and radioactive rich foam having specific gravity of about 0.1 gr/ml was
radiation damage, and burns and infections resulting from 35
released.
chemical and biological warfare agents.
While the invention will now be described in connection EXAMPLE 3
with certain preferred embodiments in the following
examples so that aspects thereof may be more fully under Iodine Non-pressurized Foam
stood and appreciated, it is not intended to limit the invention 40
to these particular embodiments. On the contrary, it is The composition of Example 1 (50 ml) at ambient tem
intended to cover all alternatives, modifications and equiva perature was added to a 125 ml container, equipped with a
lents as may be included within the scope of the invention as foaming dispenser that works without gas propellants (Air
defined by the appended claims. Thus, the following spray International Inc., 3768 Park Central Blvd. North, Pom
examples serve to illustrate the practice of this invention, it 45
pano Beach, Fla. 33064, USA). Upon pressing the aerosol
being understood that the particulars shown are by way of valve, rich foam having specific gravity of about 0.1 gr/ml to
example and for purposes of illustrative discussion of pre about 0.3 gr/ml was released.
ferred embodiments of the present invention only and are What is claimed is:
presented in the cause of providing what is believed to be the 1. A foamable composition comprising
most useful and readily understood description of formula 50 a. about 0.1% to about 5% by weight iodine;
tion procedures as well as of the principles and conceptual b. about 80% to about 99.6% by weight of at least one
aspects of the invention. solvent;
EXAMPLE1 c. about 0.1% to about 5% by weight of at least one foam
adjuvant comprising at least one fatty alcohol, at least
Foamable Iodine Composition 55 one fatty acid, or a mixture thereof, and
d. about 0.1% to about 5% by weight of at least one surface
The table below lists the components of the foamable com active agent; and
position. e. a liquefied or compressed gas propellant, wherein the
weight ratio of the propellant to the remainder of the
60 composition is about 3:97 to about 25.75, said compo
sition housed in a pressurized container comprising a
Ingredient % (w.fw) Function valve configured to release said composition as break
able foam.
Iodine (I2) 1% Active agent 2. The composition claim 1, having specific gravity of
Purified Water 64.3%. Water
Glycofurol 30% Water miscible solvent 65 about 0.02 gr/ml to about 0.35 gr/ml.
Stearyl alcohol 1% Foam adjuvant 3. The composition of claim 1, wherein the iodine is
selected from native iodine and complexed iodine.
 US 7,575,739 B2
11 12
4. The composition of claim 3, wherein the complexed 16. The composition of claim 1, wherein the at least one
iodine is selected from cadexomer-iodine, diiodhydrin, domi foam adjuvant is selected from a fatty alcohol, a fatty acid and
odol, hydriodic acid, iodinated glycerol, iodoform, and povi a hydroxy fatty acid and mixtures thereof.
done-iodine. 17. The composition of claim 1, wherein the at least one
5. The composition of claim 1, wherein the at least one foam adjuvant comprises between about 0.4% and about
Solvent comprises water. 2.5% of the composition.
6. The composition of claim 5, further comprising a water 18. The composition of claim 1, wherein the at least one
miscible organic solvent. Surface active agent is a nonionic Surface active agent.
7. The composition of claim 6, wherein the water miscible 19. The composition of claim 12, wherein the ratio of
organic solvent is selected from the group consisting of a 10 non-ionic to ionic Surface active agent is about 3:2.
polyhydroxy solvent and a poly-ethoxylated compound. 20. The composition of claim 12, wherein the ionic surface
8. The composition of claim 7, wherein the polyhydroxy active agent comprises a Zwitterionic Surface active agent and
Solvent is selected from the group consisting of ethylene the ratio of Zwitterionic to non-ionic Surface active agent is
about 1:2.
glycol, propylene glycol, glycerol, butanediols and isomers
thereof, pentaerythritol, sorbitol, mannitol, dimethyl isosor 15 21. The composition of claim 12, wherein the ionic surface
bide, polyethylene glycol, polypropylene glycol, diethylene active agent comprises an anionic Surface active agent and the
glycol monoethyl ether and mixtures thereof. amount of anionic Surface active agent is about the same as or
9. The composition of claim 7, wherein the poly-ethoxy is less than the amount of non-ionic Surface active agent.
lated compound is selected from the group consisting of 22. The composition of claim 1, further comprising about
polyethylene glycol, tetrahydrofurfuryl alcohol and polyeth 0.1% to about 5% by weight of at least one gelling agent.
yleneglycol. 23. The composition of claim 22, wherein the at least one
gelling agent comprises naturally-occurring polymeric mate
10. The composition of claim 6, wherein the water to water rials, chemically modified Starches, semi-synthetic poly
miscible organic solvent ratio is in the range of about 1:10 to meric materials, synthetic polymeric materials, acrylic acid/
about 10:1. 25 ethyl acrylate copolymers and carboxyvinyl polymers.
11. The composition of claim 1, wherein the at least one 24. The composition of claim 22, wherein the at least one
Surface active agent is selected from the group consisting of gelling agent comprises locust bean gum, guar gum, Sodium
anionic Surface active agents, cationic Surface active agents, alginate, Sodium caseinate, egg albumin, gelatin agar, carra
nonionic Surface active agents, Zwitterionic Surface active geenin gum, Sodium alginate, Xanthan gum, quince seed
agents, amphoteric Surface active agents, ampholytic Surface 30 extract, tragacanth gum, starch, a cellulose ether, hydrox
active agents and mixtures thereof. ypropyl guar gum, soluble starch, cationic cellulose, cationic
12. The composition of claim 11, wherein the at least one guar, a carboxyvinyl polymer, polyvinylpyrrolidone, polyvi
Surface-active agent is a mixture of a non-ionic Surface-active nyl alcohol, a polyacrylic acid polymer, a polymethacrylic
agent and an ionic Surface-active agent. acid polymer, a polyvinyl acetate polymer a, a polyvinyl
13. The composition of claim 12, wherein the non-ionic 35 chloride polymer, a polyvinylidene chloride polymer, a poly
Surface active agent to ionic Surface active agent weight ratio alkenyl polyether cross-linked polymer of acrylic acid, or a
is in the range of about 4:1 to about 1:4. mixture thereof.
14. The composition of claim 12, wherein the non-ionic 25. The composition of claim 22, wherein the at least one
Surface acting agent to ionic Surface acting agent weight ratio gelling agent comprises hydroxypropylmethyl cellulose,
is in the range of about 2:1 to about 1:2. 40 hydroxyethylcellulose, methylcellulose, carboxymethylcel
15. The composition of claim 11, wherein the at least one lulose, or a mixture thereof.
surface-active agent has a HLB value higher than about 8. k k k k k
 UNITED STATES PATENT AND TRADEMARK OFFICE
CERTIFICATE OF CORRECTION

PATENT NO. : 7,575,739 B2 Page 1 of 1

APPLICATION NO. : 10/835359
DATED : August 18, 2009
INVENTOR(S) : Tamarkin et al.
It is certified that error appears in the above-identified patent and that said Letters Patent is hereby corrected as shown below:

On the Title Page:

The first or sole Notice should read --

Subject to any disclaimer, the term of this patent is extended or adjusted under 35 U.S.C. 154(b)
by 1279 days.

Signed and Sealed this

Seventh Day of September, 2010

David J. Kappos
Director of the United States Patent and Trademark Office