U.S. patent application number 16/008210 was filed with the patent office on 2018-12-13 for antiseptic, antiseborrheic and exfoliating composition to remove or prevent acne.
The applicant listed for this patent is GRUPO MEDIFARMA S.A. DE C.V.. Invention is credited to Jose Agustin Rogelio MAGANA CASTRO, Pedro PENA SANTOYO, Laura V ZQUEZ CERVANTES.
Application Number | 20180353448 16/008210 |
Document ID | / |
Family ID | 49230828 |
Filed Date | 2018-12-13 |
United States Patent
Application |
20180353448 |
Kind Code |
A1 |
MAGANA CASTRO; Jose Agustin Rogelio
; et al. |
December 13, 2018 |
ANTISEPTIC, ANTISEBORRHEIC AND EXFOLIATING COMPOSITION TO REMOVE OR
PREVENT ACNE
Abstract
The invention refers to an antimicrobial, exfoliating and
seboregulating hydrosoluble composition comprising a combination of
diallyl disulphide modified oxide (DDMO) and alpha hydroxyethanoic
acid (glycolic acid), which acts removing bacteria affecting the
skin including those caused by acne, said composition also provides
deep cleansing, exfoliating action, reduces epidermal cohesion
facilitating cellular change, preventing the occurrence of several
forms of acne in the skin and additionally producing seboregulating
effects by avoiding blockage of sebaceous glands.
Inventors: |
MAGANA CASTRO; Jose Agustin
Rogelio; (Mexico City, MX) ; V ZQUEZ CERVANTES;
Laura; (Mexico City, MX) ; PENA SANTOYO; Pedro;
(Mexico City, MX) |
|
Applicant: |
Name |
City |
State |
Country |
Type |
GRUPO MEDIFARMA S.A. DE C.V. |
Morelos |
|
MX |
|
|
Family ID: |
49230828 |
Appl. No.: |
16/008210 |
Filed: |
June 14, 2018 |
Related U.S. Patent Documents
|
|
|
|
|
|
Application
Number |
Filing Date |
Patent Number |
|
|
14421616 |
Feb 13, 2015 |
|
|
|
PCT/MX2013/000099 |
Aug 22, 2013 |
|
|
|
16008210 |
|
|
|
|
Current U.S.
Class: |
1/1 |
Current CPC
Class: |
A61Q 19/10 20130101;
A61K 31/191 20130101; A61P 17/00 20180101; A61K 2800/28 20130101;
A61Q 19/008 20130101; A61Q 17/005 20130101; A61K 8/365 20130101;
A61P 31/02 20180101; A61K 31/10 20130101; A61P 31/04 20180101; A61K
8/46 20130101; A61P 17/08 20180101; A61P 17/10 20180101 |
International
Class: |
A61K 31/191 20060101
A61K031/191; A61K 31/10 20060101 A61K031/10 |
Foreign Application Data
Date |
Code |
Application Number |
Aug 23, 2012 |
MX |
MX/A/2012/009806 |
Claims
1. An antimicrobial, exfoliating and seboregulating pharmaceutical
hydrosoluble composition to remove or prevent skin microbial
injuries, including acne, characterized in that it comprises from
0.001 to 10% p/w of the DDMO composition, from 1 to 12% p/w of
alpha hydroxyethanoic acid (glycolic acid), from 0.3 to 24% p/w of
one or more surfactants, from 0.3 to 10% p/w of a moisturizing
agent, from 0.2 to 10% p/w of an aromatizing agent and from 40 to
70% p/w of the composition of an aqueous solvent.
2. The composition according to claim 1, characterized in that the
surfactants are selected from the group consisting of lineal
alkylbenzensulfates and ionic alkyl sulfates.
3. The composition according to claims 1 and 2, characterized in
that the surfactants preferably are sodium lauryl sulfate, sodium
lauryl ether sulfate and ammonium lauryl sulfate.
4. The composition according to claim 1, characterized in that the
moisturizing agent is selected from the group consisting of
ethylene glycol, propylene glycol, glycerin, sorbitol, low
molecular weight polyethylenes, polyoxyethylated glycerols,
polyoxyethylated sugars.
5. The composition according to claim 1, characterized in that the
aromatizing agent is selected from those available for the
pharmaceutical and food industry.
6. The composition according to claim 1, characterized in that the
solvent is selected from water and water-hydrosoluble alcohol
mixtures.
7. The use of the composition according to claim 1, for making a
medicine to remove, reduce or prevent acne.
8. The use of the composition according to claims 1 to 6, for
making a medicine to remove bacteria causing acne, providing deep
and delicate cleansing to normal and oily skin, providing
exfoliating action, eliminating death cells from the skin, removing
grease and fat excess present in skin with acne, avoiding the
obstruction of pores, removing the comedonal block and avoiding the
formation of new blackheads and pustules.
9. A method for removing, reducing and preventing acne,
characterized in that it comprises to administer the skin of an
individual in need of said treatment an antimicrobial and
antiseptic pharmaceutical hydrosoluble composition according to any
of claims 1 to 6.
Description
RELATED APPLICATIONS
[0001] This application is a continuation of U.S. application Ser.
No. 14/421,616, filed on Feb. 13, 2015, which is a 35 U.S.C. 371
National Stage Filing of International Application No.
PCT/MX2013/000099, filed on Aug. 22, 2013, which claims priority to
Mexican Application No. MX/A/2012/009806, filed on Aug. 23, 2012.
The contents of the aforementioned applications are hereby
incorporated by reference in their entireties.
FIELD OF THE INVENTION
[0002] The present invention relates to a hydrosoluble
pharmaceutical antiseptic, antiseborrheic and exfoliating
composition comprising a combination of diallyl disulphide modified
oxide (DDMO) and alpha hydroxyethanoic acid (glycolic acid) to
remove bacteria affecting the skin, besides said composition
provides a deep cleansing because it reduces the epidermal cohesion
and facilitates the cellular replacement, preventing or removing
the occurrence of several forms of alterations in the skin.
BACKGROUND OF THE INVENTION
[0003] The skin has a microbial flora, which can be affected by
changes in normal conditions of the skin, more likely acne is the
most frequency of these alterations, due to the multiple factors
altering it and producing a balance loss of the microbial
flora.
[0004] Acne is an inflammatory illness of the pilosebaceous
follicles, associated to the keratinization and seborrhea
alterations; characterized by the formation of skin wounds such as:
blackheads, papulae, pustules, cysts or abscesses, which frequently
leave residual scars.
[0005] Acne is undoubtedly the most frequent skin disease in the
entire world; traditionally the three main factors considered to
intervene in the appearance of acne were microbial infection,
overproduction of fat and abnormal peeling of epidermal cells that
finally cause an excess in the keratinization, but recent studies
add as causing effects of acne genetic predisposition and
inflammatory factor.
[0006] It is calculated that about 85% of the population between
the ages of 11 and 30 suffer from acne; this represents only in
Mexico an approximate total of 20 million people. The incidence
curves show a maximum peak at 18 years old, from this point a
gradual decrease is appreciated, which increases after 30 years of
age; however, between 25 and 35% of adults over 35 years old go
through occasional acne exacerbations.
[0007] The cause of acne is precisely unknown, due to the fact that
a great amount of factors jointly intervene, however, among them it
is worth mentioning the genetic factor, which in combination with
the endocrinal, inflammatory and infectious factors, are somehow
the cause of the polymorphic characteristic of acne.
[0008] There are 5 main primary pathogenic factors interacting in a
complex manner to produce acne injuries. [0009] 1. Genetic
predisposition. [0010] 2. Overproduction of fat by sebaceous
glands. [0011] 3. Alteration in the keratinization process with
abnormal peeling of the sebaceous follicular epithelium (causing
comedogenesis). [0012] 4. Proliferation of Propionibacterium acnes.
[0013] 5. Release of inflammatory intermediaries on the skin,
mainly alpha-TNF and alpha IL-1.
[0014] The genetic predisposition is not mediated by one simple
Mendelian character, but it is caused by an intermediary of a
polygenic mechanism, which originates special receptiveness of the
pilosebaceous follicle, in order to more intensely responds to
androgens, different from how healthy people respond.
[0015] Research made about the role of fat in acne has allowed to
establishing that the sebaceous lipids are regulated by the
peroxisome proliferator activated-receptors (PPAR) and by sterol
transcription factors.
[0016] Other research of the sebaceous gland function has
contributed to obtaining information about the main role these
glands play in regulating skin functions. The sebaceous gland has
direct and indirect antibacterial activities. Likewise, the
sebaceous gland produces antibacterial peptides and proinflammatory
cytokines that are induced in sebocytes due to the presence of
bacteria.
[0017] Androgens are hormones synthesized in testicles, ovaries and
suprarenal cortex. During puberty, through little known mechanisms,
the hypophysis starts to secrete greater amounts of luteinizing
hormones (HL) and follicle-stimulating hormones (FSH), which
together are responsible for the increase in testicular growth,
spermatogenesis, and steroidogenesis. Testosterone acts upon
sebaceous glands, increasing their size and fat synthesis; in women
the mechanism is similar. Through biopsies to the face skin in
patients with acne, it has been proven that during puberty the
sebaceous glands are bigger and foliated.
[0018] Some time ago it was believed that acne was just an
infectious process caused by the bacteria "Acne bacillus", now
called Propionibacterium acnes. The cutaneous flora is essentially
a triad lead by the Propionibacterium acnes, in addition to
Staphylococcus epidermis and yeast, which can be Pityrosporum ovale
or Pityrosporum orbiculare.
[0019] It is possible that the association between bacteria and the
pathogenesis of the acne is reinforced by well-documented findings
about clinical improvement in patients with acne treated with
systemic antibiotics. The antibacterial therapy does not affect the
P. orbiculare or P. ovale since they reside on the upper part of
the acrofundibulum of the sebaceous follicle. The anaerobe P. acnes
on the other hand seems to play a central role in the development
of acne inflammation. The most important evidence might be the
demonstration that therapy with antibiotics results in a
significant suppression of P. acnes, which is accompanied in one
reduction in the number of inflammatory injuries.
[0020] Propionibacterium acnes and Staphylococcus epidermidis are
produces of a lipase that hydrolyzes triglycerides from fat in
fat-free acids, which are potent irritants from the follicular
channel, when applied on the skin or intradermally injected, they
cause inflammation and blackheads.
[0021] It must also be noted that the Propionibacterium acnes
alternately activates the complement system, this fact has allowed
to propose that this infectious mechanism could also play an
important role in the production of acne inflammatory injuries.
[0022] During puberty, and in response to the androgens produced in
greater amounts in this stage, the sebaceous glands that were
relatively inactive, increase in size and become more foliated,
thus increasing the production of fat spilled on the outside;
thereby the first sign of acne: seborrhea.
[0023] The recently synthesized fat contains triglycerides,
squalene and wax esters, and it is known that Propionibacterium
acnes through a lipase hydrolyzes triglycerides from this sebaceous
material, thus converting them into fat free acids, which in
addition to other irritant substances as squalene and oleic acid
cause inflammation of the follicular channel, which responds to the
inflammation with hyperkeratosis. The resulting corneous material
fall in the light of the follicle, which in addition to the fat
excess forms wax substituting and easing the follicle walls,
accordingly by not being able to excrete material, it inflames
more, causing the first and most important acne elemental injury:
the blackhead, causing dilation of the follicular hole due to the
pressure the wax applies when trying to be expelled.
[0024] In several studies, it was been studied in depth the role of
the inflammatory mediators, as well as the interrelation of this
factor with sebaceous lipids and matrix metaloproteinases (MMP's)
in the physiology of acne.
[0025] One of the pioneer researches in this field was developed by
Jeremy and co-workers in 2003, who researched the initial events of
acne injuries and found that the immunological changes and
inflammatory responses occurred before the hyperproliferation of
keratinocytes, with a similar pattern to a type IV retarded
hypersensitivity. An important fact is that the whole process
starts by the exacerbated regulation of IL1-.beta. having a
proinflammatory action in response to the linoleic acid relative
deficiency caused by the fat excess and by the disturbance of the
barrier function inside the follicle. Vowels and co-workers proved
in an in vitro study the presence of a P. acnes soluble factor that
also induces the production of pro-inflammatory cytokines in
cellular lines derived from human monocytes. This product of P.
acnes induces the synthesis of the alpha tumor necrosis factor
(.alpha.-TNF) and interleucine 1-beta (IL1-.beta.) in said cellular
lines. It was also shown that the induction of cytokines by P.
acnes would happen through the activation of the "TOLL-LIKE-2"
Receptor (TLR-2) shooting inflammatory responses.
[0026] Other recent studies have proved that this chain of events
occurs in inflammatory injuries from patients with facial acne. It
has been shown that the Propionibacterium acnes also induces type
Toll receptors. This provides additional evidence that the
inflammatory cytokines, which act through autocrine and paracrine
mechanisms amplifying their corresponding receptors and amplifying
the signaling way that activates the Activator Protein-1 (AP-1)
that is a transcriptional factor.
[0027] In treating acne, the use of antimicrobials is a normal and
habitual behavior among doctors, since there is clinically an
improvement in patients with acne when using this type of products,
this due to the strengthening factor of P. acnes in the fat
metabolism that creates an irritant effect causing greater
inflammation on the patient.
[0028] The diallyl disulphide oxide (DDO) is also known as allicin,
is the product from the conversion of allina, which is found in
garlic (Allium sativum), by means of allinase enzyme catalysis. It
is a sulfurated compound containing diverse pharmacological
activities of interest. The DDO is not naturally found in garlic,
but when the bulb fractures, it is cut or grinded, liberates
allina, which when contacting the allinase enzyme creates the
active principle. Allina is found in amounts varying from
0.22-0.24% by weight of garlic and is an amino acid that is it not
a structural part of any protein and it is not biochemically
essential for human nutrition.
[0029] Since it is a not much stable compound, the DDO quickly
loses its properties, on the other hand if garlic is heated over
60.degree. C. it loses its properties. It has a strong oxidative
power that could cause harm to intestinal cells.
[0030] It has been shown that DDO has in vitro activity against
Candida albicans, some Trichomonas, Staphylococcus aureus;
Escherichia coli, Salmonella typhi, S. paratyphi, Shigella
dysenterica and Vibro cholera species.
[0031] The structural formula of allicin is shown below:
##STR00001##
[0032] In 1944 Cavallito and his co-workers were able to isolate
and identify the active compound from the extracts of Allium
sativum which they called allicin and in 1947 they were able to
synthesize the diallyl disulphide oxide (allicin), but
unfortunately they were not able to make the molecule thereof
stable, since it kept losing its efficacy in a very short period of
time. A group of Mexican researchers from 2000 and 2005 were able
to stabilize the diallyl disulphide oxide, adding a co-factor,
compound called diallyl disulphide modified oxide [DDMO], which is
much more stable than allicin and it seems to maintain its
properties.
[0033] The diallyl disulphide modified oxide [DDMO], is the
chemical compound called [1,2-alpha-glucodiallyl-disulphide oxide,
2-propen+chloride-6 alkyl (benzyl, methyl, octyl
ammonium-hydroxymethylamine); whose structural formula is
represented as follows:
##STR00002##
[0034] In diverse studies it has been shown the activity of
allicin, however its little stability has been a limitation in its
possible therapeutic applications. Accordingly, it is clear that
the application of the stability properties of compound DDMO, will
allow the therapeutic application based on its antibacterial and
anti-septic properties among others from allicin.
[0035] On the other hand, hydroxyethanoic acid (HAA), is also
called glycolic acid, which is an acid of small molecular chain
having the ability to penetrate the skin faster that deeper layers.
It is shown colorless, odorless, and hygroscopic crystalline solid
that is highly water-soluble and in related solvents. This acid is
largely used in dermatologic treatments, there are studies
demonstrating its efficacy, through methods such as computerized
morphometry on corneal layers from biopsies. Normally it is
employed in association with other dermatologic products supporting
the cellular reconstruction of the skin, thus becoming the
so-called "soft-peeling" base. The treatment action with
hydroxyethanoic acid is to decrease the corneal layer thickness of
the skin and to increase the malpighian layer thickness; the
fractions of areas occupied by collagen in dermal layers
significantly increases, thereby there is an improvement in the
appearance of atrophic scars from acne and in the treatment of
human skin wrinkles. It is also an excellent exfoliator, thus
helping to significantly prevent and combat acne in any body part.
The glycolic acid also lets other components to more easily
penetrate the skin, thus it is advisable to also use the so-called
complete treatments. The hydroxic acid also has seboregulating
properties by increasing the peeling of cells and thus avoiding
blockage of the sebaceous glands and the formation of blackheads
and other acne injuries.
OBJECT OF THE INVENTION
[0036] A first object of the present invention is to provide
antimicrobial, exfoliating and seboregulating pharmaceutical
hydrosoluble compositions comprising a combination of diallyl
disulphide modified oxide (DDMO) and alpha-hydroxyethanoic acid
(glycolic acid) to remove or prevent acne.
[0037] A second object is to obtain compositions comprising a
combination of diallyl disulphide modified oxide (DDMO) and
alpha-hydroxyethanoic acid (glycolic acid),
antimicrobials/antiseptics, stable, biodegradable and non-poisonous
topical application exfoliants and seboregulators having as an
antimicrobial function a wide action spectrum, not just against
gram negative and gram positive microorganisms, but against fungus
as well.
[0038] The previous objects are representative, but they shall not
be considered as limitative to the present invention, wherein it is
further shown its treatment methods, applications and/or
pharmaceutical uses in the preparation of medicaments to remove,
reduce or prevent microbial injuries of the skin, including
acne.
DESCRIPTION OF THE INVENTION
[0039] The present invention is related to antimicrobial,
exfoliating and seboregulating pharmaceutical hydrosoluble
compositions comprising from 0.001 to 10% p/w of the DDMO
composition, from 1 to 12% p/w of alpha-hydroxyethanoic acid
(glycolic acid), from 0.3 to 24% p/w of one or more surfactants,
from 0.3 to 10% p/w of a moisturizing agent, from 0.2 to 10% p/w of
an aromatizing agent and from 40 to 70% p/w of the composition of
an aqueous solvent.
[0040] Particularly, the object compositions of the present
invention comprise one or more surfactants selected from the group
consisting of lineal alkyl benzene sulfates and ionic alkyl
sulfates.
[0041] The surfactants useful in the object compositions of the
present invention preferably are sodium lauryl sulfate and sodium
lauryl ether sulfate.
[0042] The ionic alkyl surfactants, such as sodium lauryl sulfate
that is an anionic surfactant, are used in a variety of
pharmaceutical non-parenteral formulations. For example, the sodium
lauryl sulfate is a detergent and moisturizing agent, effective in
acid, alkaline solutions and in hard water. It is used in medicated
shampoos, such as skin cleaner and dentifrices, it is usually known
as "Cosmetic Detergent", makes foam and bubbles and is good for
removing grease and oil from skin and hair.
[0043] Likewise, the sodium lauryl ether sulfate is the most
frequently used active anion surfactant in the manufacture of
cleaning, scrubbing and domestic washing products, as well as
cosmetic and personal hygiene products. The sodium lauryl ether
sulfate does not irritate the skin and if from natural origin;
additionally it is valued for its easy degradations and properties
in relation to the formation of foam. The sodium lauryl ether
sulfate is mainly used in the production process of shampoos,
liquid soaps, face skin creams, dental creams, etc.
[0044] The surfactant preferably used in the present invention are
sodium lauryl sulfate, sodium lauryl ether sulfate and ammonium
lauryl sulfate.
[0045] The moisturizing agent is selected from the group consisting
of ethylene glycol, propylene glycol, glycerin, sorbitol, low
molecular weight polyethylenes, polyoxyethylated glycerols,
polyoxyethylated sugars, for example, MEA acetamide, and the like.
Preferably, the moisturizing agent is glycerin, which has a wide
variety of applications, such as emulsifier, softening agent,
laminate, stabilizing and moisturizing agent for baking shop,
ice-cream shop and cigar store, in body lotions, mouthwashes, as
protecting means for freezing of red blood cells, sperm, corneas
and other tissues in printing inks, paint resins; antifreezing
mixtures; and as raw material for nitroglycerin. It is used in the
manufacture of countless prepared pharmaceuticals and cosmetics;
for example in soaps, glycerin increases its detergency, whitening
and softening of the skin. Between 8-15% of glycerin can be found
in the compositions of these soaps.
[0046] Other moisturizing agents useful in the compositions claimed
in the present invention comprise among others:
[0047] A aromatizing agent selected from any of the available ones
for the pharmaceutical and food industry.
[0048] An aqueous solvent, which is selected from water and
water-hydrosoluble alcohol mixtures.
[0049] With these elements, it is possible to extract a wide range
of antimicrobial, exfoliating and seboregulating pharmaceutical
compositions containing DDMO and alpha-hydroxyethanoic acid
(glycolic acid), useful in treating and preventing skin microbial
injuries.
[0050] Said compositions contribute to eliminate bacteria causing
acne providing a deep and delicate cleansing of the skin; even in
oily skins, improving the habitual look and freshness. In addition
to its antimicrobial action, it provides an exfoliating action,
reducing the epidermal adhesion and facilitating the cellular
change, eliminating dead skin cells. Also, they remove the grease
and oil excess present in the acne skin, thus preventing
obstruction of the pores, removing comedonal block and avoiding
formation of new blackheads and pustules.
[0051] The information obtained from microbiologic tests
(antimicrobial challenge) of the DDMO and alpha-hydroxyethanoic
acid (glycolic acid) against several bacteria, has proven the great
antibacterial capacity of the formulations, insisting on the
results against Propionibacterium acnes, thus proving the removal
of said bacteria in a matter of seconds.
[0052] The antimicrobial action mechanism of DDMO, probably
comprises the following:
[0053] 1. Alteration of the microbial mechanism, inhibiting the
action of 11 essential enzymes for cellular respiration of the
microorganism. This inhibiting effect is created from the chemical
reaction of the sulfhydryl radicals of DDMO about the molecular
structure of the sulfurated enzymes of the microorganism, whether
by inserting sulfurated radicals or by modifying the enzyme
protein, thus causing death of the microorganism.
[0054] 2. Through reactions of oxide-reduction creating free
radicals (ROS), which by oxidative stress break the cellular wall
of the microorganism, by acting "sequestering" oxygen serving as
link between the NAG (n-Acetyl glucosamine acid) and NAM (N-Acetyl
muramic acid) chains, thus weakening the microorganism wall causing
rupture and thereby death of the microorganism.
[0055] 3. Inhibition of the genetic transcription process and
unfolding of the microorganism proteins, through the activation of
the polymerase ARN enzyme, which is an enzyme, since being of
sulfurated composition, is vulnerable to chemical attack from the
DDMO.
[0056] 4. Alteration of the metal metabolism in the microorganism,
also causing metabolic alterations therein.
[0057] The foregoing has been inferred from studies made with
allicin, reported by Yosuda et al, Biosci. Biotechnol. Biochem.,
63(3) 591-594, 1999; Feldherg et al, Antimicrobial Agents and
Chemotherapy, December 1988, 1763-1768; Munchberg et al, Org.
Biomol. Chem., 2007, 5, 1505-1518; among others. Considering that
DDMO is an stabilized allicin molecule owing its antimicrobial
action precisely to this allicin fragment, whose activity is
preserved without alteration as shown in the microbiological
tests.
[0058] The microbiological challenges were made with collection
microorganisms, universally required to test the product
effectiveness. The results proved that in 30 seconds of contact
with the composition from Example 1, 100.00% was removed from the
challenged microorganisms, including Candida albicans. The results
from the study are shown in Table 1.
TABLE-US-00001 TABLE 1 Studies from microbial challenge Test
Microorganism Contact Time 30 Sec Escherichia coli 100% ATCC 10536
Pseudomona aerugiosa 100% ATCC 9027 Klebsiellapneumoniae 100% ATCC
10031 Proteus vulgaris 100% ATCC 6380 Staphylococcus aureus 100%
ATCC 6538 Staphylococcus epidermis 100% ATCC 12228 Candida albicans
100% ATCC 1031
[0059] Additionally, challenge tests were made against
Propionilbacterium acnes, anaerobic bacteria previously referred to
as one of the main causes of infection caused by acne, thus
obtaining excellent results, such as it is shown below in Table
2.
TABLE-US-00002 TABLE 2 Contact Time Eradication Test Microorganism
30 seconds 60 seconds Propionibacterium acnes 98% 99.999%
[0060] The results of these microbial challenges are more
encouraging that those reported by Fujisawa et al, Biosci.
Biotechnol. Biochem. 73 (9) 1984-1955, 2009; Tsao et al Journal of
Medical Microbiology (2007) 56, 803-808. And they confirm the
review by Ankri and Mirelman, Microbes and Infection, 2, 1999,
125-129 and by Domingo and Lopez-Brea in Rev. Esp. Quimioterap.
December 2003, Vol. 16 (no. 4) 285-293 (2003).
EXAMPLE 1
[0061] An antimicrobial and antiseptic hydrosoluble composition was
prepared containing:
TABLE-US-00003 Component Kg a-hydroxyethanoic acid 57.1 DDMO 4
Sodium lauryl sulfate 50 Sodium lauryl ether sulfate 50 Glycerin
2.5 Blue fragrance 3 Purified water 333.4
EXAMPLE 2
[0062] A second composition was prepared containing the following
elements:
TABLE-US-00004 Component Kg a-hydroxyethanoic acid 58 DDMO 5 Sodium
lauryl sulfate 40 Sodium lauryl ether sulfate 60 Ethylene glycol
2.5 Floral fragrance 3 Purified water 331.5
EXAMPLE 3
[0063] A third example of the object compositions of the present
invention is shown, thus proving that the embodiments of the same
only limit to preserving the homogeneous distribution aspects of
all components.
TABLE-US-00005 Component Kg a-hydroxyethanoic acid 57.1 DDMO 4
Sodium lauryl ether sulfate 100 Sorbitol 2 Blue fragrance 3
Purified water-ethanol (9:1) 333.9
Clinical Trials:
[0064] A clinical trial was made applying the product of the
present invention (example 1) during 28 days to 20 patients with
moderate acne, according to the classification shown in Table 3
below.
TABLE-US-00006 TABLE 3 Grade* Description 0 Clean skin with no
inflammatory or non-inflammatory wounds 1 Almost clean; Little
non-inflammatory wounds and no more tan two inflammatory wounds 2
Middle severity; greater than grade 1; some non-inflammatory
wounds, few inflammatory wounds (only papules/pustules; no nodular
wounds) 3 Moderate severity; greater than grade 2; many
non-inflammatory wounds and several can be inflammatory, but no
more than two nodular wounds. 4 Severe; greater than grade 3; many
inflammatory and non- inflammatory wounds; and some nodular wounds.
*FDA's classification scale of acne
[0065] The number of wounds from each patient was counted by two
different observers before treatment and during the same each week.
The resulting data is shown in table 4, wherein it can be seen that
the treatment gave an average reduction close to 35% of the active
wounds after 28 days of treatment.
TABLE-US-00007 TABLE 4 No. Of Inflammatory Wounds Number Day 0 7
days 14 days 21 days 28 days 1 58 +/- 5 51 +/- 5 45 +/- 4 41 +/- 3
37 +/- 3
[0066] On the other hand, patients were asked to assess the
presence of grease, through the use of drying paper, measuring the
number of sheets needed in order not to get the forehead stained 2
hours after cleaning with the product, thus discovering that
patients considerably reduced the number of drying sheets used for
cleaning the grease, the results are shown in Table 5.
TABLE-US-00008 TABLE 5 No. Of Sheets Day 0 7 days 14 days 21 days
28 days 5 +/- 2 2 +/- 2 1 +/- 2 1 +/- 1 1 +/- 1
[0067] The results show that the antiseptic, antiseborrheic and
exfoliating composition of the present invention is able to achieve
an effective treatment for seborrhea and acne. These results show
that the treatment for these disorders according to the present
invention is clearly better than the pre-existing methods.
* * * * *