(19)

& 
(11) EP 1 549 327 B1
(12) EUROPEAN PATENT SPECIFICATION

(45) Date of publication and mention (51) Int Cl.:

of the grant of the patent: A61K 31/136 (2006.01) A61P 9/14 (2006.01)
16.11.2011 Bulletin 2011/46 A61K 47/06 (2006.01) A61K 9/00 (2006.01)

(21) Application number: 03808036.2 (86) International application number:

PCT/US2003/022816
(22) Date of filing: 22.07.2003
(87) International publication number:
WO 2004/032944 (22.04.2004 Gazette 2004/17)

(54) COMPOSITION FOR TREATING HEMORRHOIDS

Zusammensetzung zur Behandlung von Hämorrhoiden
COMPOSITION POUR LE TRAITEMENT DES HEMORROIDES

(84) Designated Contracting States: (74) Representative: Tomkinson, Alexandra

AT BE BG CY CZ DE DK EE ES FI FR GB GR HU Bailey Walsh & Co L.L.P.
IT NL PT RO SE SI SK TR 5 York Place
Leeds LS1 2SD (GB)
(30) Priority: 10.10.2002 US 190718
28.04.2003 US 424394 (56) References cited:
WO-A-01/28515 US-A- 3 812 250
(43) Date of publication of application: US-A- 4 626 433 US-A- 4 746 675
06.07.2005 Bulletin 2005/27 US-B1- 6 242 010

(73) Proprietor: Carroll, Gaye L. • DATABASE WPI Week 199444 Thomson

Magnolia, AR 72753 (US) Scientific, London, GB; AN 1992-147958
XP002525035 & JP 06 092317 B (NIPPON KURIN
(72) Inventor: Carroll, Gaye L. GEJI K) 16 November 1994 (1994-11-16)
Magnolia, AR 72753 (US)
EP 1 549 327 B1

Note: Within nine months of the publication of the mention of the grant of the European patent in the European Patent
Bulletin, any person may give notice to the European Patent Office of opposition to that patent, in accordance with the
Implementing Regulations. Notice of opposition shall not be deemed to have been filed until the opposition fee has been
paid. (Art. 99(1) European Patent Convention).

Printed by Jouve, 75001 PARIS (FR)

 1 EP 1 549 327 B1
Description
Field of the Invention
[0001] The present invention relates to a composition
which is particularly useful in the treatment of hemor-
rhoids. More particularly, the present invention relates to
a hemorrhoid-treating composition which includes an
ointment mixture of the antiseptic and bactericide gentian
violet (methylrosaniline) and a lubricant such as petrole-
um jelly, also known as petrolatum or mineral jelly. The
composition further includes a suppository capsule. The
composition imparts a soothing and healing effect on
swollen hemorrhoids, and particularly, on bleeding hem-
orrhoids.
Background of the Invention
[0002] Hemorrhoids are swollen blood vessels in the
rectum. There are two basic types of hemorrhoids: inter-
nal and external. Internal hemorrhoids are swollen and
inflamed veins far up in the rectum. Internal hemorrhoids
cannot be seen or felt and usually are not painful due to
the paucity in nerve endings in the upper portion of the
rectum. While internal hemorrhoids are most commonly
manifested by anal bleeding, they may prolapse, or pro-
trude outside the anal sphincter. Usually, prolapsed in-
ternal hemorrhoids may be gently pushed back into place
in the rectum.
[0003] External hemorrhoids are swollen blood ves-
sels in the anus and are usually manifested by pain as
well as bleeding. When external hemorrhoids prolapse,
or protrude from the anal sphincter, blood clots some-
times form, causing an extremely painful condition known
as thrombosis. While they usually disappear by them-
selves within about a week, thrombosed hemorrhoids
may be removed by a physician or may be treated with
a pain-reducing medication to reduce the pain.
[0004] It is believed that hemorrhoids are caused by
the exertion of abdominal pressure on rectal veins, caus-
ing the veins to swell and become irritated. The abdom-
inal pressure may be caused by a variety of factors and
conditions including obesity, pregnancy, prolonged
standing or sitting, liver disease, straining during bowel
movements, coughing, sneezing, vomiting or holding the
breath during physical activity. Hemorrhoids are largely
preventable by the adoption of a high-fiber diet. On the
other hand, persons whose diet consists largely of low-
fiber, processed foods tend to run the highest risk of de-
veloping hemorrhoids. Furthermore, inadequate fluid in-
take can contribute to the development of hemorrhoids
by causing the development of hard stools which irritate
and inflame the rectal veins.
[0005] About half of persons living in the United States
will be afflicted with hemorrhoids at some point during
their lives. Hemorrhoids most often strike persons be-
tween the ages of 20 and 50. Some evidence indicates
that "weak" veins, which are most susceptible to devel-
2
oping hemorrhoids, are inherited.
[0006] US-A-3 812 250 discloses a vaginal supposito-
ry comprising methylrosaniline for use in the treatment
of vaginal fungus infestations and JP-B-609 2317 dis-
5 closes a combination therapy comprising the antifungal
miconazole nitrate, gentamycin and hydrocortisone for
use in the treatment of hemorrhoids.
Summary of the Invention
10
[0007] The present invention is generally directed to a
composition for the treatment of hemorrhoids. More par-
ticularly, the present invention relates to a hemorrhoid-
treating composition which includes a mixture of the an-
15 tiseptic and bactericide gentian violet (methylrosaniline)
and a lubricant such as petroleum jelly, also known as
petroleum or mineral jelly. In another embodiment, the
composition is prepared as a suppository using a suitable
suppository base. The composition imparts a soothing
20 and bealing effect on swollen hemorrhoids, and particu-
larly, on bleeding hemorrhoids.
Description of the Preferred Embodiments
25 [0008] The present invention includes a composition
for the treatment of hemorrhoids, particularly external he-
morrhoids. The composition is easy to apply and pro-
motes pain reduction, as well as healing, of the hemor-
rhoids, including inflammation and torn tissue associated
30 with hemorrhoids. In a preferred embodiment, the com-
position includes an ointment mixture of non-prescription
strength, 1% gentian violet (methylrosaniline) which is
thoroughly mixed with a lubricant such as petroleum jelly,
also known as petrolatum or mineral jelly. The methylro-
35 saniline is an effective antiseptic and bactericide which
prevents or fights infection and reduces pain. The lubri-
cant provides a vehicle for effective delivery of the meth-
ylrosaniline to the inflamed hemorrhoid tissue. In a typical
embodiment, the composition includes seven (7) drops
40 of the liquid methylrosaniline bactericide/antiseptic per
teaspoon of the lubricant. The bactericide/antisepcic may
be dispensed from a medicine dropper such as an EZY
CARE® straight-tip or bent-tip, glass medicine dropper
available from Apothecary Products, inc. of Minneapolis,
45 MN. The EZY CARE® medicine dropper has a capacity
of 1ml of liquid, or approximately 30-35 drops. Accord-
ingly, in a preferred embodiment the composition mixture
includes at least 0.2ml to 0.3ml of the methylrosaniline
per teaspoon of lubricant.
50 [0009] However it is understood that other types of
medicine droppers may be used to dispense the drops
into the lubricant. After the methylrosaniline is added to
the lubricant, the two components are thoroughly mixed
until the composition mixture assumes the substantially
55 homogenous violet color of the methylrosaniline. After
formation, the composition is typically placed in a typically
6 oz capped, plastic applicator rube for subsequent ap-
plication.
2
 3 EP 1 549 327 B1
[0010] In another embodiment, the composition is pre-
pared in the form of a suppository capsule using a suit-
able suppository vehicle or base. Preferably, the suppos-
itory base is glycerinated gelatin, although alternative
suppository bases, including cocoa butter and polyeth-
ylene glycol, in non-exclusive particular, may be used.
The active ingredient baciertcide/annseptic gentian violet
(methylrosaniline) is added to the suppository base in a
quantity of typically at least 0.2ml to 0.3ml of 1% non-
prescription strength gentian violet (methylrosaniline) per
teaspoon (5ml) of suppository base. The methylro-
saniline may be dispensed from a medicine dropper such
as an EZY CARE® straight-tip or bent-tip, glass medicine
dropper available from Apothecary Products, Inc of Min-
neapolis, MN, for example. The therapeutic quantity of
methylrosaniline equates to typically at least seven (7)
drops of the methylrosaniline per teaspoon of suppository
base. The methylrosaniline is then thoroughly mixed with
the suppository base to obtain a substantially homoge-
nous suppository mixture. One teaspoon of the suppos-
itory mixture may be formed or shaped into two suppos-
itory capsules each having dimensions of typically about
2.25 inch in diameter and 1.5 inch in length, with a tapered
end for anal insertion of the suppository. In that case,
each suppository capsule typically has at least 2-4 drops
of the methylrosaniline. However, it is understood that
the suppository mixture may be shaped into suppository
capsules having any suitable dimensions and shape.
[0011] One possibly method of applying the ointment
composition to the inflamed hemorrhoidal tissue includes
dispensing the composition from a typically 6-ounce,
capped plastic tube. A replaceable applicator cap having
a smooth, rounded applicator tip may be provided on the
capped tube for applying the composition to the hemor-
rhoids in the anal area. Preferably, the applicator tip is
–" long, and the top of the 6ounce tube, as well as the
base of the applicator tip, is ’" in diameter. The applicator
rip tapers from the ’" base to the h" tip thereof. Appli-
cator openings arc provided in the sides of the applicator
tip for dispensing the composition from the tip to the in-
flamed hemorrhoidal tissue.
[0012] It is understood that the tube and applicator cap
heretofore described represent only one example of stor-
age and application of the composition. Accordingly, the
composition may be stored in any type of suitable con-
tainer for subsequent application, and may be applied
through the applicator cap heretofore described or
through any other type of applicator or other instrument
suitable for the purpose. The composition may also be
applied manually to the inflamed area. Furthermore, the
patient afflicted with prolapsed hemorrhoids may lubri-
cate his or her fingers with the composition mixture and
use the lubricated fingers to gently push the prolapsed
hemorrhoidal tissue back into the anal canal The com-
position mixture reduces hemorrhoidal pain and pro-
motes healing of the inflamed hemorrhoidal tissue.
[0013] The invention will be better understood by con-
sideration of the following examples
4
EXAMPLE 1
[0014] A composition mixture was prepared by drop-
ping seven (7) drops of non-prescription strength gentian
5 violet (methylrosaniline) bactericide/antiseptic, using an
EZY CARE® medicine dropper, into one (1) teaspoon of
petroleum jelly and then thoroughly mixing the methylro-
saniline with the petroleum jelly until the resulting com-
position mixture assumed the substantially homogenous
10 violet color of the methylrosaniline. The composition mix-
ture was placed in 6-ounce capped tube having an ap-
plicator cap for subsequent application of the composi-
tion to inflamed hemorrhoidal tissue.
15 EXAMPLE 2
[0015] The composition mixture prepared according to
EXAMPLE 1 above was applied to the inflamed hemor-
rhoidal tissue of a patient using the applicator cap on the
20 tube. The composition mixture was applied as often as
necessary to relieve pain. The composition mixture sig-
nificantly reduced pain associated with the hemorrhoids
and promoted healing of the inflamed hemorrhoidal tis-
sue.
25
EXAMPLE 3
[0016] A patient afflicted with inflamed hemorrhoids
applied the composition mixture prepared according to
30 EXAMPLE 1 to the patient’s inflamed hemorrhoidal tissue
using the patient’s fingers. The composition mixture was
applied as often as necessary to relieve pain. The com-
position mixture significantly reduced pain associated
with the hemorrhoids and promoted healing of the in-
35 flamed hemorrhoidal tissue.
EXAMPLE 4
[0017] A patient afflicted with prolapsed hemorrhoids
40 lubricated the patient’s fingers using the composition mix-
ture prepared according to EXAMPLE 1 above. The pa-
tient used the lubricated fingers to gently push the pro-
lapsed hemorrhoids back into the patient’s anal canal.
The composition significantly reduced pain associated
45 with the hemorrhoids and promoted healing of the in-
flamed hemorrhoidal tissue.
EXAMPLE 5
50 [0018] Suppository capsules were prepared by drop-
ping seven (7) drops of non-prescription strength gentian
violet (methylrosaniline) bactericide/antiseptic, using an
EZY CARE® medicine dropper, into one (1) teaspoon of
glycerinated gelatin and then thoroughly mixing the meth-
55 ylrosaniline with the glycerinated gelatin until the result-
ing suppository mixture was substantially homogenous.
The suppository mixture was shaped into two (2) sup-
pository capsules for subsequent anal insertion to treat
3
 5 EP 1 549 327 B1
inflamed hemorrhoidal tissue.
EXAMPLE 6
[0019] A suppository capsule prepared according to
EXAMPLE 5 above was applied by anal insertion to in-
flamed hemorrhoidal tissue of a patient. The suppository
capsules were applied as often as necessary to relieve
pain. The suppository capsules significantly reduced
pain associated with the hemorrhoids and promoted
healing of the inflamed hemorrhoidal tissue.
Claims
1. Use of a composition for the manufacture of a med-
icament for treating hemorrhoids, characterised in
that said composition comprising;
a quantity of methylrosaniline mixed with a quantity
of lubricant or a pharmaceutically acceptable sup-
pository base to define a composition mixture.
2. Use of the composition of claim 1 wherein said lu-
bricant comprises petroleum jelly.
3. Use of the composition of claim 1 wherein said meth-
ylrosaniline and said lubricant arc present in said
composition mixture in a ratio of at least 0.2ml to
0.3ml of said methylrosaniline per teaspoon of said
lubricant.
4. Use of a composition of claim 1 wherein said sup-
pository base comprises glycerinated gelatin, cocoa
butter or polyethylene glycol.
5. Use of a composition of claim 1 wherein said meth-
ylrosaniline is present in said suppository base in a
ratio of at least 0.2ml to 0.3ml of said methylro-
saniline per teaspoon of said suppository base.
Patentansprüche
1. Verwendung einer Zusammensetzung für die Her-
stellung eines Medikaments zur Behandlung von
Hämorrhoiden, dadurch gekennzeichnet, dass
die Zusammensetzung Folgendes umfasst:
eine Methylrosanilinmenge, gemischt mit einer
Gleitmittelmenge oder einer pharmazeutisch
akzeptablen Zäpfchenbasis zum Definieren ei-
nes Zusammensetzungsgemischs.
2. Verwendung der Zusammensetzung nach Anspruch
1, wobei das genannte Gleitmittel Vaseline umfasst.
3. Verwendung der Zusammensetzung nach Anspruch
1, wobei das genannte Methylrosanilin und das ge-
6
nannte Gleitmittel in dem genannten Zusammenset-
zungsgemisch in einem Verhältnis von wenigstens
0,2 ml zu 0,3 ml des genannten Methylrosanilins pro
Teelöffel des genannten Gleitmittels vorhanden
5 sind.
4. Verwendung einer Zusammensetzung nach An-
spruch 1, wobei die genannte Zäpfchenbasis Glyce-
ringelatine, Kakaobutter oder Polyethylenglykol auf-
10 weist.
5. Verwendung einer Zusammensetzung nach An-
spruch 1, wobei das genannte Methylrosanilin in der
genannten Zäpfchenbasis in einem Verhältnis von
15 wenigstens 0,2 ml bis 0,3 ml des genannten Methyl-
rosanilins pro Teelöffel der genannten Zäpfchenba-
sis vorhanden ist.
20 Revendications
1. Utilisation d’une composition pour la fabrication d’un
médicament pour le traitement d’hémorroïdes, ca-
ractérisée en ce que ladite composition compre-
25 nant:
une [certaine] quantité de méthylrosaniline mé-
langée à une [certaine] quantité de lubrifiant ou
à une base pour suppositoires acceptable phar-
30 maceutiquement pour définir un mélange de
composition.
2. Utilisation de la composition selon la revendication
1, ledit lubrifiant comprenant de la gelée de pétrole.
35
3. Utilisation de la composition selon la revendication
1, ladite méthylrosaniline et ledit lubrifiant étant pré-
sents dans ledit mélange de composition dans un
rapport d’au moins 0,2 à 0,3 ml de ladite méthylro-
40 saniline par cuillerée à café dudit lubrifiant.
4. Utilisation d’une composition selon la revendication
1, ladite base pour suppositoires comprenant de la
gélatine glycérinée, du beurre de cacao ou du poly-
45 éthylène glycol.
5. Utilisation d’une composition selon la revendication
1, ladite méthylrosaniline étant présente dans ladite
base pour suppositoires dans un rapport d’au moins
50 0,2 à 0,3 ml de ladite méthylrosaniline par cuillerée
à café de ladite base pour suppositoires.
55
4
 EP 1 549 327 B1

REFERENCES CITED IN THE DESCRIPTION

This list of references cited by the applicant is for the reader’s convenience only. It does not form part of the European
patent document. Even though great care has been taken in compiling the references, errors or omissions cannot be
excluded and the EPO disclaims all liability in this regard.

Patent documents cited in the description

• US 3812250 A [0006] • JP 6092317 B [0006]