WO1998034628A1 - Composition for the treatment of haemorrhoids and other anorectal inflammations - Google Patents

Composition for the treatment of haemorrhoids and other anorectal inflammations Download PDF

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Publication number
WO1998034628A1
WO1998034628A1 PCT/GB1997/000338 GB9700338W WO9834628A1 WO 1998034628 A1 WO1998034628 A1 WO 1998034628A1 GB 9700338 W GB9700338 W GB 9700338W WO 9834628 A1 WO9834628 A1 WO 9834628A1
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WO
WIPO (PCT)
Prior art keywords
parts
weight
mixture
lotion
mixing
Prior art date
Application number
PCT/GB1997/000338
Other languages
French (fr)
Inventor
Jeffery Wade Ivy
Curtis Emery Payne
Christopher Dominic Burda
Original Assignee
Au Pharmaceuticals, Inc.
Kiddle, Simon, John
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Au Pharmaceuticals, Inc., Kiddle, Simon, John filed Critical Au Pharmaceuticals, Inc.
Priority to AU16122/97A priority Critical patent/AU1612297A/en
Priority to PCT/GB1997/000338 priority patent/WO1998034628A1/en
Publication of WO1998034628A1 publication Critical patent/WO1998034628A1/en

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/53—Lamiaceae or Labiatae (Mint family), e.g. thyme, rosemary or lavender
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/16—Ginkgophyta, e.g. Ginkgoaceae (Ginkgo family)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/23—Apiaceae or Umbelliferae (Carrot family), e.g. dill, chervil, coriander or cumin
    • A61K36/232—Angelica
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/25—Araliaceae (Ginseng family), e.g. ivy, aralia, schefflera or tetrapanax
    • A61K36/258—Panax (ginseng)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/53—Lamiaceae or Labiatae (Mint family), e.g. thyme, rosemary or lavender
    • A61K36/532—Agastache, e.g. giant hyssop
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/88—Liliopsida (monocotyledons)
    • A61K36/886—Aloeaceae (Aloe family), e.g. aloe vera
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/88—Liliopsida (monocotyledons)
    • A61K36/898—Orchidaceae (Orchid family)

Definitions

  • the present invention relates to compositions for the treatment of haemorrhoids and other anorectal inflammation, to the medical uses of these compositions and methods of making the compositions.
  • the present invention relates to compositions comprising hamamelis water (witch hazel) , menthol and epinephrine and/or ephedrine or pharmaceutically acceptable salts thereof.
  • These compositions can be formulated as externally applied lotions for treating irritation or mild inflammation of the skin or mucous membranes, thereby relieving pain in haemorrhoids and other anorectal inflammation.
  • the present invention broadly concerns compositions comprising hamamelis water, menthol and epinephrine and/or ephedrine, or pharmaceutically acceptable salts thereof, such as epinephrine hydrochloride and/or ephedrine sulphate, in combination with a pharmaceutically acceptable carrier.
  • compositions are useful in the treatment of hemorrhoids or other forms of anorectal inflammation.
  • the compositions are formulated as lotions suitable for delivery by a spray to the site of application of a patient.
  • hamamelis water is present in the composition in an amount from about 5.0 to 30.0 parts by weight, more preferably from about 9.0 to 27.5 parts by weight, and still more preferably from about 9.0 to 11.0 parts by weight or from about 22.5 to 27.5 parts by weight.
  • menthol is present in the composition in an amount from 0.01 to 0.5 parts by weight, more preferably from about 0.05 to 0.2 parts by weight, and still more preferably from about 0.09 to 0.11 parts by weight.
  • the epinephrine or pharmaceutically acceptable salt thereof is present in the composition in an amount from about 0.001 to 0.01 parts by weight, more preferably from about 0.002 to 0.007 parts by weight and still more preferably from about 0.0045 and 0.0055 parts by weight.
  • the ephedrine is present in an amount from 0.10 to 0.50 parts by weight, more preferably from about 0.20 to 0.3 parts by weight, and still more preferably from about 0.225 to 0.275 parts by weight.
  • each essential oil included is present in an amount 0.01 to 0.5 parts by weight, more preferably from about 0.05 to 0.10 parts by weight.
  • the essential oils are selected from the group consisting of vanilla, hyssop, melissa, angelica and/or lavender oils.
  • the present invention provides a composition comprising:
  • the present invention provides a composition comprising:
  • compositions may further comprise gingko, preferably in an amount from about 0.01 to 0.5 parts by weight. Additionally or alternatively, the compositions may comprises aloe powder, preferably in an amount from about 1.0 to 10.0 parts by weight, and more preferably from about 4.0 to 5.0 parts by weight .
  • the present invention provides a compositions as described above for use in a method of medical treatment.
  • the present invention provides the use of a composition as described above in the preparation of a medicament for the treatment of hemorrhoids or other anorectal inflammation.
  • this invention provides an externally applied composition (e.g. a lotion) for relieving pain in haemorrhoids and other anorectal inflammation and the method of making such lotion.
  • the active ingredients of the invention perform the five functions of vasoconstrictor, astringent, analgesic, antipruritic and anaesthetic.
  • the compositions are formulated to have a viscosity to enable the analgesic lotion to be applied by a spray applicator directly to the site of application, providing temporary relief from the pain and burning sensations caused by inflamed haemorrhoidal tissues and other anorectal inflammation.
  • the compositions additionally temporarily reduce the swelling associated with irritation in haemorrhoids and other anorectal disorders .
  • the active ingredient of the invention can be formulated in a wide variety of compositions which may comprise, in addition to one of the above substances, a pharmaceutically acceptable excipient, carrier, buffer, stabiliser or other materials well known to those skilled in the art. Such materials should be non-toxic and should not interfere with the efficacy of the active ingredient.
  • Exemplary ingredients of carriers include one or more of purified water, Carbomer, polypropylene glycol, methylparaben, propylparaben, EDTA, DEA cetyl phosphate, stearic acid, glycyl stearate, PEG 100 stearate, C 12-15 alkyl benzoate, jojoba oil, ginseng, imidazolidinyl urea and/or triethanolamine .
  • the compositions can be administered by the patient or a physician in a "therapeutically effective amount", this being sufficient to show benefit to the individual .
  • the actual amount of the composition administered, and rate and time-course of administration, will depend on the nature and severity of what is being treated. Prescription of treatment, e.g.
  • hamamelis water is contained in the lotion in an amount from 9.0000 to 11.0000 parts by weight and, preferably, in an amount of about 10.0000 parts by weight.
  • Epinephrine hydrochloride is contained in the lotion in an amount from 0.0045 to 0.0055 parts by weight and preferably, in an amount of about 0.0050 parts by weight.
  • Menthol crystals are contained in the lotion in an amount from 0.0900 to 0.1100 parts by weight and, preferably, in an amount of about 0.1000 parts by weight.
  • Aloe powder such as that sold under the name Aloe Vera
  • Phytogel 1:199 is contained in the lotion in an amount from 4.0653 to 4.9687 parts by weight and, preferably, in an amount of about 4.5170 parts by weight.
  • Purified water is contained in the lotion in an amount from 64.2907 to 78.5775 parts by weight and, preferably, in an amount of about 71.4341 parts by weight.
  • Carbomer also known as carboxy polymethylene, such as that sold by B. F. Goodrich under the name Carbopol 1342, is contained in the lotion in an amount from 0.3499 to 0.4277 parts by weight and, preferably, in an amount of about 0.3888 parts by weight .
  • Propylene glycol such as that sold by ARCO Chemical Company under the name Propylene Glycol USP, is contained in the lotion in an amount from 4.0000 to 4.8888 parts by weight and, preferably, in an amount of about 4.4444 parts by weight.
  • Methylparaben also known as methyl hydroxybenzoate, such as that sold by NIPA Laboratories, Inc under the name Nipa Esters methyl p-hydroxybenzoate, is contained in the lotion in an amount from 0.1000 to 0.1222 parts by weight and, preferably, in an amount of about 0.1111 parts by weight.
  • Propylparaben also known as propyl hydroxybenzoate
  • Propylparaben is contained in the lotion in an amount from 0.1000 to 0.1222 parts by weight and, preferably, in an amount of about 0.1111 parts by weight .
  • Tetrasodium ethylenediaminetetraacetate is contained in the lotion in an amount from 0.1000 to 0.1222 parts by weight and, preferably, in an amount of about 0.1111 parts by weight .
  • Diethanolamine cetyl phosphate such as that sold by Givaudan Corporation under the name Amphisol, is contained in the lotion in an amount from 0.7000 to 0.8555 parts by weight and, preferably, in an amount of about 0.7777 parts by weight .
  • Stearic acid is contained in the lotion in an amount from 1.0000 to 1.2222 parts by weight and, preferably, in an amount of about 1.1111 parts by weight.
  • Glyceryl stearate is contained in the lotion in an amount from 0.2500 to 0.3055 parts by weight and, preferably, in an amount of about 0.2777 parts by weight.
  • PEG 100 stearate is contained in the lotion in an amount from 0.2500 to 0.3055 parts by weight and, preferably, in an amount of about 0.2777 parts by weight.
  • C 12-15 alkyl benzoate such as that sold by Finetex, Inc under the name Finsolv TN, is contained in the lotion in an amount from 5.0000 to 6.1111 parts by weight and, preferably, in an amount of about 5.5555 parts by weight.
  • Jojoba oil such as that sold by LIPO Chemicals, Inc under the name Lipovol J, is contained in the lotion in an amount from
  • Ginseng American 1:1 PB propylene glycol
  • PB propylene glycol
  • GERMALL 115 is contained in the lotion in an amount from 0.2000 to 0.2444 parts by weight and, preferably, in an amount of about 0.2222 parts by weight.
  • Triethanolamine is contained in the lotion in an amount from 0.2000 to 0.2444 parts by weight and, preferably, in an amount of about 0.2222 parts by weight.
  • the active ingredient hamamelis water (witch hazel) performs the function of an astringent.
  • the active ingredient epinephrine hydrochloride performs the function of a vasoconstrictor.
  • the active ingredient menthol performs three functions of an analgesic, antipruritic, and anaesthetic.
  • the preferred embodiment of the invention is in a lotion form which may be directly applied to the site of the haemorrhoids or other anorectal inflammation.
  • Purified water in an amount from 64.2907 to 78.5775 parts by weight is supplied in a stainless steel kettle equipped with a mixer and a heat exchanger attached to the kettle for heating and cooling the ingredients in the kettle.
  • the 75 °C mixture is then cooled to 55 °C.
  • a solution having a temperature of 55 °C and obtained from 2.0000 to 2.4444 parts by weight C 12-15 alkyl benzoate, from 0.0900 to 0.1100 parts by weight menthol crystals is mixed into the 55 °C mixture.
  • the 55°C mixture is then cooled to a temperature of no more than 45°C.
  • 0.2000 to 0.2444 parts by weight ginseng American 1:1 propylene glycol, from 0.2000 to 0.2444 parts by weight imidazolidinyl urea, and from 0.2000 to 0.2444 parts by weight triethanolamine are then mixed into the 45 °C mixture.
  • first alternative embodiment of the invention certain essential oils may be added to provide additional cooling and lubrication for the lotion.
  • the first alternative embodiment of the invention comprises the formula of the preferred embodiment of the invention together with the following essential oils.
  • Vanilla planifolia is contained in the first alternative embodiment of the lotion in an amount of from 0.5400 to 0.6600 parts by weight and, preferably, in an amount of about 0.6000 by weight .
  • Hyssopus officinalis is contained in the first alternative embodiment of the lotion in an amount of from 0.0900 to 0.1100 parts by weight and, preferably, in an amount of about 0.1000 by weigh .
  • Melissa officinalis is contained in the first alternative embodiment of the lotion in an amount of from 0.0900 to 0.1100 parts by weight and, preferably, in an amount of about 0.1000 by weight .
  • the essential oil Angelica (from the botanical species), is the essential oil Angelica (from the botanical species).
  • Angelica archangelia is contained in the first alternative embodiment of the lotion in an amount of from 0.0900 to 0.1100 parts by weight and, preferably, in an amount of about 0.1000 by weight .
  • Lavendula officinalis is contained in the first alternative embodiment of the lotion in an amount of from 0.0900 to 0.1100 parts by weight and, preferably, in an amount of about 0.1000 by weight .
  • the amount of purified water is adjusted to be from 63.3906 to 77.4774 parts by weight instead of from 64.2907 to 78.5775 parts by weight in order to accommodate the added volume of the essential oils.
  • the essential oils are added to the lotion after the epinephrine hydrochloride is added.
  • the ingredient gingko may be added to the formulation.
  • gingko is contained in the lotion in an amount from 0.2000 to 0.2444 parts by weight and, preferably, in an amount of about 0.2222 parts by weight.
  • the amount of purified water in each alternative embodiment is adjusted to compensate for the weight of the gingko.
  • the gingko is added to the lotion when the ginseng is added.
  • Adding 0 000 to 0.2444 parts by weight of gingko to the first alternative em-xxiiment of the invention will cause the amount of purified water in this second alternative embodiment of the invention to be present in an amount from 63.1908 to 772330 parts by weight and, preferably, in an amount of about 70.2119 parts by weight
  • Adding 02000 to 0.2444 parts by weight of gingko to the preferred embodiment of the invention will cause the amount of purified water in this third alternative embodiment of the invention to be present in an amount from 64.0908 to 78.3330 parts by weight and, preferably, in an amount of about 71.211 parts by weight.
  • the active ingredient epinephrine hydrochloride may be replaced by the active ingredient ephedrine sulfate.
  • ephedrine sulfate is contained in the lotion in an amount from 0.2250 to 0.2750 parts by weight and, preferably, in an amount of about 02500 parts by weight
  • the amount of hamamelis water is contained in the lotion in an amount from 22.5000 to 27.5000 parts by weight and, preferably, in an amount of about 25.0000 parts by weight
  • the amount of purified water in this fourth alternative embodiment of the invention is then adjusted to be present in an amount from 50.5701 to 61.8079 parts by weight and, preferably, in an amount of about 56.1890 parts by weight
  • the other ingredients are present in the same amounts are they are in the preferred embodiment of the invention.
  • the following example describes the steps to be followed in manufacturing this fourth alternative embodiment of the invention.
  • Purified water in an amount from 63.3906 to 77.4774 parts by weight is supplied in a stainless steel kettle equipped with a mixer and a heat exchanger attached to the kettle for heating and cooling the ingredients in the kettle.
  • the 75 ° C. mixture is then cooled to 55 ° C.
  • a solution having a temperature of 55 ° C. and obtained from 2.0000 to 2.4444 parts by weight C 12-15 alkyl benzoate, from 0.0900 to 0.1100 parts by weight menthol crystals is mixed
  • the 55 ° C. mixture is then cooled to a temperature of no more than 45 ° C.
  • ginseng American 1:1 propylene glycol from 02000 to 02444 parts by weight imidazolidinyl urea, from 02000 to 0.2444 parts by weight triet--anolamine are then mixed into the 45 ° C. mixture.
  • vanilla From 0.5400 to 0.6600 parts by weight vanilla, from 0.0900 to 0.1100 parts hyssop, from
  • a fifth alternative embodiment of the invention may be formed by adding gingko to the formulation of the fourth alternative embodiment of the invention. Adding 020OO to 02444 parts by weight of gingko, and preferably, in an amount of about 02222 parts by weight, to the fourth alternative embodiment of the invention will require the amount of purified water in mis
  • a sixth alternative embodiment of the invention provides a formulation of the invention having a suitable viscosity to enable the lotion to be applied by a spray applicator directly to the site of application.
  • hamamelis water (witch hazel)
  • foe lotion contained in foe lotion in an amount from 9.0000 to 11.0000 parts by weight and, preferably, in an amount of about 10.0000 parts by weight.
  • Epinephrine hydrochloride is contained in the lotion in an amount from 0.0045 to 0.0055 parts by weight and, preferably, in an amount of about 0.0050 parts by weight
  • Menthol crystals are contained in the lotion in an amount from 0.0900 to 0.1100 parts by weight and, preferably, in an amount of about 0.1000 parts by weight
  • Aloe powder such as that sold under the name Aloe Vera Phytogel 1:199, is contained in the lotion in an amount from 4.0500 to 4.9500 parts by weight and, preferably, in an amount of
  • Purified water is contained in the lotion in an amount from 612405 to 74.8495 parts by weight and, preferably, in an amount of about 68.0450 parts by weight
  • Carbomer also known as carboxy polymethylene, such as that sold by B. F. Goodrich under the name Carbopol 1342, is contained in the lotion in an amount from 4.5000 to 5.5000 parts by weight and, preferably, in an amount of about 5.0000 parts by weight
  • Propylene glycol such as that sold by ARCO Chemical Company under the name Propylene Glycol USP, is cc*-t-rined in the lotion in an amount from 3.6000 to 4.4000 parts by
  • Methylparaben also known as methyl hydroxybenzoate, such as that sold by NTPA
  • Nipa Esters methyl p-hydroxybenzoate is contained in the lotion in an amount from 0.1800 to 02200 parts by weight and, preferably, in an amount of about
  • Propylparaben also known as propyl hydroxybenzoate, is contained in the lotion in an amount from 0.0900 to 0.1100 parts by weight and, preferably, in an amount of about 0.1000
  • Tetrasodium efoylenedia inetetraacetate (tetrasodium EDTA) is contained in the lotion
  • Dieth-molamine cetyl phosphate such as that sold by Givaudan Corporation under the name Amphisol, is contained in the lotion in an amount from 0.9000 to 1.1000 parts by weight and, preferably, in an amount of about 1.0000 parts by weight
  • Stearic acid is contained in the lotion in an amount from 0.9000 to 1.1 00 parts by weight and, preferably, in an amount of about 1.0000 parts by weight
  • C 12-15 alkyl benzoate such as that sold by Finetex, Inc. under the name Finsolv TN, is contained in the lotion in an amount from 4.5000 to 5.5000 parts by weight and, preferably, in an amount of about 5.0000 parts by weight
  • Jojoba oil such as that sold by LIPO Chemicals, Inc. under the name Lipovol J, is contained in the lotion in an amount from 0.0900 to 0.1100 parts by weight and, preferably, in an amount of about 0.1000 parts by weight Ginseng American 1 : 1 PB (propylene glycol) is contained in the lotion in an amount from 0.0900 to 0.1100 parts by weight and, preferably, in an amount of about 0.1000 parts by weight Ginseng American 1 : 1 PB (propylene glycol) is contained in the lotion in an amount from
  • Imidazolidinyl urea such as that sold by Sutton Laboratories, Inc. under the name GERMALL 115, is contained in the lotion in an amount from 0.1350 to 0.1650 parts by weight and, preferably, in an amount of about 0.1500 parts by weight
  • Triethanolamine is contained in the lotion in an amount from 0.4500 to 0.5500 parts by weight and, preferably, in an amount of about 0.5000 parts by weight
  • the active ingredient hamamelis water (witch hazel) performs the function of an astringent
  • the active ingredient epinephrine hydrochloride performs the function of a vasoconstrictor.
  • the active ingredient menthol performs the three functions of an analgesic, antipruritic, and
  • Purified water in an amount from 61.2405 to 74.8495 parts by weight is supplied in a stainless steel kettle equipped with a mixer and a heat exchanger attached to the kettle for heating and cooling the ingredients in the kettle.
  • phase A (tetrasodium EDTA) are added and mixed into the smooth and uniform mixture while heating to a tem t xaature of 75 ° C. This solution is referred to as the "phase A" mixture.
  • phase B A second mixture referred to as the "phase B" mixture is mixed as follows. From 0.9000
  • dieth-molamine cetyl phosphate (DEA cetyl phosphate) is mixed with from 0.9000 to 1.1000 parts by weight stearic acid. Then from 4.5000 to 5.5000 parts by weight C 12-15 alkyl benzoate, and from 0.0900 to 0.1100 parts by weight jojoba oil, and from 0.1800 to 02200 parts by weight ginseng, and from 0.0900 to 0.1100 parts by weight propylparaben are
  • phase B M mixture is then mixed into the "phase A” mixture creating a “phase C” mixture.
  • phase C is then mixed into the "phase
  • phase C mixture.
  • the "phase C” mixture is then mixed for about ten minutes at a temperature of
  • phase C 75 ° C.
  • the "phase C” mixture is then cooled to 40 ° C.
  • phase D A "phase D” mixture is then created by mixing from 0.0045 to 0.0055 parts by weight epinephrine hydrochloride and from 0.1350 to 0.1650 parts by weight imidazolidinyl urea at a temperature of approximately 40 ° C.
  • the "phase D” mixture is then mixed into the "phase C” mixture to create the final mixture.
  • the final mixture is then cooled to approximately 25 ° C
  • a seventh alternative embodiment of the invention certain g «wn*H oils may be added to provide additional cooling and lubrication for the lotion.
  • the seventh alternative embodiment of the invention comprises the formula of the sixth alternative embodiment of the invention together with the following essential oils.
  • the essential oil Vanilla (from the botanical species Vanilla plantfolia) is contained in the
  • the seventh alternative embodiment of the lotion in an amount of from 0.0900 to 0.1100 parts by weight and, preferably, in an amount of about 0.1000 by weight
  • the essential oil Hyssop (from the botanical species Hyssopus officinalis) is contained in the seventh alternative embodiment of the lotion in an amount of from 0.0450 to 0.0550 parts by weight and, preferably, in an amount of about 0.0500 by weight
  • the essential oil Melissa (from the botanical species Melissa officinalis) is contained in the seventh alternative embodiment of the lotion in an amount of from 0.0450 to 0.0550 parts by weight and, preferably, in an amount of about 0.0500 by weight
  • the essential oil Angelica (from the botanical species Angelica archangeUa) is contained
  • the essen ial oil Lavender (from the botanical species L v n ⁇ da officinalis) is contained in the seventh alternative embodiment of the lotion in an amount of from 0.0450 to 0.0550 parts by weight and, preferably, in an amount of about 0.0500 by weight
  • the amount of purified water is adjusted to be from 60.9705 to 74.5195 parts by weight instead of from 61 405 to 74.8495 parts by weight in order to accommodate the added volume of the essential oils.
  • Purified water in an amount from 60.9705 to 74.5195 parts by weight is supplied in a stainless steel kettle equipped with a mixer and a heat exchanger attached to the kettle for heating and cooling the ingredients in the kettle.
  • phase B A second mixture referred to as the "phase B" mixture is mixed as follows. From 0.9000 to 1.1000 parts by weight diethanolamine cetyl phosphate (DEA cetyl phosphate) is mixed with from 0.9000 to 1.1000 parts by weight stearic acid.
  • DEA cetyl phosphate diethanolamine cetyl phosphate
  • phase C mixture. From 0.4500 to 0.5500 parts by weight of triethanolamine is then mixed into the "phase C” mixture- The "phase C” mixture is then mixed for about ten minutes at a temperature of approximately 75 ° C. The "phase C” mixture is then cooled to 40 ⁇ C.
  • phase D mixture is then created by mixing from 0.0900 to 0.1100 parts by weight of
  • menthol crystals and from 0.0900 to 0.1100 parts by weight vanilla and from 0.0450 to 0.0550 parts by weight lavender at a temperature of approximately 40 ° C.
  • the "phase D” mixture of menthol and vanilla and lavender is then mixed into the "phase C” mixture to create a new "phase D” mixture consisting of the "phase C” mixture and menthol and vanilla and lavender.
  • phase E rnixture is then created by mixing from 0.0045 to 0.0055 part3 by weight epinephrine hydrochloride and from 0.1350 to 0.1650 parts by weight imidazolidinyl urea at a temperature of approximately 40 ⁇ C.
  • the "phase E” -mxture is then mixed into the "phase D” mixture to create the final mixture.
  • the final mixture is then cooled to approximately 25 • C.

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Abstract

This invention relates to an externally applied lotion that causes irritation or mild inflammation of the skin or mucous membranes for the purpose of relieving pain in haemorrhoids and the method of making such lotion. The formulation of the present invention contains ingredients to perform the five functions of vasoconstrictor, astringent, analgesic, antipruritic, and anesthetic. An alternate embodiment of the invention provides a formulation of the invention having a suitable viscosity to enable the lotion to be applied by a spray applicator directly to the site of application.

Description

COMPOSITION FOR THE TREATMENT OF HAEMORRHOIDS AND OTHER ANORECTAL INFLAMMAΗONS
Field of the Invention
The present invention relates to compositions for the treatment of haemorrhoids and other anorectal inflammation, to the medical uses of these compositions and methods of making the compositions. In particular, the present invention relates to compositions comprising hamamelis water (witch hazel) , menthol and epinephrine and/or ephedrine or pharmaceutically acceptable salts thereof. These compositions can be formulated as externally applied lotions for treating irritation or mild inflammation of the skin or mucous membranes, thereby relieving pain in haemorrhoids and other anorectal inflammation.
Summary of the Invention
Accordingly, the present invention broadly concerns compositions comprising hamamelis water, menthol and epinephrine and/or ephedrine, or pharmaceutically acceptable salts thereof, such as epinephrine hydrochloride and/or ephedrine sulphate, in combination with a pharmaceutically acceptable carrier. These compositions are useful in the treatment of hemorrhoids or other forms of anorectal inflammation. Preferably, the compositions are formulated as lotions suitable for delivery by a spray to the site of application of a patient.
Preferably, hamamelis water (witch hazel) is present in the composition in an amount from about 5.0 to 30.0 parts by weight, more preferably from about 9.0 to 27.5 parts by weight, and still more preferably from about 9.0 to 11.0 parts by weight or from about 22.5 to 27.5 parts by weight.
Preferably, menthol is present in the composition in an amount from 0.01 to 0.5 parts by weight, more preferably from about 0.05 to 0.2 parts by weight, and still more preferably from about 0.09 to 0.11 parts by weight.
Preferably, the epinephrine or pharmaceutically acceptable salt thereof (e.g. epinephrine hydrochloride) is present in the composition in an amount from about 0.001 to 0.01 parts by weight, more preferably from about 0.002 to 0.007 parts by weight and still more preferably from about 0.0045 and 0.0055 parts by weight. Preferably, in compositions comprising ephedrine or a pharmaceutically acceptable salt thereof (e.g. ephedrine sulphate), the ephedrine is present in an amount from 0.10 to 0.50 parts by weight, more preferably from about 0.20 to 0.3 parts by weight, and still more preferably from about 0.225 to 0.275 parts by weight. In embodiments of the invention comprising essential oils, preferably each essential oil included is present in an amount 0.01 to 0.5 parts by weight, more preferably from about 0.05 to 0.10 parts by weight. Preferably, the essential oils are selected from the group consisting of vanilla, hyssop, melissa, angelica and/or lavender oils.
In one preferred embodiment, the present invention provides a composition comprising:
(a) from about 9.0 to 11.0 parts by weight hamamelis water; (b) from about 0'.09 to 0.11 parts by weight menthol; and,
(c) from about 0.0045 to 0.0055 parts by weight epinephrine hydrochloride, in combination with a pharmaceutically acceptable carrier.
In a further preferred embodiment, the present invention provides a composition comprising:
(a) from about 22.5 to 27.5 parts by weight hamamelis water;
(b) from about 0.09 to 0.11 parts by weight menthol; and,
(c) from about 0.225 to 0.275 parts by weight ephedrine sulphate, in combination with a pharmaceutically acceptable carrier.
In some embodiments, the above compositions may further comprise gingko, preferably in an amount from about 0.01 to 0.5 parts by weight. Additionally or alternatively, the compositions may comprises aloe powder, preferably in an amount from about 1.0 to 10.0 parts by weight, and more preferably from about 4.0 to 5.0 parts by weight .
In a further aspect, the present invention provides a compositions as described above for use in a method of medical treatment.
In a still further aspect, the present invention provides the use of a composition as described above in the preparation of a medicament for the treatment of hemorrhoids or other anorectal inflammation. Thus, this invention provides an externally applied composition (e.g. a lotion) for relieving pain in haemorrhoids and other anorectal inflammation and the method of making such lotion. Typically, the active ingredients of the invention perform the five functions of vasoconstrictor, astringent, analgesic, antipruritic and anaesthetic. As noted above, in some embodiments the compositions are formulated to have a viscosity to enable the analgesic lotion to be applied by a spray applicator directly to the site of application, providing temporary relief from the pain and burning sensations caused by inflamed haemorrhoidal tissues and other anorectal inflammation. Preferably, the compositions additionally temporarily reduce the swelling associated with irritation in haemorrhoids and other anorectal disorders .
As mentioned above, the active ingredient of the invention can be formulated in a wide variety of compositions which may comprise, in addition to one of the above substances, a pharmaceutically acceptable excipient, carrier, buffer, stabiliser or other materials well known to those skilled in the art. Such materials should be non-toxic and should not interfere with the efficacy of the active ingredient. Exemplary ingredients of carriers include one or more of purified water, Carbomer, polypropylene glycol, methylparaben, propylparaben, EDTA, DEA cetyl phosphate, stearic acid, glycyl stearate, PEG 100 stearate, C12-15 alkyl benzoate, jojoba oil, ginseng, imidazolidinyl urea and/or triethanolamine . The compositions can be administered by the patient or a physician in a "therapeutically effective amount", this being sufficient to show benefit to the individual . The actual amount of the composition administered, and rate and time-course of administration, will depend on the nature and severity of what is being treated. Prescription of treatment, e.g. decisions on dosage etc, is within the responsibility of general practitioners and other medical doctors, and typically takes account of the disorder to be treated, the condition of the individual patient, the site of delivery, the method of administration and other factors known to practitioners. Examples of the techniques and protocols mentioned above can be found in Remington's Pharmaceutical Sciences, 16th edition, Osol, A. (ed) , 1980.
Detailed Description In the preferred embodiment of the invention hamamelis water (witch hazel) is contained in the lotion in an amount from 9.0000 to 11.0000 parts by weight and, preferably, in an amount of about 10.0000 parts by weight.
Epinephrine hydrochloride is contained in the lotion in an amount from 0.0045 to 0.0055 parts by weight and preferably, in an amount of about 0.0050 parts by weight.
Menthol crystals are contained in the lotion in an amount from 0.0900 to 0.1100 parts by weight and, preferably, in an amount of about 0.1000 parts by weight. Aloe powder, such as that sold under the name Aloe Vera
Phytogel 1:199, is contained in the lotion in an amount from 4.0653 to 4.9687 parts by weight and, preferably, in an amount of about 4.5170 parts by weight.
Purified water is contained in the lotion in an amount from 64.2907 to 78.5775 parts by weight and, preferably, in an amount of about 71.4341 parts by weight.
Carbomer, also known as carboxy polymethylene, such as that sold by B. F. Goodrich under the name Carbopol 1342, is contained in the lotion in an amount from 0.3499 to 0.4277 parts by weight and, preferably, in an amount of about 0.3888 parts by weight .
Propylene glycol, such as that sold by ARCO Chemical Company under the name Propylene Glycol USP, is contained in the lotion in an amount from 4.0000 to 4.8888 parts by weight and, preferably, in an amount of about 4.4444 parts by weight.
Methylparaben, also known as methyl hydroxybenzoate, such as that sold by NIPA Laboratories, Inc under the name Nipa Esters methyl p-hydroxybenzoate, is contained in the lotion in an amount from 0.1000 to 0.1222 parts by weight and, preferably, in an amount of about 0.1111 parts by weight.
Propylparaben, also known as propyl hydroxybenzoate, is contained in the lotion in an amount from 0.1000 to 0.1222 parts by weight and, preferably, in an amount of about 0.1111 parts by weight . Tetrasodium ethylenediaminetetraacetate (tetrasodium EDTA) is contained in the lotion in an amount from 0.1000 to 0.1222 parts by weight and, preferably, in an amount of about 0.1111 parts by weight .
Diethanolamine cetyl phosphate (DEA cetyl phosphate) , such as that sold by Givaudan Corporation under the name Amphisol, is contained in the lotion in an amount from 0.7000 to 0.8555 parts by weight and, preferably, in an amount of about 0.7777 parts by weight .
Stearic acid is contained in the lotion in an amount from 1.0000 to 1.2222 parts by weight and, preferably, in an amount of about 1.1111 parts by weight.
Glyceryl stearate is contained in the lotion in an amount from 0.2500 to 0.3055 parts by weight and, preferably, in an amount of about 0.2777 parts by weight.
PEG 100 stearate is contained in the lotion in an amount from 0.2500 to 0.3055 parts by weight and, preferably, in an amount of about 0.2777 parts by weight.
C 12-15 alkyl benzoate, such as that sold by Finetex, Inc under the name Finsolv TN, is contained in the lotion in an amount from 5.0000 to 6.1111 parts by weight and, preferably, in an amount of about 5.5555 parts by weight.
Jojoba oil, such as that sold by LIPO Chemicals, Inc under the name Lipovol J, is contained in the lotion in an amount from
0.1000 to 0.1222 parts by weight and, preferably, in an amount of about 0.1111 parts by weight. Ginseng American 1:1 PB (propylene glycol) is contained in the lotion in an amount from 0.2000 to 0.2444 parts by weight and, preferably, in an amount of about 0.2222 parts by weight.
Imidazolidinyl urea, such as that sold by Sutton
Laboratories, Inc under the name GERMALL 115, is contained in the lotion in an amount from 0.2000 to 0.2444 parts by weight and, preferably, in an amount of about 0.2222 parts by weight.
Triethanolamine is contained in the lotion in an amount from 0.2000 to 0.2444 parts by weight and, preferably, in an amount of about 0.2222 parts by weight. This completes the description of the preferred embodiment of the invention. The active ingredient hamamelis water (witch hazel) performs the function of an astringent. The active ingredient epinephrine hydrochloride performs the function of a vasoconstrictor. The active ingredient menthol performs three functions of an analgesic, antipruritic, and anaesthetic. The preferred embodiment of the invention is in a lotion form which may be directly applied to the site of the haemorrhoids or other anorectal inflammation.
The following example describes the steps to be followed in manufacturing the preferred embodiment of the invention.
Purified water in an amount from 64.2907 to 78.5775 parts by weight is supplied in a stainless steel kettle equipped with a mixer and a heat exchanger attached to the kettle for heating and cooling the ingredients in the kettle.
From 0.3499 to 0.4277 parts by weight carbomer is dusted onto the water and mixed into the water.
As soon as the carbomer and water are smooth and uniform, from 4.0653 to 4.9687 parts by weight aloe powder, from 4.0000 to 4.8888 parts by weight propylene glycol, from 0.1000 to 0.1222 parts by weight methylparaben, from 0.1000 to 0.1222 parts by weight propylparaben, and from 0.1000 to 0.1222 parts by weight tetrasodium ethylenediaminetetraacetate (tetrasodium EDTA) are added and mixed into the smooth and uniform mixture while heating to a temperature of 75 °C.
Upon reaching a temperature of 75°C, from 0.7000 to 0.8555 parts by weight diethanolamine cetyl phosphate (DEA cetyl phosphate), from 1.0000 to 1.2222 parts by weight stearic acid, from 0.2500 to 0.3055 parts by weight glyceryl stearate, from 0.2500 to 0.3055 parts by weight PEG 100 stearate, and from 3.0000 to 3.6666 parts by weight C 12-15 alkyl benzoate is mixed into the 75 °C mixture.
The 75 °C mixture is then cooled to 55 °C.
A solution having a temperature of 55 °C and obtained from 2.0000 to 2.4444 parts by weight C 12-15 alkyl benzoate, from 0.0900 to 0.1100 parts by weight menthol crystals is mixed into the 55 °C mixture.
The 55°C mixture is then cooled to a temperature of no more than 45°C.
From 0.1000 to 0.1222 parts by weight jojoba oil, from
0.2000 to 0.2444 parts by weight ginseng American 1:1 propylene glycol, from 0.2000 to 0.2444 parts by weight imidazolidinyl urea, and from 0.2000 to 0.2444 parts by weight triethanolamine are then mixed into the 45 °C mixture.
From 9.0000 to 11.0000 parts by weight hamamelis water (witch hazel), from 0.0045 to 0.0055 parts epinephrine hydrochloride are then mixed into the 45 °C mixture.
This completes the description of the steps to be followed in manufacturing the preferred embodiment of the invention.
In a first alternative embodiment of the invention certain essential oils may be added to provide additional cooling and lubrication for the lotion. The first alternative embodiment of the invention comprises the formula of the preferred embodiment of the invention together with the following essential oils.
The essential oil Vanilla (from the botanical species
Vanilla planifolia) is contained in the first alternative embodiment of the lotion in an amount of from 0.5400 to 0.6600 parts by weight and, preferably, in an amount of about 0.6000 by weight .
The essential oil Hyssop (from the botanical species
Hyssopus officinalis) is contained in the first alternative embodiment of the lotion in an amount of from 0.0900 to 0.1100 parts by weight and, preferably, in an amount of about 0.1000 by weigh .
The essential oil Melissa (from the botanical species
Melissa officinalis) is contained in the first alternative embodiment of the lotion in an amount of from 0.0900 to 0.1100 parts by weight and, preferably, in an amount of about 0.1000 by weight .
The essential oil Angelica (from the botanical species
Angelica archangelia) is contained in the first alternative embodiment of the lotion in an amount of from 0.0900 to 0.1100 parts by weight and, preferably, in an amount of about 0.1000 by weight .
The essential oil Lavender (from the botanical species
Lavendula officinalis) is contained in the first alternative embodiment of the lotion in an amount of from 0.0900 to 0.1100 parts by weight and, preferably, in an amount of about 0.1000 by weight .
In this first alternative embodiment of the invention the amount of purified water is adjusted to be from 63.3906 to 77.4774 parts by weight instead of from 64.2907 to 78.5775 parts by weight in order to accommodate the added volume of the essential oils. During the manufacturing process, the essential oils are added to the lotion after the epinephrine hydrochloride is added.
This completes the description of the first alternative embodiment of the invention.
In further alternative embodiments of the invention the ingredient gingko may be added to the formulation. In these alternative embodiments of the invention gingko is contained in the lotion in an amount from 0.2000 to 0.2444 parts by weight and, preferably, in an amount of about 0.2222 parts by weight. The amount of purified water in each alternative embodiment is adjusted to compensate for the weight of the gingko. During the manufacturing process, the gingko is added to the lotion when the ginseng is added.
Adding 0 000 to 0.2444 parts by weight of gingko to the first alternative em-xxiiment of the invention will cause the amount of purified water in this second alternative embodiment of the invention to be present in an amount from 63.1908 to 772330 parts by weight and, preferably, in an amount of about 70.2119 parts by weight
Adding 02000 to 0.2444 parts by weight of gingko to the preferred embodiment of the invention will cause the amount of purified water in this third alternative embodiment of the invention to be present in an amount from 64.0908 to 78.3330 parts by weight and, preferably, in an amount of about 71.211 parts by weight.
In a fourth alternative embodiment of the invention the active ingredient epinephrine hydrochloride may be replaced by the active ingredient ephedrine sulfate. In this fourth alternative embodiment of the invention ephedrine sulfate is contained in the lotion in an amount from 0.2250 to 0.2750 parts by weight and, preferably, in an amount of about 02500 parts by weight The amount of hamamelis water is contained in the lotion in an amount from 22.5000 to 27.5000 parts by weight and, preferably, in an amount of about 25.0000 parts by weight The amount of purified water in this fourth alternative embodiment of the invention is then adjusted to be present in an amount from 50.5701 to 61.8079 parts by weight and, preferably, in an amount of about 56.1890 parts by weight The other ingredients are present in the same amounts are they are in the preferred embodiment of the invention. The following example describes the steps to be followed in manufacturing this fourth alternative embodiment of the invention.
Purified water in an amount from 63.3906 to 77.4774 parts by weight is supplied in a stainless steel kettle equipped with a mixer and a heat exchanger attached to the kettle for heating and cooling the ingredients in the kettle.
From 0.3499 to 0.4277 parts by weight carbomer is dusted onto the water and mixed into the water.
As soon as the carbomer and water are smooth and uniform, from 4.0653 to 4.9687 parts by weight aloe powder, from 4.0000 to 4.8888 parts by weight propylene glycol, from 0.1000 to 0.1222 parts by weight methylparaben, from 0.1000 to 0.1222 parts by weight propylparaben, and from 0.100O to 0.1222 parts by weight tetrasodium ethylenedinrritnetetraacetate (tetrasodium EDTA) are added and mixed into the smooth and uniform mixture while heating to a temperature of 75 ° C.
Upon reaching a temperature of 75 ° C, from 0.7000 to 0.8555 parts by weight diethanolamine cetyl phosphate (DEA cetyl phosphate), from 1.0000 to 1.2222 parts by weight stearic acid, from 0.2500 to 0-3055 parts by weight glyceryl stearate, from 02500 to 0.3055 parts by weight PEG 100 stearate, and from 3.0000 to 3.6666 parts by weight C 12-15 alkyl benzoate are mixed into the 75 ° C. mixture.
The 75 ° C. mixture is then cooled to 55 ° C.
A solution having a temperature of 55 ° C. and obtained from 2.0000 to 2.4444 parts by weight C 12-15 alkyl benzoate, from 0.0900 to 0.1100 parts by weight menthol crystals is mixed
into the 55 ° C. mixture. The 55 ° C. mixture is then cooled to a temperature of no more than 45 ° C.
From 0.1000 to 0.1222 parts by weight jojoba oil, from 02000 to 0.2444 parts by weight
ginseng American 1:1 propylene glycol, from 02000 to 02444 parts by weight imidazolidinyl urea, from 02000 to 0.2444 parts by weight triet--anolamine are then mixed into the 45 ° C. mixture.
From 9.0000 to 11.0000 parts by weight hamamelis water (witch hazel), from 0.0045 to 0.0055 parts epinephrine hydrochloride are then mixed into the 45 ° C. mixture.
From 0.5400 to 0.6600 parts by weight vanilla, from 0.0900 to 0.1100 parts hyssop, from
0.0900 to 0.1100 parts melissa, from 0.0900 to 0.1100 parts angelica, from 0.0900 to 0.1100 parts lavender, are then mixed into the 45 ° C. mixture.
This completes the description of the steps to be followed in manufacturing the fourth alternative embodiment of the invention.
A fifth alternative embodiment of the invention may be formed by adding gingko to the formulation of the fourth alternative embodiment of the invention. Adding 020OO to 02444 parts by weight of gingko, and preferably, in an amount of about 02222 parts by weight, to the fourth alternative embodiment of the invention will require the amount of purified water in mis
fifth alternative embodiment of the invention to be adjusted to be present in an amount from 63.1908 to 772330 parts by weight and, preferably, in an amount of about 702119 parts by weight During the rn-mufacturiπg process, the gingko is added to the lotion when the ginseng is A sixth alternative embodiment of the invention provides a formulation of the invention having a suitable viscosity to enable the lotion to be applied by a spray applicator directly to the site of application.
In the sixth alternative embodiment of the invention hamamelis water (witch hazel) is
contained in foe lotion in an amount from 9.0000 to 11.0000 parts by weight and, preferably, in an amount of about 10.0000 parts by weight.
Epinephrine hydrochloride is contained in the lotion in an amount from 0.0045 to 0.0055 parts by weight and, preferably, in an amount of about 0.0050 parts by weight
Menthol crystals are contained in the lotion in an amount from 0.0900 to 0.1100 parts by weight and, preferably, in an amount of about 0.1000 parts by weight
Aloe powder, such as that sold under the name Aloe Vera Phytogel 1:199, is contained in the lotion in an amount from 4.0500 to 4.9500 parts by weight and, preferably, in an amount of
about 4.5000 parts by weight
Purified water is contained in the lotion in an amount from 612405 to 74.8495 parts by weight and, preferably, in an amount of about 68.0450 parts by weight
Carbomer, also known as carboxy polymethylene, such as that sold by B. F. Goodrich under the name Carbopol 1342, is contained in the lotion in an amount from 4.5000 to 5.5000 parts by weight and, preferably, in an amount of about 5.0000 parts by weight
Propylene glycol, such as that sold by ARCO Chemical Company under the name Propylene Glycol USP, is cc*-t-rined in the lotion in an amount from 3.6000 to 4.4000 parts by
weight and, preferably, in an amount of about 4.0000 parts by weight Methylparaben, also known as methyl hydroxybenzoate, such as that sold by NTPA
Laboratories, Inc. under the name Nipa Esters methyl p-hydroxybenzoate, is contained in the lotion in an amount from 0.1800 to 02200 parts by weight and, preferably, in an amount of about
02000 parts by weight
Propylparaben, also known as propyl hydroxybenzoate, is contained in the lotion in an amount from 0.0900 to 0.1100 parts by weight and, preferably, in an amount of about 0.1000
parts by weight
Tetrasodium efoylenedia inetetraacetate (tetrasodium EDTA) is contained in the lotion
in an amount from 0.0900 to 0.1100 parts by weight and, preferably, in an amount of about
0.1000 parts by weight
Dieth-molamine cetyl phosphate (DEA cetyl phosphate), such as that sold by Givaudan Corporation under the name Amphisol, is contained in the lotion in an amount from 0.9000 to 1.1000 parts by weight and, preferably, in an amount of about 1.0000 parts by weight
Stearic acid is contained in the lotion in an amount from 0.9000 to 1.1 00 parts by weight and, preferably, in an amount of about 1.0000 parts by weight
C 12-15 alkyl benzoate, such as that sold by Finetex, Inc. under the name Finsolv TN, is contained in the lotion in an amount from 4.5000 to 5.5000 parts by weight and, preferably, in an amount of about 5.0000 parts by weight
Jojoba oil, such as that sold by LIPO Chemicals, Inc. under the name Lipovol J, is contained in the lotion in an amount from 0.0900 to 0.1100 parts by weight and, preferably, in an amount of about 0.1000 parts by weight Ginseng American 1 : 1 PB (propylene glycol) is contained in the lotion in an amount from
0.1800 to 02200 parts by weight and, preferably, in an amount of about 02000 parts by weight
Imidazolidinyl urea, such as that sold by Sutton Laboratories, Inc. under the name GERMALL 115, is contained in the lotion in an amount from 0.1350 to 0.1650 parts by weight and, preferably, in an amount of about 0.1500 parts by weight
Triethanolamine is contained in the lotion in an amount from 0.4500 to 0.5500 parts by weight and, preferably, in an amount of about 0.5000 parts by weight
This completes the description of the sixth alternative embodiment of the invention. The active ingredient hamamelis water (witch hazel) performs the function of an astringent The active ingredient epinephrine hydrochloride performs the function of a vasoconstrictor. The active ingredient menthol performs the three functions of an analgesic, antipruritic, and
anesthetic.
The following example describes the steps to be followed in manufacturing the sixth alternative embodiment of the invention.
Purified water in an amount from 61.2405 to 74.8495 parts by weight is supplied in a stainless steel kettle equipped with a mixer and a heat exchanger attached to the kettle for heating and cooling the ingredients in the kettle.
From 4.5000 to 5.5000 parts by weight carbomer is dusted onto the water and mixed into
foe water.
As soon as the carbomer and water are smooth and uniform, from 9.0000 to 11.0000 parts by weight hamamelis water (witch hazel), from 4.0500 to 4.9500 parts by weight aloe powder,
from 3.6000 to 4.4000 parts by weight propylene glycol, from 0.1800 to 0.2200 parts by weight methylparaben, from 0.0900 to 0.1100 parts by weight tetrasodium efoylenediaminetetraacetate
(tetrasodium EDTA) are added and mixed into the smooth and uniform mixture while heating to a temtxaature of 75 ° C. This solution is referred to as the "phase A" mixture.
A second mixture referred to as the "phase B" mixture is mixed as follows. From 0.9000
to 1.1000 parts by weight dieth-molamine cetyl phosphate (DEA cetyl phosphate) is mixed with from 0.9000 to 1.1000 parts by weight stearic acid. Then from 4.5000 to 5.5000 parts by weight C 12-15 alkyl benzoate, and from 0.0900 to 0.1100 parts by weight jojoba oil, and from 0.1800 to 02200 parts by weight ginseng, and from 0.0900 to 0.1100 parts by weight propylparaben are
added and mixed into the "phase B" mixture while heating to a temperature of 75 ° C.
The "phase BM mixture is then mixed into the "phase A" mixture creating a "phase C" mixture. From 0.4500 to 0.5500 parts by weight of triethanolamine is then mixed into the "phase
C" mixture. The "phase C" mixture is then mixed for about ten minutes at a temperature of
Figure imgf000016_0001
75 ° C. The "phase C" mixture is then cooled to 40 ° C.
From 0.0900 to 0.1100 parts by weight of menthol crystals is then mixed into the "phase C" mixture.
A "phase D" mixture is then created by mixing from 0.0045 to 0.0055 parts by weight epinephrine hydrochloride and from 0.1350 to 0.1650 parts by weight imidazolidinyl urea at a temperature of approximately 40 ° C. The "phase D" mixture is then mixed into the "phase C" mixture to create the final mixture. The final mixture is then cooled to approximately 25 ° C
This completes the description of the steps to be followed in manufacturing the sixth alternative embodiment of the invention. In a seventh alternative embodiment of the invention certain g«wn*H oils may be added to provide additional cooling and lubrication for the lotion. The seventh alternative embodiment of the invention comprises the formula of the sixth alternative embodiment of the invention together with the following essential oils.
The essential oil Vanilla (from the botanical species Vanilla plantfolia) is contained in the
seventh alternative embodiment of the lotion in an amount of from 0.0900 to 0.1100 parts by weight and, preferably, in an amount of about 0.1000 by weight
The essential oil Hyssop (from the botanical species Hyssopus officinalis) is contained in the seventh alternative embodiment of the lotion in an amount of from 0.0450 to 0.0550 parts by weight and, preferably, in an amount of about 0.0500 by weight
The essential oil Melissa (from the botanical species Melissa officinalis) is contained in the seventh alternative embodiment of the lotion in an amount of from 0.0450 to 0.0550 parts by weight and, preferably, in an amount of about 0.0500 by weight
The essential oil Angelica (from the botanical species Angelica archangeUa) is contained
in foe seventh alternative embodiment of the lotion in an amount of from 0.0450 to 0.0550 parts
by weight and, preferably, in an amount of about 0.0500 by weight
The essen ial oil Lavender (from the botanical species L v nώda officinalis) is contained in the seventh alternative embodiment of the lotion in an amount of from 0.0450 to 0.0550 parts by weight and, preferably, in an amount of about 0.0500 by weight
In this seventh alternative embodiment of the invention the amount of purified water is adjusted to be from 60.9705 to 74.5195 parts by weight instead of from 61 405 to 74.8495 parts by weight in order to accommodate the added volume of the essential oils. 16
The following example describes the steps to be followed in manufacturing the seventh alternative embodiment of the invention.
Purified water in an amount from 60.9705 to 74.5195 parts by weight is supplied in a stainless steel kettle equipped with a mixer and a heat exchanger attached to the kettle for heating and cooling the ingredients in the kettle.
From 4.5000 to 5.5000 parts by weight carbomer is dusted onto the water and mixed into the water.
As soon as the carbomer and water are smooth and uniform, from 9.0000 to 11.0000 parts by weight hamamelis water (witch hazel), from 4.0500 to 4.9500 parts by weight aloe powder, from 3.6000 to 4.4000 parts by weight propylene glycol, from 0.1800 to 02200 parts by weight inefoylparaben, from 0.0900 to 0.1100 parts by weight tetrasodium efoyienediaminetetraacctate (tetrasodium EDTA) are added and mixed into the smooth and uniform mixture while heating to a temperature of 75 α C. This solution is referred to as the "phase A" mixture.
A second mixture referred to as the "phase B" mixture is mixed as follows. From 0.9000 to 1.1000 parts by weight diethanolamine cetyl phosphate (DEA cetyl phosphate) is mixed with from 0.9000 to 1.1000 parts by weight stearic acid. Then from 4.5000 to 5.5000 parts by weight C 12-15 alkyl benzoate, and from 0.0900 to 0.1100 parts by weight jojoba oil, and from 0.1800 to 02200 parts by weight ginseng, and from 0.0450 to 0.0550 parts by weight hyssop, and from 0.0450 to 0.0550 parts by weight melissa, and from 0.0450 to 0.0550 parts by weight angelica, and from 0.0900 to 0.1100 parts by weight propylparaben are added and mixed into the "phase B" mixture while hraring to a temperature of 75 ° C. The "phase B" mixture is then mixed into the "phase A" mixture creating a "phase C"
mixture. From 0.4500 to 0.5500 parts by weight of triethanolamine is then mixed into the "phase C" mixture- The "phase C" mixture is then mixed for about ten minutes at a temperature of approximately 75 ° C. The "phase C" mixture is then cooled to 40 β C.
A "phase D" mixture is then created by mixing from 0.0900 to 0.1100 parts by weight of
menthol crystals and from 0.0900 to 0.1100 parts by weight vanilla and from 0.0450 to 0.0550 parts by weight lavender at a temperature of approximately 40 ° C. The "phase D" mixture of menthol and vanilla and lavender is then mixed into the "phase C" mixture to create a new "phase D" mixture consisting of the "phase C" mixture and menthol and vanilla and lavender.
A "phase E" rnixture is then created by mixing from 0.0045 to 0.0055 part3 by weight epinephrine hydrochloride and from 0.1350 to 0.1650 parts by weight imidazolidinyl urea at a temperature of approximately 40 β C. The "phase E" -mxture is then mixed into the "phase D" mixture to create the final mixture. The final mixture is then cooled to approximately 25 • C.
This completes the description of the steps to be followed in m-mufecturing the seventh
alternative embodiment of the invention.
Although foe description above contains very specific formulae for embodiments of the
invention, these should not be construed as limiting the scope of the invention but as merely providing illustrations of some of the presently preferred embodiments of this invention. Thus foe scope of the invention should be determined by the appended claims and their legal
equivalents, rather than by foe examples given.

Claims

CLAIMS :
1. A composition comprising hamamelis water, menthol and epinephrine and/or ephedrine, or pharmaceutically acceptable salts thereof, in combination with a pharmaceutically acceptable carrier.
2. The composition of claim 1 wherein the epinephrine is present as epinephrine hydrochloride and/or the ephedrine in present as ephedrine sulphate.
3. The composition of claim 1 or claim 2 comprising:
(a) from about 9.0 to 11.0 parts by weight hamamelis water; (b) from about 0.09 to 0.11 parts by weight menthol; and;
(c) from about 0.0045 to 0.0055 parts by weight epinephrine hydrochloride .
4. The composition of claim 1 or claim 2 comprising: (a) from about 22.5 to 27.5 parts by weight hamamelis water;
(b) from about 0.009 to 0.11 parts by weight menthol; and;
(c) from about 0.225 to 0.275 parts by weight ephedrine sulphate .
5. The composition of any one of the preceding claims formulated as a lotion for spray application.
6. The composition of any one of the preceding claims further comprising one or more essential oils.
7. The composition of claim 6 wherein the essential oils are vanilla oil, hyssop, melissa, angelica and/or lavender.
8. The composition of any one of the preceding claims further comprising gingko.
9. The composition of claim 8 wherein the gingko is present from about 0.01 to 0.5 parts by weight.
10. The composition of any one of the preceding claims further comprising aloe powder.
11. The composition of claim 10 wherein the aloe powder is present from about 4.0 to 5.0 parts by weight.
12. The composition of any one of claims 1 to 11 for use in a method of medical treatment.
13. Use of a composition of any one of claims 1 to 11 in the preparation of a medicament for the treatment of hemorrhoids or other anorectal inflammation.
14. A lotion comprising: from 9.0000 to 11.0000 parts by weight hamamelis water; from 0.0045 to 0.0055 parts by weight epinephrine hydrochloride; from 0.0900 to 0.1100 parts by weight menthol crystals; from 4.0653 to 4.9687 parts by weight aloe powder; from 0.3499 to 0.4277 parts by weight carbomer; from 4.0000 to 4.8888 parts by weight propylene glycol; from 0.1000 to 0.1222 parts by weight methylparaben; from 0.1000 to 0.1222 parts by weight propylparaben; from 0.1000 to 0.1222 parts by weight tetrasodium EDTA; from 0.7000 to 0.8555 parts by weight DEA cetyl phosphate; from 1.0000 to 1.2222 parts by weight stearic acid; from 0.2500 to 0.3055 parts by weight glyceryl stearate; from 0.2500 to 0.3055 parts by weight PEG 100 stearate; from 5.0000 to 6.1111 parts by weight C 12-15 alkyl benzoate; from 0.1000 to 0.1222 parts by weight jojoba oil; from 0.2000 to 0.2444 parts by weight ginseng; from 0.2000 to 0.2444 parts by weight imidazolidinyl urea; and from 0.2000 to 0.2444 parts by weight triethanolamine.
15. The lotion of claim 14 comprising: about 10.0000 parts by weight hamamelis water; about 0.0050 parts by weight epinephrine hydrochloride; about 0.1000 parts by weight menthol crystals; about 4.5170 parts by weight aloe powder; about 4.4444 parts by weight propylene glycol; about 0.1111 parts by weight methylparaben; about 0.1111 parts by weight propylparaben; about 0.1111 parts by weight tetrasodium EDTA; about 0.7777 parts by weight DEA cetyl phosphate; about 1.1111 parts by weight stearic acid; about 0.2777 parts by weight glyceryl stearate; about 0.2777 parts by weight PEG 100 stearate; about 5.5555 parts by weight C 12-15 alkyl benzoate; about 0.1111 parts by weight jojoba oil; about 0.2222 parts by weight ginseng; about 0.2222 parts by weight imidazolidinyl urea; and about 0.2222 parts by weight triethanolamine.
16. A lotion comprising: from 22.5000 to 27.5000 parts by weight hamamelis water; from 0.2250 to 02750 parts by weight ephedrine sulphate; from 0.0900 to 0.1100 parts by weight menthol crystals; from 4.0653 to 4.9687 parts by weight aloe powder; from 0.3499 to 0.4277 parts by weight carbomer; from 4.0000 to 4.8888 parts by weight propylene glycol; from 0.1000 to 0.1222 parts by weight methylparaben; from 0.1000 to 0.1222 parts by weight propylparaben; from 0.1000 to 0.1222 parts by weight tetrasodium EDTA; from 0.7000 to 0.8555 parts by weight DEA cetyl phosphate; from 1.0000 to 1.2222 parts by weight stearic acid; from 0.2500 to 0.3055 parts by weight glyceryl stearate; from 0.2500 to 0.3055 parts by weight PEG 100 stearate; from 5.0000 to 6.1111 parts by weight C 12-15 alkyl benzoate; from 0.1000 to 0.1222 parts by weight jojoba oil; from 0.2000 to 0.2444 parts by weight ginseng; from 0.2000 to 0.2444 parts by weight imidazolidinyl urea; and from 0.2000 to 0.2444 parts by weight triethanolamine.
17. The lotion of claim 16 comprising: about 25.0000 parts by weight hamamelis water; about 0.2500 parts by weight ephedrine sulphate; about 0.1000 parts by weight menthol crystals; about 4.5170 parts by weight aloe powder; about 0.3888 parts by weight carbomer; about 4.4444 parts by weight propylene glycol; about 0.1111 parts by weight methylparaben; about 0.1111 parts by weight propylparaben; about 0.1111 parts by weight tetrasodium EDTA; about 0.7777 parts by weight DEA cetyl phosphate; about 1.1111 parts by weight stearic acid; about 0.2777 parts by weight glyceryl stearate; about 0.2777 parts by weight jojoba oil; about 0.2222 parts by weight ginseng; about 0.2222 parts by weight imidazolidinyl urea; and about 0.2222 parts by weight triethanolamine.
18. The lotion of any one of claims 14 to 17 additionally comprising: about 0.6000 parts by weight vanilla; and about 0.1000 parts by weight hyssop; and about 0.1000 parts by weight melissa; and about 0.1000 parts by weight angelica; and about 0.1000 parts by weight lavender.
19. The lotion of any one of claims 14 to 18 additionally comprising about 0.2222 parts by weight gingko.
20. A lotion comprising: from 9.0000 to 11.0000 parts by weight hamamelis water; from 0.0045 to 0.0055 parts by weight epinephrine hydrochloride; from 0.0900 to 0.1100 parts by weight menthol crystals; from 4.0500 to 4.9500 parts by weight aloe powder; from 4.5000 to 5.5000 parts by weight carbomer; from 3.6000 to 4.4000 parts by weight propylene glycol; from 0.1800 to 0.2200 parts by weight methylparaben; from 0.0900 to 0.1100 parts by weight tetrasodium EDTA; from 0.9000 to 1.1000 parts by weight DEA cetyl phosphate; from 4.5000 to 5.5000 parts by weight C 12-15 alkyl benzoate; from 0.0900 to 0.1100 parts by weight jojoba oil; from 0.1800 to 0.2200 parts by weight ginseng; from 0.1350 to 0.1650 parts by weight imidazolidinyl urea; and from 0.4500 to 0.5500 parts by weight triethanolamine.
21. A lotion as claimed in claim 20 additionally comprising: from 0.0900 to 0.1100 parts by weight vanilla; and from 0.0450 to 0.0550 parts by weight hyssop; from 0.0450 to 0.0550 parts by weight melissa; and from 0.0450 to 0.0550 parts by weight angelica; and from 0.0450 to 0.0550 parts by weight lavender.
22. A lotion comprising: about 10.0000 parts by weight hamamelis water; about 0.0050 parts by weight epinephrine hydrochloride; about 0.1000 parts by weight menthol crystals; about 4.5000 parts by weight aloe powder; about 5.0000 parts by weight carbomer; about 4.0000 parts by weight propylene glycol; about 0.2000 parts by weight methylparaben; about 0.1000 parts by weight propylparaben; about 1.0000 parts by weight stearic acid; about 0.1000 parts by weight tetrasodium EDTA; about 1.0000 parts by weight DEA cetyl phosphate; about 5.0000 parts by weight C 12-15 alkyl benzoate; about 0.1000 parts by weight jojoba oil; about 0.2000 parts by weight ginseng; about 0.1500 parts by weight imidazolidinyl urea; and about 0.5000 parts by weight triethanolamine.
23. A lotion as claimed in claim 22 comprising: about 0.1000 parts by weight vanilla; and about 0.0500 parts by weight hyssop; and about 0.0500 parts by weight melissa; and about 0.0500 parts by weight angelica; and about 0.0500 parts by weight lavender.
24. A method of making a lotion comprising the steps of: heating purified water; continuously mixing from 0.3499 to 0.4277 parts by weight carbomer into the water being heated until smooth and uniform; and then adding from 4.063 to 4.9687 parts by weight aloe powder, from 4.0000 to 4.8888 parts by weight propylene glycol, from
0.1000 to 0.1222 parts by weight methylparaben, from 0.1000 to
0.1222 parts by weight propylparaben, from 0.1000 to 0.1222 parts by weight tetrasodium EDTA, into the smooth and uniform mixture while heating to a temperature of 75 ┬░C; mixing into the 75┬░C mixture from 0.7000 to 0.8555 parts by weight DEA cetyl phosphate, from 1.0000 to 1.2222 parts by weight stearic acid, from 0.2500 to 0.3055 parts by weight glyceryl stearate, from 0.2500 to 0.3055 parts by weight PEG 100 stearate, from 3.0000 to 3.6666 parts by weight C 12-15 alkyl benzoate; cooling the 75 ┬░C mixture to 55 ┬░C; mixing into the 55┬░C mixture a solution having a temperature of 55┬░C obtained from 2.0000 to 2.4444 parts by weight C 12-15 alkyl benzoate, from 0.0900 to 0.1100 parts per weight menthol crystals until smooth and uniform; cooling the
55 ┬░C mixture to no more than 45 ┬░C; mixing into the 45┬░C mixture from 0.1000 to 0.1222 parts by weight jojoba oil; from 0.2000 to 0.2444 parts by weight ginseng; from 0.2000 to 0.2444 parts by weight imidazolidinyl urea; from
0.2000 to 0.2444 parts by weight hamamelis water and from 0.0045 to 0.0055 parts by weight epinephrine hydrochloride.
25. The method of claim 24 additionally comprising the step of: adding and mixing into the 45┬░C mixture from 0.5400 to
0.6600 parts by weight vanilla, and from 0.0900 to 0.1100 parts by weight hyssop, and from 0.0900 to 0.1100 parts by weight melissa, and from 0.0900 to 0.1100 parts by weight angelica, and from 0.0900 to 0.1100 parts by weight lavender when the epinephrine hydrochloride is added.
26. The method of claim 24 or claim 25 additionally comprising the step of: adding and mixing into the 45┬░C mixture from 0.2000 to 0.2444 parts by weight gingko when the ginseng is added.
27. A method of making a lotion, comprising the steps of: heating purified water; continuously mixing from 0.3499 to 0.4277 parts by weight carbomer into the water being heated until smooth and uniform; and then adding from 4.0653 to 4.9687 parts by weight aloe powder, from 4.0000 to 4.8888 parts by weight propylene glycol, from 0.1000 to 0.1222 parts by weight methylparaben, from 0.1000 to 0.1222 parts by weight propylparaben, from 0.1000 to 0.1222 parts by weight tetrasodium EDTA, into the smooth and uniform mixture while heating to a temperature of 75 ┬░C; mixing into the 75┬░C mixture from 0.7000 to 0.8555 parts by weight DEA cetyl phosphate, from 1.0000 to 1.2222 parts by weight stearic acid, from 0.2500 to 0.3055 parts by weight glyceryl stearate, from 0.2500 to 0.3055 parts by weight PEG 100 stearate, from 3.0000 to 3.6666 parts by weight C 12-15 alkyl benzoate; cooling the 75 ┬░C mixture to 55 ┬░C; mixing into the 55 ┬░C mixture a solution having a temperature of 55┬░C obtained from 2.0000 to 2.4444 parts by weight C 12-15 alkyl benzoate, from 0.0900 to 0.1100 parts per weight menthol crystals until smooth and uniform; cooling the 55 ┬░C mixture to no more than 45 ┬░C; mixing into the 45┬░C mixture from 0.1000 to 0.1222 parts by weight jojoba oil; from 0.2000 to 0.2444 parts by weight ginseng; from 0.2000 to 0.2444 parts by weight imidazolidinyl urea; from 0.2000 to 0.2444 parts by weight triethanolamine and mixing into the 45┬░C mixture from 22.5000 to 27.5000 parts by weight hamamelis water and from 0.2250 to 0.2750 parts by weight ephedrine sulphate .
28. The method of claim 27 additionally comprising the steps of: adding and mixing into the 45 ┬░C mixture from 0.2000 to 0.2444 parts by weight gingko when the ginseng is added.
29. A method of making a lotion, comprising the steps of: heating purified water; continuously mixing from 4.5000 to 5.5000 parts by weight carbomer into the water being heated until smooth and uniform to make a first mixture; adding to said first mixture 9.0000 to 11.0000 parts by weight hamamelis water, from 4.0500 to 4.9500 parts by weight aloe powder, from 3.6000 to 4.4000 parts by weight propylene glycol, from 0.1800 to 0.2200 parts by weight methylparaben, and from 0.0900 to 0.1100 parts by weight tetrasodium EDTA into the smooth and uniform mixture while heating to a temperature of 75 ┬░C; mixing into the first mixture, a second mixture at a temperature of 75 ┬░C made from 0.9000 to 1.1000 parts by weight DEA cetyl phosphate, and from 0.9000 to 1.1000 parts by weight stearic acid, and from 4.5000 to 5.5000 parts by weight C 12-15 alkyl benzoate, and from 0.0900 to 0.1100 parts by weight jojoba oil, and from 0.1800 to 0.2200 parts by weight ginseng and from 0.0900 to 0.1100 parts by weight propylparaben; mixing into the combined first and second mixtures from 0.4500 to 0.5500 parts by weight of triethanolamine; cooling the combined first and second mixtures with triethanolamine to 40 ┬░C; mixing into the combined first and second mixtures with triethanolamine from 0.0900 to 0.1100 parts by weight of menthol crystals; mixing into the combined first and second mixtures with triethanolamine and menthol crystals a third mixture made from 0.0045 to 0.0055 parts by weight epinephrine hydrochloride and from 0.1350 to 0.1650 parts by weight imidazolidinyl urea at a temperature of approximately 40 ┬░C to make a final mixture; and cooling the final mixture to a temperature of approximately 25┬░C.
30. A method of making a lotion, .comprising the steps of: heating purified water and continuously mixing from 4.5000 to 5.5000 parts by weight carbomer into the water being heated until smooth and uniform to make a first mixture; adding to said first mixture from 9.0000 to 11.0000 parts by weight hamamelis water (witch hazel), from 4.0500 to 4.9500 parts by weight aloe powder, from 3.6000 to 4.4000 parts by weight propylene glycol, from 0.1800 to 0.2200 parts by weight methylparaben, and from 0.0900 to 0.1100 parts by weight tetrasodium EDTA into the smooth and uniform mixture while heating to a temperature of 75┬░; mixing into the first mixture a second mixture at a temperature of 75┬░C made from 0.9000 to 1.1000 parts by weight DEA cetyl phosphate, and from 0.9000 to 1.1000 parts by weight stearic acid, and from 4.5000 to 5.5000 parts by weight C 12-15 alkyl benzoate, and from 0.0900 to 0.1100 parts by weight jojoba oil, and from 0.1800 to 0.2200 parts by weight ginseng, and from 0.0450 to 0.0550 parts by weight hyssop, and from 0.0450 to 0.0550 parts by weight melissa, and from 0.0450 to 0.0550 parts by weight angelica, and from 0.0900 to 0.1100 parts by weight propylparaben; mixing into the combined first and second mixtures from 0.4500 to 0.5500 parts by weight of triethanolamine; cooling the combined first and second mixtures with triethanolamine to 40┬░C; mixing into the combined first and second mixtures with triethanolamine a third mixture made from 0.0900 to 0.1100 parts by weight of menthol crystals and from 0.0900 to 0.1100 parts by weight vanilla and from 0.0450 to 0.0550 parts by weight lavender at a temperature of approximately 40┬░C; mixing into the combined first and second and third mixtures with triethanolamine a fourth mixture made from 0.0045 to 0.0055 parts by weight epinephrine hydrochloride and from 0.1350 to 0.1650 parts by weight imidazolidinyl urea at a temperature of approximately 40 ┬░C to make a final mixture; and cooling the final mixture to a temperature of approximately 25┬░C.
PCT/GB1997/000338 1997-02-05 1997-02-05 Composition for the treatment of haemorrhoids and other anorectal inflammations WO1998034628A1 (en)

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