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NZ768459B2 - Topical composition - Google Patents
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NZ768459B2 - Topical composition - Google Patents

Topical composition Download PDF

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Publication number
NZ768459B2
NZ768459B2 NZ768459A NZ76845919A NZ768459B2 NZ 768459 B2 NZ768459 B2 NZ 768459B2 NZ 768459 A NZ768459 A NZ 768459A NZ 76845919 A NZ76845919 A NZ 76845919A NZ 768459 B2 NZ768459 B2 NZ 768459B2
Authority
NZ
New Zealand
Prior art keywords
composition
discontinuous
phase
composition according
polyaphron dispersion
Prior art date
Application number
NZ768459A
Other versions
NZ768459A (en
Inventor
Nigel Crutchley
Michelle Georgiou
Stephen Lenon
Morten Praestegaard
Original Assignee
Therapeutics Limited
Filing date
Publication date
Priority claimed from EP18162664.9A external-priority patent/EP3542788A1/en
Application filed by Therapeutics Limited filed Critical Therapeutics Limited
Publication of NZ768459A publication Critical patent/NZ768459A/en
Publication of NZ768459B2 publication Critical patent/NZ768459B2/en

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • 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
    • A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/047—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates having two or more hydroxy groups, e.g. sorbitol
    • 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
    • A61K31/075—Ethers or acetals
    • A61K31/085—Ethers or acetals having an ether linkage to aromatic ring nuclear carbon
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • A61K31/353—3,4-Dihydrobenzopyrans, e.g. chroman, catechin
    • A61K31/355—Tocopherols, e.g. vitamin E
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
    • 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
    • A61K31/59—Compounds containing 9, 10- seco- cyclopenta[a]hydrophenanthrene ring systems
    • A61K31/593—9,10-Secocholestane derivatives, e.g. cholecalciferol, i.e. vitamin D3
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics

Abstract

The present invention relates to a composition for topical application comprising a polyaphron dispersion, the polyaphron dispersion comprising a continuous aqueous phase and at least one discontinuous oil phase, wherein the polyaphron dispersion comprises calcipotriol, betamethasone dipropionate, alpha-tocopherol and butylated hydroxyanisole, and wherein the composition has a pH of 7.75 ± 0.5.

Claims (19)

Claims:
1. A composition for topical application comprising a polyaphron dispersion, the polyaphron dispersion comprising a continuous aqueous phase and at least one 5 discontinuous oil phase, wherein the polyaphron dispersion comprises calcipotriol, betamethasone dipropionate, alpha-tocopherol and butylated hydroxyanisole, and wherein the composition has a pH of 7.75 ± 0.5. 10 2. The composition according to claim 1, wherein the composition has a pH of
2. 75 ± 0.25.
3. The composition according to claim 1 wherein the composition comprises, by weight of the composition: 15 from 0.001 to 0.01 wt% calcipotriol; and/or from 0.02 to 0.1 wt% betamethasone; and/or from 0.001 to 0.005 wt% alpha-tocopherol; and/or from 0.05 to 0.5 wt% butylated hydroxyanisole. 20
4. The composition according to any one of the preceding claims wherein: the calcipotriol is predominantly in at least one of said discontinuous oil phase(s); and/or the betamethasone dipropionate is predominantly in at least one of said discontinuous oil phase(s); and/or 25 the alpha-tocopherol is predominantly in at least one of said discontinuous oil phase(s); and/or the butylated hydroxyanisole is predominantly in at least one of said discontinuous oil phase(s). 30
5. The composition according to any one of the preceding claims, wherein at least one of said discontinuous oil phase(s) comprises medium chain triglycerides and isopropyl myristate, wherein the isopropyl myristate and medium chain triglycerides are present in a weight ratio of from 3:1 to 12:1. 35
6. The composition according to any one of the preceding claims, wherein the polyaphron dispersion further comprises a discontinuous phase comprising a non- solvent oil.
7. The composition according to claim 6, wherein the non-solvent oil is mineral oil. 20841034_1 (GHMatters) P114486.NZ
8. The composition according to any one of the preceding claims, wherein said discontinuous oil phase(s) comprises a first discontinuous phase, a second discontinuous phase and, optionally a third discontinuous phase comprising mineral oil, 5 wherein the calcipotriol is predominantly in the first discontinuous phase, wherein the betamethasone dipropionate is predominantly in the second discontinuous phase, and wherein the alpha-tocopherol and the butylated hydroxyanisole are predominantly in the first discontinuous phase, or predominantly in the first and second 10 discontinuous phases collectively.
9. The composition according to claim 8, wherein the first discontinuous phase and the second discontinuous phase each comprise the same pharmaceutically acceptable oil, 15 wherein the pharmaceutically acceptable oil is a blend of caprilic capric triglycerides (CCT) and isopropyl myristate, and wherein the isopropyl myristate and caprilic capric triglycerides are present in a weight ratio of from 3:1 to 12:1. 20
10. The composition according to any one of the preceding claims, wherein the continuous aqueous phase comprises at least 4 wt% isopropanol by weight of the composition.
11. The composition according to any one of the preceding claims, wherein the 25 composition is chemically stable for at least 6 months at 25 ºC ± 2 ºC, as measured at 60% RH ± 5%; and/or wherein the composition is chemically stable for at least 12 months at 5 ºC ± 3 ºC, as measured at 60% RH ± 5%. 30
12. A composition for topical application comprising a polyaphron dispersion, the polyaphron dispersion comprising a continuous aqueous phase and at least one discontinuous oil phase, wherein the polyaphron dispersion comprises calcipotriol, betamethasone dipropionate, alpha-tocopherol and butylated hydroxyanisole, 35 wherein at least one of said discontinuous oil phase(s) comprises medium chain triglycerides and isopropyl myristate, and wherein the isopropyl myristate and medium chain triglycerides are present in a weight ratio of from 3:1 to 12:1. 20841034_1 (GHMatters) P114486.NZ
13. A composition for topical application comprising a polyaphron dispersion, wherein the polyaphron dispersion comprises: (i) calcipotriol; 5 (ii) betamethasone or an ester thereof; (iii) alpha-tocopherol; and (iv) butylated hydroxyanisole.
14. A method of treatment of a non-human animal body by therapy, the method 10 comprising administering to the non-human animal body the composition according to any one of the preceding claims.
15. Use of the composition according to any one of claims 1 to 13 in the manufacture of a medicament for the treatment of psoriasis in a human subject.
16. A method of manufacturing a composition for topical application, the method comprising: (a) preparing a first polyaphron dispersion comprising calcipotriol, alpha- tocopherol and butylated hydroxyanisole; 20 (b) preparing a second polyaphron dispersion comprising betamethasone dipropionate and preferably further comprising alpha-tocopherol and butylated hydroxyanisole; and mixing together the first and second polyaphron dispersions to form the composition.
17. A method according to claim 16 further comprising: preparing a third polyaphron dispersion comprising a non-solvent oil, preferably wherein the non-solvent oil is mineral oil; and mixing the third polyaphron dispersion with the first and second polyaphron 30 dispersions to form the composition.
18. Use of a combination of alpha-tocopherol and butylated hydroxyanisole in a composition for topical application to stabilise: (iii) calcipotriol; and/or 35 (iv) betamethasone dipropionate.
19. A composition according to any one of claims 1 to 13, substantially as herein described, with reference to any one of the Examples and/or
NZ768459A 2019-03-18 Topical composition NZ768459B2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP18162664.9A EP3542788A1 (en) 2018-03-19 2018-03-19 Topical composition comprising calcipotriol and betamethasone dipropionate
PCT/EP2019/056735 WO2019179958A1 (en) 2018-03-19 2019-03-18 Topical composition

Publications (2)

Publication Number Publication Date
NZ768459A NZ768459A (en) 2024-08-30
NZ768459B2 true NZ768459B2 (en) 2024-12-03

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