CA2484184C - Minoxidil foam formulation - Google Patents

Minoxidil foam formulation Download PDF

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Publication number
CA2484184C
CA2484184C CA2484184A CA2484184A CA2484184C CA 2484184 C CA2484184 C CA 2484184C CA 2484184 A CA2484184 A CA 2484184A CA 2484184 A CA2484184 A CA 2484184A CA 2484184 C CA2484184 C CA 2484184C
Authority
CA
Canada
Prior art keywords
composition
minoxidil
surfactant
nozzle
water
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
CA2484184A
Other languages
French (fr)
Other versions
CA2484184A1 (en
Inventor
Stephen Tickle
Elizabeth Joan Jacques
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
NUPHARM LABORATORIES Ltd
Original Assignee
NUPHARM LABORATORIES Ltd
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 NUPHARM LABORATORIES Ltd filed Critical NUPHARM LABORATORIES Ltd
Publication of CA2484184A1 publication Critical patent/CA2484184A1/en
Application granted granted Critical
Publication of CA2484184C publication Critical patent/CA2484184C/en
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/02Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/04Dispersions; Emulsions
    • A61K8/046Aerosols; Foams
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34Alcohols
    • A61K8/342Alcohols having more than seven atoms in an unbroken chain
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/37Esters of carboxylic acids
    • A61K8/375Esters of carboxylic acids the alcohol moiety containing more than one hydroxy group
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/39Derivatives containing from 2 to 10 oxyalkylene groups
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/40Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/44Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
    • A61K8/442Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof substituted by amido group(s)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/494Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom
    • A61K8/4953Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom containing pyrimidine ring derivatives, e.g. minoxidil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/4993Derivatives containing from 2 to 10 oxyalkylene groups
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/84Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions otherwise than those involving only carbon-carbon unsaturated bonds
    • A61K8/86Polyethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/92Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
    • A61K8/922Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • A61K9/12Aerosols; Foams
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q7/00Preparations for affecting hair growth

Abstract

A pharmaceutical dosage form comprises an active ingredient selected from the group consisting of:- minoxidil, minoxidil sulphate, other soluble minoxidil salts and mixtures thereof; a surfactant; water; and optional further excipients; the formulation being adapted to form a foam when administered by spraying.

Description

MINOXIDIL FOAM FORMULATION
This invention relates to a formulation of the pharmaceutical substance minoxidil.
Minoxidil is used for treatment of hereditary hair loss. Previously known formulations comprise a lotion applied using a dropper or by a roller. Minoxidil is sparingly soluble in water and current products comprise propylene glycol, ethanol and water. Such formulations are awkward to administer and thorough coverage of the area to be treated can be difficult.
According to a first aspect of the present invention a pharmaceutical dosage form comprises an active ingredient selected from the group consisting of:-minoxidil, minoxidil sulphate, other soluble minoxidil salts and mixtures thereof;
a surfactant;
water; and optional further excipients;
the formulation being adapted to form a foam when administered by spraying.
Percentages and amounts referred to in the specification are by weight unless stated otherwise. Percentages are selected to total 100%
Dosage forms in accordance with this invention confer several advantages. The absence of ethanol and aerosol prapellents reduces the risk of flammability. Ethanol can be an irritant to a user's skin. The absence of halocarbon aerosol propellents is beneficial to the environment.
Preferably the amount of active ingredient is about 2-5%
Preferably the amount of surfactant is about 2-10% Any combination of anionic, cationic, non-ionic or amphoteric surfactants and non-ionic block copolymers may be used.
Preferably ethoxylated glycerides, ethoxylated sorbitan esters, polyethoxylated and hydrogenated caster oil, nonionic block copolymers and amphoterics may be used.
Especially preferred surfactants may be selected from:-PEG 40 hydrogenated caster oil Polysorbate 20 Cocamidopropyl betaine Glyceryl cocoate PEG 6 caprylic/capric glycerides Poloxamer F 68 Preferred formulations in which the active is minoxidil base include' propylene glycol. An amount of about 50 - 80% is preferred. Propylene glycol is nonessential when the active minoxidil sulphate or other salt.
Preferred formulations include about 20-30% water.
Formulations in accordance with this invention produce a quick breaking foam when sprayed through a fine mesh or nozzle. This allows the foam to be rubbed in easily. The concentration of the active is selected to allow the dose to be administered in a volume of about 0.2-1.0, preferably 0.3-0.6, more preferably about 0.45cm3 of the formulation solution.
Preferred formulations include buffers, pH stabilisers, emollients, skin conditioning agents and other excipients known to those skilled in the art.
According to the second aspect of the second invention, there is provided a spray apparatus comprising a reservoir, metered dose valve and a dosage form in accordance with the first aspect of the present invention.
The invention is further described by means of example, but not in any limitative sense.
Example 1 A formulation containing minoxidil base was prepared using the following ingredients:
w/v Minoxidil 2.0 Propylene Glycol 70.0 Preservative qs Cocamidopropyl betaine 4.0 as 50% solution Water to 100m1 Example 2 A formulation containing minoxidil sulphate was prepared using the following ingredients:
%w/v 1 S Minoxidil sulphate 2.766 equal to 2.0% as base Preservative qs Cocamidopropyl betaine 2.0 as 50% solution Water to 100rn1 Example 3 Test Method For Evaluation of Foam Quality Equipment ~ Analytical top pan balance - five place with top opening.
Clean 20m1 syringe.
Clamp and clamp stand.
~ 2 clean beakers - one of which must be at least 150m1 volume.
~ Stopwatch.
Method 1. Position the clamp stand adjacent to the balance.
2. Open the balance top and position the syringe in the clamp directly over the balance S pan.
3. Place a clean empty beaker on the balance pan and either tare the beaker, or record the weight.
4. Take the clean ISOmI beaker and pump at least 100m1 of foam into it.
S. Immediately draw up the foam into the syringe, remove the plunger so that the barrel is full.
6. Immediately place the syringe I the clamp over the tared beaker.
7. Start the stop watch and record the foaxnlsolution that drips from the syringe every minute for a minimum of five minutes.
The weights were plotted against time to give a comparison of foam qualities.
The lower the solution weights were indicative of firmer foams.
The foam quality Was evaluated gravimetrically and it was found that the cocamidopropyl betaine, polysorbate 20 and glyceryl cocoate produced firmer longer lasting foams. The PEG 6 caprylic/capric glycerides, poloxamer F68 and PEG 40 hydrogenated castor oil produced quick breaking foams.
The results are shown in Figure 1.
The product was found to be comparable with the current market products.

Claims (8)

1. A foamable composition comprising:
- 2-5% minoxidil base;

- 2-10% surfactant;

- 50-80% propylene glycol; and -water;

wherein said composition is free of ethanol and aerosol propellant.
2. The composition of claim 1 wherein said surfactant comprises an anionic, cationic, non-ionic or amphoteric surfactant or a non ionic block copolymer, or a mixture thereof.
3. The composition of claim 1 wherein said surfactant comprises an ethoxylated glyceride, an ethoxylated sorbitan ester, a polyethoxylated or hydrogenated castor oil, PEG hydrogenated caster oil, Polysorbate 20, cocamidopropyl betaine, glyceryl cocoate, a PEG 6 caprylic/capric glyceride or poloxamer F68, or a mixture thereof.
4. The composition of any one of claims 1-3 further comprising one or more of a buffer, a pH stabilizer, an emollient, or a skin conditioning agent.
5. The composition of any one of claims 1-4 comprising 20-30% of said water.
6. A device for preparing a minoxidil-containing foam, comprising a reservoir, a metered dose valve, and a nozzle, wherein said reservoir contains the composition of any one of claims 1-5.
7. The device of claim 6 wherein said nozzle comprises a mesh.
8. A method of preparing a minoxidil-containing foam, comprising providing the composition of any one of claims 1-5, and spraying said composition through a mesh or nozzle.
CA2484184A 2003-10-11 2004-10-07 Minoxidil foam formulation Expired - Fee Related CA2484184C (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB0323908.4 2003-10-11
GBGB0323908.4A GB0323908D0 (en) 2003-10-11 2003-10-11 Pharmaceutical foam formulation

Publications (2)

Publication Number Publication Date
CA2484184A1 CA2484184A1 (en) 2005-04-11
CA2484184C true CA2484184C (en) 2012-01-03

Family

ID=29433776

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2484184A Expired - Fee Related CA2484184C (en) 2003-10-11 2004-10-07 Minoxidil foam formulation

Country Status (3)

Country Link
US (1) US20050079139A1 (en)
CA (1) CA2484184C (en)
GB (2) GB0323908D0 (en)

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Also Published As

Publication number Publication date
GB0323908D0 (en) 2003-11-12
GB2406791B (en) 2008-02-06
US20050079139A1 (en) 2005-04-14
GB2406791A (en) 2005-04-13
CA2484184A1 (en) 2005-04-11
GB0421825D0 (en) 2004-11-03

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