Classifications

• • 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
  • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
  • A61K9/7015—Drug-containing film-forming compositions, e.g. spray-on
• • 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
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/13—Amines
  • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
  • A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
• • 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
  • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
  • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
  • A61K8/81—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions involving only carbon-to-carbon unsaturated bonds
  • A61K8/8141—Compositions of homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and at least one being terminated by only one carboxyl radical, or of salts, anhydrides, esters, amides, imides or nitriles thereof; Compositions of derivatives of such polymers
  • A61K8/8152—Homopolymers or copolymers of esters, e.g. (meth)acrylic acid esters; Compositions of derivatives of such polymers
• • 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
  • A61K9/12—Aerosols; Foams
• • 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
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P35/00—Antineoplastic agents
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q19/00—Preparations for care of the skin
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
  • A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
  • A61K2800/59—Mixtures
  • A61K2800/594—Mixtures of polymers
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
  • A61K2800/80—Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
  • A61K2800/95—Involves in-situ formation or cross-linking of polymers

Definitions

• the Eudragit RS type contains, for example, 30% by weight of Eudragit RS100, Eudragit RSPO, and Eudragit RS30D (ethyl acrylate, methyl methacrylate, trimethylammonium chloride ethyl methacrylate copolymer (composition ratio 1: 2: 0.1)). It is available as an aqueous suspension).
• the Eudragit RL type is an acrylic acid-based polymer having a composition ratio of constituents of 1: 2: 0.2. It has an average molecular weight (Mw) of about 32,000 and is insoluble in water regardless of pH.
• a preferred embodiment of the present invention is a composition that is substantially free of lower monohydric alcohols.
• Substantially free means that the lower monohydric alcohol is not intentionally added in the manufacturing process. That is, the content of the lower monohydric alcohol in the composition substantially free of the lower monohydric alcohol is usually 0% by weight, and even if it may be mixed in a very small amount, the content is less than 1% by weight ( More preferably less than 0.5% by weight).
• Fatty acid esters that are liquid at room temperature selected from diethyl sebacate, diisopropyl sebacate, diisopropyl adipic acid and medium-chain fatty acid triglycerides, are more preferred, among which diethyl sebacate and diisopropyl adipate are more preferred, and diisopropyl adipate is particularly preferred. preferable.
• the content of the plasticizer with respect to the total amount of the composition of the present invention is preferably 1.3 to 35% by weight, more preferably 1.5 to 20% by weight, and 2 to 2 to 20% by weight. 8% by weight is particularly preferable. If the amount of the plasticizer is less than 1.3% by weight, the film forming property and water resistance are lowered, and if it is more than 35% by weight, the film becomes sticky, which is not preferable.
• the composition of the present invention can contain one or more substances selected from, for example, light anhydrous silicic acid, titanium oxide, talc, and calcium carbonate in order to suppress the shine of the film.
• the content of these substances with respect to the total amount of the composition of the present invention is preferably 0.8 to 3% by weight, particularly preferably 1 to 3% by weight.
• Hemangiomas tufted angioma, hemangioendothelioma (ie, Kaposi-like hemangioendothelioma), hemangiomas in von Hippel-Lindau syndrome, fibrohemangiomas and hemangiolipomas in Brutaviel's disease, purulent granuloma, blood vessels It can be used to treat hemangiomas selected from the group including, but not limited to, hemangiomas such as Kaposi hemangiomas, proliferative arteriovenous malformations, and tumor-related hemangiomas. When the composition of the present invention is used for the treatment of hemangiomas, it is preferable to use it during the proliferative phase.
• the composition according to the present invention not only has high water resistance but also has excellent detergency, the film should be promptly removed from the skin when side effects occur due to the medicinal components contained in the film. Allows the use of medicinal ingredients to be discontinued. Therefore, the composition of the present invention is particularly suitable as a therapeutic agent for diseases of infants who are required to have high safety.
• composition of the present invention may contain other components other than the above-mentioned polymers, medicinal ingredients, plasticizers, surfactants, light anhydrous silicic acid, titanium oxide, talc, calcium carbonate, pH adjusters, additives, and water.
• the total content of other components with respect to the total amount of the composition of the present invention is preferably 5% by weight or less in total, more preferably 3% by weight or less, and 1% by weight. % Or less is particularly preferable.
• each polymer and purified water were weighed, a plasticizer and optionally a surfactant / thickener / medicinal ingredient were added and stirred until uniform.
• the composition of each formulation example (formulation examples 1 to 12) is as shown in Tables 2, 4 and 5 (values of each component in the table indicate weight%).
• the content of the polymer shown in the table is the content of the polymer solid content
• the content of the purified water shown in the table is in the aqueous suspension when the aqueous suspension (aqueous dispersion) of the polymer is used. It is the total amount of water contained and purified water added.
• the pharmaceutical product examples 2 to 4 in which the polymers (a1) and (a2) are mixed have a shorter washing time and remain behind. The result was less. Further, when the pharmaceutical examples 2 to 4 were compared, the amount of the residual residue was less when the surfactant (HCO-60) was added. In particular, in the pharmaceutical product example 4 in which the concentration of the surfactant is high, 11 out of 14 panelists evaluated that there was no residue (score 4). Regarding visibility, it was confirmed that the visibility was enhanced depending on the concentration of the surfactant.
• composition of each pharmaceutical example and the evaluation by each panelist are shown in the table below.

Landscapes

• Health & Medical Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Epidemiology (AREA)
• Dermatology (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Engineering & Computer Science (AREA)
• Inorganic Chemistry (AREA)
• Chemical Kinetics & Catalysis (AREA)
• General Chemical & Material Sciences (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Organic Chemistry (AREA)
• Dispersion Chemistry (AREA)
• Birds (AREA)
• Medicinal Preparation (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Priority Applications (7)

Applications Claiming Priority (1)

Publications (1)

Family

ID=80117454

Family Applications (2)

Family Applications After (1)

Country Status (6)

Cited By (2)

Citations (7)

Family Cites Families (7)

• 2020
  • 2020-08-05 WO PCT/JP2020/030050 patent/WO2022029938A1/ja not_active Ceased
• 2021
  • 2021-08-04 KR KR1020227044213A patent/KR20230047960A/ko active Pending
  • 2021-08-04 EP EP21852270.4A patent/EP4194018A4/en not_active Withdrawn
  • 2021-08-04 JP JP2022541589A patent/JP7802670B2/ja active Active
  • 2021-08-04 WO PCT/JP2021/028942 patent/WO2022030540A1/ja not_active Ceased
  • 2021-08-04 CN CN202180046716.3A patent/CN115916273A/zh active Pending
  • 2021-08-04 US US18/040,399 patent/US20230277476A1/en not_active Abandoned

Patent Citations (7)

Non-Patent Citations (1)

Also Published As

Similar Documents

Legal Events