WO2007026645A1 - 植物精油成分を有効成分とするダイエット用組成物、その組成物を含むダイエット用シート状組成物及び経皮吸収型ダイエット用医薬製剤、並びにこれらの製造方法 - Google Patents
植物精油成分を有効成分とするダイエット用組成物、その組成物を含むダイエット用シート状組成物及び経皮吸収型ダイエット用医薬製剤、並びにこれらの製造方法 Download PDFInfo
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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)
- A61K36/63—Oleaceae (Olive family), e.g. jasmine, lilac or ash tree
-
- 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)
- A61K36/61—Myrtaceae (Myrtle family), e.g. teatree or eucalyptus
-
- 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)
- A61K36/73—Rosaceae (Rose family), e.g. strawberry, chokeberry, blackberry, pear or firethorn
- A61K36/738—Rosa (rose)
-
- 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)
- A61K36/75—Rutaceae (Rue family)
- A61K36/752—Citrus, e.g. lime, orange or lemon
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- 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
- A61K47/02—Inorganic compounds
-
- 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
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- 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
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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- 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
- A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
Definitions
- Dietary composition comprising a plant essential oil component as an active ingredient, dietary sheet-like composition containing the composition, pharmaceutical preparation for percutaneous absorption type diet, and methods for producing them
- the present invention relates to a composition having a diet effect comprising an essential oil component obtained from plants as an active ingredient, a sheet-like composition for diet containing the composition, a pharmaceutical preparation for percutaneous absorption type diet, and these It relates to the manufacturing method.
- NASH National Cholesterol Education Program
- BMI Body Mass Index
- Table 2 shows lifestyle-related diseases that are easily associated with obesity, such as diabetes, hypertension, hyperlipidemia, gout, arteriosclerosis.
- Orthopedic diseases osteoarthritis, lumbar spondylosis
- Obesity is mainly due to upper body obesity (also called male-type obesity, abdominal obesity, or apple-type obesity), with fat mainly on the abdomen due to the distribution of accumulation of body fat. It was categorized into lower body obesity (called female type obesity or pear type obesity), and it became clear that upper body obesity has a higher risk of complications of lifestyle-related diseases.
- upper body obesity also called male-type obesity, abdominal obesity, or apple-type obesity
- lower body obesity called female type obesity or pear type obesity
- upper body obesity and lower body obesity is based on the waist circumference because it has a strong correlation with the complications associated with obesity, and is determined to be upper body obesity when the male is 85 cm or larger and the female is 90 cm or larger.
- the fat accumulated in the upper body is divided into visceral fat accumulation type obesity (visceral fat obesity) and subcutaneous fat accumulation type obesity (subcutaneous fat obesity) in which fat accumulates under the abdominal wall, depending on the accumulated site. Divided.
- a visceral fat type obesity is determined when the visceral fat area is 100 cm 2 or more.
- BMI is 25 or more, and the disease shown in Table 2 above is already combined, or 2) Upper body obesity is suspected, and abdominal CT scan In cases where visceral fat obesity was confirmed in Japan, any case that falls under any of these cases was regarded as “obesity” requiring medical treatment. Other than this, it is simply “obesity”.
- Non-Patent Document 1 hereinafter referred to as Conventional Example 1.
- Non-Patent Document 1 Obesity Text page 147 September 1, 2004, 2nd edition issued
- the present invention provides an essential oil adsorbent coated with neroli oil to give an essential oil-coated resin, and carbon-coated particles (NR) coated with the essential oil desorption regulator, jasmine oil, and essential oil adsorbed.
- a composition for diet containing carbon coated particles (CFS) in which the above-mentioned essential oil-coated coffin is coated with an essential oil desorption control material, and a skin-absorbing pharmaceutical preparation comprising these as active ingredients is there. Since this percutaneously absorbable diet pharmaceutical preparation contains a plant-derived essential oil as an active ingredient, the above-described side effects that are problematic in the conventional diet pharmaceutical preparations described above may not occur. There is no dependency problem.
- the composition comprises an essential oil-coated coffin by coating a hydrophilic coffin with the neroli oil
- the essential oil adsorbent is coated with carbon-coated particles (NR) obtained by coating the essential oil-coated resin with carbon fine powder, and jasmine oil to form an essential oil-coated resin, and the essential oil-coated resin is coated with an essential oil desorption regulator.
- carbon-coated particles (CFS) it may contain carbon-coated particles (LV) that are coated with an essential oil adsorbent with lavender oil to form an essential oil-coated resin, and the essential oil-coated resin is coated with an essential oil desorption regulator.
- the diet effect is much higher than when the essential oil is used alone.
- a carbon-coated particle in which an essential oil adsorbent is further coated with rose oil to form an essential oil-coated coffin, and the essential oil-coated coffin is coated with an essential oil desorption regulator. It is preferable to include a core (RO) and carbon-coated particles (LM) in which an essential oil adsorbent is coated with lemon oil to form an essential oil-coated resin, and the essential oil-coated resin is coated with an essential oil desorption regulator.
- a composition combining these carbon-coated particles provides a much higher diet effect than when the essential oil is used alone.
- the diet composition of the present invention includes cineoleic eucalyptus.
- the amount of neroli oil used in the production of the carbon-coated particles (NR) is the total amount of essential oil used in the production of the composition. 9 to 21% by weight, and the amount of jasmine oil used in the production of the carbon-coated particles (CFS) is 9 to 15% by weight of the total amount of essential oil used in the production of the composition.
- the amount of lavender oil used in the production of the carbon-coated particles (LV) is 65 to 75% by weight of the total amount of essential oil used in the production of the composition
- the carbon-coated particles ( NR) The amount of neroli oil used in the production is 15.5 to 20.5 wt% of the total essential oil used in the production of the composition, the amount of jasmine oil used in the production of the carbon-coated particles (CFS). Is preferably 9.5 to 14.5% by weight of the total amount of essential oil used in the production of the composition.
- the amount of neroli oil is 10-12% by weight of the total amount of essential oil used in the production of the composition
- the amount of lemon oil used in the production of the carbon-coated particles (LM) is 24.% of the total amount of essential oil used in the production of the composition.
- Rose oil used in the production of carbon-coated particles (RO), 5 to 27% by weight Is preferably 13.5 to 17% by weight of the total amount of essential oil used in the production of the composition.
- the sheet-like composition for diet of the present invention includes (a) a combination of the above-described essential oil-coated particles, (b) an essential oil desorption regulator, (c) a free water removing agent, and (d) a heat generating agent. And a sheet-forming base containing a heat conduction inhibitor and an absorption accelerator.
- a sheet-form composition for a pharmaceutical preparation for skin-absorbing diet in which an active ingredient is uniformly distributed can be obtained, and the composition is cut into a desired size.
- a composition containing an active ingredient in an amount corresponding to the physical condition of the patient can be easily produced.
- the essential oil adsorbent is a polybulal alcohol-based hydrophilic resin having a saponification value of 98.0 to 98.5.
- a water-absorbing resin is preferred.
- the acrylic polymer water-absorbing resin preferably has a water absorption capacity in the range of 400 to 800 times the dry resin volume.
- the essential oil desorption regulator is a porous carbon material having a surface area of 200 to 800 m 2 Zg.
- the exothermic agent that is preferably present is preferably artificial zeolite having a pore diameter of 0.1 to 0.8 nm.
- the heat conduction inhibitor is preferably a polysaccharide composite.
- the absorption promoter is preferably a monoterpene compound, and the monoterpene compound is preferably L-menthol or limonene.
- the sheet forming base is preferably a thermoplastic resin having a can value of about 88.0, such as PVA.
- the present invention also provides a combination of the above-described essential oil-coated particles, an essential oil desorption regulator, a free water removing agent, a heat generating agent, a heat conduction inhibitor, an absorption accelerator, and a sheet forming base. And a sheet-like composition for diet comprising a pressure-bonding sheet.
- the base for sheet formation including the essential oil desorption regulator, the free moisture removing agent, the heat generating agent, the heat conduction preventing agent, and the absorption accelerator is as described above.
- the pressure-bonding sheet is preferably made of synthetic fiber paper having a basis weight of about 18 to about 20 g.
- the present invention also includes (1) carbon-coated particles (NR) in which an essential oil adsorbent is coated with neroli oil to form an essential oil-coated resin, and the essential oil-coated resin is coated with an essential oil desorption regulator.
- Carbon oil coated particles (CFS) in which the essential oil adsorbent is coated with the essential oil adsorbent with jasmine oil to form the essential oil-coated resin, and the essential oil-coated resin is coated with the essential oil desorption regulator, and (3) the essential oil adsorbed with the lavender oil A diet plaster comprising carbon oil-coated particles (LV) coated with an essential oil-coated resin and coated with an essential oil desorption regulator.
- a safe and highly effective diet plaster can be produced by combining these essential oil-coated particles.
- the diet plaster of the present invention is (4) coated with an essential oil adsorbent with mouth oil to obtain an essential oil-coated greaves.
- the plaster for diet of the present invention instead of the above-mentioned combination of essential oil-coated particles, is (1) an essential oil-adsorbing material coated with a refined oil, and an essential oil-coated resin. Cover the essential oil adsorbent with carbon-coated particles (NR) coated with essential oil desorption preparation material and (2) jasmine oil.
- NR carbon-coated particles
- Carbon oil-coated particles (JS) obtained by coating the essential oil-coated resin with the essential oil desorption control material, and (3) any one selected from the group consisting of cineoleic eucalyptus oil, mugwort oil and sage oil
- the essential oil adsorbent is coated to make an essential oil-coated resin, the carbon-coated particles (CE) coated with the essential oil-coated resin with the essential oil desorption control material, and (4) the essential oil adsorbent is coated with rose oil.
- Carbon oil-coated particles (RO) coated with the essential oil desorption control material, and (5) lemon oil, and the essential oil adsorbent is coated with the essential oil-coated fat. It includes carbon-coated particles (LM) coated with essential oil-coated coconut oil with an essential oil desorption control material.
- the diet plaster of the present invention preferably further comprises an absorption accelerator and a base.
- Or limonene is preferred.
- the above bases include lard, beef tallow, fatty oil, branched paraffin, solid paraffin, white petrolatum, caproic acid, enanthic acid, strong prillic acid, pelargonic acid, undecylic acid, lauric acid, Tridecyl acid, myristic acid, pentadecylic acid, palmitic acid, heptadecyl acid, stearic acid, oleic acid, myristyl palmitate, stearyl stearate, myristyl myristate, ceryl lignocerate, lanolin, Glyceryl laurate, glyceryl monomyristate, glyceryl monooleate, glyceryl monostearate, glyceryl dilaurate, glyceryl dimyristylate, glyceryl distearate, glyceryl trilaurate, glyceryl trimyristate,
- the base is preferably a water-soluble base selected from the group strength of carboxybule polymer, hydroxypropylcellulose, macaque gall, and methylcellulose.
- a carboxybutyl polymer is used as the water-soluble base, it is preferable to use at least diisopropylethanolamine and diisopropyl adipate as neutralizing agents.
- each of the above-described essential oils is weighed in a predetermined amount, and these are refined.
- a method for producing a preparation for transdermal absorption diet is weighed in a predetermined amount, and these are refined.
- the present invention further provides an essential oil film forming step in which each of the above-described essential oils is weighed in a predetermined amount, individually mixed with the essential oil adsorbent, and a surface film is formed on the surface of the essential oil adsorbent by each essential oil. And after the essential oil film is formed, a porous carbon substance is added to cover the surface of the essential oil film to form carbon-coated particles; a predetermined amount of carbon-coated particles and absorption promotion
- each essential oil adsorbed on the surface of the essential oil adsorbent to form a surface film is coated with carbon particles, and these carbon-coated particles are further Covered with sheet material. Therefore, each essential oil, which is an active ingredient, does not come into direct contact with the skin, and each essential oil is continuously released for a long time, whereby a transdermal absorption preparation can be produced.
- a sheet-shaped transdermal absorption preparation or plaster having a desired size containing a desired amount of the active ingredient can be obtained.
- the percutaneous absorption-type diet preparation of the present invention has no side effects like conventional diet preparations, and can be easily discontinued by removing the applied site force. . Furthermore, the administration period is not limited.
- a percutaneous absorption-type diet preparation can be easily produced.
- a desorbent for essential oils By using the coated carbon-coated particles, the sustained release effect is high.
- compositions for a percutaneous absorption-type diet preparation of the present invention a preparation having an appropriate dose can be produced for each patient to be administered by cutting into an appropriate size. Furthermore, according to the method for producing a composition for a percutaneous absorption-type diet preparation of the present invention, a formulation for a percutaneous absorption-type diet containing a desired amount of a medicinal component by changing the content of carbon-coated particles. Compositions can be produced.
- FIG. 1 is a graph showing a decrease in the amount of leptin in a crystal when OB-A to OB-C and OBT-A to OBT-C are attached.
- FIG. 2 is a graph showing a decrease in abdominal subdermal fat weight when OB-A to OB-C and OBT-A to OBT-C are applied.
- FIG. 3 is a graph showing weight gain between a general feed feeding group and a high fat feed feeding group.
- FIG. 4 is a graph showing the difference in abdominal fat weight when a reference amount or double amount of OBT-A or OBT-B is applied.
- FIG. 5 is a graph showing the difference in plasma leptin levels when OBT-A or OBT-B reference amount or double amount of preparation is applied.
- the neroli oil used in the present invention is obtained by steam distillation of Daidai (Citrus surantium L. subsp. Amara Engel) flowers originating in France, Italy, Spain, Morocco, Algieria, etc., and the oil yield is About 0.1%.
- Ingredients include trinalol and linalyl acetate (approx. 35-40%), ⁇ -terpineol, geraol, geralacetate, nerolidol (number 0 / ⁇ ), other ⁇ -vinene, dipentene, camphene, oxime, etc. Terpenes, and nitrogen-containing compounds such as anthranilic acid and indole.
- the essential oil obtained from the flower power of Daidai from France or Spain which also contains gera-ol and nerolidol.
- Jasmine oil is cultivated in southern France, Italy, Egypt, Morocco It is an essential oil obtained from Jasminum officinale L. or J. officinale L. var. Grandiflorum.
- Lavender oil is obtained by steam-distilling lavender (Lavendula officinalis Chaix.) Flowers, mainly in France, Italy, Hungary, the former Soviet Union, England, North America, Australia and Hokkaido. Ingredients include linalool (10-20%), linalyl acetate (30-60%), lavandulol, lavandulyl acetate, 3-octanol, ⁇ -vinene, 13 binene, limonene, cineol, citronellal, etc. Containing. In the present invention, it is preferable to use Italian, Hungarian, and French lavender because they contain a relatively large amount of lavandulyl acetate.
- Lavandin oil is obtained by steam distillation of Lavandula hybrida Reverch flowers originating in South France. Lavandin is said to be a cross between lavender and L. latifolia Villars. Ingredients include linalool, linalyl acetate, linalooloxide, cineol, d-camphor, d-labandolol and the like. In the present invention, it is preferable to use lavandin from South France because it contains a relatively large amount of linalyl acetate and cineol.
- Rose oil is a damask from Bulgaria, Tonoreco, Russian damascena Mill. Forma trigintipetala Dieck, France, Sydney, Moracan, Rosa centifolia L., Iran, Morocco Obtained from rose (Rosa damascena Mill.) Flowers.
- 1-citronellol hereinafter referred to as "1-” may be referred to as "L-"
- phenethyl alcohol which are main components, gera-ol , Nerol, linalool, fuarnesol, important components rose oxide and damasenone, other damascones, nonon, stearobutene, methyl eugenol, and the like.
- composition of the present invention it is possible to use a product made in France where the use of the above-mentioned rose absolute is preferable because the quality and supply of the essential oil are stable. High content of phenethyl alcohol. /.
- Cineol-based eucalyptus oil is native to Switzerland and can be obtained by steam distillation of leaves of cineole-based eucalyptus (Eucalyptus globulus Labill.), which is mainly produced in North America, Mexico, Africa, and southern Spain. Oil yield is 0.75-1.25%.
- Ingredients include cineol (70-80%), a-vinene, camphene, pinocarbeol, pinocarbon, myrtenol, berbenone, carvone, eudesmol, and C to C
- composition of the present invention the use of the cineol-based eucalyptus oil as described above is used.
- Grapefruit oil is obtained from grapefruit (Citrus paradisi Mac fayden), which is mainly produced in California, Florida, Texas, Israel and Brazil. Grapefruit peel is obtained by mechanical pressing of grapefruit peel, and grapefruit petidalen oil is obtained by steam distillation of leaves and twigs.
- Ingredients include the ability to contain 90% or more of d-limonene.
- octyl aldehyde, citral, geraol and its acetate ester are also included.
- California grapefruit oil containing octylaldehyde it is preferable to use California grapefruit oil containing octylaldehyde.
- Lemon oil is obtained by pressing the peel of lemon (Citrus limone (shi)), which is mainly produced in California, Sicily, Calabria, Spain, and Brazil and is also cultivated in Japan. Contains d-limonene, citral, octylaldehyde, noraldehyde, linalool, geraol, and various other terpenoids.
- shi lemon
- an essential oil obtained from a California lemon containing nonyl aldehyde is used.
- Orange oil is obtained by pressing the fruits of sweet orange (Citrus sinensis Osbeck var. Bra siliensis Tanaka) widely cultivated around the world, including California, Florida, Spain, Brazil, Italy, and Japan. And can be obtained separately. Ingredients include limonene, citral, n-decylaldehyde, linalool, terbinol, n-nor alcohol, and limonene accounts for 90% or more. As a reference example, it is preferable to use an essential oil obtained from California orange in terms of the content of n-decylaldehyde.
- the grapefruit oil, lemon oil, and orange oil described above may be the same as other essential oils that are commercially available from fragrance manufacturers such as Ogawa Fragrance Co., Ltd. .
- L-menthol (5-methyl-2- (1-methylethyl) cyclohexanol) is usually referred to as menthol. Chemically, there are 12 isomers. The one with the cool flavour unique to mint is natural and synthetic 1-menthol. L-menthol is a colorless columnar or needle-like crystal that is soluble in ethanol but hardly soluble in water. It gradually sublimes at room temperature.
- a synthetic product can be obtained by hydrogenating d-citronellal obtained by fractionating citronella oil as 1-isopulegol. Also, using myrcene obtained from Pinenka et al. As a raw material, optical activity can be obtained by producing citronellal with a special catalyst and asymmetric synthesis of menthol without optical resolution, or by hydrogenating thymol. It can also be obtained from menthol mixtures by optical contamination.
- Limonene (p-menta 1,8-gen) is a monocyclic monoterpene hydrocarbon in which menthane force is also induced, and d-form and 1-form (hereinafter referred to as "L-form"). , Sometimes optical isomers). It is a liquid with a lemon-like aroma and is insoluble in water. Among the limonenes, the d form is contained in orange peel oil, lemon oil, bergamot oil, wikiweed, etc., and one is contained in pine needle oil and heart force oil. The racemate is called dipentene and is contained in a large amount in turpentine oil and camphor oil.
- d-Limonene is obtained by distilling the essential oil obtained by steam distillation of the skin of orange, lemon and the like.
- L-limonene is obtained by fractionating a Japanese-style hearth oil obtained by steam-distilling a whole-planted Japanese-style hearth plant mainly in Hokkaido, Okayama, Brazil, Noraguay, China and other countries.
- Dipentene is obtained by fractionating camphor oil.
- the essential oil adsorbent used in the formulation for transdermal absorption of the present invention refers to an adsorbent for each essential oil described above, and a polyvinyl alcohol having a saponification value of 98.0 to 98.5. It is preferable to use a hydrophilic (CVA) -based hydrophilic resin. If the saponification value is less than 98.0, the surface of the carrier gels and loses its function as an adsorption carrier. However, if the Keny value is 98.0 to 98.5, the function as a stable adsorption carrier can be maintained without gelation.
- CVA hydrophilic
- the free water removing agent used in the percutaneous absorption type diet preparation of the present invention refers to an agent that removes the water present on the skin surface at the site of application, and is an acrylic polymer water-absorbing resin. It is preferable. Many of these acrylic polymer water-absorbing resins have a high water-absorbing ability, and also have good adhesion when heated during the production of the composition described below.
- Such an acrylic water-absorbing resin can be used as long as it can sufficiently absorb the water generated on the skin surface of the application site while the preparation is applied to the application site. Those having a volume of 400 to 800 times are preferred. If it is less than 400 times, it may not be able to absorb water, and a water absorption capacity exceeding 800 times is not necessary. Specific examples include Sunflesh (Sanyo Chemical Industry Co., Ltd.) and Aqua Keep (registered trademark, manufactured by Sumitomo Seika Co., Ltd.). Can. It is preferable to use sunfresh because crushed sunfresh has better adhesion than aqua particles, which are spherical particles.
- the essential oil desorption regulator used in the percutaneous absorption-type diet preparation of the present invention covers the surface of the essential oil adsorbent that has adsorbed each essential oil and formed a film on the surface, and has been adsorbed. It refers to a porous carbon material that regulates the desorption of the essential oil composition. Specific examples include various activated carbons that adsorb various molecules. Using activated charcoal with a surface area of 200 to 1, OOOm 2 Zg is preferred because it uses less 400 to 800 m 2 Zg because it reduces the amount of essential oil adsorbed on the activated carbon and is easily desorbed. preferable.
- the activated carbon has a surface area within this range, various commercially available products can be used. Specific examples include Shirakaba P (Takeda Pharmaceutical Co., Ltd.). From the viewpoint of a small adsorption area and cost, white birch P is preferably used.
- the sheet-forming base used in the percutaneous absorption-type diet preparation of the present invention is a base that forms the above-mentioned composition for diet preparation into a sheet, a heating agent, It contains a conduction inhibitor, an absorption accelerator, and a thermoplastic rosin.
- the exothermic agent refers to a substance that adsorbs moisture in the air and generates heat of adsorption. Desorption of the essential oil composition adsorbed on the adsorption carrier is performed using the thermal energy generated at this time.
- zeolite can be mentioned.
- artificial zeolite that does not contain metal and has a pore size of 0.1 to 0.8 nm in order to supply energy for desorption of essential oils. More preferably 4 nm is used.
- Commercially available products can be used as long as the zeolite has such a pore size, and specific examples include Zeorum (Tosoichi Co., Ltd.).
- the heat conduction inhibitor refers to a compound that can prevent conduction of heat generated suddenly by the free water adsorbed on the free water adsorbent.
- Specific examples include chitosan, cellulose and other polysaccharides.
- chitosan has the advantage that chitosan can be used as a carrier for such a dye when it contains a dye in the preparation.
- cellulose or the like can be used to prevent heat conduction as described above.
- the absorption enhancer is a monotel that acts to promote absorption of essential oil in the preparation.
- Pen compound Specific examples include L-menthol, and commercially available products may be used. Of these, the use of L-menthol has the advantage of evaporating the remaining free moisture present on the skin surface and drying the skin to create an environment where essential oils are easily absorbed.
- the thermoplastic resin preferably has, for example, a key value of about 88.0 such as PVA.
- the percutaneous absorption-type diet preparation of the present invention must be heated to form a sheet. At this time, it is possible to use the above-mentioned carbon-coated particles that can form a sheet that adheres without closing the gaps between the fats and oils at a low temperature of about 180 ° C. without causing the above-described essential oils to be diffused more than necessary. I like it.
- Gocelan L 0301 registered trademark, Nippon Synthetic Chemical Co., Ltd.
- Gocelan L 0301 registered trademark, Nippon Synthetic Chemical Co., Ltd.
- the percutaneous absorption-type diet preparation of the present invention after mixing each essential oil-coated particle produced as described above, among these carbon-coated particles and a base defined in the Japanese Pharmacopoeia, It can also be used as a plaster using a hydrophobic oily base used as a base for ointments and suppositories, or a water-soluble base that is extremely soluble in water. it can.
- Examples of the oleaginous base include lard, beef tallow, fatty oil, hydrocarbon, higher alcohol, higher fatty acid, higher fatty acid ester, glycols, vegetable oil, animal oil and the like.
- hydrocarbons include, for example, liquid paraffin, which is a mixture of various hydrocarbons, branched paraffin (trade name: Isopar (registered trademark), Exxon's Mobil Corp.), solid paraffin, white petrolatum, etc. Can be mentioned.
- Examples of higher fatty acids include, for example, cabronic acid, enanthic acid, strong prillic acid, pelargonic acid, undecylic acid, lauric acid, tridecylic acid, myristic acid, pentadecylic acid, palmitic acid, heptadecylic acid, stearic acid And oleic acid.
- higher fatty acid esters include fatty acid esters such as myristyl palmitate, stearyl stearate, myristyl myristate, and ceryl lignocerate, lanolin, various waxes described later, glyceryl laurate, glyceryl monomyristylate, and glyceryl monoester. Olate, glyceryl monostearate, glyceryl dilaurate, glyceryl dimyristylate, glyceryl distearate, glyceryl trilaurate, glyceryl trimyristate, Dali Examples include seryl tristearate.
- fatty acid esters such as myristyl palmitate, stearyl stearate, myristyl myristate, and ceryl lignocerate, lanolin, various waxes described later, glyceryl laurate, glyceryl monomyristylate, and glyceryl monoest
- fatty oils examples include vegetable oils such as soybean oil, camellia oil, rapeseed oil, peanut oil, sesame oil, safflower oil, animal oils such as mink oil, egg yolk oil, squall, lanolin, fish oil, whale oil, and liver oil. Also included are hardened oils obtained by adding hydrogen to these fatty oils.
- Examples of the wax include carnauba wax, beeswax, and white beeswax. ⁇ Examples of serine include yellow petrolatum and white petrolatum.
- white petrolatum which can be blended without changing almost all drugs, can be suitably used.
- a white ointment can be prepared, and an absorption accelerator can be appropriately added thereto to form a plaster.
- Examples of the water-soluble base include carboxybule polymer, hydroxypropyl cellulose (hereinafter also referred to as "HPC"), macrogol, and methylcellulose.
- HPC hydroxypropyl cellulose
- HPC which is excellent in compatibility with propylene glycol and the like, which can be used as a base for a functional ointment, can also be used.
- an acidic water-soluble polymer for a base when used, it is possible to suppress irritation to the skin by appropriately adding at least diisopropyl ethanolamine and diisopropyl adipate as neutralizing agents.
- the main ingredient of the present invention is a fat-soluble plant essential oil
- an oil-based base for example, L-menthol or limonene can be suitably used as necessary.
- L-menthol or limonene can be suitably used as necessary.
- menthol can be used in the above-mentioned amounts.
- the percutaneous absorption-type diet preparation of the present invention comprises the above essential oil, the above essential oil adsorbent, a free water removing agent, an essential oil desorption regulator, and a sheet forming base as follows. It can be mixed and manufactured. Below, a manufacturing method is demonstrated.
- each essential oil is weighed in a predetermined amount.
- Each essential oil weighed in step 2 is mixed with the essential oil adsorbent PVA separately, and a surface film is formed on the surface of the PVA with each essential oil. Gatsutsu Thus, when three types of essential oil are used, three types of essential oil-coated particles are formed.
- a predetermined amount of activated carbon which is the above-described essential oil desorption regulator, is added to cover the surface of the essential oil film of each essential oil-coated particle, thereby forming each carbon-coated particle.
- this mixture is placed on a pressure-bonding sheet, and another pressure-bonding sheet is placed on the pressure-sensitive adhesive sheet, and heated to produce a sheet-shaped composition for transdermal absorption diet preparation of the present invention.
- the pressure-bonding sheet it is preferable to use synthetic fiber paper (basis weight: 18 to 20 g).
- the sheet-shaped diet composition thus produced is cut into an appropriate size, for example, 2 ⁇ 4 cm, to obtain a sheet-shaped diet composition piece, and the four sides of the composition piece are heat sealed. Place between two sheet-like materials such as non-woven fabric cut to the extent possible. Next, four sides of these sheet-like materials are heat-sealed to prepare one piece of the preparation for transdermal absorption of the present invention.
- the sheet-like material is selected from a group force that also has paper, woven fabric, or nonwoven fabric strength.
- the essential oil component contained in the composition for transdermal absorption diet is preferably a gas molecule. It is more preferable that it is a non-woven fabric, in that these are easy to permeate when passed through the gaps between the sheet-forming base particles.
- a plaster it is produced as follows. First, a predetermined amount of the essential oil is weighed, and then the essential oil weighed with PVA is mixed with PVA, and a surface film is formed on the surface of the PVA with the essential oil. A predetermined amount of the above-mentioned activated carbon is added to cover the surface of the essential oil film to form carbon-coated particles A.
- the weighed menthol is mixed with another PVA. After covering the surface of the PVA as in the case of the above essential oil, activated carbon is added to form carbon-coated particles B.
- composition for diet preparation and the formulation for diet of the present invention can be produced.
- Reference Example is produced in the same manner except that the carbon-coated particles of a single essential oil are used in place of the combination of the above-described three types of carbon-coated particles of the essential oil. In this way, the preparation of Reference Example can be used.
- the case where a sheet-like preparation is used as a transdermal absorption preparation and the case where a plaster is used is described as an example.
- the above-described essential oil-coated particles are used as an absorption accelerator.
- it can be mixed with a commonly used ointment base to make an ointment, or it can be made into a cream or the like.
- composition for percutaneous absorption diet the preparation for percutaneous absorption diet (Example of the present invention), the positive control preparation (Reference Example), and the placebo (Comparative Example) of the present invention.
- Neroli oil, jasmine oil, lavender oil, rose oil, cineole eucalyptus oil and L Menthol was purchased from Ogawa Fragrance Co., Ltd. Grapefruit oil, lemon oil, and orange oil were also purchased from Ogawa Fragrance Co., Ltd.
- Shin-Etsu Poval C-17GP was purchased from Shin-Etsu Chemical Co., Ltd.
- Gocelan L-3031 was purchased from Nippon Synthetic Chemical Co., Ltd.
- Sunfresh (registered trademark) was purchased from Sanyo Chemical Industries as an acrylic water-absorbing resin.
- Hakuho P as activated carbon from Takeda Pharmaceutical Co., Ltd.
- Zeolum registered trademark
- Zeolite Zeolite from Tosoh Corporation.
- chitosan Koichi Chitosan was purchased from Koyo Chemical Co., Ltd.
- Chemical fiber paper was purchased from Nippon Paperboard Daishowa Co., Ltd., and non-woven fabric was purchased from Nisshinbo Co., Ltd.
- the carbon-coated particles were prepared according to the formulation shown in Table 1 below.
- formulation name OBT-A, OBT-B, and OBT-C
- the combination of carbon-coated particles prepared in the amounts shown in Table 1 1.
- lg Was prepared to be included per piece.
- ⁇ 4- a 223 2 3 223
- neroli oil (N), jasmine oil C and lavender oil (L) are shown in Table 3 above. Separately weighed in the indicated amounts and placed in three 5 OOmL clear glass sealed containers, respectively. Where the above amount of PV A (Shin-Etsu Poval C-17GP) was added and mixed at room temperature to coat the surface of the PVA with each essential oil.
- activated carbon in the amount shown in Table 3 above was added to these containers and mixed to form carbon-coated particles of each essential oil.
- Each prepared carbon-coated particle was stored in a highly airtight container, for example, a glass container with a lid with a lid, and stored at room temperature.
- each carbon-coated particle was weighed in the amount shown in Table 3 to form a combination of carbon-coated particles A B and C.
- a C correspond to the formulation numbers OBT-A OBT-B and OBT-C.
- the above bases are: Sun Fresh (manufactured by Sanyo Chemical Industries, Ltd.), Zeorum (Zeolite, manufactured by Tosoh Corporation), L-Menthol (manufactured by Ogawa Fragrance Co., Ltd.), Koyo Chitosan (Koyo) Chemical Co., Ltd.) were prepared by mixing and stirring one by one in this order.
- the carbon-coated particle combination A shown in Table 3 was named OBT-A, the one containing B was named OBT-B, and the one containing C was named OBT-C.
- the loss rate of essential oil during thermocompression bonding described later was calculated as 15%.
- Each carbon-coated particle was prepared in the same procedure as described above using grapefruit oil, lemon oil, or orange oil. Instead of the combination of the above carbon-coated particles, a preparation containing any one of the carbon-coated particles alone was produced in the same manner as described above and used as a reference example. Grapefruit oil containing carbon-coated particles was named OB-A, lemon oil containing carbon-coated particles was named OB-B, and orange oil containing carbon-coated particles was named OB-C. Tables 8 and 9 below show the carbon-coated particles contained in the three types of Reference Example preparations and their compositions.
- the placebo was produced in the same manner as above except that a black fine paper of the same size was used instead of the sheet-like composition containing each essential oil-coated particle.
- Test animals were 5 weeks old ICR male mice purchased from Tokyo Experimental Animals Co., Ltd., with a room temperature of 24 ⁇ 1 ° C and a light / dark cycle of 12 hours (lights on at 8 o'clock, lights off at 20 o'clock). A group of 10 animals per group was acclimated for 1 week with free access to water and feed.
- the diet preparation (invention example), the reference preparation (reference example), and the placebo (comparative example) were assigned to each cage, and pasting was repeated for 14 days.
- Pentobarbital was purchased from Dainippon Pharmaceutical Co., Ltd.
- a mouse levtin ELISA kit was purchased from Morinaga Co., Ltd. to measure the amount of levtin in plasma.
- mice The day before the start of application, the mouse was anesthetized with pentobarbital (70 mg / kg, i.p.), and the waist was shaved. From the start of application, diet preparation, reference preparation and placebo were applied under light ether anesthesia. These were replaced once a day, this replacement was repeated for 2 weeks, 24 hours after the final application, the mice were decapitated, and blood and abdominal subcutaneous fat were collected.
- pentobarbital 70 mg / kg, i.p.
- Fig. 1 shows the effect on plasma lebutin levels.
- the reference product for each product is indicated as 1
- the product containing twice the amount of the reference product is shown as 2.
- the leptin level in plasma is twice that of OB-B (X 2). Only a significant decrease was observed.
- OBT-A reference product (X l), doubled amount (X2), and doubled amount of OBT-B (X2) were affixed, a significant decrease was observed. It was shown that it has the effect of reducing the amount of levtin.
- Fig. 2 shows the effect on the abdominal subcutaneous fat tissue weight.
- the reference product for each product is indicated as 1, and the product containing twice the amount of the reference product is shown as 2.
- a 4-week-old ICR male mouse was purchased from Tokyo Experimental Animal Co., Ltd., and kept in a cage under conditions of a room temperature of 24 ⁇ 1 ° C and a light / dark cycle of 12 hours (lights on at 8 o'clock, lights off at 20:00).
- a group of 10 animals per week was acclimated for one week with free access to water and feed.
- a high fat diet (High Fat Diet 32) was purchased from Nippon Claire Co., Ltd., and MF was purchased from Oriental Yeast Co., Ltd. as a general feed. Pentobarbital was purchased from Dainippon Pharmaceutical Co., Ltd. In addition, a mouse leptin ELISA kit was purchased from Morinaga Co., Ltd. to measure the amount of leptin in plasma.
- Examples of the diet preparation of the present invention include the above-mentioned OBT-A standard product (OBT-AX 1) and doubled amount (OBT-AX 2), OBT-B standard product (OBT-BX 1) and doubled amount (OBT—BX 2) was used.
- OBT-AX 1 OBT-A standard product
- OBT-BX 1 OBT-B standard product
- OT—BX 2 OBT—BX 2
- mice in which obesity was induced by feeding the above ICR male mice with the above high fat diet for 4 weeks were used.
- the group with the control formulation affixed to the general feed group was defined as the negative control group, and the group with the control formulation affixed to the high fat feed group was defined as the positive control group.
- each group of mice was measured daily. On the 28th day after the start of feeding each feed, each group of mice was anesthetized with bentobarpital (70 mg / kg, i.p.) and the circumference of the trunk was shaved. Each preparation was applied under light ether anesthesia and repeated once a day for 14 days.
- mice were decapitated 24 hours after the final application (day 43), and blood and abdominal subcutaneous fat tissue were collected. The collected blood was quickly mixed by inversion, centrifuged at 10,000 X g for 15 minutes at 4 ° C, and the resulting plasma was stored frozen at 80 ° C as a sample for measuring leptin levels.
- the amount of leptin in plasma was determined using a mouse leptin ELISA kit, as in Example 3 above. The weight of the abdominal subcutaneous adipose tissue was measured.
- the pharmaceutical preparation for diet of the present invention is useful in the field of medicine such as prevention or treatment of obesity by reducing the amount of levtin in mouse plasma or the weight of subcutaneous abdominal fat.
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Abstract
Description
Claims
Priority Applications (4)
Application Number | Priority Date | Filing Date | Title |
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JP2007533224A JPWO2007026645A1 (ja) | 2005-08-31 | 2006-08-28 | 植物精油成分を有効成分とするダイエット用組成物、その組成物を含むダイエット用シート状組成物及び経皮吸収型ダイエット用医薬製剤、並びにこれらの製造方法 |
EP06783091A EP1932532A1 (en) | 2005-08-31 | 2006-08-28 | Dieting composition comprising plant-derived essential oil as active ingredient, sheet-type dieting composition comprising the composition, transdermal pharmaceutical preparation for dieting, and methods for production of the preparation |
CA002620687A CA2620687A1 (en) | 2005-08-31 | 2006-08-28 | Composition for diet comprising plant essential oil as active ingredient,sheet type composition for diet comprising thereof, percutaneous pharmaceutical agent for diet comprising thereof, and method for producing thereof |
US12/071,865 US20080233219A1 (en) | 2005-08-31 | 2008-02-27 | Composition for diet comprising plant essential oil as active ingredient, sheet type composition for diet comprising thereof, percutaneous pharmaceutical agent for diet comprising thereof, and method for producing thereof |
Applications Claiming Priority (2)
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JP2005-250735 | 2005-08-31 | ||
JP2005250735 | 2005-08-31 |
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US12/071,865 Continuation US20080233219A1 (en) | 2005-08-31 | 2008-02-27 | Composition for diet comprising plant essential oil as active ingredient, sheet type composition for diet comprising thereof, percutaneous pharmaceutical agent for diet comprising thereof, and method for producing thereof |
Publications (1)
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WO2007026645A1 true WO2007026645A1 (ja) | 2007-03-08 |
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PCT/JP2006/316862 WO2007026645A1 (ja) | 2005-08-31 | 2006-08-28 | 植物精油成分を有効成分とするダイエット用組成物、その組成物を含むダイエット用シート状組成物及び経皮吸収型ダイエット用医薬製剤、並びにこれらの製造方法 |
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US (1) | US20080233219A1 (ja) |
EP (1) | EP1932532A1 (ja) |
JP (1) | JPWO2007026645A1 (ja) |
CN (1) | CN101300020A (ja) |
CA (1) | CA2620687A1 (ja) |
RU (1) | RU2008112216A (ja) |
WO (1) | WO2007026645A1 (ja) |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
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WO2014051113A1 (ja) * | 2012-09-28 | 2014-04-03 | 株式会社資生堂 | Vegfc産生促進剤 |
JP2015182972A (ja) * | 2014-03-24 | 2015-10-22 | 株式会社コーセー | 抗糖化剤 |
Families Citing this family (4)
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KR100982716B1 (ko) * | 2008-08-04 | 2010-09-16 | 니라팜 주식회사 | 아로마테라피 패치 |
CN102743304B (zh) * | 2012-07-19 | 2013-10-30 | 贵州宏宇药业有限公司 | 具有美体塑身功能的复方精油及其制备方法 |
CN103432560B (zh) * | 2013-09-10 | 2014-11-05 | 南方医科大学 | 一种治疗单纯性肥胖症的外用药物及其制备方法 |
KR101541016B1 (ko) * | 2015-06-03 | 2015-08-04 | 연세대학교 산학협력단 | 피노카베올의 신규한 용도 |
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2006
- 2006-08-28 JP JP2007533224A patent/JPWO2007026645A1/ja active Pending
- 2006-08-28 CN CNA2006800405590A patent/CN101300020A/zh active Pending
- 2006-08-28 WO PCT/JP2006/316862 patent/WO2007026645A1/ja active Application Filing
- 2006-08-28 CA CA002620687A patent/CA2620687A1/en not_active Abandoned
- 2006-08-28 RU RU2008112216/15A patent/RU2008112216A/ru unknown
- 2006-08-28 EP EP06783091A patent/EP1932532A1/en not_active Withdrawn
-
2008
- 2008-02-27 US US12/071,865 patent/US20080233219A1/en not_active Abandoned
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Cited By (5)
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WO2014051113A1 (ja) * | 2012-09-28 | 2014-04-03 | 株式会社資生堂 | Vegfc産生促進剤 |
JPWO2014051113A1 (ja) * | 2012-09-28 | 2016-08-25 | 株式会社 資生堂 | Vegfc産生促進剤 |
US10624829B2 (en) | 2012-09-28 | 2020-04-21 | Shiseido Company, Ltd. | VEGFC production promoter |
US11213472B2 (en) | 2012-09-28 | 2022-01-04 | Shiseido Company, Ltd. | VEGFC production promoter |
JP2015182972A (ja) * | 2014-03-24 | 2015-10-22 | 株式会社コーセー | 抗糖化剤 |
Also Published As
Publication number | Publication date |
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EP1932532A1 (en) | 2008-06-18 |
RU2008112216A (ru) | 2009-10-10 |
CN101300020A (zh) | 2008-11-05 |
CA2620687A1 (en) | 2007-03-08 |
US20080233219A1 (en) | 2008-09-25 |
JPWO2007026645A1 (ja) | 2009-03-05 |
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