CN1728986A - Use of molded bodies for external application - Google Patents
Use of molded bodies for external application Download PDFInfo
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- CN1728986A CN1728986A CN 03824235 CN03824235A CN1728986A CN 1728986 A CN1728986 A CN 1728986A CN 03824235 CN03824235 CN 03824235 CN 03824235 A CN03824235 A CN 03824235A CN 1728986 A CN1728986 A CN 1728986A
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- molding
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
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- 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
- A61K8/73—Polysaccharides
- A61K8/733—Alginic acid; Salts thereof
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- 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
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- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08L—COMPOSITIONS OF MACROMOLECULAR COMPOUNDS
- C08L5/00—Compositions of polysaccharides or of their derivatives not provided for in groups C08L1/00 or C08L3/00
- C08L5/04—Alginic acid; Derivatives thereof
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- Organic Chemistry (AREA)
- Medicinal Preparation (AREA)
- Cosmetics (AREA)
Abstract
The invention relates to the use of a molded body comprising at least one skeleton-forming agent, excluding proteins, one or several optional active substances, and one or several optional adjuvants for external application. Also disclosed are a method for producing said molded bodies and novel molded bodies.
Description
The molding that the skeleton that the present invention relates to contain at least a nonprotein forms agent, also can contain one or more active substances and one or more auxiliary agents optionally suitably the time is used for the purposes of external, and also relates to a kind of method and novel molding for preparing described molding.
Germany Patent document DE 4201172 has put down in writing medicinal or beauty treatment usefulness and has contained the granule that forms agent based on proteinic skeleton among DE 4201173 and the DE 4201179.These granules are particularly useful for preparing oral pharmaceutical preparation.This particulate preparation process is, will form the dispersion that agent and optional beauty treatment or active constituents of medicine form by the protein skeleton earlier and splash in the refrigerative inert fluid of the degree of depth, preferably splashes in the liquid nitrogen, separates then through refrigerated granule and lyophilization.But in order to form granule under these conditions, just need exist the protein skeleton to form agent, particularly collagen or collagen derivant, could form stable granule under these conditions because have only described protein skeleton to form agent.This phenomenon perhaps is that active force is relevant between particular molecule with protein molecule.
According to the prepared grain diameter of above-mentioned Germany Patent document, record is 0.2 to 12mm in the overview section of description.But in an embodiment, getable maximum particle diameter only is 4mm.Wherein the mean diameter that refers to that is to say, granule will stand the fluctuation of bigger particle diameter more or less.
But,, preferably need have identical shaped and relatively large molding particle diameter particularly for the external beautifying use.The end user can use these moldings easily.Generally speaking, the molding of powder or granule or inhomogeneous formation all is not suitable for this purpose.People are devoted to provide the molding that uses a kind of size of dosage form in the time of can allowing at every turn to use.In addition, bigger, also want to give distincter outward appearance impression such as molding that can be painted.
In addition, the use of protein skeleton formation agent is not preferred in some situation.Therefore, some end user particularly in cosmetics, preference is used pure plant product more and more.In addition, these reasons also come from the consideration on the basic ethical.
In addition, mix protein and also require comparatively complicated procedure of processing usually.And time spent and in its characteristic range outside on skin, the character that the protein skeleton forms agent under a lot of situations can be restricted, because they always are made up of identical aminoacid.
Therefore people wish to exist a kind of proteinic beauty treatment or medicine molding preparation of not being based on more and more, especially for the molding of external dispenser.But when people wish to obtain a kind of based on plant, as those according to used method makes in aforementioned patent documentation, when forming agent such as the skeleton of alginate, but be surprised to find, can't make by these methods at all and to have regular shape, particularly have sufficient size and have a required deliquescent molding of enough externals.
It is preparations about oral formulations that many documents are arranged, and this preparation process comprises the lyophilization step.For example EP-A-0352190 discloses the compositions that is made of solid-state and porous unit body, and said composition includes subparticle or nano-particle.Their preparation process is especially at first put into unguentum the cavity of mould, then carries out freeze-drying process.The task that EP-A-0352190 proposed is to look for a kind of taste and can quick oral formulations soluble in water can covered.Wherein do not mention the local application of preparation.Similarly, disclose among the EP-A-0399902 make by lyophilizing, be used for preparation equally and have the taste of covering effect and can rapidly-soluble pharmaceutical preparation.The preparation that orally uses by lyophilizing equally only can be used for of making is disclosed among the US-A-4758598.The dissolubility excipient that is used for medicament is carried out oral administration is disclosed among the US-A-4079018.Put down in writing the drug-supplying system of oral administration that can controllable release among the US 4695463.In addition, also disclose a kind of freeze-dried composition among the EP-A-0412449, but it does not have the geometry of rule.Which does not have disclose the possible approach that how to prepare the regular molding with big shape in the aforesaid documents, and can easily dissolve and play the effect of carrier for active principle when requiring these moldings to be used on the skin outside.
Therefore, the new purposes that task of the present invention is to provide the molding that contains active component to be used for external, this molding contains and is not based on proteinic skeleton and forms agent.Described molding should be relatively large, and having enough cohesivenesss is mechanical strength, molding regularly, and can easily dissolve on being administered to skin the time, and should be able to bring comfortable use feeling.In addition, these moldings also should be suitable for holding different active component, and are special in cosmetic activity composition and medical treatment or active constituents of medicine, and the effect of playing their carrier.
Therefore, the present invention proposes and contain at least a nonprotein skeleton formation agent, the molding that also can contain one or more active substances and one or more auxiliary agents optionally in the time of suitably is used for the purposes of external.
Within the scope of the present invention, it is a kind of geometrical body with regular shape that so-called molding can be regarded as, for example particularly spheroid, cuboid, cone, star body, it perhaps can also be the molding of natural imitation circle object, as those animal shapes, as marine animal such as Asterias amurensis Lutken, marine product such as shell etc., plant and plant are local as leaves etc.According to the following preparation method that is used to prepare the used molding of the present invention that will narrate, can obtain all these moldings.According to the present invention, also several described moldings can be put in the container.Here also can refer to the mixture of the molding of different geometries.Described molding can be divided into the aliquot encapsulation separately.But preferred, particularly when being used for cosmetics, make several moldings adjacent contact in container.
Volume itself to used molding is also unrestricted, but depends on its preparation method.Reasonably be that the preferred volume value is at least about 0.1cm
3, preferred 0.3cm
3, more preferably at least about 0.5cm
3, most preferably at least about 0.8cm
3As for the higher limit of used volume, reasonably be to be restricted to be no more than about 6cm
3, preferably be no more than about 5cm
3, more preferably no more than about 4cm
3The size of molding is especially determined by molding external position.Therefore, use bigger molding just can be applied on the bigger body surface area or hair and (for example directly the molding of moistening is coated on back etc., or as bath additives), opposite, preferably use less molding when going up being applied to less body surface area (for example buccal etc.).
The diameter of molding (maximum spacings in the molding of various geometries between 2) should be suitably at least about 3mm, preferably at least about 5mm, more preferably at least about 7mm, especially preferably be no more than about 60mm until comparatively being desirably at least about 8mm, preferred about 50mm, 40mm more preferably from about, especially preferably about 30mm.
Particularly preferred a kind of molding has geometry spherical in shape substantially, and sphere diameter is between 3 to 30mm, preferably between 5 to 20mm, more preferably between 7 to 15mm, between 8 to 13mm.
The skeleton that the used molding of the present invention contains at least a nonprotein forms agent.So-called skeleton forms agent and typically refers to so-called hydrocolloid, and promptly (part) is water miscible, natural or synthetic and can form the polymer of gel or viscosity solution in Aquo System.More satisfactory skeleton forms agent and is selected from polysaccharide or synthetic polymer.Preferred skeleton forms agent and is selected from polysaccharose substance.Polysaccharide for example comprises, homopolysaccharide or heteropolysaccharide, for example alginate, particularly sodium alginate, carrageenin, pectin, traganth, guar gum, angle bean nuclear powder, agar, arabic gum, xanthan gum, the starch of natural and modification, dextran, dextrin, maltodextrin, chitosan, glucosan, as β-1,3-glucosan, β-1, the 4-glucosan, as cellulose, mucopolysaccharide is as hyaluronic acid etc.Synthetic polymer comprises, for example: cellulose ether, polyvinyl alcohol, polyvinylpyrrolidone, the synthetic cellulose derivant is as methylcellulose, carboxycellulose, carboxymethyl cellulose, cellulose esters, cellulose ether such as hydroxypropyl cellulose, polyacrylic acid, polymethylacrylic acid, poly-(methyl methacrylate) are (PMMA), polymethacrylates (PMA), polyvinyl alcohol etc.Also can use multiple skeleton to form the mixture of agent.According to the present invention, particularly preferably be alginate, extremely preferably sodium alginate.Preferably low viscous skeleton forms agent, the sodium alginate that does not particularly have calcium, (calcium content＜3 weight %, preferred＜2 weight %, more preferably＜1.5 sodium alginate of weight %), that is to say that those preferred viscosities are lower than 2000mPas, more preferably less than 1000mPas, (also be that to form solution (1% solution w/w) that agent forms in the distilled water of 99ml be under the condition of 6-8 at 20 ℃ and pH value for the skeleton of 1g most preferably less than 100mPas, have less than 2000 or 1000, or the viscosity number of 100mPas) skeleton form agent.Preferably use this low viscous skeleton to form agent on the one hand owing to the restriction of working condition, as sodium alginate, on the other hand, use this low viscous skeleton to form the dissolving that agent also can be convenient to preparation, perhaps after having added water, can bring higher disintegrate or rate of dissolution and therefore make on skin, to scatter easily.Especially, the use of this low-viscosity alginates type material can make the used molding of the present invention have bigger rate of dissolution.
Preferably form polysaccharide that agent uses as skeleton among the present invention is to have about 103 to about 108, preferred about 104 to 107 more satisfactory average molar mass more satisfactoryly.
It is close skin and preferably can form the film that one deck has defencive function on being applied to skin the time that skeleton forms agent.
For clarity sake, should further be mentioned that the what is called skeleton of the nonprotein " form agent " do not get rid of based on the activity of proteins composition in category of the present invention, such as enzyme, hormone etc.
The used molding of the present invention also can contain one or more active component, preferred at least a active component when suitable.Active component is particularly including the beauty treatment that the external of being applicable to is arranged or medical treatment or active constituents of medicine.The used molding of the present invention preferably contains at least a beauty treatment and/or active constituents of medicine.Accordingly, used molding preferably also refers to cosmetics or pharmaceutical preparation among so-called the present invention.Beauty treatment in the scope of the invention is with molding or use the molding of improving looks and making with active component, basically be the preparation that belongs to defined in food and the article of everyday use method (LMBG), that is to say it is to constitute described material or preparation, be to be used for human body outside those regulations are and to be used for cleaning, nursing, or window dressing or body odor, or give the material of fragrance, unless they be prescribed especially be used for alleviating or eliminate a disease, pain, somatic damage or slight illness.In this scope, beauty treatment molding used among the present invention is for example, to take a shower and use preformulation, skin washing and skin cleaner, skin-care agent, particularly face skin nursing agent, ocular region cosmetic product, the lip nursing agent, manicure agent, foodcare agent, hair-care agent, shampoo particularly, hair conditioner, gentle detergent etc., the sunscreen sent out, the agent of skin brown, the plain agent of skin depigmentation, deodorizer, Antihydrotika, depilatory, the combination of anthelmintic etc. or these preparations.
The beauty treatment chemical compound can also be that its example includes such as medicable chemical compound on the dermatological in the time of suitably: the anti-acne agent, anti-microbial agents, anti-evaporating agent, astringent, deodorizer, depilatory, skin conditioning agent, the skin smooth agent is used to improve preparation such as the glycerol or the carbamide of skin water combination, sunscreen, keratolytic, free radical scavenger, antiseborrheic, remove the moss agent, anticorrosion active component is used for the treatment of the active component of skin aging symptom and/or is used to adjust the preparation of skin difference and/or hypertrophy and/or pigementation, vitamin such as vitamin C, active component with zest side effect, as alpha-hydroxy acid, β-hydroxy acid, 2-ketoacid, beta-keto acid, biostearin (vitamin A, retinal, xanthoplane acid), dihydroxy-anthracene phenols (dioxo anthrol), Anthranoide, peroxide (particularly benzoyl peroxide), loniten, lithium salts, antimetabolite, vitamin D and derivant thereof; Catechol, flavonoid, ceramide, fatty material is as mineral oil, as paraffin oil or vaseline oil, silicone oil, vegetable oil such as cocos nucifera oil, Prunus dulcis acid, Fructus Pruni oil, Semen Maydis oil, Simmondsia chinensis oil, olive oil, American Avocado Tree oil, Oleum sesami, Petiolus Trachycarpi oil, eucalyptus oil, oil of rosemary, Essential lavender oil, Oleum Pini, thyme oil, Oleum menthae, cardamom oil, orange blossom oil, soybean oil, bran oil, Testa oryzae oil, vegetable oil and Oleum Ricini, Semen Tritici aestivi seed oil and isolated vitamin E therefrom, Folium Salicis Babylonicae vegetable oil, vegetable lecithin (for example soybean lecithin) separates the sphingolipid/ceramide from plant, animal oil or fat, as oils and fats, lanoline, butter oil, fatty acid ester, the fat of aliphatic alcohol and fusing point are corresponding to wax (animal wax such as the Cera Flava of skin temperature, Brazil wax and candelilla wax, mineral wax such as microwax and synthetic wax such as Tissuemat E or silicone wax), and all are suitable for the oil of cosmetic purpose, for example at the CTFA-collection of thesis, Cosmetic Ingredient Handbook, front page, 1988, The Cosmetic, Toiletry and FragranceAssociation, Inc., mentioned those polyunsaturated fatty acids among the Washington, basic fatty acid (for example gamma-Linolenic acid), enzyme, coenzyme presses down enzyme material, hydration reagent, the skin placebo, cleaning agent or foaming agent and inorganic or synthetic delustring filler, grinding agent.
In addition, also can should be mentioned that active components of plants extract or quintessence oil that therefrom obtains or simple substance.Generally speaking, the active components of plants extract all is selected from usually by solid-state plant extract, liquid plant extract, water loving plant extract, lipophilic plant extract, each kind of plant inclusions; And their mixture, as flavonoid and aglycone thereof; Rutin, Quercitroside, daflon, hyperin, (newly) hesperidin, Hesperidin, Semen Ginkgo (for example ginkgetin glucosides (Ginkoflavonglycoside)), Fructus Crataegi extract (for example oligomeric procyanidin), Semen Fagopyri Esculenti (for example rutin), the Flos Sophorae Immaturus (for example rutin), birch leaf (for example Quercitroside glucoside, hyperin and rutin), Fols sambuci williamsii (for example rutin), Flos Tiliae (ether oil that for example contains Quercitroside and farnesol), hypericum oil (for example olive oil quintessence oil), Flos Inulae, arnica (the oiliness quintessence oil that for example contains the flower of ether oil, the polarity quintessence oil that contains flavonoid), Herba leucadis ciliatae (for example flavone, ether oil); Immunostimulant; Leaf Echinacea Species (for example alcohol quintessence oil, fresh water, pressed liquor), Eleutherokokkus senticosus; Alkaloid; Rauwolfine (for example third moderate pulse inflammation), Herba Catharanthi Rosei (for example minorine); Other plant medical agent: Aloe, Aesculus chinensis Bunge (for example Aescin), Bulbus Allii (for example Oleum Bulbus Allii), Fructus Ananadis comosi (for example bromelain), Radix Ginseng (for example ginsenoside), Herba Silybi mariani fruit (for example standardized silymarin extract), phyllodium tree root (for example ruscogenin), Rhizoma et radix valerianae (Valepotriate for example, Tct.Valerianae), piper meehysticum (for example Kavalactone), Flos lupuli (Flos Humuli Lupuli) (for example bitter material of Flos lupuli (Flos Humuli Lupuli)), Herba Passiflorae Caeruleae (Passi-florae) extract, Radix Gentianae (for example ethanol extraction), the drug extract that contains anthraquinone for example contains the aloe vera juice of aloin, pollen extract, algae extract, licorice root extract, Petiolus Trachycarpi extract, Galphimia (for example Urtinktur), Herba Visci tree (for example water-ethanol quintessence oil), phytosterol (for example cupreol), Herba Verbasci Thapsi (for example water-ethanol extract), drosera (for example mulse extract), Fructus Hippophae (juice that for example therefrom obtains or Oleum Hippophae), Radix althaeae roseae, the harbinger-of-spring root extract is from Radix Malvae sylvestris, Symphytum officinale, Caulis Hederae Sinensis, the Herba Equiseti Hiemalis, common milfoil, ribgrass (for example squeezing juice), Herba Urticae Cannabinae, Herba Chelidonii, the fresh plant extract of Herba Coriandri; Plant extract and aloe vera extract from Norolaena lobata, Flos Tagetis Erectae, Teeoma siems, Fructus Momordicae charantiae.
Preferred cosmetic activity composition is natural and synthetic Moisture factor, as glycerol, and carbamide and ceramide, shielding medicine for skin, skin lightener, vitamin, antioxidant, so-called age resister, counter-stimulus, sunscreen etc.
Different with the above-mentioned molding that is mainly used in the cosmetics, the molding (medicament) of so-called therapeutic use refers to and contains at least a medicine or treatment usefulness, special also is those of the active component used of dermatosis, and especially in the medical method scope they still be prescribed be used for treating, alleviation or prevent disease, misery, somatic damage or ailing.These medicaments or the active component that are given for the external purpose are the active component or the transdermal active component of activation skin.They comprise, for example: be used for the treatment of dermopathic medicament, but the analgesic of external, dextropropoxyphene for example, pentazocine, dolantin, buprenorphine; Rheumatism/anti-inflammatory (NSAR) class, indomethacin for example, diclofenac, naproxen, ketoprofen, ibuprofen, flurbiprofen, salicylic acid and Salicylate are biological as aspirin, Oxicame; Steroid hormone, betamethasone for example, dexamethasone, prednisolone, ethinylestradiol, Medroergotamin, my alkali of dihydro wheat; The gout medicament, as benzbromarone, allopurinol; The external preparation for skin medicament comprises antibacterial, antifungal, and the antiviral activity composition, inflammation suppresses active component, antipruritic active component, narcotic activity composition, benzocaine for example, corticoid, acne medicament, parasiticide active component; But external hormone; Antidote; Immunity tranquilizer etc., but the material of all externals.
Preferred therapeutic agent is an analgesic, for example immune tranquilizer, and hormone is used for the treatment of dermatosis such as nervous dermatoses, medicament of anaphylaxis dermatosis etc. and herpes agent.
Skeleton forms agent, particularly polysaccharide also can have certain therapeutical effect (for example preferred skeleton that uses forms agent alginic acid (sodium) salt and can play antivirus action to a certain extent), but they but do not belong to active component according to the present invention.
Employed molding randomly contains one or more auxiliary agents among the present invention in addition.Auxiliary agent comprises: the surfactant except above-mentioned detergent surfactant, as dispersant, emulsifying agent etc., filler, pH value regulator, as buffer substance, stabilizing agent, cosolvent, medicine and beauty treatment usefulness or other dyestuff and pigment, preservative agent, plasticizer, lubricant or antiseize paste etc.Particularly preferred auxiliary agent is a squalane lubricating oil.
Molding of the present invention can be used for human body or animal body outward.The external process is following carrying out, and promptly water or contain the aqueous solution moistening molding of the present invention of one or more active component and/or auxiliary agent perhaps makes it soluble in water.Different according to amount of liquid and used molding material dissolves, molding can be dissolved fully and be formed solution or disintegrate and form gel.If molding of the present invention is dissolved in the water of volume more, then usually indication be exactly the occasion of usefulness of taking a shower, and this use liquid belongs to external category of the present invention.Only use a spot of water or active ingredient solution and/or compounding agent solution just can the moistening molding but preferred use will make, and directly on skin or hair, form gel, and rub there and massage.
The invention still further relates to a kind of assembly, it contains at least a molding used according to the present invention and at least a aqueous solution that contains one or more active component and/or auxiliary agent, and this assembly is whole spatial organization form (using suit, external member, kit etc.).So-called active ingredient solution can be meant, for example, the solution of volatile active component and/or auxiliary agent, and they can or should not be blended in the molding by lyophilization according to preparation method, as some composition of ether oil, perfume etc.
Amount and kind according to the active component and/or the auxiliary agent of other existence, the skeleton at least about 10 weight % that the used molding of the present invention can preferably contain in the molding gross weight forms agent, more preferably at least about 15 weight %, preferred again 30 weight %, most preferably form agent until the skeleton of 100 weight % at least about 50 weight %, polysaccharide especially preferably is as sodium alginate.
Usually, molding also contains the water of residual volume.According to the difference (hydrophilic, hydrophobic) of the kind of active component, water content can as many as 20 weight %.Deposit after by lyophilizing making molding, water content can change, and normally improves.After making, the water content of molding is preferably at about 2 weight % to 15 weight %, more preferably at 2 weight % to 12 weight %.
Used molding contains 0 to 85 weight % among the present invention, one or more active component of preferred 0.000001 weight % to 50 weight %.Amount ratio depend on to a great extent so-called active component whether be beauty treatment with or the therapeutically active composition.Special therapeutically active composition in some cases can be to use very on a small quantity.
Molding contains one or more auxiliary agents of 0 to 85 weight %.Molding can contain the auxiliary agent of 0.1 to 70 weight %, more preferably the auxiliary agent of 5 to 60 weight %.
Particularly with the shared occasion of other active ingredient solution under, also can use those only to form the molding that agent and other optional auxiliary agent constitute by hydrophilic skeleton.
Preferred a kind of auxiliary agent is a squalane.Wherein refer to a kind of beautification oil.Although hydrophobic property is arranged, squalane still can shockingly play and improve the deliquescent effect of molding, and this just convenient outer skin that is used for.In addition, though it is not the active component of indication in the category of the present invention, squalane liquid also has the skin nursing effect.In a preferred embodiment, molding contains the squalane (content can be determined by extracting with diethyl ether according to the Weibull Stoldt method described in official's compilation of the inspection method ASU of foundation § 35LMBG) of 10 to the 60 weight % that have an appointment.
In category of the present invention, above-mentioned substance not to be got rid of in the layout situation aspect the auxiliary agent kind, these auxiliary agents also can play some beauty treatment and/or therapeutical effect.
Particularly preferred molding comprises:
One or more skeletons of-at least 10 weight % form agent, polysaccharide particularly, as sodium alginate, the sodium alginate that does not particularly have calcium, and the aqueous solution of its 1 weight % or the suspension that forms in water (are dissolved in 1g in the 99ml water under 20 ℃, pH6-8) should preferably have less than 2000, be more preferably less than 1000, preferred especially viscosity less than 100mPas
One or more active component of-0.000001 weight % to 50 weight %,
One or more auxiliary agents of-0.1 weight % to 70 weight %, special in squalane, and
-be no more than 20 weight %, preferably be no more than the water of 15 weight %,
And prerequisite is not contain the protein that forms agent as skeleton in the molding.
The molding that the present invention is used, for example above-mentioned composition preferably contains at least a nonprotein skeleton and forms agent, randomly contains one or more active component and the optional topical composition that contains one or more auxiliary agents, preferably has
-0.005g/cm
3To being no more than 0.8g/cm
3, preferred 0.01g/cm
3To being no more than 0.8g/cm
3Density,
-0.1cm
3To 6cm
3, preferred 0.8cm
3To 6cm
3Volume and
-the diameter of 6mm (maximum spacing of point-to-point transmission on the molding) at least.
The used molding of the present invention is the equally distributed porous molding of inclusions (do not consider may exist under some situation coating).
The rate of dissolution of the molding that the present invention is used is to utilize the testing equipment that meets the PharmEU regulation, measure according to " tablet and capsular disintegration time " method of testing, its rate of dissolution was preferably less than 4 minutes, was more preferably less than 1 minute (molding for the 9mm diameter is complete hydration to occur and do not have visible micronucleus in＜20 seconds).
Molding used among the present invention can make by the method that comprises following these steps:
(a) preparation contains at least a biopolymer, optional active component and optional solution or the suspension that contains one or more auxiliary agents that contains one or more physiologically actives,
(b) with solution-cast in mould,
(c) in mould frozen soln and
(d) lyophilizing forms molding through refrigerated solution.
Optionally also can between these steps, increase other steps, particularly can be after step c), carry out one and spray the process of handling the molding surface by machining or by using such as active ingredient solution, pigment solution and/or dissolution rate modifiers.But preferred molding does not have face coat, and is preferably homogeneous texture, this means each component same distribution on whole molding.
More reasonably be in process of production, at first make the aqueous solution that skeleton forms agent, and then optionally be added into and mix one or more active component or one or more auxiliary agents.
In order to give molding enough mechanical stabilities, just require solution or suspension to have certain density skeleton and form agent.This concentration depends on that naturally used skeleton forms the kind of agent.More rational concentration value is at least about 0.1 weight %, in the solution total amount, is preferably at least about 0.25 weight % to being no more than about 20 weight %, preferably less than 15 weight %, is more preferably less than 10 weight % (skeleton forms agent weight with respect to total solution weight).Concentration is high again to be not preferably then because otherwise solution viscosity can be too high and increase the difficulty of processing of solution therefrom.The content of the skeleton formation agent in solution or the suspension can have influence on the density (molding weight is with respect to the volume of molding geometry) of gained molding fatefully.When water or active ingredient solution and/or compounding agent solution carried out moistening, density value still was the variable of an important relevant rate of dissolution of moulding bodies.The concentration of skeleton formation agent is high more in the solution, and then the density of molding is also just high more, and vice versa.From density value/porosity or rate of dissolution angle, skeleton forms agent concentration in prepared solution or the suspension in step (a), should be preferably from about 0.25 weight % extremely in the scope of about 15 weight %.The concentration value that the preferred skeleton that uses forms the agent sodium alginate is preferably 0.5 to 5 weight %, more preferably 1 to 4 weight %.
The density of the molding that the present invention is used should be about 0.01g/cm more satisfactoryly
3To being no more than 0.8g/cm
3, be preferably about 0.015g/cm
3To being no more than 0.5g/cm
3, more preferably about 0.02g/cm
3To being no more than 0.1g/cm
3As above used term density is the molding gravimetric value with the stereometer of the external shape of molding.
The gravimetric value of each molding depends on its size naturally.Usually the weight of each molding is about 10 to 200mg, is preferably 20 to 100mg.For example, the 12mm diameter sphere has preferred 20 to 80mg weight, and more preferably 30 to 60mg.This corresponding preferable range is also arranged for other diameter sphere.
Experience freeze dried formulations prepared from solutions process and be preferably as follows and carry out, promptly at first prepare the solution that skeleton forms agent, and form to skeleton then and sneak into the active component or the auxiliary agent that can exist when suitable in the agent solution.If use oil-soluble active component, then preferably they are dissolved in the oil of using as auxiliary agent when suitable (particularly squalane), and then join skeleton and form in the solution of agent and go.The advantage of this preparation method is to form stable solution or suspension.Need not use emulsifying agent, and in the course of processing, and when using oil-soluble or oiliness auxiliary agent or active component, the phenomenon of phase separation of solution or suspension can not take place.
The solution-cast that will so make is in the mould that has corresponding to molding and cavity that have required geometry then.Mould is preferably by natural rubber, silicone rubber, vulcanite formations such as (natural gum).Preferably gummy mould.Also can carry out coating in the time of suitably to mold materials.The molding cavity that will inject solution has the shape of required molding usually.That is to say that the volume of cavity corresponds essentially to the volume of resulting molding thereafter.
Because when freezing, be packed into the solution of cavity or the volume of suspension and can increase (density variation between water and the ice), so can not fill up cavity fully usually.In this way just can obtain complete symmetric molding.For example in by the method that is added dropwise to degree of depth cooling solution (for example liquid nitrogen), then can't realize this point,, thereby make more or less deviation is always arranged with regular shape because what occur therein is asymmetrical Temperature Distribution.But the molding of these non-regular molding but is unfavorable in the end product of beauty treatment usefulness.Usually, this also will carry out follow-up machining according to the molding that drop-method makes to those with regard to meaning, and this is unnecessary in the method used according to the present invention.In the molding that makes according to drop-method, along with the increase of molding volume always more and more needs this following process, because what occur in the method is tangible irregular outward appearance, and this scrambling particularly has more intensive performance in big more molding.
After in the cavity that solution is packed into mould, frozen soln or suspension.The cooling of solution or freezing can carrying out with any means.Preferably in the used method of the present invention, cool off by advertising cold air.Some other method comprises, for example mould is immersed in the liquid gas, as is immersed in the liquid nitrogen.In this process, cooldown rate can influence the size of formed ice crystal.They can have influence on the pore-size distribution in the formed molding again.If form less megacryst, then molding has less macrovoid.If form many very little crystal, then molding also just has many very little holes.Crystal is more little, and then the cooldown rate of solution or suspension is also just high more.
Required cryogenic temperature especially depends on the severe degree that the active component that contains in the solution or auxiliary agent freezing point reduce.Temperature is below freezing to liquid nitrogen temperature (196 ℃) from water more satisfactoryly.Preferred cryogenic temperature is-20 to-80 ℃ approximately.After solution or suspension are freezing, just from mould, take out molding and also will carry out following process in some cases.The following process process can be carried out with mechanical means, for example by surface treatment (polishing, polishing etc.).Also can carry out coating in addition and handle, for example with the saline solution spray, in order to form the agent molding, particularly when using the saline solution of sodium alginate and polyvalent metal ion such as forming the littler skeleton of dissolubility.Also a kind of pigment solution can be coated on through refrigerated molding surface, in order to form colored molding.
Then molding is carried out lyophilizing.Freeze-drying process can carry out by known method, for example is documented in the method among DE4328329 C2 or DE 4028622 C2.
Come to set forth in more detail the present invention by the following examples.
Embodiment
Embodiment 1 (sodium alginate spheroid, diameter 12mm)
The basic model of having only alginate
2g Protanal LF 10/60 (sodium alginate)
98g water
Under stirring condition, the 2g sodium alginate added (2% solution w/w) in 98 water.Evenly (degassing) mixture is cast in the mould, advertise air carry out freezing, taking-up and then carry out lyophilizing from mould with known method.Obtain about 110 spheroids.
Embodiment 2 (spheroid, diameter 12mm)
Alginate and squalane
2g Protanal LF 10/60 (sodium alginate)
The 1g squalane
97g water
Under stirring condition, add in the 97g water 2g sodium alginate and mix homogeneously.Add the 1g squalane subsequently while stirring.Evenly (degassing) mixture is cast in the mould, advertise air carry out freezing, taking-up and then carry out lyophilizing from mould with known method.
Embodiment 3 (spheroid, diameter 9mm)
Alginate and squalane and glycerol
2.0g Protanal LF 10/60 (sodium alginate)
0.9g squalane
0.6g glycerol
96.5g water
Under stirring condition, the 2g sodium alginate is dissolved in the 96.5g water.Then under stirring condition, be added into the mixture that 0.9g squalane and 0.6g glycerol are formed.Evenly (degassing) mixture is cast in the mould, advertise air carry out freezing, taking-up and then carry out lyophilizing from mould with known method.
Embodiment 4:(spheroid, diameter 12mm)
Alginate and squalane and carbamide
2.0g Protanal LF 10/60 (sodium alginate)
1.0g squalane
1.0g carbamide
96.0g water
Under stirring condition, 2g sodium alginate and 1.0g carbamide are dissolved in the 96.0g water.Then under stirring condition, be added into the squalane of 1.0g.Evenly (degassing) mixture is cast in the mould, advertise air carry out freezing, taking-up and then carry out lyophilizing from mould with known method.
Embodiment 5:(spheroid, diameter 12mm)
Alginate and squalane and ceramide
2.0g Protanal LF 10/60 (sodium alginate)
1.5g squalane
0.01g ceramide
96.4g water
Under stirring condition, the 2g sodium alginate is dissolved in the 96.4g water.Then under stirring condition, be added into the mixture that 1.5g squalane and 0.01g ceramide are formed.Evenly (degassing) mixture is cast in the mould, advertise air carry out freezing, taking-up and then carry out lyophilizing from mould with known method.
Claims (14)
1. contain the purposes that at least a nonprotein skeleton forms agent, the molding that randomly contains one or more active component and randomly contain one or more auxiliary agents is used for external.
2. the purposes of claim 1 is used for outside beauty treatment.
3. the purposes of claim 1 is used for external treatment.
4. each purposes in the claim 1 to 3, it is a kind of polysaccharide or derivatives thereof at least that skeleton wherein forms agent.
5. each purposes in the claim 1 to 4, it is sodium alginate that skeleton wherein forms agent.
6. each purposes in the claim 1 to 5, wherein molding has 0.1cm
3To 6cm
3Volume and spheric geometry.
7. each purposes in the claim 1 to 6 wherein obtains containing the molding that at least a nonprotein skeleton forms agent, randomly contains one or more active component and randomly contain one or more auxiliary agents by lyophilizing through the solution or the dispersion liquid of freezing mistake.
8. the purposes of claim 7, molding wherein can make by the method that includes following steps:
(a) prepare solution or the suspension that contains at least a biopolymer, randomly contains the active component of one or more physiologically actives and randomly contain one or more auxiliary agents,
(b) with solution-cast in mould,
(c) in mould frozen soln and
(d) lyophilizing forms molding through refrigerated solution.
9. the purposes of each molding in the claim 1 to 8, wherein, the external of molding is directly undertaken by the end user.
10. the purposes of each molding in the claim 1 to 8 wherein, thereby wants the aqueous solution moistening molding of water or one or more active component and/or auxiliary agent to form gel, and on paint skin or the hair.
11. molding, it contains:
One or more skeletons of-at least 10 weight % form agent, and the aqueous solution of its 1 weight % or the suspension that forms in water have the viscosity less than 2000mPas under the condition of 20 ℃ and pH6-8,
One or more active component of-0.000001 weight % to 50 weight %,
One or more auxiliary agents of-0.1 weight % to 70 weight %, and
-be no more than the water of 20 weight %,
And prerequisite is not contain the protein that forms agent as skeleton in the molding.
12. the molding of claim 11, it is sodium alginate that skeleton wherein forms agent.
13. preferably as claim 11 or the 12 described moldings that are used for external that contain at least a nonprotein skeleton formation agent, randomly contain one or more active component and randomly contain one or more auxiliary agents, it has:
-0.01g/cm
3To 0.8g/cm
3Density,
-0.1cm
3To 6cm
3Volume and
-the diameter of 6mm (maximum spacing of point-to-point transmission on the molding) at least.
14. assembly contains each defined molding and at least a aqueous solution that contains one or more active component and/or auxiliary agent at least a claim 1 to 13, and is whole spatial organization form.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE2002148314 DE10248314A1 (en) | 2002-10-16 | 2002-10-16 | Use of a molded body comprising a nonprotein gelling agent for external application, especially cosmetic or therapeutic |
| DE10248314.0 | 2002-10-16 | ||
| DE10317982.8 | 2003-04-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1728986A true CN1728986A (en) | 2006-02-01 |
Family
ID=32049334
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 03824235 Pending CN1728986A (en) | 2002-10-16 | 2003-09-30 | Use of molded bodies for external application |
Country Status (2)
| Country | Link |
|---|---|
| CN (1) | CN1728986A (en) |
| DE (1) | DE10248314A1 (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101904813A (en) * | 2009-04-22 | 2010-12-08 | 苏维拉克皮肤及健康护理公司 | Freeze-dried coated mechanograph |
| CN112842931A (en) * | 2021-02-04 | 2021-05-28 | 甘肃天际生物科技有限公司 | Animal collagen freeze-dried ball, cosmetic set and preparation process |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2386616T3 (en) | 2009-04-22 | 2012-08-23 | Dr. Suwelack Skin & Health Care Ag | Lyophilized molded body containing magnesium ascorbyl phosphate |
| JP6113944B2 (en) | 2009-04-22 | 2017-04-12 | メドスキン ソリューションズ ドクター ズベラック アーゲーＭｅｄＳｋｉｎ Ｓｏｌｕｔｉｏｎｓ Ｄｒ．Ｓｕｗｅｌａｃｋ ＡＧ | Freeze-dried molded product, production method thereof, and use thereof |
| WO2024182500A1 (en) * | 2023-02-28 | 2024-09-06 | Onelogy Inc. | Dried cosmetic preparation for rehydration and use |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4695463A (en) * | 1985-05-24 | 1987-09-22 | Warner-Lambert Company | Delivery system for active ingredients and preparation thereof |
| IT1219942B (en) * | 1988-05-13 | 1990-05-24 | Fidia Farmaceutici | POLYSACCHARIDIC ESTERS |
| FR2647343B1 (en) * | 1989-05-24 | 1994-05-06 | Rhone Poulenc Sante | NOVEL POROUS PHARMACEUTICAL FORM AND ITS PREPARATION |
| JP2865320B2 (en) * | 1989-08-07 | 1999-03-08 | 株式会社資生堂 | Solid cosmetic composition |
| FR2706246B1 (en) * | 1993-06-11 | 1995-11-17 | Raymond Bontemps | Process for the manufacture and preservation of fresh vegetable cosmetic substances free of preservative and applied in the frozen state. |
| DE19911041A1 (en) * | 1999-03-12 | 2000-09-14 | Henkel Kgaa | Flexible and absorbent carriers for treating the skin equipped with nanoparticle dispersions |
| DE19920557B4 (en) * | 1999-05-05 | 2004-09-09 | Biotec Asa | Process for the production of collagen-free cosmetic preparations |
| GB0000677D0 (en) * | 2000-01-12 | 2000-03-08 | Lush Limited | Cosmetic product |
| FR2806300B1 (en) * | 2000-03-16 | 2002-05-03 | Oreal | COSMETIC COMPOSITION IN THE FORM OF A SOLID AQUEOUS GEL, COMPRISING A POLYVINYL ALCOHOL AND PROCESS FOR PREPARING THIS COMPOSITION |
| FR2808195B1 (en) * | 2000-04-28 | 2006-12-08 | Lyophilisation Alimentaire | LYOPHILIZED COSMETIC OR DERMATOLOGICAL PATCH |
-
2002
- 2002-10-16 DE DE2002148314 patent/DE10248314A1/en not_active Withdrawn
-
2003
- 2003-09-30 CN CN 03824235 patent/CN1728986A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101904813A (en) * | 2009-04-22 | 2010-12-08 | 苏维拉克皮肤及健康护理公司 | Freeze-dried coated mechanograph |
| CN112842931A (en) * | 2021-02-04 | 2021-05-28 | 甘肃天际生物科技有限公司 | Animal collagen freeze-dried ball, cosmetic set and preparation process |
Also Published As
| Publication number | Publication date |
|---|---|
| DE10248314A1 (en) | 2004-04-29 |
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