KR20110101097A - Percutaneously absorbable medicine comprising vitamin - Google Patents

Percutaneously absorbable medicine comprising vitamin Download PDF

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KR20110101097A
KR20110101097A KR1020110019838A KR20110019838A KR20110101097A KR 20110101097 A KR20110101097 A KR 20110101097A KR 1020110019838 A KR1020110019838 A KR 1020110019838A KR 20110019838 A KR20110019838 A KR 20110019838A KR 20110101097 A KR20110101097 A KR 20110101097A
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transdermal absorption
drug
vitamin
transdermal
present
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KR1020110019838A
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Korean (ko)
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김철준
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주식회사 티디에스팜
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/70Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7023Transdermal patches and similar drug-containing composite devices, e.g. cataplasms

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  • Dermatology (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Life Sciences & Earth Sciences (AREA)
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  • General Health & Medical Sciences (AREA)
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Abstract

The present invention comprises a drug-containing layer, a drug-containing layer and a peeling layer containing a transdermal absorption composition containing 0.01 to 25 parts by weight of vitamins, wherein the transdermal absorption composition is a transdermal absorption accelerator, a polymer, a drug promoting agent, a moisturizing agent and a pH. The present invention relates to a vitamin transdermal absorption agent further comprising at least one member selected from the group consisting of modulators, wherein the transdermal absorption agent according to the present invention is excellent in rapid expression of drug efficacy, skin permeability, and long-term sustainability of the drug. Because of low skin irritation, vitamins can be safely delivered to the body without any side effects even after long-term use, which is particularly useful for the treatment of children and the elderly who have difficulty in oral administration.

Description

Percutaneously Absorbable Medicine Comprising Vitamin

The present invention relates to a vitamin transdermal absorption preparation, more specifically, it is possible to express a quick effect, excellent skin permeability and long-term persistence of the drug, low skin irritation such as erythema, edema, vitamins without any side effects even during long-term use The present invention relates to a vitamin transdermal absorption preparation that can be safely delivered to the body, which can be particularly useful for elderly patients who can release the drug 24 hours and have difficulty in oral administration.

The present invention relates to a therapeutic transdermal absorption composition comprising a vitamin, more preferably including a vitamin and further comprising at least one selected from the group consisting of a transdermal absorption accelerator, a polymer, a drug enhancer, a humectant and a pH adjuster. will be.

The present invention also relates to a transdermal absorption preparation comprising a drug protective layer, a drug-containing layer and a release layer including the transdermal absorption composition.

Here, vitamins are not the main nutrients of life, but are generic terms of organic compounds that are indispensable for maintaining normal development and nutrition of life.

(1) Nutritional side: Plants that are autotrophic don't need to be supplied externally because they synthesize their own vitamins, but they often require vitamins in tissue cultures that culture cut tissues or cells. The two vitamins have been used in many cultures since J. Bonner discovered that thiamin and pyridoxine are essential for growth and that nicotinic acid promotes growth in the cultivation of cut muscles of sunflower. In callus culture, thiamine-HCl, pyridoxine-HCl, and nicotinic acid are often used at concentrations of 0.1-1 mg / L, respectively. However, callus, such as the tropical tree Bauhinia blakeana (a type of Hongkong Orchard tree), uses 40 mg / L thiamine-HCl. In the growth point of coffee, high concentration vitamins such as thiamine 30μM, pyridoxine 15μM and nicotinic acid 15μM are used. Thiamine may have a green effect of callus, and is considered to be an important ingredient to be added to the medium along with cytokinin in the callus of callus. The administration of vitamins is important in cultivation or self-cultivation, and is often used for fertility cultures. In poppy cultures, an example of obtaining normal mature seeds by administering 0.25 mg / L of thiamine, 0.25 mg / L of pyridoxine, 1.25 mg / L of nicotinic acid, and 0.25 mg / L of calcium pantothenate is known.

(2) Functional side: It is a group of organic compounds that the organisms need in order to perform their normal physiological function, but they can't biosynthesize by themselves and must be consumed as nutrients from other natural products. Animals are usually made of substances other than proteins, carbohydrates, fats and minerals. The history of vitamins begins with the record of chewing the leaves of spruce for the treatment of scurvy, and in the 17th century, ocean and marine boats were already loaded with oranges and lemons to prevent scurvy. Initial research has been successful in improving the diet and treating it with water or alcohol extract of rice bran. However, it was only in the twentieth century that each thought to be a deficiency of certain substances and continued to apply to scurvy and rickets. Thus, finding vitamin B1, C, and other foods that were inadequate food intake caused the disease, named D ~ H, physiological action K, P, etc. in the order of discovery. Vitamins are largely divided into water-soluble vitamins (vitamin B group, choline, inositol, ascorbic acid) and fat-soluble vitamins (vitamins A, D, E, K). Currently, all of them have been separated, and the chemical structure has been determined, so that in addition to the conventional alphabetical naming, a unique name combining the function and chemical structure is given. Also, vitamins are not amines, so they are called vitamins by eliminating their mother's e. In general, microorganisms and plants do not need to be supplied externally because they synthesize vitamins by themselves, but bacteria or fungi that cannot be autotrophized require various vitamins, and each type is species-specific, so it is widely used for biological quantification of vitamins. It is becoming. Qualitative and quantitative methods include chemical or physicochemical methods and biological quantification methods.

These vitamins have been ingested only by injection or oral until now, but have not been developed as a transdermal absorbent. Percutaneous absorption formulations have the advantage of being less likely to develop side effects than injections or oral medications to be applied to the skin and can be conveniently used by patients.

Thus, the present inventors completed the present invention after confirming that the effect is not only rapidly expressed after administration of the transdermal absorbent containing vitamins, but also shows sustained skin permeability and almost no skin irritation.

An object of the present invention devised to solve the above problems is to provide a vitamin transdermal absorption preparation capable of rapid effect expression, excellent skin permeability and long-term sustainability of the drug.

In addition, another object of the present invention is low skin irritation, such as erythema, edema can be delivered safely to the body without any side effects even after long-term use, particularly useful for elderly patients who can release the drug 24 hours and difficult oral administration To provide a vitamin transdermal absorption preparation that can be used.

According to a feature of the present invention for achieving the object as described above, the present invention comprises a drug protective layer, a drug containing layer and a release layer containing a transdermal absorption composition containing 0.01 to 25 parts by weight of vitamins, the transdermal Absorption composition is characterized in that it further comprises one or more selected from the group consisting of transdermal absorption accelerators, polymers, drug enhancers, moisturizers and pH adjusting agents.

In addition, the transdermal absorption accelerator is characterized in that at least one selected from the group consisting of hydrocarbons, alcohols, fatty acids, esters, amides, surfactants, terpenes, urea and azone.

In addition, the content of the percutaneous absorption accelerator is characterized in that 0.1 to 30 parts by weight.

In addition, the polymer may be gelatin, hyaluronic acid or salts thereof, collagen, residue rubber, acacia rubber, collapsing rubber, carrageic acid, arginic acid, sodium arginate, agar, gum arabic, toragan rubber, karaya rubber, pectin, starch, Methylcellulose, ethylcellulose, hydroxyethylcellulose, sodium carboxymethylcellulose, soluble starch, carboxymethyl starch, dialdehyde starch, polyvinyl alcohol, polyvinylpyrrolidone, polyvinylacrylate, polyacrylic acid, sodium polyacrylate, polyethylene Oxide, polyacrylic acid copolymer, methyl acrylate--2-ethylhexyl copolymer, methyl vinyl ether-maleic anhydride copolymer, and isobutylene-maleic anhydride copolymer.

In addition, the content of the polymer is characterized in that 0.5 to 50 parts by weight.

In addition, the moisturizing agent is characterized in that at least one member selected from the group consisting of glycerin, propylene glycol, sorbitol, ethylene glycol, diethylene glycol, polyethylene glycol, polypropylene glycol and butylene glycol.

As described above, the present invention enables rapid effect expression and is excellent in long-term persistence of skin permeability and efficacy.

In addition, the skin irritation such as erythema, edema can be delivered to the body safely without any side effects even after long-term use, it can be used particularly useful for elderly patients who can release the drug 24 hours and difficult to oral administration.

1 is a graph showing the skin permeation rate of vitamins from the transdermal absorption preparations according to Examples 1 to 5 of the present invention in hairless mouse skin.
Figure 2 is a graph showing the absorbance over time of vitamins from transdermal absorbents using high performance liquid chromatography according to Examples 1 to 5 of the present invention in hairless mouse skin.
FIG. 3 is a graph showing the change between the concentration and the absorbance shown in FIGS. 1 and 2.

Specific details of other embodiments are included in the detailed description and the drawings.

Advantages and features of the present invention and methods for achieving them will be apparent with reference to the embodiments described below in detail with the accompanying drawings. However, the present invention is not limited to the embodiments disclosed below, but can be implemented in various different forms, and only the embodiments make the disclosure of the present invention complete, and the general knowledge in the art to which the present invention belongs. It is provided to fully inform the person having the scope of the invention, which is defined only by the scope of the claims. Like reference numerals refer to like elements throughout the specification.

Hereinafter, the vitamin transdermal absorption preparation according to the embodiments of the present invention.

The present invention relates to a therapeutic transdermal absorption composition comprising a vitamin.

Preferably, the transdermal absorption composition may further include one or more selected from the group consisting of transdermal absorption accelerators, polymers, drug enhancers, moisturizers and pH adjusters.

The present invention also relates to a transdermal absorption preparation comprising a drug protective layer, a drug-containing layer comprising the composition for transdermal absorption, and a release layer.

Hereinafter, the present invention will be described in detail.

The transdermal absorption composition of the present invention contains a vitamin as an active ingredient.

In the composition of the present invention, the content of vitamin preferably contains 0.01 to 25 parts by weight, more preferably 3 to 20 parts by weight. Such a compounding ratio is preferable in view of maintaining the skin permeability of the drug, the sustainability of the drug and the stability of the drug, etc., and economically excellent vitamin-containing transdermal absorption preparations. Here, when the blending amount of the vitamin is less than 0.01 parts by weight, sufficient drug efficacy cannot be obtained. When the blending amount exceeds 25 parts by weight, problems such as crystal precipitation and reduction of adhesion of the drug may occur.

Preferably, the transdermal absorption composition may further include one or more selected from the group consisting of transdermal absorption accelerators, polymers, drug enhancers, moisturizers and pH adjusters.

The percutaneous absorption promoting agent functions to help the percutaneous absorption of the vitamin. Percutaneous absorption accelerators should not be irritating to the skin, should be fast and reversible in their absorption promoting effect, and should selectively promote only the permeation of the desired drug and should not affect the permeation of other substances or loss of substance in the body.

In the present invention, as a transdermal absorption accelerator, a general kind used in transdermal absorption preparations can be used, and preferably, hydrocarbons (eg, alkanes, alkenes, etc.), alcohols (eg, alkanols, alkenols, ethanol, etc.) Polyalcohols, glycols such as polyethylene glycol, propylene glycol, etc.), fatty acids (e.g. lauric acid, oleic acid, stearic acid, etc.), esters (e.g. dibutyl adipate, isopropyl myristate, glyceryl monolaurate, etc.) , Amides (eg 2-pyrrolidone, etc.), surfactants (eg Tween 20), terpenes (eg menthol, eucalyptol, etc.), urea and azone. More preferably polyethylene glycol, propylene glycol, lauric acid, stearic acid, oleic acid, dibutyl adipate, isopropyl myristate, glyceryl monolaurate, dimethylsulfuroxide, pyrrolidone, tween, ethanol, menthol and eucal At least one selected from the group consisting of liptol may be used as a transdermal absorption accelerator.

Such absorption accelerators promote skin permeation through various mechanisms. For example, in the case of surfactants, it is known to modify proteins by interacting with the stratum corneum. This effect is more effective for polar drugs because surfactants work strongly with substances in protein components of the intracellular pathway called keratin.

Cationic polymer absorption accelerators include dialkylamino groups such as dimethylaminoethyl acrylate (DMAEA), dimethylaminoethyl methacrylate (DMAEMA), and dimethylaminomino acrylamide (DMAPMAAm). Monomers; Styrene monomers having dialkylamino groups such as dimethylaminonostyrene (DMASt) and dimethylaminoethyl styrene (DMAMSt); Homopolymers or copolymers composed of monomers having a vinylpyrrolidone group such as 4-vinylpyrrolidone, 2-vinylpyrrolidone, etc. It is preferable to use.

Substances such as oleic acid and azone act on the fat component of the stratum corneum, increasing fluidity and thus increasing the absorption of the drug.

In the transdermal absorption composition of the present invention, the preferred content of the transdermal absorption accelerator is 0.1 to 30 parts by weight. Herein, when the content of the percutaneous absorption accelerator is less than 0.1 part by weight, it is difficult to properly exhibit the absorption promoting effect and the constant drug release property of the active ingredient vitamin, and when it exceeds 30 parts by weight, the drug is caused by the interaction between the percutaneous absorption accelerator and the vitamin. There is a fear that the release of and the adhesiveness of the increase in content is feared is not preferred.

The polymer is preferably gelatin, hyaluronic acid or salts thereof, collagen, residue rubber, acacia rubber, collapsing rubber, carrageic acid, arginic acid, sodium arginate, agar, gum arabic, toragan rubber, karaya rubber, pectin, starch , Methylcellulose, ethylcellulose, hydroxyethylcellulose, sodium carboxymethylcellulose, soluble starch, carboxymethyl starch, dialdehyde starch, polyvinyl alcohol, polyvinylpyrrolidone, polyvinylacrylate, polyacrylic acid, sodium polyacrylate, And at least one member selected from the group consisting of polyethylene oxide, polyacrylic acid copolymer, methyl acrylate--2-ethylhexyl copolymer, methylvinyl ether-maleic anhydride copolymer, and isobutylene-maleic anhydride copolymer. The polymer is preferred because it is easier to use and less irritant to the skin than a polymer such as polyisobutylene, which is used by melting in a solvent such as toluene when preparing a transdermal absorbent.

In addition, acrylate polymer, polyisobutylene, polyisoprene, styrene-isoprene-butadiene copolymer, styrene-butadiene copolymer One selected from the group consisting of rubber polymers such as copolymers or silicone polymers of polydimethylsiloxane is used.

More preferably, at least one selected from the group consisting of gelatin, polyvinyl alcohol, sodium polyacrylate, and sodium carboxycellulose may be used as the polymer.

The preferred content of the polymer in the transdermal absorption composition is 0.5 to 50 parts by weight, the polymer within this range can effectively exhibit the function of maintaining the water content and improving stability, adhesion to the skin.

The drug enhancer is preferably one or more selected from the group consisting of natural sulfur, cactus extract, peppermint oil, lavender, rosemary and sage. These drug enhancers play a role in enhancing the efficacy of vitamins. In the present transdermal absorption composition, the preferred amount of the drug enhancer is 0.1 to 10 parts by weight.

Peppermint (Menthol) is a perennial herb with Lamiaceae, and is known to have an allergic, analgesic and antiseptic effect. Peppermint is steam distilled after cutting the stems for 1 year and 3 times in autumn, before flowering. 70-90% of the essential oils thus obtained are menthol components, specifically, L-menthol, iso-mentone, pinene, camphor, limonene, and the like, and other components include vitamin C, carotene, phytol, betaine, and the like. May be included.

Natural sulfur (MSM) prevents the loss of moisture in skin tissue and maintains the skin's elasticity. In addition, it is known to detoxify harmful substances deposited on skin tissue, and mineral sulfur has been frequently used as a treatment for skin diseases since ancient times. In addition, it is effective in chronic joint diseases caused by abnormal sulfur metabolism in cartilage and muscle, and anti-allergic action is also recognized. Drinking promotes flow in the intestine, eliminating constipation and helping bile to improve liver function.

Lavender is a perennial plant belonging to the Lamiaceae family, which is native to the Mediterranean Sea, Southern Europe, Central Europe, India, and South France. The name Lavendula L. Lavenda is known to help calm the mind, induce sleep, and help with insomnia and headaches. In addition, it is effective for sunburn and skin improvement and sterilization, soothing, analgesic, insect repellent, as well as to relax the mind helps sleep and calms the mind.

Rosemary is a perennial evergreen tree that is resistant to cold (-5 ~ 0 ℃), antibacterial, bactericidal, disinfecting, memory enhancement, elimination of lethargy, headache, fatigue, anti-aging, dandruff suppression, eye cleaning It is known to have effects, tablets, analgesic, and insect repellent.

Sage uses varieties such as Clary Sage, Tricolor Sage, Golden Variegated Sage, Pineapple Sage and Purple Sage. For medicinal purposes, the leaves are boiled and used for sore throat and gastroenteritis. It has antiseptic and antiseptic effect such as antiseptic, antibacterial and anti-inflammatory. It is also used as an anti-inflammatory agent for inflammation. It also washes away fatigue after a stroke or heavy exercise.

The moisturizing agent is preferably one or more selected from the group consisting of glycerin, propylene glycol, sorbitol, ethylene glycol, diethylene glycol, polyethylene glycol, polypropylene glycol and butylene glycol. The moisturizing agent contributes to maintaining the proper wet state of the transdermal absorption composition of the present invention and improving the volatilization of water. In the present transdermal absorption composition, the preferred amount of the humectant is 0.1 to 40 parts by weight.

As the pH adjusting agent, at least one selected from the group consisting of citric acid, tartaric acid, acetic acid, malic acid, succinic acid, tartaric acid, triethanolamine, diisopropanolamine and diethanolamine is used, and the pH of the transdermal absorption composition is used. It is preferable to adjust to 4-8, Preferably 4.5-7, More preferably, it is the range of 5-6.5. In this pH range, it is possible to alleviate skin irritation, to release the drug from the preparation, to improve the absorption of the percutaneous and the stability of the preparation or to maintain the stickiness, and the content of the pH adjuster is suitably used depending on the pH concentration. The content of the pH adjuster in the present transdermal absorption composition is 0.1 to 10 parts by weight.

Percutaneous absorption preparations containing the vitamin of the present invention may include a drug protective layer, a drug-containing layer comprising the composition for transdermal absorption, and a release layer.

The drug protective layer is an impermeable layer that is applied to prevent the loss of drugs and additives in the drug-containing layer and the drug-containing layer, and is thin and flexible to prevent the drug from being lost from the preparation during attachment or storage to the skin. Do not cause allergic reaction because of no reactivity. As the drug protection layer, a single layer film such as polyester, polyurethane, polyethylene, polypropylene, polyolefin, polyethylene terephthalate, aluminum treated polyester, or a non-woven fabric, cotton cloth, fabric, etc. having water absorption ability is laminated on the single layer film. A multilayer laminate film or the like can be used, and any of drug-protective films used in conventional transdermal absorption preparations may be used.

The drug-containing layer is a layer containing a composition for transdermal absorption containing the above-mentioned vitamins, more preferably containing vitamins and as an auxiliary component for enhancing skin penetration or medicinal benefits of the above-mentioned transdermal absorption accelerator, polymer It further comprises one or more selected from the group consisting of medicament enhancers, humectants and pH adjusters. As a support body of a drug containing layer, the nonwoven fabric and film used by the conventional percutaneous absorption preparation are used.

The release layer is attached to the skin-adhesive side of the drug-containing layer until the formulation is applied to the skin to protect the drug and additives in the drug-containing layer and to support the formulation, to remove when the product is applied to the skin, conventional transdermal Films such as polystyrene, polyester, polyethylene, polypropylene, aluminum and cellulose used in the absorbent may be used, and these films may be laminated as necessary. In addition, it is preferable to use what remove | eliminates the debris of a matrix, and does not remain in a peeling layer easily when a peeling layer removes a peeling layer from a formulation, You may use what kind of substance or form normally used for transdermal absorption preparations.

The preparation method of the transdermal absorbent preparation containing the vitamin of the present invention is as follows.

The polymer is mixed and dispersed with purified water and a moisturizing agent as necessary, and then pH adjusters and other additives are added as necessary to make a uniform mixture to make A solution. If necessary, the vitamin is uniformly mixed with the transdermal absorption accelerator to make B solution, and then mixed with stirring B solution in A solution to prepare a drug-containing layer having increased adhesiveness over time. The prepared drug-containing layer is coated on the drug protection film with a coater, and a peeling film is attached thereon to prepare a transdermal absorption preparation of the present invention.

The transdermal absorbent of the present invention may be formulated in conventional transdermal formulations such as patches, cataplasmases, platases and the like, preferably in the intermediate form between cataplasmas and patches, the general composition of which is based on cataplasmases. However, the amount and thickness of the coating is prepared in a similar manner to the patch, and the formulation improves the convenience and skin friendliness, and variety of adhesion when used.

The preferred area of the transdermal absorbent preparation of the present invention is 5 to 140 cm, the preferred weight is 5 to 30 g, and it is preferable to adhere to the affected part once or twice a day.

The transdermal absorption preparations containing the vitamin of the present invention can express a quick effect by the combination of the optimal transdermal absorption promoting agent to enhance the skin penetration of the vitamin, and excellent skin permeability and long-term sustainability of the drug. In addition, the skin is composed of components with excellent skin compatibility, less skin side effects such as erythema, edema, and can deliver vitamins safely to the body even after long-term use. Therefore, the percutaneous absorption preparation of the present invention can be used particularly useful in elderly patients who are difficult to oral administration because the drug can be released for 24 hours.

Such a present invention will be described in more detail based on the following Examples and Test Examples, but the present invention is not limited thereto.

The following examples and test examples use vitamin B6.

Examples 1-5

1.75 g of polymer gelatin, 0.88 g of polyvinyl alcohol, 4.1 g of sodium polyacrylate, 2.25 g of sodium carboxycellulose, 4 g of kaolin as excipient, 18.5 g of concentrated glycerin as moisturizer and 17.14 g of D-sorbitol solution in 50.5 g of purified water It was. Thereafter, 0.88 g of tartaric acid was added as a pH adjuster to prepare a uniform mixture.

1.5 g of vitamin B6 was uniformly mixed and stirred with the percutaneous absorption accelerators listed in Table 1 below.

A mixture of vitamin B6 and a transdermal absorption accelerator in the above prepared mixture was mixed while stirring to prepare a transdermal absorption composition of the present invention.

The prepared composition was coated on the drug protection film with a coater and a peeling film was attached thereon to prepare a transdermal absorbent preparation of the present invention.

Using the same composition and method as described above, the percutaneous absorption preparations of Examples 1 to 5 were prepared by only changing the type and content of the percutaneous absorption promoting agent described in Table 1 below.

                                                              (Unit: g) Percutaneous absorption accelerator Example 1 Example 2 Example 3 Example 4 Example 5 Polyethylene glycol 0.8 Lauryl acid 1.2 Isopropyl myristate 2.7 N-methylpyrrolidone 3.2 Dimethylsulfooxide 4.3

Test Example 1

In order to determine the skin permeability of the vitamin-containing transdermal absorbent preparations prepared in Examples 1 to 5, the skin of a hairless mouse and Franz diffusion cell (effective area: 4 cm 2, volume of the acceptor: 11 ml) were used. Skin permeation test was performed under sink condition.

The receptor phase was filled with Franz Diffusion Cell using phosphate buffer pH5.8 (sigma), maintained at 37 ± 0.5 ° C., followed by mounting the skin and applying the transdermal absorbent to the epidermal layer of the skin. The permeation test was carried out by adhesion. The skin was removed from the 4 week-old hairless rat, and then the skin layer was removed, and the fat layer of the dermal layer was used. After the skin was mounted on the diffusion device, the aqueous phase was stirred at 600 rpm using a magnetic stirrer during the experiment.

After a certain period of time after application to quantify the drug permeated, 1 ml of the aqueous phase was taken to perform high performance liquid chromatography (HPLC), and the Franz diffusion cell was again filled with the aqueous phase. High performance liquid chromatography installed a Capsel Pack C8 (size 4.6 * 250mm, H 2 O) column in the HPLC column holder, set the flow rate to 600 μl / min, the UV detector wavelength to 195 nm, and the elution solvent was acetonitrile: phosphoric acid. Buffer = 40: 60 was carried out using a mixed solvent. Phosphate buffer solution was prepared to pH 1.5 with potassium phosphate 0.01M and phosphate mixed solution. 10 μl of the sample was injected, and the column temperature was operated at 35 ° C. and the HPLC system was quantitatively analyzed. The results are shown in Table 2 and FIG. 1.

Example 1 Example 2 Example 3 Example 4 Example 5 15min 0.3398 0.4684 0.6932 0.4471 0.4168 30min 0.8216 1.1969 1.5942 1.0495 1.1030 45min 1.3979 2.1261 2.6056 1.8921 2.0220 60min 1.9852 3.1258 3.7477 2.8119 3.0216 120 min 2.7360 4.5005 5.2855 4.3003 4.7515 180 min 3.5025 5.9740 6.8101 5.9044 6.4626 240min 4.2747 7.4019 8.3550 7.6025 8.2638 300min 4.9664 8.9297 9.4759 9.1791 9.8650

Absorbance values with time by the high performance liquid chromatography (HPLC) are shown in Table 3 and FIG. 2 below.

Example 1 Example 2 Example 3 Example 4 Example 5 15min 3259 4476 6603 4274 3987 30min 4602 6937 8570 5744 6538 45min 5497 8837 9615 8018 8740 60min 5601 9504 10852 8748 9503 120 min 7149 13054 14597 14129 16415 180 min 7297 13988 14472 15225 16238 240min 7351 13557 14665 16114 17090

From Table 2 and Figure 1, after about 15, 30, 45, 60 minutes after the start of the experiment showed about about 3mg of vitamin B6 skin permeation, after that vitamin B6 per 1 to 2mg per hour was continuously permeated skin You can check it. That is, according to the loading dose of vitamin B6, the skin permeation amount was initially increased, and as time passed, the skin permeation amount was decreased, but the permeation amount was constant up to 5 hours.

In conclusion, the results of skin permeation experiments showed that all of the mouse skin followed the Higuchi diffusion equation, and the average amount of permeation up to the first hour was about 3mg, which was more than twice the hourly per hour after 1 hour.

In addition, referring to FIG. 3, a change between concentration and absorbance can be seen.

Those skilled in the art will appreciate that the present invention can be embodied in other specific forms without changing the technical spirit or essential features of the present invention. Therefore, it should be understood that the embodiments described above are exemplary in all respects and not restrictive. The scope of the present invention is indicated by the scope of the following claims rather than the detailed description, and all changes or modifications derived from the meaning and scope of the claims and the equivalent concept are included in the scope of the present invention. Should be interpreted.

Claims (6)

A drug protective layer, a drug containing layer and a release layer containing a transdermal absorption composition containing 0.01 to 25 parts by weight of a vitamin,
The transdermal absorption composition is a transdermal absorption accelerator, characterized in that it further comprises at least one selected from the group consisting of a transdermal absorption accelerator, a polymer, a drug enhancer, a moisturizer and a pH adjuster.
The method of claim 1,
The percutaneous absorption accelerator is a vitamin transdermal absorption agent, characterized in that at least one selected from the group consisting of hydrocarbons, alcohols, fatty acids, esters, amides, surfactants, terpenes, urea and azone.
The method of claim 1,
The percutaneous absorption accelerator is a vitamin transdermal absorption agent, characterized in that 0.1 to 30 parts by weight.
The method of claim 1,
The polymer is gelatin, hyaluronic acid or salts thereof, collagen, residue rubber, acacia rubber, collapsing rubber, carrageic acid, arginic acid, sodium arginate, agar, gum arabic, toragan rubber, karaya rubber, pectin, starch, methylcellulose , Ethylcellulose, hydroxyethylcellulose, sodium carboxymethylcellulose, soluble starch, carboxymethyl starch, dialdehyde starch, polyvinyl alcohol, polyvinylpyrrolidone, polyvinylacrylate, polyacrylic acid, sodium polyacrylate, polyethylene oxide, Percutaneous absorption of vitamins, characterized in that at least one member selected from the group consisting of polyacrylic acid copolymer, methyl acrylate--2-ethylhexyl copolymer, methyl vinyl ether-maleic anhydride copolymer and isobutylene-maleic anhydride copolymer Formulation.
The method of claim 1,
The content of the polymer is a vitamin transdermal absorption agent, characterized in that 0.5 to 50 parts by weight.
The method of claim 1,
The moisturizing agent is a vitamin transdermal absorbent, characterized in that at least one selected from the group consisting of glycerin, propylene glycol, sorbitol, ethylene glycol, diethylene glycol, polyethylene glycol, polypropylene glycol and butylene glycol.






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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20160144107A (en) * 2015-06-08 2016-12-16 오석태 Food-skin patch including nutrient for absorbing into skin

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Publication number Priority date Publication date Assignee Title
KR20160144107A (en) * 2015-06-08 2016-12-16 오석태 Food-skin patch including nutrient for absorbing into skin

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