KR20170032800A - Soluble microneedle patch for treatment of hepatitis C - Google Patents
Soluble microneedle patch for treatment of hepatitis C Download PDFInfo
- Publication number
- KR20170032800A KR20170032800A KR1020150164916A KR20150164916A KR20170032800A KR 20170032800 A KR20170032800 A KR 20170032800A KR 1020150164916 A KR1020150164916 A KR 1020150164916A KR 20150164916 A KR20150164916 A KR 20150164916A KR 20170032800 A KR20170032800 A KR 20170032800A
- Authority
- KR
- South Korea
- Prior art keywords
- hepatitis
- therapeutic agent
- microneedle
- skin
- microneedles
- Prior art date
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Classifications
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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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
-
- 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
- A61K9/0021—Intradermal administration, e.g. through microneedle arrays, needleless injectors
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61L—METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
- A61L26/00—Chemical aspects of, or use of materials for, wound dressings or bandages in liquid, gel or powder form
- A61L26/0061—Use of materials characterised by their function or physical properties
- A61L26/0066—Medicaments; Biocides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
- A61M37/00—Other apparatus for introducing media into the body; Percutany, i.e. introducing medicines into the body by diffusion through the skin
- A61M37/0015—Other apparatus for introducing media into the body; Percutany, i.e. introducing medicines into the body by diffusion through the skin by using microneedles
Abstract
The present invention relates to a skin administration system for a hepatitis C therapeutic agent capable of exerting an excellent effect by stably impregnating a hepatitis C therapeutic agent and delivering it effectively into the skin. The present invention relates to a skin administration system comprising a micro- .
Description
The present invention relates to a microneedle and a microneedle patch.
In general, microneedle is used for delivery of an active substance such as a drug in vivo, detection of an analyte in the body, and biopsy. The delivery of the pharmacologically or cosmetically active ingredient using microneedles is intended for the delivery of the active substance through the skin, not the vascular system such as blood vessels or lymphatic vessels.
Examples of the method using the microneedle include a method of forming a predetermined number of holes or more on the skin using a microneedle device such as a roller with a microneedle attached thereto, (Active ingredient) is coated on the skin to allow the active ingredient to be administered simultaneously with the perforation of the skin.
On the other hand, hepatitis C is a disease in which inflammation of the liver occurs due to the immune response of the body in response to infection with hepatitis C virus (HCV). Hepatitis C is infected by body fluids such as blood infected with the hepatitis C virus. It can be transmitted from a mother with hepatitis C when the baby is born (vertical infection), or by sexual contact, transfusion, or reuse of contaminated syringes. In this way, hepatitis C virus enters the blood, and then it is located in the hepatocyte. Our body causes an immune reaction to remove the virus, which causes the hepatocytes infected with the virus to be destroyed, resulting in inflammation of the liver.
Conventionally, the treatment of hepatitis C has been carried out in the form of oral administration, and has a disadvantage in that the concentration in the body is introduced into the body and the maintenance period is very short.
Therefore, there is a need for new methods that can be effectively used for the treatment of hepatitis C even without side effects.
A problem to be solved by the present invention is to provide a system for effectively delivering a therapeutic agent for hepatitis C into the skin by stably immobilizing a therapeutic agent for hepatitis C in a soluble micro needle and a method for producing such a system.
Accordingly, the present invention provides a soluble micro-needle comprising a hepatitis C therapeutic agent.
The present invention also provides a microneedle patch comprising the microneedles.
In addition, the present invention provides a method for producing a microneedle comprising a hepatitis C therapeutic agent.
In order to solve the above problems, the present invention provides a soluble micro-needle comprising a therapeutic agent for hepatitis C, and more preferably, the material forming the micro-needle is dissolved in the skin, and when the micro- Dissolving or collapsing, whereby the therapeutic agent for hepatitis C is released into the skin.
The inventors of the present invention have found that the conventional oral dosage form is administered at a concentration higher than necessary as well as the fact that the therapeutic agent for hepatitis C can be effectively delivered into the skin by impregnating the therapeutic agent with the hepatitis C in a soluble micro needle after a long period of study, Of the present invention can be remarkably improved, and the present invention has been completed.
As used herein, the term "hepatitis C treatment agent" is a term including both approved hepatitis C treatment agent and unapproved hepatitis C treatment agent, and the approved hepatitis C treatment agent includes, but is not limited to, ribavirin Ribavirin, Simeprevir, Asunaprevir, Daclatasvir, Sofosbuvir, and the like, and mixtures of two or more thereof.
The present inventors have studied various administration systems and no system is similar to the method of impregnating the dissolvable micro needles of the hepatitis C treatment agent. The inventors of the present invention have surprisingly invented that, after various efforts, the micro-needle was impregnated with a therapeutic agent for hepatitis C, and a remarkable effect was confirmed by administering the therapeutic agent for hepatitis C without side effects. In addition, with the micro needle according to the present invention, an untrained general person can easily inoculate the therapeutic agent for hepatitis C without side effects in a noninvasive manner, and can exert an excellent effect because the therapeutic agent can be delivered into the transdermal system.
As used herein, the term "impregnation" may refer to a form in which a therapeutic agent for hepatitis C is contained in a microneedle, preferably i) a therapeutic agent for hepatitis C in combination with a soluble substance for forming microneedles (Including a form in which a therapeutic agent for hepatitis C is dispersed in the micro-needle structure), or ii) a micro-needle is punctured to contain a hepatitis C therapeutic agent in the hole. When preparing micro-needles in the form of i) and ii) above, the therapeutic agent for hepatitis C can penetrate effectively into the skin, and in particular, when producing micro-needles in the form of i) . ≪ / RTI >
Therefore, it is most preferable that the substance forming the microneedles is dissolved in the living body so that the therapeutic agent for hepatitis C contained in the microneedles is effectively released into the skin.
In a preferred embodiment of the present invention, the material forming the microneedles is dissolved in the skin to dissolve or collapse the microneedles when the microneedles are applied to the skin, so that the therapeutic agent for hepatitis C contained in the microneedles effectively It can penetrate.
In the present invention, the microneedles are preferably soluble in the skin. For example, hyaluronic acid, sodium carboxymethyl cellulose (Na-CMC), or the like may be used to form a soluble microneedle. , Water-soluble polymers such as vinylpyrrolidone-vinyl acetate copolymer, polyvinyl alcohol, and polyvinyl pyrrolidone; Sugars such as Xylose, Sucrose, Maltose, Lactose and Trehalose; Or a mixture thereof may be used. Considering the skin penetration strength of the micro-needle and the dissolution rate in the skin in general, it is preferable to use hyaluronic acid, sodium carboxymethyl cellulose (Na-CMC), and saccharide (Trehalose) is preferable, and it is more preferable to mix glycerin.
Preferably, the microneedles of the present invention may further include plasticizers, surfactants, preservatives, anti-inflammatory agents, etc. in addition to the above-mentioned components for forming microneedles.
Examples of the plasticizer include polyols such as ethylene glycol, propylene glycol, dipropylene glycols, butylene glycol, and glycerin. Or may be used in combination.
The length of the microneedle according to the present invention is not limited to a specific size, but it is preferable that the microneedle is applied within a range that does not contact the nerve and the blood vessel because the microneedle may affect pain and drug delivery efficiency . Accordingly, the length of the microneedles according to the present invention is not limited thereto, but may preferably be about 200 to 500 [mu] m.
In the present invention, the therapeutic agent for hepatitis C is contained in an amount of 0.00001 to 1% by weight, preferably 0.0001 to 0.5% by weight, more preferably 0.001 to 0.1% by weight, based on the total weight of the micro needle. If it is contained in an amount of less than 0.00001% by weight, it may not exhibit an effective effect, and if it is contained in an amount exceeding 1% by weight, side effects may be caused, which is not preferable.
When the microneedles according to the present invention are applied to the skin, the skin permeation amount can be remarkably improved as compared with the conventional skin administration systems.
The present invention also provides a microneedle patch comprising the microneedles, that is, a microneedle patch for administration (or delivery) of a hepatitis C therapeutic agent to which the microneedles are attached.
In the present invention, the patch may refer to a sheet having one or more micro-needles impregnated with the hepatitis C therapeutic agent of the present invention and having a surface with the micro-needle attached thereto. The size of the sheet is not limited to a specific size and can be appropriately adjusted according to the amount or the attachment site of the hepatitis C therapeutic agent to be absorbed into the skin. In addition, one or more, preferably a plurality of micro-needles may be attached to the surface of the sheet which can be attached to the skin.
In addition, the surface of the patch that can be adhered to the skin may contain a therapeutic agent for hepatitis C, so that the therapeutic agent for hepatitis C can penetrate into the hole formed by the micro-needle. In order to achieve a superior skin administration effect, The therapeutic agent is preferably impregnated with a fine needle.
The present invention also provides a method for preparing a microcapsule comprising the steps of: S1) filling a mold with a substance for forming a microneedle comprising a hepatitis C therapeutic agent and a skin-soluble substance; And S2) heating and drying the mold, and then separating the mold, wherein the therapeutic agent is a hepatitis C therapeutic agent.
The method can be prepared by impregnating a microcutaneous needle with a therapeutic agent for hepatitis C, and the impregnation is preferably, but not exclusively, i) the treatment of hepatitis C with a solubility in skin forming a microneedle, , ii) a hole in the fine needle to contain the hepatitis C therapeutic agent in the hole, and the like.
In the present invention, in order to impregnate a therapeutic agent for hepatitis C into micro-needles, a material for forming a micro-needle structure and a therapeutic agent for hepatitis C are mixed together in a mold for microneedle formation, and the mold is heated, And then the micro-needle can be produced.
In the present invention, the in-skin solubility material may include, for example, hyaluronic acid, sodium carboxymethyl cellulose (Na-CMC), vinyl pyrrolidone-vinyl acetate copolymer, polyvinyl alcohol vinyl alcohol, and polyvinyl pyrrolidone; Sugars such as Xylose, Sucrose, Maltose, Lactose and Trehalose; Or a mixture thereof may be used.
The present invention provides a method for producing a hepatitis C therapeutic agent administration system capable of exhibiting an excellent effect through effective skin transfer of a hepatitis C therapeutic agent.
The microneedles according to the present invention originally solved the problem of overdosing and short maintenance period which have been pointed out as problems in the conventional oral administration form of hepatitis C infection.
BRIEF DESCRIPTION OF THE DRAWINGS The accompanying drawings, which are incorporated in and constitute a part of the specification, illustrate exemplary embodiments of the invention and, together with the description of the invention, Should not be construed as limited.
FIG. 1 is a view showing one example of various methods for manufacturing a microneedle according to the present invention.
FIG. 2 shows a Franz diffusion cell for evaluating the drug release behavior of the microneedles according to the present invention.
Figure 3 is a graph showing the content of Ribavirin in an acceptor solution.
Hereinafter, embodiments of the present invention will be described in detail to facilitate understanding of the present invention. However, the embodiments according to the present invention can be modified into various other forms, and the scope of the present invention should not be construed as being limited to the following embodiments. Embodiments of the invention are provided to more fully describe the present invention to those skilled in the art.
≪ Preparation of soluble fine needle >
Soluble microneedles are prepared by solution casting method, and they are prepared by casting solution into mold, filling solution into micro mold by vacuum or centrifugation and drying.
Conventional synthetic and natural water-soluble polymers were used for the materials forming the microneedle structure.
≪ Preparation of soluble micro-needle including hepatitis C therapeutic agent (Example 1) >
(Unit: wt%)
Hyaluronic acid (HA), sodium carboxymethyl cellulose (Na-CMC) and trehalose were dissolved in purified water, and then glycerin, PEG-40 hydrogenated castor oil (HCO-40) 0.0 > Ribavirin < / RTI > was added to prepare a microneedle solution. The prepared solution was cast in a silicon microneedle mold and then centrifuged at 3000 rpm for 10 minutes to fill the micro mold with the solution. After the solution was filled, it was dried in a drying oven (70 ° C) for 3 hours, and the fine needle was separated from the silicone mold using an adhesive film (Example 1).
<Experimental Example 1>
Drug release behavior
The present inventors measured the content of Ribavirin in the acceptor solution with Franz diffusion cell using liquid chromatography (Liquid Chromatography) over time.
Ribavirin - impregnated microneedles were attached to pig skin to compare the skin permeability of Ribavirin over time.
As a result, as shown in FIG. 3, it was confirmed that the pig skin into which Ribavirin had been infiltrated by the microneedles containing Ribavirin gradually released with time. This has the effect of reducing the number of drug administration because of the longer time to stay in the body as compared to conventional injections.
Claims (8)
Wherein the material forming the microneedle is dissolved in the skin.
The microneedle forming material may be selected from the group consisting of hyaluronic acid, sodium-carboxymethylcellulose, sodium carboxymethyl cellulose (Na-CMC), vinylpyrrolidone-vinyl acetate copolymer, polyvinyl alcohol Poly vinyl alcohol, polyvinyl pyrrolidone, saccharides, or a mixture of two or more thereof.
Wherein the microneedles further comprise a plasticizer in addition to the material forming the microneedles.
Wherein the therapeutic agent for hepatitis C is contained in an amount of 0.00001 to 1% by weight based on the total weight of the micro-needle.
Wherein the microneedles improve the skin permeation amount of the hepatitis C therapeutic agent.
S2) heating the mold, drying and then separating the mold.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR1020150130629 | 2015-09-15 | ||
| KR20150130629 | 2015-09-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20170032800A true KR20170032800A (en) | 2017-03-23 |
Family
ID=58496336
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020150164916A KR20170032800A (en) | 2015-09-15 | 2015-11-24 | Soluble microneedle patch for treatment of hepatitis C |
Country Status (1)
| Country | Link |
|---|---|
| KR (1) | KR20170032800A (en) |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20140125364A (en) | 2012-02-17 | 2014-10-28 | 코스메드 파마소티컬 씨오 쩜 엘티디 | Microneedle of short-time dissolution type |
-
2015
- 2015-11-24 KR KR1020150164916A patent/KR20170032800A/en unknown
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20140125364A (en) | 2012-02-17 | 2014-10-28 | 코스메드 파마소티컬 씨오 쩜 엘티디 | Microneedle of short-time dissolution type |
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