KR20230063270A - A device for drug delivery comprising microneedle - Google Patents
A device for drug delivery comprising microneedle Download PDFInfo
- Publication number
- KR20230063270A KR20230063270A KR1020210148349A KR20210148349A KR20230063270A KR 20230063270 A KR20230063270 A KR 20230063270A KR 1020210148349 A KR1020210148349 A KR 1020210148349A KR 20210148349 A KR20210148349 A KR 20210148349A KR 20230063270 A KR20230063270 A KR 20230063270A
- Authority
- KR
- South Korea
- Prior art keywords
- drug delivery
- microneedle
- delivery device
- drug
- present
- Prior art date
Links
- 238000012377 drug delivery Methods 0.000 title claims abstract description 36
- 239000003814 drug Substances 0.000 claims abstract description 28
- 229940079593 drug Drugs 0.000 claims abstract description 27
- 206010003246 arthritis Diseases 0.000 claims abstract description 10
- 229960002702 piroxicam Drugs 0.000 claims description 17
- QYSPLQLAKJAUJT-UHFFFAOYSA-N piroxicam Chemical compound OC=1C2=CC=CC=C2S(=O)(=O)N(C)C=1C(=O)NC1=CC=CC=N1 QYSPLQLAKJAUJT-UHFFFAOYSA-N 0.000 claims description 17
- 239000000463 material Substances 0.000 claims description 10
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims description 9
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims description 8
- 229920000747 poly(lactic acid) Polymers 0.000 claims description 8
- 239000004626 polylactic acid Substances 0.000 claims description 8
- 239000002562 thickening agent Substances 0.000 claims description 7
- UXFQFBNBSPQBJW-UHFFFAOYSA-N 2-amino-2-methylpropane-1,3-diol Chemical group OCC(N)(C)CO UXFQFBNBSPQBJW-UHFFFAOYSA-N 0.000 claims description 6
- 239000002904 solvent Substances 0.000 claims description 6
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 4
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims description 4
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 4
- 229920001432 poly(L-lactide) Polymers 0.000 claims description 4
- 239000004633 polyglycolic acid Substances 0.000 claims description 4
- 229950008885 polyglycolic acid Drugs 0.000 claims description 4
- 239000001856 Ethyl cellulose Substances 0.000 claims description 3
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 claims description 3
- ZRVUJXDFFKFLMG-UHFFFAOYSA-N Meloxicam Chemical compound OC=1C2=CC=CC=C2S(=O)(=O)N(C)C=1C(=O)NC1=NC=C(C)S1 ZRVUJXDFFKFLMG-UHFFFAOYSA-N 0.000 claims description 3
- 229920002988 biodegradable polymer Polymers 0.000 claims description 3
- 239000004621 biodegradable polymer Substances 0.000 claims description 3
- 235000019325 ethyl cellulose Nutrition 0.000 claims description 3
- 229920001249 ethyl cellulose Polymers 0.000 claims description 3
- SYTBZMRGLBWNTM-UHFFFAOYSA-N flurbiprofen Chemical compound FC1=CC(C(C(O)=O)C)=CC=C1C1=CC=CC=C1 SYTBZMRGLBWNTM-UHFFFAOYSA-N 0.000 claims description 3
- 229960002390 flurbiprofen Drugs 0.000 claims description 3
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 3
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 3
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 3
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims description 3
- DKYWVDODHFEZIM-UHFFFAOYSA-N ketoprofen Chemical compound OC(=O)C(C)C1=CC=CC(C(=O)C=2C=CC=CC=2)=C1 DKYWVDODHFEZIM-UHFFFAOYSA-N 0.000 claims description 3
- 229960000991 ketoprofen Drugs 0.000 claims description 3
- 229960001929 meloxicam Drugs 0.000 claims description 3
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims description 3
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 3
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 3
- HXKKHQJGJAFBHI-UHFFFAOYSA-N 1-aminopropan-2-ol Chemical compound CC(O)CN HXKKHQJGJAFBHI-UHFFFAOYSA-N 0.000 claims description 2
- PIICEJLVQHRZGT-UHFFFAOYSA-N Ethylenediamine Chemical compound NCCN PIICEJLVQHRZGT-UHFFFAOYSA-N 0.000 claims description 2
- GSEJCLTVZPLZKY-UHFFFAOYSA-N Triethanolamine Chemical compound OCCN(CCO)CCO GSEJCLTVZPLZKY-UHFFFAOYSA-N 0.000 claims description 2
- CBTVGIZVANVGBH-UHFFFAOYSA-N aminomethyl propanol Chemical compound CC(C)(N)CO CBTVGIZVANVGBH-UHFFFAOYSA-N 0.000 claims description 2
- ZBCBWPMODOFKDW-UHFFFAOYSA-N diethanolamine Chemical compound OCCNCCO ZBCBWPMODOFKDW-UHFFFAOYSA-N 0.000 claims description 2
- HPNMFZURTQLUMO-UHFFFAOYSA-N diethylamine Chemical compound CCNCC HPNMFZURTQLUMO-UHFFFAOYSA-N 0.000 claims description 2
- 229940102253 isopropanolamine Drugs 0.000 claims description 2
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 claims description 2
- 229960000281 trometamol Drugs 0.000 claims description 2
- ZFFMLCVRJBZUDZ-UHFFFAOYSA-N 2,3-dimethylbutane Chemical group CC(C)C(C)C ZFFMLCVRJBZUDZ-UHFFFAOYSA-N 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 238000013271 transdermal drug delivery Methods 0.000 abstract description 5
- 210000003491 skin Anatomy 0.000 description 20
- 238000000576 coating method Methods 0.000 description 13
- 239000000243 solution Substances 0.000 description 13
- 239000011248 coating agent Substances 0.000 description 11
- 239000004205 dimethyl polysiloxane Substances 0.000 description 8
- 229920000435 poly(dimethylsiloxane) Polymers 0.000 description 8
- 238000009472 formulation Methods 0.000 description 7
- 239000010410 layer Substances 0.000 description 7
- 239000000203 mixture Substances 0.000 description 7
- 238000010521 absorption reaction Methods 0.000 description 5
- 238000009792 diffusion process Methods 0.000 description 5
- 238000002360 preparation method Methods 0.000 description 5
- AFCARXCZXQIEQB-UHFFFAOYSA-N N-[3-oxo-3-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)propyl]-2-[[3-(trifluoromethoxy)phenyl]methylamino]pyrimidine-5-carboxamide Chemical compound O=C(CCNC(=O)C=1C=NC(=NC=1)NCC1=CC(=CC=C1)OC(F)(F)F)N1CC2=C(CC1)NN=N2 AFCARXCZXQIEQB-UHFFFAOYSA-N 0.000 description 4
- 230000000144 pharmacologic effect Effects 0.000 description 4
- 238000003756 stirring Methods 0.000 description 4
- VZSRBBMJRBPUNF-UHFFFAOYSA-N 2-(2,3-dihydro-1H-inden-2-ylamino)-N-[3-oxo-3-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)propyl]pyrimidine-5-carboxamide Chemical compound C1C(CC2=CC=CC=C12)NC1=NC=C(C=N1)C(=O)NCCC(N1CC2=C(CC1)NN=N2)=O VZSRBBMJRBPUNF-UHFFFAOYSA-N 0.000 description 3
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 3
- UAOMVDZJSHZZME-UHFFFAOYSA-N diisopropylamine Chemical compound CC(C)NC(C)C UAOMVDZJSHZZME-UHFFFAOYSA-N 0.000 description 3
- 230000007246 mechanism Effects 0.000 description 3
- 230000037317 transdermal delivery Effects 0.000 description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
- 102000004005 Prostaglandin-endoperoxide synthases Human genes 0.000 description 2
- 108090000459 Prostaglandin-endoperoxide synthases Proteins 0.000 description 2
- 239000012790 adhesive layer Substances 0.000 description 2
- 230000001186 cumulative effect Effects 0.000 description 2
- 238000005520 cutting process Methods 0.000 description 2
- -1 diisophanolamine Chemical compound 0.000 description 2
- 238000003618 dip coating Methods 0.000 description 2
- 238000001035 drying Methods 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 238000010579 first pass effect Methods 0.000 description 2
- 238000002347 injection Methods 0.000 description 2
- 239000007924 injection Substances 0.000 description 2
- 238000004811 liquid chromatography Methods 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 229910052751 metal Inorganic materials 0.000 description 2
- 239000002184 metal Substances 0.000 description 2
- NIPNSKYNPDTRPC-UHFFFAOYSA-N N-[2-oxo-2-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)ethyl]-2-[[3-(trifluoromethoxy)phenyl]methylamino]pyrimidine-5-carboxamide Chemical compound O=C(CNC(=O)C=1C=NC(=NC=1)NCC1=CC(=CC=C1)OC(F)(F)F)N1CC2=C(CC1)NN=N2 NIPNSKYNPDTRPC-UHFFFAOYSA-N 0.000 description 1
- 208000034530 PLAA-associated neurodevelopmental disease Diseases 0.000 description 1
- 208000008469 Peptic Ulcer Diseases 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 1
- 230000001760 anti-analgesic effect Effects 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 230000001754 anti-pyretic effect Effects 0.000 description 1
- 239000002221 antipyretic Substances 0.000 description 1
- 230000008901 benefit Effects 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 239000007853 buffer solution Substances 0.000 description 1
- 238000005119 centrifugation Methods 0.000 description 1
- 239000000919 ceramic Substances 0.000 description 1
- 239000011247 coating layer Substances 0.000 description 1
- 239000002537 cosmetic Substances 0.000 description 1
- 229940043279 diisopropylamine Drugs 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 230000001747 exhibiting effect Effects 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- PCHJSUWPFVWCPO-UHFFFAOYSA-N gold Chemical compound [Au] PCHJSUWPFVWCPO-UHFFFAOYSA-N 0.000 description 1
- 239000010931 gold Substances 0.000 description 1
- 229910052737 gold Inorganic materials 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- 238000004128 high performance liquid chromatography Methods 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 230000009545 invasion Effects 0.000 description 1
- 239000002075 main ingredient Substances 0.000 description 1
- 229910000402 monopotassium phosphate Inorganic materials 0.000 description 1
- 235000019796 monopotassium phosphate Nutrition 0.000 description 1
- 239000008188 pellet Substances 0.000 description 1
- 230000037368 penetrate the skin Effects 0.000 description 1
- 208000011906 peptic ulcer disease Diseases 0.000 description 1
- 239000008363 phosphate buffer Substances 0.000 description 1
- 239000008055 phosphate buffer solution Substances 0.000 description 1
- PJNZPQUBCPKICU-UHFFFAOYSA-N phosphoric acid;potassium Chemical compound [K].OP(O)(O)=O PJNZPQUBCPKICU-UHFFFAOYSA-N 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 239000011148 porous material Substances 0.000 description 1
- 210000004258 portal system Anatomy 0.000 description 1
- 238000003825 pressing Methods 0.000 description 1
- 150000003180 prostaglandins Chemical class 0.000 description 1
- QEVHRUUCFGRFIF-MDEJGZGSSA-N reserpine Chemical compound O([C@H]1[C@@H]([C@H]([C@H]2C[C@@H]3C4=C(C5=CC=C(OC)C=C5N4)CCN3C[C@H]2C1)C(=O)OC)OC)C(=O)C1=CC(OC)=C(OC)C(OC)=C1 QEVHRUUCFGRFIF-MDEJGZGSSA-N 0.000 description 1
- 229910052710 silicon Inorganic materials 0.000 description 1
- 239000010703 silicon Substances 0.000 description 1
- 230000037384 skin absorption Effects 0.000 description 1
- 231100000274 skin absorption Toxicity 0.000 description 1
- 231100000245 skin permeability Toxicity 0.000 description 1
- 229910001220 stainless steel Inorganic materials 0.000 description 1
- 239000010935 stainless steel Substances 0.000 description 1
- 210000000434 stratum corneum Anatomy 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 238000002834 transmittance Methods 0.000 description 1
- 238000002525 ultrasonication Methods 0.000 description 1
- 210000000707 wrist Anatomy 0.000 description 1
Images
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—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
-
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/5415—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; 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
-
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
- A61M2037/0023—Drug applicators using microneedles
-
- 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
- A61M2205/00—General characteristics of the apparatus
- A61M2205/02—General characteristics of the apparatus characterised by a particular materials
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Dermatology (AREA)
- Inorganic Chemistry (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Biomedical Technology (AREA)
- Anesthesiology (AREA)
- Medical Informatics (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Heart & Thoracic Surgery (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Physical Education & Sports Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
Description
본 발명은 마이크로니들을 포함하는 관절염 치료용 약물 전달 장치에 관한 것이다.The present invention relates to a drug delivery device for treating arthritis including a microneedle.
마이크로니들을 포함하는 약물 전달 장치는, 대략 수백 마이크로미터의 길이를 갖는 마이크로니들이 피부의 각질층을 통과하여 피내로 활성성분을 전달하게 하는 경피적 약물전달 시스템이다.A drug delivery device including a microneedle is a transdermal drug delivery system in which a microneedle having a length of about several hundred micrometers passes through the stratum corneum of the skin and delivers an active ingredient into the skin.
마이크로니들은 기존의 주사제제의 경피 전달 효능 및 경피 약물전달 시스템인 패치의 편의성을 결합하여, 피부 침습에 의한 통증을 최소화하면서 활성물질의 경피적 전달을 효율적으로 달성할 수 있을 것으로 예상하고 있다.Microneedles are expected to be able to efficiently achieve transdermal delivery of active substances while minimizing pain caused by skin invasion by combining the transdermal delivery efficacy of conventional injection preparations and the convenience of patches, which are transdermal drug delivery systems.
그러나, 현실적으로는 아직까지 의약품으로서 마이크로니들 제형이 개발되어 상용화된 사례가 없으며, 단지 화장품과 같은 피부미용 용도로서만 상용화되고 있는 실정이다.However, in reality, there is no case in which a microneedle formulation has been developed and commercialized as a pharmaceutical yet, and is commercialized only for skin care purposes such as cosmetics.
본 발명은 마이크로니들을 포함하는 관절염 치료용 약물 전달 장치를 제공하기 위한 것이다.The present invention is to provide a drug delivery device for treating arthritis, including a microneedle.
관절염 치료제로서 사용되고 있는 비스테로이드성 항염증제(이하에서는, NSAID와 혼용하여 기재한다)는 국소 미세환경에서 작용하며, 시클로옥시제나제(COX)의 활성을 억제함으로써, 해열, 소염 및 진통 작용을 나타낸다.Non-steroidal anti-inflammatory drugs (hereinafter, described in combination with NSAIDs) used as therapeutic agents for arthritis act in the local microenvironment and suppress the activity of cyclooxygenase (COX), thereby exhibiting antipyretic, anti-inflammatory and analgesic actions.
대부분의 NSAID 계열 약물은 일반적으로 경구용으로 투여되고 있으나, 경구투여시 위점막 장애 및 소화성 궤양과 같은 부작용이 나타나는 것으로 확인되고 있다.Although most NSAID-type drugs are generally administered orally, it has been confirmed that side effects such as gastric mucosal disorder and peptic ulcer appear when administered orally.
특히, NSAID 중 피록시캄은 문맥계를 통하여 초회통과효과(first pass effect)를 거쳐 대사되는데, 용변으로 배설되는 약물의 양이 투여량의 5% 미만이고, 대사물의 활성은 본래 피록시캄의 프로스타글란딘 합성 억제 활성보다 1,000배나 적은 것으로 알려져 있다. 이러한 문제점들을 해결하기 위해서, 초회통과효과를 피하여 피록시캄을 투여할 수 있는 경피 전달 시스템의 개발이 필요하다.In particular, among NSAIDs, piroxicam is metabolized through a first pass effect through the portal system. It is known to be 1,000 times less than prostaglandin synthesis inhibitory activity. In order to solve these problems, it is necessary to develop a transdermal delivery system capable of administering piroxicam while avoiding the first pass effect.
그러나, 피록시캄은 다른 NSAID 약물에 비하여 상대적으로 큰 분자량(mw=331.35)과 낮은 피부 투과성, 낮은 용해도로 인하여 경피 투여 경로로 제제화하기가 어렵다However, compared to other NSAID drugs, piroxicam is difficult to formulate through the transdermal route due to its relatively high molecular weight (mw=331.35), low skin permeability, and low solubility.
따라서, 피록시캄과 같은 NSAID 계열의 관절염 치료 약물을 경피적으로 투여할 수 있는 제제의 개발이 필요하다.Therefore, it is necessary to develop a formulation capable of transdermally administering an NSAID-type arthritis drug such as piroxicam.
본 발명은 마이크로니들을 포함하는 관절염 치료용 약물 전달 장치에 관한 것이다.The present invention relates to a drug delivery device for treating arthritis including a microneedle.
구체적으로 본 발명은, 마이크로 니들; 마이크로 니들의 적어도 일부의 표면에 코팅된 약물층; 및 마이크로 니들을 지지하는 지지체를 포함하는 관절염 치료용 약물 전달 장치에 관한 것이다.Specifically, the present invention, micro needle; A drug layer coated on at least a portion of the surface of the microneedle; and a drug delivery device for treating arthritis, comprising a support for supporting the microneedle.
본 발명에 따른 약물 전달 장치에서 상기 약물층은 NSAID 약물을 함유할 수 있다. 예를 들어, 상기 약물층은 피록시캄, 멜록시캄, 플루르비프로펜 또는 케토프로펜과 같은 약물을 함유할 수 있다.In the drug delivery device according to the present invention, the drug layer may contain an NSAID drug. For example, the drug layer may contain a drug such as piroxicam, meloxicam, flurbiprofen or ketoprofen.
본 발명에 따른 약물 전달 장치에서, 상기 약물층은 추가로 증점제 및 용해보조제를 더 포함하는 것이 바람직하다.In the drug delivery device according to the present invention, the drug layer preferably further includes a thickener and a solubilizing agent.
본 발명에 사용될 수 있는 증점제로는 하이드록시프로필 셀룰로오스, 하이드록시프로필메틸 셀룰로오스, 폴리비닐피롤리돈 및 에틸 셀룰로오스과 같은 물질로부터 1종 이상이 선택되어 사용될 수 있으나, 이러한 물질로 한정되는 것은 아니다.As the thickener that can be used in the present invention, one or more types may be selected from materials such as hydroxypropyl cellulose, hydroxypropylmethyl cellulose, polyvinylpyrrolidone, and ethyl cellulose, but are not limited thereto.
본 발명에 사용될 수 있는 용해보조제로는 2-아미노-2-메틸-1,3-프로판디올, 아미노메틸 프로판디올, 트로메타민, 아미노메틸 프로판올, 디에탄올아민, 디이소판올아민, 트리에탄올아민, 에틸렌디아민, 디이소프로필아민, 디에틸아민 및 이소프로판올아민과 같은 물질로부터 1종 이상이 선택되어 사용될 수 있으나, 이러한 물질로 한정되는 것은 아니다.As the solubilizing agent that can be used in the present invention, 2-amino-2-methyl-1,3-propanediol, aminomethyl propanediol, tromethamine, aminomethyl propanol, diethanolamine, diisophanolamine, triethanolamine, At least one selected from materials such as ethylenediamine, diisopropylamine, diethylamine and isopropanolamine may be used, but is not limited to these materials.
본 발명의 약물 전달 장치에서, 상기 마이크로니들 및 이를 지지하는 지지체는 마이크로니들로 성형이 가능한 임의의 재질, 예를 들어, 실리콘, 금속, 세라믹, 고분자 물질(폴리머) 등이 사용될 수 있으며, 바람직하게는 생분해성 고분자 물질이 사용될 수 있다. 본 발명에서 사용될 수 있는 생분해성 고분자 물질은 PLA(폴리락트 산), L-PLA(폴리-L-락트 산), PGA(폴리-글리콜 산) 및 PLGA(폴리-락트-코-글리콜 산)과 같은 물질로부터 1종 이상 선택될 수 있다.In the drug delivery device of the present invention, the microneedle and the support supporting the microneedle may be made of any material that can be molded into the microneedle, for example, silicon, metal, ceramic, high molecular material (polymer), etc., preferably. A biodegradable polymeric material may be used. Biodegradable polymer materials that can be used in the present invention are PLA (polylactic acid), L-PLA (poly-L-lactic acid), PGA (poly-glycolic acid) and PLGA (poly-lactic-co-glycolic acid) and One or more may be selected from the same material.
본 발명의 약물 전달 장치에서 마이크로니들의 길이는 약 100~800㎛일 수 있으며, 종횡비(aspect ratio: 즉, 마이크로니들의 최대 직경에 대한 마이크로니들의 길이의 비)는 약 1:2 내지 1:5 일 수 있으나, 이러한 범위로 한정되는 것은 아니다.In the drug delivery device of the present invention, the length of the microneedle may be about 100 to 800 μm, and the aspect ratio (ie, the ratio of the length of the microneedle to the maximum diameter of the microneedle) is about 1:2 to 1: 5, but is not limited to this range.
본 발명에 따른 약물 전달 장치의 지지체는 필요에 따라 임의의 크기로 제조할 수 있으나, 작은 크기(예를 들어, 지지체의 면적이 6cm2 또는 그 이하)로 제조하여도 목적하는 약리 효과를 얻을 수 있을 정도의 약물량이 피부를 투과할 수 있다.The support of the drug delivery device according to the present invention can be manufactured in any size as needed, but the desired pharmacological effect can be obtained even when manufactured in a small size (eg, the area of the support is 6 cm 2 or less). A sufficient amount of the drug can penetrate the skin.
본 발명에 따른 약물 전달 장치는 경피적 약물 전달 효율이 우수하다.The drug delivery device according to the present invention has excellent transdermal drug delivery efficiency.
따라서, 본 발명에 따른 약물 전달 장치는, 기존의 경피 흡수 패치 제형보다 훨씬 적은 크기로도 동등한 약리 효과가 나타나도록 할 수 있으며, 또한 짧은 피부 부착 시간에도 경피적으로 충분한 약물 전달이 일어나게 할 수 있다.Therefore, the drug delivery device according to the present invention can achieve equivalent pharmacological effects even with a much smaller size than conventional transdermal absorption patch formulations, and can also ensure sufficient drug delivery transdermally even with a short skin attachment time.
도 1은 본 발명에 따른 약물 전달 장치의 단면을 모식적으로 도시한 것이다.
도 2는 본 발명에 따른 약물 전달 장치의 일 실시예 및 이의 부분 확대도이다.
도 3은 본 발명에 따른 약물 전달 장치의 경피 흡수 시험 결과를 그래프로 도시한 것이다.1 schematically shows a cross section of a drug delivery device according to the present invention.
2 is an embodiment of a drug delivery device according to the present invention and a partially enlarged view thereof.
3 is a graph showing the transdermal absorption test results of the drug delivery device according to the present invention.
이하, 본 발명의 이해를 돕기 위하여 실시예를 들어 상세하게 설명하기로 한다. 그러나, 하기의 실시예는 본 발명의 내용을 예시하는 것일 뿐, 본 발명의 범위가 하기 실시예에 의하여 한정되는 것은 아니다. 본 발명의 실시예는 당업계에서 평균적인 지식을 가진 자에게 본 발명을 보다 완전하게 설명하기 위하여 제공되는 것이다.Hereinafter, examples will be described in detail to aid understanding of the present invention. However, the following examples are merely illustrative of the content of the present invention, and the scope of the present invention is not limited by the following examples. The embodiments of the present invention are provided to more completely explain the present invention to those skilled in the art.
실시예Example 1: 코팅 방식의 1: coating method 마이크로니들microneedle 제조 manufacturing
실시예Example 1-1: 코팅층으로 사용될 코팅용액의 제조 1-1: Preparation of coating solution to be used as a coating layer
20mL 바이알에 에탄올(94.5%) 5ml 및 용해보조제인 AMPD (2-amino-2-methyl-1,3-propanediol) 66.65mg을 순차적으로 넣고 3분간 초음파 처리를 진행하였다. 이후, 여기에 증점제로서 하이드록시프로필 셀룰로오스 200mg을 취하여 넣은 후, 마그네틱 교반기를 이용하여 2시간 동안 교반하였다. 이후, 여기에 주성분인 피록시캄 100mg을 넣고, 롤믹서를 이용하여 3시간 동안 혼합하여, 코팅용액을 제조하였다.5 ml of ethanol (94.5%) and 66.65 mg of 2-amino-2-methyl-1,3-propanediol (AMPD) as a solubilizing agent were sequentially put into a 20 mL vial, and ultrasonication was performed for 3 minutes. Thereafter, 200 mg of hydroxypropyl cellulose as a thickener was added thereto, followed by stirring for 2 hours using a magnetic stirrer. Thereafter, 100 mg of piroxicam, the main ingredient, was added thereto and mixed for 3 hours using a roll mixer to prepare a coating solution.
실시예Example 1-2: 지지체의 제조 1-2: Preparation of support
길이 400um, 너비 150um에 해당하는 규격을 가진 마이크로니들 401개가 지름 1cm의 원 내에 분포하도록 설계하였다. 이러한 설계에 맞추어 제작된 양각의 금속 몰드를 사용하여 음각의 PDMS(폴리디메틸실록산) 몰드를 제작하였다.401 microneedles with dimensions of 400um in length and 150um in width were designed to be distributed in a circle with a diameter of 1cm. A negative PDMS (polydimethylsiloxane) mold was produced using the positive metal mold manufactured according to this design.
이와 같이 제작된 PDMS 몰드 내에 PLA (Polylactic acid) 펠렛(pellet)을 넣은 후, 190도의 오븐에 넣어 1시간 동안 가열하여 녹였다. 이후, 오븐에서 몰드를 꺼내어 상온에서 완전히 냉각시켰다, 완전히 식은 PDMS 음각 몰드로부터 PLA 재질의 고형화된 마이크로니들 및 지지체를 분리하여, 마이크로니들(12)이 일체형으로 배열된 지지체(11)를 제조하였다.After putting PLA (Polylactic acid) pellets in the PDMS mold prepared as described above, they were melted by heating for 1 hour in an oven at 190 degrees. Then, the mold was taken out of the oven and completely cooled at room temperature. The solidified microneedle made of PLA and the support were separated from the completely cooled PDMS intaglio mold, and the
실시예Example 1-3: 1-3: 마이크로니들microneedle 코팅 coating
딥 코팅 방법을 사용하여, 상기 실시예 1-1에서 제조된 코팅용액으로 마이크로니들 지지체(11, 12)의 표면을 코팅하였다.Using the dip coating method, the surfaces of the microneedle supports 11 and 12 were coated with the coating solution prepared in Example 1-1.
구체적으로, 딥 코팅 기기를 사용하여, PLA 마이크로니들을 진공 흡착하고, 지름 1.5cm, 두께 300um인 코팅용액 담지체(reservoir) 내에 코팅용액을 도포하였다. 진공 흡착기에 흡착 고정된 PLA 마이크로니들이 일정 속도로 코팅용액이 도포된 담지체로 내려오도록 하여 마이크로니들을 코팅용액으로 코팅시킨다. 이러한 코팅 공정을 5회 반복한다. 이후, 상온 진공 챔버에서 건조시킨다. 건조가 완료된 샘플은 데시케이터에 보관한다. Specifically, a PLA microneedle was vacuum adsorbed using a dip coating device, and the coating solution was applied to a coating solution reservoir having a diameter of 1.5 cm and a thickness of 300 um. The microneedle is coated with the coating solution by allowing the PLA microneedle adsorbed and fixed to the vacuum adsorber to descend at a constant speed to the carrier coated with the coating solution. This coating process is repeated 5 times. Then, it is dried in a room temperature vacuum chamber. The dried sample is stored in a desiccator.
도 1 이와 같이 제조된 약물 전달 장치의 단면을 모식적으로 도시한 것으로서, 상기 약물 전달 장치는 마이크로 니들(12); 마이크로 니들(12)의 적어도 일부의 표면에 코팅된 약물층(20); 및 마이크로 니들(12)을 지지하는 지지체(11)를 포함하여 구성되며, 상기 약물층(20)은 NSAID 약물인 피록시캄(21)을 함유한다.1 schematically shows a cross-section of a drug delivery device prepared as described above, wherein the drug delivery device includes a
상기와 같이 제조된 지지체는 피부에 접착시킬 수 있도록 원형 또는 정방형의 접착층 위에 접착 및 고정된 후에 피부에 적용될 수 있다.The support prepared as described above may be applied to the skin after being adhered and fixed on a circular or square adhesive layer so as to be adhered to the skin.
대안으로서, 상기와 같이 지지체가 고정된 접착층은 손목 또는 손가락 마디에 용이하게 접착될 수 있도록 스트랩(strap)을 구비할 수 있다. 도 2는 이와 같이 스트랩이 연결된 형태의 약물 전달 장치의 일 실시예 및 이의 지지체와 마이크로니들을 각각 확대하여 도시한 도면이다.Alternatively, the adhesive layer to which the support is fixed may include a strap so as to be easily attached to the wrist or knuckle. FIG. 2 is an enlarged view of an embodiment of a drug delivery device having a strap connected thereto, and its support and microneedles, respectively.
실시예Example 2: 용해성 2: solubility 마이크로니들microneedle 제조 manufacturing
실시예 1-1에서 제조한 코팅용액과 실시예 1-2에서 제조한 PDMS 몰드를 사용하여 용해성(dissolving) 마이크로니들을 제조한다.A dissolving microneedle was prepared using the coating solution prepared in Example 1-1 and the PDMS mold prepared in Example 1-2.
구체적으로, 상기 실시예 1-2에서 제조한 PDMS 몰드 내에 상기 실시예1-2에서 제조한 코팅용액 0.25g 내지 0.3g을 넣은 후, 3000 rpm 의 원심분리 공정을 5분씩 5회 반복하여 PDMS 몰드 내의 팁의 끝까지 코팅용액을 채운다. 이후, 상온에서 건조공정을 거친 후, 건조가 완료되면 PDMS 몰드로부터 고형화된 마이크로니들 및 지지체를 분리하여, 피록시캄이 함유된, 마이크로니들이 일체형으로 배열된 지지체를 제조하였다.Specifically, after putting 0.25 g to 0.3 g of the coating solution prepared in Example 1-2 into the PDMS mold prepared in Example 1-2, the centrifugation process at 3000 rpm was repeated 5 times for 5 minutes each to form a PDMS mold. Fill the coating solution to the end of the inner tip. Thereafter, after drying at room temperature, when the drying was completed, the solidified microneedles and the support were separated from the PDMS mold to prepare a support containing piroxicam and having the microneedles integrally arranged.
실험예Experimental example : : 경피transdermal 투과 시험 permeation test
실시예 1에서 제조한 약물 전달 장치의 경피 투과 시험을 다음과 같은 방법으로 실시하였다:A transdermal permeation test of the drug delivery device prepared in Example 1 was conducted in the following manner:
프란쯔 타입의 확산 기구(Franz-type diffusion cell) 내의 리셉터에 등장의 인산염 완충액(pH 7.4 phosphate buffer 용액)을 넣고, 피부 온도와 유사하게 32℃를 유지시키면서, 마그네틱 교반기로 600rpm의 교반속도로 일정하게 교반하여 용액내의 용존 기체를 제거하였다.Put isotonic phosphate buffer (pH 7.4 phosphate buffer solution) into the receptor in the Franz-type diffusion cell, maintain 32 ℃ similar to skin temperature, and stir at a constant stirring speed of 600 rpm with a magnetic stirrer The dissolved gas in the solution was removed by stirring.
인간 사체 피부(Cadaver human skin)는 사용하기 2시간 전에 냉동실에서 꺼내어 해동시킨 후 사용한다.Cadaver human skin is taken out of the freezer 2 hours before use and thawed before use.
이후, 프란쯔 타입의 확산기구의 상부 공여셀에 맞도록 (1) 대조군으로서 현재 시판 중인 피록시캄 함유 경피 흡수 제제를 절단하여 샘플을 준비하고 (2) 실시예에서 제조한 마이크로니들은 더마플라스트TM 밴드위에 부착하여 준비한다.Then, (1) as a control, a sample was prepared by cutting a commercially available transdermal preparation containing piroxicam to fit into the upper donor cell of the Franz-type diffusion mechanism, and (2) the microneedle prepared in Example was Dermafla. Prepare it by attaching it on the strap TM band.
(1)과 (2)의 샘플을 인간 사체 피부에 붙이되, (2)의 샘플은 마이크로니들을 인간 사체 피부에 10초간 50N의 힘으로 누른 후 프란쯔 타입의 확산기구에 장착하였다.The samples of (1) and (2) were attached to human cadaver skin, and the sample of (2) was attached to a Franz-type diffusion mechanism after pressing the microneedle to the human cadaver skin with a force of 50 N for 10 seconds.
(2)의 샘플은 1시간 투여 및 24시간 투여를 각각 시험하였으며, 1시간 투여하는 경우에는 프란쯔 타입의 확산기구에 장착하기 1시간 전에 미리 피부에 적용하고, 1시간 후에 마이크로니들 샘플을 제거하고 나서 프란쯔 타입의 확산기구에 장착하였다. Sample (2) was tested for 1-hour administration and 24-hour administration, respectively. In the case of 1-hour administration, it was applied to the skin 1 hour before being attached to the Franz type diffusion device, and the microneedle sample was removed after 1 hour. Then, it was mounted on a Franz-type diffusion mechanism.
이후 일정 시간마다 리셉터 부분의 용액을 채취하고, 채취한 양만큼의 새로운 완충용액을 보충해 주었다. 채취한 시료 중에 존재하는 피록시캄의 양을 고성능 액체크로마토그래피(HPLC)로 분석하였다.After that, the solution of the receptor part was collected at regular intervals, and a new buffer solution was replenished as much as the sampled amount. The amount of piroxicam present in the collected samples was analyzed by high-performance liquid chromatography (HPLC).
<액체크로마토그래피 조건><Liquid chromatography conditions>
컬럼 : 안지름 약 4.6 mm, 길이 250mm인 스테인레스강관에 공경 5.0 ㎛의 액체크로마토그래프용 옥타데실실릴실리카켈을 충전한 칼럼 (Hypersil gold C18 혹은 이와 동등한 칼럼)Column: A column filled with octadecylsilylsilica gel for liquid chromatography with a pore diameter of 5.0 μm in a stainless steel tube with an inside diameter of about 4.6 mm and a length of 250 mm (Hypersil gold C18 or equivalent column)
이동상 : 10mM 인산이수소칼륨액: 아세토니트릴=6:4 (인산으로 pH 3.0 조절)Mobile phase: 10 mM potassium dihydrogen phosphate solution: acetonitrile = 6:4 (pH 3.0 adjusted with phosphoric acid)
유속 : 1.0 mL/minFlow rate: 1.0 mL/min
칼럼온도 : 25℃Column temperature: 25℃
주입량 : 20 ㎕Injection volume: 20 μl
검출기 : 자외부흡광광도계 330 ㎚Detector: UV spectrophotometer 330 nm
각 채취 시점의 시료 중에 존재하는 피록시캄의 양을 누적한 값이, 대조군 경피 흡수 제제 또는 마이크로니들에 함유된 피록시캄 중에서 피부를 투과한 피록시캄의 양(cumulative dermal absorption)에 해당한다. The cumulative value of the amount of piroxicam present in the sample at each collection point corresponds to the amount of piroxicam that penetrated the skin (cumulative dermal absorption) among the control percutaneous absorption formulation or piroxicam contained in the microneedle .
실험 결과, 본 발명에 따른 마이크로니들에 의하여 피부를 투과한 피록시캄의 양(제제 1cm2 당 피부를 투과한 피록시캄의 양)이 기존의 시판 중인 경피 흡수 제제보다 훨씬 많다는 것을 확인할 수 있었다.As a result of the experiment, it was confirmed that the amount of piroxicam that penetrated the skin by the microneedle according to the present invention (the amount of piroxicam that penetrated the skin per 1 cm 2 of the formulation) was much higher than that of conventional transdermal absorption formulations on the market. .
아울러, 본 발명에 따른 마이크로니들을 1시간 적용하였을 때의 약물의 피부투과량과 24시간 적용하였을 때의 약물의 피부 투과량이 크게 차이나지 아니하였다. 이는 본 발명에 따른 마이크로니들을 1시간 피부에 적용하는 경우, 24시간 적용한 경우와 동등하게 국소적인 약리작용이 나타날 수 있음을 의미한다. 따라서, 투약 순응도 측면에서 우수한 장점이 있다.In addition, the skin permeation amount of the drug when the microneedle according to the present invention was applied for 1 hour and the skin permeation amount of the drug when applied for 24 hours did not significantly differ. This means that when the microneedle according to the present invention is applied to the skin for 1 hour, a local pharmacological action may appear equivalent to the case of application for 24 hours. Therefore, there is an excellent advantage in terms of medication compliance.
한편, 대조군 및 본 발명에 따른 마이크로니들을 절단하지 아니하고 제조된 크기 그대로 피부에 적용하였을 때의 피부 투과량을 계산하면 아래 표와 같다:On the other hand, the skin permeation amount when the microneedle according to the control group and the present invention was applied to the skin as it was prepared without cutting was calculated as shown in the table below:
* 마이크로 니들의 크기는 지름 1cm 인 원의 면적이다.* The size of a microneedle is the area of a circle with a diameter of 1 cm.
위 실험 결과로부터, 본 발명에 따른 마이크로니들은 그 크기를 적게 하여도 기존의 시판 중인 경피 흡수 패치제와 약물 투과량이 동등한 것으로 나타났다. 따라서, 본 발명에 따른 마이크로니들은 그 크기를 대폭 감소하여도, 기존의 경피 흡수 제제와 동등한 약리효과를 나타낼 것이다.From the above experimental results, it was found that the microneedle according to the present invention has the same drug permeation amount as the existing commercially available transdermal absorption patch even though the size thereof is small. Therefore, even if the size of the microneedle according to the present invention is significantly reduced, it will exhibit pharmacological effects equivalent to conventional transdermally absorbable preparations.
본 발명에 따른 약물 전달 장치는 경피적 약물 전달 효율이 우수하다.The drug delivery device according to the present invention has excellent transdermal drug delivery efficiency.
11: 지지체
12: 마이크로니들
20: 약물층
21: 약물11: support
12: microneedle
20: drug layer
21: drug
Claims (11)
마이크로니들의 적어도 일부의 표면에 코팅된 약물층; 및
마이크로니들을 지지하는 지지체
를 포함하는 관절염 치료용 약물 전달 장치.microneedle;
A drug layer coated on at least a portion of the surface of the microneedle; and
A support that supports the microneedle
A drug delivery device for treating arthritis comprising a.
상기 증점제는 하이드록시프로필 셀룰로오스, 하이드록시프로필메틸 셀룰로오스, 폴리비닐피롤리돈 및 에틸 셀룰로오스로 이루어진 군으로부터 선택되는 1종 이상이고,
상기 용해보조제는 2-아미노-2-메틸-1,3-프로판디올, 아미노메틸 프로판디올, 트로메타민, 아미노메틸 프로판올, 디에탄올아민, 디이소판올아민, 트리에탄올아민, 에틸렌디아민, 디이소프로필아민, 디에틸아민 및 이소프로판올아민으로 이루어진 군으로부터 선택되는 1종 이상인 약물 전달 장치.According to claim 4,
The thickener is at least one selected from the group consisting of hydroxypropyl cellulose, hydroxypropylmethyl cellulose, polyvinylpyrrolidone and ethyl cellulose,
The solubilizing agent is 2-amino-2-methyl-1,3-propanediol, aminomethyl propanediol, tromethamine, aminomethyl propanol, diethanolamine, diisophanolamine, triethanolamine, ethylenediamine, diisopropyl A drug delivery device comprising at least one selected from the group consisting of amine, diethylamine and isopropanolamine.
상기 마이크로니들은 NSAID 약물, 증점제 및 용해보조제를 포함하되, 이들 성분이 고형화된 것인 약물 전달 장치.micro needle; And a drug delivery device for treating arthritis comprising a support for supporting the microneedle,
The microneedle includes an NSAID drug, a thickener, and a solubilizing agent, wherein these components are solidified.
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR1020210148349A KR20230063270A (en) | 2021-11-01 | 2021-11-01 | A device for drug delivery comprising microneedle |
| PCT/KR2022/016948 WO2023075575A1 (en) | 2021-11-01 | 2022-11-01 | Drug delivery device comprising microneedles |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR1020210148349A KR20230063270A (en) | 2021-11-01 | 2021-11-01 | A device for drug delivery comprising microneedle |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20230063270A true KR20230063270A (en) | 2023-05-09 |
Family
ID=86158360
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020210148349A KR20230063270A (en) | 2021-11-01 | 2021-11-01 | A device for drug delivery comprising microneedle |
Country Status (2)
| Country | Link |
|---|---|
| KR (1) | KR20230063270A (en) |
| WO (1) | WO2023075575A1 (en) |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20190113143A (en) | 2018-03-27 | 2019-10-08 | 연세대학교 산학협력단 | Micro needle applicator |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2636673T3 (en) * | 2010-04-28 | 2017-10-06 | Kimberly-Clark Worldwide, Inc. | Device for the administration of rheumatoid arthritis medications |
| KR101798326B1 (en) * | 2016-04-07 | 2017-11-15 | 가천대학교 산학협력단 | Preparation apparatus for coated micro-needles |
| US20210060320A1 (en) * | 2017-12-28 | 2021-03-04 | Nichiban Co., Ltd. | Transdermal drug delivery system and method for using same |
| KR102093235B1 (en) * | 2019-03-20 | 2020-03-25 | 주식회사 쿼드메디슨 | Microneedles and methof of mamufacture |
| KR102435401B1 (en) * | 2019-08-13 | 2022-08-24 | 주식회사 쿼드메디슨 | A microneedle and the manufacturing method of the same |
-
2021
- 2021-11-01 KR KR1020210148349A patent/KR20230063270A/en active Search and Examination
-
2022
- 2022-11-01 WO PCT/KR2022/016948 patent/WO2023075575A1/en active Application Filing
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20190113143A (en) | 2018-03-27 | 2019-10-08 | 연세대학교 산학협력단 | Micro needle applicator |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2023075575A1 (en) | 2023-05-04 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| Saroha et al. | Transdermal patch: A discrete dosage form | |
| US8907153B2 (en) | Adhesive peel-forming formulations for dermal delivery of drugs and methods of using the same | |
| JP4592250B2 (en) | Novel pharmaceutical composition for administering N-0923 | |
| US4933184A (en) | Menthol enhancement of transdermal drug delivery | |
| KR101737960B1 (en) | Pharmaceutical composition for external use | |
| AU2017428907B2 (en) | Method of rapidly achieving therapeutic concentrations of zolmitriptan for treatment of migraines and cluster headaches | |
| JP2009518374A (en) | Transdermal administration of active agents, especially diclofenac | |
| KR20060120156A (en) | Method and apparatus for reducing the incidence of tobacco use | |
| JPH06507888A (en) | Medetomidine formulation for transdermal administration | |
| KR20070011469A (en) | Apparatus and method for transdermal delivery of fentanyl-based agents | |
| EP2777692B1 (en) | Composition for enhancing transdermal absorption of drug and patch preparation | |
| US11660265B2 (en) | Method of rapidly achieving therapeutic concentrations of triptans for treatment of migraines and cluster headaches | |
| KR20170000745A (en) | Soluble microneedle patch for photosensitizer delivery | |
| KR20230063270A (en) | A device for drug delivery comprising microneedle | |
| KR100437672B1 (en) | Release-controlled transdermal administration of risperidone | |
| EP0418341A4 (en) | Percutaneous drug delivery system | |
| US20090136554A1 (en) | Transdermal sustained release drug delivery | |
| Lunter et al. | Progress in Topical and Transdermal Drug Delivery Research—Focus on Nanoformulations | |
| KR20120056322A (en) | Transdermal system of zanamivir as active ingredient | |
| KR20240064153A (en) | A device for drug delivery comprising microneedle | |
| Vennapoosa et al. | Formulation and evaluation of a matrix-type Transdermal patch containing Rivastigmaine Tartarate | |
| KR100552651B1 (en) | Plaster comprising non-steroidal anti-inflammatory drugs | |
| KR20060123551A (en) | Transdermal delivery device for dihydropyridine type calcium antagonists containing at least one fatty acid | |
| Arkvanshi et al. | Transdermal delivery a preclinical and clinical perspective of drugs delivered via patches | |
| KR100535302B1 (en) | Tulobuterol-containing transdermal delivery preparation |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A201 | Request for examination |