JPS61502683A - Bandages for sustained release of drugs - Google Patents
Bandages for sustained release of drugsInfo
- Publication number
- JPS61502683A JPS61502683A JP60503039A JP50303985A JPS61502683A JP S61502683 A JPS61502683 A JP S61502683A JP 60503039 A JP60503039 A JP 60503039A JP 50303985 A JP50303985 A JP 50303985A JP S61502683 A JPS61502683 A JP S61502683A
- Authority
- JP
- Japan
- Prior art keywords
- bandage
- adhesive
- drug
- styrene
- microns
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 229940079593 drug Drugs 0.000 title claims description 65
- 239000003814 drug Substances 0.000 title claims description 65
- 238000013268 sustained release Methods 0.000 title description 2
- 239000012730 sustained-release form Substances 0.000 title description 2
- 239000000853 adhesive Substances 0.000 claims description 38
- 230000001070 adhesive effect Effects 0.000 claims description 38
- 239000008188 pellet Substances 0.000 claims description 30
- -1 polypropylene Polymers 0.000 claims description 17
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 claims description 13
- 229910052782 aluminium Inorganic materials 0.000 claims description 13
- 239000000463 material Substances 0.000 claims description 13
- 239000007787 solid Substances 0.000 claims description 13
- 239000004820 Pressure-sensitive adhesive Substances 0.000 claims description 12
- 239000010410 layer Substances 0.000 claims description 12
- 229920000728 polyester Polymers 0.000 claims description 12
- 239000011888 foil Substances 0.000 claims description 11
- 229920000468 styrene butadiene styrene block copolymer Polymers 0.000 claims description 9
- 239000012790 adhesive layer Substances 0.000 claims description 8
- 238000000034 method Methods 0.000 claims description 8
- VSKJLJHPAFKHBX-UHFFFAOYSA-N 2-methylbuta-1,3-diene;styrene Chemical compound CC(=C)C=C.C=CC1=CC=CC=C1.C=CC1=CC=CC=C1 VSKJLJHPAFKHBX-UHFFFAOYSA-N 0.000 claims description 7
- 239000004743 Polypropylene Substances 0.000 claims description 7
- 229920006243 acrylic copolymer Polymers 0.000 claims description 7
- FACXGONDLDSNOE-UHFFFAOYSA-N buta-1,3-diene;styrene Chemical compound C=CC=C.C=CC1=CC=CC=C1.C=CC1=CC=CC=C1 FACXGONDLDSNOE-UHFFFAOYSA-N 0.000 claims description 7
- 239000011248 coating agent Substances 0.000 claims description 7
- 238000000576 coating method Methods 0.000 claims description 7
- 229920001155 polypropylene Polymers 0.000 claims description 7
- 239000004698 Polyethylene Substances 0.000 claims description 6
- 229920000573 polyethylene Polymers 0.000 claims description 6
- 239000011347 resin Substances 0.000 claims description 6
- 229920005989 resin Polymers 0.000 claims description 6
- 229920001577 copolymer Polymers 0.000 claims description 5
- 239000004744 fabric Substances 0.000 claims description 5
- 239000002480 mineral oil Substances 0.000 claims description 5
- 235000010446 mineral oil Nutrition 0.000 claims description 5
- 229920003048 styrene butadiene rubber Polymers 0.000 claims description 5
- 229920000297 Rayon Polymers 0.000 claims description 4
- 239000003795 chemical substances by application Substances 0.000 claims description 4
- 239000003844 drug implant Substances 0.000 claims description 4
- 239000004745 nonwoven fabric Substances 0.000 claims description 4
- 229920006264 polyurethane film Polymers 0.000 claims description 4
- 239000002964 rayon Substances 0.000 claims description 4
- 229920005573 silicon-containing polymer Polymers 0.000 claims description 4
- 238000011200 topical administration Methods 0.000 claims description 4
- 239000004677 Nylon Substances 0.000 claims description 3
- 239000002174 Styrene-butadiene Substances 0.000 claims description 3
- MTAZNLWOLGHBHU-UHFFFAOYSA-N butadiene-styrene rubber Chemical compound C=CC=C.C=CC1=CC=CC=C1 MTAZNLWOLGHBHU-UHFFFAOYSA-N 0.000 claims description 3
- 229920001778 nylon Polymers 0.000 claims description 3
- 239000011115 styrene butadiene Substances 0.000 claims description 3
- 210000000434 stratum corneum Anatomy 0.000 claims 3
- 238000001647 drug administration Methods 0.000 claims 2
- WCVOGSZTONGSQY-UHFFFAOYSA-N 2,4,6-trichloroanisole Chemical compound COC1=C(Cl)C=C(Cl)C=C1Cl WCVOGSZTONGSQY-UHFFFAOYSA-N 0.000 claims 1
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 claims 1
- 239000005977 Ethylene Substances 0.000 claims 1
- 238000003475 lamination Methods 0.000 claims 1
- 238000004090 dissolution Methods 0.000 description 12
- TWBNMYSKRDRHAT-RCWTXCDDSA-N (S)-timolol hemihydrate Chemical compound O.CC(C)(C)NC[C@H](O)COC1=NSN=C1N1CCOCC1.CC(C)(C)NC[C@H](O)COC1=NSN=C1N1CCOCC1 TWBNMYSKRDRHAT-RCWTXCDDSA-N 0.000 description 7
- NIXOWILDQLNWCW-UHFFFAOYSA-N 2-Propenoic acid Natural products OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 7
- 239000000203 mixture Substances 0.000 description 7
- 239000005060 rubber Substances 0.000 description 7
- 229960004605 timolol Drugs 0.000 description 7
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 description 6
- 239000003522 acrylic cement Substances 0.000 description 6
- 229920001971 elastomer Polymers 0.000 description 6
- 238000004519 manufacturing process Methods 0.000 description 5
- 239000003381 stabilizer Substances 0.000 description 5
- SMZOUWXMTYCWNB-UHFFFAOYSA-N 2-(2-methoxy-5-methylphenyl)ethanamine Chemical compound COC1=CC=C(C)C=C1CCN SMZOUWXMTYCWNB-UHFFFAOYSA-N 0.000 description 4
- IMNFDUFMRHMDMM-UHFFFAOYSA-N N-Heptane Chemical compound CCCCCCC IMNFDUFMRHMDMM-UHFFFAOYSA-N 0.000 description 4
- 238000000338 in vitro Methods 0.000 description 4
- 239000011159 matrix material Substances 0.000 description 4
- 239000012528 membrane Substances 0.000 description 4
- 210000004379 membrane Anatomy 0.000 description 4
- IOLCXVTUBQKXJR-UHFFFAOYSA-M potassium bromide Chemical compound [K+].[Br-] IOLCXVTUBQKXJR-UHFFFAOYSA-M 0.000 description 4
- 238000012360 testing method Methods 0.000 description 4
- XTXRWKRVRITETP-UHFFFAOYSA-N Vinyl acetate Chemical compound CC(=O)OC=C XTXRWKRVRITETP-UHFFFAOYSA-N 0.000 description 3
- 239000000654 additive Substances 0.000 description 3
- 150000001875 compounds Chemical class 0.000 description 3
- 239000000126 substance Substances 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- NLHHRLWOUZZQLW-UHFFFAOYSA-N Acrylonitrile Chemical compound C=CC#N NLHHRLWOUZZQLW-UHFFFAOYSA-N 0.000 description 2
- PPBRXRYQALVLMV-UHFFFAOYSA-N Styrene Chemical compound C=CC1=CC=CC=C1 PPBRXRYQALVLMV-UHFFFAOYSA-N 0.000 description 2
- 210000000476 body water Anatomy 0.000 description 2
- 125000004432 carbon atom Chemical group C* 0.000 description 2
- 238000009792 diffusion process Methods 0.000 description 2
- 238000005538 encapsulation Methods 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 238000013508 migration Methods 0.000 description 2
- 230000005012 migration Effects 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 229960003733 phenylephrine hydrochloride Drugs 0.000 description 2
- OCYSGIYOVXAGKQ-FVGYRXGTSA-N phenylephrine hydrochloride Chemical compound [H+].[Cl-].CNC[C@H](O)C1=CC=CC(O)=C1 OCYSGIYOVXAGKQ-FVGYRXGTSA-N 0.000 description 2
- 229920001296 polysiloxane Polymers 0.000 description 2
- 230000002459 sustained effect Effects 0.000 description 2
- HBKBEZURJSNABK-MWJPAGEPSA-N 2,3-dihydroxypropyl (1r,4ar,4br,10ar)-1,4a-dimethyl-7-propan-2-yl-2,3,4,4b,5,6,10,10a-octahydrophenanthrene-1-carboxylate Chemical compound C([C@@H]12)CC(C(C)C)=CC1=CC[C@@H]1[C@]2(C)CCC[C@@]1(C)C(=O)OCC(O)CO HBKBEZURJSNABK-MWJPAGEPSA-N 0.000 description 1
- GOXQRTZXKQZDDN-UHFFFAOYSA-N 2-Ethylhexyl acrylate Chemical compound CCCCC(CC)COC(=O)C=C GOXQRTZXKQZDDN-UHFFFAOYSA-N 0.000 description 1
- HRPVXLWXLXDGHG-UHFFFAOYSA-N Acrylamide Chemical compound NC(=O)C=C HRPVXLWXLXDGHG-UHFFFAOYSA-N 0.000 description 1
- 239000004821 Contact adhesive Substances 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
- 229920002633 Kraton (polymer) Polymers 0.000 description 1
- CERQOIWHTDAKMF-UHFFFAOYSA-N Methacrylic acid Chemical compound CC(=C)C(O)=O CERQOIWHTDAKMF-UHFFFAOYSA-N 0.000 description 1
- VVQNEPGJFQJSBK-UHFFFAOYSA-N Methyl methacrylate Chemical compound COC(=O)C(C)=C VVQNEPGJFQJSBK-UHFFFAOYSA-N 0.000 description 1
- 235000010627 Phaseolus vulgaris Nutrition 0.000 description 1
- 244000046052 Phaseolus vulgaris Species 0.000 description 1
- 102000006335 Phosphate-Binding Proteins Human genes 0.000 description 1
- 108010058514 Phosphate-Binding Proteins Proteins 0.000 description 1
- QYKIQEUNHZKYBP-UHFFFAOYSA-N Vinyl ether Chemical compound C=COC=C QYKIQEUNHZKYBP-UHFFFAOYSA-N 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 239000000464 adrenergic agent Substances 0.000 description 1
- 125000005250 alkyl acrylate group Chemical group 0.000 description 1
- 125000000217 alkyl group Chemical group 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 239000002876 beta blocker Substances 0.000 description 1
- 229920001400 block copolymer Polymers 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 239000000470 constituent Substances 0.000 description 1
- 238000013270 controlled release Methods 0.000 description 1
- 230000003111 delayed effect Effects 0.000 description 1
- 239000006185 dispersion Substances 0.000 description 1
- 239000012738 dissolution medium Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 238000010348 incorporation Methods 0.000 description 1
- 238000002844 melting Methods 0.000 description 1
- 230000008018 melting Effects 0.000 description 1
- 150000002734 metacrylic acid derivatives Chemical class 0.000 description 1
- FQPSGWSUVKBHSU-UHFFFAOYSA-N methacrylamide Chemical compound CC(=C)C(N)=O FQPSGWSUVKBHSU-UHFFFAOYSA-N 0.000 description 1
- 239000003094 microcapsule Substances 0.000 description 1
- 239000000178 monomer Substances 0.000 description 1
- 210000004400 mucous membrane Anatomy 0.000 description 1
- 230000037311 normal skin Effects 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 239000004014 plasticizer Substances 0.000 description 1
- 229920006267 polyester film Polymers 0.000 description 1
- 229920002635 polyurethane Polymers 0.000 description 1
- 239000004814 polyurethane Substances 0.000 description 1
- 229920000915 polyvinyl chloride Polymers 0.000 description 1
- 239000004800 polyvinyl chloride Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 230000001681 protective effect Effects 0.000 description 1
- 239000013464 silicone adhesive Substances 0.000 description 1
- 231100000444 skin lesion Toxicity 0.000 description 1
- 206010040882 skin lesion Diseases 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 230000002747 voluntary effect Effects 0.000 description 1
- 239000002759 woven fabric Substances 0.000 description 1
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
- A61K9/70—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
- A61K9/703—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61F—FILTERS IMPLANTABLE INTO BLOOD VESSELS; PROSTHESES; DEVICES PROVIDING PATENCY TO, OR PREVENTING COLLAPSING OF, TUBULAR STRUCTURES OF THE BODY, e.g. STENTS; ORTHOPAEDIC, NURSING OR CONTRACEPTIVE DEVICES; FOMENTATION; TREATMENT OR PROTECTION OF EYES OR EARS; BANDAGES, DRESSINGS OR ABSORBENT PADS; FIRST-AID KITS
- A61F13/00—Bandages or dressings; Absorbent pads
- A61F13/02—Adhesive bandages or dressings
- A61F13/023—Adhesive bandages or dressings wound covering film layers without a fluid retention layer
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61F—FILTERS IMPLANTABLE INTO BLOOD VESSELS; PROSTHESES; DEVICES PROVIDING PATENCY TO, OR PREVENTING COLLAPSING OF, TUBULAR STRUCTURES OF THE BODY, e.g. STENTS; ORTHOPAEDIC, NURSING OR CONTRACEPTIVE DEVICES; FOMENTATION; TREATMENT OR PROTECTION OF EYES OR EARS; BANDAGES, DRESSINGS OR ABSORBENT PADS; FIRST-AID KITS
- A61F13/00—Bandages or dressings; Absorbent pads
- A61F13/02—Adhesive bandages or dressings
- A61F13/023—Adhesive bandages or dressings wound covering film layers without a fluid retention layer
- A61F13/0243—Adhesive bandages or dressings wound covering film layers without a fluid retention layer characterised by the properties of the skin contacting layer, e.g. air-vapor permeability
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61F—FILTERS IMPLANTABLE INTO BLOOD VESSELS; PROSTHESES; DEVICES PROVIDING PATENCY TO, OR PREVENTING COLLAPSING OF, TUBULAR STRUCTURES OF THE BODY, e.g. STENTS; ORTHOPAEDIC, NURSING OR CONTRACEPTIVE DEVICES; FOMENTATION; TREATMENT OR PROTECTION OF EYES OR EARS; BANDAGES, DRESSINGS OR ABSORBENT PADS; FIRST-AID KITS
- A61F13/00—Bandages or dressings; Absorbent pads
- A61F13/02—Adhesive bandages or dressings
- A61F13/0246—Adhesive bandages or dressings characterised by the skin-adhering layer
- A61F13/0253—Adhesive bandages or dressings characterised by the skin-adhering layer characterized by the adhesive material
-
- 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
- A61K9/703—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
- A61K9/7084—Transdermal patches having a drug layer or reservoir, and one or more separate drug-free skin-adhesive layers, e.g. between drug reservoir and skin, or surrounding the drug reservoir; Liquid-filled reservoir patches
Landscapes
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Dermatology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Heart & Thoracic Surgery (AREA)
- Vascular Medicine (AREA)
- Biomedical Technology (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Medicinal Preparation (AREA)
Abstract
(57)【要約】本公報は電子出願前の出願データであるため要約のデータは記録されません。 (57) [Summary] This bulletin contains application data before electronic filing, so abstract data is not recorded.
Description
【発明の詳細な説明】 薬剤の徐放用包帯 １豆立且１ 本発明は、経皮または局所投与された薬剤の制御された放出用包帯および系に関 し、さらに詳しくは患者の正常の皮膚水分が薬剤の溶解および放出を行う改良さ れた包帯に関する。[Detailed description of the invention] Bandages for sustained release of drugs 1 bean stand and 1 The present invention relates to dressings and systems for the controlled release of transdermally or topically administered drugs. and more specifically, the patient's normal skin moisture improves drug dissolution and release. Concerning bandages.
発明の背景 本出願および添付請求の範囲において用いられるように、「薬剤」の語は、その 最も広い意味において、治療の目的に適用される局所的あるいは全身的な任意の タイプのすべての薬剤に適用するように企図される。Background of the invention As used in this application and the appended claims, the term "drug" In the broadest sense, any local or systemic treatment applied for therapeutic purposes. It is intended to apply to all types of drugs.
近年、着用者の皮膚または粘膜への薬剤の放出に企図された多くの包帯が提供さ れて来た。このような先行包帯の１群は、特別の活性剤の、皮膚病変などと直接 接触する感圧接着剤への混入を教示する、米国特許第３．６３２．７４０号、第 ３．７６９．０７１号および第３・。In recent years, a number of bandages have been offered that are designed to release drugs into the skin or mucous membranes of the wearer. It came. One group of such advanced dressings is the use of special active agents, which are applied directly to skin lesions, etc. No. 3,632,740, which teaches incorporation into contacting pressure sensitive adhesives. No. 3.769.071 and No. 3.
８９６．７８９号明細書によって示されている。これらの包帯は、放出速度の制 御手段を有さず、また薬剤と皮膚の直接接触の故に多くの用途には好ましくなか った。No. 896.789. These bandages are designed to control the rate of release. It is undesirable for many applications because of the lack of control measures and the direct contact of the drug with the skin. It was.
先行包帯の他の群は、米国特許第３，５９８．１２２号および第４，０６９，３ ０７号明細書によって示された特に企図された拡散膜および薬剤溜めを用いた。Other groups of prior bandages include U.S. Pat. Nos. 3,598,122 and 4,069,3. The specifically designed diffusion membrane and drug reservoir shown by the '07 patent were used.
これらの包帯は、複雑、高価であり、しかも困難かつ正確な製造技術を伴った。These bandages were complex, expensive, and involved difficult and precise manufacturing techniques.
薬剤溜めの種々の検討の結果は薬剤の微粒子のマイクロカプセル化および層状構 造の不連続層を含むマトリックス内のマイクロカプセルの分散に到達した。この ような包帯の代表は、米国特許第３，９９６．９３４号および第３．５９８，１ ２３号明細書である。再び、このような包帯は、複雑、高価かつ製造困難である 。The results of various studies on drug reservoirs indicate the microencapsulation and layered structure of drug particles. The dispersion of microcapsules within a matrix containing discontinuous layers of structure was reached. this Representatives of such bandages are U.S. Pat. Nos. 3,996,934 and 3,598,1 This is Specification No. 23. Again, such bandages are complex, expensive and difficult to manufacture. .
米国特許第４．２８６．５９２号明細書には、薬剤が溶解キャリヤーマトリック スに分散された他の積層品包帯が教示され、しかも薬剤の溶解速度および投与速 度を制御する接着剤の使用が論じられている。ここで、また包帯は複雑かつ高価 であり、しかも特別の製造パラメーターが必要であった。U.S. Pat. No. 4,286,592 discloses that the drug is dissolved in a carrier matrix. Other laminate dressings have been taught that are dispersed in a liquid, and that also improve drug dissolution and administration rates. The use of adhesives to control the degree is discussed. Here, also the bandage is complicated and expensive Moreover, special manufacturing parameters were required.
一層簡単な包帯は、米国特許第４．３０７，７１７号明ｍｓに示されているが、 なお薬剤はマトリックスに分散され、しかも溶解速度の制御の問題を扱っていな かった。A simpler bandage is shown in U.S. Pat. No. 4,307,717, but Note that the drug is dispersed in a matrix, and the problem of controlling dissolution rate is not addressed. won.
及ｒｇ４ｏυＬＦＥ 本発明は、長期間にわたって持続した実質的に一定の放出速度は固体形の薬剤を 用いて得られるという発見から生じる。その最も広い形態において、本発明の包 帯は液体不透過性裏材、固体薬剤、好ましくはペレット形および透湿性皮膚接触 接着剤のみを含む。固体薬剤の制御された溶解速度は、着用者の皮膚から発散す る水または水蒸気とのその接触から生じる。and rg4oυLFE The present invention provides that a sustained substantially constant release rate over an extended period of time is arises from the discovery that it can be obtained using In its broadest form, the invention encompasses The strip has a liquid-impermeable backing, a solid drug, preferably in pellet form and a moisture-permeable skin contact Contains only adhesive. The controlled dissolution rate of the solid drug allows it to evaporate from the wearer's skin. resulting from its contact with water or steam.
固体薬剤は、その純粋な形で使用でき、しかも添加された賦形剤、マトリックス または溶、解キャリヤーは必要ない。得られた有益な結果は、身体水分とその中 への薬剤の溶解性の相関関係およびこのような水分が接着剤を通して薬剤まで通 り、かつ溶解した薬剤は接着剤を通して患者の皮膚まで戻ることができることか ら得られる。Solid drugs can be used in their pure form and without added excipients, matrices. Or dissolving, no dissolving carrier is required. The beneficial results obtained are due to the fact that body water and The relationship between the solubility of the drug and the ability of such moisture to pass through the adhesive to the drug. and that the dissolved drug can return to the patient's skin through the adhesive. obtained from
、溶解速度のこれ以上の制御は多くの方法で得ることができる。１つの方法は、 ゛接着剤の組成および（または）その厚さを変えることによるものである。他の 方法は、接着剤を、薬剤が可溶性であるが、患者の身体水分におけるよりも多少 可溶性で、あるビヒクルに混入することである。, further control of dissolution rate can be obtained in a number of ways. One method is By changing the composition of the adhesive and/or its thickness. other The method uses an adhesive so that the drug is soluble, but somewhat less so than in the patient's body water. It is soluble and can be incorporated into certain vehicles.
包帯はまた、接着剤用のキャリヤーウェブを含有してもよい。このキャリヤーウ ェブ材料は、また溶解速度に影響をおよぼすように選ぶことができる。そのあら ゆる形の中で、本発明の包帯′は簡単、有効であり、製造が安価でしかも薬剤溜 め、マトリックス、マクロカプセル北、拡散膜などの先行技術の装置の好ましく ない特徴を除く。The bandage may also contain a carrier web for the adhesive. This carrier The web material can also be selected to affect the rate of dissolution. That's it In all forms, the bandage of the present invention is simple, effective, inexpensive to manufacture, and has no drug reservoir. Preferably of prior art devices such as membranes, matrices, macrocapsules, diffusion membranes, etc. Except for no features.
本発明の他の特徴および利点は、下記の記載および特許請求の範囲から明らかで あり、しかも本発明の好ましい特徴およびその原理を具体化する構造を示す添付 図面に具体的に説明される。Other features and advantages of the invention will be apparent from the following description and claims. and the attachments illustrating preferred features of the invention and structures embodying its principles. This is specifically explained in the drawings.
図面の簡単な説明 第１図は、接着剤層の１部を切欠いて内部構造を示す、本発明の原理を具体化す る包帯の斜視図である。Brief description of the drawing FIG. 1 shows an embodiment of the principle of the invention, with a portion of the adhesive layer cut away to show the internal structure. FIG.
第２図は、第１図の線２−２の面上で取った拡大縦断面図であり； 第３図は、包帯の変形の同様な図であり、第４図は、包帯の他の変形の同様な図 であり、かつ第５図は、２種の代表的薬剤の溶解を時間に対してプロットしたグ ラフであり、例１．２および３の包帯用の薬剤はチモロール（ｔｉｍｏｌｏｌ） であり、例４の包帯用薬剤は塩酸フェニレフリン（ｐｈｅｎｙｌｅｐｈｒｉｎｅ ｈｙｄｒｏｃｈｌｏｒｉｄｅ ）である。FIG. 2 is an enlarged longitudinal cross-sectional view taken on the plane of line 2--2 of FIG. 1; FIG. 3 is a similar illustration of a variant of the bandage, and FIG. 4 is a similar illustration of another variant of the bandage. and Figure 5 is a graph plotting the dissolution of two representative drugs against time. The drug for the dressings of Examples 1.2 and 3 is timolol. The dressing agent of Example 4 was phenylephrine hydrochloride. Hydrochloride).
明の好ましい実ＩＭ態様の嘗 図面の種々の図を一層詳細に参照して、第１図および明の基本包帯構造が図示さ れる。包帯１０は、可撓性液体不透過性裏材層またはシート１２を含む。裏材シ ート１２を選んで、薬剤のその中の移行を防ぎしかも適用した場合に薬剤の位置 方向拡散を確保する。これについ−で、裏材シートは、気体不透過性および液体 不透過性であってもよく、この裏材シートはその溶解または気化状態の薬剤不透 過性であることのみが必要である。仁のために、アルミニウムはく、ポリエステ ル、ポリプロピレン、ポリエチレン、ポリウレタンフィルム、およびアルミニウ ムはくとポリエステルの積層品を初め種々の薄いシート状材料が適している。望 ましくは、基材シート１２は厚さ６ミクロン〜５０ミクロンの範囲内を有し、薄 くかつ可撓性である。Preferred embodiments of actual IM Referring in more detail to the various figures of the drawings, the basic bandage structure of FIG. 1 and Ming is illustrated. It will be done. Bandage 10 includes a flexible liquid-impermeable backing layer or sheet 12 . Backing material 12 to prevent migration of the drug therein and to improve the location of the drug when applied. Ensure directional spread. In this regard, the backing sheet is gas-impermeable and liquid-impermeable. The backing sheet may be impermeable to the drug in its dissolved or vaporized state. It only needs to be hypersexual. For the sake of strength, aluminum foil, polyester film, polypropylene, polyethylene, polyurethane film, and aluminum film. Various thin sheet materials are suitable, including laminates of membrane and polyester. Desire Preferably, the base sheet 12 has a thickness in the range of 6 microns to 50 microns, and is thin. It is compact and flexible.
裏材シート１２上に１．圧縮された固体薬剤製の薄いペレット１４が位置する。1 on the backing sheet 12. A thin pellet 14 of compressed solid drug is located.
固体薬剤ベレット１４は、実質的に円形の形状であり、しかもペレットの厚さよ りも実質的に大きい寸法の内面１６を有し得る。これについて、ペレット１４は 直径０．５α〜１０αの範囲、厚さ５ミクロン〜ｉ、ｏｏｏミク１０ンの範囲で あってもよく、しかも質１１■〜１．０ＯＯｆｌ！９を有する。比較的大きい表 面積１６の意味は、説明が進むに伴って明らかになる。The solid drug pellet 14 is substantially circular in shape and has a thickness similar to that of the pellet. The inner surface 16 may also have substantially larger dimensions. Regarding this, pellet 14 is In the range of diameter 0.5α to 10α, thickness of 5 microns to i, ooo micron of 10 nm. It's okay, and the quality is 11■~1.0OOfl! It has 9. relatively large table The meaning of area 16 will become clear as the explanation progresses.
皮膚接触接着剤１８の層は、ペレット１４を覆い、しかもペレット１４を基材シ ート１２上に保持する。１１１８は、アクリル系共重合体、スチレン−ブタジェ ン−スチレン、スチレン−イソプレン−スチレンおよびシリコーン重合体のよう な従来・の感圧接着剤の何れかを含んでもよく、また粘着付与樹ｌをも含有して もよい。A layer of skin-contact adhesive 18 covers pellet 14 and also connects pellet 14 to the substrate sheet. hold it on the port 12. 1118 is an acrylic copolymer, styrene-butadiene -styrene, styrene-isoprene-styrene and silicone polymers. It may contain any of the conventional pressure sensitive adhesives and may also contain a tackifier. Good too.
アクリル系接着剤は、゛当業界において既知の種々の感圧接着剤共重合体から選 ばれてもよい。慨して、有用な感圧接着剤としては、アクリル酸および（または ）メタクリル酸、メタクリル酸メチルおよびアクリル酸２−エチル−ヘキシルの ような１個〜１０個の炭素原子を含有するアルキルアクリレートおよびアルキル メタクリレートエステル、アクリルアミドおよびメタクリルアミドおよび酢酸ビ ニル、アクリロニトリルおよびプロごルビニルエーテルのような１個〜１０個の 炭素原子を含有するアルキルビニルエーテルのような追加共１合可能七ノエチレ ン系不飽和単り体の共重合体がある。The acrylic adhesive may be selected from a variety of pressure sensitive adhesive copolymers known in the industry. It doesn't matter if it's found out. Generally, useful pressure sensitive adhesives include acrylic acid and/or ) of methacrylic acid, methyl methacrylate and 2-ethyl-hexyl acrylate. Alkyl acrylates and alkyl containing 1 to 10 carbon atoms such as Methacrylate esters, acrylamide and methacrylamide and vinyl acetate from 1 to 10 such as acrylonitrile, acrylonitrile, and progol vinyl ether. Additional compounds such as alkyl vinyl ethers containing carbon atoms There are copolymers of monounsaturated monomers.
さらに詳しくは、感圧アクリル系接着剤は、モンサンド製のゲルヴア（Ｇｅｌｖ ａ ） ＲＡ −７８８、エイブリー・ケミカル（Ａｖｅｒｙ Ｃｈｅｍｉｃａ ｌ） 製のＡＳ−３５１およびアシュランド製のエアロセット（Ａｅｒｏｓｅｔ ） １０８５のような商標または商品名の下に販売されている、アクリル酸２ −エチル−ヘキシル、酢酸ビニルおよびアクリル酸の共重合体を含んでもよい。More specifically, the pressure-sensitive acrylic adhesive is Gelv a) RA-788, Avery Chemical l) AS-351 manufactured by AS-351 and Aeroset manufactured by Ashland. ) Acrylic acid 2, sold under trademarks or trade names such as 1085 -Copolymers of ethyl-hexyl, vinyl acetate and acrylic acid may also be included.
感圧ゴムをベースとする接着剤は、同様に、スチレン−ブタジェン−スチレン（ ＳＢＳ）および（または）スチレン−イソプレン−スチレン（ＳＩＳ）ブロック 共重合体、１種またはそれ以上の可塑剤および安定剤の種々のコンパウンドから 選ばれてもよい。このような感圧接着剤としテハ、クラトン（Ｋｒａｔｏｎ＞ １１０１ （ＳＯ３）ま−たは１１０７（ＳＩＳ）（シェル・ケミカル・カンパ ニー）のようなゴムをベースとするブロック共重合体、ヘルコリン（Ｈｅｒｃｏ ｌｙｎ） Ｄ 、ピッコライト（Ｐｉｃｃｏｌｙｔ−ｅ ）Ａ−１１５、スタビ ライト−エステル（５ｔａｂｉ ｌ １ｔｅＥｓｔｅｒ ） １０およびフオシ ル（Ｆｏｒａｌ ） ８５のような商標またｔよ商品名の下に販売されている１ 種またはそれ以上の粘着付与樹脂および適当な安定剤のコンパウンドを含んでも よい。Adhesives based on pressure-sensitive rubber are likewise styrene-butadiene-styrene ( SBS) and/or styrene-isoprene-styrene (SIS) blocks From various compounds of copolymers, one or more plasticizers and stabilizers May be selected. Such pressure-sensitive adhesives include Teha and Kraton. 1101 (SO3) or 1107 (SIS) (Shell Chemical Company) Rubber-based block copolymers such as Herco lyn) D, Piccolyt-e A-115, Stabilizer Light-ester (5tabi l 1teEster) 10 and fosi 1 sold under trademarks and trade names such as Foral 85. may contain a compound of species or more tackifying resins and suitable stabilizers. good.
さらにとりわけ、感圧ゴムをベースとした接着剤は、スチレン−ブタジェン−ス チレンまたはスチレン−イソプレン−スチレン１０％〜３０％、粘着付与樹脂３ ０％〜７０％および安定剤１％〜３％を含んでもよい。More particularly, adhesives based on pressure-sensitive rubber are styrene-butadiene-based. Styrene or styrene-isoprene-styrene 10% to 30%, tackifying resin 3 It may contain 0% to 70% and 1% to 3% stabilizer.
シリコーン接着剤ｔｉｔ、ダウ・コーニング３５５およびゼネラル・エレクトリ ック製のＰＳＡ５９５またはＰＳＡ６５７４のような商標または商品名の下に販 売された型の部分縮合されたシリコーンガムおよび樹脂の溶媒溶液を含んでもよ い。Silicone adhesive tit, Dow Corning 355 and General Electric sold under trademarks or trade names such as PSA595 or PSA6574 manufactured by May contain solvent solutions of partially condensed silicone gums and resins of the marketed type. stomach.
接着剤層１８の厚さおよび組成は、後に記載される薬剤ぺＩＩフット４の溶解速 度の制御に影響をおよぼすことが見いだされた。従って、アクリル系接着剤によ り、ゴムをベースとする接着剤よりも迅速な溶解速度が可能になることが分かり 、しかも接着剤は同様に粘着付与樹脂または他の添加剤または充てん剤を含有し てもよい。厚さ１０ミクロン〜１５０ミクロンの接着剤層は、関連する特別の薬 剤および適用によって有効であることが分かった。接着剤Ｗ１１８は、記載され る例から分かるように薬剤溶解ビヒクルの添加によってさらに変性できる。The thickness and composition of the adhesive layer 18 depend on the dissolution rate of the drug Pe II foot 4 described later. was found to have an effect on the control of temperature. Therefore, acrylic adhesive was found to enable faster dissolution rates than rubber-based adhesives. , and the adhesive also contains tackifying resins or other additives or fillers. It's okay. The adhesive layer, which is between 10 microns and 150 microns thick, is It has been found to be effective depending on the agent and application. Adhesive W118 is described As can be seen from the example above, further modification can be achieved by the addition of a drug dissolution vehicle.
粉末形の圧縮可能または取扱い可能の任意の固体薬−剤は、どのような添加剤の 添加もなしにその純粋な形で使用できる。一般に、薬剤は、約１５０’Ｃ未満の 比較的低融点を有し、しかも比較的水溶性である。チモロールおよび塩酸フェニ レフリンのようなアドレナリン作動剤をもって満足すべき結果が得られた。Any solid drug that is compressible or handleable in powder form may contain any additives. It can be used in its pure form without any additives. Generally, the drug is less than about 150'C It has a relatively low melting point and is relatively water soluble. Timolol and phenychloride Satisfactory results have been obtained with adrenergic agents such as Refrin.
第３図においては、接着剤層１８がキャリヤーウェブ２０の外部被覆を含む、包 帯１ｏの変性形を図示する。In FIG. 3, the adhesive layer 18 is shown in a package comprising an outer coating of carrier web 20. Figure 3 illustrates a modified form of band 1o.
示すように、キャリヤーウェブは、同様にその内側またはペレット側の上を接着 剤１９の層をもって被覆される。The carrier web is similarly glued on its inside or pellet side as shown. It is coated with a layer of agent 19.
接着剤層１９は、厚さ２０ミクロン〜３００ミクロンで変わってもよく、しかも 層１８と同じでもよいかあるいは異なった接着剤を含んでもよい。好ましくは、 キャリヤーウェブ２ｏは、ナイロン、ポリエチレン、ポリプロピレン、レーヨン 、セルロース−レーヨンまたはポリエステルヲ含み、しかも布ｆｉｆｆ１１ ｇ ｍ／ｍ２〜１００ｇｍ／ｍ ＠有ｔル。１ｆｆ１０．５９ｍ／７７Ｌ２〜ｉ ｏ ｏｇｍ、’ＴｒＬ２を有するガーゼまたはセルロース系材料の不織布もまた使用 できる。キャリヤーウェブ材料の選択は、構成材料の極性に明らかに関連する溶 解速度に影響をおよぼし得る。従って、例えばナイロンのような比較的極性分子 製のキャリヤーは溶解速度を遅くす°る傾向のあることが見いだされた。The adhesive layer 19 may vary in thickness from 20 microns to 300 microns, and Layer 18 may include the same or a different adhesive. Preferably, Carrier web 2o is made of nylon, polyethylene, polypropylene, rayon. , contains cellulose-rayon or polyester, and has 11 g of cloth m/m2~100gm/m @with. 1ff10.59m/77L2~i o Non-woven fabrics of gauze or cellulosic materials with ogm,’TrL2 are also used can. The choice of carrier web material is clearly related to the polarity of the constituent materials. Can affect solution speed. Therefore, relatively polar molecules such as nylon It has been found that carriers made of aluminum tend to slow down the rate of dissolution.
第４図においては、包帯１０の他の変性形を図示する。In FIG. 4, another modified version of bandage 10 is illustrated.
この実施態様において、不透過性基材シート１２は、外層２２によって覆われて 、仕上げされた触感、外観お−よび着用適性を包帯に与える。外層２２は、可撓 性、順応性、軽量および快適に着用できなければならない。これついて、外層２ ２は、ポリエチレン、ポリプロピレン、ポリ塩化ビニルおよびポリウレタンのｒ ！ｊＩＮ性フィルム、またはキャリヤーウェブ１８と同じ組成の非閉塞性織布ま たは不織布あるいは挙げた材料の何れかの穿孔フィルムを含み、しかも厚さ１０ ミクロン〜２００ミクロンの範囲であってもよい。In this embodiment, the impermeable base sheet 12 is covered by an outer layer 22. , giving the bandage a finished feel, appearance and wearability. The outer layer 22 is flexible. It must be flexible, adaptable, lightweight and comfortable to wear. Regarding this, outer layer 2 2 is polyethylene, polypropylene, polyvinyl chloride and polyurethane r ! jIN film, or a non-occlusive woven fabric having the same composition as the carrier web 18. or non-woven fabric or a perforated film of any of the listed materials, and has a thickness of 10 It may range from microns to 200 microns.
最終仕上げとして、包帯１０は保護ライナー（図示ぜ。As a final touch, bandage 10 is fitted with a protective liner (shown).
ず）、例えば感圧層１８に剥離可能に接着された、当業界において既知のシリコ ーンまたはポリフルオロエチレン被覆剥離ライナーを含有するのが好ましい。こ のようなライナーは、厚さ約２５ミクロン〜２００ミクロンの紙またはフィルム 製であってもよく、しかも使用前の接着剤を保護し、かつ貯蔵中接着剤中の薬剤 移行を防止する。), e.g. a silicone material known in the art, releasably adhered to the pressure sensitive layer 18. Preferably, the release liner includes a rubber or polyfluoroethylene coated release liner. child A liner such as paper or film approximately 25 microns to 200 microns thick The adhesive may be made of a material that protects the adhesive before use and prevents chemicals in the adhesive during storage. Prevent migration.
下記の例は、本発明を具体的に説明するが、本発明を何ら限定するとは意図され ない。The following examples illustrate the invention but are not intended to limit the invention in any way. do not have.
例１ β−アドレナリン作動性遮断剤のチモロールを８０時間をこえる時間経皮的に投 与する包帯を下記のように製造した。チモロールの５０■のウェーハ状ペレット を、標準臭化カリウムペレットプレスにおいて製造し、実質的円形ペレットは直 径約１．２５αおよび厚さ約３５０ミクロンを有した。薬剤ペレットを、厚さ５ ０ミクローンのアルミニウムはく上に載置し、次いでこれに厚さ５０ミクロンの アクリル系接着剤の層を被せ、前記接着剤を、固形分４０％〜５０％において溶 液（トルエン、ヘプタン）から塊法型し、ここでアクリル系画分はアクリル酸２ −エチル−ヘキシル、酢酸ビニルおよびアクリル酸の反応によって製造されたア クリル系共重合体を含む。生体外剥離試験は、ｐｌ＋７．４のホスフェート綴器 溶液をもって標準装置および技術、すなわち標準Ｕ、Ｓ、Ｐ、２型溶解装置を用 いた包帯について行われた。薬剤の一定放出は、８０時間を越える時間にわたっ て接続し、その後放出は著しり遅りなり、次いで薬剤は実質的に使い尽くされた 。４時間〜７２時間、薬剤放出は直線速度に近チモロール投与用包帯を製造した 。例１におけるように、薬剤の５０ηベレツトを製造し、次いで厚さ５０ミクロ ンのアルミニウムはく上に載置した。次いで、ベレットに、鉱油５％を含有する 粘着付与されたスチレン−ブタジェン−スチレン感圧接着剤を被せ、前記接着剤 を固形分４０％〜５０％において溶液（トルエン、ヘプタン）から塊法型し、こ こでゴム画分は、スチレン−ブタジェン−スチレンブロック共重合体１８％、ラ ンダムスチレン−ブタジェン共重合体１５％、粘着付与樹ｒＭ６１％鉱油５％お よび安定剤１％のコンパ１クンドを含む。Example 1 The beta-adrenergic blocker timolol is administered transdermally for more than 80 hours. The dressings provided were manufactured as follows. 50 wafer shaped pellets of Timolol were produced in a standard potassium bromide pellet press, and substantially circular pellets were produced directly. It had a diameter of about 1.25α and a thickness of about 350 microns. Drug pellets, thickness 5 0 micron aluminum foil, which is then covered with a 50 micron thick A layer of acrylic adhesive is applied, and the adhesive is dissolved at a solids content of 40% to 50%. The acrylic fraction is extracted from a liquid (toluene, heptane) using the bulk method. - Acrylic acid produced by the reaction of ethyl-hexyl, vinyl acetate and acrylic acid Contains acrylic copolymer. In vitro peel test was performed using phosphate binding device with pl+7.4. Using standard equipment and techniques, i.e., standard U, S, P, Type 2 dissolution equipment, with the solution This was done on the bandage that was used. Constant release of drug over a period of over 80 hours after which the release was significantly delayed and the drug was essentially used up. . From 4 hours to 72 hours, drug release was close to linear in the preparation of timolol administration bandages. . As in Example 1, a 50 η pellet of drug was prepared and then 50 microns thick. It was placed on top of an aluminum foil. The pellets were then loaded with 5% mineral oil. Cover with a tackified styrene-butadiene-styrene pressure sensitive adhesive, was molded from a solution (toluene, heptane) at a solid content of 40% to 50% using the bulk method. Here, the rubber fraction consists of 18% styrene-butadiene-styrene block copolymer and rubber fraction. 15% dam styrene-butadiene copolymer, 61% tackifying resin rM, 5% mineral oil. and 1% Compa 1 Kundo stabilizer.
比較のために、チモロールの溶解度は、水中的８１１１！Ｆ／“ｄおよび鉱油巾 約４■／−である。同じ標準生体外剥離試験において、薬剤の実質的に一定の放 出が１２０時間を越える時間持続し、その後放出は著しく遅くなり、次いで薬剤 は実質的に使用し尽くされた。８時間〜１００時間、薬剤放出は、直線速度に近 づいた。For comparison, the solubility of timolol in water is 8111! F/“d and mineral oil wipes It is about 4■/-. In the same standard in vitro peel test, virtually constant release of drug was observed. The release lasts for more than 120 hours, after which the release slows down significantly and then the drug has been virtually exhausted. From 8 to 100 hours, drug release was close to linear rate. I found it.
例３ チモロールの投与用包帯を、薬剤のベレットを製造し、次いでこのベレツｉ〜を 例１および例２のようにアルミニウムはく上に載置することによって製造した。Example 3 A bandage for administration of timolol is prepared by manufacturing a drug beret, and then applying this beret to Manufactured as in Examples 1 and 2 by mounting on aluminum foil.
次いで、このベレットに、布ｆｆ１ｆｆｉ１９．９ｚｒｒＬ／ＴｒＬ２を有する 不織ポリエステル製の接着キャリヤーウェアを被せた。このキャリヤーウェブを 、ベレット側に、厚さ２５ミクロンの例１におけると同じ組成を有するアクリル 系接着剤をもって、かつ非ペレットまたは皮膚接触側を厚さ５０ミクロンの同じ 組成のアクリル系接着剤をもってあらかじめ被覆した。同じ標準生体外剥離試験 において、薬剤の実質的に一定の放出は、１２ＯＲ間を越える時間持続し、その 後、放出は著しく遅くなり、次いで薬剤は実質的に使い尽くされた。１５時間〜 ９６時間、薬剤放出は直線速度に近づいた。Then, this beret has cloth ff1ffi19.9zrrL/TrL2. Covered with adhesive carrier wear made of non-woven polyester. This carrier web , on the pellet side, an acrylic having the same composition as in Example 1 with a thickness of 25 microns. 50 micron thick on the non-pellet or skin contact side. It was pre-coated with an acrylic adhesive of the same composition. Same standard in vitro peel test , the substantially constant release of the drug lasts for more than 12 ORs and that Afterwards, the release slowed significantly and the drug was then essentially exhausted. 15 hours~ At 96 hours, drug release approached a linear rate.
例４ 薬剤塩酸フェニレフリンの投与用包帯を、下記の様に製造した。薬剤の７０■の ウェーハ状ベレットを標準臭化カリウム ベレットプレスにおいて製造し、実質 的に円形のベレットは直径約１．２５１ＪおよびＩｆざ杓３５−〇ミクロンを有 した。薬剤ベレットを厚さ５０ミクロンのアルミニウムはく上にｌ！！した。こ れに、布ｆｆ１ｆｉ１９．９ｇＴｒＬ／ｒｒＬ２を有する不織ポリエステル製の 接着キャリヤーウェブを被せた。このキャリヤーウェブは、ベレット側に厚さ２ ５ミクロンの例２におけると同じ組成を有する粘着付与されたスチレン−ブタジ ェン−スチレン感圧接着剤を、かつ非ペレットまたは皮膚接触側に厚さ５０ミク ロンの例１におけると同じ組成を有するアクリル系接着剤をもって被覆した。同 じ標準生体外剥離試験において、薬剤の実質的に一定の放出は、３５時間を越え る時間持続し、その後薬剤放出は著しく遅（なり、次いで、薬剤は実質的に使い 尽くされた。約１時間〜３２時間、薬剤放出は直線速度に近づいた。Example 4 A dressing for administration of the drug phenylephrine hydrochloride was manufactured as follows. 70■ of drugs The wafer-like pellets are manufactured in a standard potassium bromide pellet press, and the The generally circular pellet has a diameter of approximately 1.251J and a diameter of 35-0 microns. did. Place the drug pellet on a 50 micron thick aluminum foil! ! did. child In addition, a non-woven polyester fabric with fabric ff1fi19.9gTrL/rrL2 Covered with adhesive carrier web. This carrier web has a thickness of 2 mm on the pellet side. Tackified styrene-butadiene with the same composition as in Example 2 for 5 microns 50 μm thick on the non-pellet or skin contact side. It was coated with an acrylic adhesive having the same composition as in Ron's Example 1. same In the same standard in vitro peel test, substantially constant release of drug was observed over 35 hours. for a period of Exhausted. From about 1 hour to 32 hours, drug release approached a linear rate.
前記から、本発明は、長期間にわたって薬剤の持続した経皮または局所投与用の 簡単、有効かつ安価な包帯を提供することが分かる。固体薬剤の使用によって、 この型の包帯にこれまで必要であった型のすべてのマトリックス、カプセル化お よび溶解媒質が除かれる。「包帯」の用語は、その包括的意味においてその形態 または形状がどのようであっても、任意の皮膚接着装置にも適用するように用い られると理解されたい。本°明細書においては好ましい実ｍ態様が具体的に説明 および記載されたが、添付請求の範囲の精神および範囲から逸脱することなく当 業者によって変化および改変をなし得る。本発明は下記請求の範囲に規定される 。From the foregoing, the present invention provides a method for sustained transdermal or topical administration of drugs over long periods of time. It can be seen that it provides a simple, effective and inexpensive bandage. By using solid drugs, All the matrix, encapsulation and encapsulation of the type previously required for this type of bandage and the dissolution medium is removed. The term "bandage" in its inclusive sense refers to the form of or used to apply to any skin adhesive device, no matter how it is shaped. I want to be understood. In this specification, preferred embodiments are specifically explained. and as described herein, without departing from the spirit and scope of the appended claims. Variations and modifications may be made by manufacturers. The invention is defined in the following claims. .
手続補正書（自発） 昭和６１年Ｚ月２０Procedural amendment (voluntary) Z month 20, 1986
Claims (30)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US62857784A | 1984-07-06 | 1984-07-06 | |
| US628577 | 1984-07-06 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPS61502683A true JPS61502683A (en) | 1986-11-20 |
Family
ID=24519477
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP60503039A Pending JPS61502683A (en) | 1984-07-06 | 1985-07-03 | Bandages for sustained release of drugs |
Country Status (7)
| Country | Link |
|---|---|
| EP (1) | EP0191783A4 (en) |
| JP (1) | JPS61502683A (en) |
| AU (1) | AU584025B2 (en) |
| CA (1) | CA1253805A (en) |
| DK (1) | DK100586D0 (en) |
| WO (1) | WO1986000536A1 (en) |
| ZA (1) | ZA855137B (en) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5322695A (en) * | 1987-01-09 | 1994-06-21 | Hercon Laboratories Corporation | Moisture-vapor-permeable dressing |
| US5139023A (en) * | 1989-06-02 | 1992-08-18 | Theratech Inc. | Apparatus and method for noninvasive blood glucose monitoring |
| KR920700014A (en) * | 1989-06-02 | 1992-02-19 | 테오도르 에이취. 스탠리 | Non-Invasive Blood Glucose Testing Apparatus and Method |
| DE19519593C1 (en) * | 1995-05-29 | 1996-08-29 | Horstmann Michael | Transdermal therapeutic system with thermoplastic back layer |
| FR2776517B1 (en) * | 1998-03-24 | 2000-06-09 | Oreal | THERMAL EFFECT PATCH AND USE THEREOF |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR945952A (en) * | 1947-04-29 | 1949-05-19 | Auxiliary device for the use of chemicals and minerals for therapeutic purposes | |
| FR2205306A1 (en) * | 1972-11-08 | 1974-05-31 | Expl Marques Brevets Soc | Medicated dressing for inaccessible site applicant. - permitting diffusion- of powder or tablet to a seat of pain, inflammation or infection |
| US4207890A (en) * | 1977-01-04 | 1980-06-17 | Mcneilab, Inc. | Drug-dispensing device and method |
| US4286592A (en) * | 1980-02-04 | 1981-09-01 | Alza Corporation | Therapeutic system for administering drugs to the skin |
| US4486193A (en) * | 1981-07-22 | 1984-12-04 | Alza Corporation | Method for treating ischemic conditions by administering drug by two routes |
-
1985
- 1985-07-03 JP JP60503039A patent/JPS61502683A/en active Pending
- 1985-07-03 EP EP19850903618 patent/EP0191783A4/en not_active Withdrawn
- 1985-07-03 AU AU46066/85A patent/AU584025B2/en not_active Ceased
- 1985-07-03 WO PCT/US1985/001295 patent/WO1986000536A1/en not_active Application Discontinuation
- 1985-07-05 CA CA000486374A patent/CA1253805A/en not_active Expired
- 1985-07-08 ZA ZA855137A patent/ZA855137B/en unknown
-
1986
- 1986-03-05 DK DK100586A patent/DK100586D0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP0191783A4 (en) | 1987-12-09 |
| AU4606685A (en) | 1986-02-10 |
| ZA855137B (en) | 1986-02-26 |
| CA1253805A (en) | 1989-05-09 |
| DK100586A (en) | 1986-03-05 |
| AU584025B2 (en) | 1989-05-11 |
| DK100586D0 (en) | 1986-03-05 |
| EP0191783A1 (en) | 1986-08-27 |
| WO1986000536A1 (en) | 1986-01-30 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US4655768A (en) | Bandage for sustained delivery of drugs | |
| US3731683A (en) | Bandage for the controlled metering of topical drugs to the skin | |
| EP1225951B1 (en) | A dual adhesive transdermal drug delivery system | |
| JP6487039B2 (en) | Device for delivery of skin care composition | |
| US7063859B1 (en) | Barrier film lined backing layer composition and method for topical administration of active agents | |
| KR950005865B1 (en) | Plaster | |
| JP2002544157A (en) | Drug release device | |
| JP2000514063A (en) | Non-occlusive drug delivery device and method of manufacturing the same | |
| JPH07265353A (en) | Nonobstructive adhesive patch for application of medicine onskin | |
| MXPA01000128A (en) | Topical plaster with non-steroidal antirheumatic agents with an acid group. | |
| JP2001328935A (en) | Patch | |
| JPS61502683A (en) | Bandages for sustained release of drugs | |
| JP2001104359A (en) | Cooling sheet | |
| JPH0472805B2 (en) | ||
| JPH0429927A (en) | Plaster | |
| JP3233732B2 (en) | Method for producing breathable adhesive tape | |
| JP2869167B2 (en) | Sustained-release patch preparation | |
| JPH05305108A (en) | Wrapping structure of paste agent | |
| JP5512910B2 (en) | Tulobuterol-containing percutaneous absorption preparation and patch using the same | |
| JP3240184B2 (en) | Hygroscopic patch | |
| JP2697191B2 (en) | Transdermal formulation | |
| JP2540861B2 (en) | Poultice | |
| JPS62230720A (en) | Laminated pharmaceutical | |
| JPH06142178A (en) | Tape agent and tape preparation having decreased stimulus on skin | |
| JP3277239B2 (en) | Topical patch for eperisone or tolperisone |