JP6318355B2 - ビソプロロール含有貼付製剤 - Google Patents
ビソプロロール含有貼付製剤 Download PDFInfo
- Publication number
- JP6318355B2 JP6318355B2 JP2013185599A JP2013185599A JP6318355B2 JP 6318355 B2 JP6318355 B2 JP 6318355B2 JP 2013185599 A JP2013185599 A JP 2013185599A JP 2013185599 A JP2013185599 A JP 2013185599A JP 6318355 B2 JP6318355 B2 JP 6318355B2
- Authority
- JP
- Japan
- Prior art keywords
- bisoprolol
- pressure
- sensitive adhesive
- weight
- adhesive layer
- 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.)
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- 229960002781 bisoprolol Drugs 0.000 title claims description 67
- 238000002360 preparation method Methods 0.000 title claims description 42
- 239000004820 Pressure-sensitive adhesive Substances 0.000 claims description 73
- 239000010410 layer Substances 0.000 claims description 53
- 229920002367 Polyisobutene Polymers 0.000 claims description 41
- 239000000853 adhesive Substances 0.000 claims description 31
- 230000001070 adhesive effect Effects 0.000 claims description 31
- -1 inorganic acid salt Chemical class 0.000 claims description 25
- 125000005843 halogen group Chemical group 0.000 claims description 20
- 239000007788 liquid Substances 0.000 claims description 10
- 239000012790 adhesive layer Substances 0.000 claims description 7
- 150000003839 salts Chemical class 0.000 claims description 6
- 125000005907 alkyl ester group Chemical group 0.000 claims description 4
- 235000014113 dietary fatty acids Nutrition 0.000 claims description 4
- 239000000194 fatty acid Substances 0.000 claims description 4
- 229930195729 fatty acid Natural products 0.000 claims description 4
- 235000011837 pasties Nutrition 0.000 claims description 4
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical group [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 claims description 3
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical group [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims description 3
- 229910052801 chlorine Inorganic materials 0.000 claims description 3
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 3
- 229910052731 fluorine Inorganic materials 0.000 claims description 3
- 125000001153 fluoro group Chemical group F* 0.000 claims description 3
- 229910052740 iodine Inorganic materials 0.000 claims description 3
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- 230000000844 anti-bacterial effect Effects 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 230000003078 antioxidant effect Effects 0.000 description 1
- 239000012298 atmosphere Substances 0.000 description 1
- 239000000440 bentonite Substances 0.000 description 1
- 229910000278 bentonite Inorganic materials 0.000 description 1
- SVPXDRXYRYOSEX-UHFFFAOYSA-N bentoquatam Chemical compound O.O=[Si]=O.O=[Al]O[Al]=O SVPXDRXYRYOSEX-UHFFFAOYSA-N 0.000 description 1
- 229960005400 bisoprolol fumarate Drugs 0.000 description 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 229920005549 butyl rubber Polymers 0.000 description 1
- 229910000019 calcium carbonate Inorganic materials 0.000 description 1
- 229910052799 carbon Inorganic materials 0.000 description 1
- 239000006229 carbon black Substances 0.000 description 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 1
- 150000001732 carboxylic acid derivatives Chemical class 0.000 description 1
- 229960001777 castor oil Drugs 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 239000012461 cellulose resin Substances 0.000 description 1
- 229960000541 cetyl alcohol Drugs 0.000 description 1
- 239000013522 chelant Substances 0.000 description 1
- 238000010382 chemical cross-linking Methods 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 238000004587 chromatography analysis Methods 0.000 description 1
- 229920006147 copolyamide elastomer Polymers 0.000 description 1
- 239000003431 cross linking reagent Substances 0.000 description 1
- 238000002425 crystallisation Methods 0.000 description 1
- 230000008025 crystallization Effects 0.000 description 1
- 125000002704 decyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 238000000151 deposition Methods 0.000 description 1
- 229940031578 diisopropyl adipate Drugs 0.000 description 1
- VNGOYPQMJFJDLV-UHFFFAOYSA-N dimethyl benzene-1,3-dicarboxylate Chemical compound COC(=O)C1=CC=CC(C(=O)OC)=C1 VNGOYPQMJFJDLV-UHFFFAOYSA-N 0.000 description 1
- 125000000118 dimethyl group Chemical group [H]C([H])([H])* 0.000 description 1
- FBSAITBEAPNWJG-UHFFFAOYSA-N dimethyl phthalate Natural products CC(=O)OC1=CC=CC=C1OC(C)=O FBSAITBEAPNWJG-UHFFFAOYSA-N 0.000 description 1
- 229960001826 dimethylphthalate Drugs 0.000 description 1
- 125000003438 dodecyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 238000010894 electron beam technology Methods 0.000 description 1
- 238000010828 elution Methods 0.000 description 1
- HDERJYVLTPVNRI-UHFFFAOYSA-N ethene;ethenyl acetate Chemical group C=C.CC(=O)OC=C HDERJYVLTPVNRI-UHFFFAOYSA-N 0.000 description 1
- UIWXSTHGICQLQT-UHFFFAOYSA-N ethenyl propanoate Chemical compound CCC(=O)OC=C UIWXSTHGICQLQT-UHFFFAOYSA-N 0.000 description 1
- 125000005448 ethoxyethyl group Chemical group [H]C([H])([H])C([H])([H])OC([H])([H])C([H])([H])* 0.000 description 1
- LVGKNOAMLMIIKO-QXMHVHEDSA-N ethyl oleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC LVGKNOAMLMIIKO-QXMHVHEDSA-N 0.000 description 1
- 229940093471 ethyl oleate Drugs 0.000 description 1
- 229920001038 ethylene copolymer Polymers 0.000 description 1
- 239000005038 ethylene vinyl acetate Substances 0.000 description 1
- 239000003925 fat Substances 0.000 description 1
- 239000000835 fiber Substances 0.000 description 1
- 239000002657 fibrous material Substances 0.000 description 1
- 239000012458 free base Substances 0.000 description 1
- 239000011086 glassine Substances 0.000 description 1
- 229910052736 halogen Inorganic materials 0.000 description 1
- 150000002367 halogens Chemical class 0.000 description 1
- 125000003187 heptyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 229920001519 homopolymer Polymers 0.000 description 1
- 229930195733 hydrocarbon Natural products 0.000 description 1
- 150000002430 hydrocarbons Chemical class 0.000 description 1
- 239000012433 hydrogen halide Substances 0.000 description 1
- 229910000039 hydrogen halide Inorganic materials 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 150000002513 isocyanates Chemical class 0.000 description 1
- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 description 1
- NLYAJNPCOHFWQQ-UHFFFAOYSA-N kaolin Chemical compound O.O.O=[Al]O[Si](=O)O[Si](=O)O[Al]=O NLYAJNPCOHFWQQ-UHFFFAOYSA-N 0.000 description 1
- 239000002655 kraft paper Substances 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 229940039717 lanolin Drugs 0.000 description 1
- 235000019388 lanolin Nutrition 0.000 description 1
- 238000004811 liquid chromatography Methods 0.000 description 1
- 229940057995 liquid paraffin Drugs 0.000 description 1
- 239000000395 magnesium oxide Substances 0.000 description 1
- CPLXHLVBOLITMK-UHFFFAOYSA-N magnesium oxide Inorganic materials [Mg]=O CPLXHLVBOLITMK-UHFFFAOYSA-N 0.000 description 1
- AXZKOIWUVFPNLO-UHFFFAOYSA-N magnesium;oxygen(2-) Chemical compound [O-2].[Mg+2] AXZKOIWUVFPNLO-UHFFFAOYSA-N 0.000 description 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
- 239000011976 maleic acid Substances 0.000 description 1
- FPYJFEHAWHCUMM-UHFFFAOYSA-N maleic anhydride Chemical compound O=C1OC(=O)C=C1 FPYJFEHAWHCUMM-UHFFFAOYSA-N 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 238000001465 metallisation Methods 0.000 description 1
- BFOQBMCQGCJJTA-UHFFFAOYSA-N methanesulfonic acid;prop-2-enamide Chemical compound CS(O)(=O)=O.NC(=O)C=C BFOQBMCQGCJJTA-UHFFFAOYSA-N 0.000 description 1
- LVHBHZANLOWSRM-UHFFFAOYSA-N methylenebutanedioic acid Natural products OC(=O)CC(=C)C(O)=O LVHBHZANLOWSRM-UHFFFAOYSA-N 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- RZRNAYUHWVFMIP-UHFFFAOYSA-N monoelaidin Natural products CCCCCCCCC=CCCCCCCCC(=O)OCC(O)CO RZRNAYUHWVFMIP-UHFFFAOYSA-N 0.000 description 1
- JXTPJDDICSTXJX-UHFFFAOYSA-N n-Triacontane Natural products CCCCCCCCCCCCCCCCCCCCCCCCCCCCCC JXTPJDDICSTXJX-UHFFFAOYSA-N 0.000 description 1
- 125000001400 nonyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical class CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 description 1
- KSCKTBJJRVPGKM-UHFFFAOYSA-N octan-1-olate;titanium(4+) Chemical compound [Ti+4].CCCCCCCC[O-].CCCCCCCC[O-].CCCCCCCC[O-].CCCCCCCC[O-] KSCKTBJJRVPGKM-UHFFFAOYSA-N 0.000 description 1
- 229960002446 octanoic acid Drugs 0.000 description 1
- 125000002347 octyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 235000014593 oils and fats Nutrition 0.000 description 1
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 description 1
- 239000004006 olive oil Substances 0.000 description 1
- 235000008390 olive oil Nutrition 0.000 description 1
- 150000001451 organic peroxides Chemical class 0.000 description 1
- 239000005022 packaging material Substances 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 description 1
- 230000002093 peripheral effect Effects 0.000 description 1
- 239000005011 phenolic resin Substances 0.000 description 1
- 229920001200 poly(ethylene-vinyl acetate) Polymers 0.000 description 1
- 229920003229 poly(methyl methacrylate) Polymers 0.000 description 1
- 229920002432 poly(vinyl methyl ether) polymer Polymers 0.000 description 1
- 229920000058 polyacrylate Polymers 0.000 description 1
- 229920002239 polyacrylonitrile Polymers 0.000 description 1
- 229920006350 polyacrylonitrile resin Polymers 0.000 description 1
- 229920002857 polybutadiene Polymers 0.000 description 1
- 229920006289 polycarbonate film Polymers 0.000 description 1
- 229920000570 polyether Polymers 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920001721 polyimide Polymers 0.000 description 1
- 239000004926 polymethyl methacrylate Substances 0.000 description 1
- 229920001451 polypropylene glycol Polymers 0.000 description 1
- 229920000346 polystyrene-polyisoprene block-polystyrene Polymers 0.000 description 1
- 150000003097 polyterpenes Chemical class 0.000 description 1
- 239000004800 polyvinyl chloride Substances 0.000 description 1
- 229920000915 polyvinyl chloride Polymers 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- UIIIBRHUICCMAI-UHFFFAOYSA-N prop-2-ene-1-sulfonic acid Chemical compound OS(=O)(=O)CC=C UIIIBRHUICCMAI-UHFFFAOYSA-N 0.000 description 1
- 239000000473 propyl gallate Substances 0.000 description 1
- 229940075579 propyl gallate Drugs 0.000 description 1
- 235000010388 propyl gallate Nutrition 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 230000005855 radiation Effects 0.000 description 1
- 239000000741 silica gel Substances 0.000 description 1
- 229910002027 silica gel Inorganic materials 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 229920002379 silicone rubber Polymers 0.000 description 1
- 239000004945 silicone rubber Substances 0.000 description 1
- 238000000638 solvent extraction Methods 0.000 description 1
- 238000001179 sorption measurement Methods 0.000 description 1
- 229940032094 squalane Drugs 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 239000010959 steel Substances 0.000 description 1
- 229920000468 styrene butadiene styrene block copolymer Polymers 0.000 description 1
- 125000000020 sulfo group Chemical group O=S(=O)([*])O[H] 0.000 description 1
- 239000013589 supplement Substances 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- OGIDPMRJRNCKJF-UHFFFAOYSA-N titanium oxide Inorganic materials [Ti]=O OGIDPMRJRNCKJF-UHFFFAOYSA-N 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
- KHPCPRHQVVSZAH-UHFFFAOYSA-N trans-cinnamyl beta-D-glucopyranoside Natural products OC1C(O)C(O)C(CO)OC1OCC=CC1=CC=CC=C1 KHPCPRHQVVSZAH-UHFFFAOYSA-N 0.000 description 1
- ZIBGPFATKBEMQZ-UHFFFAOYSA-N triethylene glycol Chemical compound OCCOCCOCCO ZIBGPFATKBEMQZ-UHFFFAOYSA-N 0.000 description 1
- VLPFTAMPNXLGLX-UHFFFAOYSA-N trioctanoin Chemical compound CCCCCCCC(=O)OCC(OC(=O)CCCCCCC)COC(=O)CCCCCCC VLPFTAMPNXLGLX-UHFFFAOYSA-N 0.000 description 1
- 125000002948 undecyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 229920001567 vinyl ester resin Polymers 0.000 description 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
- 239000002759 woven fabric Substances 0.000 description 1
- 239000008096 xylene Substances 0.000 description 1
- 239000011787 zinc oxide Substances 0.000 description 1
Images
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
- 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
- A61K9/7038—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer
- A61K9/7046—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds
- A61K9/7053—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
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- 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
-
- 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
- A61K9/7038—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer
- A61K9/7046—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds
- A61K9/7053—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
- A61K9/7061—Polyacrylates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
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- Bioinformatics & Cheminformatics (AREA)
- Dermatology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Adhesives Or Adhesive Processes (AREA)
- Adhesive Tapes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
[1] 支持体の片面に、ビソプロロールと粘着剤とを含有する粘着剤層が積層されたビソプロロール含有貼付製剤であって、粘着剤層中のハロゲン原子の含有量が0.01〜100重量ppmであることを特徴とするビソプロロール含有貼付製剤。
[2] ハロゲン原子の含有量がフッ素原子、塩素原子、臭素原子およびヨウ素原子の合計含有量である前記[1]に記載のビソプロロール含有貼付製剤。
[3] ビソプロロールがその塩を含む前記[1]または[2]に記載のビソプロロール含有貼付製剤。
[4] 前記塩が無機酸塩である前記[3]に記載のビソプロロール含有貼付製剤。
J0=ηSP/c(1+0.31ηSP)(cm3/g) (Schulz-Blaschke式) (1)
ηSP=t/to−1
t:溶液のフロータイム (Hagenbach-Couette補正式による)
t0:溶媒のフロータイム (Hagenbach-Couette補正式による)
c:溶液の濃度(g/cm3)
J0=3.06×10−2Mv0.65 (2)
Mv:粘度平均分子量
なお、粘着付与剤の軟化点は、好ましくは90℃〜150℃、より好ましくは95℃〜145℃である。軟化点が90℃〜150℃であると、粘着剤層の各含有成分との相溶性が良好で、均一に混合しやすくなる傾向にある。なお、本発明における軟化点は環球法によって測定される値である。
第1のポリイソブチレン(粘度平均分子量:4,000,000)15.1重量部、第2のポリイソブチレン(粘度平均分子量:55,000)26.1重量部、粘着付与剤(軟化点が140℃である脂環族飽和炭化水素樹脂)27.4重量部、液状の有機成分(ミリスチン酸イソプロピル)30重量部、およびビソプロロール1.4重量部を、トルエン400重量部と混合し、溶解させてトルエン溶液を調製した。なお、前記ビソプロロールとしては、精製したビソプロロール、またはビソプロロールの塩酸塩を添加して塩酸塩の含有量を制御したビソプロロールを使用した。使用したビソプロロールに含まれる塩酸塩の含有量(=100×ビソプロロールに含まれる塩酸塩の量/(ビソプロロールおよびビソプロロールに含まれる塩酸塩の合計量))を表1に示す。乾燥後の粘着剤層の厚さが160μmとなるように、シリコーン剥離処理を施したポリエチレンテレフタレート(PET)製ライナー(厚さ75μm)上に得られたトルエン溶液を塗布し、これを熱風循環式乾燥機中で100℃および5分間乾燥して粘着剤層を形成した。この粘着剤層を、厚さ3.5μmのPET製フィルムと12g/m2のPET製不織布との積層フィルムの不織布に貼り合わせ、ビソプロロール含有貼付製剤を得た。
得られたビソプロロール含有貼付製剤を、温度20±10℃、相対湿度30±10%の環境下にて、60mm×60mmのサイズに打ち抜いた後、PET/Al/ポリアクリロニトリル系樹脂の積層体からなる包材(100mm×100mm)にて、ポリアクリロニトリル系樹脂が内面になるように包装し、50℃で保存し、後述する粘着力、色彩b*値およびビソプロロールの類縁物質を測定した。ここでビソプロロールの類縁物質とは、ビソプロロールの分解生成物またはビソプロロールとビソプロロール以外の成分との反応によって生じる生成物を指す。
保存前、保存1ヶ月後および3ヶ月後のビソプロロール含有貼付製剤(実施例1〜4)の粘着力を、以下の方法で測定した。ステンレス板(JIS G4305に規定されるSUS304鋼板)の表面を、まず360番の耐水研磨紙にて均一に研磨し、次いで酢酸エチルを染み込ませた布で洗浄した。ビソプロロール含有貼付製剤を切断して、幅24mmおよび長さ50mmの試験片を調製した。ライナーを剥離した試験片の粘着面を、質量850gのゴムローラーを用いてステンレス板の研磨および洗浄した表面に貼り合せた(ゴムローラー通過速度300mm/分、通過回数2回)。試験片を貼り合せたステンレス板を23±2℃、50±10%R.H.の雰囲気下に30分間静置した。ステンレス板から試験片の一端を約5mm剥がして180°角に折り返し、補助紙(幅30mm)を貼り付けた。引張り試験機を用い、補助紙の一端を上部の留金にはさみ、ステンレス板を下部の留金にはさみ、23±2℃、50±10%R.H.の雰囲気下で、300mm/分の速度で180°方向に試験片を連続して引き剥がし、粘着力を測定した。結果(24mm幅の試験片で測定した値)を表2に示す。また、表2には、保存前の粘着力に対する保存後の粘着力の割合(=100×保存後の粘着力/保存前の粘着力)も示す。
保存6ヶ月後のビソプロロール含有貼付製剤(実施例1および2)の色彩b*値(L*a*b*表色系)を、色彩色差計(型番CR−400、コニカミノルタ社製)によって測定した(測定面:積層フィルム(支持体)のPET製フィルム面)。結果を表3に示す。色彩b*値が高いほど黄変していることを示す。
保存6ヶ月後のビソプロロール含有貼付製剤(実施例1および2)をテトラヒドロフランにて抽出し、この抽出液を以下の条件のHPLCで分析した。ビソプロロールのHPLCピーク面積に対するビソプロロールの全類縁物質のHPLCピークの面積合計の割合(=100×全類縁物質のHPLCピーク面積の合計/ビソプロロールのHPLCピーク面積)を類縁物質量として算出した。その結果を表4に示す。
(HPLCの測定条件)
カラム:内径4.6mm、長さ15cmのステンレス管に粒子径が3μmの液体クロマトグラフィー用オクチルシリル化シリカゲルを充てんしたもの
カラム温度:40℃
移動相:
移動相A(リン酸緩衝液(pH2.5))
移動相B(リン酸緩衝液(pH2.5)/アセトニトリル=1/4)
溶出条件:移動相Aおよび移動相Bの混合比を変えて濃度勾配制御する
流量:1.2mL/分
検出器:紫外吸光光度計(波長:225nm)
2 粘着剤層
3 剥離ライナー
10 貼付製剤
Claims (3)
- 支持体の片面に、ビソプロロールと、粘着剤としてポリイソブチレンと、粘着付与剤と、液状またはペースト状の有機成分として脂肪酸アルキルエステル類とを含有する粘着剤層が積層されたビソプロロール含有貼付製剤であって、
粘着剤層中のハロゲン原子の含有量が0.01〜40重量ppmであり、
ビソプロロールがその塩を含み、
粘着剤層中のビソプロロールの含有量が0.5〜40重量%であり、ポリイソブチレンの含有量が15〜60重量%であり、粘着付与剤の含有量が10〜55重量%であり、脂肪酸アルキルエステル類の含有量が5〜70重量%であることを特徴とするビソプロロール含有貼付製剤。 - ハロゲン原子の含有量がフッ素原子、塩素原子、臭素原子およびヨウ素原子の合計含有量である請求項1に記載のビソプロロール含有貼付製剤。
- 前記塩が無機酸塩である請求項1または2に記載のビソプロロール含有貼付製剤。
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