TW201735904A - 口腔內貼附劑 - Google Patents

口腔內貼附劑 Download PDF

Info

Publication number: TW201735904A
Authority: TW; Taiwan
Prior art keywords: drug; oral; layer; drug layer; patch
Prior art date: 2016-02-25

Application number

TW106106122A

Other languages

English (en)

Chinese (zh)

Inventor

中村晃太

崎山勝弘

深町□広

田中幸司

Original Assignee

久光製藥股份有限公司

Priority date (The priority date 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 date listed.)

2016-02-25

Filing date

2017-02-23

Publication date

2017-10-16

2017-02-23 Application filed by 久光製藥股份有限公司 filed Critical 久光製藥股份有限公司

2017-10-16 Publication of TW201735904A publication Critical patent/TW201735904A/zh

Links

239000003814 drug Substances 0.000 claims abstract description 119
230000008595 infiltration Effects 0.000 claims abstract description 38
238000001764 infiltration Methods 0.000 claims abstract description 38
229940079593 drug Drugs 0.000 claims description 117
239000010410 layer Substances 0.000 claims description 100
229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 19
235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 19
239000004386 Erythritol Substances 0.000 claims description 17
UNXHWFMMPAWVPI-UHFFFAOYSA-N Erythritol Natural products OCC(O)C(O)CO UNXHWFMMPAWVPI-UHFFFAOYSA-N 0.000 claims description 17
UNXHWFMMPAWVPI-ZXZARUISSA-N erythritol Chemical compound OC[C@H](O)[C@H](O)CO UNXHWFMMPAWVPI-ZXZARUISSA-N 0.000 claims description 17
235000019414 erythritol Nutrition 0.000 claims description 17
229940009714 erythritol Drugs 0.000 claims description 17
239000003623 enhancer Substances 0.000 claims description 16
210000000214 mouth Anatomy 0.000 claims description 16
239000003795 chemical substances by application Substances 0.000 claims description 14
230000003204 osmotic effect Effects 0.000 claims description 14
239000000546 pharmaceutical excipient Substances 0.000 claims description 13
239000011230 binding agent Substances 0.000 claims description 10
WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 9
238000009736 wetting Methods 0.000 claims description 9
229920002125 Sokalan® Polymers 0.000 claims description 8
FBPFZTCFMRRESA-UHFFFAOYSA-N hexane-1,2,3,4,5,6-hexol Chemical compound OCC(O)C(O)C(O)C(O)CO FBPFZTCFMRRESA-UHFFFAOYSA-N 0.000 claims description 7
229940069328 povidone Drugs 0.000 claims description 7
239000012790 adhesive layer Substances 0.000 claims description 5
210000004877 mucosa Anatomy 0.000 claims description 4
239000000411 inducer Substances 0.000 claims 1
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239000002831 pharmacologic agent Substances 0.000 abstract 1
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239000000845 maltitol Substances 0.000 description 14
235000010449 maltitol Nutrition 0.000 description 14
VQHSOMBJVWLPSR-WUJBLJFYSA-N maltitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-WUJBLJFYSA-N 0.000 description 14
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238000012360 testing method Methods 0.000 description 6
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ZAFYATHCZYHLPB-UHFFFAOYSA-N zolpidem Chemical group N1=C2C=CC(C)=CN2C(CC(=O)N(C)C)=C1C1=CC=C(C)C=C1 ZAFYATHCZYHLPB-UHFFFAOYSA-N 0.000 description 6
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KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
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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 2
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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 2
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 2
KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 description 2
VJHCJDRQFCCTHL-UHFFFAOYSA-N acetic acid 2,3,4,5,6-pentahydroxyhexanal Chemical compound CC(O)=O.OCC(O)C(O)C(O)C(O)C=O VJHCJDRQFCCTHL-UHFFFAOYSA-N 0.000 description 2
WNLRTRBMVRJNCN-UHFFFAOYSA-N adipic acid Chemical compound OC(=O)CCCCC(O)=O WNLRTRBMVRJNCN-UHFFFAOYSA-N 0.000 description 2
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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 description 2
JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 2
238000002156 mixing Methods 0.000 description 2
235000019426 modified starch Nutrition 0.000 description 2
210000004400 mucous membrane Anatomy 0.000 description 2
229940068196 placebo Drugs 0.000 description 2
239000000902 placebo Substances 0.000 description 2
239000000243 solution Substances 0.000 description 2
239000012085 test solution Substances 0.000 description 2
VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 2
229960000820 zopiclone Drugs 0.000 description 2
FJIKWRGCXUCUIG-HNNXBMFYSA-N (3s)-7-chloro-5-(2-chlorophenyl)-3-hydroxy-1-methyl-3h-1,4-benzodiazepin-2-one Chemical compound O=C([C@H](O)N=1)N(C)C2=CC=C(Cl)C=C2C=1C1=CC=CC=C1Cl FJIKWRGCXUCUIG-HNNXBMFYSA-N 0.000 description 1
BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 description 1
SVUOLADPCWQTTE-UHFFFAOYSA-N 1h-1,2-benzodiazepine Chemical compound N1N=CC=CC2=CC=CC=C12 SVUOLADPCWQTTE-UHFFFAOYSA-N 0.000 description 1
JHGHLTNIQXXXNV-UHFFFAOYSA-N 2-[6-methyl-2-(4-methylphenyl)imidazo[1,2-a]pyridin-3-yl]acetic acid Chemical compound C1=CC(C)=CC=C1C1=C(CC(O)=O)N2C=C(C)C=CC2=N1 JHGHLTNIQXXXNV-UHFFFAOYSA-N 0.000 description 1
YDHIMEXEGOCNHU-UHFFFAOYSA-N 2-pyridin-3-ylacetamide Chemical compound NC(=O)CC1=CC=CN=C1 YDHIMEXEGOCNHU-UHFFFAOYSA-N 0.000 description 1
DEXFNLNNUZKHNO-UHFFFAOYSA-N 6-[3-[4-[2-(2,3-dihydro-1H-inden-2-ylamino)pyrimidin-5-yl]piperidin-1-yl]-3-oxopropyl]-3H-1,3-benzoxazol-2-one Chemical compound C1C(CC2=CC=CC=C12)NC1=NC=C(C=N1)C1CCN(CC1)C(CCC1=CC2=C(NC(O2)=O)C=C1)=O DEXFNLNNUZKHNO-UHFFFAOYSA-N 0.000 description 1
GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 1
WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 description 1
SGHZXLIDFTYFHQ-UHFFFAOYSA-L Brilliant Blue Chemical compound [Na+].[Na+].C=1C=C(C(=C2C=CC(C=C2)=[N+](CC)CC=2C=C(C=CC=2)S([O-])(=O)=O)C=2C(=CC=CC=2)S([O-])(=O)=O)C=CC=1N(CC)CC1=CC=CC(S([O-])(=O)=O)=C1 SGHZXLIDFTYFHQ-UHFFFAOYSA-L 0.000 description 1
FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 1
FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 1
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239000004375 Dextrin Substances 0.000 description 1
239000001856 Ethyl cellulose Substances 0.000 description 1
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 description 1
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GRYLNZFGIOXLOG-UHFFFAOYSA-N Nitric acid Chemical compound O[N+]([O-])=O GRYLNZFGIOXLOG-UHFFFAOYSA-N 0.000 description 1
OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 description 1
241000206572 Rhodophyta Species 0.000 description 1
190000007496 Rilmazafone Chemical compound 0.000 description 1
229920001800 Shellac Polymers 0.000 description 1
KDYFGRWQOYBRFD-UHFFFAOYSA-N Succinic acid Natural products OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 description 1
229930006000 Sucrose Natural products 0.000 description 1
CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
150000007513 acids Chemical class 0.000 description 1
239000004480 active ingredient Substances 0.000 description 1
239000001361 adipic acid Substances 0.000 description 1
235000011037 adipic acid Nutrition 0.000 description 1
BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 description 1
229920003144 amino alkyl methacrylate copolymer Polymers 0.000 description 1
229940049706 benzodiazepine Drugs 0.000 description 1
KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 description 1
125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 description 1
229950008138 carmellose Drugs 0.000 description 1
235000015165 citric acid Nutrition 0.000 description 1
238000013329 compounding Methods 0.000 description 1
150000001875 compounds Chemical class 0.000 description 1
230000035597 cooling sensation Effects 0.000 description 1
229960005168 croscarmellose Drugs 0.000 description 1
239000001767 crosslinked sodium carboxy methyl cellulose Substances 0.000 description 1
238000013461 design Methods 0.000 description 1
235000019425 dextrin Nutrition 0.000 description 1
230000000694 effects Effects 0.000 description 1
229920001249 ethyl cellulose Polymers 0.000 description 1
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238000011156 evaluation Methods 0.000 description 1
239000001530 fumaric acid Substances 0.000 description 1
238000004128 high performance liquid chromatography Methods 0.000 description 1
230000001939 inductive effect Effects 0.000 description 1
239000004310 lactic acid Substances 0.000 description 1
235000014655 lactic acid Nutrition 0.000 description 1
239000007788 liquid Substances 0.000 description 1
230000007774 longterm Effects 0.000 description 1
229960004033 lormetazepam Drugs 0.000 description 1
239000000314 lubricant Substances 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
239000001630 malic acid Substances 0.000 description 1
235000011090 malic acid Nutrition 0.000 description 1
238000004519 manufacturing process Methods 0.000 description 1
150000007522 mineralic acids Chemical class 0.000 description 1
229910017604 nitric acid Inorganic materials 0.000 description 1
230000009972 noncorrosive effect Effects 0.000 description 1
150000007524 organic acids Chemical class 0.000 description 1
235000005985 organic acids Nutrition 0.000 description 1
239000012466 permeate Substances 0.000 description 1
229950002503 rilmazafone Drugs 0.000 description 1
239000004208 shellac Substances 0.000 description 1
229940113147 shellac Drugs 0.000 description 1
ZLGIYFNHBLSMPS-ATJNOEHPSA-N shellac Chemical compound OCCCCCC(O)C(O)CCCCCCCC(O)=O.C1C23[C@H](C(O)=O)CCC2[C@](C)(CO)[C@@H]1C(C(O)=O)=C[C@@H]3O ZLGIYFNHBLSMPS-ATJNOEHPSA-N 0.000 description 1
235000013874 shellac Nutrition 0.000 description 1
230000004622 sleep time Effects 0.000 description 1
229960002920 sorbitol Drugs 0.000 description 1
239000003381 stabilizer Substances 0.000 description 1
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239000000126 substance Substances 0.000 description 1
150000005846 sugar alcohols Chemical class 0.000 description 1
230000002459 sustained effect Effects 0.000 description 1
229940095064 tartrate Drugs 0.000 description 1
JOFWLTCLBGQGBO-UHFFFAOYSA-N triazolam Chemical compound C12=CC(Cl)=CC=C2N2C(C)=NN=C2CN=C1C1=CC=CC=C1Cl JOFWLTCLBGQGBO-UHFFFAOYSA-N 0.000 description 1
229960003386 triazolam Drugs 0.000 description 1
150000003852 triazoles Chemical class 0.000 description 1

Classifications

- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- 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
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- 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

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Public Health (AREA)
Life Sciences & Earth Sciences (AREA)
Veterinary Medicine (AREA)
General Health & Medical Sciences (AREA)
Medicinal Chemistry (AREA)
Pharmacology & Pharmacy (AREA)
Epidemiology (AREA)
Animal Behavior & Ethology (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Engineering & Computer Science (AREA)
Oil, Petroleum & Natural Gas (AREA)
Inorganic Chemistry (AREA)
Medicinal Preparation (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

TW106106122A 2016-02-25 2017-02-23 口腔內貼附劑 TW201735904A (zh)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
JP2016034513		2016-02-25

Publications (1)

Publication Number	Publication Date
TW201735904A true TW201735904A (zh)	2017-10-16

Family

ID=59686226

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
TW106106122A TW201735904A (zh)	2016-02-25	2017-02-23	口腔內貼附劑

Country Status (3)

Country	Link
JP (2)	JP6615978B2 (fr)
TW (1)	TW201735904A (fr)
WO (1)	WO2017146104A1 (fr)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
CA3121634A1 (fr) *	2018-12-11	2020-06-18	Myospots Australia Pty Ltd	Tampon adhesif

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* Cited by examiner, † Cited by third party
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JPS60237018A (ja) *	1984-05-09	1985-11-25	Tanpei Seiyaku Kk	口腔内付着性組成物
JPH01101975A (ja) *	1987-10-14	1989-04-19	Sekisui Chem Co Ltd	口腔粘膜用貼付剤
JP2000063268A (ja) *	1998-06-12	2000-02-29	Lion Corp	口腔粘膜付着型徐放性錠剤及び歯周疾患治療剤
JP2000178185A (ja) *	1998-12-18	2000-06-27	Lion Corp	口腔粘膜付着型徐放性錠剤
EP2462926B1 (fr) *	2006-05-23	2015-12-30	Orahealth Corporation	Comprimé d'adhérence orale bi-couche avec adhésif de gomme d'acacia
US20110008431A1 (en) *	2007-04-02	2011-01-13	Toyo Boseki Kabushiki Kaisha	Therapeutic tablet for postherpetic neuralgia and method of treating postherpetic neuralgia
WO2009021106A1 (fr) *	2007-08-07	2009-02-12	Acelrx Pharmaceuticals, Inc.	Compositions et procédés de sédation et d'analgésie procédurales utilisant les formes posologiques transmucosales orales
US20110091544A1 (en) *	2009-10-16	2011-04-21	Acelrx Pharmaceuticals, Inc.	Compositions and Methods for Mild Sedation, Anxiolysis and Analgesia in the Procedural Setting
KR101751631B1 (ko) *	2013-05-31	2017-06-27	히사미쓰 세이야꾸 가부시키가이샤	구강 첩부제

2017
- 2017-02-22 WO PCT/JP2017/006622 patent/WO2017146104A1/fr not_active Ceased
- 2017-02-22 JP JP2018501737A patent/JP6615978B2/ja active Active
- 2017-02-23 TW TW106106122A patent/TW201735904A/zh unknown
2019
- 2019-11-05 JP JP2019200713A patent/JP6959313B2/ja active Active

Also Published As

Publication number	Publication date
WO2017146104A1 (fr)	2017-08-31
JP6615978B2 (ja)	2019-12-04
JP2020015772A (ja)	2020-01-30
JPWO2017146104A1 (ja)	2018-10-04
JP6959313B2 (ja)	2021-11-02

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