JPS62500523A - 薬剤の経皮送達促進の生理学的手段 - Google Patents
薬剤の経皮送達促進の生理学的手段Info
- Publication number
- JPS62500523A JPS62500523A JP60504771A JP50477185A JPS62500523A JP S62500523 A JPS62500523 A JP S62500523A JP 60504771 A JP60504771 A JP 60504771A JP 50477185 A JP50477185 A JP 50477185A JP S62500523 A JPS62500523 A JP S62500523A
- Authority
- JP
- Japan
- Prior art keywords
- transdermal delivery
- skin
- delivery system
- anticholinergic
- anticholinergic agent
- 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
- 230000002708 enhancing effect Effects 0.000 title description 2
- 238000013271 transdermal drug delivery Methods 0.000 title description 2
- 230000037317 transdermal delivery Effects 0.000 claims description 60
- 229940121948 Muscarinic receptor antagonist Drugs 0.000 claims description 54
- 239000000812 cholinergic antagonist Substances 0.000 claims description 54
- 229940079593 drug Drugs 0.000 claims description 46
- 239000003814 drug Substances 0.000 claims description 46
- 239000013543 active substance Substances 0.000 claims description 34
- 230000009885 systemic effect Effects 0.000 claims description 10
- 238000000034 method Methods 0.000 claims description 9
- 230000001262 anti-secretory effect Effects 0.000 claims description 8
- 239000011159 matrix material Substances 0.000 claims description 8
- 150000003242 quaternary ammonium salts Chemical group 0.000 claims description 5
- 238000009792 diffusion process Methods 0.000 claims description 4
- 230000001737 promoting effect Effects 0.000 claims description 4
- 230000001070 adhesive effect Effects 0.000 claims description 3
- 239000000853 adhesive Substances 0.000 claims description 2
- 239000004820 Pressure-sensitive adhesive Substances 0.000 claims 1
- 230000002745 absorbent Effects 0.000 claims 1
- 239000002250 absorbent Substances 0.000 claims 1
- 238000005507 spraying Methods 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 description 27
- 230000000694 effects Effects 0.000 description 19
- 230000035900 sweating Effects 0.000 description 19
- 230000001078 anti-cholinergic effect Effects 0.000 description 14
- 239000003795 chemical substances by application Substances 0.000 description 12
- 210000004243 sweat Anatomy 0.000 description 12
- 230000035515 penetration Effects 0.000 description 8
- 230000015572 biosynthetic process Effects 0.000 description 6
- 230000001965 increasing effect Effects 0.000 description 6
- 230000000699 topical effect Effects 0.000 description 6
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 5
- 230000000903 blocking effect Effects 0.000 description 5
- 239000003623 enhancer Substances 0.000 description 5
- 239000002674 ointment Substances 0.000 description 5
- 241000699670 Mus sp. Species 0.000 description 4
- 230000001166 anti-perspirative effect Effects 0.000 description 4
- 239000003213 antiperspirant Substances 0.000 description 4
- 230000001713 cholinergic effect Effects 0.000 description 4
- 238000012377 drug delivery Methods 0.000 description 4
- 239000000203 mixture Substances 0.000 description 4
- 102000005962 receptors Human genes 0.000 description 4
- 108020003175 receptors Proteins 0.000 description 4
- 230000028327 secretion Effects 0.000 description 4
- 239000000126 substance Substances 0.000 description 4
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 3
- 206010033799 Paralysis Diseases 0.000 description 3
- OIPILFWXSMYKGL-UHFFFAOYSA-N acetylcholine Chemical compound CC(=O)OCC[N+](C)(C)C OIPILFWXSMYKGL-UHFFFAOYSA-N 0.000 description 3
- 229960004373 acetylcholine Drugs 0.000 description 3
- 230000009471 action Effects 0.000 description 3
- 230000004888 barrier function Effects 0.000 description 3
- 230000008901 benefit Effects 0.000 description 3
- 230000004941 influx Effects 0.000 description 3
- 150000003856 quaternary ammonium compounds Chemical class 0.000 description 3
- 230000001568 sexual effect Effects 0.000 description 3
- 239000002904 solvent Substances 0.000 description 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
- 229920000742 Cotton Polymers 0.000 description 2
- 206010044565 Tremor Diseases 0.000 description 2
- 239000004480 active ingredient Substances 0.000 description 2
- 150000003863 ammonium salts Chemical class 0.000 description 2
- 210000004556 brain Anatomy 0.000 description 2
- 230000001886 ciliary effect Effects 0.000 description 2
- 230000007423 decrease Effects 0.000 description 2
- 230000003247 decreasing effect Effects 0.000 description 2
- 238000011161 development Methods 0.000 description 2
- 230000018109 developmental process Effects 0.000 description 2
- 239000004744 fabric Substances 0.000 description 2
- 230000004907 flux Effects 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- 230000007246 mechanism Effects 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 210000005036 nerve Anatomy 0.000 description 2
- 210000000653 nervous system Anatomy 0.000 description 2
- 230000001734 parasympathetic effect Effects 0.000 description 2
- 230000037368 penetrate the skin Effects 0.000 description 2
- 239000003961 penetration enhancing agent Substances 0.000 description 2
- 230000035479 physiological effects, processes and functions Effects 0.000 description 2
- 238000011160 research Methods 0.000 description 2
- 230000004044 response Effects 0.000 description 2
- 150000003839 salts Chemical class 0.000 description 2
- 231100000245 skin permeability Toxicity 0.000 description 2
- 239000007921 spray Substances 0.000 description 2
- 230000002889 sympathetic effect Effects 0.000 description 2
- 238000012360 testing method Methods 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- IGWCFPFGZULDHY-UHFFFAOYSA-N (1,1-dimethylpyrrolidin-1-ium-3-yl) 2-hydroxy-2-phenyl-2-thiophen-2-ylacetate Chemical compound C1[N+](C)(C)CCC1OC(=O)C(O)(C=1C=CC=CC=1)C1=CC=CS1 IGWCFPFGZULDHY-UHFFFAOYSA-N 0.000 description 1
- JXYWFNAQESKDNC-BTJKTKAUSA-N (z)-4-hydroxy-4-oxobut-2-enoate;2-[(4-methoxyphenyl)methyl-pyridin-2-ylamino]ethyl-dimethylazanium Chemical group OC(=O)\C=C/C(O)=O.C1=CC(OC)=CC=C1CN(CCN(C)C)C1=CC=CC=N1 JXYWFNAQESKDNC-BTJKTKAUSA-N 0.000 description 1
- AXTGDCSMTYGJND-UHFFFAOYSA-N 1-dodecylazepan-2-one Chemical group CCCCCCCCCCCCN1CCCCCC1=O AXTGDCSMTYGJND-UHFFFAOYSA-N 0.000 description 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical group CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
- 108010013043 Acetylesterase Proteins 0.000 description 1
- CPELXLSAUQHCOX-UHFFFAOYSA-M Bromide Chemical compound [Br-] CPELXLSAUQHCOX-UHFFFAOYSA-M 0.000 description 1
- 241000723347 Cinnamomum Species 0.000 description 1
- 241000255925 Diptera Species 0.000 description 1
- 208000003098 Ganglion Cysts Diseases 0.000 description 1
- 241000238631 Hexapoda Species 0.000 description 1
- 241000282412 Homo Species 0.000 description 1
- RKUNBYITZUJHSG-UHFFFAOYSA-N Hyosciamin-hydrochlorid Natural products CN1C(C2)CCC1CC2OC(=O)C(CO)C1=CC=CC=C1 RKUNBYITZUJHSG-UHFFFAOYSA-N 0.000 description 1
- 241000699666 Mus <mouse, genus> Species 0.000 description 1
- 208000006550 Mydriasis Diseases 0.000 description 1
- SNIOPGDIGTZGOP-UHFFFAOYSA-N Nitroglycerin Chemical compound [O-][N+](=O)OCC(O[N+]([O-])=O)CO[N+]([O-])=O SNIOPGDIGTZGOP-UHFFFAOYSA-N 0.000 description 1
- 239000000006 Nitroglycerin Substances 0.000 description 1
- 206010034010 Parkinsonism Diseases 0.000 description 1
- 241000700159 Rattus Species 0.000 description 1
- 208000005400 Synovial Cyst Diseases 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 230000002350 accommodative effect Effects 0.000 description 1
- 238000009825 accumulation Methods 0.000 description 1
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 1
- 229910052782 aluminium Inorganic materials 0.000 description 1
- 150000001412 amines Chemical class 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- RKUNBYITZUJHSG-SPUOUPEWSA-N atropine Chemical compound O([C@H]1C[C@H]2CC[C@@H](C1)N2C)C(=O)C(CO)C1=CC=CC=C1 RKUNBYITZUJHSG-SPUOUPEWSA-N 0.000 description 1
- 229960000396 atropine Drugs 0.000 description 1
- 230000002567 autonomic effect Effects 0.000 description 1
- 210000000467 autonomic pathway Anatomy 0.000 description 1
- 230000000975 bioactive effect Effects 0.000 description 1
- 239000002981 blocking agent Substances 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 210000005098 blood-cerebrospinal fluid barrier Anatomy 0.000 description 1
- 125000002091 cationic group Chemical group 0.000 description 1
- 230000009956 central mechanism Effects 0.000 description 1
- 210000001175 cerebrospinal fluid Anatomy 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- XGGHHHBGPSNXFE-ZSHCYNCHSA-N chembl1186610 Chemical compound C1[C@H](OC(=O)C(CCC)CCC)C[C@@H]2CC[C@H]1[N+]2(C)C XGGHHHBGPSNXFE-ZSHCYNCHSA-N 0.000 description 1
- OEYIOHPDSNJKLS-UHFFFAOYSA-N choline Chemical compound C[N+](C)(C)CCO OEYIOHPDSNJKLS-UHFFFAOYSA-N 0.000 description 1
- 229960001231 choline Drugs 0.000 description 1
- 235000017803 cinnamon Nutrition 0.000 description 1
- 230000006378 damage Effects 0.000 description 1
- 238000001804 debridement Methods 0.000 description 1
- 239000000645 desinfectant Substances 0.000 description 1
- MNSQDVCVWNXBFQ-UHFFFAOYSA-N dihexyverine Chemical compound C1CCCCC1(C1CCCCC1)C(=O)OCCN1CCCCC1 MNSQDVCVWNXBFQ-UHFFFAOYSA-N 0.000 description 1
- 229960003215 dihexyverine Drugs 0.000 description 1
- 230000010339 dilation Effects 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 208000002173 dizziness Diseases 0.000 description 1
- 206010013781 dry mouth Diseases 0.000 description 1
- 230000002500 effect on skin Effects 0.000 description 1
- 239000013013 elastic material Substances 0.000 description 1
- 230000002964 excitative effect Effects 0.000 description 1
- 210000000609 ganglia Anatomy 0.000 description 1
- 239000003457 ganglion blocking agent Substances 0.000 description 1
- 210000004211 gastric acid Anatomy 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 210000004907 gland Anatomy 0.000 description 1
- 239000003292 glue Substances 0.000 description 1
- 229960003711 glyceryl trinitrate Drugs 0.000 description 1
- 210000003128 head Anatomy 0.000 description 1
- BHEPBYXIRTUNPN-UHFFFAOYSA-N hydridophosphorus(.) (triplet) Chemical compound [PH] BHEPBYXIRTUNPN-UHFFFAOYSA-N 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 230000030214 innervation Effects 0.000 description 1
- 230000000622 irritating effect Effects 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 230000010534 mechanism of action Effects 0.000 description 1
- MBABOKRGFJTBAE-UHFFFAOYSA-N methyl methanesulfonate Chemical compound COS(C)(=O)=O MBABOKRGFJTBAE-UHFFFAOYSA-N 0.000 description 1
- 230000004899 motility Effects 0.000 description 1
- 230000002644 neurohormonal effect Effects 0.000 description 1
- 230000003472 neutralizing effect Effects 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 230000037311 normal skin Effects 0.000 description 1
- 229950005306 octatropine methylbromide Drugs 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 230000000149 penetrating effect Effects 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 150000003018 phosphorus compounds Chemical class 0.000 description 1
- 230000001766 physiological effect Effects 0.000 description 1
- 238000002203 pretreatment Methods 0.000 description 1
- 210000001747 pupil Anatomy 0.000 description 1
- 206010037844 rash Diseases 0.000 description 1
- 210000003296 saliva Anatomy 0.000 description 1
- 238000005201 scrubbing Methods 0.000 description 1
- 230000003248 secreting effect Effects 0.000 description 1
- 230000037380 skin damage Effects 0.000 description 1
- 230000004936 stimulating effect Effects 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 210000000225 synapse Anatomy 0.000 description 1
- 230000005062 synaptic transmission Effects 0.000 description 1
- 150000003512 tertiary amines Chemical class 0.000 description 1
- 239000003860 topical agent Substances 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 229940100640 transdermal system Drugs 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- 230000032258 transport Effects 0.000 description 1
- 230000002485 urinary effect Effects 0.000 description 1
- 235000021419 vinegar Nutrition 0.000 description 1
- 239000000052 vinegar Substances 0.000 description 1
- 230000000007 visual effect Effects 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
- 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)
- Bioinformatics & Cheminformatics (AREA)
- Dermatology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US65991984A | 1984-10-11 | 1984-10-11 | |
| US659919 | 2003-09-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPS62500523A true JPS62500523A (ja) | 1987-03-05 |
Family
ID=24647370
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP60504771A Pending JPS62500523A (ja) | 1984-10-11 | 1985-10-09 | 薬剤の経皮送達促進の生理学的手段 |
Country Status (15)
| Country | Link |
|---|---|
| EP (1) | EP0198034B1 (enEXAMPLES) |
| JP (1) | JPS62500523A (enEXAMPLES) |
| KR (1) | KR930009787B1 (enEXAMPLES) |
| AU (1) | AU592322B2 (enEXAMPLES) |
| CA (1) | CA1264033A (enEXAMPLES) |
| DE (1) | DE3583234D1 (enEXAMPLES) |
| DK (1) | DK269986A (enEXAMPLES) |
| FI (1) | FI862493A7 (enEXAMPLES) |
| GR (1) | GR852469B (enEXAMPLES) |
| IE (1) | IE59291B1 (enEXAMPLES) |
| IL (1) | IL76635A0 (enEXAMPLES) |
| MY (1) | MY100471A (enEXAMPLES) |
| NO (1) | NO862321L (enEXAMPLES) |
| NZ (1) | NZ213753A (enEXAMPLES) |
| WO (1) | WO1986002272A1 (enEXAMPLES) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2002523458A (ja) * | 1998-08-31 | 2002-07-30 | アーサー エム． ボブローブ， | ヒトにおけるのぼせの処置のための方法 |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SU1705319A1 (ru) * | 1987-10-23 | 1992-01-15 | Всесоюзный Научно-Исследовательский Институт Биотехнологии | Состав полимерной диффузионной матрицы дл трансдермального введени лекарственных веществ |
| AU2002340058A1 (en) * | 2001-09-26 | 2003-04-07 | Alison B. Lukacsko | Compositions and methods for inhibiting eccrine perspiration in humans |
| ATE520390T1 (de) | 2004-12-27 | 2011-09-15 | Beiersdorf Ag | Glycopyrrolat in kosmetischen zubereitungen |
| KR102232806B1 (ko) | 2013-02-28 | 2021-03-29 | 더미라, 인코포레이티드 | 글리코피롤레이트 염 |
| US9006462B2 (en) | 2013-02-28 | 2015-04-14 | Dermira, Inc. | Glycopyrrolate salts |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US376886A (en) * | 1888-01-24 | Joseph beeakley holder | ||
| US3767786A (en) * | 1961-04-20 | 1973-10-23 | Procter & Gamble | Inhibiting perspiration with scopolamine esters |
| US4031894A (en) * | 1975-12-08 | 1977-06-28 | Alza Corporation | Bandage for transdermally administering scopolamine to prevent nausea |
| NL8104929A (nl) * | 1980-11-12 | 1982-06-01 | Alza Corp | Anticholinergische preparaten, alsmede de bereiding en de toepassing ervan. |
| US4379454A (en) * | 1981-02-17 | 1983-04-12 | Alza Corporation | Dosage for coadministering drug and percutaneous absorption enhancer |
-
1985
- 1985-10-09 AU AU49685/85A patent/AU592322B2/en not_active Ceased
- 1985-10-09 WO PCT/US1985/001951 patent/WO1986002272A1/en active IP Right Grant
- 1985-10-09 JP JP60504771A patent/JPS62500523A/ja active Pending
- 1985-10-09 DE DE8585905267T patent/DE3583234D1/de not_active Expired - Lifetime
- 1985-10-09 KR KR1019860700351A patent/KR930009787B1/ko not_active Expired - Fee Related
- 1985-10-09 NZ NZ213753A patent/NZ213753A/xx unknown
- 1985-10-09 IL IL76635A patent/IL76635A0/xx not_active IP Right Cessation
- 1985-10-09 EP EP85905267A patent/EP0198034B1/en not_active Expired - Lifetime
- 1985-10-10 CA CA000492685A patent/CA1264033A/en not_active Expired
- 1985-10-10 IE IE249185A patent/IE59291B1/en not_active IP Right Cessation
- 1985-10-11 GR GR852469A patent/GR852469B/el unknown
-
1986
- 1986-06-09 DK DK269986A patent/DK269986A/da not_active Application Discontinuation
- 1986-06-10 NO NO862321A patent/NO862321L/no unknown
- 1986-06-11 FI FI862493A patent/FI862493A7/fi not_active Application Discontinuation
-
1987
- 1987-09-22 MY MYPI87001837A patent/MY100471A/en unknown
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2002523458A (ja) * | 1998-08-31 | 2002-07-30 | アーサー エム． ボブローブ， | ヒトにおけるのぼせの処置のための方法 |
Also Published As
| Publication number | Publication date |
|---|---|
| GR852469B (enEXAMPLES) | 1986-02-12 |
| FI862493A0 (fi) | 1986-06-11 |
| WO1986002272A1 (en) | 1986-04-24 |
| EP0198034A1 (en) | 1986-10-22 |
| IE59291B1 (en) | 1994-02-09 |
| EP0198034B1 (en) | 1991-06-12 |
| IL76635A0 (en) | 1986-02-28 |
| AU592322B2 (en) | 1990-01-11 |
| AU4968585A (en) | 1986-05-02 |
| CA1264033A (en) | 1989-12-27 |
| MY100471A (en) | 1990-10-15 |
| NZ213753A (en) | 1988-09-29 |
| FI862493A7 (fi) | 1986-06-11 |
| DK269986A (da) | 1986-08-11 |
| DK269986D0 (da) | 1986-06-09 |
| IE852491L (en) | 1986-04-11 |
| KR870700364A (ko) | 1987-12-28 |
| KR930009787B1 (ko) | 1993-10-11 |
| DE3583234D1 (de) | 1991-07-18 |
| NO862321L (no) | 1986-08-07 |
| NO862321D0 (no) | 1986-06-10 |
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