CN1067811A - 利用透过皮肤来吸收尼古丁的投药组包及方法 - Google Patents
利用透过皮肤来吸收尼古丁的投药组包及方法 Download PDFInfo
- Publication number
- CN1067811A CN1067811A CN 92105287 CN92105287A CN1067811A CN 1067811 A CN1067811 A CN 1067811A CN 92105287 CN92105287 CN 92105287 CN 92105287 A CN92105287 A CN 92105287A CN 1067811 A CN1067811 A CN 1067811A
- Authority
- CN
- China
- Prior art keywords
- nicotine
- group bag
- dispensing group
- skin
- acid ester
- 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.)
- Withdrawn
Links
- SNICXCGAKADSCV-JTQLQIEISA-N (-)-Nicotine Chemical compound CN1CCC[C@H]1C1=CC=CN=C1 SNICXCGAKADSCV-JTQLQIEISA-N 0.000 title claims abstract description 130
- 229960002715 nicotine Drugs 0.000 title claims abstract description 130
- SNICXCGAKADSCV-UHFFFAOYSA-N nicotine Natural products CN1CCCC1C1=CC=CN=C1 SNICXCGAKADSCV-UHFFFAOYSA-N 0.000 title claims abstract description 130
- 238000000034 method Methods 0.000 title claims abstract description 18
- 238000010521 absorption reaction Methods 0.000 claims abstract description 29
- 235000002637 Nicotiana tabacum Nutrition 0.000 claims abstract description 15
- 235000019788 craving Nutrition 0.000 claims abstract description 9
- 241000208125 Nicotiana Species 0.000 claims abstract description 7
- OSWPMRLSEDHDFF-UHFFFAOYSA-N methyl salicylate Chemical compound COC(=O)C1=CC=CC=C1O OSWPMRLSEDHDFF-UHFFFAOYSA-N 0.000 claims description 37
- 150000002148 esters Chemical class 0.000 claims description 36
- 239000002253 acid Substances 0.000 claims description 32
- 241000124033 Salix Species 0.000 claims description 30
- 229920000642 polymer Polymers 0.000 claims description 29
- 239000000203 mixture Substances 0.000 claims description 27
- 239000003795 chemical substances by application Substances 0.000 claims description 26
- HIQIXEFWDLTDED-UHFFFAOYSA-N 4-hydroxy-1-piperidin-4-ylpyrrolidin-2-one Chemical group O=C1CC(O)CN1C1CCNCC1 HIQIXEFWDLTDED-UHFFFAOYSA-N 0.000 claims description 25
- 229960001047 methyl salicylate Drugs 0.000 claims description 18
- 239000011159 matrix material Substances 0.000 claims description 15
- 238000002360 preparation method Methods 0.000 claims description 15
- 239000011248 coating agent Substances 0.000 claims description 11
- 238000000576 coating method Methods 0.000 claims description 11
- 230000008569 process Effects 0.000 claims description 7
- 229920002125 Sokalan® Polymers 0.000 claims description 6
- 239000004584 polyacrylic acid Substances 0.000 claims description 6
- 230000001737 promoting effect Effects 0.000 claims description 5
- 239000004615 ingredient Substances 0.000 claims description 3
- 239000002998 adhesive polymer Substances 0.000 claims 3
- 229920002959 polymer blend Polymers 0.000 claims 2
- 239000003814 drug Substances 0.000 abstract description 17
- 244000061176 Nicotiana tabacum Species 0.000 abstract description 8
- 239000010410 layer Substances 0.000 description 44
- 239000000463 material Substances 0.000 description 11
- 230000004907 flux Effects 0.000 description 10
- 201000004624 Dermatitis Diseases 0.000 description 9
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 9
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 8
- 230000000391 smoking effect Effects 0.000 description 8
- 239000000243 solution Substances 0.000 description 8
- 238000012360 testing method Methods 0.000 description 8
- 239000003963 antioxidant agent Substances 0.000 description 7
- 230000003078 antioxidant effect Effects 0.000 description 7
- 235000006708 antioxidants Nutrition 0.000 description 7
- 238000003475 lamination Methods 0.000 description 7
- 239000000758 substrate Substances 0.000 description 7
- 230000002500 effect on skin Effects 0.000 description 6
- 229920000058 polyacrylate Polymers 0.000 description 5
- -1 polyethylene Polymers 0.000 description 5
- 230000001681 protective effect Effects 0.000 description 5
- GYCKQBWUSACYIF-UHFFFAOYSA-N Ethyl salicylate Chemical compound CCOC(=O)C1=CC=CC=C1O GYCKQBWUSACYIF-UHFFFAOYSA-N 0.000 description 4
- 229960005070 ascorbic acid Drugs 0.000 description 4
- 235000010323 ascorbic acid Nutrition 0.000 description 4
- 239000011668 ascorbic acid Substances 0.000 description 4
- 150000001875 compounds Chemical class 0.000 description 4
- 229940005667 ethyl salicylate Drugs 0.000 description 4
- 239000010408 film Substances 0.000 description 4
- 210000004072 lung Anatomy 0.000 description 4
- 239000002184 metal Substances 0.000 description 4
- 229910052751 metal Inorganic materials 0.000 description 4
- 230000003647 oxidation Effects 0.000 description 4
- 238000007254 oxidation reaction Methods 0.000 description 4
- 230000035699 permeability Effects 0.000 description 4
- 239000013047 polymeric layer Substances 0.000 description 4
- 239000000126 substance Substances 0.000 description 4
- 206010002198 Anaphylactic reaction Diseases 0.000 description 3
- 241000283973 Oryctolagus cuniculus Species 0.000 description 3
- 230000036783 anaphylactic response Effects 0.000 description 3
- 208000003455 anaphylaxis Diseases 0.000 description 3
- 230000008859 change Effects 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- AQCRXZYYMOXFAN-UHFFFAOYSA-N 2-(1-methyl-2-pyrrolidinyl)-pyridine Chemical compound CN1CCCC1C1=CC=CC=N1 AQCRXZYYMOXFAN-UHFFFAOYSA-N 0.000 description 2
- VYZAHLCBVHPDDF-UHFFFAOYSA-N Dinitrochlorobenzene Chemical compound [O-][N+](=O)C1=CC=C(Cl)C([N+]([O-])=O)=C1 VYZAHLCBVHPDDF-UHFFFAOYSA-N 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- 206010020751 Hypersensitivity Diseases 0.000 description 2
- 208000027418 Wounds and injury Diseases 0.000 description 2
- 230000001154 acute effect Effects 0.000 description 2
- 230000008901 benefit Effects 0.000 description 2
- 210000001124 body fluid Anatomy 0.000 description 2
- 239000010839 body fluid Substances 0.000 description 2
- 238000005266 casting Methods 0.000 description 2
- 238000006243 chemical reaction Methods 0.000 description 2
- 230000006378 damage Effects 0.000 description 2
- 238000010790 dilution Methods 0.000 description 2
- 239000012895 dilution Substances 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 238000002474 experimental method Methods 0.000 description 2
- 230000002349 favourable effect Effects 0.000 description 2
- 239000011888 foil Substances 0.000 description 2
- 230000004927 fusion Effects 0.000 description 2
- 208000014674 injury Diseases 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 231100000344 non-irritating Toxicity 0.000 description 2
- ZQBAKBUEJOMQEX-UHFFFAOYSA-N phenyl salicylate Chemical compound OC1=CC=CC=C1C(=O)OC1=CC=CC=C1 ZQBAKBUEJOMQEX-UHFFFAOYSA-N 0.000 description 2
- 238000011084 recovery Methods 0.000 description 2
- 238000009738 saturating Methods 0.000 description 2
- 238000003860 storage Methods 0.000 description 2
- FWIQGIQRNBVZEN-UHFFFAOYSA-N 4-ethoxy-2-(2-ethoxy-2-oxoethyl)-2-hydroxy-4-oxobutanoic acid Chemical compound CCOC(=O)CC(O)(C(O)=O)CC(=O)OCC FWIQGIQRNBVZEN-UHFFFAOYSA-N 0.000 description 1
- BRPCDOLEVHTTRE-UHFFFAOYSA-N 6-oxo-6-propan-2-yloxyhexanoic acid Chemical compound CC(C)OC(=O)CCCCC(O)=O BRPCDOLEVHTTRE-UHFFFAOYSA-N 0.000 description 1
- 201000009030 Carcinoma Diseases 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 1
- DNXHEGUUPJUMQT-CBZIJGRNSA-N Estrone Chemical compound OC1=CC=C2[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1 DNXHEGUUPJUMQT-CBZIJGRNSA-N 0.000 description 1
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 description 1
- IJMWOMHMDSDKGK-UHFFFAOYSA-N Isopropyl propionate Chemical compound CCC(=O)OC(C)C IJMWOMHMDSDKGK-UHFFFAOYSA-N 0.000 description 1
- AXISYYRBXTVTFY-UHFFFAOYSA-N Isopropyl tetradecanoate Chemical class CCCCCCCCCCCCCC(=O)OC(C)C AXISYYRBXTVTFY-UHFFFAOYSA-N 0.000 description 1
- 239000004698 Polyethylene Substances 0.000 description 1
- 239000004743 Polypropylene Substances 0.000 description 1
- XUIMIQQOPSSXEZ-UHFFFAOYSA-N Silicon Chemical compound [Si] XUIMIQQOPSSXEZ-UHFFFAOYSA-N 0.000 description 1
- 206010040880 Skin irritation Diseases 0.000 description 1
- 206010043458 Thirst Diseases 0.000 description 1
- 230000002730 additional effect Effects 0.000 description 1
- 239000000853 adhesive Substances 0.000 description 1
- 230000001070 adhesive effect Effects 0.000 description 1
- 230000001476 alcoholic effect Effects 0.000 description 1
- 150000001298 alcohols Chemical class 0.000 description 1
- 125000001931 aliphatic group Chemical group 0.000 description 1
- 125000000217 alkyl group Chemical group 0.000 description 1
- 208000026935 allergic disease Diseases 0.000 description 1
- 239000005030 aluminium foil Substances 0.000 description 1
- 210000002821 alveolar epithelial cell Anatomy 0.000 description 1
- 150000001408 amides Chemical class 0.000 description 1
- 230000008485 antagonism Effects 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000005540 biological transmission Effects 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
- 239000003153 chemical reaction reagent Substances 0.000 description 1
- 235000019504 cigarettes Nutrition 0.000 description 1
- 238000010276 construction Methods 0.000 description 1
- 238000005520 cutting process Methods 0.000 description 1
- 230000002354 daily effect Effects 0.000 description 1
- YSAVZVORKRDODB-WDSKDSINSA-N diethyl tartrate Chemical compound CCOC(=O)[C@@H](O)[C@H](O)C(=O)OCC YSAVZVORKRDODB-WDSKDSINSA-N 0.000 description 1
- 238000009792 diffusion process Methods 0.000 description 1
- LQZZUXJYWNFBMV-UHFFFAOYSA-N dodecan-1-ol Chemical compound CCCCCCCCCCCCO LQZZUXJYWNFBMV-UHFFFAOYSA-N 0.000 description 1
- 125000004494 ethyl ester group Chemical group 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 238000001704 evaporation Methods 0.000 description 1
- 230000008020 evaporation Effects 0.000 description 1
- 230000003203 everyday effect Effects 0.000 description 1
- 239000004744 fabric Substances 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 239000012456 homogeneous solution Substances 0.000 description 1
- 229930195733 hydrocarbon Natural products 0.000 description 1
- 150000002430 hydrocarbons Chemical class 0.000 description 1
- 230000009610 hypersensitivity Effects 0.000 description 1
- 230000006872 improvement Effects 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 229940074928 isopropyl myristate Drugs 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 239000012466 permeate Substances 0.000 description 1
- 239000000902 placebo Substances 0.000 description 1
- 229940068196 placebo Drugs 0.000 description 1
- 229920000728 polyester Polymers 0.000 description 1
- 229920000573 polyethylene Polymers 0.000 description 1
- 239000010695 polyglycol Substances 0.000 description 1
- 229920000151 polyglycol Polymers 0.000 description 1
- 229920006254 polymer film Polymers 0.000 description 1
- 229920001155 polypropylene Polymers 0.000 description 1
- 229920002635 polyurethane Polymers 0.000 description 1
- 239000004814 polyurethane Substances 0.000 description 1
- 239000011241 protective layer Substances 0.000 description 1
- 239000003542 rubefacient Substances 0.000 description 1
- 210000000582 semen Anatomy 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- 239000010703 silicon Substances 0.000 description 1
- 229910052710 silicon Inorganic materials 0.000 description 1
- 230000036556 skin irritation Effects 0.000 description 1
- 231100000475 skin irritation Toxicity 0.000 description 1
- 239000012453 solvate Substances 0.000 description 1
- 238000000638 solvent extraction Methods 0.000 description 1
- 238000013112 stability test Methods 0.000 description 1
- 239000010409 thin film Substances 0.000 description 1
- 230000035922 thirst 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
- A61K9/7038—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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/465—Nicotine; Derivatives thereof
-
- 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
- A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Dermatology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US72112991A | 1991-06-26 | 1991-06-26 | |
| US721,129 | 1991-06-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1067811A true CN1067811A (zh) | 1993-01-13 |
Family
ID=24896654
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 92105287 Withdrawn CN1067811A (zh) | 1991-06-26 | 1992-06-26 | 利用透过皮肤来吸收尼古丁的投药组包及方法 |
Country Status (6)
| Country | Link |
|---|---|
| EP (1) | EP0544900A4 (enrdf_load_stackoverflow) |
| CN (1) | CN1067811A (enrdf_load_stackoverflow) |
| AU (1) | AU2294192A (enrdf_load_stackoverflow) |
| CA (1) | CA2094913A1 (enrdf_load_stackoverflow) |
| TW (1) | TW221970B (enrdf_load_stackoverflow) |
| WO (1) | WO1993000057A1 (enrdf_load_stackoverflow) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1951375B (zh) * | 2005-10-13 | 2010-11-03 | 日东电工株式会社 | 烟碱透皮制剂及其生产方法 |
| CN104083344A (zh) * | 2005-06-21 | 2014-10-08 | 日东电工株式会社 | 烟碱经皮递送系统 |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2166869A1 (en) * | 1993-07-09 | 1995-01-19 | Ooi Wong | Method and device for providing nicotine replacement therapy transdermally/transbuccally |
| EP2377540A1 (en) * | 2010-03-31 | 2011-10-19 | Hexal AG | Transdermal patch containing 17-deacetyl norgestimate |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4933184A (en) * | 1983-12-22 | 1990-06-12 | American Home Products Corp. (Del) | Menthol enhancement of transdermal drug delivery |
| CH672888A5 (enrdf_load_stackoverflow) * | 1986-11-07 | 1990-01-15 | Mepha Ag | |
| US4908213A (en) * | 1989-02-21 | 1990-03-13 | Schering Corporation | Transdermal delivery of nicotine |
| DE4020144A1 (de) * | 1990-06-25 | 1992-01-09 | Lohmann Therapie Syst Lts | Pflaster mit hohem gehalt an weichmachenden inhaltsstoffen |
-
1992
- 1992-06-04 TW TW81104426A patent/TW221970B/zh not_active IP Right Cessation
- 1992-06-24 AU AU22941/92A patent/AU2294192A/en not_active Abandoned
- 1992-06-24 WO PCT/US1992/005271 patent/WO1993000057A1/en not_active Application Discontinuation
- 1992-06-24 EP EP19920915353 patent/EP0544900A4/en not_active Withdrawn
- 1992-06-24 CA CA002094913A patent/CA2094913A1/en not_active Abandoned
- 1992-06-26 CN CN 92105287 patent/CN1067811A/zh not_active Withdrawn
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104083344A (zh) * | 2005-06-21 | 2014-10-08 | 日东电工株式会社 | 烟碱经皮递送系统 |
| CN1951375B (zh) * | 2005-10-13 | 2010-11-03 | 日东电工株式会社 | 烟碱透皮制剂及其生产方法 |
Also Published As
| Publication number | Publication date |
|---|---|
| EP0544900A4 (en) | 1993-12-01 |
| AU2294192A (en) | 1993-01-25 |
| WO1993000057A1 (en) | 1993-01-07 |
| TW221970B (enrdf_load_stackoverflow) | 1994-04-01 |
| EP0544900A1 (en) | 1993-06-09 |
| CA2094913A1 (en) | 1992-12-27 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C03 | Withdrawal of patent application (patent law 1993) | ||
| WW01 | Invention patent application withdrawn after publication |