KR20050120726A - 준안정성 약제학적 조성물 - Google Patents
준안정성 약제학적 조성물 Download PDFInfo
- Publication number
- KR20050120726A KR20050120726A KR1020047020966A KR20047020966A KR20050120726A KR 20050120726 A KR20050120726 A KR 20050120726A KR 1020047020966 A KR1020047020966 A KR 1020047020966A KR 20047020966 A KR20047020966 A KR 20047020966A KR 20050120726 A KR20050120726 A KR 20050120726A
- Authority
- KR
- South Korea
- Prior art keywords
- pharmaceutical composition
- physiologically active
- active substance
- composition
- volatile solvent
- Prior art date
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- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 27
- 239000002904 solvent Substances 0.000 claims abstract description 53
- 239000013543 active substance Substances 0.000 claims abstract description 48
- 238000001704 evaporation Methods 0.000 claims abstract description 11
- 230000008020 evaporation Effects 0.000 claims abstract description 11
- 230000037317 transdermal delivery Effects 0.000 claims abstract description 10
- 239000000203 mixture Substances 0.000 claims description 56
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 42
- 210000003491 skin Anatomy 0.000 claims description 39
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims description 31
- 239000002244 precipitate Substances 0.000 claims description 24
- 230000008018 melting Effects 0.000 claims description 15
- 238000002844 melting Methods 0.000 claims description 15
- MUMGGOZAMZWBJJ-DYKIIFRCSA-N Testostosterone Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 MUMGGOZAMZWBJJ-DYKIIFRCSA-N 0.000 claims description 14
- 229960002428 fentanyl Drugs 0.000 claims description 13
- IVLVTNPOHDFFCJ-UHFFFAOYSA-N fentanyl citrate Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O.C=1C=CC=CC=1N(C(=O)CC)C(CC1)CCN1CCC1=CC=CC=C1 IVLVTNPOHDFFCJ-UHFFFAOYSA-N 0.000 claims description 13
- 239000003380 propellant Substances 0.000 claims description 11
- 210000000434 stratum corneum Anatomy 0.000 claims description 11
- 239000007921 spray Substances 0.000 claims description 10
- 210000002615 epidermis Anatomy 0.000 claims description 9
- 229960003604 testosterone Drugs 0.000 claims description 9
- 238000010521 absorption reaction Methods 0.000 claims description 7
- -1 lopinirol Chemical compound 0.000 claims description 7
- BFPYWIDHMRZLRN-SLHNCBLASA-N Ethinyl estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 BFPYWIDHMRZLRN-SLHNCBLASA-N 0.000 claims description 6
- 239000000443 aerosol Substances 0.000 claims description 6
- 150000001875 compounds Chemical class 0.000 claims description 6
- 229960002568 ethinylestradiol Drugs 0.000 claims description 6
- 238000000034 method Methods 0.000 claims description 6
- 150000003839 salts Chemical class 0.000 claims description 5
- LVGUZGTVOIAKKC-UHFFFAOYSA-N 1,1,1,2-tetrafluoroethane Chemical group FCC(F)(F)F LVGUZGTVOIAKKC-UHFFFAOYSA-N 0.000 claims description 4
- 230000000699 topical effect Effects 0.000 claims description 4
- XSVMFMHYUFZWBK-NSHDSACASA-N Rivastigmine Chemical compound CCN(C)C(=O)OC1=CC=CC([C@H](C)N(C)C)=C1 XSVMFMHYUFZWBK-NSHDSACASA-N 0.000 claims description 3
- 150000001298 alcohols Chemical class 0.000 claims description 3
- VMWNQDUVQKEIOC-CYBMUJFWSA-N apomorphine Chemical compound C([C@H]1N(C)CC2)C3=CC=C(O)C(O)=C3C3=C1C2=CC=C3 VMWNQDUVQKEIOC-CYBMUJFWSA-N 0.000 claims description 3
- 229960004046 apomorphine Drugs 0.000 claims description 3
- 229960004136 rivastigmine Drugs 0.000 claims description 3
- YSGQGNQWBLYHPE-CFUSNLFHSA-N (7r,8r,9s,10r,13s,14s,17s)-17-hydroxy-7,13-dimethyl-2,6,7,8,9,10,11,12,14,15,16,17-dodecahydro-1h-cyclopenta[a]phenanthren-3-one Chemical compound C1C[C@]2(C)[C@@H](O)CC[C@H]2[C@@H]2[C@H](C)CC3=CC(=O)CC[C@@H]3[C@H]21 YSGQGNQWBLYHPE-CFUSNLFHSA-N 0.000 claims description 2
- 239000004215 Carbon black (E152) Substances 0.000 claims description 2
- 229920002125 Sokalan® Polymers 0.000 claims description 2
- 239000001913 cellulose Substances 0.000 claims description 2
- 229920002678 cellulose Polymers 0.000 claims description 2
- 229930195733 hydrocarbon Natural products 0.000 claims description 2
- 239000007788 liquid Substances 0.000 claims description 2
- 229920006395 saturated elastomer Polymers 0.000 claims description 2
- 239000002562 thickening agent Substances 0.000 claims 3
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 claims 1
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 1
- 230000001078 anti-cholinergic effect Effects 0.000 claims 1
- 150000002430 hydrocarbons Chemical class 0.000 claims 1
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 claims 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 1
- 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 claims 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 1
- 230000000717 retained effect Effects 0.000 claims 1
- TXHZXHICDBAVJW-UHFFFAOYSA-N rizatriptan Chemical compound C=1[C]2C(CCN(C)C)=CN=C2C=CC=1CN1C=NC=N1 TXHZXHICDBAVJW-UHFFFAOYSA-N 0.000 claims 1
- 229960000425 rizatriptan Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 description 27
- 229940079593 drug Drugs 0.000 description 26
- 238000009792 diffusion process Methods 0.000 description 12
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 8
- 239000004480 active ingredient Substances 0.000 description 7
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 6
- 238000009472 formulation Methods 0.000 description 6
- 230000035515 penetration Effects 0.000 description 6
- 230000009467 reduction Effects 0.000 description 6
- 238000002425 crystallisation Methods 0.000 description 5
- 230000008025 crystallization Effects 0.000 description 5
- 230000000694 effects Effects 0.000 description 5
- 239000007787 solid Substances 0.000 description 5
- 230000001419 dependent effect Effects 0.000 description 4
- 239000000243 solution Substances 0.000 description 4
- WVDDGKGOMKODPV-UHFFFAOYSA-N Benzyl alcohol Chemical compound OCC1=CC=CC=C1 WVDDGKGOMKODPV-UHFFFAOYSA-N 0.000 description 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- 206010040880 Skin irritation Diseases 0.000 description 3
- 230000004888 barrier function Effects 0.000 description 3
- 239000013078 crystal Substances 0.000 description 3
- 210000004207 dermis Anatomy 0.000 description 3
- 238000010952 in-situ formation Methods 0.000 description 3
- 150000002632 lipids Chemical class 0.000 description 3
- 239000012047 saturated solution Substances 0.000 description 3
- 230000036556 skin irritation Effects 0.000 description 3
- 231100000475 skin irritation Toxicity 0.000 description 3
- 238000000935 solvent evaporation Methods 0.000 description 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 2
- 229910052782 aluminium Inorganic materials 0.000 description 2
- 230000008901 benefit Effects 0.000 description 2
- 230000008859 change Effects 0.000 description 2
- 238000009826 distribution Methods 0.000 description 2
- 238000002474 experimental method Methods 0.000 description 2
- 230000008014 freezing Effects 0.000 description 2
- 238000007710 freezing Methods 0.000 description 2
- 238000000338 in vitro Methods 0.000 description 2
- 238000011065 in-situ storage Methods 0.000 description 2
- 230000004941 influx Effects 0.000 description 2
- 230000007794 irritation Effects 0.000 description 2
- 230000037311 normal skin Effects 0.000 description 2
- 230000008447 perception Effects 0.000 description 2
- 230000000144 pharmacologic effect Effects 0.000 description 2
- 239000012453 solvate Substances 0.000 description 2
- 238000003860 storage Methods 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 229940041677 topical spray Drugs 0.000 description 2
- 238000011282 treatment Methods 0.000 description 2
- YFMFNYKEUDLDTL-UHFFFAOYSA-N 1,1,1,2,3,3,3-heptafluoropropane Chemical compound FC(F)(F)C(F)C(F)(F)F YFMFNYKEUDLDTL-UHFFFAOYSA-N 0.000 description 1
- 208000018522 Gastrointestinal disease Diseases 0.000 description 1
- 102000011782 Keratins Human genes 0.000 description 1
- 108010076876 Keratins Proteins 0.000 description 1
- 230000018199 S phase Effects 0.000 description 1
- 239000011149 active material Substances 0.000 description 1
- 239000003242 anti bacterial agent Substances 0.000 description 1
- 229940088710 antibiotic agent Drugs 0.000 description 1
- 235000019445 benzyl alcohol Nutrition 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 238000013270 controlled release Methods 0.000 description 1
- 230000001186 cumulative effect Effects 0.000 description 1
- 238000000113 differential scanning calorimetry Methods 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 239000013583 drug formulation Substances 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 230000002500 effect on skin Effects 0.000 description 1
- 239000003623 enhancer Substances 0.000 description 1
- 230000002708 enhancing effect Effects 0.000 description 1
- 238000000605 extraction Methods 0.000 description 1
- 239000003349 gelling agent Substances 0.000 description 1
- 238000004128 high performance liquid chromatography Methods 0.000 description 1
- 230000004968 inflammatory condition Effects 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 239000003607 modifier Substances 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 230000000149 penetrating effect Effects 0.000 description 1
- 230000035699 permeability Effects 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 229940124531 pharmaceutical excipient Drugs 0.000 description 1
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- 238000002360 preparation method Methods 0.000 description 1
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- 206010040872 skin infection Diseases 0.000 description 1
- 231100000245 skin permeability Toxicity 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 229910001220 stainless steel Inorganic materials 0.000 description 1
- 239000010935 stainless steel Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- 238000013271 transdermal drug delivery Methods 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
- 230000004580 weight loss Effects 0.000 description 1
Classifications
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
- A61K31/568—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
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- 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
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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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- A61K31/567—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
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- 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
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- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
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Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Endocrinology (AREA)
- Inorganic Chemistry (AREA)
- Reproductive Health (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Rheumatology (AREA)
- Gynecology & Obstetrics (AREA)
- Dermatology (AREA)
- Diabetes (AREA)
- Psychology (AREA)
- Urology & Nephrology (AREA)
- Psychiatry (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AUPS3173A AUPS317302A0 (en) | 2002-06-25 | 2002-06-25 | Metastable pharmaceutical compositions |
| AUPS3173 | 2002-06-25 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20050120726A true KR20050120726A (ko) | 2005-12-23 |
Family
ID=3836732
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020047020966A KR20050120726A (ko) | 2002-06-25 | 2003-06-24 | 준안정성 약제학적 조성물 |
Country Status (9)
| Country | Link |
|---|---|
| EP (1) | EP1531867A4 (fr) |
| JP (2) | JP2005534670A (fr) |
| KR (1) | KR20050120726A (fr) |
| AU (1) | AUPS317302A0 (fr) |
| BR (1) | BR0312003A (fr) |
| CA (1) | CA2490057A1 (fr) |
| EA (1) | EA012648B1 (fr) |
| NZ (1) | NZ537436A (fr) |
| WO (1) | WO2004000361A1 (fr) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2688571A1 (fr) | 2011-03-22 | 2014-01-29 | The Population Council, Inc. | Rénégération de myéline par des androgènes |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH0794378B2 (ja) * | 1989-08-18 | 1995-10-11 | 久光製薬株式会社 | エアゾール剤 |
| JPH0383924A (ja) * | 1989-08-28 | 1991-04-09 | Kanebo Ltd | 経皮投与用組成物 |
| JP2974081B2 (ja) * | 1990-07-26 | 1999-11-08 | 小池化学株式会社 | 人体用エアゾール組成物 |
| JP2769925B2 (ja) * | 1990-10-18 | 1998-06-25 | ミネソタ マイニング アンド マニュファクチャリング カンパニー | ベクロメタゾン１７，２１ジプロピオネートを含んで成るエアロゾル製剤 |
| CA2101496A1 (fr) * | 1992-07-31 | 1994-02-01 | Masao Kobayashi | Base pour administration transdermique |
| AUPN814496A0 (en) * | 1996-02-19 | 1996-03-14 | Monash University | Dermal penetration enhancer |
| DE19616539A1 (de) * | 1996-04-25 | 1997-11-06 | Luitpold Pharma Gmbh | Acetylsalicylsäure enthaltende alkoholische Lösungen zur perkutanen Anwendung, deren Verwendung zur antithrombotischen Therapie sowie Arzneimittel |
| US5968919A (en) * | 1997-10-16 | 1999-10-19 | Macrochem Corporation | Hormone replacement therapy drug formulations for topical application to the skin |
| HUP0105336A3 (en) * | 1999-02-05 | 2004-06-28 | Cipla Ltd Mumbai | Topical spray compositions |
| US6368618B1 (en) * | 1999-07-01 | 2002-04-09 | The University Of Georgia Research Foundation, Inc. | Composition and method for enhanced transdermal absorption of nonsteroidal anti-inflammatory drugs |
| NZ524601A (en) * | 2000-08-30 | 2006-04-28 | Unimed Pharmaceuticals Inc | Method for treating erectile dysfunction and increasing libido in men |
| KR20030048021A (ko) * | 2000-08-30 | 2003-06-18 | 유니메드 파마슈티칼스, 인크. | 여성의 테스토스테론 및 관련된 스테로이드의 농도를증가시키는 방법 |
-
2002
- 2002-06-25 AU AUPS3173A patent/AUPS317302A0/en not_active Abandoned
-
2003
- 2003-06-24 KR KR1020047020966A patent/KR20050120726A/ko not_active Application Discontinuation
- 2003-06-24 NZ NZ537436A patent/NZ537436A/en not_active IP Right Cessation
- 2003-06-24 CA CA002490057A patent/CA2490057A1/fr not_active Abandoned
- 2003-06-24 JP JP2004514438A patent/JP2005534670A/ja not_active Withdrawn
- 2003-06-24 EA EA200500083A patent/EA012648B1/ru not_active IP Right Cessation
- 2003-06-24 EP EP03729714A patent/EP1531867A4/fr not_active Withdrawn
- 2003-06-24 WO PCT/AU2003/000785 patent/WO2004000361A1/fr active Application Filing
- 2003-06-24 BR BR0312003-1A patent/BR0312003A/pt not_active IP Right Cessation
-
2010
- 2010-07-30 JP JP2010172167A patent/JP2010248250A/ja not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| EA200500083A1 (ru) | 2005-08-25 |
| JP2005534670A (ja) | 2005-11-17 |
| BR0312003A (pt) | 2005-03-22 |
| EP1531867A1 (fr) | 2005-05-25 |
| NZ537436A (en) | 2007-01-26 |
| WO2004000361A1 (fr) | 2003-12-31 |
| CA2490057A1 (fr) | 2003-12-31 |
| EP1531867A4 (fr) | 2011-03-23 |
| AUPS317302A0 (en) | 2002-07-18 |
| JP2010248250A (ja) | 2010-11-04 |
| EA012648B1 (ru) | 2009-12-30 |
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| A201 | Request for examination | ||
| E902 | Notification of reason for refusal | ||
| E601 | Decision to refuse application |