CA1090256A - Medicament pack and agent for the treatment of climacteric deficiency symptoms - Google Patents
Medicament pack and agent for the treatment of climacteric deficiency symptomsInfo
- Publication number
- CA1090256A CA1090256A CA288,196A CA288196A CA1090256A CA 1090256 A CA1090256 A CA 1090256A CA 288196 A CA288196 A CA 288196A CA 1090256 A CA1090256 A CA 1090256A
- Authority
- CA
- Canada
- Prior art keywords
- oestrogen
- pack
- daily
- dosage
- daily dosages
- 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.)
- Expired
Links
- 239000003795 chemical substances by application Substances 0.000 title claims abstract description 14
- 230000007812 deficiency Effects 0.000 title claims abstract description 12
- 208000024891 symptom Diseases 0.000 title claims abstract description 12
- 239000003814 drug Substances 0.000 title abstract description 3
- 239000000262 estrogen Substances 0.000 claims abstract description 156
- 239000000583 progesterone congener Substances 0.000 claims abstract description 44
- 229940088597 hormone Drugs 0.000 claims abstract description 15
- 239000005556 hormone Substances 0.000 claims abstract description 15
- 239000002552 dosage form Substances 0.000 claims abstract description 12
- 238000002360 preparation method Methods 0.000 claims abstract description 11
- PROQIPRRNZUXQM-ZXXIGWHRSA-N estriol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H]([C@H](O)C4)O)[C@@H]4[C@@H]3CCC2=C1 PROQIPRRNZUXQM-ZXXIGWHRSA-N 0.000 claims description 61
- PROQIPRRNZUXQM-UHFFFAOYSA-N (16alpha,17betaOH)-Estra-1,3,5(10)-triene-3,16,17-triol Natural products OC1=CC=C2C3CCC(C)(C(C(O)C4)O)C4C3CCC2=C1 PROQIPRRNZUXQM-UHFFFAOYSA-N 0.000 claims description 52
- RSEPBGGWRJCQGY-RBRWEJTLSA-N Estradiol valerate Chemical compound C1CC2=CC(O)=CC=C2[C@@H]2[C@@H]1[C@@H]1CC[C@H](OC(=O)CCCC)[C@@]1(C)CC2 RSEPBGGWRJCQGY-RBRWEJTLSA-N 0.000 claims description 35
- 239000008298 dragée Substances 0.000 claims description 35
- WWYNJERNGUHSAO-XUDSTZEESA-N (+)-Norgestrel Chemical compound O=C1CC[C@@H]2[C@H]3CC[C@](CC)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 WWYNJERNGUHSAO-XUDSTZEESA-N 0.000 claims description 20
- 229960004400 levonorgestrel Drugs 0.000 claims description 20
- 239000000825 pharmaceutical preparation Substances 0.000 claims description 16
- 230000001076 estrogenic effect Effects 0.000 claims description 8
- 230000003152 gestagenic effect Effects 0.000 claims description 6
- IMONTRJLAWHYGT-ZCPXKWAGSA-N Norethindrone Acetate Chemical compound C1CC2=CC(=O)CC[C@@H]2[C@@H]2[C@@H]1[C@@H]1CC[C@](C#C)(OC(=O)C)[C@@]1(C)CC2 IMONTRJLAWHYGT-ZCPXKWAGSA-N 0.000 claims description 5
- 229960000978 cyproterone acetate Drugs 0.000 claims description 5
- UWFYSQMTEOIJJG-FDTZYFLXSA-N cyproterone acetate Chemical compound C1=C(Cl)C2=CC(=O)[C@@H]3C[C@@H]3[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(C)=O)(OC(=O)C)[C@@]1(C)CC2 UWFYSQMTEOIJJG-FDTZYFLXSA-N 0.000 claims description 5
- 229960001652 norethindrone acetate Drugs 0.000 claims description 5
- 239000004480 active ingredient Substances 0.000 claims description 4
- 238000007911 parenteral administration Methods 0.000 claims description 4
- 206010067572 Oestrogenic effect Diseases 0.000 claims 4
- 239000000203 mixture Substances 0.000 description 56
- 229920002261 Corn starch Polymers 0.000 description 24
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 24
- 235000019759 Maize starch Nutrition 0.000 description 24
- 239000008101 lactose Substances 0.000 description 24
- 239000000454 talc Substances 0.000 description 24
- 235000012222 talc Nutrition 0.000 description 24
- 229910052623 talc Inorganic materials 0.000 description 24
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 22
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 22
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 22
- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 description 16
- 229930182833 estradiol Natural products 0.000 description 15
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 12
- 229940070710 valerate Drugs 0.000 description 7
- 235000019359 magnesium stearate Nutrition 0.000 description 6
- 150000002148 esters Chemical class 0.000 description 5
- 230000000694 effects Effects 0.000 description 4
- 239000000902 placebo Substances 0.000 description 4
- 210000005000 reproductive tract Anatomy 0.000 description 4
- WVDDGKGOMKODPV-UHFFFAOYSA-N Benzyl alcohol Chemical compound OCC1=CC=CC=C1 WVDDGKGOMKODPV-UHFFFAOYSA-N 0.000 description 3
- -1 diol valerate Chemical class 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 2
- RJKFOVLPORLFTN-LEKSSAKUSA-N Progesterone Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 RJKFOVLPORLFTN-LEKSSAKUSA-N 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- 150000007513 acids Chemical class 0.000 description 2
- 239000013543 active substance Substances 0.000 description 2
- SESFRYSPDFLNCH-UHFFFAOYSA-N benzyl benzoate Chemical compound C=1C=CC=CC=1C(=O)OCC1=CC=CC=C1 SESFRYSPDFLNCH-UHFFFAOYSA-N 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 239000000470 constituent Substances 0.000 description 2
- 210000004696 endometrium Anatomy 0.000 description 2
- 230000032050 esterification Effects 0.000 description 2
- 238000005886 esterification reaction Methods 0.000 description 2
- VBRVDDFOBZNCPF-BRSFZVHSSA-N estriol succinate Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H]([C@H](OC(=O)CCC(O)=O)C4)OC(=O)CCC(O)=O)[C@@H]4[C@@H]3CCC2=C1 VBRVDDFOBZNCPF-BRSFZVHSSA-N 0.000 description 2
- 238000006266 etherification reaction Methods 0.000 description 2
- 150000002170 ethers Chemical class 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 229940053934 norethindrone Drugs 0.000 description 2
- VIKNJXKGJWUCNN-XGXHKTLJSA-N norethisterone Chemical compound O=C1CC[C@@H]2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 VIKNJXKGJWUCNN-XGXHKTLJSA-N 0.000 description 2
- 229940068196 placebo Drugs 0.000 description 2
- 230000035755 proliferation Effects 0.000 description 2
- 125000001424 substituent group Chemical group 0.000 description 2
- 210000004291 uterus Anatomy 0.000 description 2
- DBPWSSGDRRHUNT-CEGNMAFCSA-N 17α-hydroxyprogesterone Chemical class C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)C)(O)[C@@]1(C)CC2 DBPWSSGDRRHUNT-CEGNMAFCSA-N 0.000 description 1
- HUHXLHLWASNVDB-UHFFFAOYSA-N 2-(oxan-2-yloxy)oxane Chemical class O1CCCCC1OC1OCCCC1 HUHXLHLWASNVDB-UHFFFAOYSA-N 0.000 description 1
- UYIFTLBWAOGQBI-BZDYCCQFSA-N Benzhormovarine Chemical compound C([C@@H]1[C@@H](C2=CC=3)CC[C@]4([C@H]1CC[C@@H]4O)C)CC2=CC=3OC(=O)C1=CC=CC=C1 UYIFTLBWAOGQBI-BZDYCCQFSA-N 0.000 description 1
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical group FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 description 1
- 241001077885 Gesta Species 0.000 description 1
- 208000032843 Hemorrhage Diseases 0.000 description 1
- 206010060800 Hot flush Diseases 0.000 description 1
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 description 1
- 206010046788 Uterine haemorrhage Diseases 0.000 description 1
- 125000003668 acetyloxy group Chemical group [H]C([H])([H])C(=O)O[*] 0.000 description 1
- 230000002730 additional effect Effects 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 150000005215 alkyl ethers Chemical class 0.000 description 1
- 230000003042 antagnostic effect Effects 0.000 description 1
- 235000019445 benzyl alcohol Nutrition 0.000 description 1
- 229960002903 benzyl benzoate Drugs 0.000 description 1
- 230000000740 bleeding effect Effects 0.000 description 1
- 125000001246 bromo group Chemical group Br* 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 125000004432 carbon atom Chemical group C* 0.000 description 1
- 239000004359 castor oil Substances 0.000 description 1
- 235000019438 castor oil Nutrition 0.000 description 1
- 210000003679 cervix uteri Anatomy 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 125000004122 cyclic group Chemical group 0.000 description 1
- 229960003843 cyproterone Drugs 0.000 description 1
- DUSHUSLJJMDGTE-ZJPMUUANSA-N cyproterone Chemical compound C1=C(Cl)C2=CC(=O)[C@@H]3C[C@@H]3[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)C)(O)[C@@]1(C)CC2 DUSHUSLJJMDGTE-ZJPMUUANSA-N 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 208000002173 dizziness Diseases 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 230000002526 effect on cardiovascular system Effects 0.000 description 1
- 229960000445 ethisterone Drugs 0.000 description 1
- 230000002349 favourable effect Effects 0.000 description 1
- 229910052731 fluorine Inorganic materials 0.000 description 1
- 239000011737 fluorine Substances 0.000 description 1
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 description 1
- 125000005843 halogen group Chemical group 0.000 description 1
- 206010022437 insomnia Diseases 0.000 description 1
- 230000003340 mental effect Effects 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 description 1
- 229940079411 norgestrel 0.5 mg Drugs 0.000 description 1
- 238000012856 packing Methods 0.000 description 1
- HUPQYPMULVBQDL-UHFFFAOYSA-N pentanoic acid Chemical compound CCCCC(O)=O.CCCCC(O)=O HUPQYPMULVBQDL-UHFFFAOYSA-N 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 239000000186 progesterone Substances 0.000 description 1
- 229960003387 progesterone Drugs 0.000 description 1
- ULWHHBHJGPPBCO-UHFFFAOYSA-N propane-1,1-diol Chemical class CCC(O)O ULWHHBHJGPPBCO-UHFFFAOYSA-N 0.000 description 1
- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical compound O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 description 1
- 230000033764 rhythmic process Effects 0.000 description 1
- 239000008159 sesame oil Substances 0.000 description 1
- 235000011803 sesame oil Nutrition 0.000 description 1
- 150000003431 steroids Chemical class 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 230000035900 sweating Effects 0.000 description 1
- 230000002195 synergetic effect Effects 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 230000009466 transformation Effects 0.000 description 1
- 210000001215 vagina Anatomy 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 210000003905 vulva Anatomy 0.000 description 1
Classifications
-
- 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
- A61K31/56—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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19762645307 DE2645307A1 (de) | 1976-10-05 | 1976-10-05 | Neue mittel und neue methoden zur behandlung klimakterischer ausfallerscheinungen |
| DEP2645307.6 | 1976-10-05 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA1090256A true CA1090256A (en) | 1980-11-25 |
Family
ID=5989934
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA288,196A Expired CA1090256A (en) | 1976-10-05 | 1977-10-05 | Medicament pack and agent for the treatment of climacteric deficiency symptoms |
Country Status (9)
| Country | Link |
|---|---|
| AU (1) | AU512918B2 (enrdf_load_stackoverflow) |
| BE (1) | BE859410A (enrdf_load_stackoverflow) |
| CA (1) | CA1090256A (enrdf_load_stackoverflow) |
| DE (1) | DE2645307A1 (enrdf_load_stackoverflow) |
| DK (1) | DK438077A (enrdf_load_stackoverflow) |
| GB (1) | GB1578240A (enrdf_load_stackoverflow) |
| NL (1) | NL7709742A (enrdf_load_stackoverflow) |
| SE (1) | SE7711102L (enrdf_load_stackoverflow) |
| ZA (1) | ZA775980B (enrdf_load_stackoverflow) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8153616B2 (en) | 2005-10-17 | 2012-04-10 | Bayer Pharma Aktiengesellschaft | Combination preparation for oral contraception and oral therapy of dysfunctional uterine bleeding containing estradiol valerate and dienogest and method of using same |
| US8349820B2 (en) | 2006-10-20 | 2013-01-08 | Bayer Pharma Aktiengesellschaft | Use of estradiol valerate or 17β-estradiol in combination with dienogest for oral therapy to maintain and/or increase feminine libido |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3029726A1 (de) * | 1980-08-06 | 1982-02-25 | Werner Dr.med. 4400 Münster Steinschulte | Postkoitale kontrazeptiva mit norgestrel oder levonorgestrel |
| US4390531A (en) * | 1981-08-10 | 1983-06-28 | Syntex Pharmaceuticals International Ltd. | Method of contraception using peak progestogen dosage |
| US4826831A (en) * | 1983-08-05 | 1989-05-02 | Pre Jay Holdings Limited | Method of hormonal treatment for menopausal or post-menopausal disorders involving continuous administration of progestogens and estrogens |
| DE3864210D1 (de) * | 1987-07-06 | 1991-09-19 | Akzo Nv | Pharmazeutische dosierungseinheit zur vorbeugung bzw. behandlung von klimakterischen beschwerden. |
| US5276022A (en) * | 1987-09-24 | 1994-01-04 | Jencap Research Ltd. | Hormone preparation and method |
| EP0309263B1 (en) * | 1987-09-24 | 1994-03-09 | Jencap Research Limited | Hormone composition and use |
| DE4019670A1 (de) * | 1990-06-22 | 1992-01-09 | Erhard Dr Med Roemer | Arzneimittel zur behandlung der wechseljahre der frau |
| DE4104385C1 (enrdf_load_stackoverflow) * | 1991-02-09 | 1992-08-13 | Marika Dr.Med. 6509 Framersheim De Ehrlich | |
| DE4308406C1 (de) * | 1993-03-12 | 1994-06-16 | Jenapharm Gmbh | Kombinationspräparat zur Kontrazeption |
| DE4313926A1 (de) * | 1993-04-28 | 1994-11-03 | Jenapharm Gmbh | Pharmazeutisches Mehrphasenpräparat zur hormonalen Kontrazeption |
| DE4429374C1 (de) | 1994-08-12 | 1996-02-01 | Jenapharm Gmbh | Pharmazeutische Präparate zur Kontrazeption/Hormonsubstitution mit biogener Estrogenkomponente |
| DE102004019743B4 (de) | 2004-04-20 | 2008-11-27 | Bayer Schering Pharma Aktiengesellschaft | Mehrphasenpräparat zur Kontrazeption auf der Basis eines natürlichen Estrogens |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1175468A (en) * | 1967-10-19 | 1969-12-23 | Merck Ag E | Pharmaceutical Compositions |
| US3639600A (en) * | 1969-08-28 | 1972-02-01 | Upjohn Co | Process of establishing cyclicity in a human female |
| DE2529523C2 (de) * | 1975-06-30 | 1987-04-30 | Schering AG, 1000 Berlin und 4709 Bergkamen | Mittel zur Behandlung klimakterischer Ausfallerscheinungen |
-
1976
- 1976-10-05 DE DE19762645307 patent/DE2645307A1/de active Granted
-
1977
- 1977-09-05 NL NL7709742A patent/NL7709742A/xx not_active Application Discontinuation
- 1977-10-03 GB GB40925/77A patent/GB1578240A/en not_active Expired
- 1977-10-04 SE SE7711102A patent/SE7711102L/ not_active Application Discontinuation
- 1977-10-04 DK DK438077A patent/DK438077A/da not_active Application Discontinuation
- 1977-10-05 CA CA288,196A patent/CA1090256A/en not_active Expired
- 1977-10-05 AU AU29364/77A patent/AU512918B2/en not_active Expired
- 1977-10-05 BE BE181485A patent/BE859410A/xx not_active IP Right Cessation
- 1977-10-05 ZA ZA00775980A patent/ZA775980B/xx unknown
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8153616B2 (en) | 2005-10-17 | 2012-04-10 | Bayer Pharma Aktiengesellschaft | Combination preparation for oral contraception and oral therapy of dysfunctional uterine bleeding containing estradiol valerate and dienogest and method of using same |
| US8349820B2 (en) | 2006-10-20 | 2013-01-08 | Bayer Pharma Aktiengesellschaft | Use of estradiol valerate or 17β-estradiol in combination with dienogest for oral therapy to maintain and/or increase feminine libido |
Also Published As
| Publication number | Publication date |
|---|---|
| DK438077A (da) | 1978-04-06 |
| NL7709742A (nl) | 1978-04-07 |
| GB1578240A (en) | 1980-11-05 |
| AU512918B2 (en) | 1980-11-06 |
| SE7711102L (sv) | 1978-04-06 |
| AU2936477A (en) | 1979-04-12 |
| BE859410A (fr) | 1978-04-05 |
| DE2645307C2 (enrdf_load_stackoverflow) | 1988-10-13 |
| ZA775980B (en) | 1978-05-30 |
| DE2645307A1 (de) | 1978-04-06 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MKEX | Expiry |