FI119414B - Emättimensisäisesti käytettävät lääkkeen vapauttamislaitteet 17beta-estradioliprekursoreiden antamiseksi - Google Patents
Emättimensisäisesti käytettävät lääkkeen vapauttamislaitteet 17beta-estradioliprekursoreiden antamiseksi Download PDFInfo
- Publication number
- FI119414B FI119414B FI972579A FI972579A FI119414B FI 119414 B FI119414 B FI 119414B FI 972579 A FI972579 A FI 972579A FI 972579 A FI972579 A FI 972579A FI 119414 B FI119414 B FI 119414B
- Authority
- FI
- Finland
- Prior art keywords
- estradiol
- precursor
- group
- blocking group
- drug delivery
- Prior art date
Links
- 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 title claims description 230
- 239000002243 precursor Substances 0.000 title claims description 83
- 238000012377 drug delivery Methods 0.000 title claims description 40
- 229960005309 estradiol Drugs 0.000 claims description 147
- 239000011159 matrix material Substances 0.000 claims description 37
- 229920000642 polymer Polymers 0.000 claims description 37
- 230000000903 blocking effect Effects 0.000 claims description 31
- 229930182833 estradiol Natural products 0.000 claims description 29
- -1 isobutyryl Chemical group 0.000 claims description 24
- 238000002657 hormone replacement therapy Methods 0.000 claims description 22
- 208000024891 symptom Diseases 0.000 claims description 21
- 239000000203 mixture Substances 0.000 claims description 20
- 238000004519 manufacturing process Methods 0.000 claims description 18
- 125000002252 acyl group Chemical group 0.000 claims description 17
- 238000001727 in vivo Methods 0.000 claims description 16
- FHXBMXJMKMWVRG-SLHNCBLASA-N estradiol acetate Chemical group C1C[C@]2(C)[C@@H](O)CC[C@H]2[C@@H]2CCC3=CC(OC(=O)C)=CC=C3[C@H]21 FHXBMXJMKMWVRG-SLHNCBLASA-N 0.000 claims description 15
- 238000000034 method Methods 0.000 claims description 15
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 13
- 241000124008 Mammalia Species 0.000 claims description 12
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 11
- 229920001296 polysiloxane Polymers 0.000 claims description 9
- 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 7
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims description 7
- 239000003054 catalyst Substances 0.000 claims description 7
- 239000012153 distilled water Substances 0.000 claims description 7
- 229960004400 levonorgestrel Drugs 0.000 claims description 7
- QAHOQNJVHDHYRN-SLHNCBLASA-N beta-Estradiol 17-acetate Chemical group C1CC2=CC(O)=CC=C2[C@@H]2[C@@H]1[C@@H]1CC[C@H](OC(=O)C)[C@@]1(C)CC2 QAHOQNJVHDHYRN-SLHNCBLASA-N 0.000 claims description 6
- 239000007788 liquid Substances 0.000 claims description 6
- 239000000126 substance Substances 0.000 claims description 6
- 231100000252 nontoxic Toxicity 0.000 claims description 5
- 230000003000 nontoxic effect Effects 0.000 claims description 5
- 238000002360 preparation method Methods 0.000 claims description 5
- 125000001931 aliphatic group Chemical group 0.000 claims description 4
- 150000002009 diols Chemical class 0.000 claims description 4
- OFOBLEOULBTSOW-UHFFFAOYSA-N Malonic acid Chemical compound OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 claims description 3
- 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 3
- 239000000583 progesterone congener Substances 0.000 claims description 3
- 125000001501 propionyl group Chemical group O=C([*])C([H])([H])C([H])([H])[H] 0.000 claims description 3
- 125000004080 3-carboxypropanoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C(O[H])=O 0.000 claims description 2
- 125000003647 acryloyl group Chemical group O=C([*])C([H])=C([H])[H] 0.000 claims description 2
- 125000004063 butyryl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 2
- 239000003795 chemical substances by application Substances 0.000 claims description 2
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims description 2
- 125000004031 fumaroyl group Chemical group C(\C=C\C(=O)*)(=O)* 0.000 claims description 2
- 125000003099 maleoyl group Chemical group C(\C=C/C(=O)*)(=O)* 0.000 claims description 2
- 125000003431 oxalo group Chemical group 0.000 claims description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical class [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- 239000003431 cross linking reagent Substances 0.000 claims 2
- VNWKTOKETHGBQD-UHFFFAOYSA-N methane Chemical compound C VNWKTOKETHGBQD-UHFFFAOYSA-N 0.000 claims 2
- 206010033264 Ovarian hyperfunction Diseases 0.000 claims 1
- 125000001721 carboxyacetyl group Chemical group 0.000 claims 1
- 125000003897 citraconoyl group Chemical group C(\C(\C)=C/C(=O)*)(=O)* 0.000 claims 1
- 201000006564 estrogen excess Diseases 0.000 claims 1
- 230000036571 hydration Effects 0.000 claims 1
- 238000006703 hydration reaction Methods 0.000 claims 1
- 230000001939 inductive effect Effects 0.000 claims 1
- 239000000262 estrogen Substances 0.000 description 43
- 229940011871 estrogen Drugs 0.000 description 43
- 229940079593 drug Drugs 0.000 description 37
- 239000003814 drug Substances 0.000 description 37
- 238000000338 in vitro Methods 0.000 description 24
- ATJFFYVFTNAWJD-UHFFFAOYSA-N Tin Chemical group [Sn] ATJFFYVFTNAWJD-UHFFFAOYSA-N 0.000 description 16
- 238000000576 coating method Methods 0.000 description 16
- 239000011248 coating agent Substances 0.000 description 15
- 229920001971 elastomer Polymers 0.000 description 12
- 239000000806 elastomer Substances 0.000 description 12
- 239000012738 dissolution medium Substances 0.000 description 10
- 229940088597 hormone Drugs 0.000 description 9
- 239000005556 hormone Substances 0.000 description 9
- 230000036470 plasma concentration Effects 0.000 description 9
- 230000028327 secretion Effects 0.000 description 9
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 8
- 235000013870 dimethyl polysiloxane Nutrition 0.000 description 8
- 239000004205 dimethyl polysiloxane Substances 0.000 description 8
- 230000002209 hydrophobic effect Effects 0.000 description 8
- 229920000435 poly(dimethylsiloxane) Polymers 0.000 description 8
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 7
- 229960000686 benzalkonium chloride Drugs 0.000 description 7
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 description 7
- 150000003431 steroids Chemical class 0.000 description 7
- 238000009792 diffusion process Methods 0.000 description 6
- 238000003780 insertion Methods 0.000 description 6
- 230000037431 insertion Effects 0.000 description 6
- 230000007774 longterm Effects 0.000 description 6
- 210000002966 serum Anatomy 0.000 description 6
- 239000011780 sodium chloride Substances 0.000 description 6
- 238000004458 analytical method Methods 0.000 description 5
- 230000003247 decreasing effect Effects 0.000 description 5
- 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 4
- 210000004369 blood Anatomy 0.000 description 4
- 239000008280 blood Substances 0.000 description 4
- 230000007062 hydrolysis Effects 0.000 description 4
- 238000006460 hydrolysis reaction Methods 0.000 description 4
- 238000001990 intravenous administration Methods 0.000 description 4
- 239000002609 medium Substances 0.000 description 4
- 230000009245 menopause Effects 0.000 description 4
- 238000002156 mixing Methods 0.000 description 4
- 230000016087 ovulation Effects 0.000 description 4
- 230000001225 therapeutic effect Effects 0.000 description 4
- 239000004971 Cross linker Substances 0.000 description 3
- 206010030247 Oestrogen deficiency Diseases 0.000 description 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- 238000010521 absorption reaction Methods 0.000 description 3
- 230000004913 activation Effects 0.000 description 3
- 239000007864 aqueous solution Substances 0.000 description 3
- 238000003556 assay Methods 0.000 description 3
- 150000001875 compounds Chemical class 0.000 description 3
- 230000007423 decrease Effects 0.000 description 3
- 230000002950 deficient Effects 0.000 description 3
- 238000013461 design Methods 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 208000035475 disorder Diseases 0.000 description 3
- 210000000981 epithelium Anatomy 0.000 description 3
- 239000012530 fluid Substances 0.000 description 3
- 238000007429 general method Methods 0.000 description 3
- 238000004128 high performance liquid chromatography Methods 0.000 description 3
- 238000011534 incubation Methods 0.000 description 3
- 238000002347 injection Methods 0.000 description 3
- 239000007924 injection Substances 0.000 description 3
- 210000001672 ovary Anatomy 0.000 description 3
- 239000008188 pellet Substances 0.000 description 3
- 239000012086 standard solution Substances 0.000 description 3
- 238000007920 subcutaneous administration Methods 0.000 description 3
- 239000006213 vaginal ring Substances 0.000 description 3
- 229940070710 valerate Drugs 0.000 description 3
- DNXHEGUUPJUMQT-UHFFFAOYSA-N (+)-estrone Natural products OC1=CC=C2C3CCC(C)(C(CC4)=O)C4C3CCC2=C1 DNXHEGUUPJUMQT-UHFFFAOYSA-N 0.000 description 2
- 208000000044 Amnesia Diseases 0.000 description 2
- 206010003694 Atrophy Diseases 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 2
- 208000034423 Delivery Diseases 0.000 description 2
- 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 2
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 description 2
- 206010027304 Menopausal symptoms Diseases 0.000 description 2
- 208000027418 Wounds and injury Diseases 0.000 description 2
- 230000002378 acidificating effect Effects 0.000 description 2
- 239000013543 active substance Substances 0.000 description 2
- 230000037444 atrophy Effects 0.000 description 2
- TZCXTZWJZNENPQ-UHFFFAOYSA-L barium sulfate Chemical compound [Ba+2].[O-]S([O-])(=O)=O TZCXTZWJZNENPQ-UHFFFAOYSA-L 0.000 description 2
- 238000006243 chemical reaction Methods 0.000 description 2
- 230000006378 damage Effects 0.000 description 2
- 230000001419 dependent effect Effects 0.000 description 2
- 150000001991 dicarboxylic acids Chemical class 0.000 description 2
- 238000004090 dissolution Methods 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 150000002148 esters Chemical class 0.000 description 2
- 229960003399 estrone Drugs 0.000 description 2
- 238000002474 experimental method Methods 0.000 description 2
- 230000035558 fertility Effects 0.000 description 2
- 210000004907 gland Anatomy 0.000 description 2
- 239000000745 gonadal hormone Substances 0.000 description 2
- 208000014674 injury Diseases 0.000 description 2
- 210000004185 liver Anatomy 0.000 description 2
- PSGAAPLEWMOORI-PEINSRQWSA-N medroxyprogesterone acetate Chemical compound C([C@@]12C)CC(=O)C=C1[C@@H](C)C[C@@H]1[C@@H]2CC[C@]2(C)[C@@](OC(C)=O)(C(C)=O)CC[C@H]21 PSGAAPLEWMOORI-PEINSRQWSA-N 0.000 description 2
- 239000000693 micelle Substances 0.000 description 2
- 150000002763 monocarboxylic acids Chemical class 0.000 description 2
- 230000000955 neuroendocrine Effects 0.000 description 2
- 125000005474 octanoate group Chemical group 0.000 description 2
- 229940126701 oral medication Drugs 0.000 description 2
- 108090000623 proteins and genes Proteins 0.000 description 2
- PUZPDOWCWNUUKD-UHFFFAOYSA-M sodium fluoride Chemical compound [F-].[Na+] PUZPDOWCWNUUKD-UHFFFAOYSA-M 0.000 description 2
- 238000005063 solubilization Methods 0.000 description 2
- 230000007928 solubilization Effects 0.000 description 2
- 238000001356 surgical procedure Methods 0.000 description 2
- 230000001839 systemic circulation Effects 0.000 description 2
- 238000002560 therapeutic procedure Methods 0.000 description 2
- 229940044953 vaginal ring Drugs 0.000 description 2
- NQPDZGIKBAWPEJ-UHFFFAOYSA-N valeric acid Chemical compound CCCCC(O)=O NQPDZGIKBAWPEJ-UHFFFAOYSA-N 0.000 description 2
- VOXZDWNPVJITMN-UHFFFAOYSA-N 13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol Chemical compound OC1=CC=C2C3CCC(C)(C(CC4)O)C4C3CCC2=C1 VOXZDWNPVJITMN-UHFFFAOYSA-N 0.000 description 1
- 208000019901 Anxiety disease Diseases 0.000 description 1
- 101100515513 Arabidopsis thaliana XI-E gene Proteins 0.000 description 1
- 208000006820 Arthralgia Diseases 0.000 description 1
- 108010051152 Carboxylesterase Proteins 0.000 description 1
- 102000013392 Carboxylesterase Human genes 0.000 description 1
- 241000723368 Conium Species 0.000 description 1
- 206010013786 Dry skin Diseases 0.000 description 1
- 238000002965 ELISA Methods 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
- 108010093488 His-His-His-His-His-His Proteins 0.000 description 1
- 208000033830 Hot Flashes Diseases 0.000 description 1
- 206010060800 Hot flush Diseases 0.000 description 1
- 208000004044 Hypesthesia Diseases 0.000 description 1
- 206010022998 Irritability Diseases 0.000 description 1
- 239000005909 Kieselgur Substances 0.000 description 1
- 206010024870 Loss of libido Diseases 0.000 description 1
- 208000026139 Memory disease Diseases 0.000 description 1
- 206010027940 Mood altered Diseases 0.000 description 1
- 206010048886 Onychoclasis Diseases 0.000 description 1
- 208000002193 Pain Diseases 0.000 description 1
- 102000003982 Parathyroid hormone Human genes 0.000 description 1
- 108090000445 Parathyroid hormone Proteins 0.000 description 1
- 239000004698 Polyethylene Substances 0.000 description 1
- XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 description 1
- XBDQKXXYIPTUBI-UHFFFAOYSA-N Propionic acid Chemical class CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 description 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 description 1
- 206010046477 Urethral syndrome Diseases 0.000 description 1
- 240000008042 Zea mays Species 0.000 description 1
- 235000005824 Zea mays ssp. parviglumis Nutrition 0.000 description 1
- 235000002017 Zea mays subsp mays Nutrition 0.000 description 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-N acetic acid Substances CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 230000001668 ameliorated effect Effects 0.000 description 1
- 230000036506 anxiety Effects 0.000 description 1
- 229920000249 biocompatible polymer Polymers 0.000 description 1
- 230000033228 biological regulation Effects 0.000 description 1
- 230000017531 blood circulation Effects 0.000 description 1
- 230000003139 buffering effect Effects 0.000 description 1
- 150000001768 cations Chemical class 0.000 description 1
- 238000005119 centrifugation Methods 0.000 description 1
- 239000007795 chemical reaction product Substances 0.000 description 1
- VUHJZBBCZGVNDZ-TTYLFXKOSA-N chlormadinone Chemical compound C1=C(Cl)C2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)C)(O)[C@@]1(C)CC2 VUHJZBBCZGVNDZ-TTYLFXKOSA-N 0.000 description 1
- 230000004087 circulation Effects 0.000 description 1
- 239000002131 composite material Substances 0.000 description 1
- 239000000470 constituent Substances 0.000 description 1
- 239000003433 contraceptive agent Substances 0.000 description 1
- 230000002254 contraceptive effect Effects 0.000 description 1
- 238000013270 controlled release Methods 0.000 description 1
- 235000005822 corn Nutrition 0.000 description 1
- 239000000431 corpus luteum hormone Substances 0.000 description 1
- 238000005260 corrosion Methods 0.000 description 1
- 238000004132 cross linking Methods 0.000 description 1
- 230000009089 cytolysis Effects 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 238000007922 dissolution test Methods 0.000 description 1
- 238000009826 distribution Methods 0.000 description 1
- 239000003640 drug residue Substances 0.000 description 1
- 230000037336 dry skin Effects 0.000 description 1
- 230000002124 endocrine Effects 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 230000007613 environmental effect Effects 0.000 description 1
- 229960001359 estradiol 3-benzoate Drugs 0.000 description 1
- 238000009164 estrogen replacement therapy Methods 0.000 description 1
- 238000001125 extrusion Methods 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 238000011049 filling Methods 0.000 description 1
- 230000003325 follicular Effects 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 210000004392 genitalia Anatomy 0.000 description 1
- 229960005352 gestodene Drugs 0.000 description 1
- SIGSPDASOTUPFS-XUDSTZEESA-N gestodene Chemical compound O=C1CC[C@@H]2[C@H]3CC[C@](CC)([C@](C=C4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 SIGSPDASOTUPFS-XUDSTZEESA-N 0.000 description 1
- 230000035876 healing Effects 0.000 description 1
- 230000001951 hemoperfusion Effects 0.000 description 1
- 230000010224 hepatic metabolism Effects 0.000 description 1
- 230000003301 hydrolyzing effect Effects 0.000 description 1
- 230000002706 hydrostatic effect Effects 0.000 description 1
- 208000034783 hypoesthesia Diseases 0.000 description 1
- 239000007943 implant Substances 0.000 description 1
- 238000002513 implantation Methods 0.000 description 1
- 238000010348 incorporation Methods 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 230000000977 initiatory effect Effects 0.000 description 1
- 238000001746 injection moulding Methods 0.000 description 1
- 206010022437 insomnia Diseases 0.000 description 1
- 230000003834 intracellular effect Effects 0.000 description 1
- 229910052742 iron Inorganic materials 0.000 description 1
- 230000002045 lasting effect Effects 0.000 description 1
- 238000002386 leaching Methods 0.000 description 1
- 150000002632 lipids Chemical class 0.000 description 1
- 239000006210 lotion Substances 0.000 description 1
- 229960004616 medroxyprogesterone Drugs 0.000 description 1
- 229960002985 medroxyprogesterone acetate Drugs 0.000 description 1
- 229960001786 megestrol Drugs 0.000 description 1
- RQZAXGRLVPAYTJ-GQFGMJRRSA-N megestrol acetate Chemical compound C1=C(C)C2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(C)=O)(OC(=O)C)[C@@]1(C)CC2 RQZAXGRLVPAYTJ-GQFGMJRRSA-N 0.000 description 1
- 230000006984 memory degeneration Effects 0.000 description 1
- 208000023060 memory loss Diseases 0.000 description 1
- 230000003278 mimic effect Effects 0.000 description 1
- 230000007510 mood change Effects 0.000 description 1
- 206010029410 night sweats Diseases 0.000 description 1
- 230000036565 night sweats Effects 0.000 description 1
- 229960000417 norgestimate Drugs 0.000 description 1
- KIQQMECNKUGGKA-NMYWJIRASA-N norgestimate Chemical compound O/N=C/1CC[C@@H]2[C@H]3CC[C@](CC)([C@](CC4)(OC(C)=O)C#C)[C@@H]4[C@@H]3CCC2=C\1 KIQQMECNKUGGKA-NMYWJIRASA-N 0.000 description 1
- 231100000862 numbness Toxicity 0.000 description 1
- 230000002611 ovarian Effects 0.000 description 1
- 230000011599 ovarian follicle development Effects 0.000 description 1
- 230000027758 ovulation cycle Effects 0.000 description 1
- 238000012856 packing Methods 0.000 description 1
- 239000000199 parathyroid hormone Substances 0.000 description 1
- 229960001319 parathyroid hormone Drugs 0.000 description 1
- 238000005192 partition Methods 0.000 description 1
- 229920000573 polyethylene Polymers 0.000 description 1
- 229920002635 polyurethane Polymers 0.000 description 1
- 239000004814 polyurethane Substances 0.000 description 1
- 231100000683 possible toxicity Toxicity 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 230000035935 pregnancy Effects 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 229960003387 progesterone Drugs 0.000 description 1
- 239000000186 progesterone Substances 0.000 description 1
- 238000009256 replacement therapy Methods 0.000 description 1
- 230000002441 reversible effect Effects 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 229920000260 silastic Polymers 0.000 description 1
- 239000011775 sodium fluoride Substances 0.000 description 1
- 235000013024 sodium fluoride Nutrition 0.000 description 1
- 239000008279 sol Substances 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- ZQZCOBSUOFHDEE-UHFFFAOYSA-N tetrapropyl silicate Chemical compound CCCO[Si](OCCC)(OCCC)OCCC ZQZCOBSUOFHDEE-UHFFFAOYSA-N 0.000 description 1
- 231100000167 toxic agent Toxicity 0.000 description 1
- 239000003440 toxic substance Substances 0.000 description 1
- 238000013271 transdermal drug delivery Methods 0.000 description 1
- 238000000825 ultraviolet detection Methods 0.000 description 1
- 238000011144 upstream manufacturing Methods 0.000 description 1
- 210000001215 vagina Anatomy 0.000 description 1
- 230000009677 vaginal delivery Effects 0.000 description 1
- 239000000003 vaginal tablet Substances 0.000 description 1
- 230000002087 whitening 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0034—Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
- A61K9/0036—Devices retained in the vagina or cervix for a prolonged period, e.g. intravaginal rings, medicated tampons, medicated diaphragms
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/18—Feminine contraceptives
Landscapes
- Health & Medical Sciences (AREA)
- Reproductive Health (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Gynecology & Obstetrics (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IES940976 | 1994-12-19 | ||
| IES940976 | 1994-12-19 | ||
| IES950247 | 1995-04-05 | ||
| IES950247 | 1995-04-05 | ||
| PCT/IE1995/000063 WO1996019196A1 (en) | 1994-12-19 | 1995-12-19 | INTRAVAGINAL DRUG DELIVERY DEVICES FOR THE ADMINISTRATION OF 17β-OESTRADIOL PRECURSORS |
| IE9500063 | 1995-12-19 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| FI972579L FI972579L (fi) | 1997-06-17 |
| FI972579A0 FI972579A0 (fi) | 1997-06-17 |
| FI119414B true FI119414B (fi) | 2008-11-14 |
Family
ID=26319777
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| FI972579A FI119414B (fi) | 1994-12-19 | 1997-06-17 | Emättimensisäisesti käytettävät lääkkeen vapauttamislaitteet 17beta-estradioliprekursoreiden antamiseksi |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US5855906A (de) |
| EP (1) | EP0799025B1 (de) |
| JP (1) | JPH10510825A (de) |
| CN (1) | CN1138526C (de) |
| AR (1) | AR002010A1 (de) |
| AT (1) | ATE178204T1 (de) |
| AU (1) | AU692659B2 (de) |
| CA (1) | CA2207622C (de) |
| DE (1) | DE69508791T2 (de) |
| DK (1) | DK0799025T3 (de) |
| ES (1) | ES2133841T3 (de) |
| FI (1) | FI119414B (de) |
| GR (1) | GR3030614T3 (de) |
| IL (1) | IL116433A (de) |
| NO (1) | NO316707B1 (de) |
| NZ (1) | NZ298490A (de) |
| PE (1) | PE62796A1 (de) |
| TR (1) | TR199501599A2 (de) |
| WO (1) | WO1996019196A1 (de) |
Families Citing this family (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6407082B1 (en) * | 1996-09-13 | 2002-06-18 | New Life Pharmaceuticals Inc. | Prevention of ovarian cancer by administration of a vitamin D compound |
| US6511970B1 (en) | 1996-09-13 | 2003-01-28 | New Life Pharmaceuticals Inc. | Prevention of ovarian cancer by administration of products that induce transforming growth factor-beta and/or apoptosis in the ovarian epithelium |
| US6765002B2 (en) | 2000-03-21 | 2004-07-20 | Gustavo Rodriguez | Prevention of ovarian cancer by administration of products that induce transforming growth factor-β and/or apoptosis in the ovarian epithelium |
| US6034074A (en) | 1996-09-13 | 2000-03-07 | New Life Pharmaceuticals Inc. | Prevention of ovarian cancer by administration of a Vitamin D compound |
| US6028064A (en) | 1996-09-13 | 2000-02-22 | New Life Pharmaceuticals Inc. | Prevention of ovarian cancer by administration of progestin products |
| CN1184957C (zh) | 1997-05-07 | 2005-01-19 | 盖伦(化学制品)有限公司 | 用于给药睾酮和睾酮前体的阴道内给药装置 |
| US6039968A (en) * | 1997-06-24 | 2000-03-21 | Hoechst Marion Roussel | Intravaginal drug delivery device |
| US20010044431A1 (en) * | 2000-03-21 | 2001-11-22 | Rodriguez Gustavo C. | Prevention of ovarian cancer by administration of products that induce biologic effects in the ovarian epithelium |
| US20040176336A1 (en) * | 2000-03-21 | 2004-09-09 | Rodriguez Gustavo C. | Prevention of ovarian cancer by administration of products that induce biologic effects in the ovarian epithelium |
| US20050113351A1 (en) * | 2000-03-21 | 2005-05-26 | Rodriguez Gustavo C. | Prevention of ovarian cancer by administration of products that induce biologic effects in the ovarian epithelium |
| US6811549B2 (en) | 2001-02-16 | 2004-11-02 | William H. Fleming | Administration of therapeutic or diagnostic agents using interlabial pad |
| US6962908B2 (en) * | 2001-12-21 | 2005-11-08 | Warner Chilcott Company Inc. | Oral pharmaceutical products containing 17 β-estradiol-3-lower alkanoate, method of administering the same and process of preparation |
| AU2003226746A1 (en) * | 2002-03-27 | 2003-10-08 | Galen (Chemicals) Limited | Intravaginal matrix drug delivery devices |
| GB0222522D0 (en) | 2002-09-27 | 2002-11-06 | Controlled Therapeutics Sct | Water-swellable polymers |
| EP1620060B1 (de) * | 2003-04-29 | 2010-03-24 | The General Hospital Corporation | Verfahren und vorrichtungen für die verzögerte freisetzung von mehreren arzneimitteln |
| GB0417401D0 (en) | 2004-08-05 | 2004-09-08 | Controlled Therapeutics Sct | Stabilised prostaglandin composition |
| CA2596933A1 (en) * | 2005-02-03 | 2006-08-10 | Duramed Pharmaceuticals, Inc. | Devices for delivering agents to a vaginal tract |
| EP1853272A1 (de) * | 2005-02-03 | 2007-11-14 | Duramed Pharmaceuticals, Inc. | Zusammensetzungen aus unkonjugierten östrogenen und anwendungsverfahren dafür |
| CA2618349C (en) | 2005-08-11 | 2016-05-31 | Massachusetts Institute Of Technology | Intravesical drug delivery device and method |
| US20070077269A1 (en) * | 2005-10-04 | 2007-04-05 | Woodward John R | Method of birth control and hormone regulation |
| BRPI0617325B8 (pt) | 2005-10-13 | 2021-06-22 | Synthes Gmbh | luva biologicamente compatível |
| GB0613333D0 (en) | 2006-07-05 | 2006-08-16 | Controlled Therapeutics Sct | Hydrophilic polyurethane compositions |
| GB0613638D0 (en) * | 2006-07-08 | 2006-08-16 | Controlled Therapeutics Sct | Polyurethane elastomers |
| JP2009542788A (ja) * | 2006-07-12 | 2009-12-03 | コントロールド・セラピューティクス（スコットランド）・リミテッド | クリンダマイシンの塩酸塩を有する薬剤デリバリーポリマー |
| GB0620685D0 (en) * | 2006-10-18 | 2006-11-29 | Controlled Therapeutics Sct | Bioresorbable polymers |
| US8962010B2 (en) * | 2007-06-26 | 2015-02-24 | Warner Chilcott Company, Llc | Intravaginal drug delivery devices for the delivery of macromolecules and water-soluble drugs |
| EA201070703A1 (ru) * | 2007-12-11 | 2010-12-30 | Массачусетс Инститьют Оф Текнолоджи | Имплантируемое устройство для доставки лекарства и способы лечения мочевого пузыря и других полостей тела или трубчатых органов |
| EA201170297A1 (ru) | 2008-08-09 | 2011-08-30 | Массачусетс Инститьют Оф Текнолоджи | Имплантируемое устройство для доставки лекарственных средств и способ лечения мужской мочеполовой системы и окружающих тканей |
| CN102596097B (zh) | 2009-06-03 | 2015-05-20 | 弗赛特实验室有限责任公司 | 一种眼插入件 |
| DK2445571T3 (da) | 2009-06-26 | 2013-02-25 | Taris Biomedical Inc | Faste lægemiddeltabletter til implanterbare lægemiddelafgivelsesindretninger |
| US9017312B2 (en) | 2009-09-10 | 2015-04-28 | Taris Biomedical Llc | Implantable device for controlled drug delivery |
| US8580294B2 (en) | 2010-10-19 | 2013-11-12 | International Partnership For Microbicides | Platinum-catalyzed intravaginal rings |
| EP2663300B1 (de) | 2011-01-10 | 2023-03-08 | TARIS Biomedical LLC | Lidocain dosierungsschema zur verwendung bei einer anhaltenden behandlung von blasenschmerzen und schmerzhaftem harnabgang |
| BR112013019410A2 (pt) | 2011-02-04 | 2019-09-24 | Taris Biomedical Inc | dispositivo implantável para liberação controlada de fármaco de solubilidade baixa |
| WO2013040426A2 (en) | 2011-09-14 | 2013-03-21 | Forsight Labs, Llc | Ocular insert apparatus and methods |
| TWI590843B (zh) | 2011-12-28 | 2017-07-11 | 信迪思有限公司 | 膜及其製造方法 |
| DK2911623T3 (da) | 2012-10-26 | 2019-10-28 | Forsight Vision5 Inc | Oftalmisk system til langvarig frigivelse af lægemiddel til øjet |
| EP4570239A3 (de) | 2013-03-15 | 2025-08-20 | TARIS Biomedical LLC | Arzneimittelabgabevorrichtungen mit arzneimitteldurchlässiger komponente und verfahren |
| WO2014204708A1 (en) | 2013-06-21 | 2014-12-24 | DePuy Synthes Products, LLC | Films and methods of manufacture |
| SI3035991T1 (sl) | 2013-08-19 | 2021-01-29 | Taris Biomedical Llc | Večdelna naprava za dostavo zdravila |
| CN104546668B (zh) * | 2013-10-23 | 2019-03-05 | 国家卫生计生委科学技术研究所 | 液体硅橡胶为载体的药物缓控释系统的制备及应用 |
| US10137031B2 (en) | 2013-11-14 | 2018-11-27 | International Partnership For Microbicides, Inc. | Combination therapy intravaginal rings |
| DK3125964T3 (da) * | 2014-04-01 | 2024-10-14 | Poly Med Inc | Antikonceptionsmiddel og relateret enhed |
| EP3283004A4 (de) | 2015-04-13 | 2018-12-05 | Forsight Vision5, Inc. | Augeneinsatzzusammensetzung aus einem semikristallinen oder kristallinen pharmazeutischen wirkstoff |
| EP3285850A1 (de) | 2015-04-23 | 2018-02-28 | TARIS Biomedical LLC | Wirkstoffabgabevorrichtungen mit einer wirkstoffdurchlässigen komponente und verfahren |
| CN114573654B (zh) * | 2020-12-01 | 2025-09-12 | 北京奇明达企业管理有限公司 | 17-O-乙酰-17-β雌二醇的自组装的三聚体、其制备、活性和应用 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3545439A (en) * | 1968-01-04 | 1970-12-08 | Upjohn Co | Medicated devices and methods |
| US4291014A (en) * | 1979-01-11 | 1981-09-22 | Key Pharmaceuticals, Inc. | Polymeric diffusion matrix containing estradiol diacetate |
| US4438139A (en) * | 1979-08-14 | 1984-03-20 | Key Pharmaceuticals, Inc. | Polymeric diffusion matrix containing estrogens |
| SE8602666D0 (sv) * | 1986-06-16 | 1986-06-16 | Leo Ab | Intravaginal devices |
-
1995
- 1995-12-18 IL IL11643395A patent/IL116433A/en not_active IP Right Cessation
- 1995-12-19 TR TR95/01599A patent/TR199501599A2/xx unknown
- 1995-12-19 NZ NZ298490A patent/NZ298490A/xx unknown
- 1995-12-19 AU AU43991/96A patent/AU692659B2/en not_active Ceased
- 1995-12-19 WO PCT/IE1995/000063 patent/WO1996019196A1/en not_active Ceased
- 1995-12-19 JP JP8519650A patent/JPH10510825A/ja not_active Ceased
- 1995-12-19 CA CA002207622A patent/CA2207622C/en not_active Expired - Lifetime
- 1995-12-19 PE PE1995287516A patent/PE62796A1/es not_active Application Discontinuation
- 1995-12-19 ES ES95942772T patent/ES2133841T3/es not_active Expired - Lifetime
- 1995-12-19 DE DE69508791T patent/DE69508791T2/de not_active Expired - Lifetime
- 1995-12-19 EP EP95942772A patent/EP0799025B1/de not_active Expired - Lifetime
- 1995-12-19 US US08/849,329 patent/US5855906A/en not_active Expired - Lifetime
- 1995-12-19 AR ARP950100619A patent/AR002010A1/es unknown
- 1995-12-19 CN CNB951968947A patent/CN1138526C/zh not_active Expired - Lifetime
- 1995-12-19 AT AT95942772T patent/ATE178204T1/de not_active IP Right Cessation
- 1995-12-19 DK DK95942772T patent/DK0799025T3/da active
-
1997
- 1997-06-17 FI FI972579A patent/FI119414B/fi not_active IP Right Cessation
- 1997-06-17 NO NO19972798A patent/NO316707B1/no unknown
-
1999
- 1999-06-29 GR GR990401699T patent/GR3030614T3/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| NO316707B1 (no) | 2004-04-13 |
| DE69508791T2 (de) | 1999-12-02 |
| FI972579L (fi) | 1997-06-17 |
| CA2207622A1 (en) | 1996-06-27 |
| NO972798L (no) | 1997-08-19 |
| PE62796A1 (es) | 1996-12-28 |
| US5855906A (en) | 1999-01-05 |
| ES2133841T3 (es) | 1999-09-16 |
| EP0799025A1 (de) | 1997-10-08 |
| TR199501599A2 (tr) | 1996-07-21 |
| IL116433A (en) | 2002-02-10 |
| IL116433A0 (en) | 1996-03-31 |
| DK0799025T3 (da) | 1999-10-18 |
| JPH10510825A (ja) | 1998-10-20 |
| NZ298490A (en) | 1999-11-29 |
| ATE178204T1 (de) | 1999-04-15 |
| NO972798D0 (no) | 1997-06-17 |
| AU4399196A (en) | 1996-07-10 |
| FI972579A0 (fi) | 1997-06-17 |
| DE69508791D1 (de) | 1999-05-06 |
| CA2207622C (en) | 2006-10-17 |
| CN1170353A (zh) | 1998-01-14 |
| EP0799025B1 (de) | 1999-03-31 |
| GR3030614T3 (en) | 1999-10-29 |
| WO1996019196A1 (en) | 1996-06-27 |
| AR002010A1 (es) | 1998-01-07 |
| AU692659B2 (en) | 1998-06-11 |
| CN1138526C (zh) | 2004-02-18 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| FI119414B (fi) | Emättimensisäisesti käytettävät lääkkeen vapauttamislaitteet 17beta-estradioliprekursoreiden antamiseksi | |
| US8865200B2 (en) | Sustained release compositions containing progesterone receptor modulators | |
| JP3806197B2 (ja) | 腟内薬剤放出器具 | |
| EP0710491B1 (de) | Subkutan implantierbare Vorrichtung | |
| US5035891A (en) | Controlled release subcutaneous implant | |
| ES2247054T3 (es) | Combinacion farmaceutica de drospirenona micronizada y un estrogeno para terapia hormonal de sustitucion. | |
| NZ501236A (en) | Intravaginal drug delivery devices for the administration of testosterone and testosterone precursors in a polymer matrix and surrounded by a sheath | |
| US5188835A (en) | Intravaginal devices | |
| Kind et al. | Sustained release hormonal preparations | |
| KR920005824B1 (ko) | 질 내 삽입용 기구 | |
| Victor et al. | Vaginal progesterone for contraception | |
| US6642219B1 (en) | Progestogen-antiprogestogen regimens | |
| IES68528B2 (en) | Intravaginal drug delivery devices for the administration of 17beta-oestradiol precursors | |
| EP0692965A1 (de) | Verfahren und präparat zur behandlung von osteoporose | |
| Benagiano et al. | Long Acting Polydimethylsiloxane Implants for Contraception |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Patent granted |
Ref document number: 119414 Country of ref document: FI |
|
| PC | Transfer of assignment of patent |
Owner name: WARNER CHILCOTT (IRELAND) LIMITED Free format text: WARNER CHILCOTT (IRELAND) LIMITED |
|
| MA | Patent expired |