JPWO2020176004A5 - - Google Patents
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- JPWO2020176004A5 JPWO2020176004A5 JP2021572255A JP2021572255A JPWO2020176004A5 JP WO2020176004 A5 JPWO2020176004 A5 JP WO2020176004A5 JP 2021572255 A JP2021572255 A JP 2021572255A JP 2021572255 A JP2021572255 A JP 2021572255A JP WO2020176004 A5 JPWO2020176004 A5 JP WO2020176004A5
- Authority
- JP
- Japan
- Prior art keywords
- weight
- parts
- gel
- poloxamer
- solution
- 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.)
- Granted
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- 239000000243 solution Substances 0.000 claims description 123
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims description 91
- 238000000034 method Methods 0.000 claims description 72
- HYIMSNHJOBLJNT-UHFFFAOYSA-N nifedipine Chemical compound COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1C1=CC=CC=C1[N+]([O-])=O HYIMSNHJOBLJNT-UHFFFAOYSA-N 0.000 claims description 71
- 229960001597 nifedipine Drugs 0.000 claims description 71
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical group [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims description 69
- 239000000203 mixture Substances 0.000 claims description 68
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 claims description 54
- 229940044476 poloxamer 407 Drugs 0.000 claims description 52
- 229920001992 poloxamer 407 Polymers 0.000 claims description 52
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 50
- YECIFGHRMFEPJK-UHFFFAOYSA-N lidocaine hydrochloride monohydrate Chemical compound O.[Cl-].CC[NH+](CC)CC(=O)NC1=C(C)C=CC=C1C YECIFGHRMFEPJK-UHFFFAOYSA-N 0.000 claims description 47
- 238000003756 stirring Methods 0.000 claims description 45
- 229960004393 lidocaine hydrochloride Drugs 0.000 claims description 41
- 229920001993 poloxamer 188 Polymers 0.000 claims description 35
- 229940044519 poloxamer 188 Drugs 0.000 claims description 35
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 34
- 238000004519 manufacturing process Methods 0.000 claims description 34
- 229920001223 polyethylene glycol Polymers 0.000 claims description 33
- 239000007864 aqueous solution Substances 0.000 claims description 32
- 206010002153 Anal fissure Diseases 0.000 claims description 30
- 238000011200 topical administration Methods 0.000 claims description 30
- 239000002202 Polyethylene glycol Substances 0.000 claims description 29
- 239000003002 pH adjusting agent Substances 0.000 claims description 29
- 208000016583 Anus disease Diseases 0.000 claims description 28
- 208000009531 Fissure in Ano Diseases 0.000 claims description 28
- 208000002193 Pain Diseases 0.000 claims description 24
- 208000014617 hemorrhoid Diseases 0.000 claims description 24
- 229940068918 polyethylene glycol 400 Drugs 0.000 claims description 22
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 claims description 22
- 239000012535 impurity Substances 0.000 claims description 21
- 238000010879 hemorrhoidectomy Methods 0.000 claims description 18
- 239000008213 purified water Substances 0.000 claims description 18
- 238000002156 mixing Methods 0.000 claims description 17
- 238000002360 preparation method Methods 0.000 claims description 16
- 208000024891 symptom Diseases 0.000 claims description 14
- 239000012456 homogeneous solution Substances 0.000 claims description 13
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 claims description 13
- 239000004292 methyl p-hydroxybenzoate Substances 0.000 claims description 13
- 229960002216 methylparaben Drugs 0.000 claims description 13
- 229940057847 polyethylene glycol 600 Drugs 0.000 claims description 12
- NNJVILVZKWQKPM-UHFFFAOYSA-N Lidocaine Chemical compound CCN(CC)CC(=O)NC1=C(C)C=CC=C1C NNJVILVZKWQKPM-UHFFFAOYSA-N 0.000 claims description 11
- 229960004194 lidocaine Drugs 0.000 claims description 11
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 claims description 11
- 239000004405 propyl p-hydroxybenzoate Substances 0.000 claims description 11
- 229960003415 propylparaben Drugs 0.000 claims description 11
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 10
- 230000008034 disappearance Effects 0.000 claims description 9
- 230000035876 healing Effects 0.000 claims description 8
- 239000004615 ingredient Substances 0.000 claims description 8
- 230000008569 process Effects 0.000 claims description 8
- 208000011580 syndromic disease Diseases 0.000 claims description 8
- 239000002245 particle Substances 0.000 claims description 6
- 239000000825 pharmaceutical preparation Substances 0.000 claims description 6
- 229940127557 pharmaceutical product Drugs 0.000 claims description 6
- 208000035475 disorder Diseases 0.000 claims description 4
- MFBSLPHMAVHSHH-UHFFFAOYSA-M sodium;propyl 4-hydroxybenzoate;hydroxide Chemical compound [OH-].[Na+].CCCOC(=O)C1=CC=C(O)C=C1 MFBSLPHMAVHSHH-UHFFFAOYSA-M 0.000 claims 2
- 239000000499 gel Substances 0.000 description 119
- 230000000694 effects Effects 0.000 description 15
- 238000009472 formulation Methods 0.000 description 14
- 238000011282 treatment Methods 0.000 description 12
- 230000009467 reduction Effects 0.000 description 11
- 239000013543 active substance Substances 0.000 description 10
- 239000003814 drug Substances 0.000 description 9
- 239000000047 product Substances 0.000 description 9
- 241000700159 Rattus Species 0.000 description 6
- 208000005392 Spasm Diseases 0.000 description 6
- 239000012736 aqueous medium Substances 0.000 description 6
- 201000010099 disease Diseases 0.000 description 6
- 239000007788 liquid Substances 0.000 description 6
- -1 nipazole Polymers 0.000 description 6
- 239000008194 pharmaceutical composition Substances 0.000 description 6
- 241001465754 Metazoa Species 0.000 description 5
- SNIOPGDIGTZGOP-UHFFFAOYSA-N Nitroglycerin Chemical compound [O-][N+](=O)OCC(O[N+]([O-])=O)CO[N+]([O-])=O SNIOPGDIGTZGOP-UHFFFAOYSA-N 0.000 description 5
- 239000002674 ointment Substances 0.000 description 5
- 230000002265 prevention Effects 0.000 description 5
- 210000005070 sphincter Anatomy 0.000 description 5
- 238000004090 dissolution Methods 0.000 description 4
- 229940126601 medicinal product Drugs 0.000 description 4
- 230000002906 microbiologic effect Effects 0.000 description 4
- 229920001983 poloxamer Polymers 0.000 description 4
- 229960000502 poloxamer Drugs 0.000 description 4
- 208000007101 Muscle Cramp Diseases 0.000 description 3
- 239000002671 adjuvant Substances 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 239000011521 glass Substances 0.000 description 3
- 238000012423 maintenance Methods 0.000 description 3
- 239000003381 stabilizer Substances 0.000 description 3
- 239000000725 suspension Substances 0.000 description 3
- 239000002562 thickening agent Substances 0.000 description 3
- 229940127291 Calcium channel antagonist Drugs 0.000 description 2
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 2
- 239000000006 Nitroglycerin Substances 0.000 description 2
- 210000002255 anal canal Anatomy 0.000 description 2
- 238000011161 development Methods 0.000 description 2
- 239000000839 emulsion Substances 0.000 description 2
- 229960003711 glyceryl trinitrate Drugs 0.000 description 2
- 239000008240 homogeneous mixture Substances 0.000 description 2
- 238000000265 homogenisation Methods 0.000 description 2
- 238000001727 in vivo Methods 0.000 description 2
- 238000005259 measurement Methods 0.000 description 2
- 230000000144 pharmacologic effect Effects 0.000 description 2
- 238000011084 recovery Methods 0.000 description 2
- 210000002460 smooth muscle Anatomy 0.000 description 2
- BHPQYMZQTOCNFJ-UHFFFAOYSA-N Calcium cation Chemical compound [Ca+2] BHPQYMZQTOCNFJ-UHFFFAOYSA-N 0.000 description 1
- 206010010774 Constipation Diseases 0.000 description 1
- IAYPIBMASNFSPL-UHFFFAOYSA-N Ethylene oxide Chemical compound C1CO1 IAYPIBMASNFSPL-UHFFFAOYSA-N 0.000 description 1
- 206010019233 Headaches Diseases 0.000 description 1
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 1
- GOOHAUXETOMSMM-UHFFFAOYSA-N Propylene oxide Chemical compound CC1CO1 GOOHAUXETOMSMM-UHFFFAOYSA-N 0.000 description 1
- 229920002125 Sokalan® Polymers 0.000 description 1
- RTAQQCXQSZGOHL-UHFFFAOYSA-N Titanium Chemical group [Ti] RTAQQCXQSZGOHL-UHFFFAOYSA-N 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 238000004458 analytical method Methods 0.000 description 1
- 210000000436 anus Anatomy 0.000 description 1
- 230000008901 benefit Effects 0.000 description 1
- 229920001400 block copolymer Polymers 0.000 description 1
- 230000017531 blood circulation Effects 0.000 description 1
- 239000000480 calcium channel blocker Substances 0.000 description 1
- 229910001424 calcium ion Inorganic materials 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 239000003638 chemical reducing agent Substances 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 230000007547 defect Effects 0.000 description 1
- 229960004166 diltiazem Drugs 0.000 description 1
- HSUGRBWQSSZJOP-RTWAWAEBSA-N diltiazem Chemical compound C1=CC(OC)=CC=C1[C@H]1[C@@H](OC(C)=O)C(=O)N(CCN(C)C)C2=CC=CC=C2S1 HSUGRBWQSSZJOP-RTWAWAEBSA-N 0.000 description 1
- 208000002173 dizziness Diseases 0.000 description 1
- 230000008030 elimination Effects 0.000 description 1
- 238000003379 elimination reaction Methods 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 231100000869 headache Toxicity 0.000 description 1
- 208000019622 heart disease Diseases 0.000 description 1
- 230000002209 hydrophobic effect Effects 0.000 description 1
- 230000028709 inflammatory response Effects 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 239000013067 intermediate product Substances 0.000 description 1
- 208000028867 ischemia Diseases 0.000 description 1
- 239000008141 laxative Substances 0.000 description 1
- 229940125722 laxative agent Drugs 0.000 description 1
- 230000010534 mechanism of action Effects 0.000 description 1
- 239000000693 micelle Substances 0.000 description 1
- 230000004089 microcirculation Effects 0.000 description 1
- 230000004660 morphological change Effects 0.000 description 1
- 210000004877 mucosa Anatomy 0.000 description 1
- 210000003205 muscle Anatomy 0.000 description 1
- 238000006386 neutralization reaction Methods 0.000 description 1
- 238000010979 pH adjustment Methods 0.000 description 1
- 230000008058 pain sensation Effects 0.000 description 1
- 230000001717 pathogenic effect Effects 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 238000011321 prophylaxis Methods 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 230000002459 sustained effect Effects 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 229910052719 titanium Inorganic materials 0.000 description 1
- 239000010936 titanium Substances 0.000 description 1
- 230000007704 transition Effects 0.000 description 1
- 230000002883 vasorelaxation effect Effects 0.000 description 1
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/RU2019/000120 WO2020176004A1 (ru) | 2019-02-25 | 2019-02-25 | Гель для ректального и наружного применения |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2022521444A JP2022521444A (ja) | 2022-04-07 |
| JPWO2020176004A5 true JPWO2020176004A5 (enrdf_load_stackoverflow) | 2022-11-28 |
| JP7331149B2 JP7331149B2 (ja) | 2023-08-22 |
Family
ID=72235046
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021572255A Active JP7331149B2 (ja) | 2019-02-25 | 2019-02-25 | 直腸および局所投与のためのゲル |
Country Status (3)
| Country | Link |
|---|---|
| JP (1) | JP7331149B2 (enrdf_load_stackoverflow) |
| EA (1) | EA036752B1 (enrdf_load_stackoverflow) |
| WO (1) | WO2020176004A1 (enrdf_load_stackoverflow) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2024512791A (ja) * | 2021-04-01 | 2024-03-19 | スティール セラピューティクス，インク． | ニフェジピンとリドカインとを含む局所用ワイプ |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT1297886B1 (it) * | 1997-02-28 | 1999-12-20 | Carmine Antropoli | Nifedipina per uso topico |
| CN1813766A (zh) * | 2005-12-19 | 2006-08-09 | 杨树强 | 一种痔疮软膏及其制备方法 |
| RU2538079C1 (ru) * | 2013-12-30 | 2015-01-10 | Светлана Николаевна Суслина | Композиция для лечения анальных трещин |
| RU2606858C2 (ru) * | 2014-09-30 | 2017-01-10 | ОБЩЕСТВО С ОГРАНИЧЕННОЙ ОТВЕТСТВЕННОСТЬЮ "НоваМедика" | Способ растворения нифедипина в водной среде с использованием нанотехнологии. фармацевтическая композиция, содержащая раствор нифедипина в водной среде. способ количественного определения нифедипина в растворе |
| RU2641570C2 (ru) * | 2015-01-21 | 2018-01-18 | ОБЩЕСТВО С ОГРАНИЧЕННОЙ ОТВЕТСТВЕННОСТЬЮ "НоваМедика" | Гель, включающий нифедипин и лидокаина гидрохлорид (варианты), применение геля, включающего нифедипин и лидокаина гидрохлорид (варианты), способ приготовления геля, включающего нифедипин и лидокаина гидрохлорид, с использованием нанотехнологии |
| WO2016118040A1 (ru) * | 2015-01-21 | 2016-07-28 | ОБЩЕСТВО С ОГРАНИЧЕННОЙ ОТВЕТСТВЕННОСТЬЮ "НоваМедика" | Гель, содержащий нифедипин и лидокаина гидрохлорид, его применение и способ приготовления с использованием нанотехнологий |
-
2019
- 2019-02-25 WO PCT/RU2019/000120 patent/WO2020176004A1/ru active Application Filing
- 2019-02-25 EA EA201991220A patent/EA036752B1/ru unknown
- 2019-02-25 JP JP2021572255A patent/JP7331149B2/ja active Active
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