TR201810389T4 - Polimerik finasterid ve minoksidil nanopartikülleri, bunları hazırlamak için yöntem, bunları içeren aköz süspansiyon, farmasötik bileşim ve bunların kullanımı. - Google Patents
Polimerik finasterid ve minoksidil nanopartikülleri, bunları hazırlamak için yöntem, bunları içeren aköz süspansiyon, farmasötik bileşim ve bunların kullanımı. Download PDFInfo
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- TR201810389T4 TR201810389T4 TR2018/10389T TR201810389T TR201810389T4 TR 201810389 T4 TR201810389 T4 TR 201810389T4 TR 2018/10389 T TR2018/10389 T TR 2018/10389T TR 201810389 T TR201810389 T TR 201810389T TR 201810389 T4 TR201810389 T4 TR 201810389T4
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- Prior art keywords
- finasteride
- minoxidil
- pharmaceutical composition
- alopecia
- constituting
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- 239000002105 nanoparticle Substances 0.000 title claims abstract description 10
- 229960004039 finasteride Drugs 0.000 title claims abstract description 9
- DBEPLOCGEIEOCV-WSBQPABSSA-N finasteride Chemical compound N([C@@H]1CC2)C(=O)C=C[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H](C(=O)NC(C)(C)C)[C@@]2(C)CC1 DBEPLOCGEIEOCV-WSBQPABSSA-N 0.000 title claims abstract description 9
- ZFMITUMMTDLWHR-UHFFFAOYSA-N Minoxidil Chemical compound NC1=[N+]([O-])C(N)=CC(N2CCCCC2)=N1 ZFMITUMMTDLWHR-UHFFFAOYSA-N 0.000 title claims abstract description 7
- 229960003632 minoxidil Drugs 0.000 title claims abstract description 7
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract 5
- 239000007900 aqueous suspension Substances 0.000 title 1
- 201000004384 Alopecia Diseases 0.000 claims abstract description 13
- 231100000360 alopecia Toxicity 0.000 claims abstract description 7
- 230000000699 topical effect Effects 0.000 claims abstract description 3
- 239000003937 drug carrier Substances 0.000 claims abstract 2
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 4
- 229940057917 medium chain triglycerides Drugs 0.000 claims 3
- HVUMOYIDDBPOLL-XWVZOOPGSA-N Sorbitan monostearate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O HVUMOYIDDBPOLL-XWVZOOPGSA-N 0.000 claims 2
- 239000008346 aqueous phase Substances 0.000 claims 2
- WWZKQHOCKIZLMA-UHFFFAOYSA-N octanoic acid Chemical compound CCCCCCCC(O)=O WWZKQHOCKIZLMA-UHFFFAOYSA-N 0.000 claims 2
- 239000012074 organic phase Substances 0.000 claims 2
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims 2
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 claims 2
- 229920000053 polysorbate 80 Polymers 0.000 claims 2
- 229940068968 polysorbate 80 Drugs 0.000 claims 2
- 235000011076 sorbitan monostearate Nutrition 0.000 claims 2
- 239000001587 sorbitan monostearate Substances 0.000 claims 2
- 229940035048 sorbitan monostearate Drugs 0.000 claims 2
- 239000004094 surface-active agent Substances 0.000 claims 2
- 239000005632 Capric acid (CAS 334-48-5) Substances 0.000 claims 1
- 239000005635 Caprylic acid (CAS 124-07-2) Substances 0.000 claims 1
- GHVNFZFCNZKVNT-UHFFFAOYSA-N Decanoic acid Natural products CCCCCCCCCC(O)=O GHVNFZFCNZKVNT-UHFFFAOYSA-N 0.000 claims 1
- 229920002988 biodegradable polymer Polymers 0.000 claims 1
- 239000004621 biodegradable polymer Substances 0.000 claims 1
- -1 capric acid triglycerides Chemical class 0.000 claims 1
- 239000006184 cosolvent Substances 0.000 claims 1
- 229920001600 hydrophobic polymer Polymers 0.000 claims 1
- 239000006210 lotion Substances 0.000 claims 1
- 230000008018 melting Effects 0.000 claims 1
- 238000002844 melting Methods 0.000 claims 1
- 239000000346 nonvolatile oil Substances 0.000 claims 1
- 239000003960 organic solvent Substances 0.000 claims 1
- 229920000728 polyester Polymers 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
- 239000002088 nanocapsule Substances 0.000 abstract 3
- 239000004480 active ingredient Substances 0.000 abstract 1
- 239000000654 additive Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 206010068168 androgenetic alopecia Diseases 0.000 description 5
- 239000003098 androgen Substances 0.000 description 4
- 201000002996 androgenic alopecia Diseases 0.000 description 4
- 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 description 2
- 238000012377 drug delivery Methods 0.000 description 2
- 210000004209 hair Anatomy 0.000 description 2
- 210000003780 hair follicle Anatomy 0.000 description 2
- 230000003076 paracrine Effects 0.000 description 2
- 206010012442 Dermatitis contact Diseases 0.000 description 1
- 241001379910 Ephemera danica Species 0.000 description 1
- 238000010171 animal model Methods 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 230000001413 cellular effect Effects 0.000 description 1
- 238000012512 characterization method Methods 0.000 description 1
- 239000000084 colloidal system Substances 0.000 description 1
- 208000010247 contact dermatitis Diseases 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 230000008021 deposition Effects 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 238000006073 displacement reaction Methods 0.000 description 1
- 230000002500 effect on skin Effects 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 230000003325 follicular Effects 0.000 description 1
- 230000003450 growing effect Effects 0.000 description 1
- 208000024963 hair loss Diseases 0.000 description 1
- 230000003676 hair loss Effects 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 239000002502 liposome Substances 0.000 description 1
- 230000005184 men's health Effects 0.000 description 1
- 230000009456 molecular mechanism Effects 0.000 description 1
- 239000002077 nanosphere Substances 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 230000035699 permeability Effects 0.000 description 1
- 238000001050 pharmacotherapy Methods 0.000 description 1
- 229920001606 poly(lactic acid-co-glycolic acid) Polymers 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 210000004761 scalp Anatomy 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 210000003491 skin Anatomy 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 229960003604 testosterone Drugs 0.000 description 1
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- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/51—Nanocapsules; Nanoparticles
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- 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
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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
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Abstract
Bu buluş, finasterid ve minoksidil adlı iki etkin bileşenin yer aldığı polimerik nanopartiküller, tercihen nanokapsüller ve ayrıca katkı maddeleri ve bir farmasötik açıdan kabul edilebilir taşıyıcı ihtiva eden ve alopesinin tedavisinde kullanıma yönelik olan topikal uygulamalı bir farmasötik bileşim ile ilgilidir. Bu buluş, ayrıca, alopesinin tedavisi için uygun topikal uygulamalı bir bileşimi teşkil eden finasterid ve minoksidilin yer aldıkları polimerik nanopartikülleri, tercihen nanokapsülleri hazırlamaya yönelik bir hazırlama prosesi ve ayrıca bahsi geçen nanokapsüllerin bir farmasötik bileşim hazırlamak için kullanımı ile de ilgilidir.
Description
Tarifname içerisinde atifta bulunulan patent dökümanlari:
Tarifnamede belirtilen patentlestirilmemis literatür:
- DRAKE, L. et al. The effects of
finasteride on scalp skin and serum
androgen levels in men with
androgenetic alopecia. Journal of the
American Academy of Dermatology,
° INUI, S. ; ITAMI, S. Molecular basis
androgen to paracrine mediators
through derinal papilla. Journal of
Dermatological Science, 201 1, vol. 61,
1-6 [0004]
° TRUEB, RM. Molecular mechanisms
of androgenetic alopecia. Experimental
990 [0004]
o LIU, S.; YAMAUCHI, H. Different
patterns of Su-reductase expression,
cellular distribution, and testosterone
inetabolism in human follicular derinal
Biophysical Research Cominunications,
o INUI, S . ; ITAMI, S. Molecular
basis of androgenetic alopecia: From
androgen to paracrine mediators
- SCHAFFAZICK, SH et al.
Characterization and physicochemical
stability of nanoparticle polymeric
formation by interfacial polymer
deposition following solvent
displacement. International Journal of
Pharmaceutics, 1989, vol. 55
(1), R1-R4 [0011]
the permeability of hair growing
ingredient encapsulated PLGA
nanospheres to hair follicles and their
hair growing effects. Bioorganic &
Medicinal Chemistry Letters, 2007, vol.
° LADEMANN, J. et al. Nanoparticles
- An efficient carrier for drug delivery
into the hair follicles. European
Journal of Pharmaceutics and
Biophaririaceutics, 2007, vol. 66 (2),
° SINCLAIR, RD. Male androgenetic
through dermal papilla. Journal of
Derinatological Science, 2011, vol. 61,
1-6 [0005]
o ELLIS, JA ; HARRAP, SB. The
genetics of androgenetic alopecia.
Clinics in Dermatology, 2001 , vol.
alopecia. The Journal of Men's Health
o AVNESH KUMARI ; SUDESH
KUMAR YADAV ; SUBHASH C.
nanoparticle based drug delivery
systems. Colloids and
Surfaces B: Biointerfaces, 01 January
° VLADIMIR P. TORCHILIN.
RECENT ADVANCES WITH
LIPOSOMES AS HARMACEUTICAL
CARRIERS. NATURE REVIEW S,
alopecia: Part 11. The Journal of Men°s
Health & Gender, 2005, vol. 2
(1), 38-44 [0029]
- STOUT, SM; STUMPF, JL.
Finasteride Treatment of Hair Loss in
Women. The Annals of
Pharmacotherapy,
contact dermatitis to topical minoxidil
solution: Etiology and treatment.
Journal of the American Academy of
312 [0030]
o MATIAS, JR et al. Animal models of
androgen-dependent disorders of the
piloscbaceous apparatus. 1. The
androchronogenetic alopecia (AGA)
Mouse as a model for male-pattern
baldness. Archives of Dermatological
SEKILLERDEKI YAZILARIN ANLAMLARI
A = Grafik
B : Hacim
C = Partikül Büyüklügü
D = Alan basina hücre sayisi
10000
10000
40.00
Claims (6)
- ISTEMLER 1.
- Finasterid ve minoksidil etkin bilesenlerini ihtiva eden ve asagida belirtilen unsurlar ile elde edilebilecek olan bir nanokapsoid formundaki polimerik nanopartikül: (i) asagida belirtilenleri içeren bir organik faz: (a) erime noktasi IZOOC'den düsük olan polyesterler grubu arasindan seçilen bir biyobozunur polimeri teskil eden bir hidrofobik polimer, bir poli(g- kaprolakton); (b) orta boy ziiicirli trigliseritler arasindan seçilen bir sabit yag; (0) 3 ile 6 arasi bir degere tekabül eden düsük bir HLB'nin söz konusu oldugu bir lipofilik yüzey aktif madde, bir sorbitan monostearat; (d) asetonu teskil eden bir organik çözücü, (e) etanolü teskil eden bir es-çözü.cü;ve (Ü finasterid; ve (ii) asagida belirtilenleri içeren bir aköz faz: (g) polisorbat 80'i teskil eden bir hidrofilik yüzey aktif madde; (h) minoksidil; ve Istein l'e uygun poliinerik nanopartik'ul olup, burada bahsi geçen orta boy Zincirli trigliseritler, kaprilik ve kaprik asit trigliseritleridir.
- Istem l'e uygun polimerik nanopartikûl olup, burada (i) bahsi geçen organik faz asagida belirtilenleri içerir: (21) %0,05 ile %20,0 (a/a) arasi bir oranda bir poli(8-kaprolakton); (b) %0,05 ile %25,0 (a/a) arasi bir oranda orta boy Zincirli trigliseritler; (0) %0,05 ile %25,0 (a/a) arasi bir oranda bir sorbitan monostearat; (d) %10 ile %80 (a/a) arasi bir oranda aseton; (e) %0,001 ile %50 (a/a) arasi bir oranda etanol; ve (f) %0,005 ile %50,0 (a/a) arasi bir oranda finasterid; ve (ii) bahsi geçen ak'oz faz asagida belirtilenleri içerir: (g) %0,005 ile %50,0 (a/a) arasi bir oranda ininoksidil; (h) %0,05 ile %20,0 (a/a) arasi bir oranda polisorbat 80; ve (i) %10 ile %90 (a/a) arasi bir oranda su.
- 4. Asagida belirtilenleri içeren ve alopesinin tedavisinde kullaniin için olan farmasötik bilesim: (A) istemler 1 ilâ 3'e uygun, bir nanokapsoid formunda bulunan, %0,01 ile %1,0 (a/a) arasi bir oranda finasterid ve %0,01 ile %2,0 (a/a) arasi bir oranda minoksidil; ve (B) bir farmasötik açidan kabul edilebilir tasiyici.
- 5. Topikal uygulama için olan ve bir çözelti, jel veya losyon formunda bulunan, istem 4'e uygun kullanim için, farmasötik bilesim.
- 6. Alopesinin tedavisinde kullanim için, istemler l ilâ 3'ten herhangi birinde tanimlandigi gibi olan nanokapsoidler formundaki polimerik nanopartikül.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
BR102012022036-9A BR102012022036B1 (pt) | 2012-08-31 | 2012-08-31 | Nanopartícula polimérica de finasterida e minoxidil, processo de sua preparação, suspensão aquosa contendo a mesma, composição farmacêutica, e seu uso |
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TR201810389T4 true TR201810389T4 (tr) | 2018-08-27 |
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TR2018/10389T TR201810389T4 (tr) | 2012-08-31 | 2013-08-30 | Polimerik finasterid ve minoksidil nanopartikülleri, bunları hazırlamak için yöntem, bunları içeren aköz süspansiyon, farmasötik bileşim ve bunların kullanımı. |
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CN104887685A (zh) * | 2015-05-05 | 2015-09-09 | 谢秉权 | 一种治疗和/或预防男性型脱发的复方外用药 |
ES2613888B1 (es) * | 2016-08-19 | 2017-11-16 | Enrique Blanxart Sena | Composición farmacéutica para el tratamiento de la alopecia |
WO2018206077A1 (en) * | 2017-05-08 | 2018-11-15 | Merz Pharma Gmbh & Co. Kgaa | Emulsion comprising finasteride |
DK3638198T3 (da) * | 2017-06-16 | 2021-11-22 | Capilli Med Gmbh | Sammensætning til at forebygge hårtab og fremme hårvækst |
MX2018001546A (es) * | 2018-02-06 | 2019-08-07 | Centro Int De Cosmiatria S A P I De C V | Formulacion y metodo para el tratamiento de la alopecia androgenica. |
CN110448525A (zh) * | 2018-05-08 | 2019-11-15 | 无锡派列博生物医药科技有限公司 | 一种预防脱发和促生发的外用非那雄胺脂质纳米制剂及其制备方法 |
WO2020097284A1 (en) * | 2018-11-08 | 2020-05-14 | Jindal Vinay K | TOPICAL FORMULATIONS OF 5-α-REDUCTASE INHIBITORS AND USES THEREOF |
WO2020121329A1 (en) * | 2018-12-11 | 2020-06-18 | Dr Rathod Sudha Suresh | Minoxidil and castor oil nanoemulgel for alopecia |
CN112773776B (zh) * | 2019-11-11 | 2023-06-20 | 上海胜联医药科技有限公司 | 一种载药纳米粒体系 |
CN111329832B (zh) * | 2020-02-08 | 2021-07-16 | 中山大学 | 一种治疗脱发的纳米脂质载体微针及其应用 |
EP4114362A4 (en) * | 2020-03-05 | 2024-03-20 | Univ Miami | NANODRUG FORMULATIONS OF CANNABIDIOL AND THEIR METHODS OF USE |
AU2020389480A1 (en) | 2020-03-30 | 2021-10-14 | Hyundaibioscience Co.,Ltd. | Ethosomal composition including ethosomes encapsulating vitamin and dexpanthenol and method for preparing the same |
US11311556B2 (en) | 2020-05-13 | 2022-04-26 | Varsona Therapeutics, Inc. | Topical dutasteride emulsions for treating endocrine therapy-induced alopecia |
CN114910567B (zh) * | 2021-02-07 | 2023-11-24 | 株洲千金药业股份有限公司 | 一种检测非那雄胺中遗传毒性杂质的方法及其应用 |
CN113425845B (zh) * | 2021-08-10 | 2022-12-02 | 成都倍特药业股份有限公司 | 一种预防和/或治疗脱发症的传递体制剂及其制备方法和用途 |
CN113797208B (zh) * | 2021-11-17 | 2022-02-25 | 山东谷雨春生物科技有限公司 | 一种含米诺地尔的制剂及其制备方法和应用 |
KR20230113871A (ko) | 2022-01-24 | 2023-08-01 | (주) 해피론이엔지 | 발포폴리에틸렌메시를 이용한 건축물 층간소음방지 시공방법 및 구조. |
KR102623083B1 (ko) | 2022-05-02 | 2024-01-10 | (주) 해피론이엔지 | 공명공간을 제거한 1차 몰탈 타설식 소음방지 시공공법 및 시공구조 |
CN115006712B (zh) * | 2022-06-28 | 2024-01-09 | 广州汇元医药科技有限公司 | 一种米诺地尔的脂质纳米粒微针及其制备方法和应用 |
CN115252549B (zh) * | 2022-07-12 | 2023-09-08 | 科辉智药生物科技(无锡)有限公司 | 提高生发活性物质药效的组合物及其制备方法 |
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BRPI0700832B8 (pt) * | 2007-03-16 | 2021-05-25 | Biolab Sanus Farmaceutica Ltda | composição anestésica tópica compreendendo suspensão de nanocápsulas poliméricas de lidocaína e prilocaína |
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LT2344198T (lt) | 2008-09-27 | 2021-02-25 | Jina Pharmaceuticals Inc. | Farmaciniai preparatai lipidų pagrindu, skirti vietiniam naudojimui |
WO2011031990A1 (en) * | 2009-09-11 | 2011-03-17 | Follica, Inc. | Intermittent and pulse lithium treatments for modulating hair growth |
ES2384060B1 (es) * | 2010-03-24 | 2013-09-23 | Lipotec S.A. | Cápsulas de nanopartículas lipídicas. |
BRPI1002601E2 (pt) * | 2010-06-01 | 2020-06-30 | Embrapa Pesquisa Agropecuaria | composição nanoestruturada de uso veterinário para administração de fármacos |
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MX363961B (es) | 2019-04-09 |
CA2883998C (en) | 2020-08-25 |
CN104755075A (zh) | 2015-07-01 |
MY174692A (en) | 2020-05-07 |
KR20150044029A (ko) | 2015-04-23 |
EP2891486A1 (en) | 2015-07-08 |
BR102012022036A2 (pt) | 2014-11-25 |
ES2683418T3 (es) | 2018-09-26 |
AR092403A1 (es) | 2015-04-22 |
CN104755075B (zh) | 2019-07-26 |
IN2015DN01728A (tr) | 2015-05-29 |
PE20150732A1 (es) | 2015-05-17 |
US9687554B2 (en) | 2017-06-27 |
JP2015526484A (ja) | 2015-09-10 |
CO7310520A2 (es) | 2015-06-30 |
US20150216986A1 (en) | 2015-08-06 |
KR102118582B1 (ko) | 2020-06-04 |
AU2013308356A1 (en) | 2015-04-16 |
JP6352265B2 (ja) | 2018-07-04 |
MX2015002300A (es) | 2016-02-10 |
EP2891486B1 (en) | 2018-05-16 |
UY35002A (es) | 2014-03-31 |
EP2891486A4 (en) | 2016-03-23 |
UA113774C2 (xx) | 2017-03-10 |
CL2015000501A1 (es) | 2015-07-03 |
WO2014032152A1 (pt) | 2014-03-06 |
PE20191714A1 (es) | 2019-12-05 |
CA2883998A1 (en) | 2014-03-06 |
DK2891486T3 (en) | 2018-07-23 |
BR102012022036B1 (pt) | 2019-10-01 |
ZA201501255B (en) | 2016-01-27 |
AU2013308356B2 (en) | 2017-09-28 |
SA515360084B1 (ar) | 2016-10-03 |
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