EA018383B1 - Composition for treating dysplastic changes in the uterine cervix - Google Patents

Composition for treating dysplastic changes in the uterine cervix Download PDF

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Publication number
EA018383B1
EA018383B1 EA201100417A EA201100417A EA018383B1 EA 018383 B1 EA018383 B1 EA 018383B1 EA 201100417 A EA201100417 A EA 201100417A EA 201100417 A EA201100417 A EA 201100417A EA 018383 B1 EA018383 B1 EA 018383B1
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EA
Eurasian Patent Office
Prior art keywords
gallate
suppository
epigallocatechin
diindolylmethane
butylhydroxyanisole
Prior art date
Application number
EA201100417A
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Russian (ru)
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EA201100417A1 (en
Inventor
Всеволод Иванович КИСЕЛЕВ
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Всеволод Иванович КИСЕЛЕВ
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Publication date
Application filed by Всеволод Иванович КИСЕЛЕВ filed Critical Всеволод Иванович КИСЕЛЕВ
Publication of EA201100417A1 publication Critical patent/EA201100417A1/en
Publication of EA018383B1 publication Critical patent/EA018383B1/en

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    • 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
    • A61K9/02—Suppositories; Bougies; Bases therefor; Ovules
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • A61K31/353—3,4-Dihydrobenzopyrans, e.g. chroman, catechin
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/06—Aluminium, calcium or magnesium; Compounds thereof, e.g. clay
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Reproductive Health (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Inorganic Chemistry (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Urology & Nephrology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Medicinal Preparation (AREA)

Abstract

The invention relates to medicine and the pharmaceutical industry, in particular to new agents for treating dysplastic changes in the uterine cervix and the rectal mucosa. The inventive medicinal agent for treating dysplastic changes in the uterine cervix and the rectal mucosa is in the form of a suppository and is characterized in that it contains 3,3'-diindolylmethane, epigallocatechin-3-gallate, a catalyst of the inhibitory activity of epigallocatechin-3-gallate with respect to DNA methyltransferase, consisting of Mgcations in the form of a pharmaceutically acceptable magnesium salt, a lipophilic base containing solid fat, polyvinylpyrrolidone and butylhydroxyanisole and/or butylhydroxytoluene with the following component ratio, wt.%: 3,3'-diindolylmethane – 1.0-10.0; epigallocatechin-3-gallate – 1.0-8.0; polyvinylpyrrolidone – 0.5-1.2; butylhydroxyanisole – 0.3-0.5; magnesium salt – 0.1-0.2; lipophilic base – remaining. The invention is aimed at providing more effective agent based on diindolylmethane.

Description

(57) Изобретение относится к области медицины, фармацевтической промышленности и касается новых средств, используемых для лечения диспластических процессов шейки матки и слизистой прямой кишки. Лекарственное средство для лечения диспластических процессов шейки матки и слизистой прямой кишки в форме суппозитория, характеризующееся тем, что содержит 3,3'-дииндолилметан, эпигаллокатехин-3-галлат, а также катализатор ингибирующей активности эпигаллокатехин-3-галлата в отношении ДНК-метилтрансфераз, представляющий собой катионы Мд2+ в виде фармацевтически приемлемой соли магния, липофильную основу, содержащую твердый жир, поливинилпирролидон и бутилгидроксианизол и/или бутилгидрокситолуол при следующем содержании, мас.%:(57) The invention relates to medicine, the pharmaceutical industry, and relates to new agents used to treat dysplastic processes of the cervix and rectal mucosa. A medicine for the treatment of dysplastic processes of the cervix and rectal mucosa in the form of a suppository, characterized in that it contains 3,3'-diindolylmethane, epigallocatechin-3-gallate, and also a catalyst for the inhibitory activity of epigallocatechin-3-gallate in relation to DNA methyltransferases, representing MD 2+ cations in the form of a pharmaceutically acceptable magnesium salt, a lipophilic base containing solid fat, polyvinylpyrrolidone and butylhydroxyanisole and / or butylhydroxytoluene with the following content, wt.%:

018383 В1018383 B1

018383 Β1018383 Β1

3,3'-Дииндолилметан 3,3'-Diindolylmethane 1,0-10,0 1.0-10.0 Эпигаллокатехин-З-галлат Epigallocatechin-Z-Gallate 1,0-8,0 1.0-8.0 Поливинилпирролидон Polyvinylpyrrolidone 0,5-1,2 0.5-1.2 Бутилгидроксианизол и/или Butylhydroxyanisole and / or бутилгидрокситолуол butylhydroxytoluene ОД-0,5 OD-0.5 Соль магния Magnesium salt 0,1-2,0 0.1-2.0 Липофильная основа Lipophilic base остальное rest

Claims (4)

ФОРМУЛА ИЗОБРЕТЕНИЯCLAIM 1. Лекарственное средство для лечения диспластических процессов шейки матки и слизистой прямой кишки в форме суппозитория, характеризующееся тем, что содержит 3,3'-дииндолилметан, эпигаллокатехин-3-галлат, а также катализатор ингибирующей активности эпигаллокатехин-3-галлата в отношении ДНК-метилтрансфераз, представляющий собой катионы Мд24 в виде фармацевтически приемлемой соли магния, липофильную основу, содержащую твердый жир, поливинилпирролидон и бутилгидроксианизол и/или бутилгидрокситолуол при следующем содержании, в мас.%:1. A drug for the treatment of dysplastic processes of the cervix and rectal mucosa in the form of a suppository, characterized in that it contains 3,3'-diindolylmethane, epigallocatechin-3-gallate, as well as a catalyst for the inhibitory activity of epigallocatechin-3-gallate in relation to DNA- methyltransferase, which is an MD 24 cation in the form of a pharmaceutically acceptable magnesium salt, a lipophilic base containing solid fat, polyvinylpyrrolidone and butylhydroxyanisole and / or butylhydroxytoluene in the following content, in wt.%: 3,3 ’-Дииндолилметан 3.3 ’- Diindolylmethane 1,0-10,0 1.0-10.0 Эпнгаллокатехин-З-галлат Engallocatechin-Z-Gallate 1,0-8,0 1.0-8.0 Поливинилпирролвдон Polyvinylpyrrolvdone 0,5-1,2 0.5-1.2 Бутилгидроксианизол и/или Butylhydroxyanisole and / or бутилгидрокситолуол butylhydroxytoluene 0,3-0,5 0.3-0.5 Соль магния Magnesium salt 0,1-2,0 0.1-2.0 Липофильная основа Lipophilic base остальное rest
2. Лекарственное средство по п.1, характеризующееся тем, что указанный суппозиторий представляет собой вагинальный суппозиторий.2. The drug according to claim 1, characterized in that the suppository is a vaginal suppository. 3. Лекарственное средство по п.1, характеризующееся тем, что указанный суппозиторий представляет собой ректальный суппозиторий.3. The drug according to claim 1, characterized in that the suppository is a rectal suppository. 4. Лекарственное средство по любому из пп.1-3, характеризующееся тем, что катализатор ингибирующей активности эпигаллокатехин-3-галлата в отношении ДНК-метилтрансфераз представляет собой магний хлористый.4. The drug according to any one of claims 1 to 3, characterized in that the catalyst for the inhibitory activity of epigallocatechin-3-gallate in relation to DNA methyltransferases is magnesium chloride. - 7 018383- 7 018383 Фиг. 1FIG. one ПреимущественноеPreferential Зстрадиол-Zstradiol ПромоторPromoter Эпителиальная клетка, инфицированная ВПЧ / -ОНК ВПЧ!HPV-infected epithelial cell / -ONK HPV! Взаимодействие /16 а-ОНЕИ с рецептором оВуславлибает пролонгированный зффект гормона Комплекс гормон-рецептор. взаимодействуя с промотором ВПЧ, стимулирует зкспрессию генов В6 и Е7Interaction / 16 a-ONEI with the receptor o The prolonged effect of the hormone is recognized. interacting with the HPV promoter, stimulates expression of the B6 and E7 genes Ι{7| Е1 I ,Ι {7 | E1 I, Е61 <Е2<^ =1E61 <E2 <^ = 1 АЛЛIALLI ТрансляцияBroadcast Фиг. 2FIG. 2 Фиг. 3FIG. 3 Евразийская патентная организация, ЕАПВEurasian Patent Organization, EAPO Россия, 109012, Москва, Малый Черкасский пер., 2Russia, 109012, Moscow, Maly Cherkassky per., 2
EA201100417A 2008-09-04 2009-08-18 Composition for treating dysplastic changes in the uterine cervix EA018383B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
RU2008135764/15A RU2395281C2 (en) 2008-09-04 2008-09-04 Pharmaceutical composition for treatment of dysplastic processes of cervix
PCT/RU2009/000412 WO2010027294A1 (en) 2008-09-04 2009-08-18 Composition for treating dysplastic changes in the uterine cervix

Publications (2)

Publication Number Publication Date
EA201100417A1 EA201100417A1 (en) 2011-10-31
EA018383B1 true EA018383B1 (en) 2013-07-30

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EA201100417A EA018383B1 (en) 2008-09-04 2009-08-18 Composition for treating dysplastic changes in the uterine cervix

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EA (1) EA018383B1 (en)
RU (1) RU2395281C2 (en)
UA (1) UA95583C2 (en)
WO (1) WO2010027294A1 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2601893C1 (en) * 2015-11-30 2016-11-10 Всеволод Иванович Киселев Drug preparation based on indole-3-carbinol with increased epigenetic activity

Families Citing this family (7)

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RU2454232C2 (en) * 2010-09-16 2012-06-27 Федеральное государственное бюджетное учреждение "Российский онкологический научный центр имени Н.Н. Блохина" Российской академии медицинских наук (ФГБУ "РОНЦ им. Н.Н. Блохина" РАМН) Application of triindolyl methane derivatives as anticancer drugs
RU2456987C1 (en) * 2011-03-21 2012-07-27 Сергей Владимирович Енгашев Method for producing gelatine capsules of 3,31-diindolylmethane
GB2533381A (en) * 2014-12-18 2016-06-22 Nordic Labs Ltd Novel treatment of STIs
RU2601621C2 (en) * 2015-03-18 2016-11-10 Общество с ограниченной ответственностью "Фармацевтический завод иммунных лекарственных средств" Sodium deoxyribonucleate suppositories, rectal and vaginal
GB2542106A (en) * 2015-04-01 2017-03-15 Nordic Labs Ltd Novel treatment of STIs
WO2017200413A1 (en) * 2016-05-16 2017-11-23 Нордик Лабз Лимитед Means for treating sexually-transmitted infectious diseases
CN108969602A (en) * 2018-09-29 2018-12-11 南京依美生物科技有限公司 It is a kind of to treat the Chinese medicine composition and preparation method that human papilloma virus sun is turned out cloudy

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2185070C2 (en) * 1995-03-14 2002-07-20 Индена С.П.А. Tea polyphenolic fractions, their use and compositions comprising thereof
RU2196568C1 (en) * 2001-08-08 2003-01-20 Киселев Всеволод Иванович Pharmaceutical composition for prophylaxis and treatment of uterus cervix dysplasia and cancer and larynx papillomatosis and method of prophylaxis and treatment of said sicknesses based on thereof
RU2301666C2 (en) * 2002-01-11 2007-06-27 Маттиас Рат Polyphenol-base pharmaceutical composition possessing nutrient properties and its using in cancer treatment
RU2315594C1 (en) * 2006-09-01 2008-01-27 Всеволод Иванович Киселев Anti-estrogenic and anti-proliferative agent for treatment and prophylaxis of female reproductive system diseases
RU2318510C1 (en) * 2006-04-19 2008-03-10 Всеволод Иванович Киселев 3,3'-diindolylmethane (metindol)-base vaginal suppository

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2185070C2 (en) * 1995-03-14 2002-07-20 Индена С.П.А. Tea polyphenolic fractions, their use and compositions comprising thereof
RU2196568C1 (en) * 2001-08-08 2003-01-20 Киселев Всеволод Иванович Pharmaceutical composition for prophylaxis and treatment of uterus cervix dysplasia and cancer and larynx papillomatosis and method of prophylaxis and treatment of said sicknesses based on thereof
RU2301666C2 (en) * 2002-01-11 2007-06-27 Маттиас Рат Polyphenol-base pharmaceutical composition possessing nutrient properties and its using in cancer treatment
RU2318510C1 (en) * 2006-04-19 2008-03-10 Всеволод Иванович Киселев 3,3'-diindolylmethane (metindol)-base vaginal suppository
RU2315594C1 (en) * 2006-09-01 2008-01-27 Всеволод Иванович Киселев Anti-estrogenic and anti-proliferative agent for treatment and prophylaxis of female reproductive system diseases

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2601893C1 (en) * 2015-11-30 2016-11-10 Всеволод Иванович Киселев Drug preparation based on indole-3-carbinol with increased epigenetic activity

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Publication number Publication date
RU2395281C2 (en) 2010-07-27
RU2008135764A (en) 2010-03-10
EA201100417A1 (en) 2011-10-31
UA95583C2 (en) 2011-08-10
WO2010027294A1 (en) 2010-03-11

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