WO2013010915A1 - Intravaginal delivery system - Google Patents

Intravaginal delivery system Download PDF

Info

Publication number
WO2013010915A1
WO2013010915A1 PCT/EP2012/063702 EP2012063702W WO2013010915A1 WO 2013010915 A1 WO2013010915 A1 WO 2013010915A1 EP 2012063702 W EP2012063702 W EP 2012063702W WO 2013010915 A1 WO2013010915 A1 WO 2013010915A1
Authority
WO
WIPO (PCT)
Prior art keywords
acid
delivery system
intravaginal delivery
anyone
copolymers
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.)
Ceased
Application number
PCT/EP2012/063702
Other languages
English (en)
French (fr)
Inventor
Jean Paul Remon
Chris Vervaet
Hans VERSTRAELEN
Marleen TEMMERMAN
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Universiteit Gent
Original Assignee
Universiteit Gent
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Universiteit Gent filed Critical Universiteit Gent
Priority to EP12738429.5A priority Critical patent/EP2731587B1/en
Priority to JP2014520613A priority patent/JP6010120B2/ja
Priority to CN201280035030.5A priority patent/CN103648482B/zh
Priority to US14/131,495 priority patent/US9168303B2/en
Publication of WO2013010915A1 publication Critical patent/WO2013010915A1/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives thereof
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents

Definitions

  • this invention provides an intravaginal delivery system for the controlled release of one or more organic acids, said delivery system being characterized in that it comprises a combination of one or more ethylene vinyl acetate (EVA) copolymers and one or more carboxylic polymers.
  • EVA ethylene vinyl acetate
  • Slugs (Arion lusitanicus); 5 slugs per treatment group.
  • the parental slugs of Arion lusitanicus collected in local gardens along Gent and Aalter (Belgium) are bred in the laboratory in an acclimatized room (18-20°C).
  • the slugs are housed in plastic containers and fed with lettuce, cucumber, carrots and commercial dog food.
  • Treatment time was 30 min. once a day during 5 successive days.
  • the irritation and tissue damaging potency of the test items, negative and positive controls were evaluated by placing 5 slugs per treatment group daily during 30 min (contact period) on 20 mg (solids) or 100 mg (semi solids) of the test items for 5 successive days. After each 30-min contact period the slugs were transferred to a fresh Petri dish with a membrane filter moistened with 2 ml PBS until the next contact period. After the contact period mucus production was measured.
  • Table 3 Prediction model for the irritation potency of substances with a different physical state.
  • % represent mucus production expressed as % of body weight
  • the solid positive control item (DDWM/SLS 80/20) should be classified as a severe irritant (Total mucus production > 20%)
  • Adriaens E., Ameye, D., Dhondt, M. M. M., Foreman, P. and Remon, J. P. (2003).

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Reproductive Health (AREA)
  • Inorganic Chemistry (AREA)
  • Urology & Nephrology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
PCT/EP2012/063702 2011-07-15 2012-07-12 Intravaginal delivery system Ceased WO2013010915A1 (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
EP12738429.5A EP2731587B1 (en) 2011-07-15 2012-07-12 Intravaginal delivery system
JP2014520613A JP6010120B2 (ja) 2011-07-15 2012-07-12 膣内送達システム
CN201280035030.5A CN103648482B (zh) 2011-07-15 2012-07-12 阴道内递送系统
US14/131,495 US9168303B2 (en) 2011-07-15 2012-07-12 Intravaginal delivery system

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP11174103.9 2011-07-15
EP11174103 2011-07-15

Publications (1)

Publication Number Publication Date
WO2013010915A1 true WO2013010915A1 (en) 2013-01-24

Family

ID=46579003

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2012/063702 Ceased WO2013010915A1 (en) 2011-07-15 2012-07-12 Intravaginal delivery system

Country Status (5)

Country Link
US (1) US9168303B2 (enExample)
EP (1) EP2731587B1 (enExample)
JP (1) JP6010120B2 (enExample)
CN (1) CN103648482B (enExample)
WO (1) WO2013010915A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2790637A4 (en) * 2011-12-16 2015-04-29 Combinent Biomedical Systems Inc VAGINAL DRUG DELIVERY DEVICES AND METHODS OF MANUFACTURING THE SAME

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20170319833A1 (en) * 2010-03-28 2017-11-09 Evestra, Inc. Intravaginal drug delivery device
CN104274388B (zh) * 2014-09-28 2017-02-15 南京泽恒医药技术开发有限公司 维生素c缓释栓剂组合物及制备方法
EP3559107B1 (en) * 2016-12-21 2023-12-13 Braskem S.A. Modified ethylene vinyl acetate compositions, polymer blends and films made therefrom
JP2021528452A (ja) * 2018-06-25 2021-10-21 タイタン ファーマシューティカルズ インコーポレイテッド インプラントとして使用するための装填可能な多孔質構造
KR102078462B1 (ko) * 2018-07-24 2020-02-17 주식회사 디네이쳐 질환경 개선 조성물 및 이를 포함하는 개선제
CN112569225B (zh) * 2019-09-27 2022-10-21 共生地球生物科技有限公司 非药物幽门杆菌杀菌组合物
KR20210097421A (ko) * 2020-01-30 2021-08-09 주식회사 디네이쳐 펄스형 질내 약산성 환경 유지 조성물
CA3167761C (en) * 2020-02-12 2025-05-20 Shenzhen Eulikan Biotechnology Co Ltd BACTERIOSTATIC COMPOSITION, PREPARATION PROCESS AND USE

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WO2006065873A2 (en) 2004-12-14 2006-06-22 Poly-Med, Inc. Intravaginal ringed mesh device and applicator therefor
US20070196433A1 (en) 2003-04-29 2007-08-23 The Massachusetts General Hospital Corporation Methods and devices for the sustained release of multiple drugs
WO2009066006A1 (en) 2007-11-22 2009-05-28 Bayer Schering Pharma Oy Vaginal delivery system
WO2010133761A1 (en) 2009-05-19 2010-11-25 Bayer Schering Pharma Oy Intravaginal delivery system comprising one or more therapeutically active substances capable of preventing and/or treating vaginal infections

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US5543150A (en) * 1993-09-15 1996-08-06 Columbia Laboratories, Inc. Method of progesterone delivery and affect thereof
US7485666B2 (en) * 2004-06-17 2009-02-03 Kimberly-Clark Worldwide, Inc. Vaginal health products
WO2009129459A1 (en) * 2008-04-18 2009-10-22 Combinent Biomedical Systems, Inc. Devices that include ethylene-vinyl acetate copolymers and methods of making and using same
KR101993786B1 (ko) * 2010-11-12 2019-06-28 더 유니버시티 오브 유타 리서치 파운데이션 윤활제의 제어된 전달을 위한 질내 장치

Patent Citations (4)

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US20070196433A1 (en) 2003-04-29 2007-08-23 The Massachusetts General Hospital Corporation Methods and devices for the sustained release of multiple drugs
WO2006065873A2 (en) 2004-12-14 2006-06-22 Poly-Med, Inc. Intravaginal ringed mesh device and applicator therefor
WO2009066006A1 (en) 2007-11-22 2009-05-28 Bayer Schering Pharma Oy Vaginal delivery system
WO2010133761A1 (en) 2009-05-19 2010-11-25 Bayer Schering Pharma Oy Intravaginal delivery system comprising one or more therapeutically active substances capable of preventing and/or treating vaginal infections

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Title
ADRIAENS E.; REMON J.P.: "The evaluation of an alternative mucosal irritation test using slugs", TOX. APPL. PHARM., vol. 182, 2002, pages 169 - 175
ADRIAENS, E.; AMEYE, D.; DHONDT, M. M. M.; FOREMAN, P.; REMON, J. P: "Evaluation of the mucosal irritation potency of co-spray dried Amioca/Poly(Acrylic Acid) and Amioca/Carbopol 974P mixtures", J. CONTROL. RELEASE, vol. 88, no. 3, 2003, pages 393 - 399, XP004414809, DOI: doi:10.1016/S0168-3659(03)00012-9
ADRIAENS, E.; BYTHEWAY, H; DE WEVER, B.; ESCHRICH, D.; GUEST, R.; HANSEN, E.; VANPARYS, P; SCHOETERS, G.; WARREN, N.; WELTENS, R.: "Successful prevalidation of the slug mucosal irritation test to assess the eye irritation potency of chemicals Toxicol", VITRO, 2008
ADRIAENS, E.; DHONDT, M.M.M.; REMON, J.P.: "Refinement of the Slug Mucosal Irritation test as an alternative screening test for eye irritation", TOXICOL. IN VITRO, vol. 19, no. 1, 2005, pages 79 - 89, XP027831745
ADRIAENS, E.; DIERCKENS, K.; BAUTERS, T.G.M.; NELIS, H.J.; VAN GOETHEM, F.; VANPARYS, P.; REMON, J.P.: "The mucosal toxicity of different benzalkonium chloride analogues with an alternative test using slugs", PHARM. RES., vol. 18, 2001, pages 937 - 942
ADRIAENS, E.; REMON, J.P.: "Gastropods as an evaluation tool for screening the irritating potency of absorption enhancers and drugs", PHARM. RES., vol. 16, 1999, pages 1240 - 1244
ANDERSCH B.; LINDELL D.; BRANDBERG A.: "Bacterial Vaginosis and the effect of intermittent prophylactic treatment with an acid lactate gel", GYNACOL OBSTET INVEST, vol. 30, 1990, pages 114 - 119
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BHATT H.R.; GURNASINGHANI M.L.; DATTANI K.K.; LALLA J.K.: "Controlled release nitroglycerin capsules", J. OF CONTROLLED RELEASE, vol. 9, no. 1, 1989, pages 43 - 55, XP025484347, DOI: doi:10.1016/0168-3659(89)90032-1
BOSKEY E.R.; CONE R.A.; WHALEY K.J.; MOENCH T.R.: "Origins of vaginal acidity: high D/L lactate ratio is consistent with bacteria being the primary source", HUMAN REPRODUCTION, vol. 16, no. 9, 2001, pages 1809 - 1813, XP055072120, DOI: doi:10.1093/humrep/16.9.1809
CALLENS, C.; ADRIAENS, E.; DIERCKENS, K.; REMON, J.P.: "Toxicological evaluation of a bioadhesive nasal powder containing a starch and carbopol 974 p on rabbit nasal mucosa and slug mucosa", J. CONTROL. REL., vol. 76, 2001, pages 81 - 91, XP004302040, DOI: doi:10.1016/S0168-3659(01)00419-9
CEULEMANS J.; VERMEIRE A.; ADRIAENS E.; REMON J.P.; LUDWIG A.: "Evaluation of a mucoadhesive tablet for ocular use", J. CONTROL. RELEASE, vol. 77, 2001, pages 333 - 344, XP004328585, DOI: doi:10.1016/S0168-3659(01)00522-3
DHONDT, M.M.M.; ADRIAENS, E.; PINCEEL, J.; JORDEANS, K.; BACKELJAU, T.; REMON J.P.: "Slug species and populations specific effects on the end points of the Slug Mucosal Irritation test", TOXICOLOGY IN VITRO, September 2005 (2005-09-01)
DHONDT, M.M.M.; ADRIAENS, E.; REMON, J.P.: "The Evaluation of the local tolerance of vaginal formulations, with or without Nonoxynol-9, using the Slug Mucosal Irritation test", SEX. TRANS. DIS, vol. 31, no. 4, 2004, pages 229 - 235
DHONDT, M.M.M.; ADRIAENS, E.; VAN ROEY, J.; REMON, J.P: "Evaluation of the local tolerance of vaginal formulations containing TMC 120 using rabbits and slugs", EUR. J. PHARM. BIOPHARM., vol. 60, 2005, pages 419 - 425
DRAIZE, J.H.; WOODWARD, G.; CALVERY, H.O.: "Methods for the study of irritation and toxicity of substances applied to the skin and mucous membranes", J. PHARMACOL. EXP. THER., vol. 82, 1944, pages 377
HARVEY, M. D.; BABLEKIS, V.; BANKS, P. R.; SKINNER, C. D.: "Utilization of the non-covalent fluorescent dye, NanoOrange, as a potential clinical diagnostic tool - Nanomolar human serum albumin quantitation", J. CHROMATOGR. B, vol. 754, 2001, pages 345 - 356, XP004232819, DOI: doi:10.1016/S0378-4347(00)00627-7
WEYENBERG, W.; VERMEIRE, A.; DHONDT, M.M.M; ADRIAENS, E.; KESTELYN, P.; REMON, J.P.; LUDWIG, A.: "Ocular bioerodible minitablets as strategy for the managementof microbial keratitis", INVESTIGATIVE OPHTHALMOLOGY & VISUAL SCIENCE, vol. 45, no. 9, 2004, pages 3229 - 3233

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2790637A4 (en) * 2011-12-16 2015-04-29 Combinent Biomedical Systems Inc VAGINAL DRUG DELIVERY DEVICES AND METHODS OF MANUFACTURING THE SAME

Also Published As

Publication number Publication date
CN103648482A (zh) 2014-03-19
EP2731587B1 (en) 2024-12-04
EP2731587A1 (en) 2014-05-21
JP6010120B2 (ja) 2016-10-19
CN103648482B (zh) 2018-01-02
US20140154293A1 (en) 2014-06-05
JP2014520871A (ja) 2014-08-25
US9168303B2 (en) 2015-10-27

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