WO2018126049A1 - Préparations dépôt - Google Patents

Préparations dépôt Download PDF

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Publication number
WO2018126049A1
WO2018126049A1 PCT/US2017/068777 US2017068777W WO2018126049A1 WO 2018126049 A1 WO2018126049 A1 WO 2018126049A1 US 2017068777 W US2017068777 W US 2017068777W WO 2018126049 A1 WO2018126049 A1 WO 2018126049A1
Authority
WO
WIPO (PCT)
Prior art keywords
composition
sirolimus
vitamin
weight
saib
Prior art date
Application number
PCT/US2017/068777
Other languages
English (en)
Inventor
Wilma Tamraz
Huey-Ching Lin Su
Weiqi Lin
Kazuhito Yamada
Naoki Matsumoto
Sreenivasu Mudumba
Komei OKABE
Original Assignee
Durect Corporation
Santen Pharmaceutical Co., Ltd.
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
Priority claimed from CA2972296A external-priority patent/CA2972296A1/fr
Application filed by Durect Corporation, Santen Pharmaceutical Co., Ltd. filed Critical Durect Corporation
Priority to KR1020197021402A priority Critical patent/KR20190102219A/ko
Priority to EA201991594A priority patent/EA201991594A1/ru
Priority to CN201780080564.2A priority patent/CN110214029A/zh
Priority to EP17888222.1A priority patent/EP3565600A4/fr
Priority to JP2019535239A priority patent/JP2020506887A/ja
Priority to TW107122346A priority patent/TW201919620A/zh
Publication of WO2018126049A1 publication Critical patent/WO2018126049A1/fr
Priority to PCT/US2018/067724 priority patent/WO2019133735A1/fr

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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
    • A61K9/08—Solutions
    • 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
    • A61K9/0048—Eye, e.g. artificial tears
    • 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
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • 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
    • A61K31/355—Tocopherols, e.g. vitamin E
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
    • 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
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
    • 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
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • A61K31/585—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin containing lactone rings, e.g. oxandrolone, bufalin
    • 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
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • 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
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • A61K9/0048—Eye, e.g. artificial tears
    • A61K9/0051—Ocular inserts, ocular implants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7032—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a polyol, i.e. compounds having two or more free or esterified hydroxy groups, including the hydroxy group involved in the glycosidic linkage, e.g. monoglucosyldiacylglycerides, lactobionic acid, gangliosides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C31/00—Saturated compounds having hydroxy or O-metal groups bound to acyclic carbon atoms
    • C07C31/02—Monohydroxylic acyclic alcohols
    • C07C31/08—Ethanol
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G65/00—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
    • C08G65/02—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring
    • C08G65/26—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring from cyclic ethers and other compounds
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G65/00—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
    • C08G65/34—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from hydroxy compounds or their metallic derivatives
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12P—FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P19/00—Preparation of compounds containing saccharide radicals
    • C12P19/12—Disaccharides

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Ophthalmology & Optometry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

L'invention concerne des compositions pharmaceutiques comprenant un ingrédient pharmaceutique actif, un véhicule liquide à viscosité élevée, un solvant hydrophobe et un solvant hydrophile. L'invention concerne également des procédés de production et d'utilisation desdites compositions. Ces compositions sont appropriées pour être utilisées, par exemple, comme préparations dépôt.
PCT/US2017/068777 2016-06-30 2017-12-28 Préparations dépôt WO2018126049A1 (fr)

Priority Applications (7)

Application Number Priority Date Filing Date Title
KR1020197021402A KR20190102219A (ko) 2016-12-30 2017-12-28 데포 제형
EA201991594A EA201991594A1 (ru) 2016-12-30 2017-12-28 Депо-препарат
CN201780080564.2A CN110214029A (zh) 2016-12-30 2017-12-28 长效配制物
EP17888222.1A EP3565600A4 (fr) 2016-12-30 2017-12-28 Préparations dépôt
JP2019535239A JP2020506887A (ja) 2016-12-30 2017-12-28 デポー製剤
TW107122346A TW201919620A (zh) 2016-12-30 2018-06-28 貯庫型調合物
PCT/US2018/067724 WO2019133735A1 (fr) 2016-06-30 2018-12-27 Formulations à effet retard

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
US201662440658P 2016-12-30 2016-12-30
US62/440,658 2016-12-30
CA2972296A CA2972296A1 (fr) 2016-06-30 2017-06-29 Formulations de depot
US15/637,401 US10668011B2 (en) 2016-06-30 2017-06-29 Depot formulations
PCT/US2017/039968 WO2018005777A1 (fr) 2016-06-30 2017-06-29 Formulations de dépôt
CA2,972,296 2017-06-29
USPCT/US2017/039968 2017-06-29
US15/637,401 2017-06-29

Publications (1)

Publication Number Publication Date
WO2018126049A1 true WO2018126049A1 (fr) 2018-07-05

Family

ID=62709991

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2017/068777 WO2018126049A1 (fr) 2016-06-30 2017-12-28 Préparations dépôt

Country Status (7)

Country Link
EP (1) EP3565600A4 (fr)
JP (1) JP2020506887A (fr)
KR (1) KR20190102219A (fr)
CN (1) CN110214029A (fr)
EA (2) EA201990127A1 (fr)
TW (1) TW201919620A (fr)
WO (1) WO2018126049A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021176263A1 (fr) * 2020-03-02 2021-09-10 Shanghai Aucta Pharmaceuticals Co., Ltd. Formulations topiques contenant des inhibiteurs de mtor

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US5023262A (en) 1990-08-14 1991-06-11 American Home Products Corporation Hydrogenated rapamycin derivatives
EP0467606A1 (fr) 1990-07-16 1992-01-22 American Home Products Corporation Dérivés de rapamycine
WO1992005179A1 (fr) 1990-09-19 1992-04-02 American Home Products Corporation Esters d'acide carboxylique de rapamycine
US5120842A (en) 1991-04-01 1992-06-09 American Home Products Corporation Silyl ethers of rapamycin
US5120725A (en) 1991-05-29 1992-06-09 American Home Products Corporation Bicyclic rapamycins
US5120727A (en) 1991-05-29 1992-06-09 American Home Products Corporation Rapamycin dimers
US5177203A (en) 1992-03-05 1993-01-05 American Home Products Corporation Rapamycin 42-sulfonates and 42-(N-carboalkoxy) sulfamates useful as immunosuppressive agents
US5242910A (en) 1992-10-13 1993-09-07 The Procter & Gamble Company Sustained release compositions for treating periodontal disease
US5310865A (en) 1991-12-18 1994-05-10 Mitsui Toatsu Chemicals, Incorporated Polyhydroxycarboxylic acid and preparation process thereof
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US20090074786A1 (en) 2005-02-09 2009-03-19 Macusight, Inc. Formulations for treating ocular diseases and conditions
US20120330005A1 (en) 2005-07-26 2012-12-27 Durect Corporation Peroxide removal from drug delivery vehicle
US8367097B2 (en) 2005-02-09 2013-02-05 Santen Pharmaceutical Co., Ltd. Liquid formulations for treatment of diseases or conditions
WO2016148228A1 (fr) * 2015-03-18 2016-09-22 参天製薬株式会社 Composition pharmaceutique à libération prolongée
WO2018005777A1 (fr) * 2016-06-30 2018-01-04 Durect Corporation Formulations de dépôt

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US8586103B2 (en) * 2008-02-08 2013-11-19 Foresee Pharmaceuticals, Llc Non-polymeric compositions for controlled drug delivery
KR20140015266A (ko) * 2010-11-24 2014-02-06 듀렉트 코퍼레이션 생분해성 약물 전달 조성물

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WO1992005179A1 (fr) 1990-09-19 1992-04-02 American Home Products Corporation Esters d'acide carboxylique de rapamycine
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US5242910A (en) 1992-10-13 1993-09-07 The Procter & Gamble Company Sustained release compositions for treating periodontal disease
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US20040101557A1 (en) * 1995-06-07 2004-05-27 Gibson John W. High viscosity liquid controlled delivery system and medical or surgical device
US5747058A (en) 1995-06-07 1998-05-05 Southern Biosystems, Inc. High viscosity liquid controlled delivery system
US6329386B1 (en) 1997-09-26 2001-12-11 Abbott Laboratories Tetrazole-containing rapamycin analogs with shortened half-lives
US6376517B1 (en) 1998-08-14 2002-04-23 Gpi Nil Holdings, Inc. Pipecolic acid derivatives for vision and memory disorders
US6890546B2 (en) 1998-09-24 2005-05-10 Abbott Laboratories Medical devices containing rapamycin analogs
US20090074786A1 (en) 2005-02-09 2009-03-19 Macusight, Inc. Formulations for treating ocular diseases and conditions
US8367097B2 (en) 2005-02-09 2013-02-05 Santen Pharmaceutical Co., Ltd. Liquid formulations for treatment of diseases or conditions
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US20120330005A1 (en) 2005-07-26 2012-12-27 Durect Corporation Peroxide removal from drug delivery vehicle
WO2016148228A1 (fr) * 2015-03-18 2016-09-22 参天製薬株式会社 Composition pharmaceutique à libération prolongée
WO2018005777A1 (fr) * 2016-06-30 2018-01-04 Durect Corporation Formulations de dépôt

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CAUFIELD ET AL., HYDROGENATED RAPAMYCIN DERIVATIVES
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KAO ET AL., BICYCLIC RAPAMYCINS
KAO ET AL., RAPAMYCIN DIMERS
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PAIVA ET AL.: "Incorporation Of Acetate, Propionate, And Methionine Into Rapamycin By Streptomycetes hygroscopicus", J NAT PROD, vol. 54, 1991, pages 167 - 177
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US11813250B2 (en) 2020-03-02 2023-11-14 Shanghai Aucta Pharmaceuticals Co., Ltd. Topical formulations containing mTOR inhibitors

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