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WO2019007019A1 - Préparation de nanoparticules polymères de psoralène et procédé de préparation associé - Google Patents

Préparation de nanoparticules polymères de psoralène et procédé de préparation associé Download PDF

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Publication number
WO2019007019A1
WO2019007019A1 PCT/CN2018/072175 CN2018072175W WO2019007019A1 WO 2019007019 A1 WO2019007019 A1 WO 2019007019A1 CN 2018072175 W CN2018072175 W CN 2018072175W WO 2019007019 A1 WO2019007019 A1 WO 2019007019A1
Authority
WO
WIPO (PCT)
Prior art keywords
psoralen
parts
preparation
polymer nanoparticle
polylactide
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/CN2018/072175
Other languages
English (en)
Chinese (zh)
Inventor
蔡宇
李倩文
袁月玲
张荣华
杨丽
王冰月
黄青青
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.)
Jinan University
University of Jinan
Original Assignee
Jinan University
University of Jinan
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 Jinan University, University of Jinan filed Critical Jinan University
Publication of WO2019007019A1 publication Critical patent/WO2019007019A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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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
    • A61K9/48—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
    • A61K9/5107—Excipients; Inactive ingredients
    • A61K9/513—Organic macromolecular compounds; Dendrimers
    • A61K9/5146—Organic macromolecular compounds; Dendrimers obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyamines, polyanhydrides
    • 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
    • A61K31/365—Lactones
    • A61K31/366—Lactones having six-membered rings, e.g. delta-lactones
    • A61K31/37—Coumarins, e.g. psoralen
    • 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
    • A61K9/48—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
    • A61K9/5107—Excipients; Inactive ingredients
    • A61K9/5123—Organic compounds, e.g. fats, sugars
    • 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
    • A61K9/48—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
    • A61K9/5192—Processes

Definitions

  • the present application adopts the following technical solutions.
  • a psoralen polymer nanoparticle preparation is prepared from the following parts by weight: 1-4 parts of psoralen, 10-60 parts of polylactide-glycolide, 30-110 parts of soybean phospholipid, 5 -11 parts of polyethylene glycol 1000 vitamin E succinate.
  • the psoralen polymer nanoparticle preparation is prepared from the following parts by weight: 2-3 parts of psoralen, 40-50 parts of polylactide-glycolide, 70-110 Parts of soybean phospholipid, 5-7 parts of polyethylene glycol 1000 vitamin E succinate.
  • the psoralen polymer nanoparticle preparation is made up of the following parts by weight: 2 parts of psoralen, 50 parts of polylactide-glycolide, 70 parts of soybean phospholipid, 6 Part of polyethylene glycol 1000 vitamin E succinate.
  • the organic solvent is ethanol or acetone.
  • the mass fraction of ethanol in the aqueous ethanol solution is 4%.
  • the organic phase is uniformly injected into the aqueous phase with a syringe.
  • the supernatant liquid was filtered through a 0.45 ⁇ m aqueous filter to obtain a psoralen polymer nanoparticle preparation.
  • the nanoparticle solution is centrifuged at 1000 rpm for 5 min.
  • the beneficial effects of the present application are: the present application uses an appropriate amount of psoralen, polylactide-glycolide, soybean phospholipid and polyethylene glycol 1000 vitamin E succinate as raw materials, especially
  • the psoralen polymer nanoparticle preparation with high encapsulation efficiency can be prepared by using polyethylene glycol 1000 vitamin E succinate as a surfactant and soybean phospholipid as a lipid.
  • the encapsulation efficiency of the psoralen polymer nanoparticle preparation can be further improved, and the encapsulation efficiency can be as high as 84.97%.
  • Emulsion The syringe uniformly injects the organic phase into the aqueous phase to form a mixed solution; after heating the mixture to 60-80 ° C, the mixture is stirred at 10-30 rpm for 30-120 min to form an emulsion.
  • PLGA refers to polylactide-glycolide having a mass ratio of lactic acid to glycolic acid of 1:1.
  • the preparation method of the psoralen polymer nanoparticle preparation provided by the embodiment is basically the same as the preparation method of the embodiment 4, and the difference is:
  • Step (1) was taken as: 3.3 mg of psoralen, 52.5 mg of polylactide-glycolide (same as in Example 4), 32.5 mg of soybean phospholipid, 8.3 mg of synthetic phospholipid (DLPC) and 100 mg, respectively. Tween-80, spare.
  • Step (3) The aqueous phase is prepared by dissolving soybean phospholipid, synthetic phospholipid and Tween-80 in 20 mL of a 4 wt.% aqueous solution of ethanol to form an aqueous phase, which is ready for use.
  • Step (3) The aqueous phase is prepared by dissolving the synthetic phospholipid and dimethylaminoborane in 20 mL of a 4 wt.% aqueous solution of ethanol to form an aqueous phase, which is ready for use.
  • Step (1) was taken as: 3.2 mg of psoralen, 51.2 mg of polylactide-glycolide (same as in Example 4), 6.3 mg of synthetic phospholipid (DLPC), 32.6 mg of soybean phospholipid and 21.8, respectively.
  • Mg (MTC), spare was taken as: 3.2 mg of psoralen, 51.2 mg of polylactide-glycolide (same as in Example 4), 6.3 mg of synthetic phospholipid (DLPC), 32.6 mg of soybean phospholipid and 21.8, respectively. Mg (MTC), spare.
  • the preparation method of the psoralen polymer nanoparticle preparation provided by the embodiment is basically the same as the preparation method of the embodiment 4, and the difference is:
  • Step (1) was taken as: 3.1 mg of psoralen, 49.2 mg of polylactide-glycolide (same as in Example 4), 6.1 mg of synthetic phospholipid (DLPC), and 100 mg of dimethylaminocarb, respectively. Borane (DMAB) and 20 mg (MTC), ready for use.
  • DMAB Borane
  • MTC 20 mg
  • the preparation method of the psoralen polymer nanoparticle preparation provided by the embodiment is basically the same as the preparation method of the embodiment 4, and the difference is:

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Physics & Mathematics (AREA)
  • Optics & Photonics (AREA)
  • Biomedical Technology (AREA)
  • Nanotechnology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne une préparation de nanoparticules polymères de psoralène et un procédé de préparation associé, appartenant au domaine technique des préparations de nanoparticules polymères. La préparation de nanoparticules polymères de psoralène à efficacité d'encapsulation élevée est préparée à l'aide d'une quantité appropriée de psoralène, de polylactide-glycolide, de phospholipide de soja, et de succinate de vitamine E et de poly(éthylèneglycol) 1000 en tant que matières premières, et en particulier à l'aide du succinate de vitamine E et de poly(éthylèneglycol) 1000 en tant que tensioactif et d'un phospholipide de soja en tant que lipide. Par optimisation des conditions de préparation de la préparation de nanoparticules polymères de psoralène, l'efficacité d'encapsulation de la préparation de nanoparticules polymères de psoralène peut être davantage améliorée. L'efficacité d'encapsulation peut atteindre 84,97 %.
PCT/CN2018/072175 2017-07-06 2018-01-11 Préparation de nanoparticules polymères de psoralène et procédé de préparation associé Ceased WO2019007019A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201710547252.X 2017-07-06
CN201710547252.XA CN107157953A (zh) 2017-07-06 2017-07-06 一种补骨脂素聚合物纳米粒制剂以及制备方法

Publications (1)

Publication Number Publication Date
WO2019007019A1 true WO2019007019A1 (fr) 2019-01-10

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CN (1) CN107157953A (fr)
WO (1) WO2019007019A1 (fr)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107157953A (zh) * 2017-07-06 2017-09-15 暨南大学 一种补骨脂素聚合物纳米粒制剂以及制备方法
CN108379242A (zh) * 2018-05-06 2018-08-10 广州加原医药科技有限公司 一种大蒜素螺旋藻多糖聚合物脂质纳米粒制剂以及制备方法
CN111000828A (zh) * 2019-12-06 2020-04-14 暨南大学 一种大黄素脂质聚合物纳米粒及其制备方法和应用
CN110960510A (zh) * 2019-12-30 2020-04-07 暨南大学 一种MnO2/FA/PSO纳米制剂及其制备方法和应用
CN111973813A (zh) * 2020-09-07 2020-11-24 乐普（北京）医疗器械股份有限公司 一种用于多孔球囊血管成形术的雷帕霉素纳米粒
CN113476475B (zh) * 2021-06-25 2022-11-15 江汉大学 一种水杨酸锌纳米粒及其制备方法和应用
CN116327707B (zh) * 2023-03-21 2025-09-16 暨南大学 补骨脂素甘露糖化壳聚糖聚合物纳米颗粒及其制备方法与应用

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104224752A (zh) * 2014-09-18 2014-12-24 暨南大学 一种补骨脂素-槲皮素复合固体脂质纳米粒制剂及其制备
CN107157953A (zh) * 2017-07-06 2017-09-15 暨南大学 一种补骨脂素聚合物纳米粒制剂以及制备方法
CN107320458A (zh) * 2017-07-06 2017-11-07 暨南大学 一种包封率高的补骨脂素聚合物纳米粒制剂及其制备方法

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1470289A (zh) * 2002-07-26 2004-01-28 北京华京五方实用纳米科技开发有限公 一种高分子纳米药物载体和制剂的制备方法
US20070128289A1 (en) * 2005-12-07 2007-06-07 Zhao Jonathon Z Nano-and/or micro-particulate formulations for local injection-based treatment of vascular diseases
US9161943B2 (en) * 2007-12-31 2015-10-20 Industrial Technology Research Institute Sustained release composition and manufacturing method thereof
CN103751787A (zh) * 2013-12-18 2014-04-30 清华大学深圳研究生院 维生素e tpgs在制备多孔药物载体微粒中的用途
CN104013600A (zh) * 2014-06-05 2014-09-03 暨南大学 一种包载补骨脂素的纳米结构脂质载体制剂及其制备方法

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104224752A (zh) * 2014-09-18 2014-12-24 暨南大学 一种补骨脂素-槲皮素复合固体脂质纳米粒制剂及其制备
CN107157953A (zh) * 2017-07-06 2017-09-15 暨南大学 一种补骨脂素聚合物纳米粒制剂以及制备方法
CN107320458A (zh) * 2017-07-06 2017-11-07 暨南大学 一种包封率高的补骨脂素聚合物纳米粒制剂及其制备方法

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
FANG, LIANG: "Vitamin E-TPGS", PLOYMER SCIENCE IN PHARMACEUTICS, 31 August 2015 (2015-08-31), pages 172, 173 *
WANG, LAIYOU ET AL.: "Preparations of Psoralen-Loaded PLGA Nanoparticles and Its Characteristics of Penetration Across Human Skin", CHINESE PHARMACEUTICAL JOURNAL, vol. 34, no. 17, 30 September 2008 (2008-09-30), pages 1317 - 1321, ISSN: 1001-2494 *

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