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1. WO2020228206 - METHOD FOR PREPARING CISPLATIN NANO-DRUG FOR TREATMENT OF OVARIAN CANCER

Publication Number WO/2020/228206
Publication Date 19.11.2020
International Application No. PCT/CN2019/105921
International Filing Date 16.09.2019
IPC
A61K 47/69 2017.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
69the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
A61K 33/243 2019.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
33Medicinal preparations containing inorganic active ingredients
24Heavy metals; Compounds thereof
243Platinum; Compounds thereof
A61K 47/54 2017.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
54the modifying agent being an organic compound
A61K 47/64 2017.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
62the modifying agent being a protein, peptide or polyamino acid
64Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
CPC
A61K 33/243
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
33Medicinal preparations containing inorganic active ingredients
24Heavy metals; Compounds thereof
243Platinum; Compounds thereof
A61K 47/545
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
54the modifying agent being an organic compound
545Heterocyclic compounds
A61K 47/64
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
62the modifying agent being a protein, peptide or polyamino acid
64Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
A61K 47/6931
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
69the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
6921the form being a particulate, a powder, an adsorbate, a bead or a sphere
6927the form being a solid microparticle having no hollow or gas-filled cores
6929the form being a nanoparticle, e.g. an immuno-nanoparticle
6931the material constituting the nanoparticle being a polymer
A61K 47/6939
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
69the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
6921the form being a particulate, a powder, an adsorbate, a bead or a sphere
6927the form being a solid microparticle having no hollow or gas-filled cores
6929the form being a nanoparticle, e.g. an immuno-nanoparticle
6931the material constituting the nanoparticle being a polymer
6939the polymer being a polysaccharide, e.g. starch, chitosan, chitin, cellulose or pectin
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
Applicants
  • 南方医科大学 SOUTHERN MEDICAL UNIVERSITY [CN]/[CN]
Inventors
  • 王莺 WANG, Ying
  • 王沂峰 WANG, Yifeng
  • 罗家懋 LUO, Jiamao
Agents
  • 广州市天河庐阳专利事务所(普通合伙) GUANGZHOU TIANHE LUYANG PATENT OFFICE (GENERAL PARTNERSHIP)
Priority Data
201910400677.715.05.2019CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) METHOD FOR PREPARING CISPLATIN NANO-DRUG FOR TREATMENT OF OVARIAN CANCER
(FR) PROCÉDÉ DE PRÉPARATION D'UN NANOMÉDICAMENT DE CISPLATINE POUR LE TRAITEMENT DU CANCER DE L'OVAIRE
(ZH) 一种治疗卵巢癌的顺铂纳米药物的制备方法
Abstract
(EN)
A method for preparing a cisplatin nano-drug for the treatment of ovarian cancer. The method comprises the steps of: first coupling carboxylated heparin with folic acid and a tumor-targeting cyclopeptide (cRGD) to prepare a carboxylated heparin-folic acid-cyclopeptide, then adding cisplatin and mixing for reaction so as to chelate the cisplatin with the carboxylated heparin-folic acid-cyclopeptide, adding protamine after 24 hours of dialysis so as to connect together, by electric charge attraction, the positively charged protamine to the negatively charged carboxylated heparin-folic acid-cyclopeptide-cisplatin, and compress the cisplatin inside a carrier, and finally preparing a cisplatin nano-drug. The cisplatin nano-drug prepared by the method has significant effects of inhibiting cancer proliferation and metastasis, and has low toxicity and side effects.
(FR)
L'invention concerne un procédé de préparation d'un nanomédicament de cisplatine pour le traitement du cancer de l'ovaire. Le procédé comprend les étapes consistant à : coupler d'abord de l'héparine carboxylée avec de l'acide folique et un cyclopeptide ciblant une tumeur (cRGD) pour préparer un cyclopeptide d'acide folique-héparine carboxylée, puis ajouter du cisplatine et le mélanger pour la réaction de manière à chélater le cisplatine avec le cyclopeptide d'acide folique-héparine carboxylée, ajouter de la protamine après 24 heures de dialyse de manière à connecter ensemble, par attraction de charges électriques, la protamine positivement chargée au cyclopeptide d'acide folique-héparine carboxylée-cisplatine chargé négativement, et à comprimer le cisplatine à l'intérieur d'un support, et enfin préparer un nanomédicament de cisplatine. Le nanomédicament de cisplatine préparé par le procédé présente des effets significatifs d'inhibition de la prolifération du cancer et des métastases, et présente une toxicité et des effets secondaires faibles.
(ZH)
一种治疗卵巢癌的顺铂纳米药物的制备方法,该方法的步骤如下:先将羧基化肝素与叶酸和肿瘤靶向环肽(cRGD)偶联,制备竣羧基化肝素-叶酸-环肽,然后加入顺铂混合反应,使顺铂与羧基化肝素-叶酸-环肤进行鳌合,透析24h后加入鱼精蛋白,带正电荷的鱼精蛋白与负电荷的羧基化肝素-叶酸-环肤-顺铂通过电荷吸引连接在一起,顺铂被压缩在载体内部,最终制得顺铂纳米药物。该方法制备的顺铂纳米药物抑制癌增殖和转移的效果显著,且毒副作用低。
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