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1. (WO2010075665) A FORMULATION OF SILIBININ WITH HIGH EFFICIENCY AND PROLONGED ACTION AND THE PREPARATION METHOD THEREOF
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2010/075665 International Application No.: PCT/CN2009/001300
Publication Date: 08.07.2010 International Filing Date: 23.11.2009
IPC:
A61K 31/357 (2006.01) ,A61K 9/22 (2006.01) ,A61K 9/52 (2006.01) ,A61K 47/02 (2006.01) ,A61K 47/30 (2006.01) ,A61P 1/16 (2006.01) ,A61P 31/12 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
335
having oxygen as the only ring hetero atom, e.g. fungichromin
357
having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9
Medicinal preparations characterised by special physical form
20
Pills, lozenges or tablets
22
Sustained or differential release type
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9
Medicinal preparations characterised by special physical form
48
Preparations in capsules, e.g. of gelatin, of chocolate
52
Sustained or differential release type
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
02
Inorganic compounds
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
30
Macromolecular compounds
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1
Drugs for disorders of the alimentary tract or the digestive system
16
for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31
Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12
Antivirals
Applicants:
江苏大学 JIANGSU UNIVERSITY [CN/CN]; 中国江苏省镇江市丹徒路301号 No. 301 Dantu Road Zhenjiang Jiangsu 212013, CN (AllExceptUS)
徐希明 XU, Ximing [CN/CN]; CN (UsOnly)
余江南 YU, Jiangnan [CN/CN]; CN (UsOnly)
曹霞 CAO, Xia [CN/CN]; CN (UsOnly)
朱源 ZHU, Yuan [CN/CN]; CN (UsOnly)
Inventors:
徐希明 XU, Ximing; CN
余江南 YU, Jiangnan; CN
曹霞 CAO, Xia; CN
朱源 ZHU, Yuan; CN
Agent:
南京知识律师事务所 ZHISHI LAW FIRM OF INTELLECTUAL PROPERTY; 中国江苏省南京市新模范马路5号南京科技广场B座9楼 9F, Block B, Nanjing Sci-Tech Center 5# Xinmofan Road, Nanjing Jiangsu 210009, CN
Priority Data:
200810242993.831.12.2008CN
Title (EN) A FORMULATION OF SILIBININ WITH HIGH EFFICIENCY AND PROLONGED ACTION AND THE PREPARATION METHOD THEREOF
(FR) FORMULE DE SILIBININE D'EFFICACITÉ ÉLEVÉE ET D'ACTION PROLONGÉE ET SA MÉTHODE D'ÉLABORATION
(ZH) 一种水飞蓟宾高效长效制剂及其制法
Abstract:
(EN) A formulation of silibinin with high efficiency and prolonged action and the preparation method thereof are disclosed. Said formulation consists of a solid dispersion of silibinin, silicon dioxide nanoparticles of silibinin, sustained-release matrix materials and release accelerator, wherein the mass ratio of the solid dispersion, nanoparticles, matrix materials and accelerator is 1: 0.5~1.25: 0.1~0.3: 0.1~03. The drug loading rate of the nanopartiles of silibinnin is 51.29-51.77%. The solid dispersion comprises silibinin, polyvidone K30, soybean phospholipid, acrylic resin IV in the mass ratio of 1: 1~3: 0.3~0.8: 0.2~0.5.
(FR) La présente invention concerne une formule de silibinine d'efficacité élevée et d'action prolongée ainsi que sa méthode d'élaboration. Ladite formule est constituée d'une dispersion solide de silibinine, de nanoparticules de dioxyde de silicium comportant de la silibinine, de matériaux de matrice de libération prolongée et d'un accélérateur de libération, le rapport massique de la dispersion solide, des nanoparticules, des matériaux de matrices et de l'accélérateur étant de 1 : 0,5~1,25 : 0,1~0,3 : 0,1~0.3. La proportion de charge en médicaments des nanoparticules de silibinine est comprise entre 51,29 et 51,77 %. La dispersion solide comprend de la silibinine, de la polyvidone K30, des phospholipides de soja et une résine acrylique IV dans un rapport massique 1 : 1~3 : 0,3~0,8 : 0,2~0,5.
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: Chinese (ZH)
Filing Language: Chinese (ZH)
Also published as:
US20120029064