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1. (WO2009134092) POORLY SOLUBLE DRUG-CONTAINING RELEASE-CONTROLLED POLYMERIC NANOPARTICLE FORMULATION
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2009/134092    International Application No.:    PCT/KR2009/002291
Publication Date: 05.11.2009 International Filing Date: 30.04.2009
IPC:
A61K 9/51 (2006.01), A61K 9/127 (2006.01), A61K 9/00 (2006.01), A61K 47/00 (2006.01)
Applicants: KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY [KR/KR]; 111 Gwanhangno, Yuseong-gu Daejeon 305-806 (KR) (For All Designated States Except US).
CHUNG, Bong Hyun [KR/KR]; (KR) (For US Only).
LIM, Yong Taik [KR/KR]; (KR) (For US Only).
HAN, Jung Hyun [KR/KR]; (KR) (For US Only)
Inventors: CHUNG, Bong Hyun; (KR).
LIM, Yong Taik; (KR).
HAN, Jung Hyun; (KR)
Agent: LEE, Won-Hee; (KR)
Priority Data:
10-2008-0041018 01.05.2008 KR
Title (EN) POORLY SOLUBLE DRUG-CONTAINING RELEASE-CONTROLLED POLYMERIC NANOPARTICLE FORMULATION
(FR) PRÉPARATION À BASE DE NANOPARTICULES POLYMÈRES À LIBÉRATION CONTRÔLÉE CONTENANT UN MÉDICAMENT À FAIBLE SOLUBILITÉ
(KO) 난용성 약물 함유 서방성 고분자 나노입자 제형
Abstract: front page image
(EN)The present invention relates to a release-controlled polymeric nanoparticle formulation containing biphenyl-dimethyl-dicarboxylate, a poorly soluble drug, and more particularly, to a nano-sized polymer formulation having a particle size distribution of narrow range, in which the biphenyl-dimethyl-dicarboxylate, a poorly soluble drug, is impregnated in biodegradable polymer and the surface of the formulation is coated with an emulsifier. The polymeric nanoparticle formulation according to the present invention can be effectively used in the treatment of hepatic disease since the formulation enhances the dissolution rate of biphenyl-dimethyl-dicarboxylate which is a poorly soluble drug to increase bioavailability, and releases drugs gradually to keep the drugs at a constant density in blood over a long period of time. The polymeric nanoparticle formulation of the present invention may prevent an excessive use of biphenyl-dimethyl-dicarboxylate caused due to the low dissolution rate in a body and low bioavailability of conventional formulations containing biphenyl-dimethyl-dicarboxylate.
(FR)La présente invention concerne une préparation à base de nanoparticules polymères à libération contrôlée qui contient du biphényl-diméthyl-dicarboxylate, un médicament à faible solubilité, et plus particulièrement, une préparation à base de nanoparticules polymères présentant une répartition granulométrique dans une plage limitée, dans laquelle le biphényl-diméthyl-dicarboxylate, un médicament à faible solubilité, est introduit dans un polymère biodégradable et la surface de la préparation est enrobée par un émulsifiant. La préparation à base de nanoparticules polymères de la présente invention peut être utilisée de manière efficace dans le traitement des maladies hépatiques étant donné qu'elle augmente la vitesse de dissolution du biphényl-diméthyl-dicarboxylate qui est un médicament à faible solubilité afin d'améliorer la biodisponibilité, et libère les médicaments progressivement pour maintenir ces derniers à une densité constante dans le sang sur une durée prolongée. Ladite préparation à base de nanoparticules polymères peut assurer une prévention contre une utilisation excessive de biphényl-diméthyl-dicarboxylate due à la faible vitesse de dissolution dans le corps et à la faible biodisponibilité de préparations classiques contenant du biphényl-diméthyl-dicarboxylate.
(KO)본 발명은 난용성 약물인 비페닐디메틸디카르복실레이트(Biphenyl-Dimethyl-Dicarboxylate; BDD) 함유 서방성 고분자 나노입자 제형에 관한 것으로, 더욱 구체적으로는 난용성 약물인 BDD가 생분해성 고분자에 함침되어 있고 표면에 유화제가 코팅되어 있는 좁은 범위의 입도분포를 갖는 나노 크기의 고분자 제형에 관한 것이다. 본 발명에 따른 상기 고분자 나노입자 제형은 난용성 약물인 BDD의 용출률을 개선시켜 생체이용률을 증가시키고, 약물을 서서히 방출하여 혈액 내에서 약물이 일정한 농도로 장기간 유지됨으로써 간 질환 치료에 효과적으로 사용될 수 있으며, 종래 BDD 함유 제형의 체내 용출량 및 생체이용률의 저하로 인한 과량의 BDD 사용량을 줄일 수 있다.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, 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, 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, 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 (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, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG).
Publication Language: Korean (KO)
Filing Language: Korean (KO)