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bortezomib-based release system
专利权人:
NANOSILICAL DEVICES S.R.L.
发明人:
ANGELO LIGUORI,ANTONELLA LEGGIO,CATIA MORELLI,LUIGI PASQUA,SEBASTINO ANDO
申请号:
BR112017023250
公开号:
BR112017023250A2
申请日:
2016.04.29
申请国别(地区):
BR
年份:
2018
代理人:
摘要:
class of molecules obtained for the conjugation of species or substrate to bortezomib by stable boronic diester-type bonds in a neutral environment capable of being degraded to a slightly acidic ph (4.5? 5.0) releasing the bortezomib drug and also conjugated to the surface of a micro- or nanosite (a type of substrate) for drug release to become a constituent thereof. they represent a class of bortezomib prodrugs with respect to boronic ester hydrolysis. may be used in the transport and release of bortezomib when diffusion is required in slightly acidic ph environments after passing through neutral ph environments where the drug remains stably conjugated as a non-biologically active boronic ester. Intracellular release of bortezomib may be used, where the latter will allow the drug to be transported biologically active through blood flow while undergoing ph-induced chemical degradation once introduced into the intracellular environment, inducing diffusion of the therapeutically effective form of bortezomib. in the situation, it is used as a constituent of a drug delivery system anchored therein and provided as a release function capable of reaching the intracellular environment at ph 4.5, where the degradation of the prodrug to which the invention relates will occur by diffusion of bortezomib.classe de moléculas obtidas para a conjugação de espécie ou substrato a bortezomibe por ligações do tipo de diéster borônico estáveis em um ambiente neutro, capazes de ser degradadas em um ph levemente ácido (4,5 ? 5,0) liberando o fármaco bortezomibe e também conjugadas na superfície de um micro- ou nanossitema (um tipo de substrato) para a liberação de fármacos tornando-se um constituinte das mesmas. elas representam uma classe de profármacos de bortezomibe com respeito à hidrólise do éster borônico. podem ser usadas no transporte e liberação de bortezomibe quando é necessário difundi-lo em ambientes de ph levemente ácido após passar através de ambientes de ph neutro em que o
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